Propranolol is a non-selective beta blocker that was first synthesized in the 1960s. It is used to treat a variety of conditions, including hypertension, angina, and heart rhythm problems. Propranolol works by blocking the effects of adrenaline and noradrenaline on the heart and blood vessels. It is also used to prevent migraine headaches and to treat tremors. Propranolol is a common subject of research due to its diverse therapeutic applications, its potential for new uses, and the ongoing investigation of its mechanisms of action and side effects.'
Propranolol: A widely used non-cardioselective beta-adrenergic antagonist. Propranolol has been used for MYOCARDIAL INFARCTION; ARRHYTHMIA; ANGINA PECTORIS; HYPERTENSION; HYPERTHYROIDISM; MIGRAINE; PHEOCHROMOCYTOMA; and ANXIETY but adverse effects instigate replacement by newer drugs.
propranolol : A propanolamine that is propan-2-ol substituted by a propan-2-ylamino group at position 1 and a naphthalen-1-yloxy group at position 3.
ID Source | ID |
---|---|
PubMed CID | 4946 |
CHEMBL ID | 27 |
CHEBI ID | 8499 |
SCHEMBL ID | 3955 |
SCHEMBL ID | 12264958 |
MeSH ID | M0017773 |
Synonym |
---|
propanolol |
unii-9y8nxq24vq |
racemic-propranolol |
9y8nxq24vq , |
EN300-40731 |
1-(naphthalen-1-yloxy)-3-[(propan-2-yl)amino]propan-2-ol |
AB00053537-10 |
BRD-A10070317-003-06-9 |
gtpl564 |
2-propanol, 1-[(1-methylethyl)amino]-3-(1-naphthalenyloxy)- |
KBIO1_000023 |
DIVK1C_000023 |
1-[(1-methylethyl)amino]-3-(naphthalen-1-yloxy)propan-2-ol |
ccris 3082 |
sumial |
corpendol |
propanix |
euprovasin |
propranololum [inn-latin] |
sawatal |
proprasylyt |
2-propanol, 1-(isopropylamino)-3-(1-naphthyloxy)- |
einecs 208-378-0 |
betalong |
propanolol [inn-spanish] |
1-isopropylamino-3-(1-naphthyloxy)-2-propanol |
betadren |
propranolol [inn:ban] |
propranololo [dcit] |
reducor |
BIO1_000367 |
CBDIVE_006180 |
BIO1_001345 |
BIO1_000856 |
SPECTRUM5_000751 |
PDSP2_001592 |
PRESTWICK3_000952 |
PRESTWICK2_000952 |
IDI1_000023 |
PDSP1_001608 |
PDSP2_001591 |
BSPBIO_002682 |
BPBIO1_001040 |
LOPAC0_000896 |
PDSP1_000767 |
BSPBIO_000944 |
propranolol, d |
propranolol,(+) |
propranolol,(-) |
chembl27 , |
propanolol,(+/-) |
bdbm25761 |
[2-hydroxy-3-(naphthalen-1-yloxy)propyl](propan-2-yl)amine |
propanolol(-) |
1-(isopropylamino)-3-(1-naphthyloxy)propan-2-ol |
anapriline |
1-(1-naphthyloxy)-2-hydroxy-3-(isopropylamino)propane |
1-(isopropylamino)-3-(1-naphthoxy)-propan-2-ol |
AB00053537 |
propranolol |
525-66-6 |
C07407 |
DB00571 |
CMAP_000071 |
propranololo |
propanalol |
beta-propranolol |
3-(naphthalen-1-yloxy)-1-(propan-2-ylamino)propan-2-ol |
CHEBI:8499 , |
1-((1-methylethyl)amino)-3-(1-naphthalenyloxy)-2-propanol |
propranololum |
NCGC00024690-03 |
2-propanol, 1-((1-methylethyl)amino)-3-(1-naphthalenyloxy)- |
(1)-1-(isopropylamino)-3-(naphthyloxy)propan-2-ol |
(+-)-propranolol |
2-propanol, 1-(isopropylamino)-3-(1-naphthyloxy)-, (+-)- |
d,l-propranolol |
einecs 235-867-6 |
racemic propranolol |
2-propanol, 1-((1-methylethyl)amino)-3-(1-naphthalenyloxy)-, (+-)- |
KBIO3_002993 |
KBIOGR_001347 |
KBIOGR_001684 |
KBIO2_002515 |
KBIO3_001902 |
KBIO2_007651 |
KBIO3_001766 |
KBIO2_005083 |
KBIOSS_002523 |
KBIOGR_002515 |
SPBIO_001658 |
SPBIO_001361 |
SPECTRUM4_000974 |
SPECTRUM2_001301 |
PRESTWICK0_000952 |
NINDS_000023 |
SPBIO_003093 |
PRESTWICK1_000952 |
SPECTRUM2_001699 |
SPECTRUM3_000883 |
SPECTRUM4_001222 |
SPECTRUM3_001071 |
OPREA1_304193 |
PDSP1_001607 |
PDSP2_000755 |
NCGC00024690-02 |
HMS2090L21 |
NCGC00015798-07 |
L000679 |
.beta.-propranolol |
ay-64043- |
dl-propranolol |
AKOS000588816 |
propranolol (tn) |
propranolol (inn) |
D08443 |
FT-0650563 |
1-isopropylamino-3-(naphthalen-1-yloxy)-propan-2-ol |
1-naphthalen-1-yloxy-3-(propan-2-ylamino)propan-2-ol |
STK735510 |
1-(naphthalen-1-yloxy)-3-(propan-2-ylamino)propan-2-ol |
1-(isopropylamino)-3-naphthalen-1-yloxy-propan-2-ol |
CCG-103643 |
NCGC00015798-04 |
NCGC00015798-09 |
NCGC00015798-05 |
NCGC00015798-08 |
NCGC00015798-06 |
3-[(methylethyl)amino]-1-naphthyloxypropan-2-ol |
propranalol |
FT-0674088 |
BBL023437 |
propranolol [mi] |
propranolol [vandf] |
(+/-)-propranolol |
propranolol [who-dd] |
13013-17-7 |
propranolol [inn] |
AKOS016050338 |
SCHEMBL3955 |
FE-0204 |
1(-alpha-naphthoxy)-3-(iso-propylamino)-2-propanol |
1-(alpha-naphthoxy)-3-(iso-propylamino)-2-propanol |
1-((1-methylethyl)amino)-3-(1-naphthyloxy)-2-propanol |
1-(alpha-naphthoxy)-3-(isopropylamino)-2-propanol |
ici 45520 (salt/mix) |
dociton (salt/mix) |
obsidan (salt/mix) |
avlocardyl (salt/mix) |
nsc 91523 (salt/mix) |
(.+/-.)-propranolol |
inderal (salt/mix) |
SCHEMBL12264958 |
W-109550 |
HMS3428G03 |
(a+/-)-propranolol hydrochloride |
AB00053537_11 |
AB00053537_12 |
DTXSID6023525 , |
1-(isopropylamino)-3-(naphthalen-1-yloxy)propan-2-ol |
b-propranolol |
SBI-0050871.P003 |
Q423364 |
1h-pyrrole-2-carboxylic acid, 4-acetyl-5-methyl-3-(trifluoromethyl)-, ethyl ester |
F0001-3681 |
BRD-A10070317-003-17-6 |
BCP26001 |
SDCCGSBI-0050871.P004 |
beta-propranolol;dociton |
BCP31343 |
NCGC00015798-19 |
HY-B0573B |
CS-0069968 |
NCGC00015798-15 |
1-isopropylamino-3-(naphthalen-1-yloxy)propan-2-ol |
dtxcid903525 |
propranololum (inn-latin) |
c07aa05 |
propanolol (inn-spanish) |
Propranolol (PROP) is a nonselective β-adrenergic receptor antagonist used to treat hypertension and cardiac arrhythmias. It has been the first-line therapy for problematic infantile hemangioma (IH), the most frequent childhood vascular tumor.
Oral propranolol has a therapeutic function against ROP, likely through the downregulation of HIF-1α via the PI3K/Akt/ERK pathway. It has a blocking effect on the sodium current ("membrane-stabilizing" effect), and it has been hypothesized that the efficacy of nadolol might be due to a similar effect. Propr ethanol has a small depressant effect on global and segmental left ventricular function in patients with coronary artery disease.
Propranolol has been used in the first-line therapy of infantile hemangioma (IH) for a number of years; however, the mechanisms through which propr ethanol regulates IH are not yet fully understood. Propr ethanol has been suggested as an option for the treatment of various types of cancer.
Propranolol can inhibit the proliferation, migration, invasion, adhesion, and tube formation of hemangioma endothelial cells. It can also block VEGF-mediated angiogenesis signaling pathway. PropranolOL in a lower dose of 1-1.5 mg/kg/day is safe and efficacious in the treatment of infantile hemangIoma.
Propranolol treatment beginning before high-altitude (4,300 m) ascent reduced heart rate during maximal and submaximal exercise in six healthy men treated with propranolols. PropranolOL treatment led to an externalization of beta-receptors from light vesicle to sarcolemmal fractions.
Oral propranolol therapy at a fixed dose of 2 mgkg(-1), given in three equally divided doses, is a very safe and effective regimen in the treatment of IH. Both clonidine and pro Pranolol attenuated the toxic effects of relatively low dose levels of digitoxin. At higher digitoxin dose levels only propr ethanol was able to reduce significantly the ED50 and the LD50.
We have studied the pharmacodynamic effects of ramipril, propranolol, and their combination, as well as the effect of pro Pranolol on the pharmacokinetics of Ramipril in 12 healthy men. In vitro kinetics and in vivo pharmacokinetic profiles after oral administration of timolol, metoprolol and propr ethanol were investigated in rats.
Excerpt | Reference | Relevance |
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"The aims of this study were to describe the pharmacokinetics of propranolol in the cat, to compare pharmacokinetic parameters for propranolol in the cat with those of four other species and to apply the two-step infusion method of Wagner (Clin." | ( Pharmacokinetics of propranolol in the cat and comparisons with humans and three other species. Garg, DC; Jallad, NS; Wagner, JG; Weidler, DJ, 1979) | 0.82 |
"Our preliminary pharmacodynamic studies on the lower urinary tract of adult female dogs indicate that cholinergic and adrenergic (alpha and beta) neuroreceptors in the urethra appear to coordinate the detrusor and urethral function during micturition." | ( Cholinergic and adrenergic neuroreceptors in urinary tract of female dogs. Evaluation of function with pharmacodynamics. Gonick, P; Heber, D; Khanna, OP, 1975) | 0.25 |
" Patients with cirrhosis had a significantly longer quinidine half-life (9 +/- 1 hr; p less than ." | ( Quinidine pharmacokinetics in patients with cirrhosis or receiving propranolol. Black, M; Humphries, WC; Kessler, KM; Spann, JF, 1978) | 0.49 |
"The tendency for patients with essential hypertension to differ markedly in antihypertensive response to propranolol could arise from pathophysiologic or pharmacokinetic differences between them." | ( Pathophysiologic and pharmacokinetic determinants of the antihypertensive response to propranolol. DeQuattro, V; Esler, M; Randall, O; Zweifler, A, 1977) | 0.69 |
" Pharmacokinetic variables have been determined that allow: (1) derivation of the loading dose necessary to achieve rapid control of blood pressure with propranolol hydrochloride, guanethidine, minoxidil and clonidine hydrochloride; (2) reduced frequency of dosing with methyldopa, hydralazine hydrochloride, prazosin hydrochloride, propranolol and clonidine; and (3) alteration of propranolol and hydralazine dosage based on physiologic factors (e." | ( Using pharmacokinetics in drug therapy. V: Contributions to developing dosage regimens for antihypertensive drugs. Schumacher, GE, 1979) | 0.46 |
" Antipyrine elimination half-life (t1/2), volume of distribution (Vd), and total clearance were determined after each trial." | ( Impairment of antipyrine clearance in humans by propranolol. Franke, K; Greenblatt, DJ; Huffman, DH, 1978) | 0.51 |
" Pharmacokinetic data were obtained in hypertensive male patients (4) after treatment with 14C-radioactively labelled acebutolol hydrochloride." | ( [Pharmacokinetics of acebutolol]. Collins, RF, 1975) | 0.25 |
" Consequently, hepatic elimination is unaffected by drug binding in blood, In contrast, the distribution of drug into the tissues is reduced by plasma binding, so that drug half-life (T 1/2), which varies from 11/2-3 hours among individuals is more prolonged in people with relatively low plasma binding." | ( Pharmacokinetics of propranolol: a review. Shand, DG, 1976) | 0.58 |
" The biological half-life was reduced and the central volume of distribution, volume of distribution at pseudo-equilibrium and total clearance (TC) were markedly increased." | ( Comparison of the pharmacokinetics of intravenous dl-propranolol in borderline and permanent hypertension. Alexandre, JM; Chevillard, C; Frydman, A; Lemaire, P; Safar, ME; Simon, A; Weiss, YA, 1976) | 0.51 |
" A significant increase in the fraction of the dose available to the systemic circulation was also found, together with a modification of apparent plasma half-life and volume of distribution in regular dialysis patients during the dialysis day as compared with the after-dialysis day." | ( Pharmacokinetics and effects of propranolol in terminal uraemic patients and in patients undergoing regular dialysis treatment. Bianchetti, G; Brancaccio, D; Gomeni, R; Graziani, G; Leonetti, G; Manfrin, M; Morganti, A; Morselli, PL; Ponticelli, C; Sega, R, 1976) | 0.54 |
"A novel method for detecting and quantitating pharmacokinetic drug-drug interactions is described." | ( New method for detecting and quantitating pharmacokinetic drug-drug interactions applied to ethanol-propranolol. Lin, YJ; Wagner, JG; Weidler, DJ, 1976) | 0.47 |
" The changes in the volumes of distribution of propranolol and verapamil during exercise may contribute to preventing an increase in the half-life of these drugs in patients performing prolonged physical exercise." | ( Exercise and the pharmacokinetics of propranolol, verapamil and atenolol. Mooij, JM; Schiffers, PM; van Baak, MA, 1992) | 0.81 |
"We evaluated the degree of inhibition of angiotensin converting enzyme (ACE), principally by cilazapril, by assessing the blood pressure response to a continuous infusion of increasing doses of angiotensin I, and assessed the possible pharmacokinetic and pharmacodynamic interactions between cilazapril and propranolol in healthy volunteers and patients with mild to severe essential hypertension." | ( Clinical pharmacodynamic studies with cilazapril and a combination of cilazapril and propranolol. Belz, GG; Breithaupt, K; Erb, KA; Essig, J, 1991) | 0.68 |
"The pharmacokinetic and pharmacodynamic profiles of lacidipine, a 1,4-dihydropyridine calcium antagonist, and the beta-adrenoceptor blocker propranolol were determined alone and in combination in 24 healthy male volunteers." | ( The pharmacokinetic and pharmacodynamic interaction between lacidipine and propranolol in healthy volunteers. Hall, ST; Harding, SM; Hassani, H; Keene, ON; Pellegatti, M, 1991) | 0.71 |
" An earlier tmax and a higher Cmax and AUC were observed in the subjects who received piperine and propranolol." | ( Effect of piperine on bioavailability and pharmacokinetics of propranolol and theophylline in healthy volunteers. Bano, G; Bedi, KL; Johri, RK; Raina, RK; Sharma, SC; Zutshi, U, 1991) | 0.74 |
"Stereoselectivity in pharmacokinetics may be characterized by a measurable difference between enantiomers in a pharmacokinetic parameter." | ( Stereoselectivity in pharmacokinetics: a general theory. Boddy, AV; Levy, RH, 1991) | 0.28 |
" Misoprostol had no significant effect on the t/2, Cmax or AUC of propranolol either after a single dose or at steady state." | ( Misoprostol does not alter the pharmacokinetics of propranolol. Bennett, PN; Fenn, GC; Lee, CE; Notarianni, LJ, 1991) | 0.77 |
" Serial blood samples were collected up to 24 h after dose 13 on day 5 to determine possible pharmacokinetic interactions between the two drugs." | ( Pharmacokinetics of diltiazem and propranolol when administered alone and in combination. Dimmitt, DC; Elvin, AT; Giesing, DH; Lanman, RC; Yu, DK, 1991) | 0.56 |
"The disposition of 4'-hydroxypropranolol (HOP) was determined after iv administration to dogs (2 mg/kg; N = 5) and the pharmacokinetic parameters were calculated from plasma measurements." | ( Pharmacokinetics and metabolism of the pharmacologically active 4'-hydroxylated metabolite of propranolol in the dog. Christ, DD; Oatis, JE; Walle, T; Walle, UK, ) | 0.64 |
" Pharmacokinetic parameters were compared with those obtained previously in non-obese control subjects." | ( Comparison of propranolol and sotalol pharmacokinetics in obese subjects. Barré, J; Cheymol, G; Cohen, A; Hugues, FC; Le Jeunne, C; Poirier, JM, 1990) | 0.64 |
" In obese subjects the pharmacokinetic data calculated for sotalol (total clearance (CL), volume of distribution (V beta), half-life of elimination (t1/2), were comparable with those measured in the controls." | ( [Comparison of beta-blocking agents pharmacokinetics in obese and non-obese subjects]. Cheymol, G, 1990) | 0.28 |
" Potential pharmacodynamic and pharmacokinetic interactions between verapamil and propranolol were evaluated in two double-blind, randomised, balanced, crossover studies employing the same six healthy males." | ( Evaluation of potential pharmacodynamic and pharmacokinetic interactions between verapamil and propranolol in normal subjects. Brodie, MJ; McInnes, GT; Murdoch, DL; Murray, GD; Thompson, GG; Thomson, GD, 1991) | 0.73 |
" Pharmacokinetic variable values in elderly subjects did not differ in a clinically significant manner from those in younger subjects." | ( Pharmacokinetics of misoprostol in the elderly, in patients with renal failure and when coadministered with NSAID or antipyrine, propranolol or diazepam. Karim, A; Nicholson, PA; Smith, M, 1990) | 0.48 |
"A comparative pharmacokinetic study of a new controlled release multiple unit propranolol formulation and a conventional propranolol tablet was carried out in twelve healthy human volunteers in a randomized balanced crossover design." | ( Pharmacokinetic evaluation of conventional and controlled release dosage form of propranolol. Chattaraj, SC; Das, SK, 1990) | 0.73 |
" Pharmacodynamic relationships were determined by fitting percent change in ACL and heart rate at maximal exertion with 1-propranolol with the Emax model (maximal effect) and nonlinear regression." | ( Pharmacodynamics of propranolol on left ventricular function: assessment by Doppler echocardiography. Clifton, GD; Harrison, MR; Pennell, AT, 1990) | 0.81 |
"The study aimed at investigating an effect of propranolol on lidocaine pharmacokinetic parameters, especially elimination rate and total clearance rate." | ( [Effect of propranolol on lidocaine pharmacokinetics]. Bijoś, P; Droździk, M; Feszak, J; Gawrońska-Szklarz, G; Goertz, K; Wójcicki, J, ) | 0.78 |
" A possible pharmacodynamic interaction between oxazepam and the beta-adrenoceptor antagonists was examined using a simple reaction time test (SRT) and by measurement of postural sway." | ( Single dose pharmacokinetics and pharmacodynamics of oral oxazepam during concomitant administration of propranolol and labetalol. Døssing, M; Hamberg, O; Loft, S; Olesen, KL; Sonne, J; Thyssen, H; Victor, MA; Vollmer-Larsen, A, 1990) | 0.49 |
" Comparable mean quinapril pharmacokinetic parameter values as well as comparable mean quinaprilat pharmacokinetic parameter values determined following quinapril administered alone and following quinapril administered with propranolol, indicate that propranolol does not alter the single dose pharmacokinetics of quinapril or quinaprilat." | ( Multiple-dose propranolol administration does not influence the single dose pharmacokinetics of quinapril and its active metabolite (quinaprilat). Caillé, G; Colburn, WA; Ferry, JJ; Frank, GJ; Horvath, AM; Lacasse, Y; Olson, SC; Pilon, D, 1990) | 0.82 |
" The half-life for MTP (3." | ( Pharmacokinetics and metabolism of oral doses of a 4'-methylthio derivative of propranolol in man. Conradi, EC; Cowart, TD; Gaffney, TE; Walle, T; Walle, UK, 1990) | 0.51 |
" Co-administration of nicardipine significantly increased the AUC and the mean Cmax of propranolol." | ( Influence of nicardipine on the pharmacokinetics and pharmacodynamics of propranolol in healthy volunteers. Dupont, AG; Massart, DL; Musch, G; Schoors, DF; Vercruysse, I, 1990) | 0.73 |
"The effect of partial gastrectomy on the pharmacokinetic parameters of (+)- and (-)-propranolol were investigated in six dogs." | ( Effects of truncal vagotomy and partial gastrectomy on the pharmacokinetics of propranolol enantiomers in dogs. Derendorf, H; Harrison, D; Hocking, MP; Limberg, J; Schaefer, HG, 1990) | 0.73 |
"Because both quinidine and propranolol bind to the cytochrome P-450 responsible for the oxidation of debrisoquin, six healthy male subjects were studied to determine whether an interaction occurred between the two drugs and the pharmacodynamic consequences of that interaction." | ( Quinidine reduces clearance of (+)-propranolol more than (-)-propranolol through marked reduction in 4-hydroxylation. Anthony, LB; Roden, DM; Wood, AJ; Zhou, HH, 1990) | 0.85 |
" The plasma concentrations of both (+)- and (-)-propranolol were lower in Chinese than in white subjects, resulting in significantly lower peak plasma concentrations and areas under the concentration-time curve (AUC) in Chinese subjects, the half-life of elimination did not differ significantly between Chinese and white subjects or between the two isomers." | ( Differences in stereoselective disposition of propranolol do not explain sensitivity differences between white and Chinese subjects: correlation between the clearance of (-)- and (+)-propranolol. Wood, AJ; Zhou, HH, 1990) | 0.79 |
" The elimination half-life of moricizine is 2 to 6 hours, but its duration of antiarrhythmic action is much longer suggesting active metabolites." | ( Clinical pharmacokinetics of moricizine. Barbey, JT; Schwartz, SL; Siddoway, LA; Woosley, RL, 1990) | 0.28 |
"The pharmacokinetic profile and the cardiovascular actions of desethyl-N-acetylprocainamide (NAPADE) were studied in chloralose-urethane anesthetized dogs." | ( Cardiovascular actions and pharmacokinetics of desethyl-N-acetylprocainamide in the dog. King, LW; Lertora, JJ, 1986) | 0.27 |
" The short duration of the bypass procedure and the continuous changes during the process hamper a rigorous pharmacokinetic evaluation." | ( Cardiopulmonary bypass and the pharmacokinetics of drugs. An update. Bogaert, MG; Buylaert, WA; Herregods, LL; Mortier, EP, 1989) | 0.28 |
" No clinically relevant pharmacokinetic interactions between cilazapril and propranolol were found." | ( Pharmacokinetic and pharmacodynamic interactions between the ACE inhibitor cilazapril and beta-adrenoceptor antagonist propranolol in healthy subjects and in hypertensive patients. Belz, GG; Breithaupt, K; Erb, K; Essig, J; Hoogkamer, JF; Kleinbloesem, CH; Kneer, J, 1989) | 0.71 |
"In an open, crossover study, the pharmacokinetic and pharmacodynamic profiles of lisinopril and enalapril, administered alone and in combination with propranolol, were evaluated in 12 volunteers." | ( Comparative pharmacokinetics and pharmacodynamics of lisinopril and enalapril, alone and in combination with propranolol. Bendtsen, F; Henriksen, JH, 1989) | 0.69 |
" The isolated vagus nerve-trachea tube preparation of the guinea-pig is well suited for the concommitant study of pharmacodynamic and pharmacokinetic properties of bronchodilator drugs." | ( Pharmacodynamic and pharmacokinetic aspects on the transport of bronchodilator drugs through the tracheal epithelium of the guinea-pig. Jeppsson, AB; Roos, C; Waldeck, B; Widmark, E, 1989) | 0.28 |
" The Cmax was significantly higher with C propranolol in both phases." | ( Pharmacodynamic and pharmacokinetic study of propranolol in patients with cirrhosis and portal hypertension. Blanc, M; Calès, P; Cotonat, J; Grasset, D; Meskens, C; Pascal, JP; Ravaud, A; Vinel, JP, 1989) | 0.8 |
"The pharmacokinetic and pharmacodynamic studies of four different brands of propranolol (Inderal, Ciplar, Corbeta and Propal) were carried out after single and multiple dosing on six normal adult healthy volunteers in a randomized crossover fashion to determine any inter-brand variations in bioavailability and pharmacodynamic effects." | ( Comparative pharmacokinetic and pharmacodynamic study of four different brands of propranolol in normal volunteers. Biswas, NR; Garg, SK; Kumar, N; Mukherjee, S; Sharma, PL, 1989) | 0.73 |
" The half-life of propranolol and lidocaine in the initial phase of elimination correlated with the degree of portal-arterial disorders in liver blood supply." | ( [Usefulness of the evaluation of blood supply and mass of the liver for predicting the rate of pharmacokinetics of lidocaine, propranolol and phenazone]. Becker, A; Bołdys, H; Hartleb, M; Kloc, T; Mańczyk, I, 1989) | 0.82 |
" The doubling of the dose administered was reflected in blood concentrations but not in pharmacodynamic parameters." | ( Pharmacokinetic and pharmacodynamic comparison of two doses of long acting propranolol (80 and 160 mg) in healthy subjects. Berlin, I; Cournot, A; Duchier, J; Flouvat, B; Robinet, D; Rossi, A; Sarmini, H, 1989) | 0.51 |
"vg application, both the AUC and the Cmax values of PPL were significantly greater than those of orally dosed females, while no statistically significant differences were found in the tmax values." | ( A comparative study of the pharmacokinetics of propranolol and its major metabolites in the rat after oral and vaginal administration. Buttar, HS; Qureshi, SA, 1989) | 0.53 |
"The pharmacokinetic and pharmacodynamic effects of nisoldipine, a 1,4-dihydropyridine calcium entry blocker, and the lipophilic beta-adrenoceptor blocker propranolol were assessed alone and in combination in 12 healthy men." | ( Pharmacokinetic and pharmacodynamic interactions between nisoldipine and propranolol. Leenen, FH; Levine, MA; Ogilvie, RI, 1988) | 0.7 |
"Comparative pharmacokinetic studies with the beta-receptor blocking drugs propranolol, metoprolol, sotalol and atenolol, differing greatly in lipophilicity, and their main route of elimination were performed in light-dark-synchronized rats after equimolar single (6 mumoles/kg) or multiple (6 X 6 mumoles/kg) drug application." | ( Chronopharmacokinetics of beta-receptor blocking drugs of different lipophilicity (propranolol, metoprolol, sotalol, atenolol) in plasma and tissues after single and multiple dosing in the rat. Fink, M; Lemmer, B; Ohm, T; Winkler, H, 1985) | 0.73 |
" The poor metaboliser phenotype is associated with increased plasma drug concentrations, a prolongation of elimination half-life and more intense and sustained beta-blockade." | ( The polymorphic oxidation of beta-adrenoceptor antagonists. Clinical pharmacokinetic considerations. Lennard, MS; Tucker, GT; Woods, HF, ) | 0.13 |
"Pharmacokinetic and pharmacodynamic interactions between nifedipine and two beta-blocking agents were investigated." | ( Pharmacokinetic and pharmacodynamic interactions between nifedipine and propranolol or betaxolol. Canal, M; Carbon, C; Cascio, B; Domart, Y; Flouvat, B; Larribaud, J; Orofiamma, B; Roux, A; Vinceneux, P, 1986) | 0.5 |
" The pharmacokinetic parameters show an enhanced plasma elimination of both drugs at interrupted enterohepatic circulation compared to the control group." | ( The pharmacokinetics of exaprolol and propranolol in rats with interrupted enterohepatic circulation. Bezek, S; Durisová, M; Faberová, V; Misánikova, K; Motheová, O; Trnovec, T; Zemánek, M, ) | 0.4 |
" The duration of action and elimination half-life both averaged less than 15 min." | ( Pharmacodynamics and onset of action of esmolol in anesthetized dogs. Gorczynski, RJ; Quon, CY, 1986) | 0.27 |
"The pharmacodynamic profile of bisoprolol, a new beta 1-selective adrenoceptor antagonist, was investigated in four independent studies including 36 healthy male volunteers." | ( Pharmacodynamic profile of bisoprolol, a new beta 1-selective adrenoceptor antagonist. Bühring, KU; Leopold, G; Pabst, J; Simane, Z; Ungethüm, W; Wiemann, H, 1986) | 0.27 |
"82 ml/min/kg) and prolonged elimination half-life (29 vs." | ( Bromazepam pharmacokinetics: influence of age, gender, oral contraceptives, cimetidine, and propranolol. Burstein, ES; Friedman, H; Greenblatt, DJ; Harmatz, JS; Locniskar, A; Ochs, HR; Shader, RI, 1987) | 0.49 |
" Betaxolol (Kerlon, 8) was found to exhibit an appropriate preclinical pharmacological and human pharmacokinetic profile (elevated oral bioavailability and prolonged plasma half-life) for the treatment of chronic cardiovascular diseases such as hypertension and angina." | ( Synthesis of a series of compounds related to betaxolol, a new beta 1-adrenoceptor antagonist with a pharmacological and pharmacokinetic profile optimized for the treatment of chronic cardiovascular diseases. Binet, JL; Cavero, IG; Lefèvre-Borg, F; Manoury, PM; Rousseau, J, 1987) | 0.27 |
"01) increased half-life (8." | ( The effects of a beta-2 selective adrenergic agonist and a beta-nonselective antagonist on theophylline clearance. Bertino, JS; Goldberg, A; Lombardi, TP; Middleton, E; Slaughter, RL, 1987) | 0.27 |
" It is concluded that only on the basis of the respective receptor occupancy one may delineate pharmacodynamic differences of different drugs of the same class in man." | ( In vitro receptor occupancy allows to establish equieffective doses of beta-blockers with different pharmacodynamic profiles in man. Investigations with propranolol and bufuralol. Belz, GG; Matthews, JH; Palm, D; Wellstein, A, 1985) | 0.47 |
" The plasma half-life and area under the plasma concentration-time curve of antipyrine were unchanged." | ( Potential drug interactions with misoprostol: effects on the pharmacokinetics of antipyrine and propranolol. Bennett, PN; Fenn, GC; Notarianni, LJ, 1988) | 0.49 |
" The results indicate that Betalong (SR propranolol) satisfies the pharmacokinetic criteria expected of a sustained release preparation of propranolol and may be useful in single daily dose." | ( Pharmacokinetic study of a new sustained release preparation of propranolol in normal healthy volunteers. Biswas, NR; Garg, SK; Gyawali, K; Kumar, N; Lal, R; Narendranath, KA; Sharma, PL, 1988) | 0.78 |
"The interactions of propranolol, nimodipine, and amiodarone with membrane lipids were examined in an effort to explain their different pharmacokinetic and pharmacodynamic properties." | ( Possible molecular basis for the pharmacokinetics and pharmacodynamics of three membrane-active drugs: propranolol, nimodipine and amiodarone. Chester, DW; Herbette, LG; Katz, AM; Trumbore, M, 1988) | 0.81 |
"05) between dosage forms in the mean (n = 28) area under the plasma concentration-time curve (AUC), maximum plasma concentration (Cmax) or time to Cmax (tmax) for propranolol or its active metabolite, 4-hydroxypropranolol." | ( Steady state relative bioavailability and pharmacokinetics of oral propranolol in black and white North Americans. Lesko, LJ; Perkal, M; Sharoky, M; Turner, R, ) | 0.56 |
" Compared with conventionally formulated propranolol, long acting propranolol has a prolonged terminal half-life (8 to 11 hours), due to slower absorption from the gut." | ( Pharmacokinetics of long acting propranolol. Implications for therapeutic use. Nace, GS; Wood, AJ, 1987) | 0.82 |
" ANOVA revealed significant circadian changes in the peak propranolol concentration (Cmax), with a maximum at 08 h and a minimum at 02 h after drug intake; tmax was not dependent on the circadian phase." | ( Circadian changes in the pharmacokinetics and cardiovascular effects of oral propranolol in healthy subjects. Langner, B; Lemmer, B, 1988) | 0.75 |
" An elevation of the mean Cmax was found, from 73." | ( Pharmacokinetic interaction between nifedipine and propranolol. Koren, G; Levy, M; Turetz-Abramovitch, M; Zylber-Katz, E, 1988) | 0.53 |
" administration of antipyrine, the systemic clearance was decreased, the volume of distribution was unchanged and the half-life was increased 48 hr after catheter implantation." | ( Alteration of the pharmacokinetics and metabolism of propranolol and antipyrine elicited by indwelling catheters in the rat. Belpaire, FM; Bogaert, MG; Chindavijak, B; De Smet, F, 1988) | 0.52 |
" Elimination half-life was similar for the two populations (3." | ( Comparative pharmacokinetics of intravenous propranolol in obese and normal volunteers. Barre, J; Cheymol, G; Dry, J; Poirier, JM; Pradalier, A, 1987) | 0.53 |
"This double-blind, placebo-controlled, four-period cross-over study was undertaken to evaluate the sustained-release characteristics of long-acting propranolol hydrochloride (Inderal LA, Ayerst Laboratories, New York, NY) 60 mg qd, to compare the pharmacokinetic and pharmacodynamic properties of this formulation with conventional propranolol 20 mg tid, and to evaluate the proportionality of long-acting propranolol 60 mg (LA 60 mg) and long-acting propranolol 80 mg (LA 80 mg)." | ( Pharmacokinetics and pharmacodynamics of long-acting propranolol 60-mg capsules: a comparative evaluation. Dey, M; Dorick, DM; Garg, DC; Jallad, NS; Marino, MR; Martinez, JJ; Weidler, DJ, 1987) | 0.72 |
"Peculiarities of propranolol pharmacokinetics in patients with acute myocardial infarction were determined after oral administration of 80 mg of the drug and compared with control group of patients with stage II hypertensive disease: a significant increase of Cmax, Tmax and AUC without changes of kel and T1/2." | ( [Pharmacokinetic characteristics of propranolol in patients with a history of acute myocardial infarct]. Kalenikov, EI; Katrukha, SP; Kukes, VG; Zagrebin, SV, ) | 0.75 |
" The differences between the average pharmacokinetic parameter estimates for the group did not differ significantly between the two periods of study." | ( Propranolol pharmacokinetics during the menstrual cycle. Abdu-Aguye, I; Dunlop, D; Patel, P; Turner, P, 1986) | 1.71 |
" The pharmacokinetic data are consistent with a decrease in intrinsic hepatic clearance of propranolol, leading to an increase in bioavailability at steady-state." | ( Propranolol pharmacokinetics and pharmacodynamics after single doses and at steady-state. Bottorff, MB; Lalonde, RL; Mirvis, DM; Pieper, JA; Straka, RJ, 1987) | 1.94 |
"This investigation was conducted to compare the pharmacokinetic and pharmacodynamic effects of single and multiple doses of conventional propranolol and long-acting propranolol in healthy human volunteers." | ( Comparative pharmacodynamics and pharmacokinetics of conventional and long-acting propranolol. Chalavarya, G; Fencik, M; Garg, DC; Jallad, NS; Kraml, M; Mishriki, A; Weidler, DJ, ) | 0.56 |
" There were no statistical differences in the pharmacokinetic parameters between the both preparations." | ( [Comparative pharmacokinetic studies on the relative biologic availability of two propranolol preparations in patients with steady state essential hypertension]. Faulhaber, HD; Gohlke, HR; Prehm, C; Rostock, G, 1986) | 0.5 |
"01) with no change in plasma half-life or plasma binding." | ( Increased clearance of propranolol and theophylline by high-protein compared with high-carbohydrate diet. Bai, SA; Fagan, TC; Gaffney, TE; Oexmann, MJ; Walle, T; Walle, UK, 1987) | 0.58 |
"Various pharmacokinetic parameters--disposition half-life, t1/2,z, metabolic clearance CLm, volume of distribution V, intrinsic clearance of unbound drug CLuint, and unbound volume of distribution of tissues (distributive tissue volume/fraction of drug in tissue unbound, VT/fuT--are compared in rat and human for nine weakly acidic drugs, phenytoin, hexobarbital, pentobarbital, phenylbutazone, warfarin, tolbutamide, valproate, phenobarbital, and amobarbital, and six weakly basic drugs, quinidine, chlorpromazine, propranolol, pentazocin, antipyrine, and diazepam." | ( Prediction of the disposition of nine weakly acidic and six weakly basic drugs in humans from pharmacokinetic parameters in rats. Hanano, M; Iga, T; Sawada, Y; Sugiyama, Y, 1985) | 0.43 |
" The pharmacokinetic profiles of the isoxicam plasma concentration/time data obtained over 96 h following the doses of isoxicam before and during propranolol administration were compared." | ( The effect of administration of propranolol on the pharmacokinetics of isoxicam. Besner, JG; Caillé, G; Lacasse, Y; Larivière, L; Vézina, M, ) | 0.62 |
"The pharmacokinetic properties of propranolol and atenolol were evaluated both in 9 patients with cirrhosis and in 12 healthy subjects." | ( Hemodynamic and pharmacokinetic study of propranolol and atenolol in cirrhosis patients. Decourt, S; Flouvat, B; Lebrec, D; Leneveu, A; Rocher, I; Rosier, SP, 1985) | 0.81 |
"The pharmacokinetic parameters of nipradilol (NIP), a new potent antihypertensive and antianginal agent, and propranolol were determined after oral, intravenous and intraportal administration to the beagle dog implanted with cannula in portal vein at a dose of 1 mg/kg." | ( Pharmacokinetics of nipradilol (K-351), a new antihypertensive agent. II. Influence of the route of administration on bioavailability in dogs. Fujii, M; Ito, T; Kojima, J; Suzuki, J; Yoshimura, M, 1985) | 0.48 |
"The pharmacodynamic activities of two beta adrenergic antagonists, propranolol and practolol, were compared in eight hypertensive patients." | ( Pharmacodynamic studies of beta adrenergic antagonism induced in man by propranolol and practolol. Bodem, G; Brammell, HL; Chidsey, CA; Weil, JV, 1973) | 0.72 |
" The clearance of both antipyrine and d-propranolol was increased and the half-life decreased significantly by phenobarbital." | ( Increased clearance of antipyrine and d-propranolol after phenobarbital treatment in the monkey. Relative contributions of enzyme induction and increased hepatic blood flow. Branch, RA; Nies, AS; Shand, DG; Wilkinson, GR, 1974) | 0.79 |
" The half-life of total radioactivity is greatly lengthened in the presence of severe renal failure while the half-lives of the pharmacologically active propranolol and 4-hydroxymetabolite are slightly reduced." | ( Pharmacodynamics of propranolol in renal failure. Foulkes, DM; Joekes, AM; Thompson, FD, 1972) | 0.77 |
" These results suggest the need for cautious interpretation of some venous pharmacokinetic data." | ( Instantaneous input hypothesis in pharmacokinetic studies. Chen, ML; Chiou, WL; Lam, G; Lee, MG, 1981) | 0.26 |
" 4 The peak blood level of betaxolol was reached 2 to 4 hr after its administration, the first-pass loss is likely to be low and the half-life is 12." | ( Beta-adrenoceptor blocking effects and pharmacokinetics of betaxolol (SL 75212) in man. Bianchetti, G; Chauvin, M; Giudicelli, JF; Gomeni, R; Morselli, PL; Richer, C; Thuillez, C, 1980) | 0.26 |
" No significant change in plasma half-life occurred and there was no correlation between the mean steady-state propranolol concentration and beta-adrenergic blockade or antihypertensive effect." | ( Relationship of propranolol pharmacokinetics to antihypertensive effect and beta-adrenergic blockade in the treatment of hypertension. Dunning, AJ; Krediet, RT; Offerhaus, L, 1980) | 0.82 |
" The l-isomer had a longer plasma half-life than dl-propranolol at each dose during the beta-phase." | ( Pharmacokinetics of propranolol isomers and their relationships with beta adrenoceptor blocking activity in rabbits administered with dl-propranolol. Ishikawa, H; Kawashima, K, 1980) | 0.84 |
"1 The speed of onset of the pharmacodynamic activity of intravenous propranolol, practolol, oxprenolol and metoprolol was determined, using attenuation of isoprenaline-induced tachycardia as the end-point, in 16 patients with clinically coronary heart disease." | ( Speed of onset of pharmacodynamic activity of propranolol, practolol, oxprenolol and metoprolol after intravenous infection in man. Lochan, R; Silke, B; Taylor, SH, 1981) | 0.76 |
" Although there was a statistically significant difference in certain pharmacokinetic parameters (maximum plasma concentration, area under the curve, elimination constant and elimination half-life) between elderly patients (more that 60 years) and young persons (20-30 years) no significant differences were found as far as smoking and nonsmoking is concerned." | ( Influence of smoking and age on pharmacokinetics of beta-receptor blockers. Beveridge, T; Fitscha, P; Hitzenberger, G; Nüesch, E; Pacha, W, 1982) | 0.26 |
" The present study did not show significant pharmacokinetic and pharmacodynamic interactions between nifedipine and lipophilic beta-adrenoceptor blockers." | ( Study of the influence of nifedipine on the pharmacokinetics and pharmacodynamics of propranolol, metoprolol and atenolol. Bellens, R; Degre, S; Degreve, M; Fitzsimons, TJ; Gangji, D; Herchuelz, A; Juvent, M; Niset, G; Poortmans, J; Wathieu, M, 1984) | 0.49 |
" The study reported here was designed to show whether the pharmacokinetics of verapamil are influenced by concurrent treatment with three different beta-adrenoceptor blockers, and whether there is any pharmacodynamic interaction between these drugs." | ( Pharmacokinetics and pharmacodynamics of verapamil in combination with atenolol, metoprolol and propranolol. Fitzsimons, TJ; Holt, D; Johnston, A; Warrington, SJ, 1984) | 0.49 |
"Higher AUC and Cmax values were obtained for metoprolol, oxprenolol and propranolol in groups receiving the low-dose oestrogen-ethinyl oestradiol oral contraceptive, but statistical significance was reached only with metoprolol AUC." | ( Beta-adrenoceptor blocker pharmacokinetics and the oral contraceptive pill. Jack, DB; Kendall, MJ; Quarterman, CP; Smith, SR; Zaman, R, 1984) | 0.5 |
" Unlike other calcium antagonists, detailed pharmacokinetic data are available for verapamil." | ( Clinical pharmacokinetics of verapamil. Blouin, RA; Hamann, SR; McAllister, RG, ) | 0.13 |
" The elimination half-life with LA was significantly longer than with CV (6." | ( Clinical pharmacokinetics and pharmacological actions of a long-acting formulation of propranolol. Ebihara, A; Kondo, K; Ohashi, K; Usami, M, 1984) | 0.49 |
"We have examined the analysis of pharmacodynamic data in normal subjects receiving propranolol, flecainide or the two together." | ( Application of second-order polynomial equations to the study of pharmacodynamic interactions: the effect of flecainide acetate and propranolol on cardiac output and vascular resistance. Berry, DA; Borrell, G; Holtzman, JL; Kvam, DC; Mottonen, L, 1984) | 0.7 |
" Propranolol was assayed in plasma by gas-liquid chromatography with electron-capture detection and the pharmacokinetic parameters were investigated." | ( Pharmacokinetics of propranolol during pregnancy. Kinney, CD; McDevitt, DG; Murnaghan, GA; O'Hare, MF, 1984) | 1.5 |
" Pharmacokinetic studies were carried out on the fifth day after injection of the renal toxin (renal failure group) or saline (control group)." | ( Pharmacokinetics of l-propranolol during repetitive dosing in normal and uranyl nitrate-induced renal failure rats. Shen, DD; Terao, N, 1984) | 0.58 |
" Additionally, physiological parameters considered to be relevant to the pharmacokinetic handling (absorption rate and splanchnic hemodynamics) were studied." | ( Interaction between oral hydralazine and propranolol. I. Changes in absorption, presystemic clearance and splanchnic blood flow. Bourne, R; Constantinides, S; Corbett, H; Heinzow, B; McLean, AJ, 1984) | 0.53 |
"The possibility to apply impedance cardiography technique and individual statistical analysis based on Dixon's criterion to pharmacodynamic studies of single hydralazine ( apressine ), prazosine ( pratsiol ), endralazine ( mirethilan ), propranolol (obsidan) doses is discussed." | ( [Methodologic approach to individual evaluation of the pharmacodynamic effects of single doses of hydralazine, endralazine, prazosine and propranolol in hypertension patients]. Izotov, AI; Postol'nikov, SF; Vygodin, VA, 1984) | 0.65 |
" The therapeutic dose, clearance, extraction coefficient, bioavailability and half-life are the object of particular study." | ( [Pharmacokinetics of anti-arrhythmics. 2. Clinical applications]. Bricaud, H; Lévy, RH; Lévy, S, 1980) | 0.26 |
" Pharmacokinetic of propranolol, phenytoin and lidocain was studied in groups of male "Fauve de Bourgogne" rabbits." | ( [Pharmacokinetics of propranolol, phenytoin and lidocaine in hypercholesterolemic rabbits]. Albin, H; Pehourcq, F; Ploux, D; Vinçon, G, ) | 0.77 |
" There was no statistically significant difference in elimination half-life (t1/2) between (+/-)- and (-)-propranolol before and after antithyroid drug therapy." | ( Pharmacokinetics and pharmacodynamics of propranolol stereoisomers in hyperthyroid patients. Ebihara, A; Ishikawa, H; Kawashima, K; Saito, K; Tawara, K; Yamamoto, K; Yoshida, S, 1981) | 0.74 |
" The pharmacodynamic study was performed according to an original technique consisting in a sequence of monitored repeated identical treadmill exercise." | ( [Comparative pharmacodynamic study of Cordanum and obzidan in stress angina pectoris patients]. Nazarenko, VA; Nikolenko, SA, 1981) | 0.26 |
" As the effects of beta-blocking agents on the symptoms of hyperthyroidism are correlated with the serum concentration of the drugs, sotalol, with its long half-life and unaltered elimination in hyperthyroidism, has certain advantages over propranolol in the treatment of thyrotoxicosis." | ( Pharmacokinetics of propranolol and sotalol in hyperthyroidism. Anttila, M; Aro, A; Korhonen, T; Sundquist, H, 1982) | 0.77 |
"1 Pharmacokinetic investigations were carried out in a group of 32 ambulant normal male volunteers in order to determine the effect of age and smoking on steady-state plasma levels of pindolol and propranolol." | ( Effects of age and smoking on the pharmacokinetics of pindolol and propranolol. Beveridge, T; Fitscha, P; Hitzenberger, G; Nüesch, E; Pacha, W, 1982) | 0.69 |
" 6 There was no significant difference in plasma propranolol levels, Cmax propranolol or AUCo-x following the three preparations." | ( Comparative pharmacological and pharmacokinetic observations on propranolol (long acting formulation) and bendrofluazide administered separately and concurrently to volunteers. Barker, NP; Castle, WM; Harron, DW; McAinsh, J; Nicholls, DP; Shanks, RG, 1982) | 0.76 |
"1 L/min) propranolol although the half-life of propranolol did not change significantly." | ( Increased clearance of propranolol in thyrotoxicosis. Crooks, J; Feely, J; Stevenson, IH, 1981) | 0.99 |
" Both arterial and venous data were then subjected to extensive pharmacokinetic analyses utilizing standard procedures." | ( Arterial and venous blood sampling in pharmacokinetic studies: propranolol in rabbits and dogs. Chiou, WL; Lam, G, 1981) | 0.5 |
" A multiexponential curve-stripping program was used for the pharmacokinetic analysis." | ( Pharmacokinetics of propranolol. Borgström, L; Johansson, CG; Larsson, H; Lenander, R, 1981) | 0.59 |
" Nicardipine increased significantly the AUC and Cmax of oral propranolol (1." | ( Influences of the calcium antagonists nicardipine and nifedipine, and the calcium agonist BAY-K-8644, on the pharmacokinetics of propranolol in rats. Dupont, AG; Massart, DL; Schoors, DF; Vercruysse, I, 1993) | 0.73 |
"The action of the beta-adrenoblocker anaprilline on the pharmacodynamic effects of strophanthin was examined in in vivo experiments during simulated rat heart failure and on isolated frog atrial specimens." | ( [Effect of anapriline on the pharmacodynamic effects of strophanthin in experiments on isolated myocardial preparations and under conditions of simulation of cardiac insufficiency]. Lemkina, SM, ) | 0.13 |
" The method is applied to pharmacokinetic studies of racemic propranolol in human plasma and urine." | ( Microassay of propranolol enantiomers and conjugates in human plasma and urine by high-performance liquid chromatography after chiral derivatization for pharmacokinetic study. Claude, JR; Ellouk-Achard, S; Fompeydie, D; Galons, H; Gramond, JP; Levresse, V; Pham-Huy, C; Saada, V; Sahui-Gnassi, A, 1994) | 0.89 |
" We assessed pharmacokinetic and pharmacodynamic interactions of the ACE inhibitor cilazapril and the beta-blocker propranolol in healthy volunteers and patients with essential hypertension." | ( Review of studies on the clinical pharmacodynamics of cilazapril. Belz, GG; Breithaupt, K; Erb, K, 1994) | 0.5 |
" Stereoselective analysis showed the apparent distribution volume and the area under plasma concentration-time curves (AUC) of R-(+)-propranolol to be, respectively, one-quarter and twice those of the S-(-)-enantiomer and differences in pharmacokinetic parameters between the two were magnified by turpentine oil pretreatment." | ( Effects of turpentine oil pretreatment on beta-blocker pharmacokinetic parameters in rats. Hasegawa, R; Kimura, T; Murai-Kushiya, M; Okada, S, 1993) | 0.49 |
"To evaluate the pharmacodynamic properties of carvedilol across a broad range of doses in relation to its enantiospecific kinetics and adrenergic receptor occupancies, relative to placebo and propranolol." | ( Dose-effect and pharmacokinetic-pharmacodynamic relationships of the beta 1-adrenergic receptor blocking properties of various doses of carvedilol in healthy humans. Belz, GG; Breithaupt, K; de Mey, C; Neugebauer, G; Palm, D; Schloos, J, 1994) | 0.48 |
"The pharmacokinetic and pharmacodynamic interactions after 7 days of oral treatment with nisoldipine (10 mg twice daily) and propranolol (80 mg twice daily) were investigated in a partially randomized, placebo-controlled crossover study of 12 healthy volunteers." | ( Pharmacokinetic and pharmacodynamic interactions during multiple-dose administration of nisoldipine and propranolol. Leenen, FH; Ogilvie, RI; Shaw-Stiffel, TA; Walker, SE, 1994) | 0.71 |
"At the end of each treatment period, pharmacokinetic parameters were measured, along with blood pressure, heart rate, cardiac function, systemic hemodynamics, plasma catecholamines, forearm blood flow, and apparent hepatic blood flow (estimated by the clearance of indocyanine green dye)." | ( Pharmacokinetic and pharmacodynamic interactions during multiple-dose administration of nisoldipine and propranolol. Leenen, FH; Ogilvie, RI; Shaw-Stiffel, TA; Walker, SE, 1994) | 0.5 |
" Therefore, the purpose of this study was to evaluate the effect of immediate-release (IR) and sustained-release (SR) verapamil on the pharmacokinetic parameters of propranolol in 12 healthy men." | ( Evaluation of dosage-release formulations on inhibition of drug clearance: effect of sustained- and immediate-release verapamil on propranolol pharmacokinetic parameters. Bleske, BE; Edwards, DJ; Rodman, DP; Shea, MJ; Touchette, MA; Welage, LS, 1994) | 0.69 |
" Coadministration of nicardipine significantly increased the AUC and Cmax and significantly decreased the Cl(o) and Cl'intr for unbound drug of (R)- and (S)-propranolol." | ( Enantioselective inhibitory effect of nicardipine on the hepatic clearance of propranolol in man. Belpaire, F; Dupont, AG; Massart, DL; Vercruysse, I; Wynant, P, 1994) | 0.71 |
"The pharmacokinetic studies of propranolol following the application of the propercuten transdermal therapeutic system were performed in conscious rabbits previously assigned to 3 groups." | ( [The pharmacokinetics of propranolol when used with the propercuten transdermal therapeutic system (experimental data)]. Belolipetskaia, VG; Chichenkov, ON; Fel'dshteĭn, MM; Metelitsa, VI; Piotrovskiĭ, VK; Shorr, VA; Vasil'ev, AE, ) | 0.72 |
"A comprehensive study was undertaken to examine the pharmacokinetic and pharmacodynamic interaction of propranolol and nifedipine in 11 patients with stable angina of effort who were treated for a long time." | ( [The pharmacokinetic interaction of propranolol and nifedipine in patients with angina of effort]. Belolipetskaia, VG; Kokurina, EV; Kukushkin, SK; Metelitsa, VI; Piotrovskiĭ, VK; Rumiantsev, DO, ) | 0.62 |
" The peak concentration of propranolol in plasma was 10." | ( Pharmacokinetics of propranolol used for suppressing tachycardia in hyperthyroidism. Masuda, H; Miyake, F; Motohashi, F; Murayama, M; Musha, H; Sugai, J; Takada, H, 1994) | 0.91 |
"We have studied the pharmacodynamic effects of ramipril, propranolol, and their combination, as well as the effect of propranolol on the pharmacokinetics of ramipril in 12 healthy men (age 24 (SD 6) y, weight 72 (7) kg)." | ( The pharmacokinetic and pharmacodynamic interactions of ramipril with propranolol. Cohen, AF; Frölich, M; Schoemaker, HC; Seibert-Grafe, M; van Griensven, JM, 1993) | 0.77 |
" Systemic exposure is limited because of extensive sequestration by the liver and/or first-pass metabolism, a plasma half-life of approximately 30 min, no circulating active metabolites, and no accumulation of drug during chronic dosing." | ( Pharmacokinetics of fluvastatin and specific drug interactions. Hwang, DS; Jokubaitis, LA; Robinson, WT; Smith, HT; Troendle, AJ, 1993) | 0.29 |
" There were similar time-variant changes in Cmax and tmax for 4-hydroxypropranolol and naphthoxylactic acid." | ( The effect of age on diurnal variation in the pharmacokinetics of propranolol in hypertensive subjects. Ebihara, A; Fujimura, A; Ohashi, K; Shiga, T; Tateishi, T, 1993) | 0.76 |
" No significant difference was observed in the elimination half-life between the two trials." | ( Differences of chronopharmacokinetic profiles between propranolol and atenolol in hypertensive subjects. Ebihara, A; Fujimura, A; Ohashi, K; Shiga, T; Tateishi, T, 1993) | 0.53 |
" Charcoal treatment significantly reduced the half-life of elimination (16." | ( Effect of oral activated charcoal on propranolol pharmacokinetics following intravenous administration to rabbits. al-Angary, AA; al-Dardiri, MM; al-Meshal, MA; el-Sayed, YM, 1993) | 0.56 |
" Different pharmacokinetic parameters were determined from the plasma concentration-time profiles using a model-independent computer programme, RAMKIN." | ( In vitro and in vivo studies on slow release propranolol hydrochloride suppositories. Pharmacokinetic and pharmacodynamic evaluation. Diwan, PV; Krishna, DR; Sastri, MS; Satyanarayana, NV, 1993) | 0.55 |
" With coadministration, the maximum peak concentration (Cmax) and area under the concentration-time curve over the dosing interval (AUC tau) of propranolol decreased 29% and 14%, respectively; Cmax and AUC tau of 4-hydroxy-propranolol decreased 15% and 21%, respectively." | ( Pharmacokinetic and pharmacodynamic evaluation during coadministration of nefazodone and propranolol in healthy men. Fulmor, IE; Lee, JS; Marathe, PH; Raymond, RH; Salazar, DE; Uderman, HD, 1995) | 0.71 |
" Plasma Pro levels were determined by HPLC with fluorescence detector and the pharmacokinetic parameters were calculated by using the MCPKP program." | ( Sex differences in pharmacokinetics of oral propranolol in healthy Chinese volunteers. Chen, X; Xie, HG, 1995) | 0.55 |
" No statistical differences were detected in the experimental propranolol pharmacokinetic parameters (maximal concentration, time of maximal concentration, terminal half-life, area under the curve, and protein binding) or derived pharmacokinetic parameters (intrinsic clearance, bioavailability, clearance, and volume of distribution)." | ( The lack of effect of aerobic exercise training on propranolol pharmacokinetics in young and elderly adults. Cediel, M; Derendorf, H; Garzarella, L; Graves, JE; Guillen, GJ; Krumerman, J; Panton, LB; Pollock, ML; Vivas, C; Williams, L, 1995) | 0.78 |
"We determined the haemodynamic, electrocardiographic and electrophysiologic effects, and the pharmacokinetic properties of 4'-hydroxypropranolol (4'-OHP) by conducting three different experiments in dogs." | ( Haemodynamic, electrocardiographic, electrophysiologic and pharmacokinetic activity of 4'-hydroxypropranolol in dogs. Muir, WW; Sams, RA; Schall, SF, 1996) | 0.72 |
"3 mg/kg) pharmacokinetic parameters was studied in rabbits." | ( The influence of selected general anesthetics on pharmacokinetic parameters of some antiarrhythmic drugs in rabbits. Part III. Propranolol. Orszulak-Michalak, D, ) | 0.34 |
"To examine the pharmacokinetic profile of propranolol in cats before and during experimentally induced hyperthyroidism." | ( Pharmacokinetics of propranolol in healthy cats during euthyroid and hyperthyroid states. Calvert, C; Ferguson, D; Jacobs, G; Sams, R; Whittem, T, 1997) | 0.88 |
"The pharmacokinetic data for the three drugs were qualitatively similar." | ( Pharmacokinetics of beta-adrenoceptor blockers in obese and normal volunteers. Carrupt, PA; Cheymol, G; Levron, JC; Poirier, JM; Snoeck, E; Testa, B; Weissenburger, J, 1997) | 0.3 |
" The Finapres measures the peripheral pressure using the volume clamp principle; it has not been validated under altered physiological conditions and during pharmacodynamic interventions." | ( Reliability of blood pressure determination with the Finapres with altered physiological states or pharmacodynamic conditions. Farrell, S; McAuley, D; Silke, B, 1997) | 0.3 |
" Apparent oral clearance and elimination half-life of propranolol were not different between EMs and PMs." | ( Impact of CYP2D6 poor metabolizer phenotype on propranolol pharmacokinetics and response. Burlew, BS; Sowinski, KM, ) | 0.64 |
" Multiple blood samples were collected for up to 12 hours on the fourth day to characterize the steady-state pharmacokinetic profile of each enantiomer." | ( Steady-state pharmacokinetics of propranolol enantiomers in healthy male volunteers. Bowles, SK; Paradiso-Hardy, FL; Walker, SE, 1998) | 0.58 |
" No stereoselective pharmacokinetic differences were observed between total (bound and unbound) and unbound (R)- and (S)-propranolol." | ( Steady-state pharmacokinetics of propranolol enantiomers in healthy male volunteers. Bowles, SK; Paradiso-Hardy, FL; Walker, SE, 1998) | 0.79 |
"Stereoselective steady-state pharmacokinetic differences in AUC(0-720) were observed between (R)- and (S)-propranolol." | ( Steady-state pharmacokinetics of propranolol enantiomers in healthy male volunteers. Bowles, SK; Paradiso-Hardy, FL; Walker, SE, 1998) | 0.79 |
"In support of clinical antianginal studies, the vasodilator nicorandil (NIC) was combined with the beta-adrenergic receptor antagonists propranolol (PRO) and atenolol (ATN) and with the calcium channel blocker diltiazem (DTZ) to determine their cardiovascular and pharmacokinetic interactions." | ( Cardiovascular and pharmacokinetic interactions between nicorandil and adjunctive propranolol, atenolol or diltiazem in conscious dogs. Humphrey, SJ, 1998) | 0.73 |
"The lipophilic beta-adrenoreceptor antagonist propranolol has been studied to define its pharmacokinetic and pharmacodynamic characteristics in hyperlipidemic patients." | ( Studies on the pharmacokinetics and pharmacodynamics of propranolol in hyperlipidemia. Droździk, M; Gawrońska-Szklarz, B; Kutrzeba, J; Sterna, Z; Sulzyc-Bielicka, V; Wójcicki, J, 1999) | 0.81 |
"Several statistical regression models and artificial neural networks were used to predict the hepatic drug clearance in humans from in vitro (hepatocyte) and in vivo pharmacokinetic data and to identify the most predictive models for this purpose." | ( Combining in vitro and in vivo pharmacokinetic data for prediction of hepatic drug clearance in humans by artificial neural networks and multivariate statistical techniques. Coassolo, P; Lavé, T; Schneider, G, 1999) | 0.3 |
" The recirculatory pharmacokinetic model incorporates data from both the initial transient oscillations and the later post-mixing portions of the blood indocyanine green concentration versus time curves to characterize not only blood volume and cardiac output but also their distribution among a central blood volume and fast and slow peripheral volumes in lumped parallel circuits." | ( Indocyanine green kinetics characterize blood volume and flow distribution and their alteration by propranolol. Avram, MJ; Enders-Klein, C; Henthorn, TK; Krejcie, TC; Niemann, CU; Shanks, CA, 2000) | 0.52 |
" Propranolol and atenolol, as representatives of lipophilic and hydrophilic beta-adrenoreceptor antagonists, have been studied in order to define their pharmacokinetic characteristics in patients after partial gastrectomy." | ( Pharmacokinetics of propranolol and atenolol in patients after partial gastric resection: a comparative study. Drozdzik, M; Gawronska-Szklarz, B; Kostyrka, R; Kozlowski, K; Pawlik, A; Sterna, R; Wójcicki, J; Wójcicki, M; Wojciechowski, G, 2000) | 1.54 |
" Pharmacokinetic parameters of propranolol and atenolol were calculated using a one-compartment open model with first-order absorption." | ( Pharmacokinetics of propranolol and atenolol in patients after partial gastric resection: a comparative study. Drozdzik, M; Gawronska-Szklarz, B; Kostyrka, R; Kozlowski, K; Pawlik, A; Sterna, R; Wójcicki, J; Wójcicki, M; Wojciechowski, G, 2000) | 0.92 |
" Pharmacokinetic parameters of propranolol were different in subjects submitted to surgery compared with healthy persons." | ( Pharmacokinetics of propranolol and atenolol in patients after partial gastric resection: a comparative study. Drozdzik, M; Gawronska-Szklarz, B; Kostyrka, R; Kozlowski, K; Pawlik, A; Sterna, R; Wójcicki, J; Wójcicki, M; Wojciechowski, G, 2000) | 0.92 |
" The biologic half-life (T1/2) of PPL obeys the allometric equation in some animal species including rats and horses, except for human." | ( Pharmacokinetics of propranolol and its metabolites in horses after intravenous or oral administration. Aramaki, S; Koizumi, T; Mori, M; Nakata, M; Shinohara, A, 2000) | 0.63 |
" Treatment effects on pharmacokinetic parameters were assessed by analysis of variance (ANOVA)." | ( Lack of pharmacokinetic interaction between the antimigraine compound, almotriptan, and propranolol in healthy volunteers. Azie, NE; Carel, BJ; Fleishaker, JC; Sisson, TA, 2001) | 0.53 |
" The present studies investigated the potential for pharmacokinetic or pharmacodynamic interaction between beta-adrenoceptor blockers and rizatriptan." | ( Influence of beta-adrenoceptor antagonists on the pharmacokinetics of rizatriptan, a 5-HT1B/1D agonist: differential effects of propranolol, nadolol and metoprolol. De Smet, M; Goldberg, MR; Halpin, R; James, I; Kari, PH; Lee, Y; Lowry, R; Olah, TV; Sciberras, D; Tomasko, L; Vyas, KP; Zhao, J, 2001) | 0.52 |
"5 days) increased the AUC(0, infinity) for rizatriptan by approximately 67% and the Cmax by approximately 75%." | ( Influence of beta-adrenoceptor antagonists on the pharmacokinetics of rizatriptan, a 5-HT1B/1D agonist: differential effects of propranolol, nadolol and metoprolol. De Smet, M; Goldberg, MR; Halpin, R; James, I; Kari, PH; Lee, Y; Lowry, R; Olah, TV; Sciberras, D; Tomasko, L; Vyas, KP; Zhao, J, 2001) | 0.52 |
" As a class, the beta blockers are quite diverse from a pharmacokinetic perspective, as they display a high range of values in plasma protein binding, percent of drug eliminated by metabolism or unchanged in the urine, and in hepatic extraction ratio." | ( Stereospecific pharmacokinetics and pharmacodynamics of beta-adrenergic blockers in humans. Brocks, DR; Mehvar, R, ) | 0.13 |
" This simple and sensitive assay method was feasibly applied to the pharmacokinetic study of propranolol after intravenous administration of 2 mg/kg of propranolol to normal and carbon tetrachloride-induced liver cirrhotic rats." | ( Determination of propranolol concentration in small volume of rat plasma by HPLC with fluorometric detection. Hong, JH; Kang, JS; Kim, HK; Lee, MH; Park, MS, 2001) | 0.87 |
" These data about new drug candidates could be integrated/connected in physiologically based pharmacokinetic (PBPK) models to estimate a priori the overall plasma and tissue kinetic behaviors under in vivo conditions." | ( Prediction of pharmacokinetics prior to in vivo studies. II. Generic physiologically based pharmacokinetic models of drug disposition. Poulin, P; Theil, FP, 2002) | 0.31 |
"This study was designed to determine the relationship of propranolol pharmacokinetic parameters with portosystemic shunt in CCl4-induced cirrhotic rats." | ( [Relationship of propranolol pharmacokinetic parameters with portosystemic shunt in CCl4-induced cirrhotic rats]. Choi, HS; Choi, YY; Hahm, JS; Kang, JS; Kim, DU; Kim, JB; Kim, JM; Koh, DH; Lee, MH; Lee, SH; Park, GT; Yun, YS, 2002) | 0.9 |
" Pharmacokinetic parameters such as C0, AUC, t1/2(beta), and CLp were determined in each group." | ( [Relationship of propranolol pharmacokinetic parameters with portosystemic shunt in CCl4-induced cirrhotic rats]. Choi, HS; Choi, YY; Hahm, JS; Kang, JS; Kim, DU; Kim, JB; Kim, JM; Koh, DH; Lee, MH; Lee, SH; Park, GT; Yun, YS, 2002) | 0.65 |
"The lipophilic beta-adrenoreceptor antagonist propranolol and hydrophilic atenolol have been studied to define their pharmacokinetic and pharmacodynamic characteristics in obese patients." | ( Comparative pharmacokinetics and pharmacodynamics of propranolol and atenolol in normolipaemic and hyperlipidaemic obese subjects. Droździk, M; Gawrońska-Szklarz, B; Jaroszynska, M; Pawlik, A; Sterna, R; Wójcicki, J, 2003) | 0.83 |
" Pharmacokinetic parameters of the drugs were calculated using a noncompartmental open model." | ( Comparative pharmacokinetics of propranolol and atenolol in primary hyperlipidemia. Droździk, M; Gawrońska-Szklarz, B; Sterna, R; Sulzyc-Bielicka, V; Telatyńska, B; Wójcicki, J, ) | 0.41 |
" Pharmacokinetic parameters were calculated according to the noncompartmental open model." | ( [Pharmacokinetic comparison of propranolol and atenolol in people with primary hypertension]. Telatyńska-Smieszek, B, 2002) | 0.6 |
" A comparison is also presented between several methods based on animal pharmacokinetic data, using the same set of proprietary compounds, and it lends further support for the use of this method, as opposed to methods that require the gathering of pharmacokinetic data in laboratory animals." | ( Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics. Gao, F; Lombardo, F; Obach, RS; Shalaeva, MY, 2004) | 0.32 |
" In the light of the results obtained, the following conclusions were drawn: 1) hyperlipidemia affects pharmacodynamic properties of lipophilic propranolol and hydrophilic atenolol, 2) a modification of the drug dosage in hyperlipidemia is warranted." | ( [Effect of hyperlipidemia on pharmacodynamics of propranolol and atenolol]. Droździk, M; Gawrońska-Szklarz, B; Sterna, R; Sulzyc-Bielicka, V; Telatyńska-Smieszek, B; Wójcicki, J, 2004) | 0.78 |
"The chimpanzee (CHP) was evaluated as a pharmacokinetic model for humans (HUMs) using propranolol, verapamil, theophylline, and 12 proprietary compounds." | ( The chimpanzee (Pan troglodytes) as a pharmacokinetic model for selection of drug candidates: model characterization and application. Bai, SA; Christ, DD; Diamond, S; Grace, JE; Grossman, SJ; He, K; Qian, M; Wong, H; Wright, MR; Yeleswaram, K, 2004) | 0.55 |
" In vivo pharmacokinetic and in vitro metabolic studies were conducted using metoprolol and propranolol, which show substantial and marginal polymorphisms in humans, respectively." | ( Pharmacokinetics and metabolism of metoprolol and propranolol in the female DA and female Wistar rat: the female DA rat is not always an animal model for poor metabolizers of CYP2D6. Iwaki, M; Komura, H, 2005) | 0.8 |
"Human pharmacokinetic parameters are often predicted prior to clinical study from in vivo preclinical pharmacokinetic data." | ( Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure. Jolivette, LJ; Ward, KW, 2005) | 0.33 |
" Kinetic parameters were derived from a two-phase physiologically based organ pharmacokinetic model." | ( Hepatic pharmacokinetics of propranolol in rats with adjuvant-induced systemic inflammation. Chang, P; Crawford, DH; Fletcher, L; Hung, DY; Roberts, MS; Siebert, GA; Whitehouse, MW, 2006) | 0.63 |
" In vitro kinetics and in vivo pharmacokinetic profiles after oral administration of timolol, metoprolol, and propranolol, were investigated in rats using the depletion assay." | ( Application of substrate depletion assay for early prediction of nonlinear pharmacokinetics in drug discovery: assessment of nonlinearity of metoprolol, timolol, and propranolol. Iwaki, M; Kawase, A; Komura, H, 2005) | 0.74 |
" Using the physiologically based pharmacokinetic (PBPK) model incorporating the obtained metabolic parameters, the plasma kinetics of propranolol was well correlated with reported values, and then used to analyze the effect of hepatic first-pass metabolism on propranolol plasma pharmacokinetics in clinical doses." | ( Analysis of hepatic metabolism affecting pharmacokinetics of propranolol in humans. Honbo, A; Iga, K; Kiriyama, A, 2008) | 0.79 |
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data." | ( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds. Lombardo, F; Obach, RS; Waters, NJ, 2008) | 0.35 |
" Comparative pharmacokinetic-pharmacodynamic studies with four beta blockers were performed in conscious rats, using heart rate under isoprenaline-induced tachycardia as a pharmacodynamic endpoint." | ( Influence of plasma protein binding on pharmacodynamics: Estimation of in vivo receptor affinities of beta blockers using a new mechanism-based PK-PD modelling approach. Boralli, VB; Danhof, M; de Lange, EC; Freijer, J; Krekels, EH; Slijkerman, P; van Steeg, TJ, 2009) | 0.35 |
"African green monkeys (vervets) have been proposed as an alternate species that might allow improved access and provide high-quality pharmacokinetic results comparable with other primates." | ( Exploration of the African green monkey as a preclinical pharmacokinetic model: oral pharmacokinetic parameters and drug-drug interactions. Bhadresa, S; Coon, DJ; Lawrence, MS; Magiera, D; Struharik, M; Ward, KW, 2009) | 0.35 |
" The pharmacokinetic parameters were estimated using previously developed barrier-limited and space-distributed models." | ( Liver fibrosis impairs hepatic pharmacokinetics of liver transplant drugs in the rat model. Asadian, P; Crawford, DH; Fletcher, LM; Khlentzos, AM; Li, P; Liu, X; Roberts, MS; Robertson, TA; Thorling, CA; Zou, YH, 2010) | 0.36 |
" Studies were undertaken using an in situ-perfused rat liver and multiple indicator dilution, and outflow data were analyzed with a physiologically based organ pharmacokinetic model." | ( Hepatic pharmacokinetics of cationic drugs in a high-fat emulsion-induced rat model of nonalcoholic steatohepatitis. Crawford, DH; Fletcher, LM; Li, P; Roberts, MS; Robertson, TA; Thorling, CA; Zhang, Q, 2011) | 0.37 |
"The aim of this study was to investigate the effect of rectal ozone on portal vein oxygenation and the pharmacokinetic changes of propranolol in patients with liver cirrhosis." | ( The effect of rectal ozone on the portal vein oxygenation and pharmacokinetics of propranolol in liver cirrhosis (a preliminary human study). Fouad, EA; Kotb, HI; Zaky, S, 2011) | 0.8 |
" There was a decrease in the elimination half-life and mean residence time." | ( The effect of rectal ozone on the portal vein oxygenation and pharmacokinetics of propranolol in liver cirrhosis (a preliminary human study). Fouad, EA; Kotb, HI; Zaky, S, 2011) | 0.59 |
" Pharmacodynamic data deal with questions such as "Does a patient respond to a particular drug dose or not," or "Does a drug cause the same effects at the same time in the same subject or not." | ( Fuzzy modeling, a novel approach to studying pharmacodynamics. Cleophas, EP; Cleophas, TJ, ) | 0.13 |
" Other potential applications include the generation of pharmacokinetic profiles from the reduced sample volumes obtained from serially bled small rodent studies, or the facilitation of analysis of limited-volume samples from neurological studies." | ( Addressing the challenge of limited sample volumes in in vitro studies with capillary-scale microfluidic LC-MS/MS. Nicholson, JK; Plumb, RS; Rainville, PD; Smith, NW; Wilson, ID, 2011) | 0.37 |
" Despite high metabolic stability, pharmacokinetic evaluation revealed poor mice exposure; therefore, a second phase of optimization was required." | ( Ethionamide boosters. 2. Combining bioisosteric replacement and structure-based drug design to solve pharmacokinetic issues in a series of potent 1,2,4-oxadiazole EthR inhibitors. Baulard, AR; Blondiaux, N; Brodin, P; Christophe, T; Déprez, B; Desroses, M; Flament, MP; Flipo, M; Jeon, HK; Lecat-Guillet, N; Leroux, F; Locht, C; Mathys, V; Piveteau, C; Siepmann, J; Soror, SH; Villemagne, B; Villeret, V; Willand, N; Wintjens, R; Wohlkönig, A, 2012) | 0.38 |
" Hepatic pharmacokinetic modelling was performed with a two-phase physiologically-based organ pharmacokinetic model with the vascular space and dispersion evaluated with the MID technique." | ( Hepatocellular necrosis, fibrosis and microsomal activity determine the hepatic pharmacokinetics of basic drugs in right-heart-failure-induced liver damage. Crawford, DH; Fletcher, LM; Li, P; Roberts, MS; Robertson, TA; Weiss, M; Zhang, Q, 2012) | 0.38 |
" Hepatic pharmacokinetic analysis showed that both the CL int and PS were significantly decreased in the RHF rat livers." | ( Hepatocellular necrosis, fibrosis and microsomal activity determine the hepatic pharmacokinetics of basic drugs in right-heart-failure-induced liver damage. Crawford, DH; Fletcher, LM; Li, P; Roberts, MS; Robertson, TA; Weiss, M; Zhang, Q, 2012) | 0.38 |
"This review aims to analyze pharmacokinetic profile, plasma level variations so as the metabolism, interactions and possible relation to clinical effect of several drugs which are used primarily as anxiolytics." | ( Understanding the pharmacokinetics of anxiolytic drugs. Altamura, AC; Bareggi, S; Maffini, M; Mauri, MC; Moliterno, D; Paletta, S, 2013) | 0.39 |
"There is a need for a more balanced assessment of the benefits and risks associated with benzodiazepine use, particularly considering pharmacokinetic profile of the drugs to ensure that patients, who would truly benefit from these agents, are not denied appropriate treatment." | ( Understanding the pharmacokinetics of anxiolytic drugs. Altamura, AC; Bareggi, S; Maffini, M; Mauri, MC; Moliterno, D; Paletta, S, 2013) | 0.39 |
" The main objectives of this study were to (1) compare the plasma propranolol concentrations (Cp-prop) following sublingual administration of a specially buffered formulation (Promptol™) to that following oral administration of Inderal(®) and (2) evaluate the utility of a special pharmacokinetic model in describing the Cp-prop following sublingual administration." | ( Clinical pharmacokinetics of buffered propranolol sublingual tablet (Promptol™)-application of a new "physiologically based" model to assess absorption and disposition. Bolger, MB; Chow, MS; Lee, BT; Tomlinson, B; Wang, Y; Wang, Z; Zuo, Z, 2013) | 0.9 |
" Pharmacokinetic and pharmacodynamic changes depend on the nature and degree of hepatic impairment and on the characteristics of the dosed drug." | ( [Effect of liver cirrhosis on pharmacokinetics and pharmacodynamics of drugs]. Perlík, F, 2013) | 0.39 |
"The aim of this study was to present a deductive compartment pharmacokinetic (PK) model to predict the concentration profiles of drugs in plasma and peritoneal fluid in peritoneal dialysis (PD) rats." | ( Effects of peritoneal dialysis on pharmacotherapy: a deductive pharmacokinetic-model approach to predict drug concentration profiles in plasma and peritoneal fluid. Aiba, T; Horiuchi, M; Kurosaki, Y; Moriyama, S; Takahata, Y, 2014) | 0.4 |
"The main pharmacokinetic area under concentration-time curve (AUC), mean retention time (MRT), half-life (t1/2) and peak plasma concentration (Cmax) of propranolol were increased by 442." | ( [Effect of acute exposure to high altitude on the pharmacokinetics of propranolol]. Hao, Y; Jia, Z; Li, W; Wang, R; Wang, Y; Xie, H; Zhang, J, 2013) | 0.82 |
" Simulations of carbamazepine dosing regimen based on the pharmacokinetic parameters of this patient were performed to allow individualization of drug therapy." | ( Slow carbamazepine clearance in a nonadherent Malay woman with epilepsy and thyrotoxicosis. Hui-Ping Khor, A; Lim, KS; Lo, YL; Ng, CC; Yeap, LL, 2014) | 0.4 |
"8-fold increase in volume of distribution and a 3-fold increase in the elimination half-life (mean ± SEM: 641±100 vs." | ( A study of the relationship between serum bile acids and propranolol pharmacokinetics and pharmacodynamics in patients with liver cirrhosis and in healthy controls. Beuers, U; Buylaert, M; Drewe, J; Haschke, M; Krähenbühl, S; Taegtmeyer, AB; Tchambaz, L; Tschöpl, M, 2014) | 0.65 |
" Compared with the rats exposed to normal altitude, the rats with acute exposure to high altitude showed significant alterations in the pharmacokinetic parameters of the drugs, shown by increased Cmax and AUC, prolonged t1/2 and MRT, and lowered Clz/F of propranolol, and by increased Tmax and prolonged t1/2 and MRT of metoprolol without obvious changes of the parameters of the compartmental model." | ( [Effect of acute exposure to high altitude on pharmacokinetics of propranolol and metoprolol in rats]. Jia, Z; Li, W; Wang, R; Xie, H; Yin, Q; Zhang, J, 2014) | 0.82 |
" These results were confirmed by an in vivo pharmacokinetic study of oral administered fexofenadine (10mg/kg) in rats." | ( Effect of diosmin on the intestinal absorption and pharmacokinetics of fexofenadine in rats. Bedada, SK; Neerati, P, 2015) | 0.42 |
" Though P-gp-mediated efflux may contribute to the limited brain penetration of etamicastat, the low permeability along with the pharmacokinetic properties of etamicastat may be perceived as the main contributors for its peripheral selectivity, which is advantageous for a cardiovascular drug candidate." | ( Role of P-glycoprotein and permeability upon the brain distribution and pharmacodynamics of etamicastat: a comparison with nepicastat. Bonifácio, MJ; Fernandes-Lopes, C; Igreja, B; Loureiro, AI; Pires, N; Soares-da-Silva, P; Wright, LC, 2015) | 0.42 |
" Pharmacodynamic evaluations included maximum change from baseline in time-matched hourly average heart rate (Emax HR) and mean arterial blood pressure (Emax MABP) over 24 hours postdose, change from baseline in PR intervals, cardiac rhythm, and forced expiratory volume in 1 second (FEV1)." | ( Pharmacokinetic and pharmacodynamic interaction of siponimod (BAF312) and propranolol in healthy subjects. Biswal, S; Legangneux, E; Marbury, TC; Pal, P; Perry, R; Polus, F; Veldandi, UK, 2015) | 0.65 |
" The pharmacokinetic parameters for topiramate, diltiazem (and active metabolites, desacetyldiltiazem [DEA], N-demethyl diltiazem [DEM]), hydrochlorothiazide, and propranolol (and its active metabolite) were assessed at steady state." | ( Pharmacokinetic interactions between topiramate and diltiazem, hydrochlorothiazide, or propranolol. Curtin, CR; Ford, L; Heald, D; Manitpisitkul, P; Shalayda, K; Wang, SS, 2014) | 0.82 |
" A comprehensive and systematic review of the literature for the summarization of pharmacokinetic parameters would be effective to explore the new safe uses of propranolol in different scenarios, without exposing humans and using virtual-human modeling approaches." | ( Clinical Pharmacokinetics of Propranolol Hydrochloride: A Review. Ahmed, N; Kalam, MN; Rasool, MF; Rehman, AU, 2020) | 1.05 |
"Clinical pharmacokinetic studies on propranolol were screened using Medline and Google Scholar databases." | ( Clinical Pharmacokinetics of Propranolol Hydrochloride: A Review. Ahmed, N; Kalam, MN; Rasool, MF; Rehman, AU, 2020) | 1.12 |
" Propranolol is a substrate of CYP2D6, CYP1A2 and CYP2C19, retaining potential pharmacokinetic interactions with co-administered drugs." | ( Clinical Pharmacokinetics of Propranolol Hydrochloride: A Review. Ahmed, N; Kalam, MN; Rasool, MF; Rehman, AU, 2020) | 1.76 |
"Physiochemical and pooled pharmacokinetic parameters of propranolol are beneficial to establish physiologically based pharmacokinetic modeling among the diseased population." | ( Clinical Pharmacokinetics of Propranolol Hydrochloride: A Review. Ahmed, N; Kalam, MN; Rasool, MF; Rehman, AU, 2020) | 1.1 |
"In traditional pharmacokinetic models, blood flow or liquid transit is often expressed as first-order kinetics." | ( Preliminary Flow Modeling by Hybrid Automata Alternating Continuous Reaction and Discrete Transit for Pharmacokinetics. Koyama, S, 2021) | 0.62 |
" A publication reported a patient treated with HDI with plasma insulin concentrations >1000 µU/mL and elimination half-life 10-18 h requiring intravenous glucose replacement for >5 days." | ( Variability in insulin pharmacokinetics following high-dose insulin therapy. Haber, PS; Hughes, HK; Jones, GRD; Roberts, DM, 2022) | 0.72 |
" This pharmacokinetic variability impacts on the severity and duration of treatable hypoglycemia post-HDI." | ( Variability in insulin pharmacokinetics following high-dose insulin therapy. Haber, PS; Hughes, HK; Jones, GRD; Roberts, DM, 2022) | 0.72 |
" Here, we investigated the roles of Cyp1a2 and Cyp2d on DLX pharmacokinetic profile and tissue distribution using a Cyp1a2 knockout (Cyp1a2-KO) mouse model together with a Cyp2d inhibitor (propranolol)." | ( The roles of Cyp1a2 and Cyp2d in pharmacokinetic profiles of serotonin and norepinephrine reuptake inhibitor duloxetine and its metabolites in mice. Barzi, M; Bissig, KD; Boyd, SR; Hakenjos, JM; Li, F; MacKenzie, KR; Qin, X; Xie, C; Young, DW, 2023) | 1.1 |
" Previous research in other lipophilic drugs shows a trend to increase the volume of distribution and half-life in obese compared to ideal weight individuals." | ( A comparative evaluation of propranolol pharmacokinetics in obese versus ideal weight individuals: A blueprint towards a personalised medicine. Bertoldi, A; De Rubis, G; Dua, K; El Mekkawi, Z; Ho, A; Kakuzada, L; Mortlock, R; Nesci, I; Pont, L; Smith, V; Williams, K, 2023) | 1.2 |
"A physiologically based pharmacokinetic (PBPK) model is developed that focuses on the kinetic parameters of drug association and dissociation with albumin, alpha-1 acid glycoprotein (AGP), and brain tissue proteins, as well as drug permeability at the blood-brain barrier, drug metabolism, and brain blood flow." | ( Physiologically Based Pharmacokinetic Model of Brain Delivery of Plasma Protein Bound Drugs. Pardridge, WM, 2023) | 0.91 |
Niludipine, either alone or combined with propranolol and penfluzide, is effective in the treatment of patients with essential hypertension. This study demonstrates that autonomic nervous system dysfunction occurs and is responsible for the elevated BMR in elderly cancer patients.
Pharmacokinetic studies of the optimised Terminalia catappa formulation and a commercial product (Ciplar LA 80) showed a significant improvement in the bioavailability. The only known interaction is with propranolol, which reduces by one-third theBioavailability of enalapril.
Excerpt | Reference | Relevance |
---|---|---|
" dl-Timolol maleate is also extremely well absorbed when given orally, being then about 10 times more active than propranolol." | ( Timolol maleate, a new beta-adrenergic receptor blocking agent. Hall, RA; Robson, RD; Share, NN, 1975) | 0.46 |
" The decrease in the DR of T4 suggests a reduction in the bioavailability of L-T4 during propranolol, possibly due to a decrease in intestinal absorption." | ( Effect of propranolol on extrathyroidal metabolism of thyroxine and 3,3',5-triiodothyronine evaluated by noncompartmental kinetics. Faber, J; Friis, T; Kirkegaard, C; Lumholtz, IB; Siersbaek-Nielsen, K, 1978) | 0.88 |
" Our object was to assess long-term clinical efficacy, kinetics (acute and chronic), and bioavailability of minoxidil in chronic renal insufficiency." | ( Long-term clinical effects, bioavailability, and kinetics of minoxidil in relation to renal function. Affrime, M; Busby, P; Kim, KE; Lowenthal, DT; Martinez, EW; Mutterperl, R; Onesti, G; Shirk, J; Swartz, C, 1978) | 0.26 |
" These results demonstrate a significantly lower oral bioavailability of (-)- as compared to (+)-propranolol in the dog, which appears to be associated with stereoselective presystemic glucuronidation of (-)-propranolol." | ( Stereoselective oral bioavailability of (+/-)-propranolol in the dog. A GC-MS study using a stable isotope technique. Walle, T; Walle, UK, 1979) | 0.74 |
" Net water absorption rate was largely unaffected by intestinal vasodilatation." | ( The effect of vasodilatation and sympathetic nerve activation on net water absorption in the cat's small intestine. Brunsson, I; Eklund, S; Jodal, M; Lundgren, O; Sjövall, H, 1979) | 0.26 |
" CV-705 was well absorbed through the digestive tract." | ( [Vasodilator action of (+/-)-1-(3, 4, 5-trimethoxybenzyl)-6-hydroxy-1, 2, 3, 4-tetrahydroisoquinoline hydrochloride (CV-705) in anesthetized dogs (author's transl)]. Ikezawa, K; Kiyomoto, A; Nagao, T; Nakajima, H; Sato, M, 1977) | 0.26 |
" 3 Gastric emptying has some influence on the time of peak plasma propranolol concentrations but individual variation in its bioavailability is determined mainly by first-pass metabolism in the liver." | ( Contribution of individual differences in gastric emptying to variability in plasma propranolol concentrations. Castleden, CM; George, CF; Short, MD, 1978) | 0.72 |
" A direct estimate of bioavailability was also possible and was found to be increased at steady-state compared with a single oral dose." | ( Direct measurement of propranolol bioavailability during accumulation to steady-state. Belcher, S; Carr, K; Shand, DG; Vestal, RE; Wilkinson, GR; Wood, AJ, 1978) | 0.57 |
"The possible influence of food intake on the bioavailability of one nonselective and one cardioselective beta adrenoceptor antagonist, propranolol and metoprolol, was examined by serial determinations of the drug concentrations in blood of healthy subjects, taking single doses of the drugs both on an empty stomach and together with a standardized breakfast." | ( Enhancement of the bioavailability of propranolol and metoprolol by food. Danielson, K; Melander, A; Scherstén, B; Wåhlin, E, 1977) | 0.73 |
" A comparison of beta-adrenoreceptor blocking activity after oral and intravenous administration provides information on the bioavailability of these drugs." | ( Experiments with pindolol (Visken) in healthy volunteers. Aellig, WH, 1977) | 0.26 |
" The bioavailability of tablets and a solution of propranolol was compared with a crossover design by obtaining plasma samples at the end of the dosage interval during chronic oral administration of various doses." | ( Disposition of propoxyphene and propranolol in children. Atwood, GF; Shand, DG; Wilson, JT, 1976) | 0.79 |
" Analysis of the results of the propranolol study suggests that an increase in the rate of absorption combined with saturation of first pass extraction may account for the increased plasma concentrations of unchanged propranolol found in coeliac disease." | ( Absorption of propranolol and practolol in Coeliac disease. Kaye, CM; Parsons, RL; Raymond, K; Trounce, JR; Turner, P, 1976) | 0.9 |
"The enantioselective oral bioavailability of propranolol (PL) from 0-isovaleryl-PL was determined and compared with parent PL in beagle dogs." | ( Enantioselective oral bioavailability of 0-isovaleryl propranolol as a potential prodrug of propranolol. Imai, T; Otagiri, M; Shameem, M, 1992) | 0.79 |
"The effect of piperine on the bioavailability and pharmacokinetics of propranolol and theophylline has been examined in a crossover study." | ( Effect of piperine on bioavailability and pharmacokinetics of propranolol and theophylline in healthy volunteers. Bano, G; Bedi, KL; Johri, RK; Raina, RK; Sharma, SC; Zutshi, U, 1991) | 0.76 |
" Analysis of the area under the plasma concentration-time curve (AUC) for the two formulations indicate no significant difference of bioavailability despite a prolonged absorption time and maintenance of effective plasma concentration for the controlled release preparation." | ( Pharmacokinetic evaluation of conventional and controlled release dosage form of propranolol. Chattaraj, SC; Das, SK, 1990) | 0.51 |
" The maximum plasma concentration (Cmax), area under the plasma concentration-time curve from 0 to 10 h (AUC (0-10] and absorption rate constant (ka) were significantly greater after the morning dose." | ( Circadian influence on effect of propranolol on exercise-induced tachycardia in healthy subjects. Ebihara, A; Fujimura, A; Kajiyama, H; Kumagai, Y; Nakashima, H; Ohashi, K; Sugimoto, K, 1990) | 0.56 |
" These results indicate that the poor absorption of P from the gastrointestinal tract might be one of the factors causing the low bioavailability of P observed after administration of the sustained-release formulation." | ( Decreased absorption as a possible cause for the lower bioavailability of a sustained-release propranolol. Kashiwada, K; Ogata, H; Ohira, M; Someya, K; Takahashi, H; Warabioka, R, 1990) | 0.5 |
" administration of the beta blockers, no significant increase in area under the plasma drug concentration-time curve was observed for propranolol and metoprolol as a function of age, but for atenolol, a significant increase in area under the plasma drug concentration-time curve was seen in the 24-month-old rats, due to a decrease in renal function, as bioavailability of atenolol did not change in function of age." | ( Effect of aging on the pharmcokinetics of atenolol, metoprolol and propranolol in the rat. Belpaire, FM; Bogaert, MG; Chauvelot-Moachon, L; de Smet, F; Rosseel, MT; Vermeulen, AM; Vynckier, LJ, 1990) | 0.72 |
"Mechanisms and variations in the food-induced increase in the bioavailability of propranolol were assessed by single-dose (80 mg) studies in healthy volunteers who took the drug on an empty stomach, immediately after a protein-rich breakfast, and together with a carbohydrate-rich, protein-poor breakfast." | ( Mechanisms and variations in the food effect on propranolol bioavailability. Liedholm, H; Melander, A; Wåhlin-Boll, E, 1990) | 0.76 |
"The systemic bioavailability of propranolol was evaluated following oral and transdermal administration in rabbits." | ( Bioavailability of propranolol following oral and transdermal administration in rabbits. Chien, YW; Corbo, M; Liu, JC, 1990) | 0.89 |
"Moricizine is well absorbed after oral administration and undergoes extensive first-pass metabolism." | ( Clinical pharmacokinetics of moricizine. Barbey, JT; Schwartz, SL; Siddoway, LA; Woosley, RL, 1990) | 0.28 |
"5 liters/min) with an associated higher bioavailability (23." | ( Pharmacokinetics and metabolism of a 4'-methylthio derivative of propranolol in the dog. Bai, SA; Easterling, DE; Haney, CA; Peet, NP; Pruett, JK; Walle, T; Walle, UK; Wilson, MJ, ) | 0.37 |
"The pharmacokinetic and pharmacodynamic studies of four different brands of propranolol (Inderal, Ciplar, Corbeta and Propal) were carried out after single and multiple dosing on six normal adult healthy volunteers in a randomized crossover fashion to determine any inter-brand variations in bioavailability and pharmacodynamic effects." | ( Comparative pharmacokinetic and pharmacodynamic study of four different brands of propranolol in normal volunteers. Biswas, NR; Garg, SK; Kumar, N; Mukherjee, S; Sharma, PL, 1989) | 0.73 |
" Marked underestimation of oral bioavailability of propranolol in humans is consistent with the RBC "barrier" effect hypothesis." | ( Erythrocytes as barriers for drug elimination in the isolated rat liver. II. Propranolol. Chiou, WL; Lee, HJ, 1989) | 0.76 |
" The area under the concentration curve after oral administration (AUCpo) was increased by 62% and the plasma oral clearance (Clpo) was decreased by 39% by cimetidine treatment, whereas the bioavailability (F) was not changed." | ( The inhibitory effects of cimetidine on elimination and distribution of propranolol in rats. Asahina, M; Kawamata, Y; Kojo, M; Nishigaki, R; Shibasaki, S; Umemura, K, 1989) | 0.51 |
" Propranolol bioavailability correlated with the diameter of the portal vein and was dependent on the size of oesophageal varices and the presence of cavernous transformation of the portal vein." | ( [Usefulness of the evaluation of blood supply and mass of the liver for predicting the rate of pharmacokinetics of lidocaine, propranolol and phenazone]. Becker, A; Bołdys, H; Hartleb, M; Kloc, T; Mańczyk, I, 1989) | 1.39 |
" The results of this study indicate that the bioavailability of (S)-propranolol, as expressed by the mean area under the concentration-time curve (AUC) and maximum serum concentration, is lower after 40 mg of the optically pure drug than after the racemic drug." | ( Pharmacokinetic data of propranolol enantiomers in a comparative human study with (S)- and (R,S)-propranolol. Lindner, W; Rath, M; Semmelrock, HJ; Stoschitzky, K, 1989) | 0.82 |
"Reduced bioavailability (F) due to hepatic first-pass extraction of an oral dose (D) is a well-known pharmacokinetic phenomenon." | ( Saturable first-pass kinetics of propranolol. Haller, H; Keller, F; Kunzendorf, U; Offermann, G; Walz, G, 1989) | 0.56 |
" There was no difference in elimination half-life, bioavailability and mean residence time of propranolol between the two doses." | ( Pharmacokinetic and pharmacodynamic comparison of two doses of long acting propranolol (80 and 160 mg) in healthy subjects. Berlin, I; Cournot, A; Duchier, J; Flouvat, B; Robinet, D; Rossi, A; Sarmini, H, 1989) | 0.73 |
" Comparison of the AUC values showed that relative bioavailability of PPL was approx." | ( A comparative study of the pharmacokinetics of propranolol and its major metabolites in the rat after oral and vaginal administration. Buttar, HS; Qureshi, SA, 1989) | 0.53 |
" Nifedipine significantly enhanced propranolol bioavailability and Cmax, but reduced its tmax, in three out of six subjects who were also good absorbers of beta-blockers when taken alone." | ( Pharmacokinetic and pharmacodynamic interactions between nifedipine and propranolol or betaxolol. Canal, M; Carbon, C; Cascio, B; Domart, Y; Flouvat, B; Larribaud, J; Orofiamma, B; Roux, A; Vinceneux, P, 1986) | 0.78 |
" Betaxolol (Kerlon, 8) was found to exhibit an appropriate preclinical pharmacological and human pharmacokinetic profile (elevated oral bioavailability and prolonged plasma half-life) for the treatment of chronic cardiovascular diseases such as hypertension and angina." | ( Synthesis of a series of compounds related to betaxolol, a new beta 1-adrenoceptor antagonist with a pharmacological and pharmacokinetic profile optimized for the treatment of chronic cardiovascular diseases. Binet, JL; Cavero, IG; Lefèvre-Borg, F; Manoury, PM; Rousseau, J, 1987) | 0.27 |
"The influence of three diets (olestra, triglyceride oil, and water) on the bioavailability of a single dose of propranolol, diazepam, norethindrone, and ethinyl estradiol was evaluated." | ( Influence of absorbable and nonabsorbable lipids and lipidlike substances on drug bioavailability. Leff, RD; Roberts, RJ, 1989) | 0.49 |
"Two multiple dose crossover pharmacokinetic studies were carried out to determine the steady-state bioavailability of newly formulated generic propranolol HCl tablets relative to Inderal tablets." | ( Bioavailability of propranolol hydrochloride tablet formulations: application of multiple dose crossover studies. Daniel, JE; Eldon, MA; Kinkel, AW; Latts, JR, ) | 0.66 |
" The only known interaction is with propranolol, which reduces by one-third the bioavailability of enalapril." | ( [Clinical pharmacology of enalapril]. Giudicelli, JF, 1985) | 0.54 |
" The bioavailability of PL in the 5% PL Carbopol ointment with AZ was 13%." | ( The percutaneous absorption of propranolol and prediction of the plasma concentration. Ito, Y; Iwaki, M; Ogiso, T; Shintani, A, 1988) | 0.56 |
"The bioavailability of propranolol applied to the oral mucosa was examined in the hamster." | ( Application of propranolol to the keratinized oral mucosa: avoidance of first-pass elimination and the use of 1-dodecylazacycloheptan-2-one (Azone) as an absorption enhancer of bioadhesive film-dosage form. Kimura, T; Kitayama, M; Kurosaki, Y; Nakayama, T; Takatori, T, 1988) | 0.94 |
" The bioavailability of slow release formulations with a zero order release kinetic is lower than standard release formulations and related to the dissolution rate in vitro." | ( Drug input rate from the GI-tract. Michaelis-Menten kinetics and the bioavailability of slow release verapamil and nifedipine. Fischer, A; Köhne, H; Menke, G; Rietbrock, N; Woodcock, BG, 1988) | 0.27 |
" Systemic bioavailability of long acting propranolol is 30 to 50% less than that of the conventional formulation." | ( Pharmacokinetics of long acting propranolol. Implications for therapeutic use. Nace, GS; Wood, AJ, 1987) | 0.82 |
" The most likely explanation for increased bioavailability of nifedipine when coadministered with propranolol is by a reduction of the hepatic "first-pass" clearance, as a result of changes in hepatic blood flow." | ( Pharmacokinetic interaction between nifedipine and propranolol. Koren, G; Levy, M; Turetz-Abramovitch, M; Zylber-Katz, E, 1988) | 0.74 |
"The concomitant administration of hydralazine with metoprolol or propranolol substantially increases the oral bioavailability of these beta-blockers, presumably via reduction of the first-pass effect." | ( Effect of hydralazine on the elimination of antipyrine in the rat. Knowlton, PW; Svensson, CK; Ware, JA, 1987) | 0.51 |
" Haem arginate administered in high doses prior to oral propranolol did not alter the bioavailability of the latter." | ( Barbiturate and ethanol sleeping times and pharmacokinetics of propranolol in mice after intravenous administration of haem arginate. Tokola, O, 1987) | 0.76 |
" In contrast, acute uremia did elicit a change in the bioavailability of orally administered S(-)-propranolol." | ( Altered S(--)-propranolol disposition in bilateral ureter-ligated rats. Laganière, S; Shen, DD, 1987) | 0.85 |
"), pharmacokinetic studies demonstrate that the rectal route enables to obtain a bioavailability which is markedly higher by oral route, and plasma concentrations at a therapeutic level." | ( [Drug administration through the rectum: reliability, tolerance]. Cheymol, G, ) | 0.13 |
" These observations indicate that propranolol bioavailability in patients with hepatosplenic schistosomiasis is increased possibly due to reduced presystemic extraction." | ( Propranolol disposition in patients with hepatosplenic schistosomiasis. Ali, HM; Arbab, BM; Harron, DW; Homeida, MM, 1987) | 1.99 |
" 6 Within both subject groups the bioavailability of 80 mg twice daily of conventional propranolol tended to be greater than 160 mg LA once daily." | ( A comparative pharmacokinetic study of conventional propranolol and long acting preparation of propranolol in patients with cirrhosis and normal controls. Bastain, W; Hayes, JR; Larkin, KA; McAinsh, JA; Shanks, RG; Watson, RG, 1987) | 0.75 |
" The pharmacokinetic data are consistent with a decrease in intrinsic hepatic clearance of propranolol, leading to an increase in bioavailability at steady-state." | ( Propranolol pharmacokinetics and pharmacodynamics after single doses and at steady-state. Bottorff, MB; Lalonde, RL; Mirvis, DM; Pieper, JA; Straka, RJ, 1987) | 1.94 |
"The relationship between dose and bioavailability of propranolol was determined in 12 healthy male subjects." | ( Relationship between plasma propranolol concentration and dose in young, healthy volunteers. Brisson, J; Davis, G; Dey, M; Dvornik, D; Enever, R; Pray, K; Zaim, B, ) | 0.67 |
"The influence of concomitant food intake on the bioavailability and presystemic primary conjugation of propranolol (80 mg) was studied in 11 healthy women." | ( Concomitant food intake can increase the bioavailability of propranolol by transient inhibition of its presystemic primary conjugation. Liedholm, H; Melander, A, 1986) | 0.73 |
" A 12% decrease in oral clearance occurred with the meal but was not statistically significant (3717 +/- 185 ml/min, fasting; 3245 +/- 498 after meal), whereas bioavailability increased 67% (27." | ( Food effects on propranolol systemic and oral clearance: support for a blood flow hypothesis. Conradi, EC; Cowart, TD; Oexmann, MJ; Olanoff, LS; Walle, T; Walle, UK, 1986) | 0.62 |
" Bioavailability was estimated after rectal administration of each suppository in rabbits and compared with oral administration." | ( Pharmaceutical evaluation of hollow type suppositories. IV. Improvement of bioavailability of propranolol in rabbits after rectal administration. Baba, K; Matsumoto, M; Matsumoto, Y; Watanabe, Y, 1986) | 0.49 |
" The partial metabolic clearance approach adopted in this study may be useful in the investigation of factors influencing the oral bioavailability of propranolol." | ( Partial metabolic clearances as determinants of the oral bioavailability of propranolol. Conradi, EC; Olanoff, LS; Walle, T; Walle, UK, 1986) | 0.7 |
" The bioavailability of propranolol was reduced by prolonged physical exercise and plasma levels of propranolol were about 30% lower at the end of the exercise day than at the end of the rest day." | ( Influence of physical exercise on the pharmacokinetics of propranolol. Arends, BG; Böhm, RO; Rahn, KH; van Baak, MA; van Kemenade, JE, 1986) | 0.82 |
" Statistical analysis of the difference in the total AUCs indicates a significantly higher bioavailability of propranolol administered by the rectal route." | ( Plasma concentrations and bioavailability of propranolol by oral, rectal, and intravenous administration in man. Cárcamo, M; Cid, E; Lucchini, L; Mella, F; Monasterio, J, ) | 0.6 |
" This most likely explains the poor bioavailability of propranolol after a sustained-release formulation." | ( Propranolol: pooled Michaelis-Menten parameters and the effect of input rate on bioavailability. Wagner, JG, 1985) | 1.96 |
" Neither the bioavailability nor the beta-adrenoceptor blocking activity of propranolol was significantly changed by concurrent administration of aluminum hydroxide gel." | ( Lack of influence of aluminum hydroxide on the bioavailability and beta-adrenoceptor blocking activity of propranolol. Chiang, BN; Hong, CY; Hu, SC; Lin, SJ, 1985) | 0.71 |
" The present results suggest that 5-ISMN shows a high bioavailability and a potency comparable to ISDN, especially in the case of peroral administration." | ( [Effects of isosorbide 5-mononitrate on cardiovascular function. (I). Effects on the left ventricular system]. Kogi, K; Saito, T, 1985) | 0.27 |
" Orally administered NIP underwent extensive first-pass metabolism leading to low bioavailability (11%), despite of complete gastrointestinal absorption." | ( Pharmacokinetics of nipradilol (K-351), a new antihypertensive agent. II. Influence of the route of administration on bioavailability in dogs. Fujii, M; Ito, T; Kojima, J; Suzuki, J; Yoshimura, M, 1985) | 0.27 |
" The theory is given and the relationship between the area under the theoretical plasma level curve and the absorption rate constant is discussed." | ( Theoretical Michaelis-Menten elimination model for propranolol. Gay, MA; McAinsh, J, ) | 0.38 |
" Area under the curve estimates suggested that the bioavailability of the slow-release formulation following single-dose administration was about one-third that of the conventional preparation." | ( Combined high-performance liquid chromatographic procedure for measuring 4-hydroxypropranolol and propranolol in plasma: pharmacokinetic measurements following conventional and slow-release propranolol administration. Drummer, OH; Louis, WJ; McNeil, J; Pritchard, E, 1981) | 0.49 |
"Previous studies have demonstrated a larger oral bioavailability of (+)- as compared to (-)-propranolol in the dog." | ( Stereochemical composition of propranolol metabolites in the dog using stable isotope-labeled pseudoracemates. Bai, SA; Walle, T; Walle, UK; Wilson, MJ, ) | 0.64 |
" The absorption rate of the free forms of sulfanilamides was increased (significantly for sulfalen and sulfapyridazine)." | ( [Sulfanilamide absorption and acetylation in rats with experimental hyperlipidemia and cellular regulation of the process of acetylation]. Lubiankina, SV; Makarov, VA; Suetina, IV; Vasilenko, IuK; Vaskanian, VL, ) | 0.13 |
" The high hepatic extraction results in low systemic bioavailability (20%) after oral drug administration." | ( Clinical pharmacokinetics of verapamil. Blouin, RA; Hamann, SR; McAllister, RG, ) | 0.13 |
" These results suggest that ethanol could substantially increase the oral bioavailability of propranolol in humans." | ( Ethanol-induced inhibition of hepatic uptake of propranolol in perfused rat liver and in man. Carruthers, G; Dorian, P; Hamilton, C; Kaplan, HL; Khouw, V; Sellers, EM, 1984) | 0.74 |
" Chlorpromazine pretreatment significantly reduced (69%) the oral clearance of propranolol, resulting in significant increases in propranolol bioavailability (159%), and in the total beta-adrenergic blocking activity (111%) after the oral dose." | ( Effects of chlorpromazine on the disposition and beta-adrenergic blocking activity of propranolol in the dog. Abramson, FP; Bai, SA, 1984) | 0.72 |
" The composite observations of the stereochemistry of propranolol metabolism in man are consistent with stereoselective ring oxidation of (+)-propranolol, leading to a greater bioavailability of the pharmacologically more active (-)-propranolol and subsequent preferential side-chain oxidation and glucuronidation of this enantiomer." | ( Stereoselective ring oxidation of propranolol in man. Fagan, TC; Gaffney, TE; Walle, T; Walle, UK; Wilson, MJ, 1984) | 0.8 |
" There were no significant alterations in elimination half-life, clearance or apparent volume of distribution per kilogram antenatally compared with postnatally: bioavailability was also unchanged." | ( Pharmacokinetics of propranolol during pregnancy. Kinney, CD; McDevitt, DG; Murnaghan, GA; O'Hare, MF, 1984) | 0.59 |
"The aim of the study was to establish whether and how circadian rhythms alter the bioavailability of, and response of circulatory and ventilatory functions to 80 mg of propranolol given at four different test times." | ( Circadian bioavailability and some effects of propranolol in healthy subjects and in liver cirrhosis. Korczyńska-Wardecka, J; Markiewicz, A; Semenowicz-Siuda, K, 1984) | 0.72 |
" The bioavailability of (-)-propranolol (5." | ( Stereoselective increase in propranolol bioavailability during chronic dosing in the dog. Bai, SA; Walle, T; Walle, UK; Wilson, MJ, 1983) | 0.85 |
" Both anti-arrhythmic efficacy and bioavailability were compared to oral drug." | ( Sublingual absorption of the quaternary ammonium antiarrhythmic agent, UM-272. Lucchesi, BR; Patterson, E; Stetson, P, 1983) | 0.27 |
"Pharmacokinetic and bioavailability parameters of propranolol were estimated in 10 healthy adult subjects after single oral doses of two commercial tablet formulations of propranolol hydrochloride (2 X 40 mg)." | ( Pharmacokinetics of glucuronidation of propranolol following oral administration in humans. Cooper, JK; Ho-Ngoc, A; Loo, JC; McGilveray, IJ; Midha, KK; Roscoe, RM; Wilson, TW, ) | 0.65 |
"The influence of aluminium hydroxide and magnesium oxide on the oral bioavailability of quinidine, procainamide and propranolol in the dog was investigated." | ( Interaction of antacids with antiarrhythmics. V. Effect of aluminium hydroxide and magnesium oxide on the bioavailability of quinidine, procainamide and propranolol in dogs. Belpaire, F; Braeckman, P; Remon, JP; Van Severen, R, 1983) | 0.67 |
" Our data indicate that hydralazine increases propranolol bioavailability by its hemodynamic actions rather than by inhibition of its metabolism." | ( Mechanism by which hydralazine increases propranolol bioavailability. Schneck, DW; Vary, JE, 1984) | 0.79 |
"Recent experiments suggest that propranolol taken orally with a carbohydrate-rich meal increases its apparent bioavailability by reducing first-pass metabolism." | ( Effect of carbohydrates on estimated hepatic blood flow. Barde, SH; Lalka, D; Mauriello, PM; Middleton, E; Svensson, CK, 1984) | 0.55 |
" The bioavailability of Inderal LA was significantly lower than that of the other preparations." | ( Pharmacokinetic and pharmacodynamic studies with a new controlled-release formulation of propranolol in normal volunteers: a comparison with other commercially available formulations. Caravaggi, M; Crema, F; Frigo, GM; Gatti, G; Grimaldi, R; Lecchini, S; Perucca, E, 1984) | 0.49 |
" The therapeutic dose, clearance, extraction coefficient, bioavailability and half-life are the object of particular study." | ( [Pharmacokinetics of anti-arrhythmics. 2. Clinical applications]. Bricaud, H; Lévy, RH; Lévy, S, 1980) | 0.26 |
"It has been suggested that alteration in the apparent oral bioavailability of propranolol taken with food may be due to a transient increase in QH." | ( Effect of food on hepatic blood flow: implications in the "food effect" phenomenon. Barde, SH; Edwards, DJ; Foster, AC; Lalka, D; Lanc, RA; Mauriello, PM; Middleton, E; Svensson, CK, 1983) | 0.49 |
" Bioavailability of Bft was not altered following administration of the fixed combination." | ( Pharmacokinetics of bendroflumethiazide alone and in combination with propranolol and hydralazine. Mutschler, E; Schäfer-Korting, M, 1982) | 0.5 |
" 2 Buccal partitioning has proved useful in the examination of the mechanism of the propranolol/aluminium hydroxide absorption interaction and may also be a suitable in vivo bioavailability screening model for other drugs which can be partitioned in the buccal membranes." | ( The use of buccal partitioning as a model to examine the effects of aluminium hydroxide gel on the absorption of propranolol. McElnay, JC; Temple, DJ, 1982) | 0.7 |
"The elimination and bioavailability of two beta-blocking agents, propranolol and sotalol, were studied in 10 thyrotoxic patients, both before and after treatment with iodine-131." | ( Pharmacokinetics of propranolol and sotalol in hyperthyroidism. Anttila, M; Aro, A; Korhonen, T; Sundquist, H, 1982) | 0.83 |
"Experiments have been carried out in dogs and man to determine the effect of hydrochlorothiazide (HCT) on the pharmacokinetics of propranolol and to evaluate the bioavailability of two dosage forms containing both propranolol and HCT (40/25 and 80/25 mg, respectively)." | ( Biopharmaceutical characteristics of a new propranolol/hydrochlorothiazide tablet combination. Dubuc, J; Dvornik, D; Kraml, M; Lee, TY; Mullane, J; Patterson-Kreuscher, S; Perdue, H, ) | 0.6 |
" To compare the bioavailability and the elimination of propranolol in seven untreated coeliac patients and six normal subjects, plasma concentrations were measured after oral and intravenous propranolol." | ( Propranolol absorption in untreated coeliac disease. Rawlins, MD; Record, CO; Sandle, GI; Ward, A, 1982) | 1.95 |
"For drugs with a high hepatic clearance, bioavailability is low due to the so-called "first pass effect"." | ( Prediction of bioavailability for drugs with a high first-pass effect using oral clearance data. Eichelbaum, M; Gugler, R; Somogyi, A, 1982) | 0.26 |
"A relative bioavailability study of conventional tablet of propranolol hydrochloride was conducted in a group of 18 healthy volunteers employing the innovator's product as the reference tablet formation." | ( The relative bioavailability of a commercial propranolol hydrochloride tablet in man. Cooper, J; Joshi, NN; Midha, KK; Roscoe, R; Wilson, TW, ) | 0.63 |
" The absorption rate constant was decreased for folic acid in the coeliac group, but increased for propranolol." | ( Altered jejunal surface pH in coeliac disease: its effect on propranolol and folic acid absorption. Allan, RN; Bishop, H; Blair, JA; Kitis, G; Lucas, ML; Sargent, A; Schneider, RE, 1982) | 0.72 |
" Accordingly, the overall oral bioavailability was 27%." | ( Bioavailability of propranolol in the dog. Reo, JP; Sanders, TM; Tse, FL, 1980) | 0.59 |
" Bioavailability of the drug had increased by twice the values measured in physiologic liver blood flow; elimination half-life had doubled." | ( [Effect of portasystemic anastomoses in childhood on propranolol pharmacokinetics]. Buchali, K; Bürger, K; Cario, WR; Glende, M; Grossmann, P; Huth, M; Lampe, D; Rüstow, B; Zimmermann, HB, 1981) | 0.51 |
" Oral bioavailability of 1- and total propranolol averaged 40." | ( No stereoselective first-pass hepatic extraction of propranolol. Bobik, A; Jackman, GP; Jennings, GL; McLean, AJ, 1981) | 0.78 |
" The results show that the presence of both diuretics increased the intestinal absorption rate constant and the percentage diffused of propranolol hydrochloride." | ( In vitro detection of possible in vivo drug interactions. Part 1. The effect of hydrochlorothiazide and frusemide on the in vitro absorption characteristics of propranolol hydrochloride. Al-Janabi, II; Anber, SA; Mustafa, RM; Razzo, FN, 1981) | 0.66 |
" kg-1, bioavailability around 25%, with a mean terminal half-life of 6 hr." | ( Pharmacokinetics of propranolol. Borgström, L; Johansson, CG; Larsson, H; Lenander, R, 1981) | 0.59 |
" Ethanol caused a decrease in the rate of absorption and an increase in the rate of elimination of propranolol." | ( Effects of acute alcohol administration on propranolol absorption. Cady, WJ; Emery, JF; Grabowski, BS; Young, WW, 1980) | 0.74 |
" The bioavailability of the sustained-release formulation was identical to that of the intravenous administration." | ( Nasal absorption of propranolol from different dosage forms by rats and dogs. Bawarshi, R; Hirai, S; Hussain, A, 1980) | 0.58 |
"Propranolol (PL) bioavailability has been shown to increase substantially when it is administered with a protein-rich meal." | ( Interaction between propranolol and amino acids in the single-pass isolated, perfused rat liver. Semple, HA; Xia, F, 1995) | 2.06 |
" Nifedipine also significantly increased the AUC and Cmax of oral propranolol (15 mg/kg), whereas with BAY-K-8644 there was only a slight increase in the bioavailability of oral propranolol (15 mg/kg)." | ( Influences of the calcium antagonists nicardipine and nifedipine, and the calcium agonist BAY-K-8644, on the pharmacokinetics of propranolol in rats. Dupont, AG; Massart, DL; Schoors, DF; Vercruysse, I, 1993) | 0.73 |
" The relative bioavailability of propranolol was 104." | ( Chronic administration of nimodipine and propranolol in elderly normotensive subjects--an interaction study. Breuel, HP; Heine, PR; Kuhlmann, J; Mück, W; Niklaus, H; Schmage, N, 1995) | 0.84 |
"The effect of single oral dose of 1 gm gugulipid was studied on bioavailability of single oral dose of propranolol (40 mg) and diltiazem (60 mg) in 10 and 7 normal healthy male volunteers respectively." | ( Effect of gugulipid on bioavailability of diltiazem and propranolol. Dalvi, SS; Desai, NK; Gupta, KC; Kshirsagar, NA; Nayak, VK; Pohujani, SM, 1994) | 0.75 |
"The large increase in propranolol (PL) bioavailability when administered with food cannot be entirely explained by a transient increase in hepatic blood flow." | ( Propranolol disposition in the single-pass isolated, perfused rat liver in the presence and absence of insulin and glucagon. Semple, HA; Xia, F, ) | 1.89 |
" In comparison with healthy volunteers referred to in literature sources, plasma clearance was reduced to 49 +/- 28 ml/min, bioavailability was increased to 72 +/- 20%, and the volume of distribution was increased to 50 +/- 34 l, probably due, in part, to a weaker protein binding -85%--effect." | ( Hemodynamic and pharmacokinetic study of tertatolol in patients with alcoholic cirrhosis and portal hypertension. Brouard, R; Caillau, H; Calès, P; Crambes, O; Desmorat, H; Jung, L; Pascal, JP; Rocher, I; Urien, S; Vinel, JP, 1993) | 0.29 |
"We investigated in the isolated perfused rat liver (IPRL) whether product inhibition of metabolism contributes to the dose-dependent bioavailability of propranolol, a drug with a high, but saturable, hepatic first-pass effect." | ( Product inhibition and dose-dependent bioavailability of propranolol in the isolated perfused rat liver preparation. Ghabrial, H; Morgan, DJ; Nand, R; Smallwood, RA; Stead, CK, 1994) | 0.73 |
" The compounds examined ranged from well- to poorly-absorbed and included compounds absorbed by active and passive mechanisms." | ( Use of everted intestinal rings for in vitro examination of oral absorption potential. Fix, JA; Leppert, PS, 1994) | 0.29 |
"After 7 days of treatment with nisoldipine and propranolol, neither drug altered the other's bioavailability or elimination parameters, and propranolol did not change the area under the plasma concentration-time curve of nisoldipine's metabolite, N-9425." | ( Pharmacokinetic and pharmacodynamic interactions during multiple-dose administration of nisoldipine and propranolol. Leenen, FH; Ogilvie, RI; Shaw-Stiffel, TA; Walker, SE, 1994) | 0.76 |
" On the other hand, the oral clearance of diltiazem was significantly reduced by 51%, and its oral bioavailability was significantly increased by 48% during propranolol coadministration." | ( Effects of propranolol on the disposition and negative dromotropic activity of diltiazem in the dog during multiple dosing. Bai, SA; Lankford, SM; Maskasame, C, ) | 0.72 |
" As a result, protein (skim milk) intake slightly, but not significantly, increased the area under the plasma concentration-time curve (AUC) and bioavailability of PL, with a slight increase (16%) in hepatic blood flow, and enhanced PL metabolism to NLA." | ( Effect of food on propranolol oral clearance and a possible mechanism of this food effect. Hata, S; Iwaki, M; Kawafuchi, R; Ogiso, T; Tanino, T, 1994) | 0.62 |
" Studies investigating the effect of food on fluvastatin pharmacokinetics have demonstrated marked reductions in the rate of bioavailability (Cmax) of 40% to 60%." | ( Pharmacokinetics of fluvastatin and specific drug interactions. Hwang, DS; Jokubaitis, LA; Robinson, WT; Smith, HT; Troendle, AJ, 1993) | 0.29 |
"There is diurnal variation in the absorption rate of propranolol in younger subjects." | ( The effect of age on diurnal variation in the pharmacokinetics of propranolol in hypertensive subjects. Ebihara, A; Fujimura, A; Ohashi, K; Shiga, T; Tateishi, T, 1993) | 0.77 |
"Previous studies have shown that the absorption rate of a lipophilic, but not hydrophilic, agent is faster after the night dosage than after the morning dosage in nocturnal rodents." | ( Differences of chronopharmacokinetic profiles between propranolol and atenolol in hypertensive subjects. Ebihara, A; Fujimura, A; Ohashi, K; Shiga, T; Tateishi, T, 1993) | 0.53 |
"Several research groups have reported that in man the oral administration of propranolol with food leads to a marked increase (about 50 per cent) in the area under the plasma concentration-time curve (AUCpo) of this well absorbed and highly metabolized drug." | ( Pharmacokinetics of D-propranolol following oral, intra-arterial and intraportal administration: contrasting effects of oral glucose pretreatment. Chow, HH; Lalka, D, 1993) | 0.83 |
" Measurement of 24-h urinary-free iodide indicated that the bioavailability of potassium iodide delivered by retention enema was at least 40%." | ( Rectal administration of iodide and propylthiouracil in the treatment of thyroid storm. Balasubramanyam, A; Go, R; Yeung, SC, 1995) | 0.29 |
"The higher oral bioavailability (AUC and Cmax) of Pro in Chinese women is in part caused by their lower oral clearance and volume of distribution." | ( Sex differences in pharmacokinetics of oral propranolol in healthy Chinese volunteers. Chen, X; Xie, HG, 1995) | 0.55 |
" These results indicate that the enhancement of the bioavailability of propranolol by coadministration of nicardipine is dependent on the delivery rate of propranolol, suggesting that the interaction is mainly due to short-term haemodynamic effects of nicardipine leading to saturation of hepatic enzymes or functional shunting." | ( Increase in plasma propranolol caused by nicardipine is dependent on the delivery rate of propranolol. Dupont, AG; Massart, DL; Vercruysse, I, 1995) | 0.85 |
"Propranolol, a beta-adrenoceptor blocker, suffers from a high degree of first-pass metabolism resulting in very low bioavailability (< 10%) following administration with conventional oral formulations." | ( Carboxymethylcellulose-sodium based transdermal drug delivery system for propranolol. Krishna, R; Pandit, JK, 1996) | 1.97 |
" This reduction in 5-HT neuron firing activity is a 5-HT-mediated response, due to an increased bioavailability of the neurotransmitter in the biophase of somatodendritic 5-HT1A autoreceptors." | ( Autoregulatory properties of dorsal raphe 5-HT neurons: possible role of electrotonic coupling and 5-HT1D receptors in the rat brain. Blier, P; de Montigny, C; Piñeyro, G; Weiss, M, 1996) | 0.29 |
" A single-dose three-way crossover bioavailability study of two extended-release experimental formulations (80 mg), Inderal LA (80 mg) and an Inderal immediate-release dosage form (2 x 40 mg) was also conducted and a comparative analysis of pharmacokinetic parameters and the in-vitro release profiles was performed to assess in-vitro/in-vivo correlation." | ( Bioavailability and in-vitro/in-vivo correlation for propranolol hydrochloride extended-release bead products prepared using aqueous polymeric dispersions. Jambhekar, SS; Rekhi, GS, 1996) | 0.54 |
" Previous evidence suggests that the dose-dependent bioavailability of racemic propranolol may be partly due to product inhibition." | ( (S)-4'-hydroxypropranolol causes product inhibition and dose-dependent bioavailability of propranolol enantiomers in the isolated perfused rat liver and in rat liver microsomes. Ghabrial, H; Morgan, DJ; Nand, RA; Smallwood, RA, 1996) | 0.88 |
"05) increase in propranolol bioavailability caused by increased fractional absorption (57 +/- 28% vs 137 +/- 73%) and decreased total body clearance (58 +/- 27 ml/min/kg vs 30 +/- 19 ml/min/kg)." | ( Pharmacokinetics of propranolol in healthy cats during euthyroid and hyperthyroid states. Calvert, C; Ferguson, D; Jacobs, G; Sams, R; Whittem, T, 1997) | 0.97 |
" The overestimated plasma profile of propranolol suggests that the low bioavailability of propranolol is a result of first-pass metabolism by the intestine wall and the liver, because the calculated absolute absorption is almost perfect." | ( Prediction of the plasma concentration profiles of orally administered drugs in rats on the basis of gastrointestinal transit kinetics and absorbability. Haruta, S; Higaki, K; Kimura, T; Kurosaki, Y; Sawamoto, T, 1997) | 0.57 |
"The time course of pharmacodynamic effects allow to resolve bioavailability relevant pharmacokinetic information, provided simple assumptions can be made about their interrelation." | ( Inverse PK/PD: estimation and differentiation of bioavailability from effect kinetics--observations with beta-adrenoceptor antagonists. De Mey, C, 1997) | 0.3 |
"The bioavailability of propranolol (PL) after oral administration of ester-type prodrug was compared in rat and dog, and the possible reason for species difference was investigated." | ( Species differences in the disposition of propranolol prodrugs derived from hydrolase activity in intestinal mucosa. Aso, T; Imai, T; Otagiri, M; Yoshigae, Y, 1998) | 0.88 |
"The bioavailability of propranolol depends on the degree of liver metabolism." | ( Pharmacokinetics and pharmacodynamics of propranolol in hypertensive patients after sublingual administration: systemic availability. Avakian, SD; Donzella, H; Mansur, AP; Paula, RS; Ramires, JA; Santos, SR, 1998) | 0.88 |
" The clearance and oral bioavailability values for theophylline, atenolol, propranolol, warfarin, BMS-182874 and BMS-A were determined from continuous withdrawal or intermittent sampling experiments." | ( Continuous blood withdrawal as a rapid screening method for determining clearance of oral bioavailability in rats. Humphreys, WG; Morrison, RA; Obermeier, MT, 1998) | 0.53 |
" The method should prove useful in drug discovery screening, where the evaluation of large numbers of compounds for systemic clearance or oral bioavailability is often necessary." | ( Continuous blood withdrawal as a rapid screening method for determining clearance of oral bioavailability in rats. Humphreys, WG; Morrison, RA; Obermeier, MT, 1998) | 0.3 |
"The purpose of this study was to evaluate the effect of formulation and processing changes on the dissolution and bioavailability of propranolol hydrochloride tablets." | ( Identification of formulation and manufacturing variables that influence in vitro dissolution and in vivo bioavailability of propranolol hydrochloride tablets. Ashraf, M; Augsburger, LL; Eddington, ND; Fossler, MJ; Lesko, LJ; Leslie, JL; Rekhi, GS; Shah, VP, 1998) | 0.71 |
"271 h-1, the migration distance of the suppository in the rectum 4 h after administration was between 1 and 5 cm, and the bioavailability of propranolol was between 60." | ( Increased bioavailability of propranolol in rats by retaining thermally gelling liquid suppositories in the rectum. Chung, SJ; Kim, CK; Lee, MH; Ryu, JM, 1999) | 0.8 |
" The present study deals with the enhancement of the oral bioavailability of propranolol HCl by synthesising the amphiphathic prodrug, which tends to aggregate in supramolecular orientations." | ( Synthesis and characterisation of palymitoyl propanolol hydrochloride auto-lymphotrophs for oral administration. Jaitely, V; Kanaujia, P; Vyas, SP, 1999) | 0.53 |
"The aim of this study was to investigate the bioavailability of isosorbide mononitrate (IS-5MN) after oral administration of Monocard 20 mg-capsules, made in "Synteza" â Pharmaceutical-Chemical Company in Poznań." | ( [The evaluation of the bioavailability of isosorbide 5-mononitrate]. Drobnik, L; Dyderski, S; Szkutnik, D; Szymańska-Shawkat, E, 1999) | 0.3 |
"The bioavailability of IS-5MN after oral administration of Monocard 20 mg is the same as after oral administration of Effox 20 mg, whose clinical efficacy was tested before." | ( [The evaluation of the bioavailability of isosorbide 5-mononitrate]. Drobnik, L; Dyderski, S; Szkutnik, D; Szymańska-Shawkat, E, 1999) | 0.3 |
"To improve bioavailability and achieve a smoother plasma-concentration profile as compared with oral administration, a matrix-dispersion-type transdermal delivery system was designed and developed for propranolol using different ratios of hydroxypropylmethylcellulose (HPMC) K4M, K15M and K100M." | ( Controlled transdermal delivery of propranolol using HPMC matrices: design and in-vitro and in-vivo evaluation. Iyer, SS; Verma, PR, 2000) | 0.77 |
"The quantitative structure-bioavailability relationship of 232 structurally diverse drugs was studied to evaluate the feasibility of constructing a predictive model for the human oral bioavailability of prospective new medicinal agents." | ( QSAR model for drug human oral bioavailability. Topliss, JG; Yoshida, F, 2000) | 0.31 |
" The fraction absorbed of PPL was approximately 70% after oral administration, and the bioavailability varied among individual horses from 1 to 79% depending on the first pass metabolism." | ( Pharmacokinetics of propranolol and its metabolites in horses after intravenous or oral administration. Aramaki, S; Koizumi, T; Mori, M; Nakata, M; Shinohara, A, 2000) | 0.63 |
" Six new models were developed using a time-dependent absorption rate coefficient, ka(t), wherein the time dependency was varied to account for the dynamic processes such as changes in fluid absorption or secretion, in absorption surface area, and in motility with time, in the gastrointestinal tract." | ( Time-dependent oral absorption models. Amidon, GL; Higaki, K; Yamashita, S, 2001) | 0.31 |
" In contrast, both compounds were well absorbed in cynomolgus monkeys." | ( Permeability of lipophilic compounds in drug discovery using in-vitro human absorption model, Caco-2. Chen, K; Krishna, G; Lin, C; Nomeir, AA, 2001) | 0.31 |
"This paper describes a graphical model for simplifying in vitro absorption, metabolism, distribution, and elimination (ADME) data analysis through the estimation of oral bioavailability (%F) of drugs in humans and other species." | ( Graphical model for estimating oral bioavailability of drugs in humans and other species from their Caco-2 permeability and in vitro liver enzyme metabolic stability rates. Hwang, KK; Mandagere, AK; Thompson, TN, 2002) | 0.31 |
"Solubilizers are often used to enhance the bioavailability of drugs with poor aqueous solubility." | ( Common solubilizers to estimate the Caco-2 transport of poorly water-soluble drugs. Kobayashi, S; Kondo, H; Takahashi, Y; Watanabe, T; Yasuda, T; Yokohama, S, 2002) | 0.31 |
"Although thrombin has been extensively researched with many examples of potent and selective inhibitors, the key characteristics of oral bioavailability and long half-life have been elusive." | ( Oxyguanidines: application to non-peptidic phenyl-based thrombin inhibitors. Bone, R; Crysler, C; Dasgupta, M; Eisennagel, S; Fedde, C; Lu, T; Murphy, L; Soll, RM; Spurlino, J; Tomczuk, B; Wang, A, 2003) | 0.32 |
" Bioavailability was similar for both formulations of propranolol." | ( Pharmacokinetics of propranolol after single and multiple dosing with sustained release propranolol or propranolol CR (innopran XL) , a new chronotherapeutic formulation. Frishman, WH; Manowitz, N; Sica, D, ) | 0.7 |
"The mechanisms responsible for the increased bioavailability of propranolol in renal dysfunction were investigated in rats." | ( The increased intestinal absorption rate is responsible for the reduced hepatic first-pass extraction of propranolol in rats with cisplatin-induced renal dysfunction. Aiba, T; Hashimoto, Y; Mizukami, A; Okabe, H; Taguchi, M; Yasuhara, M, 2003) | 0.77 |
" This might result from an increased bioavailability of propranolol on day 1 and from marked sympathetic activity." | ( Alcohol withdrawal changes cardiovascular responses to propranolol challenge. Kähkönen, S, 2003) | 0.81 |
" The relative bioavailability of PPN was increased about fivefold to sixfold after transdermal administration as compared to oral delivery." | ( Comparative in vivo evaluation of propranolol hydrochloride after oral and transdermal administration in rabbits. Diwan, PV; Ramakrishna, S; Rao, PR; Reddy, MN, 2003) | 0.6 |
"This study evaluated the effects of batch size on the in vitro dissolution and the in vivo bioavailability of immediate release formulations of propranolol hydrochloride and metoprolol tartrate." | ( Scale-up effects on dissolution and bioavailability of propranolol hydrochloride and metoprolol tartrate tablet formulations. Augsburger, LL; Eddington, ND; Lesko, LJ; Rekhi, GS, 2000) | 0.75 |
" These experiments have allowed a more complete characterization of ketoconazole as a prototypic dual Pgp/CYP3A inhibitor and its use as a tool in a preclinical setting and further demonstrate the use of the monkey to investigate the role of Pgp/CYP3A in limiting the oral bioavailability of new drug candidates." | ( Development of an in vivo preclinical screen model to estimate absorption and first-pass hepatic extraction of xenobiotics. II. Use of ketoconazole to identify P-glycoprotein/CYP3A-limited bioavailability in the monkey. Azzarano, LM; Kehler, JR; McSurdy-Freed, JE; Morgan, JA; Proksch, JW; Smith, BR; Stelman, GJ; Ward, KW; Zeigler, KS, 2004) | 0.32 |
" Moreover, administration of the matrix-in-cylinder system resulted in a 4-fold increase in propranolol bioavailability when compared with a commercial sustained release formulation (Inderal)." | ( In vitro and in vivo evaluation of a matrix-in-cylinder system for sustained drug delivery. Gielen, I; Mehuys, E; Remon, JP; Van Bree, H; Vervaet, C, 2004) | 0.54 |
" Indinavir, a widely prescribed HIV protease inhibitor, suffer from bioavailability problems where involvement of P-glycoprotein mediated drug efflux may play a significant role." | ( Reversed-phase liquid chromatography with ultraviolet detection for simultaneous quantitation of indinavir and propranolol from ex-vivo rat intestinal permeability studies. Bansal, T; Kaul, CL; Panchagnula, R; Varma, MV, 2004) | 0.54 |
" Species differences were observed in the systemic clearance of theophylline (approximately 5-fold higher in CHPs), a low clearance compound, and the bioavailability of propranolol and verapamil (lower in CHPs), both high clearance compounds." | ( The chimpanzee (Pan troglodytes) as a pharmacokinetic model for selection of drug candidates: model characterization and application. Bai, SA; Christ, DD; Diamond, S; Grace, JE; Grossman, SJ; He, K; Qian, M; Wong, H; Wright, MR; Yeleswaram, K, 2004) | 0.52 |
"To investigate the mechanism responsible for the increased bioavailability of propranolol in bilateral ureter-ligated (BUL) rats, the intestinal absorption and hepatic extraction of propranolol and metoprolol were evaluated." | ( Intestinal absorption and hepatic extraction of propranolol and metoprolol in rats with bilateral ureteral ligation. Hashimoto, Y; Higashi, T; Ohta, T; Okabe, H, 2004) | 0.81 |
"The purpose of this study was to develop and validate a method for separately evaluating the roles of gastrointestinal absorption and hepatic extraction as barriers to oral bioavailability (BA)." | ( Evaluating barriers to bioavailability in vivo: validation of a technique for separately assessing gastrointestinal absorption and hepatic extraction. Aungst, B; Dobson, G; Hidalgo, I; Letendre, L; Scott, M, 2004) | 0.32 |
" Pharmacokinetic parameters including bioavailability were calculated for each compound for each route of administration." | ( Evaluating barriers to bioavailability in vivo: validation of a technique for separately assessing gastrointestinal absorption and hepatic extraction. Aungst, B; Dobson, G; Hidalgo, I; Letendre, L; Scott, M, 2004) | 0.32 |
" Antipyrine was highly bioavailable by all routes." | ( Evaluating barriers to bioavailability in vivo: validation of a technique for separately assessing gastrointestinal absorption and hepatic extraction. Aungst, B; Dobson, G; Hidalgo, I; Letendre, L; Scott, M, 2004) | 0.32 |
"To study the correlation between the absorption rate constants of beta-adrenoreceptor antagonists in rat small intestinal segments and their molecular structural parameters." | ( [Correlation between absorption rates of beta-adrenoreceptor antagonists in rat small intestine and their molecular structures]. Fu, XC; Sun, Q, 2005) | 0.33 |
"The absorption rate constants of beta-adrenoreceptor antagonists in rat jejunum or ileum were well linearly correlated with the sum of the net charges of all hydrogen atoms and the molecular volumes." | ( [Correlation between absorption rates of beta-adrenoreceptor antagonists in rat small intestine and their molecular structures]. Fu, XC; Sun, Q, 2005) | 0.33 |
"The absorption rate constants of beta-adrenoreceptor antagonists in rat small intestinal segments are mainly related with their lipophilicity,hydrogen-bonding potential and molecular size." | ( [Correlation between absorption rates of beta-adrenoreceptor antagonists in rat small intestine and their molecular structures]. Fu, XC; Sun, Q, 2005) | 0.33 |
" The relative bioavailability of two FDA approved (Orange Book AB rating) solid oral dosage forms of metoprolol and propranolol/hydrochlorothiazide (combination tablets) was evaluated in human volunteers under fed conditions using a two-way crossover design." | ( The effect of food on the relative bioavailability of rapidly dissolving immediate-release solid oral products containing highly soluble drugs. Asafu-Adjaye, E; Ciavarella, AB; Conner, DP; Faustino, PJ; Hussain, AS; Lesko, LJ; Mehta, MU; Parekh, A; Straughn, AB; Yang, Y; Yu, LX, ) | 0.34 |
"The bioavailability of propranolol from a matrix-in-cylinder system for sustained drug delivery, consisting of a hot-melt extruded ethylcellulose pipe surrounding a drug-containing HPMC-Gelucire 44/14 core, was determined." | ( Human bioavailability of propranolol from a matrix-in-cylinder system with a HPMC-Gelucire core. Augustijns, P; Korst, A; Mehuys, E; Mols, R; Porter, C; Remon, JP; Van Bortel, L; Vervaet, C, 2005) | 0.94 |
" The hypotensive effect of isosorbid dinitrate, commonly used as a vasodilatator, was weaker at the onset of AW, being associated with the decreased bioavailability of the drug." | ( Responses to cardiovascular drugs during alcohol withdrawal. Kähkönen, S, ) | 0.13 |
" The present study concludes that mucoadhesive buccal devices of PRH can be a good way to bypass the extensive hepatic first-pass metabolism and to improve the bioavailability of PRH." | ( Formulation, evaluation, and comparison of bilayered and multilayered mucoadhesive buccal devices of propranolol hydrochloride. Patel, MM; Patel, VM; Prajapati, BG, 2007) | 0.56 |
" Previously described THQ PFTIs had limitations of poor oral bioavailability and rapid clearance from the circulation of rodents." | ( Efficacy, pharmacokinetics, and metabolism of tetrahydroquinoline inhibitors of Plasmodium falciparum protein farnesyltransferase. Ankala, S; Barrett, LK; Bauer, KD; Bendale, P; Buckner, FS; Chakrabarti, D; Floyd, D; Gelb, MH; Hamilton, AD; Hornéy, C; Hucke, O; Lombardo, LJ; Nallan, L; Rivas, KL; Smart, BP; Strickland, C; Van Voorhis, WC; Verlinde, CL; Williams, DK; Yokoyama, K, 2007) | 0.34 |
" Additional mechanisms involving blockade of Ca2+ entry in the vascular smooth muscle and increase in NO bioavailability contributes to beneficial effects of long-term propranolol treatment." | ( Vascular effects of long-term propranolol administration after chronic nitric oxide blockade. Antunes, E; Claudino, MA; De Nucci, G; Priviero, FB; Teixeira, CE; Zanesco, A, 2007) | 0.82 |
" It can be concluded that the present buccal formulation can be an ideal system to improve the bioavailability of the drug by avoiding hepatic first-pass metabolism." | ( Effect of hydrophilic polymers on buccoadhesive Eudragit patches of propranolol hydrochloride using factorial design. Patel, MM; Patel, VM; Prajapati, BG, 2007) | 0.58 |
" On the other hand, the first-order absorption rate constant of propranolol did not affect AUC values." | ( Analysis of hepatic metabolism affecting pharmacokinetics of propranolol in humans. Honbo, A; Iga, K; Kiriyama, A, 2008) | 0.83 |
" These drugs also increased the bioavailability of CSA." | ( Comparative interaction of few antihypertensive drugs with cyclosporine-A in rats. Inamdar, MN; Kumar, NP; Venkataraman, BV, 2007) | 0.34 |
" Topotecan, an anti-cancer drug widely used in metastatic carcinoma, is a P-glycoprotein substrate having oral bioavailability of 30% with large inter-patient variability." | ( Concurrent determination of topotecan and model permeability markers (atenolol, antipyrine, propranolol and furosemide) by reversed phase liquid chromatography: utility in Caco-2 intestinal absorption studies. Bansal, T; Jaggi, M; Khar, RK; Mishra, G; Mukherjee, R; Singh, M; Talegaonkar, S, 2007) | 0.56 |
" The relative bioavailability for delayed-onset sustained-release tablet was 96." | ( Preparation and evaluation of a novel delayed-onset sustained-release system of propranolol hydrochloride. Chen, HZ; Fang, C; Feng, XM; Ren, Q; Rong, ZX; Shen, HF; Zhang, WZ, 2008) | 0.57 |
"The object of the study was to evaluate locust bean gum and chitosan in ratios of 2:3; 3:2 and 4:1 (F1, F2 and F3) as a mucoadhesive component in buccal tablets and to compare the bioavailability of a propranolol hydrochloride buccal tablet with the oral tablet in healthy human volunteers." | ( In vitro and in vivo evaluation of locust bean gum and chitosan combination as a carrier for buccal drug delivery. Ramakrishnan, A; Vasanthakumar, S; Vijayaraghavan, C, 2008) | 0.53 |
" The validated method was successfully employed for bioavailability study after oral administration of 10 mg of alfuzosin hydrochloride and 5mg of solifenacin succinate tablet formulations in eight healthy volunteers under fed condition." | ( Highly sensitive and rapid LC-ESI-MS/MS method for the simultaneous quantification of uroselective alpha1-blocker, alfuzosin and an antimuscarinic agent, solifenacin in human plasma. Jangid, AG; Mistri, HN; Pudage, A; Rathod, DM; Shrivastav, PS, 2008) | 0.35 |
"Amorphous solids and crystalline salts are both of interest as a means of improving the dissolution characteristics and apparent solubility of poorly water soluble active pharmaceutical ingredients which have low bioavailability in humans." | ( An investigation into the influence of counterion on the properties of some amorphous organic salts. Li, T; Remick, DM; Sanchez-Felix, MV; Taylor, LS; Towler, CS; Wikström, H, ) | 0.13 |
" Local BH(4) supplementation augments reflex and tyramine-induced VC in aged skin, suggesting that reduced BH(4) bioavailability may contribute to attenuated VC during whole-body cooling." | ( Local tetrahydrobiopterin administration augments cutaneous vasoconstriction in aged humans. Holowatz, LA; Kenney, WL; Lang, JA, 2009) | 0.35 |
" ISV was set at either 10% or 20% for clearance and either 20% or 50% for the absorption rate constant, K(a)." | ( Role of metabolites for drugs that undergo nonlinear first-pass effect: impact on bioequivalency assessment using single-dose simulations. Braddy, AC; Jackson, AJ, 2010) | 0.36 |
" The bioavailability of propranolol increases in presence of food." | ( Formulation and evaluation of gastroretentive drug delivery system of propranolol hydrochloride. Agavekar, AJ; Chabukswar, AR; Jagdale, SC; Kuchekar, BS; Pandya, SV, 2009) | 0.89 |
" The results indicated that all the sesquiterpenes are well absorbed mainly by the passive diffusion via the transcellular pathway and metabolism may be involved during the absorption of ICL, BSE and DML." | ( Intestinal permeability of sesquiterpenes in the caco-2 cell monolayer model. Wu, Q; Xu, W; Yang, XW; Zhang, LX; Zhang, P; Zhao, B; Zou, L, 2010) | 0.36 |
" Furthermore, current water quality monitoring does not differentiate between soluble and colloidal phases in water samples, hindering our understanding of the bioavailability and bioaccumulation of pharmaceuticals in aquatic organisms." | ( Colloids as a sink for certain pharmaceuticals in the aquatic environment. Maskaoui, K; Zhou, JL, 2010) | 0.36 |
" Such strong pharmaceutical/colloid interactions may provide a long-term storage of pharmaceuticals, hence, increasing their persistence while reducing their bioavailability in the environment." | ( Colloids as a sink for certain pharmaceuticals in the aquatic environment. Maskaoui, K; Zhou, JL, 2010) | 0.36 |
" As aquatic colloids are abundant, ubiquitous, and highly powerful sorbents, they are expected to influence the bioavailability and bioaccumulation of such chemicals by aquatic organisms." | ( Colloids as a sink for certain pharmaceuticals in the aquatic environment. Maskaoui, K; Zhou, JL, 2010) | 0.36 |
"Oral bioavailability (F) is a product of fraction absorbed (Fa), fraction escaping gut-wall elimination (Fg), and fraction escaping hepatic elimination (Fh)." | ( Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination. Chang, G; El-Kattan, A; Miller, HR; Obach, RS; Rotter, C; Steyn, SJ; Troutman, MD; Varma, MV, 2010) | 0.36 |
" The very low oral bioavailability indicates that intestinal metabolism of PPL is probably quite high." | ( Effect of recombinant porcine somatotropin (rpST) on drug disposition in swine. Howard, KD; Kawalek, JC, 2010) | 0.36 |
"The Biopharmaceutical Classification System (BCS) guidance issued by the FDA allows waivers for in vivo bioavailability and bioequivalence studies for immediate-release (IR) solid oral dosage forms only for BCS class I drugs." | ( The biowaiver extension for BCS class III drugs: the effect of dissolution rate on the bioequivalence of BCS class III immediate-release drugs predicted by computer simulation. Amidon, GL; Tsume, Y, 2010) | 0.36 |
" To show the importance of physicochemical properties, the classic QSAR and CoMFA of neonicotinoids and prediction of bioavailability of pesticides in terms of membrane permeability in comparison with drugs are described." | ( Importance of physicochemical properties for the design of new pesticides. Akamatsu, M, 2011) | 0.37 |
" longifolia, its bioavailability (AUC0-∞) decreased by 29% while C(max) was reduced by 42% and T(max) was significantly prolonged by almost 86%." | ( Modification of propranolol's bioavailability by Eurycoma longifolia water-based extract. Amrah, S; Gan, SH; Ismail, R; Ismail, Z; Salman, SA; Wahab, MS; Yuen, KH, 2010) | 0.71 |
" Optimized formulation PTSso and commercial formulation Ciplar LA 80 were subjected to bioavailability studies in healthy human volunteers by estimating pharmacokinetic parameters such as Cmax, Tmax, area under curve (AUC), elimination rate constant (Kel), biological half-life (t1/2) and mean residence time (MRT)." | ( Thermal sintering: a novel technique used in the design, optimization and biopharmaceutical evaluation of propranolol HCl gastric floating tablets. Battu, JR; Kolapalli, VR; Nali, SR; Songa, AS; Venkata Srikanth, M, 2014) | 0.62 |
" Cp-prop was higher at earlier times with 3-fold greater relative bioavailability following sublingual Promptol™ compared to that from oral Inderal(®)." | ( Clinical pharmacokinetics of buffered propranolol sublingual tablet (Promptol™)-application of a new "physiologically based" model to assess absorption and disposition. Bolger, MB; Chow, MS; Lee, BT; Tomlinson, B; Wang, Y; Wang, Z; Zuo, Z, 2013) | 0.66 |
" Combining of xanthone with piperazine moiety resulted in obtaining of compounds with increased bioavailability after oral administration." | ( Synthesis and evaluation of pharmacological properties of some new xanthone derivatives with piperazine moiety. Bojarski, AJ; Gunia, A; Marona, H; Pytka, K; Satała, G; Siwek, A; Szkaradek, N; Szneler, E; Waszkielewicz, AM, 2013) | 0.39 |
" Bioavailability of tetrahydrobiopterin (BH4), an essential cofactor for catecholamine synthesis, is reduced with aging." | ( Oral sapropterin augments reflex vasoconstriction in aged human skin through noradrenergic mechanisms. Alexander, LM; Kenney, WL; Stanhewicz, AE, 2013) | 0.39 |
" The compound was orally bioavailable and displayed good plasma and brain exposure in mice." | ( Substituted 2-phenylimidazopyridines: a new class of drug leads for human African trypanosomiasis. Brun, R; Buckner, FS; Chatterjee, AK; Creason, SA; Duster, NA; Gelb, MH; Gillespie, JR; Glynne, R; Hulverson, MA; McQueen, J; Molteni, V; Nagendar, P; Nagle, A; Norcross, NR; Ranade, RM; Supek, F; Tatipaka, HB; Wenzler, T, 2014) | 0.4 |
" Linear and nonlinear (quadratic, cubic, sigmoid functions) deconvolution based in vitro-in vivo correlation (IVIVC) models were developed using in vitro dissolution data and bioavailability profile." | ( Chronotherapeutic delivery of hydroxypropylmethylcellulose based mini-tablets: an in vitro-in vivo correlation. Biswas, N; Guha, A; Kuotsu, K; Sahoo, RK, 2014) | 0.4 |
"The main objectives of the study were to determine the exposure and bioavailability of oral propranolol and to investigate their associations with serum bile acid concentration in patients with liver cirrhosis and in healthy controls." | ( A study of the relationship between serum bile acids and propranolol pharmacokinetics and pharmacodynamics in patients with liver cirrhosis and in healthy controls. Beuers, U; Buylaert, M; Drewe, J; Haschke, M; Krähenbühl, S; Taegtmeyer, AB; Tchambaz, L; Tschöpl, M, 2014) | 0.87 |
"Diosmin is a natural flavone glycoside, a potent P-glycoprotein (P-gp) inhibitor in cultured cells and have the potential to alter the bioavailability of P-gp substrate drugs." | ( Effect of diosmin on the intestinal absorption and pharmacokinetics of fexofenadine in rats. Bedada, SK; Neerati, P, 2015) | 0.42 |
"Diosmin significantly enhanced the oral bioavailability of fexofenadine by the inhibition of P-gp mediated drug efflux during the intestinal absorption." | ( Effect of diosmin on the intestinal absorption and pharmacokinetics of fexofenadine in rats. Bedada, SK; Neerati, P, 2015) | 0.42 |
" Despite its lower bioavailability and higher clearance, as compared to nepicastat, etamicastat showed preferential distribution to peripheral tissues and high plasma free fraction (15." | ( Role of P-glycoprotein and permeability upon the brain distribution and pharmacodynamics of etamicastat: a comparison with nepicastat. Bonifácio, MJ; Fernandes-Lopes, C; Igreja, B; Loureiro, AI; Pires, N; Soares-da-Silva, P; Wright, LC, 2015) | 0.42 |
" Permeability correlated well with the extent of intramolecular hydrogen bonding observed in the solution structures determined in the low-dielectric solvent CDCl3, and one compound showed an oral bioavailability of 21% in rat." | ( Probing the Physicochemical Boundaries of Cell Permeability and Oral Bioavailability in Lipophilic Macrocycles Inspired by Natural Products. Bockus, AT; Gardner, JW; Glassey, E; Hewitt, WM; Hund, KC; Jacobson, MP; Kalgutkar, AS; Lexa, KW; Liras, S; Lokey, RS; Mathiowetz, AM; Price, DA; Pye, CR; Schwochert, JA, 2015) | 0.42 |
" Pharmacokinetic studies of the optimised Terminalia catappa formulation and a commercial product (Ciplar LA 80) carried out on healthy human volunteers showed a significant improvement in the bioavailability (132%) of propranolol HCl released from from the experimental Terminalia catappa formulations compared with Ciplar LA 80." | ( Formulation of Gastric Floating System Using Bio-Sourced Terminalia Catappa Gum and in vivo Evaluation. Meka, VS; Murthy Kolapalli, VR, 2016) | 0.62 |
" In addition, both benzazaborinine analogues showed excellent bioavailability and brain penetration following subcutaneous administration in a pharmacokinetic study in rats." | ( Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. Austin, N; Rombouts, FJ; Tovar, F; Trabanco, AA; Tresadern, G, 2015) | 0.65 |
" The bioavailability of IGF-1 at both mRNA and protein levels were measured by quantitative real-time PCR and Western blot respectively." | ( Decrease of the insulin-like growth factor-1 bioavailability in spontaneously hypertensive rats with erectile dysfunction. Cheng, SP; Huang, H; Huang, JB; Liu, RH; Mao, FJ; Pan, H; Sun, YL; Xiao, S; Zhong, GJ; Zhou, ZY, 2016) | 0.43 |
"This study aimed at improving the systemic bioavailability of propranolol-HCl by the design of transdermal drug delivery system based on chitosan nanoparticles dispersed into gels." | ( Transdermal delivery of propranolol hydrochloride through chitosan nanoparticles dispersed in mucoadhesive gel. Al-Kassas, R; Cheng, AE; Kim, AM; Liu, SSM; Wen, J; Yu, J, 2016) | 0.98 |
"Capsaicin is the main pungent principle present in chili peppers has been found to possess P-glycoprotein (P-gp) inhibition activity in vitro, which may have the potential to modulate bioavailability of P-gp substrates." | ( Capsaicin pretreatment enhanced the bioavailability of fexofenadine in rats by P-glycoprotein modulation: in vitro, in situ and in vivo evaluation. Appani, R; Bedada, SK; Boga, PK, 2017) | 0.46 |
"Capsaicin pretreatment significantly enhanced the intestinal absorption and bioavailability of fexofenadine in rats likely by inhibition of P-gp mediated cellular efflux, suggesting that the combined use of capsaicin with P-gp substrates may require close monitoring for potential drug interactions." | ( Capsaicin pretreatment enhanced the bioavailability of fexofenadine in rats by P-glycoprotein modulation: in vitro, in situ and in vivo evaluation. Appani, R; Bedada, SK; Boga, PK, 2017) | 0.46 |
" Thus, ionic interaction reduced the thermodynamic activity of PRO and mobility of AACOOH, which made PRO-AACOOH obtain a significant lower bioavailability (11." | ( A systemic evaluation of drug in acrylic pressure sensitive adhesive patch in vitro and in vivo: The roles of intermolecular interaction and adhesive mobility variation in drug controlled release. Fang, L; Li, S; Liu, C; Quan, P; Zhao, Y, 2017) | 0.46 |
" Pharmacokinetic experiments show oral bioavailability through gastric absorption." | ( Pharmacology and in vivo efficacy of pyridine-pyrimidine amides that inhibit microtubule polymerization. Cescon, DW; Hansen, MD; Hoj, JP; Siddiqui-Jain, A, 2018) | 0.48 |
"The bioavailability of pharmaceuticals is governed by their sorption in soils/sediments, as the retention processes determine their concentration in surface- and ground-water." | ( Combining sorption experiments and Time of Flight Secondary Ion Mass Spectrometry (ToF-SIMS) to study the adsorption of propranolol onto environmental solid matrices - Influence of copper(II). Berrier, E; Guillon, E; Nuns, N; Sayen, S; Smith, RM, 2018) | 0.69 |
" The aim of the present study was to clarify the effect of the changes in MC on in vivo drug absorption after nasal application, and to justify the pharmacokinetic model to which the MC parameter was introduced, to enable prediction of bioavailability after intranasal administration." | ( Quantitative Estimation of the Effect of Nasal Mucociliary Function on in Vivo Absorption of Norfloxacin after Intranasal Administration to Rats. Furubayashi, T; Higaki, K; Inoue, D; Katsumi, H; Kimura, S; Kiriyama, A; Ogawara, KI; Sakane, T; Tanaka, A; Yamamoto, A; Yutani, R, 2018) | 0.48 |
"The knowledge on human serum albumin (HSA) binding is of utmost importance as it affects pharmacokinetic behavior and bioavailability of drugs." | ( Human Serum Albumin Binding in a Vial: A Novel UV-pH Titration Method To Assist Drug Design. Bajusz, D; Balogh, GT; Dargó, G; Müller, J; Simon, K, 2020) | 0.56 |
"We studied pharmacokinetics and bioavailability of verapamil, propranolol, and ethacizine in healthy volunteers after single oral administration under normal conditions and on the second day of simulated antiorthostatic hypokinesia modeling some effects of microgravity." | ( Peculiarities of Pharmacokinetics and Bioavailability of Some Cardiovascular Drugs under Conditions of Antiorthostatic Hypokinesia. Kondratenko, SN; Kovachevich, IV; Kukes, VG; Polyakov, AV; Repenkova, LG; Savelyeva, MI; Svistunov, AA, 2020) | 0.8 |
"The study depicts that propranolol is well absorbed after oral administration." | ( Clinical Pharmacokinetics of Propranolol Hydrochloride: A Review. Ahmed, N; Kalam, MN; Rasool, MF; Rehman, AU, 2020) | 1.16 |
" Gastric involvement and achlorhydria may be present, with subsequent alteration of medication bioavailability which can trigger severe arrhythmic complications." | ( Propranolol syrup to tablets change triggers electrical storm in Jervell-Lange-Nielsen syndrome. Moreno-Mata, N; Moreno-Planas, J; Ramos-Jiménez, J; Sánchez-Perez, I, 2021) | 2.06 |
" The optimized formulation was selected for a bioavailability study using albino rabbits and adopting a developed HPLC method." | ( Bucco-Adhesive Film as a Pediatric Proper Dosage Form for Systemic Delivery of Propranolol Hydrochloride: In-vitro and in-vivo Evaluation. Mansour, HF; Mohamad, SA; Salem, H; Yassin, HA, 2020) | 0.79 |
"To study the pharmacokinetics and relative bioavailability of drugs of different chemical structure and pharmacological action under conditions simulating the effects of some factors of spaceflight, as well as the peculiarities of the pharmacokinetics of acetaminophen under long-term spaceflight conditions." | ( Study of the pharmacokinetics of various drugs under conditions of antiorthostatic hypokinesia and the pharmacokinetics of acetaminophen under long-term spaceflight conditions. Badriddinova, LY; Kondratenko, SN; Kovachevich, IV; Polyakov, AV; Repenkova, LG; Savelyeva, MI; Shikh, EV; Svistunov, AA, 2021) | 0.62 |
" The aim of this study was to evaluate the effects of 5-MTHF in combination with propranolol on HVPG and nitric oxide bioavailability markers in patients with cirrhosis and portal hypertension." | ( 5-MTHF enhances the portal pressure reduction achieved with propranolol in patients with cirrhosis: A randomized placebo-controlled trial. Andreone, P; Berzigotti, A; Bosch, J; Di Donato, R; Gitto, S; Renzulli, M; Roncarati, G; Schepis, F; Simoni, P; Villa, E; Vukotic, R, 2023) | 1.38 |
" HVPG and markers of nitric oxide bioavailability (BH4, ADMA and tHcy) were measured again at the end of treatment." | ( 5-MTHF enhances the portal pressure reduction achieved with propranolol in patients with cirrhosis: A randomized placebo-controlled trial. Andreone, P; Berzigotti, A; Bosch, J; Di Donato, R; Gitto, S; Renzulli, M; Roncarati, G; Schepis, F; Simoni, P; Villa, E; Vukotic, R, 2023) | 1.15 |
"Groups were similar in terms of baseline clinical and hemodynamic data and nitric oxide bioavailability markers." | ( 5-MTHF enhances the portal pressure reduction achieved with propranolol in patients with cirrhosis: A randomized placebo-controlled trial. Andreone, P; Berzigotti, A; Bosch, J; Di Donato, R; Gitto, S; Renzulli, M; Roncarati, G; Schepis, F; Simoni, P; Villa, E; Vukotic, R, 2023) | 1.15 |
" This effect appears to be mediated by improved nitric oxide bioavailability in the hepatic microcirculation." | ( 5-MTHF enhances the portal pressure reduction achieved with propranolol in patients with cirrhosis: A randomized placebo-controlled trial. Andreone, P; Berzigotti, A; Bosch, J; Di Donato, R; Gitto, S; Renzulli, M; Roncarati, G; Schepis, F; Simoni, P; Villa, E; Vukotic, R, 2023) | 1.15 |
In a previous experiment, fetopathic effects of caffeine were significantly reduced by pretreatment with propranolol at dosage levels of 2. Maximal blood pressures during the first 5 hours following the termination of cardiopulmonary bypass were significantly positively correlated with preoperative pro Pranolol dosage. The secondary outcome measures were the duration of labour, the required dosage of oxytocin and CTG readings.
Excerpt | Relevance | Reference |
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" Drug dosage was selected to be proportionate to beta-adrenoreceptor-blocking potency; d-propranolol dosage equalled approximately that of racemic propranolol." | ( The antihypertensive action of several beta-adrenoreceptor-blocking drugs. Waal-Manning, HJ, 1976) | 0.48 |
" The two drugs caused comparable shifts of the isoproterenol dose-response curve during anesthesia." | ( Interaction of anesthesia, beta-receptor blockade, and blood loss in dogs with induced myocardial infarction. Bennett, MJ; Clarke, TN; Foëx, P; Prys-Roberts, C; Roberts, JG; Ryder, WA, 1976) | 0.26 |
" With both beta-blockers, cardiac blockade and hypotensive effect increased in a parallel fashion when the dosage was increased suggesting that the hypotensive effect is related to cardiac beta-blockade." | ( The relationship between beta-blockade, hyporeninaemic and hypotensive effect of two beta-blocking agents. Amery, A; De Plaen, JF; Fagard, R; Linjen, P; Reybrouck, T, 1976) | 0.26 |
" There is increasing evidence that certain orally administered nitrates at larger than usual dosage can further increase the tolerance to effort." | ( Pharmacotherapy of myocardial ischemia. Gorlin, R, 1976) | 0.26 |
" The different influence of 10 mg propranolol and 20 mg practolol on the stimulating effect of 40 mg furosemide on the PRA can be interpreted as a dosage problem." | ( [Cyclic AMP and plasma renin activity in renal vein blood after amitryptiline, theophylline, furosemide and beta adrenergic blocking substances (author's transl)]. Klaus, D; Klumpp, F; Lemke, R; Zehner, J, 1976) | 0.53 |
" Propranolol shifted the dose-response curves downward and to the right for all agonists; phentolamine, shifter the curves upward and to the left." | ( Effects of adrenergic amines on electrophysiological properties and automaticity of neonatal and adult canine Purkinje fibers: evidence for alpha- and beta-adrenergic actions. Danilo, P; Hordof, AJ; Ilvento, JP; Rosen, MR, 1977) | 1.17 |
" The dose-response curves in all anesthetics remained unaltered in the presence of either 3 x 10(-7) M dl-propranolol or 1 x 10(-6) M atropine." | ( Mechanisms of chronotropic effects of volatile inhalation anesthetics. Krisna, G; Paradise, RR, ) | 0.34 |
" The dose-response curves obtained were compared with similar curves previously reported for sotalol, practolol, and atenolol with identical experimental methods." | ( Influence of intrinsic sympathomimetic activity and cardioselectivity on beta adrenoceptor blockade. Brown, HC; Carruthers, SG; McDevitt, DG; Shanks, RG, 1977) | 0.26 |
" A dose-response relationship to intravenous doses of propranolol in the microgram range was obtained during a steady state of infusion of epinephrine." | ( Beta-2 adrenoceptor blocking activity of penbutolol and propranolol at very low doses. Chabria, NL; Chadha, DR; DaSilva, LM; Kulkarni, RD, 1977) | 0.75 |
" Resistance to alpha adrenergic blocking agents developed when the patient's daily propranolol dosage was lowered from 10 to 1 mg/kg." | ( Childhood pheochromocytoma: treatment with alpha methyl tyrosine for resistant hypertension. DeQuattro, V; Grushkin, CM; Lieberman, E; Robinson, RG, 1977) | 0.48 |
" The dose of penbutolol producing an effect equivalent to that of propranolol was calculating from the log dose-response curve of penbutolol." | ( Comparative potency of intravenous penbutolol and propranolol in man. Sapru, RP; Sharma, PL, 1978) | 0.75 |
" Optimal daily dosage for nadolol was 100 mg, and 112 mg for propranolol." | ( Comparison of the new beta-adrenoceptor antagonist, nadolol, and propranolol in the treatment of angina pectoris. Dahlqvist, A; Furberg, B; Raak, A; Wrege, U, 1978) | 0.74 |
" Isoprenaline evoked vasodilation and propranolol (beta-adrenoceptor antagonist) caused a parallel shift to the right of the isoprenaline log dose-response curve." | ( Identification of beta-adrenoceptors and histamine receptors in the cat nasal vasculature. Hiley, CR; Wilson, H; Yates, MS, ) | 0.4 |
"1 In spontaneously active Purkinje fibres of young cows the dose-response curves of the action of isoprenaline upon different electrophysiological parameters were measured." | ( The effects of isoprenaline and a new beta-sympathomimetic amine upon spontaneous activity, diastolic depolarization and plateau height in cardiac Purkinje fibres. Grabowski, W; Lüttgau, HC; Schulze, JJ, 1978) | 0.26 |
" Cocaine or phentolamine shifted the dose-response curve to the left." | ( Effects of ethylephrine on the rat atrial pacemaker. Aramendía, P; De Mikulic, LE; Márquez, MT, 1977) | 0.26 |
" Both timolol and acebutolol had a significant hypotensive effect at 24 hours and a low incidence of side effects, suggesting that further increases in dosage might be effective and well tolerated." | ( Randomised study of six beta-blockers and a thiazide diuretic in essential hypertension. Wilcox, RG, 1978) | 0.26 |
" Propranolol shifted the dose-response curves for the isoproterenol-induced flow increases in the common hepatic, gastro-duodenal, and cranial mesenteric arteries to the right." | ( alpha- and beta-receptor blockade of isoproterenol- and norepinephrine-induced effects on regional blood flow and blood flow acceleration. Beijer, HJ; Charbon, GA; Immink, WF, 1978) | 1.17 |
"Twenty-nine anginal patients were randomly allocated to nadolol once daily, or propranolol four times daily and titrated to optimum dosage over 14 weeks under double-blind conditions: all patients then continued on nadolol once daily." | ( Angina pectoris: effective therapy once daily. Prager, G, 1979) | 0.49 |
" Propranolol, a beta-adrenergic antagonist, when administered at a dosage of 20 mg/kg of body weight, enhanced both passive hemagglutinating and IgE (passive cutaneous anaphylaxis) antibody formation." | ( Enhancement of IgE antibody formation in the rabbit by adrenergic antagonists. Cain, WA; Homer, JT, 1979) | 1.17 |
" Specific airway conductance is measured after increasing doses of inhaled salbutamol and the extent to which the dose-response curve is displaced to the right after beta-adrenoceptor blocking drugs is used to assess bronchial beta-adrenoceptor blockade." | ( Quantitative assessment of bronchial beta-adrenoceptor blockade in man. Baldwin, CJ; Gribbin, HR; Tattersfield, AE, 1979) | 0.26 |
" Aminobenzylpropranolol inhibited catecholamine-stimulated intracellular cyclic AMP accumulation; with increasing blockade, isoproterenol dose-response curves became progressively shifted to the right but the maximal response was unaltered." | ( Quantitative relationship between beta-adrenergic receptor number and physiologic responses as studied with a long-lasting beta-adrenergic antagonist. Brooker, G; Linden, J; Terasaki, WL, 1979) | 0.64 |
" The relationship of propranolol dosage to blood levels, the effect of blood levels on pharmacological response, the metabolism and elimination of propranolol, and determination of rational dosage of the drug, are discussed." | ( Pharmacokinetics in drug therapy. I: Propranolol hydrochloride as adjunct therapy in the treatment of thyrotoxicosis. Robayo, JR, 1976) | 0.85 |
" In view of the clinical dosage levels, it is sugg ested that the antiarrhythmic effects of OPC-1085 depend predominantly on its beta blocking action." | ( Cardiac electrophysiologic action of carteolol hydrochloride (OPC-1085), a new beta-adrenergic blocking agent. Ozawa, M; Toda, H; Watanabe, Y, 1978) | 0.26 |
" The initial CSF sample was removed after a drug-free period and propranolol dosage was then increased over 1 week to 1000 mg daily in all ten patients." | ( The effect of propranolol treatment in shizophrenia on CSF amine metabolites and prolactin. Belmaker, RH; Dasberg, H; Ebstein, RP; Levy, A; Sedvall, G; Van Praag, HM, 1979) | 0.86 |
"We advocate the use of propranolol in very low dosage at the end of operation to determine a prognosis of the long-term results to be expected after valvulotomy in diverse types of pulmonary stenosis." | ( The postvalvulotomy propranolol test to determine reversibility of the residual gradient in pulmonary stenosis. Buis-Liem, TN; Geldof, WC; Moulaert, AJ; Rohmer, J, 1976) | 0.89 |
" 2 Dose-response and time course experiments revealed that propranolol greatly inhibited microsomal and mitochondrial calcium uptake whereas both acebutolol and practolol showed slight depressant effects." | ( Comparison of the actions of acebutolol, practolol and propranolol on calcium transport by heart microsomes and mitochondria. Dhalla, NS; Lee, SL, 1976) | 0.75 |
" The slopes of the dose-response curves for the two catecholamines and the maxima of the curves were the same." | ( Substitution of calorigenic effects of noradrenaline and adrenaline and differences in their inhibition by propranolol. Cervinka, M; Janský, L; Mejsnar, J, 1976) | 0.47 |
" Pretreatment with propranolol shifted the dose-response curves for the inotropic effect of both grayanotoxins slightly to the right." | ( The effects of grayanotoxin I and alpha-dihydrograyanotoxin II on guinea-pig myocardium. Akera, T; Brody, TM; Frank, M; Iwasa, J; Ku, DD, 1977) | 0.59 |
" In vitro dose-response curves to gastrin I, CCK, and the octapeptide of CCK (OP) demonstrated that both CCK and OP were partial agonists on the LES muscle." | ( Mechanism of cholecystokinin inhibition of lower esophageal sphincter pressure. Cohen, S; DiMarino, AJ; Fisher, RS, 1975) | 0.25 |
" Phentolamine, on the other hand, shifted the phenylephrine dose-response curve for contractility to the right without affecting the other parameters." | ( Biochemical and mechanical effects of phenylephrine on the heart. McNeill, JH; Verma, SC, 1976) | 0.26 |
" Noncyclic nucleotides, adenosine, adenosine 5'-monophosphate (AMP), and guanosine 5'-monophosphate (GMP) showed clear, dose-response protection against histamine death of propranolol-treated mice when they were given 45 to 90 min before histamine." | ( Hypersensitivity to histamine and systemic anaphylaxis in mice with pharmacologic beta adrenergic blockade: protection by nucleotides. Matsumura, Y; Tan, EM; Vaughan, JH, 1976) | 0.45 |
" Propranolol administration abolished the hemodynamic effects of isoproterenol and significantly decreased the response of plasma cyclic AMP; the same blocking dosage had little effect on plasma cyclic AMP changes induced by glucagon wheras the response in blood sugar was significantly reduced." | ( Effects of beta-adrenergic blockade on plasma cyclic AMP and blood sugar responses to glucagon and isoproterenol in man. Fraysse, J; Genest, J; Hamet, P; Kuchel, O; Messerli, FH; Tolis, G, 1976) | 1.17 |
" Construction of dose-response curves, however, revealed antagonism of all three parameters by propranolol and different sensitivities of the parameters to isoprenaline." | ( The beta-adrenoceptors responsible for a direct relaxation of the uncontracted nictitating membrane of the anaesthetized cat. Broadley, KJ, 1977) | 0.48 |
"13 The vasoconstrictor actions of phenylephrine, noradrenaline and adrenaline were all antagonized by the systemic administration of phentolamine, all three dose-response curves being shifted to the right." | ( The role of beta-adrenoceptors in the responses of the hepatic arterial vascular bed of the dog to phenylephrine, isoprenaline, noradrenaline and adrenaline. Richardson, PD; Withrington, PG, 1977) | 0.26 |
" These were reduced by terbutaline (1 and 10 nmol) which produced a significant shift in the histamine dose-response lines to lower absorbance values." | ( Beta-adrenoceptor mediated inhibition by terbutaline of histamine effects on vascular permeability. O'Donnell, SR; Persson, CG, 1978) | 0.26 |
" Dose-response curves of these drugs fitted the theoretical dose-response relations, but the curves of ATP and GTP were not significantly altered by propranolol." | ( Nature of catecholamine-like actions of ATP and other energy rich nucleotides on the bullfrog atrial muscle. Goto, M; Tsuda, Y; Yatani, A, 1978) | 0.46 |
" Isoprenaline, salbutamol and ritodrine caused a dose-dependent reduction of the spontaneous contractions of the pregnant myometrium and a dose-related and parallel shift to the right of the isoprenaline dose-response curve was obtained with butoxamine but not with practolol." | ( Beta-adrenoceptors in the pregnant and non-pregnant myometrium of the goat and cow. Larsen, JJ, 1979) | 0.26 |
" Therefore, 50 mg of propanolol are recommended as the proper dosage with which to examine cardiac and extracardiac beta-adrenergic receptors in cattle." | ( [Electrocardiographic functional diagnosis of the vegitative nervous system in cattle. 2. Determination of the propranolol blockade effect on cardiac beta-receptors under application of maximum isoprenaline doses]. Schumann, S, 1978) | 0.47 |
" Log dose-response curves to isoprenaline from spontaneously contracting muscle strips from rabbit uterus have been obtained." | ( Action of beta-adrenoceptor antagonists on the response to isoprenaline in the oestrogen dominated rabbit uterus. Nesheim, BI, 1975) | 0.25 |
" In the antipsychotic classification, special attention is given to side effects (extrapyramidal motor signs, tardive dyskinesias, akathisis) and to dosage for the elderly." | ( Observations on the psychopharmacology of the aged. Eisdorfer, C, 1975) | 0.25 |
"The effect of lidocaine was studied in guinea pig trachealis muscle by dose-response reversal and protection of agonist-induced contractures in a superfusion system." | ( The effect of local anesthetic, lidocaine, on guinea pig trachealis muscle in vitro. Anderson, WH; O'Brien, KP; Weiss, EB, 1975) | 0.25 |
" Maintenance quinidine dosage may have to be reduced in patients with moderate to severe hepatic cirrhosis, but not in patients receiving propranolol." | ( Quinidine pharmacokinetics in patients with cirrhosis or receiving propranolol. Black, M; Humphries, WC; Kessler, KM; Spann, JF, 1978) | 0.7 |
" Dose-response curves of isoprenaline were constructed in nine hypertensive patients before and after either propranolol or metoprolol." | ( Effect of selective and non-selective beta-adrenoreceptor blockade on calf blood flow in hypertensive patients. Clement, DL, 1978) | 0.47 |
"The relationship between long-term propranolol hydrochloride therapy and subsequent coronary bypass operation was prospectively investigated in 119 patients who were grouped three ways: propranolol therapy continued in full dosage to operation (group A), propranolol therapy discontinued or tapered 24 to 72 hours preoperatively (group B), and no preoperative propranolol therapy (control group)." | ( Preoperative propranolol therapy and aortocoronary bypass operation. Keats, AS; Ott, E; Slogoff, S, 1978) | 0.9 |
"From a study on the interrelationship between electroshock-induced convulsions, autonomic function, catecholamines, and cardiovascular homeostasis in dogs, the authors found that: (1) the asystole of electroshock (ES) was significnatly prolonged by high spinal anesthesia but not by relative alpha- or beta-adrenergic blockade; (2) increased levels of circulating catecholamines were solely responsible for the marked hypertensive response to ES, since the pressor effect could be blocked by preventing the release of catecholamines with high spinal anesthesia or by inhibiting alpha-adrenergic receptors with phenoxybenzamine; (3) the adrenal medulla appeared to be the source of most of the ES-induced increase in circulating catecholamines; (4) the asystole and arrhythmias of ES were a cholinergic effect, since they were blocked by atropine; (5) there was a dose-response relationship between the coulombs of electricity administered and the catecholamine and cardiovascular responses; and (6) that the adverse cardiovascular effects of ES therapy could be ameliorated pharmacologically." | ( Autonomic blockade and the cardiovascular and catecholamine response to electroshock. Anton, AH; Redderson, CL; Uy, DS, ) | 0.13 |
" When falls in blood pressure and plasma propranolol concentration were compared overall, a biphasic dose-response relationship was noted, with a first component at plasma propranolol concentrations of 3 to 30 ng/ml and a second at concentrations above 30 ng/ml." | ( Pathophysiologic and pharmacokinetic determinants of the antihypertensive response to propranolol. DeQuattro, V; Esler, M; Randall, O; Zweifler, A, 1977) | 0.75 |
" We conclude that the cardioselectivity of tolamolol is dose-limited but is present at the dosage of 50 mg, which is equivalent to the usual antiarrhythmic beta-adrenergic blocking dose of propranolol (40 mg)." | ( Beta-adrenergic blockade of the lung. Dose-dependent cardioselectivity of tolamolol in asthma. Chester, EH; Fleming, GM; Jones, PK; Schwartz, HJ, 1978) | 0.45 |
" The results clearly indicate that at the dosage used, the four antiarrhythmic agents (quinidine, disopyramide, prajmaliumbitartrate, propafenone) exert a negative inotropic effect on left ventricular function as far as it can be judged from the measurement of STI." | ( [The effect of some antiarrhythmic drugs on systolic time intervals in normal subjects (author's transl)]. Breithardt, G; Jochum, E; Kuhn, H; Seipel, L, 1978) | 0.26 |
" Mean duration of treatment was 16 months (range 8--36) and mean dosage 163 mg/day." | ( Long-term clinical experience with atenolol--a new selective beta-1-blocker with few side-effects from the central nervous system. Henningsen, NC; Mattiasson, I, 1979) | 0.26 |
"In a double-blind, crossover, randomized study, the therapeutic effectiveness of a single daily dose of slow-release oxprenolol (160 mg/day) was compared with a conventional dosage schedule of propranolol (40 mg three times daily) in eighteen patients with uncomplicated, stable exercise-induced angina pectoris." | ( Comparison of clinical effects of propranolol (Inderal) with once daily slow-release oxprenolol (Slow Trasicor) in angina pectoris. de Feijter, PJ; Majid, PA; Roos, JP; van der Wall, EE; Wardeh, R, 1979) | 0.73 |
"The effect of conventional propranolol tablets given twice daily has been compared with an equivalent dosage of a long-acting formulation of propranolol ('Inderal' LA)p given once daily in twenty-nine patients with mild to moderate hypertension." | ( Comparison of a once daily long-acting formulation of propranolol with conventional propranolol given twice daily in patients with mild to moderate hypertension. Douglas-Jones, AP, 1979) | 0.81 |
"Pharmacokinetic methods that have been used to improve antihypertensive drug therapy, including antihypertensive dosage regimens, are reviewed." | ( Using pharmacokinetics in drug therapy. V: Contributions to developing dosage regimens for antihypertensive drugs. Schumacher, GE, 1979) | 0.26 |
" Beta-blockers showed little evidence of useful antiarrhythmic action in the dosage used, but increasing the dosage in suspected myocardial infarction is not practicable because of the risk of hypotension." | ( Effect of beta-blockers on arrhythmias during six weeks after suspected myocardial infarction. Banks, DC; Edwards, B; Fentem, PH; Hampton, JR; Roland, JM; Wilcox, RG, 1979) | 0.26 |
" With thiazide dosage constant throughout, maximal dose titration to 386." | ( Hemodynamic effects of oxprenolol and propranolol in hypertension. Franciosa, JA; Johnson, SM; Tobian, LJ, 1979) | 0.53 |
" The maximum oral dose of captopril was 450 mg daily and the maximum oral dosage of propranolol was 360 mg daily." | ( Comparison of captopril with propranolol in the treatment of mild and moderate essential hypertension. Seedat, YK, 1979) | 0.78 |
" A heart rate in the 50s does not preclude an increase in the dosage of propranolol when necessary." | ( Pathophysiology and medical management of angina pectoris. Brest, AN; Duca, PR; Gottlieb, RS, 1977) | 0.49 |
"More recent investigations on the duration of effect and plasma half-life of propranolol suggest a simplification of dosage for the beta-blocker in the treatment of hypertension." | ( [Treatment of hypertension with propranolol in internal medicine and general practice. A field trial with a simplified twice daily administration of Dociton 80 (author's transl)]. Hiemstra, S; Steichele, C; Ziegler, E, 1977) | 0.77 |
" The fall in blood pressure during beta-adrenergic blockade with a low dosage of propranolol apparently does not depend on changed baroreflex sensitivity, but on the intrinsic action of this drug on beta-receptors." | ( Baroreflex sensitivity in hypertension during beta-adrenergic blockade. Dunning, AJ; Krediet, RT, 1979) | 0.49 |
" The slopes of the dose-response curves of insulin and parathyroid hormone were indistinguishable and different from that of 1 alpha-hydroxyvitamin D3." | ( Hypercalcemic effect of insulin in the chick. Hawrylko, J; Hinton, A; Palmieri, GM, 1979) | 0.26 |
" It is important to know how the pharmacokinetics of a drug vary with different disease states so that appropriate adjustments to dosage can be made." | ( Series on pharmacology in practice. 2. Antiarrhythmic drug therapy. Federman, J; Vlietstra, RE, 1979) | 0.26 |
" There was no correlation between reactivity, which reflects the slope of the dose-response curve beyond the threshold dose, and threshold doses, nor between the initial RL (normalized for lung volume) and either threshold or reactivity." | ( Variability of airway responses to inhaled histamine in normal subjects. Engel, LA; Habib, MP; Paré, PD, 1979) | 0.26 |
" With the use of semilogarithmic dose-response curves they have shown that 80 mg oral propranolol augmented, whereas oral pretreatment with 400 mg W10294A (an experimental bronchodilator) decreased, histamine and methacholine-induced airway constriction." | ( Modification of induced airway constriction in healthy subjects. Bouhuys, A; Littner, MR; Schachter, EN, 1979) | 0.48 |
" After a placebo control period, propranolol was begun and the dosage increased sequentially until arrhythmia suppression was achieved, side effects appeared, or a maximum dosage of 960 mg/day was reached." | ( Suppression of chronic ventricular arrhythmias with propranolol. Higgins, SB; Kornhauser, D; Nies, AS; Oates, JA; Reele, S; Shand, DG; Smith, R; Woosley, RL, 1979) | 0.79 |
" Daily dosage varied among the patients, but the mean dose was 308 mg (+/- 51 SEM)." | ( Spurious hyperbilirubinemia in uremic patients on propranolol therapy. McKinney, TD; Stone, WJ; Warnock, LG, 1979) | 0.51 |
"A patient with severe narcolepsy and cataplexy had been treated with a high dosage of methylphenidate hydrochloride, but the drug was not effective." | ( Successful treatment of narcolepsy with propranolol: a case report. Cadieux, R; Kales, A; Soldatos, CR; Tan, TL, 1979) | 0.53 |
" If the MAP was more than 108 mm Hg at the end of the week, dosage of the beta-blocker was doubled the following week; when necessary, doubling was repeated to a maximum dose of 640 mg propranolol and 400 mg atenolol daily." | ( Effects of atenolol and propranolol when added to long-term antihypertensive diuretic therapy. Boer, P; Dorhout Mees, EJ; Geyskes, GG; van Rooijen, GJ, 1979) | 0.76 |
" When nifedipine dosage was decreased." | ( Nifedipine therapy for refractory coronary arterial spasm. Heupler, FA; Proudfit, WL, 1979) | 0.26 |
" Propranolol and timolol produced a dose-dependent increase of atrial and atrioventricular nodal refractory periods; dose-response curves were parallel." | ( Effects of the beta-adrenergic blocking agents propranolol and timolol on canine cardiac refractory periods. Cheymol, G; Heckle, J; Jaillon, P; Weissenburger, J, 1979) | 1.43 |
"Five dialysis patients with residual hypertension were treated with a new sustained-release formulation of propranolol (160 mg per capsule) in a dosage of 1 to 2 capsules per day." | ( Raynaud's phenomenon in hypertensive dialysis patients taking a sustained-release propranolol formulation. Gabriel, R; Poulter, N, 1979) | 0.7 |
"7 years) with severe essential hypertension (n = 21) and renovascular hypertension (n = 1) were treated with a mean daily dosage of 16." | ( [Minoxidil in treatment resistant hypertension]. Furrer, J; Nussberger, J; Reuteler, H; Siegenthaler, W; Studer, A; Tenschert, W; Vetter, W, 1979) | 0.26 |
" These differences were maintained on repeated dosing for 8 days." | ( Observations on some properties of a long-acting preparation of propranolol. Leahey, WJ; Neill, JD; Shanks, RG; Varma, MP, 1979) | 0.5 |
" Dose-response experiments with six doses of histamine and two doses of the beta2-agonist showed unchanged calculated maximal response and an increase in D50." | ( Effects of beta2-sympathomimetic on histamine-stimulated gastric acid secretion in dogs. Gottrup, F; Ornsholt, J, 1979) | 0.26 |
" Dose-response experiments with 6 doses of pentagastrin and 1 dose of salmefamol showed a decrease in calculated maximal response (CMR) and an unchanged D50." | ( Inhibition of gastric acid secretion in dogs by a new sympathomimetic drug. Gottrup, F; Ornsholt, J, 1978) | 0.26 |
" However, the dose-response curve to EPI was shifted horizontally to the right 4 days after mating suggesting a tissue desensitization." | ( The absence of sensitivity changes of the rabbit oviduct to phenylephrine and isoproterenol during early gestation. Heilman, RD; Reo, RR, 1977) | 0.26 |
" Propranolol dosage was titrated to produce maximal beta-adrenergic blockade." | ( Efficacy of propranolol in the control of exercise-induced or augmented ventricular ectopic activity. Nixon, JV; Pennington, W; Ritter, W; Shapiro, W, 1978) | 1.55 |
" The alpha-adrenergic blocker, phentolamine, shifted the dose-response curve upward and to the left and enhanced the hyperpolarization of RAF." | ( Alpha and beta adrenergic effects on human atrial specialized conducting fibers. Bowman, FO; Hordof, AJ; Malm, JR; Mary-Rabine, L; Rosen, MR, 1978) | 0.26 |
"In 16 patients with hypertension, BP could not be controlled satisfactorily by treatment with propranolol alone (mean dosage 325 mg/day)." | ( Changes in plasma volume and extracellular fluid volume and after addition of hydralazine to propranolol treatment in patients with hypertension. Ibsen, H; Jensen, HA; Leth, A; Rasmussen, K, 1978) | 0.7 |
"In fifteen patients with hypertension, inadequately controlled during treatment with propranolol alone (mean dosage 333 mg/day), plasma volume (PV) and extracellular fluid volume (ECV) were determined." | ( Changes in plasma volume and extracellular fluid volume after addition of prazosin to propranolol treatment in patients with hypertension. Ibsen, H; Jensen, HA; Leth, A; Rasmussen, K, 1978) | 0.71 |
" These doses produced nearly equivalent shifts in isoproterenol-induced chronotropic dose-response curves, indicating equivalent degrees of beta adrenergic blockade." | ( Superiority of practolol versus propranolol in protection against ventricular fibrillation induced by coronary occlusion. Gillis, RA; Pearle, DL; Williford, D, 1978) | 0.54 |
"The effect of the use of the so-called heparin lock for blood sampling on the binding of propranolol has been studied and a cumulative dose-response curve to heparin constructed." | ( Altered drug binding due to the use of indwelling heparinized cannulas (heparin lock) for sampling. Shand, DG; Wood, AJ; Wood, M, 1979) | 0.48 |
" Although the three treatment regimens were similar with respect to safety and efficacy, the reserpine-hydroflumethiazide combination offers the advantages of more convenient dosage at lower cost." | ( Step 2 regimens in hypertension. An assessment. Berry, C; Finnerty, FA; Gyftopoulos, A; McKenney, A, 1979) | 0.26 |
" The hypotensive activity of acebutolol was confirmed when a dosage of 600 mg/day was used, with en absence of side effects." | ( [Comparative study of acebutolol and propranolol in the treatment of arterial hypertension]. Tacquet, A, 1975) | 0.53 |
" This accounts for most of the individual variation in dosage requirements." | ( Pharmacokinetics of propranolol: a review. Shand, DG, 1976) | 0.58 |
" After a two dose trial (Gillam and Prichard, 1966,) demonstrated a dose dependent anti-anginal effect, a log-dose response study demonstrated a progressive reduction in angina attacks as dosage was increased (Prichard and Gillam, 1971)." | ( Propranolol in the treatment of angina: a review. Prichard, BN, 1976) | 1.7 |
" Dosage was adjusted to achieve an optimum clinical response and a relatively high degree of beta-blockade, as judged by the virtual abolition of orthostatic and hyperventilatory tachycardia." | ( Propranolol in the treatment of anxiety. Suzman, MM, 1976) | 1.7 |
" Midway through each four-week period, drug dosage was doubled; thus, regimes were metoprolol, 150 and 300 mg/day, propranolol, 120 and 240 mg per day and placebo, 3 and 6 tablets per day." | ( Assessment of metoprolol, a cardioselective beta-blocking agent, during chronic therapy in patients with angina pectoris. Borer, JS; Comerford, MB; Sowton, E, 1976) | 0.47 |
" In the dosage employed in these patients, propranolol had no demonstrable effect on either thyroid hormone secretion, the peripheral disposal of T4, or the TSH and prl responses to TRH." | ( Failure of propranolol to alter thyroid iodine release, thyroxine turnover, or the TSH and PRL responses to thyrotropin-releasing hormone in patients with thyrotoxicosis. Dimond, RC; Earll, JM; Frantz, AG; Noel, GL; Wartofsky, L, 1975) | 0.91 |
" Its antianginal effectivess was investigated in 20 patients with documented coronary heart disease in a 44-wk study incorporating a prolonged 12-wk lead-in period, individualization of P dosage in a 6-wk dose-finding period, and a 24-wk doule-blind crossover phase." | ( Efficacy of beta adrenergic blockade in coronary heart disease: propranolol in angina pectoris. Amsterdam, EZ; Mason, DT; Miller, RR; Olson, HG; Pratt, CM, 1975) | 0.49 |
"Increments in heart rate during the TNG test (sublingual nitroglycerin with assumption of upright posture), passive head-up tilt, and postrecumbency standing were compared to the effects of intravenous isoproterenol in 15 mild hypertensives during administration of placebo and two dosage levels of propranolol." | ( Heart rate responses during treatment of hypertension with propranolol. The clinical usefulness of the nitroglycerin test. Hansson, L; Zweifler, AJ, 1976) | 0.67 |
" When keeping the heart rate constant by means of a pace maker, carbocromen even at higher dosage caused a clear-cut improvement." | ( [The effect of carbocromen on the ST segment of the epicardial electrocardiogram in a model of intermitting myocardial ischemia (author's transl)]. Kunath, B; Nitz, RE; Scholtholt, J; Sirbulescu, R, 1976) | 0.26 |
" An attempt to reduce the drug dosage should be made every 6 months, in hospital." | ( [Ventricular tachycardia of the infant. 2 new cases]. Bricaud, H; Choussat, A; Clémenty, J; Dallocchio, M; Giraudet, C; Saint-Martin, J, 1976) | 0.26 |
" Sudden cessation of propranolol for short periods may be preferable to tapering the dosage if prolonged periods of sub-optimal beta-adrenoceptor blockade are to be avoided." | ( Sudden withdrawal of propranolol in patients with angina pectoris. Myers, MG; Wisenberg, G, 1977) | 0.89 |
" By titrating dosage against the response of blood pressure and pulse rate, propranolol hydrochloride was administered orally at 160 mg/day in four divided doses." | ( Blood pressure responses to catecholamines during beta-adrenergic blockade with propranolol in hypertensive subjects. DeGuia, D; Mendlowitz, M; Vlachakis, ND, 1977) | 0.71 |
" The dose-response relationship was obtained by measuring a change in membrane resistance." | ( Effect of hemolysin produced by Vibrio parahaemolyticus on membrane conductance and mechanical tension of rabbit myocardium. Honda, T; Irisawa, H; Miwatani, T; Seyama, I; Takeda, Y, 1977) | 0.26 |
" In the presence of PBZ or phentolamine blockade, the dose-response curves of oxytocin and VP were shifted to the left, resulting in an apparent doubling of the pressor potency of the neurohypophysial peptides." | ( The site and the mechanism of phenoxy-benzamine potentiation of the pressor response to oxytocin and vasopressin: in vivo and isolated aortic strips studies. Chan, WY; Erker, EF, 1977) | 0.26 |
" The average fall in mean arterial pressure for each dosage of hydralazine was no different with or without propranolol, even though propranolol inhibited rises in plasma renin activity and pulse due to hydralazine." | ( Synergistic effects of hydralazine and alpha- or beta-adrenergic blockers: the role of plasma renin activity. Chin, BK; Das, B; Gutkin, M; Mezey, K; Modlinger, RS, ) | 0.34 |
" Compared with basal anesthesia with pentobarbital, 15 mg/kg, neither morphine nor halothane increased sensitivity to any measured effect of propranolol expressed as the slope of the log dose-response relationship." | ( Failure of general anesthesia to potentiate propranolol activity. Bragg, DA; Edmonds, CH; Hibbs, CW; Keats, AS; Slogoff, S, 1977) | 0.72 |
"1 The effects of propranolol and practolol, at equivalent myocardial beta-adrenoceptor blocking doses, (as assessed by the degree of shift of isoprenaline dose-response curves) were investigated in anaesthetized greyhounds before and after acute coronary artery ligation." | ( Comparative effects of propranolol and practolol in the early stages of experimental canine myocardial infarction. Marshall, RJ; Parratt, JR, 1976) | 0.91 |
" It is concluded that the effect of propranolol on heart rate is a predictable function of free drug concentration in man and that the contribution of individual variation in receptor sensitivity to differences in oral dosage requirement is minor compared to that of variations in bioavailability." | ( Plasma binding and the affinity of propranolol for a beta receptor in man. Frisk-Holmberg, M; Hollifield, JW; McDevitt, DG; Shand, DG, 1976) | 0.81 |
" It can be concluded that echocardiography is a feasible tool in determining changes of left ventricular dynamics during administration of vasoactive drugs, in indicating the individual dosage of a vasoactive drug in each patient and the follow-up the course of the therapeutic success." | ( [Echocardiographic evaluation of left ventricular function during therapy with cardiovascularly effective drugs]. Stefan, G, 1976) | 0.26 |
" Gallamine caused parallel rightward shifts of the dose-response curves to the agonists, with no depression of the maximal response." | ( The inhibitory effect of gallamine on muscarinic receptors. Clark, AL; Mitchelson, F, 1976) | 0.26 |
" Fusaric acid produced a shift to the right and down in the dose-response curves to all tested agonists, and antagonized acetylcholine and serotonin most effectively among these agonists." | ( Relaxation of isolated rabbit arteries by fusaric (5-butylpicolinic) acid. Asano, M; Hidaka, H, 1976) | 0.26 |
" By titrating the dosage of both drugs against pulse rate and blood pressure response, propranolol was given between 80 and 160 mg." | ( An approach to the treatment of essential hypertension. Mendlowitz, M; Vlachakis, ND, 1976) | 0.48 |
" The effective dosage of propranolol varied between 280 and 2320 mg per day." | ( [The effect of the beta-adrenergic blocking agent propranolol in mania (author's transl)]. Fritsch, W; Rackensperger, W; Schwarz, D; Stutte, KH; Zerssen, D, 1976) | 0.81 |
"Two infants with the classical involuntary movements of polymyoclonia and opsoclonus were treated with propanolol in a dosage of 2 mg/kg/24 hr." | ( Propanolol treatment of infantile polymyoclonia. Fowler, GW, 1976) | 0.26 |
" Although directly related to daily dosage of levodopa, the myoclonus was specifically blocked by the serotonin antagonist, methysergide." | ( Levodopa-induced myoclonus. Bergen, D; Goetz, C; Klawans, HL, 1975) | 0.25 |
" Dose-response curves to intravenous infusions of isoproterenol were obtained after three doses of each beta-antagonist." | ( Comparison of cardiac effects of timolol and propranolol. Achong, MR; Ogilvie, RI; Piafsky, KM, 1975) | 0.51 |
" Walking exercise induced 1:1 conduction in six patients and was promoted by the following circumstances: 1) atrial rates of 250/min or less; 2) inadequate dosage of digitalis; and 3) the administration of quinidine." | ( The influence of exercise on atrial flutter. Gooch, AS; Sumathisena, DR, 1975) | 0.25 |
" The control log dose-response curve for epinephrine stimulation showed a slight decrease in the upper concentration range." | ( Rabbit testicular contractions: bimodal interaction of prostaglandin E1 with other agonists. Ellis, LC; Hargrove, JL; Seeley, RR, 1975) | 0.25 |
" No changes in regional contractility occurred with propranolol except for a minimal increase in hypokinesis in one patient at each dosage and equivocal development of a new area of slight hypokinesis in one patient and minimal apex of dyskinesis in another at the higher dosage." | ( Left ventricular wall motion response to intravenous propranolol. Dinsmore, RE; Harthorne, JW; Shubrooks, SJ; Zir, LM, 1975) | 0.75 |
" Treatment of the strips with 5-HK in concentrations higher than 2 X 10- minus 6 M shifted the dose-response curve of serotonin to the right and downward." | ( Analysis of the effect of 5-hydroxykynurenamine,, a serotonin metabolite, on isolated cerebral arteries, aortas and atria. Toda, N, 1975) | 0.25 |
"The haemodynamic effects of intravenous propranolol at low dosage (1 and 2 mg) have been evaluated on 14 patients in the acute stage of myocardial infarction." | ( Evaluation of haemodynamic effects of intravenous propranolol at low dosage (1 and 2 mg) in acute myocardial infarction. Letac, B; Letournel, J, 1975) | 0.77 |
" In contrast, dose-response data from fasted rabbits have shown that EPI is more potent than ISO in increasing plasma glucose levels and in lowering hepatic glycogen levels." | ( The influence of propranolol on catecholamine-induced changes in carbohydrate metabolism in the rabbit. Ellis, S; Moratinos, J; Potter, DE, ) | 0.47 |
"The intrarenal distribution of blood flow in the baboon was measured using the 133xenon clearance technique, and dose-response curves for the various components of renal blood flow were determined during intra-arterial infusions of noradrenaline; the alpha-adrenergic blocking agent, phenoxybenzamine; the beta-adrenergic blocking agent, propranolol; and tyramine which causes the release of endogenous NA." | ( The effect of noradrenaline, adrenergic blocking agents, and tyramine on the intrarenal distribution of blood flow in the baboon. Bomzon, L; Farr, J; Rosendorff, C; Scriven, DR, 1975) | 0.43 |
" Whereas contractility increased in response to small doses of digitalis, displaying a linear dose-response relation independent of autonomic tone, A-V nodal transmission indexes responded minimally to less than 50 percent of the toxic dose of digitalis, and the response was dependent upon autonomic tone." | ( Dissociation of the inotropic effect of digitalis from its effect on atrioventricular conduction. Kim, YI; Noble, RJ; Zipes, DP, 1975) | 0.25 |
" Phenoxybenzamine also blocked the response to NA but a dose-response relationship was not apparent." | ( Effect of intraventricular administration of noradrenaline on water diuresis in goats. Peeters, G; Vandeputte-Van Messon, G, 1975) | 0.25 |
" At all dosage levels its effect on blood pressure was biphasic." | ( Influence of some antidepressant drugs on the circulatory system. I. Imipramine. Banaszkiewicz, W; Grzymislawska, I; Mrozikiewicz, A, 1975) | 0.25 |
" In a dosage of 300 mg a day orally trapymin had no clear influence on the non-esterified fatty acids." | ( [Influence of coronary-effective substances on the concentration of nonesterified fatty acids in the serum of patients with angina pectoris]. Heiland, G; Modersohn, D; Pankau, H; Urbaszek, W, 1975) | 0.25 |
"A double-blind trial of propranolol, in a dosage of 120 mg a day, and placebo was conducted in 11 patients with essential tremor." | ( Essential tremor: treatment with propranolol. Loewenson, RB; Tolosa, ES, 1975) | 0.84 |
" The dose-response curve of TM was parallel to that of nitroglycerin and papaverine and steeper than that of dipyridamol or adenosine." | ( [Pharmacology of cornary dilator agent, trapymin. (2) Analysis of its mode of action]. Ogawa, N; Ohnishi, H; Tsukuda, S; Yamaguchi, K, 1975) | 0.25 |
" Intraventricular injection of phenylephrine produced a dose-dependent hypothermia, whereas no dose-response relationship was obtained by isoproterenol." | ( [Role of brain biogenic amines in the central thermoregulatory mechanism of the rat (author's transl)]. Fukushima, N, 1975) | 0.25 |
" In general, the dosage of propranolol must be individually adjusted and is usually from 30 to 40 mg daily in divided doses." | ( Control of lithium tremor with propranolol. Lapierre, YD, 1976) | 0.84 |
" The bioavailability of tablets and a solution of propranolol was compared with a crossover design by obtaining plasma samples at the end of the dosage interval during chronic oral administration of various doses." | ( Disposition of propoxyphene and propranolol in children. Atwood, GF; Shand, DG; Wilson, JT, 1976) | 0.79 |
" After 3 weeks, the dosage could be doubled according to clinical criteria." | ( Efficacy of nicorandil versus propranolol in mild stable angina pectoris of effort: a long-term, double-blind, randomized study. Bucx, JJ; Henneman, JA; Hugenholtz, PG; Kelder, JC; Kerker, JP; Meeter, K; Tijssen, JG, 1992) | 0.57 |
" In pithed rats, naftopidil shifted the dose-response curve of methoxamine at equipotent hypotensive doses to the same extent to the right as does prazosin, but both drugs barely affected (in contrast to phentolamine) the response to norepinephrine." | ( Naftopidil, a new adrenoceptor blocking agent with Ca(2+)-antagonistic properties: interaction with adrenoceptors. Borbe, HO; Freud, P; Jakob, B; Müller-Beckmann, B; Sponer, G, 1992) | 0.28 |
" The pA2 values of the beta adrenergic antagonists propranolol, metoprolol and atenolol were calculated from the rightward shifts that they impose on dose-response curves of both l-isoproterenol and CGP12177." | ( Multiple beta adrenergic receptor subclasses mediate the l-isoproterenol-induced lipolytic response in rat adipocytes. Van Liefde, I; Van Witzenburg, A; Vauquelin, G, 1992) | 0.54 |
" The optimal dose should be determined on a case-by-case basis, by increasing the daily dosage gradually." | ( [Beta-blockers and migraine]. Bousser, MG; Massiou, H, 1992) | 0.28 |
" Nipradilol, at the dosage used in the present study, did not appear to exert a nitrovasodilating effect to enhance the portal pressure reduction induced by beta-blocking action." | ( Long-term haemodynamic effects of a 4-week regimen of nipradilol, a new beta-blocker with nitrovasodilating properties, in patients with portal hypertension due to cirrhosis. A comparative study with propranolol. Aramaki, T; Katsuta, Y; Komeichi, H; Kurokawa, H; Ohsuga, M; Okumura, H; Satomura, K; Sekiyama, T; Terada, H; Tsutsui, H, 1992) | 0.47 |
" Dose-response curves show similar sensitivity, but decreased responsiveness in the lean animal." | ( Food intake of lean and obese Zucker rats following ventricular infusions of adrenergic agonists. Bray, GA; Tsujii, S, 1992) | 0.28 |
"Spontaneous motor activity of normotensive and renovascular hypertensive baboons was measured during oral dosing with the beta-adrenergic antagonists atenolol HCl (2." | ( Beta-blocker effects on 24-h activity in normotensive and renovascular hypertensive baboons. Allen, RP; Bezold, HJ; Hienz, RD; Turkkan, JS, 1992) | 0.28 |
" After the administration of carvedilol on day 8, the cirazoline vasopressor response was 2 +/- 1 mmHg and the isoproterenol-induced tachycardia was 4 +/- 3 beats/min, indicating effective alpha 1- and beta-adrenergic blockade after chronic dosing with carvedilol." | ( Single and repeated doses of the vasodilator/beta-adrenergic antagonist, carvedilol, block cirazoline- and isoproterenol-mediated hemodynamic responses in the conscious rat. Gagnon, R; Slivjak, MJ; Smith, EF, 1992) | 0.28 |
"Repeated acquisition behavioral performances of normotensive and renovascular hypertensive baboons were tested before, during, and following chronic oral dosing with the beta-adrenergic antagonists atenolol HCl (2." | ( Performance of baboons under a repeated acquisition procedure during chronic oral exposure to atenolol and propranolol. Hienz, RD; Turkkan, JS, 1992) | 0.5 |
" isoproterenol tachycardia dose-response curves by dose ratios of 5, 18, and 90 in sham rabbits, respectively, and 5, 11, and 23 in wrap rabbits, respectively, indicating significant cardiac beta 1-adrenoceptor antagonism." | ( Relationship between the sympatholytic action of nebivolol and hypotension. Angus, JA; Coles, P; Cox, H; Eisenhofer, G; Ward, JE, 1992) | 0.28 |
" There were no significant differences between ET and SED cardiac preparations in either the efficacy (maximal response) or potency (EC50) of isoproterenol dose-response relationships for chronotropic or inotropic responses." | ( Adrenergic responsiveness and intrinsic sinoatrial automaticity of exercise-trained rats. Adams, HR; Allert, JA; Laughlin, MH; Schaefer, ME, 1992) | 0.28 |
" Selection of the dosage was individual under the control of circulation parameters." | ( [The action of the new beta-adrenoblocker Lopressor on the hemodynamics of hypertension patients]. Maev, IV; V'iuchnova, ES, 1992) | 0.28 |
" Dose-response curves for phentolamine and propranolol established maximally effective doses (3." | ( Influence of sympatho-adrenal system on insulin sensitivity using the euglycemic clamp technique. Funado, T; Iguchi, A; Iida, T; Kato, K; Kusunoki, M; Oshida, Y; Sakamoto, N; Sato, Y; Suga, T, 1992) | 0.55 |
" Blood glucose increased in metoprolol treated healthy and liver damaged rats after a single dosage likewise following prolonged treatment." | ( Metoprolol and propranolol treatment in carbon tetrachloride-induced hepatic injury. Kulcsár, A; Kulcsár-Gergely, J, 1992) | 0.64 |
" In a double-blind, placebo-controlled study the tremorolytic efficacy of propranolol has been assessed by a quantitative accelerometric method after a single oral dose (120 mg) and following 2 weeks of sustained treatment with two different dosage regimens of the drug (120 and 240 mg daily)." | ( Effect of propranolol in head tremor: quantitative study following single-dose and sustained drug administration. Baratti, M; Calzetti, S; Fava, R; Negrotti, A; Sasso, E, 1992) | 0.92 |
" After propranolol administration eight patients exhibited a significant maxPFV decrease, whereas the other four patients exhibited only a drop in HR, suggesting either drug inefficacy, inappropriate dosage or inadequate duration of treatment." | ( Duplex-Doppler ultrasonography in the evaluation of cirrhotic patients with portal hypertension and in the analysis of their response to drugs. Cioni, G; Cristani, A; D'Alimonte, P; Romagnoli, R; Ventura, E; Ventura, P; Vignoli, A; Zerbinati, F, ) | 0.59 |
" It was concluded that bepridil, at a mean maintenance dosage of 324 mg/day, was at least as effective as propranolol in improving exercise tolerance--specifically time to angina and total work--and that tolerability of the 2 drugs was comparable." | ( Comparative efficacy and concomitant use of bepridil and beta blockers in the management of angina pectoris. Frishman, WH, 1992) | 0.5 |
" Venom doses of 100 and 200 micrograms/kg produced tachycardia with a dose-response relationship, whereas 400 micrograms/kg evoked sinus tachycardia followed by bradycardia then tachycardia." | ( Effect of scorpion Leiurus quinquestriatus (H&E) venom on rat's heart rate and blood pressure. Abdel-Rahman, MS; Nabil, ZI; Omran, MA, 1992) | 0.28 |
" The Q-T interval developed a dose-response relationship after venom administration." | ( The role of propranolol and atropine in mitigating the toxic effects of scorpion venom on rat electrocardiogram. Abdel-Rahman, MS; Nabil, ZI; Omran, MA, 1992) | 0.66 |
" The effect of twice-daily dosing with propranolol on the pharmacokinetics and pharmacodynamics of a single oral dose of sumatriptan was investigated in 10 healthy male subjects." | ( Lack of an interaction between propranolol and sumatriptan. Breckenridge, AM; Fowler, PA; Lacey, LF; Scott, AK; Walley, T, 1991) | 0.84 |
"Determination of the alpha-adrenergic blocking potency of drugs in humans is usually done by measuring the shift in the blood pressure versus logarithm of intravenous phenylephrine dose-response relationship." | ( Determination of alpha-adrenergic blocking potency. Brodie, CL; Jamieson, MJ; Kwan, CM; Shepherd, AM, 1991) | 0.28 |
" This phenomenon contributes to the normal dose-response curve for epinephrine, according to our analysis, but only in combination with the apparent high efficiency of the receptor in the epinephrine-bound state at cyclase activation." | ( Comparisons of the combined contributions of agonist binding frequency and intrinsic efficiency to receptor-mediated activation of adenylate cyclase. Barber, R; Stickle, D, 1991) | 0.28 |
" In an intravenous cumulative dose-response study of TA-870, the plasma-free-dopamine concentration was elevated depending on the dose of TA-870." | ( A novel orally active dopamine prodrug TA-870. III. Positive inotropic effect and cardiorenal selectivity in anesthetized dogs. Akimoto, Y; Nakajima, H; Nishiyama, S; Yamaguchi, I; Yoshikawa, M, 1990) | 0.28 |
"The objectives of this study were (a) to evaluate the dose-response effect of isradipine, a dihydropyridine calcium antagonist, on the heart rate and blood pressure of males with mild to moderate hypertension; and (b) to compare these results with those obtained with propranolol, a beta-adrenoceptor blocker, on a matched patient population." | ( Isotonic and isometric responses of blood pressure and heart rate in mild to moderate hypertension with isradipine and propranolol. Cantor, A; Cristal, N, 1990) | 0.67 |
"75, 10 and 30mg) of cilazapril reduced diastolic blood pressure dose-dependently and shifted the angiotensin I dose-response curves to the right." | ( Clinical pharmacodynamic studies with cilazapril and a combination of cilazapril and propranolol. Belz, GG; Breithaupt, K; Erb, KA; Essig, J, 1991) | 0.51 |
" The non-selective phosphodiesterase inhibitor isobutylmethylxanthine (IBMX) (1 mM) resulted in a more severe suppression of the histamine and pilocarpine responses and also produced a significant suppression of the maximal response to oxotremorine and a small shift in the carbachol dose-response curve." | ( Beta-adrenoceptor induced inhibition of muscarinic receptor-stimulated phosphoinositide metabolism is agonist specific in bovine tracheal smooth muscle. Chilvers, ER; Nahorski, SR; Offer, GJ, 1991) | 0.28 |
"The efficacy of a controlled-release topical dosage form of glyceryl trinitrate (Nitroglycerin Transdermal Therapeutic System, Nitroderm TTS, NTG-TTS; CAS 55-63-0) was studied in the experimental model of congestive heart failure in beagles." | ( Efficacy of the glyceryl trinitrate transdermal therapeutic system in a dog model of heart failure. Inukai, T; Katahira, J; Nakao, K; Tanaka, M, 1991) | 0.28 |
" At dosage levels similar to arotinolol, both pindolol and labetalol were less effective in preventing cerebral lesions despite lower blood pressure." | ( Prevention of cerebral stroke by arotinolol in salt-loaded SHRSP. Hara, Y; Maniwa, T; Miyagishi, A; Noguchi, T, 1991) | 0.28 |
" To characterize the GHRP dose-response curve and compare it with that of GH-releasing hormone [GHRH-(1-44)NH2], six unanesthetized young adult cynomolgus macaques were tested with a range of iv doses of GHRP or GHRH in random order." | ( Growth hormone (GH) responses to the hexapeptide GH-releasing peptide and GH-releasing hormone (GHRH) in the cynomolgus macaque: evidence for non-GHRH-mediated responses. Hao, EH; Liu, L; Malozowski, S; Marin, G; Merriam, GR; Ren, SG; Southers, JL, 1991) | 0.28 |
"Antiarrhythmic therapy was chosen for 3-7 days by modified chronic electrophysiological study at three stages: (1) the efficacy of a drug, its action onset and termination were defined; (2) a dosage was chosen on an individual basis and the duration of drug potency was specified; (3) the dosage regimen of a drug given as a course therapy was confirmed by the results of trials." | ( [Evaluation of the possibility of selection of individual anti-arrhythmia therapy]. Antonchenko, IV; Borisova, EV; Chekhov, AM; Gimrikh, EO; Plekhanov, IG; Popov, SV; Savenkova, GM, 1991) | 0.28 |
" Dose-response lines in response to the two agonists, expressed as percent maximal contraction, did not differ among the groups." | ( Muscarinic-receptor functioning in tracheas from normal and ovalbumin-sensitive guinea pigs. Biggs, DF; Yang, ZJ, 1991) | 0.28 |
" The provocation dose at a decrease in sGaw of 50% (PD50) was calculated from the dose-response curve." | ( [Comparison of the characteristics of methacholine and of propranolol in the assessment of aspecific hyperreactivity of the airways]. Laxy, T; Schultze-Werninghaus, G; Siekmeier, R, 1991) | 0.53 |
" Two consecutive dose-response curves at 20 min apart were determined in the control group." | ( Evidence for vasoactive intestinal peptide as a mediator of non-adrenergic non-cholinergic neurotransmission in the trachea. Holmes, EP; O'Malley, NA; Venugopalan, CS, 1990) | 0.28 |
" Numerous questions concerning the exact indications of these drugs, the nature and dosage of the beta-blocker to be used, the possible combinations with other therapies and the responses to be expected remain to be answered." | ( [Beta-blockers in the treatment of heart failure]. Grosgogeat, Y; Komajda, M; Lechat, P; Salloum, J, 1990) | 0.28 |
" However, propranolol significantly shifted the methacholine dose-response curve to the left so that methacholine (0." | ( Pulmonary reactivity to methacholine during beta-adrenergic blockade: propranolol versus esmolol. Hirshman, CA; Sauder, RA; Tobias, JD, 1990) | 0.92 |
" Prazosin produced a dose-response decrease in EAD amplitude and reduced the prevalence of VT." | ( Alpha-adrenoceptor stimulation and blockade modulates cesium-induced early afterdepolarizations and ventricular tachyarrhythmias in dogs. Ben-David, J; Zipes, DP, 1990) | 0.28 |
" In I, four cumulative noradrenaline (NA) dose-response curves (10(-9) to 10(-3) M) were constructed." | ( Reversal of alpha-adrenoceptor blockade by propranolol in isolated rat pulmonary artery. Abdelrahman, A; Nguyen, H; Pang, CC, 1990) | 0.54 |
" However, the dose-response curves to phentolamine and the alpha-2 adrenoceptor agonist UK 14,304 on stimulus-induced overflow from the kidney were not significantly different after NE treatment." | ( Effects of chronic norepinephrine administration on sympathetic neurotransmission in the isolated perfused rat kidney. Eikenburg, DC, 1990) | 0.28 |
" Addition of (+)-propranolol to nonoxynol-9 shifted the dose-response curve to the left of the curves for either component alone, and a surprising synergistic action was evident." | ( Comparative effects of (+)-propranolol and nonoxynol-9 on human sperm motility in-vitro. Curtis-Prior, PB; Gadd, AL, 1990) | 0.92 |
"5 mM (+)- propranolol to nonoxynol-9, the dose-response curve moved to the left of the curves for either (+)-propranolol and nonoxynol-9 alone." | ( Comparative effects of (+)-propranolol and nonoxynol-9 on human sperm motility in-vitro. Curtis-Prior, PB; Gadd, AL, 1990) | 0.98 |
"We have investigated the effects of 8-OH-DPAT in the mouse isolated vas deferens preparation and found it to possess a biphasic (initial inhibition followed by potentiation) dose-response curve." | ( Dopamine agonist activity of 8-OH-DPAT. Cutts, S; Smith, CF, ) | 0.13 |
" Findings show that timing recommendations for dosing in relation to meals are not considered in these institutions when drug administration schedules are established." | ( Drug administration in relation to meals in the institutional setting. Kinder, S; Lubischer, A; Strong, A; Wolff, H, 1991) | 0.28 |
" Characteristic dose-response curves for acetylcholine showing greater negative inotropic response with dose were seen." | ( The effects of AF-DX 116, a cardioselective muscarinic antagonist, on the negative inotropic action of acetylcholine. Baskin, SI; Thomsen, RH, 1991) | 0.28 |
" Daily dosage was determined by the administration of progressively increasing doses of propranolol with the hepatic vein catheter in place to achieve a 25% decrease in hepatic venous pressure gradient, a decrease in hepatic venous pressure gradient to less than 12 mm Hg or a decrease in resting heart rate to less than 55 beats/min." | ( Propranolol in the prevention of the first hemorrhage from esophagogastric varices: A multicenter, randomized clinical trial. The Boston-New Haven-Barcelona Portal Hypertension Study Group. Bosch, J; Conn, HO; Fisher, RL; Garcia-Tsao, G; Grace, ND; Groszmann, RJ; Matloff, DS; Navasa, M; Rodés, J; Wright, SC, 1991) | 1.95 |
" In a double-blind dose-finding study, 58 patients were treated in five consecutive dosage steps each lasting 1-3 months." | ( Responders and non-responders to metoprolol, propranolol and nifedipine treatment in migraine prophylaxis: a dose-range study based on time-series analysis. Diener, HC; Gerber, WD; Niederberger, U; Scholz, E, 1991) | 0.54 |
" However, a dose-response curve to methacholine is helpful." | ( Characteristics of bronchial hyperresponsiveness in chronic obstructive pulmonary disease and in asthma. Anderson, SD; Du Toit, JI; Peat, JK; Salome, CM; Smith, CM; Woolcock, AJ; Zhang, YG, 1991) | 0.28 |
"Responsiveness to inhaled histamine and DL propranolol hydrochloride was measured in 31 adult asthmatics and compared with bronchoconstriction provoked by acute oral propranolol dosing (max 160 mg)." | ( Bronchoconstriction of the asthmatic airway by inhaled and ingested propranolol. Latimer, KM; Ruffin, RE, 1990) | 0.78 |
" After an initial placebo phase, 40 mg d-propranolol was administered orally every 6 h with dosage increased every 2 d until arrhythmia suppression (greater than or equal to 80% VED reduction), intolerable side effects, or a maximal dosage (1,280 mg/d) was reached." | ( Suppression of ventricular arrhythmias in man by d-propranolol independent of beta-adrenergic receptor blockade. Barbey, JT; Koshakji, RP; Lineberry, MD; Murray, KT; Reilly, C; Roden, DM; Siddoway, LA; Wood, AJ; Woosley, RL, 1990) | 0.8 |
" No change in slope of the phenylephrine dose-response curve was noted; however, consistent with the dose ratio, verapamil shifted the curve to the right with a decrease in the y intercept determined by linear regression (60." | ( Forearm vascular alpha 1-adrenergic blockade by verapamil. Abernethy, DR; Winterbottom, LM, 1990) | 0.28 |
" Patients were chosen randomly to receive oral propranolol (in a dosage to reduce resting pulse rate by 25%) or to undergo long-term injection sclerotherapy." | ( A controlled trial of oral propranolol compared with injection sclerotherapy for the long-term management of variceal bleeding. Gimson, AE; Hayes, PC; Hayllar, K; Polson, RJ; Westaby, D; Williams, R, 1990) | 0.83 |
" Under a single dosage regimen, subjects were administered either a single capsule containing controlled release propranolol equivalent to 160 mg of the drug or 80 mg of conventional propranolol tablet, twelve hourly." | ( Pharmacokinetic evaluation of conventional and controlled release dosage form of propranolol. Chattaraj, SC; Das, SK, 1990) | 0.72 |
" In potassium loaded, ureter-ligated dogs, heparin increases transmembrane potassium transfer as effectively as does a dosage of atropine large enough to cross the blood-brain barrier and its influence on potassium transfer, like that of atropine, is suppressed by beta-adrenoreceptor blockade." | ( Heparin mediates transmembrane potassium transfer in hyperkalemic dogs. Hiatt, JR; Hiatt, N, 1990) | 0.28 |
" The results suggest that metoprolol can be safely used and offers the advantages of desired clinical response, shorter preoperative preparation time, simplicity of dosage and shorter postoperative hospital stay in comparison to propranolol for preoperative treatment of hyperthyroidism." | ( The role of selective beta 1-blocker in the preoperative preparation of thyrotoxicosis: a comparative study with propranolol. Arya, R; Garg, KM; Godha, U; Jain, S; Mathur, P; Vickers, P, ) | 0.53 |
"The influence of sustained absorption on the oral availability of propranolol (P) and the metabolic disposition of P were investigated by obtaining the partial metabolic clearances (CLm) following long-acting P (LA) dosing in comparison with the conventional propranolol tablet (CP)." | ( Decreased absorption as a possible cause for the lower bioavailability of a sustained-release propranolol. Kashiwada, K; Ogata, H; Ohira, M; Someya, K; Takahashi, H; Warabioka, R, 1990) | 0.74 |
" These effects have different dose-response relationships." | ( Acute and chronic effects of propranolol on extinction of rewarded running in the rat. Salmon, P; Terry, P; Wray, N, 1990) | 0.57 |
" Dose-response curves for negative chronotropic action of adenosine in the sinus node and ventricular pacemakers were obtained in group 1 under base-line conditions, during isoproterenol infusion, and after subsequent administration of propranolol; in group 2 before and after administration of quinidine; in group 3 before and after administration of aminophylline; and in group 4 before and after administration of 1,3-dipropyl-8-phenylxanthine amine congener (XAC)." | ( Differential sensitivity of cardiac pacemakers to exogenous adenosine in vivo. Dreifus, LS; Hurt, C; Michelson, EL; Miyagawa, A; Pelleg, A, 1990) | 0.46 |
"In the smooth muscle of the rat vas deferens, 10(-5) M cocaine shifted the dose-response curve to norepinephrine to the left and enhanced the maximal contractions to norepinephrine and methacholine." | ( Propranolol blocks cocaine-induced potentiation of the contraction in the smooth muscle of the rat vas deferens. Gomi, Y; Inagaki, O; Kasuya, Y; Ono, K; Suzuki, N, 1990) | 1.72 |
" However, following 3-6 months of sustained treatment a proportion of patients required an increase in daily dosage of propranolol in order to maintain adequate symptomatic control of tremor, indicating a relative decrease in tremorolytic efficacy of the drug possibly due to long-term tolerance." | ( Clinical and computer-based assessment of long-term therapeutic efficacy of propranolol in essential tremor. Baratti, M; Calzetti, S; Fava, R; Sasso, E, 1990) | 0.72 |
" 2) No significant correlation between dosage and serum concentration of propranolol was observed, and the effective serum concentrations of propranolol were found to be different on each individual." | ( [A medical treatment of esophageal varices by propranolol]. Kimura, K; Ueno, N; Yamanaka, T, 1990) | 0.77 |
" Dose-response curves were constructed both for the autonomic agonists and the histamine-releasing agents." | ( Characterization of purified dog mastocytoma cells. Autonomic membrane receptors and pharmacologic modulation of histamine release. Barnes, PJ; Gold, WM; Phillips, MJ, 1985) | 0.27 |
" Propranolol also inhibited contractions to Ca in high K-containing solution and shifted the dose-response curve to the right." | ( Inhibitory action of propranolol on the contractions induced by nerve stimulations or calcium in the smooth muscle of rat vas deferens. Inagaki, O; Kasuya, Y; Suzuki, N, 1986) | 1.5 |
" In dose-response curves, the isoproterenol-sensitive K+ efflux was half-maximally inhibited (IC50) with 2-5 X 10(-10) M of isoproterenol concentration." | ( Stimulation of beta-adrenoceptors inhibits calcium-dependent potassium-channels in mouse macrophages. Braquet, P; Dausse, JP; Garay, R; Hannaert, P; Rosati, C, 1986) | 0.27 |
" When dosing regimens that produced stable plasma levels of both drugs were used, the observed effects were closely related to the plasma concentrations of the individual agents." | ( Nifedipine-propranolol interaction: dependence of cardiovascular effects on plasma drug concentrations. Hamann, SR; Kaltenborn, KE; McAllister, RG, 1987) | 0.66 |
" Ventricular function as assessed by echocardiography during drug dosing showed no significant changes from placebo." | ( Comparison of ethmozine to propranolol and the combination for ventricular arrhythmias. Butman, SM; Gardin, JM; Knoll, ML, 1987) | 0.57 |
" Isoprenaline potency was increased by the sheep fat-supplemented diet, which induced significant three- to eightfold leftward parallel shifts of isoprenaline dose-response curves for papillary muscle and left atrial inotropy and right atrial chronotropy." | ( Dietary lipid modulation of myocardial beta-adrenergic mechanisms, Ca2+-dependent automaticity, and arrhythmogenesis in the marmoset. Abeywardena, MY; Charnock, JS; McLennan, PL; McMurchie, EJ, 1987) | 0.27 |
" However, the dose-response curves of salbutamol on the venous and arterial systems overlapped, indicating that the increase in venous return represents a combination of properties common to both beta 1 and beta 2 adrenoceptors." | ( Dopamine and norepinephrine increase venous return by stimulating alpha and beta adrenoceptors in the dog. Banning, JW; Morgan, JP; Roebel, LE; Van Maanen, EF, 1988) | 0.27 |
" After a control period of 10 days, NTP was started with 20 mg twice a day and titrated to the maximal dosage of 2 X 40 mg/day." | ( Nitrendipine treatment in so-called therapy-resistant arterial hypertension; effect as monotherapy and in combination with propranolol on blood pressure, heart rate, other hemodynamic parameters, plasma renin activity, and catecholamines. Faulhaber, HD; Gruner, R; Hartrodt, W; Homuth, V; Menz, M; Mohnike, W; Naumann, E; Schmidt, J, 1988) | 0.48 |
" Dosage of each agent was titrated to achieve optimal clinic BP control and this dose was maintained for the duration of the study." | ( The efficacy and duration of action of sustained-release verapamil in essential hypertension. Atkins, N; Latham, AN; McCormack, PM; Mee, F; O'Brien, ET; O'Malley, K, 1989) | 0.28 |
" The dose-response curve for this action is comparable to that of propranolol." | ( Cellular electrophysiology and beta-adrenergic-blocking activity of dilevalol, the R,R-isomer of labetalol, on isolated canine cardiac tissues. Dangman, KH; Zaim, S, 1989) | 0.51 |
" Dose-response experiments revealed that insulin stimulated D-glucose transport and 2-deoxyglucose uptake between 10(-11) and 10(-7) M with a maximal four- to sixfold stimulation." | ( Stimulation of glucose transport by insulin and norepinephrine in isolated rat brown adipocytes. Bukowiecki, LJ; Marette, A, 1989) | 0.28 |
" Methacholine dose-response curves (10(-11) to 10(-7) mol iv) obtained at the conclusion of the experiments were similar among capsaicin, phosphoramidon, and control groups." | ( Tachykinins mediate bronchoconstriction elicited by isocapnic hyperpnea in guinea pigs. Drazen, JM; Hernandez, C; Leff, AR; Ray, DW; Solway, J, 1989) | 0.28 |
" BWA1433U induced a parallel shift of the adenosine dose-response curve to the right; however, it had no significant inhibitory effect on the decrease in lobar arterial pressure in response to ATP." | ( Adenosine does not mediate the pulmonary vasodilator response of adenosine 5'-triphosphate in the feline pulmonary vascular bed. Hyman, AL; Kadowitz, PJ; Lippton, H; Neely, CF; Neiman, M, 1989) | 0.28 |
" Myocardial fibrosis, on the other hand, appears to be more closely related to myocyte necrosis with respect to collagen accumulation in the same areas of the heart, its dose-response relation to the amount of isoproterenol administered, and the timing of increased DNA synthesis, or fibroblast proliferation, after myocyte loss." | ( Isoproterenol-induced myocardial fibrosis in relation to myocyte necrosis. Benjamin, IJ; Cho, K; Clark, WA; Jalil, JE; Tan, LB; Weber, KT, 1989) | 0.28 |
"To determine the role of changes in receptor density and the considerable interindividual variability in the response to beta-adrenergic antagonists, we determined the relationship between the beta-blockade produced by propranolol and the beta-adrenergic receptor density (Bmax) in 16 healthy subjects who received 10, 20, 40, and 80 mg propranolol every 8 hours for 1 day at each dosage level." | ( Interindividual differences in beta-receptor density contribute to variability in response to beta-adrenoceptor antagonists. Koshakji, RP; Silberstein, DJ; Wood, AJ; Zhou, HH, 1989) | 0.46 |
" Comparison with dose-response curves in a group of young (Y) subjects (24 +/- 3 years) given an identical dose protocol of salbutamol showed no evidence of subsensitivity of beta 2-adrenoceptor responses in the elderly (E) group (mean and 95% confidence intervals for maximum responses): delta K -0." | ( Beta-adrenoceptor responses to inhaled salbutamol in the elderly. Lipworth, BJ; McDevitt, DG; Tregaskis, BF, 1989) | 0.28 |
" ICI 147,798 produced a dose-dependent shift to the right of the dose-response (chronotropic) curve of isoproterenol with suppression of the maximal tachycardia, an effect characteristic of insurmountable beta receptor blockade." | ( Insurmountable beta receptor blockade by ICI 147,798 in rabbits. Giles, RE; Hwang, TF; Kau, ST; Keith, RA; Murthy, VS; Salama, AI; Wurm, R; Zagar, ME, 1989) | 0.28 |
" Doses were calculated to produce plasma levels approximating those achieved after oral dosing (0." | ( Effects of dilevalol on forearm circulation in essential hypertension. Cleroux, J; Giannattasio, C; Grassi, G; Mancia, G; Seravalle, G; Zanchetti, A, 1989) | 0.28 |
" Atenolol, ICI 111,581 and propranolol were given at low, medium and high doses calculated to shift dose-response curves to exogenous agonists by factors of 10-30, 100-300 and 1000-3000, respectively." | ( Mechanisms underlying the antiarrhythmic properties of beta-adrenoceptor blockade against ischaemia-induced arrhythmias in acutely prepared rats. Abraham, S; Beatch, GN; Paletta, MJ; Walker, MJ, 1989) | 0.57 |
" Dose-response curves (DRCs) were obtained in the absence and cumulative presence of propranolol (PROP; beta-antagonist), corynanthine (CORY; alpha 1-antagonist) and idazoxan (IDX; alpha 2-antagonist) to estimate effective dosages (ED) required for 15 and 75% peak reductions in renal blood flow." | ( Unmasking sensitive alpha 2-adrenoceptor-mediated renal vasoconstriction in conscious rats. Colindres, RE; Strandhoy, JW; Wolff, DW, 1989) | 0.5 |
" On a dosage basis, the order of potency of these compounds is indenolol fluorinated derivative greater than propranolol greater than indenolol greater than nadolol fluorinated derivative greater than nadolol." | ( Evaluation of the antifibrillatory activity of fluorinated derivatives of indenolol and nadolol in isolated rabbit and rat hearts: comparison with propranolol. Aboul-Enein, HY; Almotrefi, AA; Premkumar, LS, ) | 0.54 |
" By contrast, carbachol did not alter the dose-response profile to AR-L57." | ( A comparison of the cardiotonic effects of AR-L115 and AR-L57: evidence for distinct inotropic mechanisms. Hayes, JS; Pollock, GD; Wilson, H; Wyss, VL, ) | 0.13 |
" Each drug was given for a two-month period, the maximum acebutolol dosage reaching 600 mg tid and the maximum propranolol dosage 80 mg tid." | ( Comparison of acebutolol and propranolol therapy for ventricular arrhythmias. Berdoff, R; Platia, EV; Reid, PR; Stone, G, 1985) | 0.77 |
" Dose-response curves with epinephrine (alpha 2 and beta agonist), with isoproterenol (beta agonist) and epinephrine + propranolol and adenosine deaminase, were studied." | ( Lipolytic response of adipocytes to epinephrine in sedentary and exercise-trained subjects: sex-related differences. Beauville, M; Crampes, F; Garrigues, M; Marceron, M; Riviere, D, 1989) | 0.49 |
"The pharmacokinetic and pharmacodynamic studies of four different brands of propranolol (Inderal, Ciplar, Corbeta and Propal) were carried out after single and multiple dosing on six normal adult healthy volunteers in a randomized crossover fashion to determine any inter-brand variations in bioavailability and pharmacodynamic effects." | ( Comparative pharmacokinetic and pharmacodynamic study of four different brands of propranolol in normal volunteers. Biswas, NR; Garg, SK; Kumar, N; Mukherjee, S; Sharma, PL, 1989) | 0.73 |
" Despite inter-individual variations in the dose-response relationships calculated for both hormones, significant effects can be expected in the upper physiological range of concentration." | ( Inhibition of human lecithin: cholesterol acyltransferase activity by catecholamines in vitro. Schauer, I; Schauer, UJ, 1989) | 0.28 |
" Examination of diastolic blood pressures suggested some loss of antihypertensive control at the end of the dosing interval." | ( Once-daily propranolol for hypertension: a comparison of regular-release, long-acting, and generic formulations. Carter, BL; Gersema, LM; Schabold, K; Williams, GO, 1989) | 0.67 |
" Although some patients remained normotensive after discontinuation of step II drugs, a greater proportion returned to elevated BP than when step II dosage was unchanged." | ( Effects of reduction in drugs or dosage after long-term control of systemic hypertension. Borreson, RE; Fisher, SG; Freis, ED; Hamburger, R; Mezey, KC; Mukherji, B; Neal, WW; Perry, HM; Taguchi, JT; Thomas, JR, 1989) | 0.28 |
" This was associated with airway beta-adrenoceptor blockade as demonstrated by a shift in the isoproterenol dose-response curve." | ( Anticholinergic blockade of beta-blocker-induced bronchoconstriction. Barnes, PJ; Dixon, CM; Fuller, RW; Ind, PW, 1989) | 0.28 |
" However, none of the treatments studied was ideal for clinical use in the twice daily dosage used in this study." | ( Comparison of the efficacy and acceptability of nicardipine and propranolol, alone and in combination, in mild to moderate hypertension. Dow, RJ; Gough, KJ; Laing, EM; Macdonald, FC; Maclean, D; McDevitt, DG; Mitchell, ET, 1989) | 0.52 |
" This difference in drug efficacy persisted throughout the 12-hour dosing interval." | ( Discrepancy between clinic and ambulatory blood pressure measurement in the evaluation of two antihypertensive agents. Cox, JP; Fitzgerald, DJ; O'Brien, E; O'Malley, K, 1989) | 0.28 |
" F = 1 - VmVd/kaD ln (1 + kaD/QKm) This equation for single dosage can also be extended to steady state kinetics after multiple dosing in which the amount of a drug present in the hepatic circulation is considered." | ( Saturable first-pass kinetics of propranolol. Haller, H; Keller, F; Kunzendorf, U; Offermann, G; Walz, G, 1989) | 0.56 |
"A novel oral multiple-unit dosage form which overcame many of the problems commonly observed during the compression of microparticles into tablets was developed in this study." | ( A novel approach to the oral delivery of micro- or nanoparticles. Bodmeier, R; Chen, HG; Paeratakul, O, 1989) | 0.28 |
"8 mM), the dose-response curve for ATP was shifted to the left in a parallel fashion at this concentration." | ( Low calcium and calcium antagonists potentiate the contraction of guinea-pig vas deferens induced by ATP: a permissive role for P2-purinoceptors. Furukawa, T; Morishita, H, 1989) | 0.28 |
" Treadmill exercise testing was performed, 24-hour ambulatory electrocardiograms were recorded, and serum propranolol levels were assessed at 1 and 2 hours after dosing with propranolol alone, and after 2 weeks of combined therapy with either nifedipine, 10 or 20 mg, or diltiazem, 60 or 120 mg, administered every 8 hours." | ( Comparative study of the effect of nifedipine versus diltiazem on exercise performance, serum propranolol levels, and ST-segment abnormalities in patients with chronic stable angina taking propranolol. Krikler, DM; Krikler, S; Robinson, K, 1989) | 0.71 |
" In contrast, propranolol shifted the caffeine dose-response curve to the right and significantly increased the caffeine threshold in the MHS group." | ( Influence of propranolol on the in vitro response to caffeine and halothane in malignant hyperthermia-susceptible muscle. Ording, H, 1989) | 1.01 |
"vg-dosed animals than their oral dosed counterparts." | ( A comparative study of the pharmacokinetics of propranolol and its major metabolites in the rat after oral and vaginal administration. Buttar, HS; Qureshi, SA, 1989) | 0.53 |
" Dose-response curves revealed that maximal hyperglycemia was associated with hypoinsulinemia." | ( 5-HT1A and alpha-2 adrenergic receptors mediate the hyperglycemic and hypoinsulinemic effects of 8-hydroxy-2-(di-n-propylamino)tetralin in the conscious rat. Chaouloff, F; Jeanrenaud, B, 1987) | 0.27 |
" From the right shifts of isoprenaline dose-response curves 0 to 84 hr after administration of propranolol and the beta-1 selective bisoprolol, in vivo beta blockade was assessed." | ( Beta adrenoceptor subtype binding activity in plasma and beta blockade by propranolol and beta-1 selective bisoprolol in humans. Evaluation with Schild-plots. Belz, GG; Palm, D; Wellstein, A, 1988) | 0.72 |
"0 mg/kg intravenously) was administered after the highest phenylephrine infusion dosage to assure complete beta-blockade." | ( In vivo demonstration of maturational changes of the chronotropic response to alpha-adrenergic stimulation. Gelband, H; McCormack, J; Pickoff, AS; Stolfi, A; Villafañe, J; Xu, H, 1988) | 0.27 |
" Ethanol also shifted the dose-response curve for stimulation of the enzyme by isoproterenol to the right." | ( Effects of ethanol in vitro on the beta adrenergic receptor-coupled adenylate cyclase system. Bode, DC; Molinoff, PB, 1988) | 0.27 |
" Propranolol and labetalol induced a dose-dependent, parallel shift to the right in the dose-response curves of isoproterenol effects on heart rate and diastolic blood pressure, indicating that both drugs are nonselective, competitive antagonists of beta-adrenergic receptors." | ( Beta blockade by oral propranolol and labetalol. Carr, ME; Cubeddu, LX; Fuenmayor, NJ, 1985) | 1.49 |
" However, as dosage adjustment and close observation may be necessary to minimise side effects, the use of this combination should be limited to hospital practice." | ( Tolerability of combined treatment with verapamil and beta-blockers in angina resistant to monotherapy. McGourty, JC; Silas, JH; Solomon, SA, 1985) | 0.27 |
" Methoxamine produced a dose-related increase in uterine activity, prazosin produced a rightward displacement of the dose-response curve of methoxamine reaching the same maximal effect." | ( Effect of methoxamine on spontaneous motility of the isolated rat uterus. Esplugues, J; Estañ, L; Morales-Olivas, FJ; Rubio, E, 1985) | 0.27 |
" In most cases the dose-response curves were biphasic and changes in coronary flow paralleled those in oxygen consumption." | ( The effect of cholinergic agonists on coronary flow rate and oxygen consumption in isolated perfused rat heart. Erecińska, M; Nuutinen, EM; Wilson, DF, 1985) | 0.27 |
" Labetalol 400 mg significantly shifted the blood pressure dose-response curve to the right." | ( Comparative effects of adimolol, labetalol and propranolol on heart rate and blood pressure in man. Harron, DW; Riddell, JG; Shanks, RG, 1985) | 0.53 |
" If standard doses of beta-blockers are used in PM subjects, they may be susceptible to concentration-related adverse reactions and they may also require lower and less frequent dosing for control of angina pectoris." | ( Oxidation phenotype and the metabolism and action of beta-blockers. Lennard, MS, 1985) | 0.27 |
" The dose-response kinetics with four doses of bethanechol with and without somatostatin showed inhibition of a non-competitive type for gastric acid secretion and of a competitive type for antral motility with regard to amplitude." | ( Effect of somatostatin on bethanechol-stimulated gastric acid secretion and gastric antral motility in dogs with gastric fistula. Andersen, D; Bech, K; Ladegaard, L, 1985) | 0.27 |
" dosage (1." | ( Effect of age on the hepatic clearance of propranolol in rats. Araki, K; Deguchi, N; Iwamoto, K; Sugiyama, H; Watanabe, J, 1985) | 0.53 |
"25 mg/kg), the dose-response curve of clenbuterol (0." | ( Does a single priming injection of clenbuterol alter behavioral response to beta-adrenoceptor agonists and antagonists in mice through a time-dependent process? Martin, P; Simon, P; Soubrie, P, 1985) | 0.27 |
" We investigated whether the maximal response plateau or the position of the dose-response curve is due to functional inhibition by neurogenic mechanisms or to prostaglandin release." | ( Limited maximal airway narrowing in nonasthmatic subjects. Role of neural control and prostaglandin release. Daniel, EE; Hargreave, FE; Sterk, PJ; Zamel, N, 1985) | 0.27 |
" Dose-response curves were constructed for the changes in these parameters with increasing doses of isoproterenol." | ( Effects of betaxolol, propranolol, and atenolol on isoproterenol-induced beta-adrenoceptor responses. Riddell, JG; Shanks, RG, 1985) | 0.58 |
"In series of 20 patients suffering from atrial arrhythmias, hypertension or hyperkinetic heart syndrome in euthyroid subjects the effect of the new cardioselective beta-blocker celiprolol was examined when orally administered in doses of 300 mg per day against propranolol in a dosage of 160 mg per day." | ( [Effect of celiprolol compared to propranolol on thyroid metabolism]. Eber, O; Langsteger, W; Lind, P, 1985) | 0.73 |
" Isoproterenol dose-response curves were shifted significantly downward and to the right after previous treatment with and removal of isoproterenol." | ( Isoproterenol-induced desensitization to the positive inotropic effect of isoproterenol in ventricular strips isolated from carp heart (Cyprinus carpio). Hirata, T; Kitazawa, T; Kondo, H; Temma, K, 1985) | 0.27 |
" Studies of right ventricular papillary muscles from control and chronically beta-blocked cats demonstrated contractile and energetic properties as well as dose-response behavior and inotropic specificity suggestive of an increase in myocardial sensitivity to beta-adrenoceptor stimulation in the latter group." | ( Beta adrenergic receptor blockade of feline myocardium. Cardiac mechanics, energetics, and beta adrenoceptor regulation. Cooper, G; Kent, RL; McGonigle, P; Watanabe, AM, 1986) | 0.27 |
" The dose-response curves of dilevalol and labetalol were shifted to the right with propranolol pretreatment." | ( Intrinsic beta-sympathomimetic activity of dilevalol, R, R-isomer of labetalol. Matsunaga, K; Nakamura, K; Ueda, M, 1985) | 0.49 |
" If standard doses of beta-blockers are used in poor metabolisers, these subjects may be susceptible to concentration-related adverse reactions and they may also require less frequent dosing for control of angina pectoris." | ( The polymorphic oxidation of beta-adrenoceptor antagonists. Clinical pharmacokinetic considerations. Lennard, MS; Tucker, GT; Woods, HF, ) | 0.13 |
"A double-blind randomized study was designed to investigate differences in the recovery of finger skin temperature after finger cooling during dosing with placebo or one of four beta-blockers: propranolol, atenolol, pindolol, and acebutolol." | ( The influence of intrinsic sympathomimetic activity and beta-1 receptor selectivity on the recovery of finger skin temperature after finger cooling in normotensive subjects. de Boo, T; Lemmens, WA; Lenders, JW; Salemans, J; Thien, T; van't Laar, A, 1986) | 0.46 |
" The dose-response curve for stimulation by histamine of adenylate cyclase was shifted to the right in a dose-dependent manner by increasing concentrations of several H2-antagonists." | ( A study of the H2-receptor for histamine stimulating adenylate cyclase in homogenates of guinea-pig lung parenchyma. Foreman, JC; Norris, DB; Rising, TJ; Webber, SE, 1986) | 0.27 |
" Dose-response curves were constructed for the changes in heart rate, finger tremor, blood pressure and forearm blood flow produced by each infusion." | ( Effects of ICI 141,292 on exercise tachycardia and isoprenaline-induced beta-adrenoceptor responses in man. Finch, MB; McNeill, AJ; O'Connor, PC; Pringle, TH; Riddell, JG; Shanks, RG, 1986) | 0.27 |
"05) the dose-response curve of 5-HT at the autoreceptors, but was ineffective at the receptors regulating GLU release." | ( Differential pharmacology and function of two 5-HT1 receptors modulating transmitter release in rat cerebellum. Bonanno, G; Maura, G; Pittaluga, A; Raiteri, M, 1986) | 0.27 |
" Amitraz did not significantly shift the dose-response curve to isoprenaline or acetylcholine but antagonized histamine rate responses competitively in the presence of propranolol (2 X 10(-6) M)." | ( The cardiac effects of amitraz in the guinea-pig in vivo and in vitro. Pascoe, AL; Reynoldson, JA, 1986) | 0.47 |
" The latter interventions, when imposed between successive dose-response curves generated by intravenous 5HT in animals pretreated with atropine and propranolol, did not alter the positions or slopes of the curves." | ( Reflex activation of the nonadrenergic noncholinergic inhibitory nervous system in feline airways. Altiere, RJ; Diamond, L; Gillespie, MN; Szarek, JL, 1986) | 0.47 |
" PRA activity was significantly and markedly reduced by both bunolol and metoprolol shortly after dosing at a time when HR was significantly reduced but MBP was not." | ( Antihypertensive effects of 12 beta adrenoceptor antagonists in conscious spontaneously hypertensive rats: relationship to changes in plasma renin activity, heart rate and sympathetic nerve function. Antonaccio, MJ; DeForrest, JM; High, J; Sybertz, E, 1986) | 0.27 |
" If standard doses of some beta-blockers are used in poor metabolizers, these patients may be susceptible to concentration-related adverse reactions and they may also require lower and less frequent dosing for control of angina pectoris." | ( Debrisoquine polymorphism and the metabolism and action of metoprolol, timolol, propranolol and atenolol. Lennard, MS; Silas, JH; Tucker, GT; Woods, HF, 1986) | 0.5 |
" (+/-)-Propranolol caused rightward shifts, usually parallel, of the dose-response curves for (-)-isoprenaline." | ( The antinociceptive action of some beta-adrenoceptor agonists in mice. Bentley, GA; Starr, J, 1986) | 0.73 |
" The reaction patterns were similar for isoprenaline and somatostatin, whereas salmefamol induced an inhibition of longer duration and with dissimilar dose-response kinetics." | ( Beta-adrenergic agonists inhibit gastric acid and pepsin secretion through somatostatin release in dogs. Bech, K; Uvnäs-Moberg, K, 1986) | 0.27 |
" The dose-response relationship using individual maximal reduction of ET showed, on a molar basis, that bisoprolol is about 5, 7 and 10 times more effective than propranolol, atenolol and metoprolol, respectively." | ( Pharmacodynamic profile of bisoprolol, a new beta 1-selective adrenoceptor antagonist. Bühring, KU; Leopold, G; Pabst, J; Simane, Z; Ungethüm, W; Wiemann, H, 1986) | 0.47 |
"The dose-response curves of the central and peripheral airways to intravenously injected nicotine were studied in 55 anesthetized dogs." | ( Dose-response curves of central and peripheral airways to nicotine injections in dogs. Haga, T; Miyano, M; Nakamura, M; Sasaki, H; Takishima, T, 1986) | 0.27 |
"We compared the central and renal haemodynamic effects of tertatolol, a new non-cardioselective beta-adrenergic blocking drug without partial agonist activity, with those of an equipotent dosage of propranolol in two groups of 10 patients each with acute cerebral injury who had developed systemic hypertension." | ( Acute central and renal haemodynamic responses to tertatolol and propranolol in patients with arterial hypertension following head injury. Brackman, F; Degaute, JP; Leeman, M; Naeije, R; Prost, JF, 1986) | 0.7 |
" Its central and renal hemodynamic effects were compared to those of an equipotent dosage of propranolol in two groups of 10 patients each who developed arterial hypertension and a hyperdynamic circulatory state after head injury." | ( Tertatolol preserves renal perfusion in patients with arterial hypertension after head injury. Brackman, F; Degaute, JP; Leeman, M; Naeije, R; Prost, JF; Thomas, J, 1986) | 0.49 |
" Propranolol 5 mg iv, the positive control, significantly shifted the isoproterenol dose-response curve to the right." | ( The assessment of the beta-blocking activity of urapidil: a new method. Flanagan, PH; Galbraith, H; Jackson, SH; Jamieson, MJ; Patel, SS; Shepherd, AM; Stewart, W, 1986) | 1.18 |
" Intrapericardial propranolol or atenolol (50 micrograms/kg) had the same effect on isoprenaline heart rate dose-response curves and on the sympathetic component of the arterial baroreceptor-heart rate reflex as did conventional, 5-fold greater, intravenous doses of the drugs." | ( Selective manipulation of neurohumoral control of the cardiac pacemaker by drugs given intrapericardially. Lew, MJ; Ludbrook, J; Pavia, JM; Quail, AW; Rutter, PC, 1987) | 0.61 |
"Thirty-six patients with Raynaud's disease (RD) were treated with a low dosage of beta-blockers, atenolol (50 mg/day) or propranolol (20 mg/day)." | ( Beta-blockers: a new therapeutic approach to Raynaud's disease. Brotzu, G; Palmina, P; Roberto, M; Susanna, F, 1987) | 0.48 |
" In addition, adimolol significantly reduced receptor number and even by 3 days after dosing Bmax had only returned to half the control value." | ( Adimolol, a long acting beta-adrenoceptor blocker in man. Deighton, NM; Elliott, HL; Jones, CR; Meredith, PA; Reid, JL, 1987) | 0.27 |
" In contrast, the (R)-glycol appeared to act as an irreversible antagonist, producing complex dose-response curves." | ( Comparative studies with the enantiomers of the glycol metabolite of propranolol and their effects on the cardiac beta-adrenoceptor. Lyles, GA; Neilson, DG; Ogg, GD; Stevenson, IH, 1987) | 0.51 |
" 3 Propranolol, but not domperidone, shifted to the right the dose-response curve for the positive inotropic and chronotropic effects of dopamine." | ( The lack of the effect of DA-1 and DA-2 dopamine agonists on the isolated guinea-pig atria. Martinez-Mir, I; Morales-Olivas, FJ; Rubio, E, 1987) | 0.89 |
" In order to mimic the intrinsic effects of the partial agonist drugs, control dose-response curves for isoproterenol were determined in pithed rats in which the base-line heart rate was elevated by thoracic spinal cord stimulation." | ( Comparative analysis of beta-1 adrenoceptor agonist and antagonist potency and selectivity of cicloprolol, xamoterol and pindolol. Cavero, I; Hicks, PE; Langer, SZ; Lefevre-Borg, F; Manoury, P, 1987) | 0.27 |
" Patients were treated with propranolol 40 to 160 mg bid for 8 weeks, followed by atenolol 50 to 100 mg given once daily for 8 weeks, and then rechallenged with the required dosage of propranolol for 8 weeks." | ( A comparison of the side effects of atenolol and propranolol in the treatment of patients with hypertension. Chockalingam, A; Drover, A; Fifield, F; Fodor, JG; Pauls, CJ, 1987) | 0.82 |
"Changes in systolic and diastolic blood pressure, heart rate, arterial blood flow and vascular resistance in the arm and in the leg were investigated in 9 healthy volunteers (22-40 years) after oral dosing with bisoprolol 10 mg, propranolol 40 mg, and placebo in a randomized double-blind cross-over study." | ( Effects of bisoprolol on local vascular resistance. Bailliart, O; Bonnin, P; Kedra, AW; Martineaud, JP; Savin, E, 1987) | 0.46 |
" These results suggest that propranolol in the above dosage does not significantly reduce the incidence of supraventricular tachyarrhythmias after myocardial revascularisation." | ( Does low-dose propranolol reduce the incidence of supraventricular tachyarrhythmias following myocardial revascularisation? A clinical study. Bain, WH; Nashef, SA; Shafei, H; Turner, MA, 1988) | 0.93 |
" The results demonstrated a wide margin of safety for celiprolol over the recommended dosage range of 200 to 600 mg once daily." | ( Safety profile of celiprolol. Lamon, KD, 1988) | 0.27 |
" Blood pressure, ventricular rate, and echocardiographically determined ejection fraction, ejection time, and mean rate of circumferential fiber shortening (mVcf) were measured before dosing and at multiple time points during 10 hours after each dose, with subjects maintained in the supine position." | ( Pharmacodynamic comparison of L-bunolol with propranolol, metoprolol, and placebo. Bahrmann, H; Greenblatt, DJ; Labedzki, L; Ochs, HR, 1988) | 0.53 |
" In the first series of experiments cumulative dose-response curves for propranolol, atenolol and ICI 118,551, nonselective beta-, beta 1- and beta 2-selective antagonists, respectively, were constructed in rats subjected to a continuous intravenous infusion of phentolamine." | ( Pressor response to beta 1- and beta 2-blockers in conscious rats treated with phentolamine. King, KA; Pang, CC; Tabrizchi, R, 1988) | 0.51 |
" Dose-response studies (required to increase heart rate or systolic blood pressure by 25 beats/min and 20mm Hg, respectively) were performed with phenylephrine, angiotensin and isoprenaline after each drug, and placebo administration and the effects of physiological pressor stimuli were compared." | ( Vasodilating mechanism and response to physiological pressor stimuli of acute doses of carvedilol compared with labetalol, propranolol and hydralazine. Bompart, F; Graham, BR; Liu, JB; Prichard, BN; Tomlinson, B, 1988) | 0.48 |
" In Study I, 24 healthy volunteers were dosed with 4 x 10 mg test tablets, 1 x 40 mg test tablet, 4 x 10 mg Inderal tablets, and 40 mg of propranolol HCl in solution." | ( Bioavailability of propranolol hydrochloride tablet formulations: application of multiple dose crossover studies. Daniel, JE; Eldon, MA; Kinkel, AW; Latts, JR, ) | 0.66 |
" The muscarinic antagonist atropine, 1 microM, and the beta 2-adrenoceptor antagonist propranolol, 10 microM, had no effect on the dose-response curve for dimaprit-induced relaxation of the lung strip." | ( A study of the histamine H2-receptor mediating relaxation of the parenchymal lung strip preparation of the guinea-pig. Foreman, JC; Rising, TJ; Webber, SE, 1985) | 0.49 |
"The effect of celiprolol at a daily dosage of 300 mg (19 patients) was compared with that of propranolol at a daily dosage of 120 mg (14 patients) on peripheral blood flow of the calf and foot in a randomized double-blind trial." | ( [Comparative studies of the effect of a cardioselective and a noncardioselective beta-blocker on peripheral circulation in patients with arterial occlusive disease]. Klieber, M; Resch, F, 1986) | 0.49 |
"05) the dose-response curve of 5-HT." | ( Pharmacological characterization of release-regulating serotonin autoreceptors in rat cerebellum. Bonanno, G; Maura, G; Raiteri, M, 1986) | 0.27 |
" ANP produced dose-related coronary vasodilation with a threshold dosage of 2 ng/kg; a dosage of 2 micrograms/kg caused a 27 +/- 4% decrease in coronary vascular resistance." | ( Effects of atrial natriuretic peptide in the canine coronary circulation. Bache, RJ; Chen, DG; Dai, XZ; Schwartz, JS, 1988) | 0.27 |
" On the first day, a propranolol provocative dose producing a 20% change in FEV1 (PD20) was determined from the individual semilogarithmic dose-response curve." | ( Effect of vasoactive intestinal peptide (VIP) on propranolol-induced bronchoconstriction. Crimi, N; Mistretta, A; Oliveri, R; Palermo, B; Palermo, F; Polosa, R; Vancheri, C, 1988) | 0.85 |
" Dose-response curves were determined for either isoproterenol or dobutamine 30 min after treatment with hexamethonium (20mg/kg)." | ( Role of alpha-adrenergic receptors in the intrinsic inotropic selectivity of dobutamine in anesthetized dogs. Gorczynski, RJ; Shaffer, JE, 1985) | 0.27 |
" HA-1004 shifted the dose-response curve for CaCl2 to the right in a competitive manner in depolarized rabbit renal arterial strips." | ( Relaxation of vascular smooth muscle by HA-1004, an inhibitor of cyclic nucleotide-dependent protein kinase. Hidaka, H; Inagaki, M; Ishikawa, T; Watanabe, M, 1985) | 0.27 |
" Standardized dose-response curves demonstrated that the injured tissue was increasingly sensitive over time to norepinephrine and that this was more marked at physiologic levels of norepinephrine." | ( Increased vascular contraction and sensitivity to norepinephrine after endothelial denudation is inhibited by prazosin. Cole, CW; Hagen, PO; McCann, RL; Mikat, EM; O'Malley, MK; Radic, ZS, 1986) | 0.27 |
" B-HT 933 did not affect the cumulative dose-response curves of the vas deferens and of MP-LM to noradrenaline (NA) and acetylcholine (Ach) respectively." | ( Mechanism of action of B-HT 933 (azepexole) in rat vas deferens and guinea-pig ileum. Brugger, AJ; Vargas, ML, 1985) | 0.27 |
"05), as was the slope of the angiotensin II-vehicle dose-response curve (0." | ( Dopamine selectively inhibits aldosterone responses to angiotensin II in humans. Carey, RM; Drake, CR, 1986) | 0.27 |
" With bolus injections, atropine displaced the heart rate dose-response curve for atenolol to the right, implying reflex withdrawal of cardiac vagal tone, but did not alter the heart rate dose-response curve for propranolol." | ( Reflex vagal withdrawal and the hemodynamic response to intravenous isoproterenol in the presence of beta-antagonists. Arnold, JM; McDevitt, DG, 1986) | 0.46 |
" After chronic withdrawal of TSH from the growth medium, the magnitude of the response to NE is considerably reduced; however, there is no substantial shift in the dose-response curve." | ( Norepinephrine and thyroid-stimulating hormone induce inositol phosphate accumulation in FRTL-5 cells. Alling, DW; Bone, EA; Grollman, EF, 1986) | 0.27 |
" Treatment of K loaded pancreatectomized dogs with glucagon or a B receptor blockading dosage of propranolol does not alter the proportion transferred, but treatment with glucagon and propranolol reduces it." | ( Kaluresis independent K-homeostasis: glucagon and B receptor blockade in pancreatectomized dogs. Chapman, LW; Davidson, MB; Hiatt, N; Mack, H, 1986) | 0.49 |
" Variations in drug dosage and feeding regimens will, however, need to be perfected to limit catabolic effects." | ( Effect of propranolol administration on hemodynamic and metabolic responses of burned pediatric patients. Barrow, RE; Herndon, DN; Jahoor, F; Minifee, P; Rutan, TC; Wolfe, RR, 1988) | 0.68 |
" Pretreatment of the rats with reserpine (5 mg/kg) did not produce any modification of the dose-response curve to dopamine." | ( Relaxant effect of dopamine on the isolated rat uterus. Estañ, L; Martinez-Mir, I; Morales-Olivas, FJ; Rubio, E, 1988) | 0.27 |
" It is concluded that at the dosage level used in this study propranolol and verapamil were equally effective, but there were individual variations in best response to one or the other of these two drugs." | ( [Comparative study of the effects of verapamil and propranolol therapy in 16 cases of obstructive hypertrophic myocardiopathy]. Casset, D; Cosnay, P; Fauchier, JP; Itti, R; Lang, M; Lavigne, G; Raynaud, P, 1987) | 0.77 |
" Isolated rings (circular preparations) obtained from rat thoracic aortae responded to increasing concentrations of NE with dose-dependent tonic enhancement, not significantly affected by the presence of indomethacin (10(-6)M); whereas, preincubation with phentolamine (10(-6)M), yohimbine (10(-7)M) or prazosin (10(-8)M), shifted significantly to the right points of the positive inotropic dose-response curve for NE." | ( Possible prostacyclin involvement on disparate tonic responses to "in vitro" norepinephrine in circular and in longitudinal preparations from rat thoracic aorta. Chaud, M; Franchi, AM; Gimeno, AL; Gimeno, MA, 1987) | 0.27 |
" The plasma concentrations of propranolol under these steady state dosing conditions increased when misoprostol was added to propranolol." | ( Potential drug interactions with misoprostol: effects on the pharmacokinetics of antipyrine and propranolol. Bennett, PN; Fenn, GC; Notarianni, LJ, 1988) | 0.78 |
" Dosage was titrated until blood pressures were normalized (diastolic blood pressure (DBP) less than or equal to 95 mmHg) (1 mmHg = 133." | ( A novel therapeutic approach for reversal of left ventricular hypertrophy and blood pressure control in hypertensive patients treated with alpha-methyldopa or propranolol. Fernandez, PG; Kim, BK; Lee, CC; Snedden, W, 1985) | 0.47 |
" It can be concluded from these results that, in situ, the primary action of amrinone occurs on vascular smooth muscle and that a positive inotropic activity with a normal dosage of amrinone is only an indirect outcome of reflex activation of the sympathetic system." | ( Haemodynamic effects of amrinone in the anaesthetized pig. Brilla, C; Jacob, R; Kissling, G; Vogt, M, 1988) | 0.27 |
" The threshold provocative dose of histamine needed to cause a 20% fall in starting FEV1 (PD20) was measured by log dose-response curve." | ( Increased responsiveness to histamine after propranolol in subjects with asthma nonresponsive to the bronchoconstrictive effect of propranolol. Carpentiere, G; Castello, F; Marino, S, 1988) | 0.54 |
" In isolated cat papillary muscles and rabbit right atria, cumulative hydralazine log dose-response curves (0." | ( Direct effects of hydralazine on cardiac contractile function, haemodynamics, and myocardial energetics in isolated myocardium. Amsterdam, EA; Rendig, SV; Segel, LD, 1988) | 0.27 |
"The pharmacokinetics of a sustained release (SR) propranolol (Betalong) were compared with conventional propranolol (Inderal) after single and multiple dosing in 8 normal healthy volunteers." | ( Pharmacokinetic study of a new sustained release preparation of propranolol in normal healthy volunteers. Biswas, NR; Garg, SK; Gyawali, K; Kumar, N; Lal, R; Narendranath, KA; Sharma, PL, 1988) | 0.77 |
"Three consecutive dose-response curves to aerosolized histamine were obtained in 11 anesthetized dogs." | ( Characteristics of tachyphylaxis to inhaled histamine in anesthetized dogs. Antol, PJ; Fujita, M; Hyatt, RE, 1988) | 0.27 |
" We administered propranolol over a wide dosage range to a different group of animals and found that a high dose (20 mg/kg) increased separation-induced coos while decreasing the activity levels." | ( Effects of clonidine and propranolol on separation-induced distress in infant rhesus monkeys. Kalin, NH; Shelton, SE, 1988) | 0.92 |
"In the present study we set out to explain the complex atropine dose-response curves in man in relation to M-cholinoceptor subtype occupancy." | ( Complex dose-response curves of atropine in man explained by different functions of M1- and M2-cholinoceptors. Pitschner, HF; Wellstein, A, 1988) | 0.27 |
" Because results were comparable in all models, additional dosage formulations were subsequently tested only in the rabbit colon model." | ( Assessment and validation of animal models to evaluate topical effects of substances on gastrointestinal mucosa. Anderson, LD; Casper, AG; Fara, JW; Myrback, RE, 1988) | 0.27 |
" In addition, (a) the presence of non-linear absorption kinetics offers a further explanation for the considerable inter-patient variability in AUC since the ability of drug to cross the liver is a function of the concentrations attained in portal blood which will be dependent on dissolution conditions prevailing in the GI-tract, (b) depending on the choice of the dose and dosage interval of the conventional release formulation used for comparison and as a consequence of Michaelis-Menten first pass metabolism it is possible to obtain relative bioavailability data showing superiority, equivalence or bioavailability loss with the slow release form." | ( Drug input rate from the GI-tract. Michaelis-Menten kinetics and the bioavailability of slow release verapamil and nifedipine. Fischer, A; Köhne, H; Menke, G; Rietbrock, N; Woodcock, BG, 1988) | 0.27 |
" The dosage of adrenergic vasoconstrictors should be limited and gingival retraction cord containing epinephrine avoided entirely." | ( Hypertensive response to levonordefrin in a patient receiving propranolol: report of case. Mito, RS; Yagiela, JA, 1988) | 0.52 |
" Since many beta-adrenoceptor antagonists have short plasma elimination half-lives, divided daily dosing has often been necessary in order to provide continuous beta-blockade throughout the day." | ( Pharmacokinetics of long acting propranolol. Implications for therapeutic use. Nace, GS; Wood, AJ, 1987) | 0.56 |
" Propranolol dosage was titrated according to blood levels." | ( Systemic and hepatic hemodynamics after variceal hemorrhage: effects of propranolol and placebo. Huet, PM; Marleau, D; Pomier-Layrargues, G; Villeneuve, JP; Willems, B, 1987) | 1.42 |
" In vitro dissolution studies have proved to be of little value in determining the clinical activity of these new dosage forms." | ( Controlled-release formulations of propranolol and verapamil. Dunn, J, 1987) | 0.55 |
" No correlation could be found between the change in clinical symptoms and electrocardiographic, echocardiographic or hemodynamic data, nor to the dosage of V or P administered." | ( Long-term treatment of hypertrophic cardiomyopathy with verapamil or propranolol in matched pairs of patients: results of a multicenter study. Biamino, G; Bubenheimer, P; Förster, K; Hanrath, P; Hopf, R; Kaltenbach, M; Kober, G; Kuck, KH; Schlepper, M; von Olshausen, KE, 1987) | 0.51 |
" The mean supine BP 24 hours post dosing were 177/110 mmHg (placebo), 173/109 mmHg (propranolol) and 164/100 mmHg (atenolol)." | ( Atenolol or propranolol in hypertensive patients poorly controlled on captopril and frusemide. Lovell, HG; Petrie, JC; Robb, OJ; Webster, J; Witte, K, 1987) | 0.88 |
" Transient atrioventricular dissociation occurred in two patients 2 h after dosing with verapamil and propranolol or atenolol." | ( The effect of combined therapy on the pharmacokinetics and pharmacodynamics of verapamil and propranolol in patients with angina pectoris. Lennard, MS; McCourty, JC; Silas, JH; Tucker, GT, 1988) | 0.71 |
" For each agent tested in this study, dose-response curves were established." | ( Micturition in the unanesthetized rat: spinal vs. peripheral pharmacology of the adrenergic system. Durant, PA; Lucas, PC; Yaksh, TL, 1988) | 0.27 |
"25-2 h than in po dosed counterparts." | ( Transplacental and mammary passage of radioactivity in rats treated vaginally and orally with [14C]propranolol. Bura, C; Buttar, HS; Moffatt, JH, 1988) | 0.49 |
"05) and a one-log magnitude of increase in the isoproterenol-heart rate dose-response curve." | ( Effects of chronic beta-adrenergic blockade on exercise training in dogs. Horwitz, LD; Lindenfeld, J; Smoak, J; Wolfel, EE, 1988) | 0.27 |
" Propranolol and cimetidine serum samples were measured over the 24-hour dosing interval after the last propranolol dose." | ( The effect of cimetidine dose timing on oral propranolol kinetics in adults. Asgharnejad, M; Danis, M; Donn, KH; Powell, JR, 1988) | 1.44 |
" We determined the dose of propranolol (propranolol dose-response curves) required to block the effects of 1 Hz, 2 Hz, and 4 Hz bilateral ansae subclaviae stimulation on sinus nodal automaticity, AV nodal conduction, and atrial and ventricular ERPs." | ( Differential sensitivity of sinus node, atrioventricular node, atrium, and ventricle to propranolol. Chang, MS; Zipes, DP, 1988) | 0.79 |
" Their dose-response curve lay to the right of that for patients not given propranolol, and this indicates competitive inhibition." | ( Propranolol treatment in children with tetralogy of Fallot alters the response to isoprenaline after surgical repair. Barazzone, C; Berner, M; Dayer, P; Friedli, B; Jaccard, C; Oberhansli, I; Rouge, JC, 1988) | 1.95 |
"Penbutolol and propranolol were administered orally in a dosage of 40 mg once daily and 80 mg twice daily, respectively to 12 patients with hypertension and impaired renal function." | ( Comparison of the effects of penbutolol and propranolol on glomerular filtration rate in hypertensive patients with impaired renal function. Donker, AJ; Heidendal, GA; Oe, PL; Reijn, E; van der Meulen, J, 1986) | 0.89 |
" Propranolol dosage was titrated in order to produce plasma concentrations of propranolol of 50 to 150 ng per ml." | ( Propranolol for the prevention of recurrent variceal hemorrhage: a controlled trial. Huet, PM; Infante-Rivard, C; Marleau, D; Pomier-Layrargues, G; Viallet, A; Villeneuve, JP; Willems, B, ) | 2.48 |
" The dose-response curve to vasopressin and its maximal effect measured on stimulation of glucose production were unchanged in thyroidectomized rats." | ( Hormonal control of glucose production and pyruvate kinase activity in isolated rat liver cells: influence of hypothyroidism. Beylot, M; Comte, B; Khalfallah, Y; Laville, M; Riou, JP; Vidal, H, 1987) | 0.27 |
"The relationship between chronic oral dosage with a long-acting formulation of propranolol and plasma propranolol levels 22 to 23 hours later is described in 12 adult male patients with organic brain disease." | ( Plasma propranolol levels and their effect on plasma thioridazine and haloperidol concentrations. Greendyke, RM; Kanter, DR, 1987) | 0.96 |
" The dose-response curves of the effect of 10-210 mM of acetone on the ACR and the peak of NE release were parallel." | ( Correlation between positive chronotropic effect and norepinephrine release induced by acetone in the rat right atrium. Chentanez, T; Sadavongvivad, C; Tantrarungroj, K, 1987) | 0.27 |
"After multiple oral doses, propranolol has been reported to accumulate to a greater degree than expected based on its terminal elimination rate constant and dosage interval." | ( Nonlinear pharmacokinetics of unbound propranolol after oral administration. Bottorff, MB; Lalonde, RL; Mirvis, DM; Pieper, JA; Straka, RJ, 1987) | 0.84 |
"A 21 year old male developed hallucinations, personality change and severe depression following an increase in oral propranolol administration at recommended dosage levels." | ( Psychosis with propranolol: still not recognized? Blackwood, GW; Cunnane, JG, 1987) | 0.84 |
"A slurry of activated carbon (activated charcoal) in electrolyte replacement solution given by stomach tube and antiarrhythmic drugs given parenterally cured 9 of 11 calves dosed 7 to 24 h previously with a lethal amount (20g/kg) of Bryophyllum tubiflorum flower heads." | ( Curing experimental Bryophyllum tubiflorum poisoning of cattle with activated carbon, electrolyte replacement solution and antiarrhythmic drugs. Dunster, PJ; McKenzie, RA, 1987) | 0.27 |
" 4 After multiple oral dosing with 80 mg twice daily of conventional propranolol the steady-state plasma concentration (Css), area under the curve (AUC tau), peak concentration (Cmax) and trough concentration (Cmin) were significantly higher in cirrhotic patients and the peak: trough ratio (Cmax/Cmin) was significantly lower than controls." | ( A comparative pharmacokinetic study of conventional propranolol and long acting preparation of propranolol in patients with cirrhosis and normal controls. Bastain, W; Hayes, JR; Larkin, KA; McAinsh, JA; Shanks, RG; Watson, RG, 1987) | 0.76 |
"0001) after the administration of long-acting propranolol compared with conventional propranolol on both day 1 and day 7; in addition, the elimination half-life was longer after administration of the long-acting preparation (9 hr) compared with that following the conventional dosage form (4 hr)." | ( Comparative pharmacodynamics and pharmacokinetics of conventional and long-acting propranolol. Chalavarya, G; Fencik, M; Garg, DC; Jallad, NS; Kraml, M; Mishriki, A; Weidler, DJ, ) | 0.62 |
" These patients are best managed as outpatients with gradual dosage reduction over 4-12 weeks." | ( Management of benzodiazepine dependence. Lader, M; Moodley, P, 1986) | 0.27 |
" In our study linear dependence could be established only within a dosage range of 40 mg to 160 mg." | ( Dose-dependent bioavailability of propranolol. Cvelbar, P; Francetić, I; Kopitar, Z; Lenardic, A; Vrhova, B; Zorz, M, 1986) | 0.55 |
" Although there was no correlation between propranolol dosage and depressive symptoms for the population as a whole, among patients with a negative history there was a highly significant positive correlation between propranolol dosage and depression scores." | ( Depressive symptoms in propranolol users. Friedman, MJ; Griffin, SJ, 1986) | 0.84 |
" The acid inhibition was blocked by propranolol, and dose-response analysis showed inhibition of a non-competitive type." | ( Effect of serotonin on bethanechol-stimulated gastric acid secretion and gastric antral motility in dogs. Bech, K, 1986) | 0.55 |
" This could be attributed to a relatively low dosage and slow infusion speed." | ( Effects of four antiarrhythmic drugs on the induction and termination of paroxysmal supraventricular tachycardia. Ishinaga, T; Komatsu, C; Tateishi, O; Tokuhisa, Y; Yoshimura, S, 1986) | 0.27 |
" Aerosol pretreatment with the cyclooxygenase inhibitor indomethacin had no significant effect on either LTC4 or LTD4 dose-response curves; however, at the highest doses of these agonists a notable, nonsignificant inhibition of effects on both Rp and Cdyn was seen." | ( Pharmacology of aerosol leukotriene C4- and D4-induced alteration of pulmonary mechanics in anesthetized cynomolgus monkeys. Giles, RE; Krell, RD; Williams, JC, 1986) | 0.27 |
" In anaprilin therapy the drug should be individually dosed out with regard to its basal concentration in the blood and the degree of pulse retardation at rest." | ( [Pharmcodynamic evaluation of the use of anaprilin combined with merkazolil for the therapy of thyrotoxicosis]. Lebedeva, EA; Verbovaia, NI, ) | 0.13 |
" A thorough understanding of the applied pharmacology, dosage recommendations, toxicity, and practical considerations must be attained before these drugs can be used effectively." | ( Pharmacology and pharmacokinetics of drugs used to treat cardiac disease in horses. McGuirk, SM; Muir, WW, 1985) | 0.27 |
" Heart rate was lowest during propranolol dosing and blood pressure was lowest during labetalol dosing irrespective of the labetalol dose used." | ( Chronic effects of labetalol, pindolol, and propranolol on calf blood flow in intermittent claudication. Lepäntalo, M, 1985) | 0.82 |
" Patients entering the study were receiving an average propranolol dosage of 131 mg/day (range 20 to 240)." | ( Combination propranolol and bepridil therapy in stable angina pectoris. Charlap, S; Crawford, MH; DiBianco, R; Farnham, DJ; Frishman, WH; Kostis, JB; Michelson, EL; Michie, DD; Sawin, HS; Zellner, SR, 1985) | 0.9 |
", a 1000-fold inhibition of the blood pressure/isoproterenol dose-response relationship." | ( Do catecholamines play a physiologic role in regulating corpus luteum function in the pseudopregnant rabbit? Bill, CH; Gadsby, JE; Keyes, PL; Lucchesi, B; Schwartz, TS, 1985) | 0.27 |
" The dosage of 25 mg/kg (single and repeated) consistently inhibited platelet function, and the effects lasted 3 to 5 days." | ( Effects of aspirin and propranolol on feline platelet aggregation. Greene, CE, 1985) | 0.58 |
" Increased dosage of propranolol to 4 mg did not produce any further reduction of portal pressure or mucosal damage." | ( Propranolol reduces ethanol-induced gastric mucosal damage in portal hypertensive rats. Ivey, KJ; Maeda, R; Mason, GR; Sankary, H; Sarfeh, IJ; Tarnawski, A, 1986) | 2.03 |
" However, the drugs were not equivalent: In addition to its greater potency, nadolol differed from propranolol and metoprolol in the slope of its dose-response curve." | ( Comparison of four beta-blockers as assessed by 24-hour ECG recording. Coumel, P; Delhotal-Landes, B; Escoubet, B; Gourmel, B; Leclercq, JF; Maison-Blanche, P; Poirier, JM, 1986) | 0.49 |
" Propranolol also shifted the dose-response curves to the right, but was apparently more potent in preparations with basal tone than in tissues where high tone was induced by carbachol or K+." | ( Noradrenergic and non-noradrenergic relaxation at basal and high tone levels in the guinea-pig tracheal smooth muscle. Abe, M; Furukawa, T, 1986) | 1.18 |
" Propranolol decreased the migraine index more than 70% in 13 patients: five patients at a dosage of 40 mg/day, five patients at a dosage of 120 mg/day, and three patients at a dosage of 240 mg/day." | ( Propranolol plasma levels and relief of migraine. Relationship between plasma propranolol and 4-hydroxypropranolol concentrations and clinical effects. Albani, F; Baldrati, A; Baruzzi, A; Cortelli, P; D'Alessandro, R; Lugaresi, E; Sacquegna, T, 1985) | 2.62 |
" In 2 patients, verapamil caused weakness, lightheadedness, and severe sinus bradycardia (40 to 48 beats/min), and the dosage was reduced (blindly) to 240 mg/day, with the alleviation of bradycardia and associated symptoms." | ( Propranolol-verapamil versus propranolol-nifedipine in severe angina pectoris of effort: a randomized, double-blind, crossover study. Corbett, JR; Croft, CH; Fulton, KL; Hillis, LD; Winniford, MD, 1985) | 1.71 |
" One hour after 40 mg propranolol by mouth as well as during continuous oral dosing at doses that reduced heart rate 25%, cardiac output and the hepatic venous pressure gradient fell significantly, whereas arterial pressure and hepatic blood flow did not change significantly." | ( Effect of propranolol on hepatic blood flow in patients with cirrhosis. Braillon, A; Calès, P; Jirón, MI; Lebrec, D; Valla, D, 1985) | 0.99 |
"Histamine dose-response curves were performed on anesthetized tracheostomized guinea pigs that were paralyzed and mechanically ventilated at a constant tidal volume and breathing frequency." | ( Histamine dose-response curves in guinea pigs. Hogg, JC; Hulbert, WC; McLean, T; Paré, PD; Wiggs, B, 1985) | 0.27 |
" Because of an increased frequency of anginal attacks, the dosage was increased to 240 mg/day." | ( Propranolol-induced depression and psychosis. Parker, WA, ) | 1.57 |
" The finding suggests that there may be need for an altered dosage regimen in the undernourished." | ( Drug binding in the undernourished: a study of the binding of propranolol to alpha 1-acid glycoprotein. Jagadeesan, V; Krishnaswamy, K, 1985) | 0.51 |
" It was concluded that aspirin alone at the recommended dosage of one-quarter of a 5-grain tablet (1." | ( Effects of aspirin and propranolol alone and in combination on hemostatic determinants in the healthy cat. Allen, DG; Crane, S; Johnstone, IB, 1985) | 0.58 |
" The good reproducibility within subjects and the small interindividual variation suggests that isoproterenol dose-response curves may be a useful tool for such studies." | ( Plasma concentration-response relationships of two formulations of propranolol. DeLeve, LD; Endrenyi, L; Leenen, FH, 1985) | 0.51 |
" At the dosage administered, propranolol alone had no antiarrhythmic effect." | ( Antiarrhythmic therapy with flecainide in combination and comparison with propranolol. Scheininger, M; Stern, H; Theisen, F; Theisen, K, 1985) | 0.79 |
" Dosing regimens were used that produced steady state plasma levels of both drugs, and the observed effects were clearly related to the plasma concentrations of the agents." | ( Cardiovascular and pharmacokinetic consequences of combined administration of verapamil and propranolol in dogs. Hamann, SR; Kaltenborn, KE; McAllister, RG; Tan, TG; Vore, M, 1985) | 0.49 |
" Pretreatment with propranolol or the combination of propranolol and atropine prior to the histamine dose-response curve did not affect the increased response seen after cigarette smoke exposure, but pretreatment with atropine abolished it." | ( The effect of acute airway inflammation on bronchial reactivity in guinea pigs. Hogg, JC; Hulbert, WM; McLean, T, 1985) | 0.6 |
" dosing (1." | ( Reduced hepatic clearance of propranolol induced by chronic carbon tetrachloride treatment in rats. Araki, K; Deguchi, N; Iwamoto, K; Satoh, M; Watanabe, J, 1985) | 0.56 |
" Now the dose-response relationship of the propranolol effect on LCAT activity was evaluated in vitro." | ( Effect of propranolol on lecithin:cholesterol acyl transferase activity in vitro. Kirchner, F; Schauer, I; Schauer, UJ, 1985) | 0.93 |
" These results show an improvement in left ventricular relaxation dependent on the propranolol dosage and often a normalization at high dosages." | ( Effect of propranolol on left ventricular relaxation in hypertrophic cardiomyopathy: an echographic study. Baragan, J; Bourmayan, C; Dussaule, JC; Fournier, C; Gay, J; Gerbaux, A; Razavi, A, 1985) | 0.9 |
" Repetition of the dose-response to isoprenaline in the presence of the beta-adrenergic antagonist propranolol (0." | ( Isoprenaline-evinced disturbances in action potentials from hearts of young cardiomyopathic hamsters. Rossner, KL, 1985) | 0.49 |
" A steady-state propranolol dosage of 40 mg every 8 hours produced a mean trough concentration of 42 ng/ml with extremely great (fiftyfold) interindividual variability." | ( Biologic determinants of propranolol disposition: results from 1308 patients in the Beta-Blocker Heart Attack Trial. Byington, RP; Furberg, CD; McIntyre, KM; Vokonas, PS; Walle, T, 1985) | 0.92 |
" In a further seven experiments dl-sotalol was administered using the same dosage regimen." | ( d-Sotalol: a new potent class III anti-arrhythmic agent. Donaldson, R; Sutton, P; Taggart, P, 1985) | 0.27 |
" The dose-response effectiveness for the prototype antiarrhythmic drugs, propranolol, quinidine and lidocaine in converting the induced ventricular fibrillation to sinus rhythm was determined." | ( A cardiac antiarrhythmic screening test using the isolated ischaemic perfused rat heart preparation. Lee, AY; Mok, CP; Wong, TM; Zhan, CY, 1985) | 0.5 |
"The plasma concentration-response relationships of oral and intravenous pindolol and propranolol have been studied in a group of eight healthy male subjects who received each dosage form in a randomized single-blind cross-over manner." | ( Contrasts between pindolol and propranolol concentration-response relationships. Aellig, WH; Carruthers, SG; Pacha, WL, 1985) | 0.78 |
" Addition of naloxone to propranolol shifted the dose-response curve of propranolol to the left significantly, indicating an additive effect of the two drugs in their antiarrhythmic activity." | ( Cardiac antiarrhythmic evaluation of naloxone with or without propranolol using a modified chloroform-hypoxia screening test in the rat. Lee, AY; Wong, TM, ) | 0.68 |
" Dose-response curves showed that lignocaine was more active in abolishing the ouabain induced arrhythmia than the halothane-adrenaline arrhythmia and was least active on the arrhythmia caused by ligation of the coronary artery." | ( Effects of lignocaine and propranolol on experimental cardiac arrhythmias. Allen, JD; Shanks, RG; Zaidi, SA, 1971) | 0.55 |
"3 Isoprenaline dose-response curves were shifted to the right in the cats administered oxyfedrine as well as in those administered propranolol." | ( The haemodynamic effects of prolonged oral administration of oxyfedrine, a partial agonist at beta-adrenoceptors: comparison with propranolol. Parratt, JR, 1974) | 0.66 |
"68 x 10(-5) mol/kg propranolol there was a dose-response relationship with the increase of plasma renin activity (PRA) achieved after 10 min stimulation." | ( Comparison of the effects of propranolol and ICI 66082 in blocking the renin releasing effect of renal nerve stimulation in the cat. Johns, EJ; Singer, B, 1974) | 0.87 |
"3 A second cannabis extract (II) with a different ratio of cannabinoids (also administered in dosage equivalent to 10 mg Delta(9)-THC/kg) failed to affect pentobarbitone anaesthesia in mice." | ( Interaction of cannabis and general anaesthetic agents in mice. Chesher, GB; Jackson, DM; Starmer, GA, 1974) | 0.25 |
" Increasing doses of propranolol produced parallel shifts to the right in the isoproterenol dose-response curve." | ( Effects of adrenergic receptor activation and blockade on the systolic preejection period, heart rate, and arterial pressure in man. Harris, WS; Schoenfeld, CD; Weissler, AM, 1967) | 0.56 |
" Histamine at the peak of its dose-response curve, 3 x 10(-4)moles/liter, produced approximately a 300% increase in cyclic 3',5'-AMP accumulation in the guinea pig, 60% in the cat, and 90% in the human heart particles." | ( Activation of myocardial adenyl cyclase by histamine in guinea pig, cat, and human heart. Klein, I; Levey, GS, 1971) | 0.25 |
" The dose-response lines to phenylephrine were shifted in a parallel manner by propranolol 10(-8)M and 10(-7)M, suggesting that the relaxations were mediated through beta-adrenoceptors." | ( Actions of phenylephrine on beta-adrenoceptors in guinea-pig trachea. Chahl, LA; O'Donnell, SR, 1969) | 0.47 |
" Hence it is concluded that practolol is an effective drug in treating angina, and in the dosage used is of potential value in patients with asthmatic bronchitis and angina." | ( Clinical evaluation of practolol, a new cardioselective beta-blocking agent in angina pectoris. Clayton, GA; Sandler, G, 1970) | 0.25 |
" The effects of six beta-adrenoceptive antagonists [(+/-)-propranolol, (+)-propranolol, (+/-)-sotalol, (+/-)-practolol, (+/-)-pindolol and (+/-)-procinolol] were studied on airway resistance and heart rate in guinea-pigs and dose-response curves constructed." | ( Comparative study of six -adrenoceptive antagonists on airway resistance and heart rate in the guinea-pig. Advenier, C; Boissier, JR; Giudicelli, JF, 1972) | 0.49 |
" When the doses required to produce these degrees of blockade were computed from the dose-response relations for blockade of the effects of cord stimulation by propranolol, they were found to be similar for effects on heart rate and air overflow." | ( Assessment of the effectiveness of -adrenoceptor blocking agents towards cardiac and bronchiolar responses of the pithed guinea-pig to electrical stimulation of the spinal outflow. Burden, DT; Parkes, MW, 1972) | 0.45 |
"Inotropic dose-response curves were constructed for a series of beta-adrenoceptor antagonists, based on the inotropic responses of isolated dog trabecular muscles stimulated to contract at a regular rate." | ( Comparative partial agonist activity of -adrenoceptor antagonists. Nayler, WG, 1972) | 0.25 |
" 6) In the presence of cocaine, the dose-response curves plotted from the mechanical activity induced by excess [K]o or by noradrenaline shifted to the left and the maximum responses evoked by either treatment were enhanced." | ( Effects of cocaine on a hypogastric nerve-vas deferens preparation of the guinea pig. Hashiguchi, T; Ito, Y; Kuriyama, H, 1974) | 0.25 |
" All three catecholamines increased the rate of weight loss but isoprenaline was effective in a much smaller dosage than either adrenaline or noradrenaline." | ( The role of circulating catecholamines in sweat production in man. Allen, JA; Roddie, IC, 1972) | 0.25 |
"Propranolol, when given in high dosage to rats, did not induce an increase in hepatic delta-aminolaevulic acid synthetase, an enzyme which is raised in human and drug-induced animal porphyria." | ( Acute intermittent porphyria: response of tachycardia and hypertension to propranolol. Beattie, AD; Goldberg, A; Moore, MR; Ward, RL, 1973) | 1.93 |
" At the higher dosage verapamil produced a significant improvement in frequency of angina, trinitrin consumption, and exercise tolerance, and had a favourable and significant effect on the amount and duration of ischaemic S-T depression occurring in the electrocardiogram during exercise." | ( Clinical evaluation of verapamil in angina pectoris. Clayton, GA; Sandler, G; Thornicroft, SG, 1968) | 0.25 |
" There is still too little well-documented evidence concerning the beta-blocking activity of the unidentified major metabolites of propranolol to suggest any alteration in the dosage regimen used in renal failure." | ( Pharmacodynamics of propranolol in renal failure. Foulkes, DM; Joekes, AM; Thompson, FD, 1972) | 0.78 |
" The method quickly produced accurate and reproducible dose-response curves." | ( Use of cumulative dose-response curves in potency comparisons of sympathomimetic amines on the cat soleus muscle. Nott, MW; Raper, C, 1972) | 0.25 |
"No unequivocal central effects were found with either +/--propranolol (120 mg) or +/--sotalol (240 mg) in acute dosage in normal subjects." | ( Central and peripheral effects of propranolol and sotalol in normal human subjects. Lader, MH; Tyrer, PJ, 1972) | 0.77 |
" Dose-heart rate curves of the foetus and pregnant ewe to isoprenaline and the shift to the right of the isoprenaline dose-response curves by propranolol were similar in both the ewe and the foetus." | ( Beta-adrenoceptive responses in the unanaesthetized ovine foetus. Van Petten, GR; Willes, RF, 1970) | 0.45 |
"Sensitivity to propranolol varies widely, and dosage should be increased gradually." | ( Treatment of hypertension with propranolol. Gillam, PM; Prichard, BN, 1969) | 0.89 |
" In either group, the dose-response curve of dP/dt to isoproterenol was shifted upward by AR-L, but the actions of the two drugs were additive without real synergism (e." | ( In vivo interaction of AR-L 115BS (Vardax) with the adrenergic nervous system. Cohn, JN; Francis, GS; From, AH; Petein, M; Pierpont, GL, ) | 0.13 |
"The dopamine alpha- and beta-adrenoceptor dose-response curves are investigated in four patients who are exempt from cardiovascular disease." | ( The use of low doses of dopamine in intensive care medicine. D'Orio, V; el Allaf, D; Juchmès, J; Marcelle, R, 1984) | 0.27 |
" Propranolol was found to be superior to placebo only at the higher dosage regimen (240 mg daily)." | ( The response of essential tremor to propranolol: evaluation of clinical variables governing its efficacy on prolonged administration. Calzetti, S; Findley, LJ; Perucca, E; Richens, A, 1983) | 1.45 |
" Quinidine inhibited T3 formation, with a dose-response curve which was similar over the concentrations studied to that of DL-propranolol." | ( Inhibition by propranolol of 3,5,3'-triiodothyronine formation from thyroxine in isolated rat renal tubules: an effect independent of beta-adrenergic blockade. Campbell, DG; Heyma, P; Larkins, RG, 1980) | 0.83 |
" The dose-response curve for propranolol inhibition of 125I-hydroxybenzylpindolol binding duplicated that reported for its physiologic action." | ( Beta receptor occupancy. Assessment in the intact animal. Homcy, CJ; Kopiwoda, S; Strauss, HW, 1980) | 0.55 |
" Propranolol, in a dosage insufficient to change MABP, decreased both CO and CBF." | ( Relationship of cerebral blood flow to cardiac output, mean arterial pressure, blood volume, and alpha and beta blockade in cats. Davis, DH; Sundt, TM, 1980) | 1.17 |
" Dose-response relations for the depressant effects are similar for pacemaker frequency and for tension development in atrial and papillary muscle." | ( Stimulant and depressant effects of beta-adrenoceptor blocking agents on isolated heart muscle. A positive inotropic effect not mediated through andrenoceptors. Blinks, JR; Kaumann, AJ, 1980) | 0.26 |
" Prazosin (PRZ), a selective alpha 1-receptor blocker, inhibited preferentially the positive phase of the inotropic response and displaced the dose-response curve of PE to the right in nanomolar concentrations, indicating a competitive mechanism of inhibition." | ( Competitive blockade of alpha-adrenergic receptors in rat heart by prazosin. Osnes, JB; Oye, I; Skomedal, T, 1980) | 0.26 |
" Exercise tests were performed after each dosing period; isoprenaline stimulation was studied at the highest dose level." | ( Comparative pharmacodynamics and plasma levels of beta-adrenoceptor blocking drugs. Bodem, G; Gugler, R; Höffgen, K; Krist, R; Raczinski, H, 1980) | 0.26 |
" Dose-response curves to a beta agonist, albuterol, were obtained in six normal subjects by measuring specific airway conductance (sGaw) after increasing doses of inhaled albuterol." | ( Assessment of bronchial beta blockade after oral bevantolol. Baldwin, CJ; Gribbin, HR; Mackay, AD; Tattersfield, AE, 1981) | 0.26 |
" Dose-response curves for both drugs revealed that maximum attenuation of exercise tachycardia and systolic blood pressure were in the same range but suggested that indenolol induced a greater response in the lower doses." | ( Dose-response studies of indenolol, a beta adrenoceptor blocker. Daneshmend, TK; Okupa, FE; Roberts, CJ; Shrosbree, E, 1981) | 0.26 |
" Continuous intra-aortic infusion of phentolamine produced a dose-response decrease in uterine activity and blood flow." | ( Effect of adrenergic blockade on dynamics of the pregnant primate uterus (Macaca mulatta). Harbert, GM; Spisso, KR, 1981) | 0.26 |
" Coefficients of determination were calculated from the individual dose-response curves." | ( Assessment of beta blockade with propranolol. Goldberger, V; Hager, WD; Mayersohn, M; Perrier, D; Pieniaszek, HJ, 1981) | 0.54 |
" Clonidine followed by prazosin was added to their regimen on an outpatient basis to establish the dose-response for BP and catecholamines." | ( Clonidine and prazosin effects in hypernoradrenergic vasodilator-treated and beta-blocker-treated patients. Mitchell, HC; Pettinger, WA, 1981) | 0.26 |
" Log dose-response curves for increases in both heart rate (mostly beta 1), and amplitude of physiologic tremor (beta 2) were constructed for each subject in the control state and 2 hr after 10 or 40 mg propranolol, 200 mg sotalol, or placebo." | ( Propranolol and sotalol as antagonists of isoproterenol-enhanced physiologic tremor. Fish, A; Perucca, E; Pickles, H; Richens, A, 1981) | 1.89 |
" Thus, for determination of administration frequency and dosage of beta-adrenoceptor blocking drugs, not only pharmacokinetic but also pharmacological data (duration of action) are essential." | ( Duration and selectivity in beta-adrenoceptor blocking action of a beta-adrenoceptor blocking drug, D-32 in conscious dogs. Himori, N; Honma, S; Ishimori, T; Izumi, A, 1981) | 0.26 |
"Patient compliance can be improved by reducing the complexity of drug dosage and by better labeling, packaging and informational exchange." | ( Once-a-day drug regimen for psychiatric patients. Hasan, MK; Mooney, RP, 1981) | 0.26 |
" Thus shifts of the dose-response curves in BP and HR were observed." | ( A simple method to determine the ratio of cardiac to vascular beta-receptor blockade in the rat in vivo. Kudo, Y; Sokabe, H; Zehr, JE, 1981) | 0.26 |
" Standardized experiments were performed using a chronically reserpinized canine preparation for the assessment of dose-response curves of changes in hemodynamics, left ventricular contractility, heart rate, AV-conduction time, and myocardial oxygen consumption especially at therapeutic doses." | ( Sympathomimetic and cardiodepressant effects of acebutolol, oxprenolol, pindolol, and propranolol. A comparative study on changes in hemodynamics, contractility, heart rate, and AV-conduction time at therapeutic doses. Bender, F; Gülker, H; Heuer, H; Kristek, J, 1981) | 0.49 |
" Dose-response experiments with five logarithmically increased doses of pentagastrin and one dose of isoprenaline showed unchanged calculated maximum response and an increase in half-maximum acid response." | ( Effect of isoprenaline on pentagastrin-stimulated gastric acid secretion in dogs with gastric fistula. Andersen, D; Bech, K; Gottrup, F; Hovendal, CP, 1981) | 0.26 |
"To investigate the nature of the variable response to inhaled histamine in monkeys, we performed dose-response curves in a group of 10 anesthetized Macaca mulatta monkeys before and after administration of propranolol and atropine in inhaled doses sufficient to produce significant beta-adrenergic and cholinergic blockade of airway smooth muscle." | ( Bronchial response to histamine after inhaled propranolol and atropine in monkeys. Nicholls, I; Pare, PD, 1982) | 0.71 |
" Thus, it was of interest to study the dose-response relationship between an unselective (propranolol) and a beta 1-selective (atenolol) blocker and endurance exercise performance." | ( Running performance as a function of the dose-response relationship to beta-adrenoceptor blockade. Kaiser, P, 1982) | 0.49 |
" 2 Isoprenaline heart rate dose-response curves showed parallel shifts to the right after oral prizidilol, indicating antagonism by this compound at beta-adrenoceptors in the heart." | ( An assessment of beta-adrenoceptor blockade in man by prizidilol hydrochloride. Curry, PV; Pitcher, DW; Trounce, JR, 1982) | 0.26 |
"In the isolated guinea-pig right atria and tracheal strips, both propranolol and YM-09538 caused a parallel shift of the dose-response curve for isoproterenol to the right, indicating that these two drugs block nonselectively the beta 1 1- and beta 2-adrenoceptors." | ( Comparison of airway obstruction induced by propranolol and YM-09538 (a combined alpha- and beta-adrenoceptor blocking drug). Takenaka, T; Tomioka, K; Yamada, T, 1982) | 0.76 |
" The maximum of the dose-response curve to isoprenaline, constructed after incubation with Ro 03-7894 and a 3 hr bath-washout, was depressed by 89." | ( Comparison of the apparent irreversible beta-adrenoceptor antagonist Ro 03-7894 with propranolol in cardiac ventricular muscle by pharmacological and radioligand binding techniques. Broadley, KJ; Rankin, A, 1982) | 0.49 |
" 4 The fact that the shift of the dose-response curve of isoprenaline-induced tachycardia was smaller after metoprolol than after propranolol supports the hypothesis that beta 2-adrenoceptors are present in the heart." | ( Relevance of selectivity and non-selectivity in beta-adrenoceptor blocking drugs. Bonelli, J, 1982) | 0.47 |
" Alpha-2 adrenergic activation, achieved with 10 muM epinephrine and 30 muM propranolol, significantly inhibited forskolin-stimulated cyclic AMP accumulation and glycerol release, shifting the dose-response curves to the right." | ( Alpha-2 adrenergic activation inhibits forskolin-stimulated adenylate cyclase activity and lipolysis in human adipocytes. Burns, TW; Bylund, DB; Forte, LR; Langley, PE; Terry, BE, 1982) | 0.49 |
" What remains to be solved is the dosage level." | ( Clinical experiences with prenalterol as an antidote to Beta-adrenoceptor blockade. Kulling, P, 1982) | 0.26 |
" Medical treatment should be considered a failure only if maximal dosage of nitrates and beta blockers is attained without satisfactory control of symptoms." | ( What is optimal drug therapy in angina pectoris? Brest, AN; Frankl, WS, 1983) | 0.27 |
" The dose-response curve with five doses of bethanechol with and without isoprenaline was in accordance with a non-competitive inhibition." | ( Effect of isoprenaline on bethanechol-stimulated gastric acid secrtion and mucosal blood flow in dogs with gastric fistula. Bech, K; Hovendal, CP, 1982) | 0.26 |
" The present work investigates in vitro the inhibitory dose-response curves to histamine, 4-methyl-histamine and 2-pyridylethylamine in depolarized (KCl 37 mM) uterus from estrogenous sensitized rats." | ( [Inhibitory action of histamine on the isolated rat uterus]. Esplugues, J; Marti-Bonmati, E; Morales-Olivas, FJ; Morcillo, E; Rubio, E, ) | 0.13 |
" In patients who respond to modest doses of pindolol, twice or even once daily dosing is often adequate." | ( Pindolol: a review of its pharmacology, pharmacokinetics, clinical uses, and adverse effects. Golightly, LK, ) | 0.13 |
" The two events generally paralleled one another when analyzed in terms of dose-response and time-response relationships." | ( Role of cyclic AMP in adrenergically-induced tracheal muscle relaxation. Lau, YS; Lum, BK, 1983) | 0.27 |
"Nifedipine is a strong calcium antagonist; it blocks the excitation-contraction coupling, yet at therapeutic dosage levels it has few side effects." | ( What is preferable in unstable angina, beta-blockade or calcium-inhibition? Hugenholtz, PG; Serruys, PW; Simoons, ML, 1983) | 0.27 |
" Pre-treatment of the rats with syrosingopine shifted the dose-response curve to the left (enhancement) while combined propranolol (800 micrograms/kg) and phentolamine (800 micrograms/kg) shifted the dose-response curve to the right (depression)." | ( Rat endometrial bioelectric activity in vivo and in vitro: effects of adrenaline. Levin, RJ; Phillips, JC, 1983) | 0.47 |
" sGaw was measured before dosing and after 2 h, just before salbutamol was inhaled." | ( Time course of the bronchial response to salbutamol after placebo, betaxolol and propranolol. Kaik, G; Palminteri, R, 1983) | 0.49 |
" Graded bolus injections of isoprenaline sulphate were given intravenously and control dose-response curves were drawn for the changes in heart rate and blood pressure." | ( Heart rate and blood pressure responses to intravenous boluses of isoprenaline in the presence of propranolol, practolol and atropine. Arnold, JM; McDevitt, DG, 1983) | 0.48 |
" The dosage should be reduced gradually, particularly the final decrement." | ( The beta-adrenergic blockade withdrawal phenomenon. Bhattacharjee, P; Prichard, BN; Tomlinson, B; Walden, RJ, 1983) | 0.27 |
"The dose-response curves of the beta-adrenergic agonists isoprenaline (mixed beta 1 and beta 2), prenalterol (beta 1-selective), noradrenaline (more beta 1 than beta 2) and salbutamol (beta 2-selective) were studied on adipose cells of the rat, in vitro." | ( Characterization of the beta-adrenoceptor of the adipose cell of the rat. Curtis-Prior, PB; Tan, S, 1983) | 0.27 |
" The effects of isoprenaline on four parameters in the anaesthetized cat: heart rate, blood pressure, soleus muscle contractility and airway reactance, were measured and the modification of the isoprenaline dose-response relation by each of the antagonist drugs assessed." | ( The selectivity of beta-adrenoceptor antagonists on isoprenaline-induced changes in heart rate, blood pressure, soleus muscle contractility and airways function in anaesthetized cats. Letts, LG; Richardson, DP; Temple, DM; Williams, LR, 1983) | 0.27 |
" Neuroleptic medications are still the mainstay of treatment, but recent studies suggest new approaches to dosage and to the treatment of acute psychosis." | ( The pharmacologic treatment of schizophrenia: a progress report. Baldessarini, RJ; Donaldson, SR; Gelenberg, AJ, 1983) | 0.27 |
" Preincubation with cocaine, 10(-5) M, shifted the inhibitory dose-response curves of Iso and Orc to the left, 16." | ( Mechanism of action of isoprenaline, isoxuprine, terbutaline and orciprenaline on gravid human isolated myometrium. Influence of the neuronal uptake process. Calixto, JB; Simas, CM, 1984) | 0.27 |
" Similar dose-response curves were found for non-vagotomized dogs with high beta 2-adrenergic tone and dogs with low vagal tone (vagotomy) after pentagastrin and histamine stimulated acid secretion." | ( Adrenergic receptors and gastric secretion in dogs. Is a "tonic balance" relationship between vagal and beta 2-adrenergic activity a possibility? Andersen, D; Bech, K; Gottrup, F; Hovendal, C, 1984) | 0.27 |
" Isoprenaline dose-response curves for systolic and diastolic blood pressure, heart rate and PRA showed similar parallel shifts after 1 day and 2 weeks of treatment." | ( Antihypertensive effect and degree of beta-adrenoceptor blockade after short-term and semi-chronic propranolol therapy. Boer, P; Dorhout Mees, EJ; Leenen, FH, 1984) | 0.48 |
" However, in EM subjects twice-daily dosing is required even if slow release preparations are used, since plasma metoprolol concentrations may remain negligible 24 h after dosing." | ( Polymorphic metabolism of beta-adrenoceptor antagonists. Lennard, MS; Ramsay, LE; Silas, JH; Tucker, GT; Woods, HF, 1984) | 0.27 |
" The reduction in steady-state beta-adrenergic receptor drug concentration following enzyme induction is sufficiently large that an altered pharmacodynamic response would be expected if no dosage modification is made." | ( Enzyme induction and beta-adrenergic receptor blocking drugs. Branch, RA; Herman, RJ, 1984) | 0.27 |
" However, individual dose titration is recommended when switching from propranolol four times a day to nadolol once daily because of the dosage variability noted in 40 percent of the patients." | ( Nadolol compared to propranolol for treating chronic stable angina pectoris. Crawford, MH; Miller, LA; O'Rourke, RA, 1984) | 0.82 |
" However, POB shifted the dose-response curve for NAT induction by norepinephrine (NE) to the left." | ( Modulation of rat pineal acetyl-Co A:arylamine N-acetyltransferase induction by alpha adrenergic drugs. Alphs, L; Lovenberg, W, 1984) | 0.27 |
" Inhibition of aggregation by the beta-adrenoceptor antagonists was manifested as a parallel shift to the right in the dose-response curve." | ( Beta-adrenoceptor antagonists and human platelets: relationship of effects to lipid solubility. Kerry, R; Scrutton, MC; Wallis, RB, 1984) | 0.27 |
" These differences account for many of the observed variations in drug action and dosage scheduling as well as for some of the side effects." | ( Beta-adrenergic blockers. Choosing among them. McGoon, MD; Vlietstra, RE, 1984) | 0.27 |
" During a one-year treatment period following the comparative trial, the seven patients who had received bopindolol showed no evidence of tachyphylaxia, the blood-pressure remaining well controlled while the dosage was slightly reduced." | ( Bopindolol, a new long-acting beta-adrenoceptor antagonist--a randomized comparison against propranolol in hypertensive patients. Axthelm, T; Kirch, W, 1983) | 0.49 |
" Following a single oral dose of placebo, bevantolol 75 or 150 mg or propranolol hydrochloride 40 mg, forced expiratory volume in 1 second (FEV1), heart rate, blood pressure and skeletal muscle tremor were measured before and after 4 increasing intravenous doses of terbutaline sulfate to establish terbutaline dose-response curves." | ( Selectivity of bevantolol hydrochloride, a beta 1-adrenoceptor antagonist, in asthmatic patients. Löfdahl, CG; Svedmyr, K; Svedmyr, N, ) | 0.37 |
" The changes in the sinus rate values reflect the degree of beta blockade, and the antiarrhythmic efficacy depends not only on the dosage but also on the nature of the drug used." | ( Beta-blocking therapy in atrial and ventricular tachyarrhythmias: experience with nadolol. Attuel, P; Coumel, P; Escoubet, B, 1984) | 0.27 |
" The dose-response curves constructed with intra-arterial or intravenous isoprenaline behave similarly in the presence of both atenolol 50 mg and propranolol 40 mg." | ( Enhancement of physiological finger tremor by intravenous isoprenaline infusions in man: evaluation of its role in the assessment of beta-adrenoceptor antagonists. Arnold, JM; McDevitt, DG, 1984) | 0.47 |
" Bronchial beta-adrenoceptor blockade was assessed as the displacement of the bronchodilator dose-response curve to inhaled isoprenaline after each beta-adrenoceptor blocking drug compared to placebo and expressed as the dose ratio." | ( Assessment of beta-adrenoceptor selectivity of a new beta-adrenoceptor antagonist, bisoprolol, in man. Bacon, RJ; Cragg, DJ; Tattersfield, AE, 1984) | 0.27 |
" Prazosin (10(-8) M-10(-6) M, alpha 1-adrenoceptor antagonist) produced a rightward shift of the phenylephrine and clonidine dose-response curve in both the trigone and urethra." | ( Alpha 1- and alpha 2-adrenoceptors in the smooth muscle of isolated rabbit urinary bladder and urethra. Satake, N; Shibata, S; Ueda, S, 1984) | 0.27 |
" In Study 1 the short-term dose-response effects of propranolol (1-8 mg) or pindolol (0." | ( Is the intrinsic sympathomimetic activity (ISA) of beta-blocking compounds relevant in acute myocardial infarction? Ahuja, RC; Hafizullah, M; Hussain, M; Nelson, GI; Reynolds, G; Silke, B; Taylor, SH; Verma, SP, 1984) | 0.52 |
" SCH 19927 produced a competitive alpha 1- and beta 1-blockade in vitro as indicated by the parallel shift to the right of the dose-response curves for norepinephrine and isoprenaline, respectively." | ( Effects of the R, R-isomer of labetalol, SCH 19927, in isolated tissues and in spontaneously hypertensive rats during a repeated treatment. Bamonte, F; Forlani, A; Monopoli, A; Ongini, E; Parravicini, L, 1984) | 0.27 |
" Alpha-blockade was confirmed by alpha-agonist dose-response studies." | ( Effect of alpha-adrenergic blockade on arrhythmias induced by acute myocardial ischemia and reperfusion in the dog. Bolli, R; Fisher, DJ; Miller, RR; Taylor, AA; Young, JB, 1984) | 0.27 |
" All patients had diastolic blood pressures above 95 mm Hg after therapy with thiazide diuretics for 2 weeks and were randomly assigned to treatment schedules which added minoxidil and propranolol in dosage ratios of 1:2, 1:4, and 1:8." | ( Minoxidil in the management of moderate hypertension. Alleyne, GA; Nicholson, GD; Valdes, G; Westerman, RL, 1980) | 0.45 |
" No age differences were seen in the time course of amylase release following (-)-isoproterenol stimulation or in the (-)-isoproterenol dose-response curve." | ( Beta-adrenergic regulation of rat parotid gland exocrine protein secretion during aging. Baum, BJ; Ito, H; Roth, GS, 1981) | 0.26 |
" During propranolol administration, all dose-response curves to isoproterenol were predictably shifted to the right." | ( Myocardial sensitivity to isoproterenol following abrupt propranolol withdrawal in conscious dogs. Daniell, HB; Newman, WH; Walle, T; Webb, JG, ) | 0.81 |
" Some dosage schedules of antithyroid drugs are considered, and some techniques for predicting remission status and relapse of disease are reported." | ( [Hyperthyroidism in children (author's transl)]. Bozzola, M; Cisternino, M; Larizza, D; Livieri, C; Lorini, R; Salvatoni, A; Severi, F, ) | 0.13 |
" A moderate hypotension was induced by CV-1808, nifedipine, and nitroglycerin, while a significant reduction in cardiac function was seen after dosing with propranolol." | ( Effect of 2-phenylaminoadenosine (CV-1808) on ischemic ST-segment elevation in anesthetized dogs. Fujiwara, S; Hirata, M; Imamoto, T; Kawazoe, K; Matsumoto, N; Tanabe, M, ) | 0.33 |
" Similar dose-response curves for cyclic AMP production were obtained." | ( Catecholamine stimulation of testosterone production via cyclic AMP in mouse Leydig cells in monolayer culture. Cooke, BA; Dix, CJ; Golding, M; Hunter, MG, 1982) | 0.26 |
" The equipotent beta-blocking dose of each drug was obtained by comparing isoproterenol dose-response curves." | ( Effects of equipotent blocking doses of acebutolol, acebutolol's primary metabolite, and propranolol on left ventricular hemodynamics in conscious awake dogs. Griffin, G; Harrison, DC; Kernoff, R; Magder, S; Rubenson, D, ) | 0.35 |
" Analysis of results indicated that the dose-response curve for the heart rate reduction resulting from propranolol for blacks was shifted to the right with respect to that for whites." | ( Ethnic differences in response to beta 1-adrenoceptor blockade by propranolol. Joubert, PH; Venter, CP, ) | 0.58 |
" The dose-response inhibition curve is paralleled by a fenoterol-induced increase in the cAMP levels of human leukocyte preparations." | ( Inhibition of IgE-mediated histamine release from human basophils and mast cells by fenoterol. Ambrosio, G; Bonaduce, D; Condorelli, M; Genovese, A; Marone, G; Triggiani, M, 1984) | 0.27 |
" Dosage was titrated until normotension was attained and patients were then maintained on this treatment for a year." | ( The correlation of changes in systolic blood pressure with regional anatomical regression of hypertensive left ventricular hypertrophy in patients on chronic antihypertensive therapy (greater than 1 year): alpha-methyldopa compared to propranolol. Fernandez, PG; Furlong, L; Gill, V; Kim, BK; Ko, P; Lewis, H; McDonald, J; McManamon, P; Nolan, R; Reichek, N, 1984) | 0.45 |
" The beta-blocking potency, estimated from the area under the dose-response curve (beta-blocking action) of carteolol, was also 300 times greater than that of propranolol and correlated well with the extent of the structural changes in the heart." | ( Dose-related inhibitory effects of the beta-adrenoceptor blocking drugs carteolol and propranolol on cardiac hypertrophy in spontaneously hypertensive rats. Igawa, T; Ikezono, K; Kimura, Y; Watanabe, K, 1984) | 0.69 |
" Despite high drug dosage and blood levels, only mild side effects were seen." | ( High dose propranolol in the treatment of angina pectoris: relationship of dose to blood levels and hemodynamic consequences. Cassell, I; Cunningham, M; Gradman, AH; Ross, AM; Zaret, BL; Zito, RA, ) | 0.53 |
" Unexpected differences, not previously reportd, were found in the shapes of the cAMP accumulation dose-response curves of norepinephrine and isoproterenol." | ( Neonatal rat pinealocytes: typical and atypical characteristics of [125I]iodohydroxybenzylpindolol binding and adenosine 3',5'-monophosphate accumulation. Auerbach, DA; Aurbach, GD; Klein, DC; Woodard, C, 1981) | 0.26 |
"In rabbit left atrium and ileum as well as in guinea-pig tracheal chain preparations dose-response curves for isoprenaline, adrenaline, noradrenaline and fenoterol have been determined." | ( On the coexistence of beta 1- and beta 2-adrenoceptors in various organs. Nick, B; Rohm, N; Schümann, HJ; Wagner, J, 1981) | 0.26 |
"1 Plasma propranolol steady state concentration (Css) was determined during chronic dosage (160 mg/day) in 22 hyperthyroid patients (aged 16-75 years, 11 smokers, 11 non-smokers) and again following treatment when euthyroid." | ( The influence of age, smoking and hyperthyroidism on plasma propranolol steady state concentration. Crooks, J; Feely, J; Stevenson, IH, 1981) | 0.92 |
" Studies using the rat indicates that the dose-response relationship is of a threshold nature, with doses of 3 g/kg or greater abolishing spontaneous secretion." | ( Effect of ethanol on spontaneous and stimulated growth hormone secretion. Redmond, GP, 1981) | 0.26 |
" As indicated by dose-response curves, receptor occupancy of each occurs to an almost equal extent at suboptimal epinephrine concentrations." | ( Cyclic AMP-dependent and cyclic AMP-independent antagonism of insulin activation of cardiac glycogen synthase. Angelos, KL; Ramachandran, C; Walsh, DA, 1982) | 0.26 |
" A dose-response relationship could be demonstrated in propranolol treated dogs by administering DB-cAMP at 10, 100 and 1000 micrograms/min at low but not at control blood pressure." | ( Conditions for stimulation of renin release by cyclic AMP in anaesthetized dogs. Eide, I; Holdaas, H; Kiil, F; Langård, O, 1981) | 0.51 |
" These recordings disclosed qualitative differences between the alpha-and Beta-inotropic response both in dose-response and time course experiments." | ( Differences between alpha-adrenergic and beta-adrenergic inotropic effects in rat heart papillary muscles. Osnes, JB; Oye, I; Skomedal, T, 1982) | 0.26 |
" Tapering propranolol dosage is frequently used in the hope of preventing adverse withdrawal events but the success of such a maneuver has not been shown." | ( Prevention of propranolol withdrawal mechanism by prolonged small dose propranolol schedule. Lutterodt, A; Nattel, S; Rangno, RE, 1982) | 1.03 |
" Low concentrations (1 nM) of (+)-propranolol were observed to be equipotent with (+/-)-propranolol in shifting the dose-response curve of GABA-stimulated [3H]diazepam binding by approximately 1/2 log unit." | ( Nanomolar concentrations of propranolol inhibit GABA-stimulated benzodiazepine binding to rat cerebral cortex. Morgan, PF; Stone, TW, 1982) | 0.84 |
" For this purpose, dose-response curves for isoproterenol before and after addition of propranolol (5 X 10(-9) to 10(-6) M) or phentolamine (10(-6) M) to the bath were determined." | ( [Analysis of the contraction induced by isoproterenol in isolated cerebral and femoral arteries of cat]. Marín, J; Salaices, M, 1982) | 0.49 |
" Dopamine dosage should be about ten times as high to reproduce cardiodynamic and hemodynamic effects, comparable with the response to adrenaline and noradrenaline in terms of magnitude and pattern of development." | ( [Effect of dopamine on coronary circulation]. Khomaziuk, AI; Kipshidze, NN; Neshcheret, AP, 1982) | 0.26 |
" Full dose-response curves for isoproterenol were constructed in BP and HR." | ( The ratio of cardiac to vascular beta-receptor blockade of atenolol and propranolol in spontaneously hypertensive rats in vivo. Kudo, Y; Sokabe, H, 1982) | 0.5 |
" Satisfactory dose-response curves could be constructed for the isoprenaline enhanced increases in finger tremor." | ( An assessment of physiological finger tremor as an indicator of beta-adrenoceptor function. Arnold, JM; McDevitt, DG, 1983) | 0.27 |
" In the presence of YOH, the ISO dose-response curve therefore completely disappears." | ( Lipolysis in rat adipose tissue in vitro and its alpha 2 adrenergic control. Horný, I; Kadrabová, M; Mühlbachová, E; Zámostný, V, 1983) | 0.27 |
" Dose-response curves and geometric mean ED50 values revealed the presence of supersensitivity to the chronotropic and inotropic effects of isoproterenol in vitro at 72 and 96 h after withdrawal." | ( Propranolol withdrawal supersensitivity in rat cardiovascular tissue, in vitro. Tenner, TE, 1983) | 1.71 |
" Cumulative administrations of leukotrienes desensitized the lung strip, whereas non-cumulative dose-response relationships for the leukotrienes and histamine were reasonably parallel." | ( Mechanisms of leukotriene-induced contractions of guinea pig airways: leukotriene C4 has a potent direct action whereas leukotriene B4 acts indirectly. Dahlén, SE; Granström, E; Hammarström, S; Hedqvist, P; Lindgren, JA; Rådmark, O; Westlund, P, 1983) | 0.27 |
" The dose-response curve for ATP-induced contraction was shifted to the right by theophylline." | ( Effect of apamin and theophylline on adenosine-5'-triphosphate-induced response of the guinea pig gallbladder. Ishikawa, Y; Takahashi, T; Yamamura, T, 1983) | 0.27 |
" Dosages were titrated until the patient showed a sitting diastolic blood pressure less than or equal to 90 mm Hg or to a maximum dosage of 100 mg/day of hydrochlorothiazide, 320 mg of propranolol and 20 mg of prazosin." | ( Monotherapy in mild to moderate hypertension: comparison of hydrochlorothiazide, propranolol and prazosin. Benowitz, N; Inouye, I; Loge, D; Massie, B; Simpson, P; Topic, N, 1984) | 0.69 |
" Apart from the hydrochlorothiazide dosage which was fixed, the dosage of the other active drugs was titrated incrementally until the target blood pressure level was achieved." | ( An appraisal of antihypertensive efficacy and adverse reactions with two drug regimens: enalapril maleate as part of triple therapy compared to conventional triple therapy in moderate to severe hypertension. Fernandez, PG; Galway, AB; Kim, BK, 1984) | 0.27 |
" All three alpha antagonists employed produced in innervated glands parallel displacements of the dose-response curves to norepinephrine, prazosin being 30 and 100 times more potent than phentolamine and yohimbine, respectively." | ( Alpha-1 adrenoceptors mediate secretory responses to norepinephrine in innervated and denervated rat submaxillary glands. Elverdin, JC; Luchelli-Fortis, MA; Perec, CJ; Stefano, FJ, 1984) | 0.27 |
" Cumulative dose-response curves were constructed for the effect of immune IgG on nice oviductal tracts from proestrus, estrus, metestrus and diestrus, comparing them with those obtained with norepinephrine." | ( Beta-adrenergic inhibitory effect of alloimmune antibody on isolated oviductal tract of mice. Borda, ES; Cremaschi, GA; Genaro, AM; Sales, ME; Sterin-Borda, L, 1984) | 0.27 |
" A similar study was carried out with 12 patients taking propranolol for various cardiovascular problems; their dosage of this agent was not varied, however." | ( Effect of timolol eye drops in subjects receiving systemic propranolol therapy. Blondeau, P; Côté, M; Tétrault, L, 1983) | 0.75 |
" Patients were divided into two groups according to laboratory data and propranolol dosage needed for clinical compensation (group A: 240 mg/day; group B: 320-400 mg/day)." | ( Propranolol and hyperthyroidism: serum free fatty acids and glucose-induced insulin release in nondiabetic thyrotoxic patients during treatment to clinical compensation. de Medeiros, YS; Francalanci, CC; Pinho, MO; Rosenthal, D, 1983) | 1.94 |
" The double regimen caused a drop in pressure of 16/11 mm Hg after one month (daily doses 25 mg chlorthalidone, 103 +/- 25 mg propranolol), and this reduction did not change at the third month in spite of dosage increases (daily doses 25 mg chlorthalidone, 222 +/- 77 mg propranolol)." | ( A crossover trial of oxdralazine in hypertension. Criscuolo, D; Galli, F; Salvadeo, A; Segagni, S; Villa, G, 1983) | 0.47 |
" Indoramin dosage was subsequently adjusted in 25 mg steps (to maximum 150 mg daily), if necessary, at follow-up control visits every 14 days." | ( Indoramin as second step therapy in the management of benign essential hypertension. Gherardi, S; Manzoli, U; Mazzari, M; Montenero, AS; Schiavoni, G, 1983) | 0.27 |
"To test the hypothesis that the depression of cardiac performance induced by competitive blockade of sympathetic stimulation at beta-adrenoceptors could be attenuated by the addition of a high level of intrinsic sympathomimetic activity (ISA) or concomitant alpha- and beta-blockade, the haemodynamic dose-response effects of propranolol (non-cardioselective, no ISA), pindolol (non-cardioselective, high ISA) and labetalol (non-cardioselective, alpha-blocker) were compared in a randomized study of 30 patients with stable coronary artery disease." | ( Beta-blockade in ischaemic heart disease--influence of concomitant ISA or alpha-blockade on haemodynamic profile. Ahuja, RC; Nelson, GI; Silke, B; Taylor, SH, 1983) | 0.44 |
"Long-acting propranolol (Inderal LA) is a new formulation of propranolol that allows release of the drug in a controlled manner, so that the plasma concentration at 24 hr after dosing is greater with long-acting propranolol than with conventional tablets." | ( Long-acting propranolol (Inderal LA): pharmacokinetics, pharmacodynamics and therapeutic use. Mishriki, AA; Weidler, DJ, ) | 0.89 |
" Because of the complex pharmacokinetics associated with multiple-dose administration and the variation in individual patient responsiveness to the drug, 'standard' dosing recommendations are difficult to determine; use of verapamil must be titrated to a clinical end-point." | ( Clinical pharmacokinetics of verapamil. Blouin, RA; Hamann, SR; McAllister, RG, ) | 0.13 |
" Drug dosage was twice daily and titrated according to casual clinic pressures (propranolol, 40 to 240 mg twice a day; verapamil, 120 to 240 mg twice a day)." | ( Propranolol versus verapamil for the treatment of essential hypertension. Gould, BA; Hornung, RS; Jones, RI; Raftery, EB; Sonecha, T, 1984) | 1.94 |
" Cumulative dose-response curves for isoproterenol, norepinephrine and methoxamine were made for the different groups." | ( In vitro contractile responses of the uterus from 'restricted diet' rats to adrenoceptor agonists. Influence of cyclo-oxygenase inhibitors. Gimeno, AL; Gimeno, MA; Goldraij, A; Sterin, AB, 1983) | 0.27 |
"In a double-blind, cross-over study the effect and tolerance of the non-selective beta-blocker propranolol in a dosage of 80 mg twice daily was compared to that of the beta 1-selective beta-blocker metoprolol 200 mg once daily in Durules (a controlled-release formulation)." | ( Metoprolol and propranolol in the prophylactic treatment of classical and common migraine. A double-blind study. Hedman, C; Kangasniemi, P, 1984) | 0.84 |
" Acid and pepsin secretion were inhibited in dose-response manner by dopamine in innervated mucosa, but all other effects of the compounds were different in parietal cells and chief cells and in vagally innervated and denervated mucosa." | ( Dopaminergic and adrenergic influence on gastric acid and pepsin secretion stimulated by food. The role of vagal innervation. Berstad, A; Guldvog, I; Linnestad, P; Schrumpf, E, 1984) | 0.27 |
" Cumulative dose-response curves to SCh were shifted to the right in a nearly parallel manner by (+)- and (-)-propranolol which were about equiactive." | ( Curare-like effect of propranolol on rat extraocular muscles. Chiarandini, DJ, 1980) | 0.79 |
" Free propranolol concentrations were lower 7 and 11 hr after dosing in the MI group, but concentrations thereafter were of the same order as those in subjects with CP." | ( Propranolol disposition after acute myocardial infarction. Norris, RM; Paxton, JW, 1984) | 2.19 |
" The beta 1,2 antagonist employed in the test decreased the contrast dosage by 13 per cent, causing the LD50." | ( Diazepam, alpha and beta neurotransmission modifying drugs and contrast media mortality in mice. Johansson, G; Luostarinen, M; Virkkunen, P, 1984) | 0.27 |
" Blood pressure was measured in standing and supine positions at the end of a dosing interval." | ( Once-daily propranolol for hypertension. Gefter, ML; Hemmes, RJ; Lopez, LM, 1984) | 0.66 |
" Thus a very steep dose-response curve was observed for each tissue." | ( Differences in threshold for protamine toxicity in isolated atrial and ventricular tissue. Caplan, RA; Su, JY, 1984) | 0.27 |
" Indobufen was first given as a single 200 mg dose and then for a 5 day period in a dosage of 200 mg twice daily, to six healthy volunteers." | ( Indobufen interacts with the sulphonylurea, glipizide, but not with the beta-adrenergic receptor antagonists, propranolol and atenolol. Elvander-Ståhl, E; Melander, A; Wåhlin-Boll, E, 1984) | 0.48 |
"Whole-body autoradiography of rats dosed with [14C]propranolol or [14C]nadolol have confirmed physicochemical predictions that nadolol, in contrast to propranolol, penetrates the CNS only to a slight extent, if at all." | ( Autoradiography of nadolol and propranolol in the rat. Saxey, A; Schiff, AA, 1984) | 0.81 |
" In both groups the AUC over the steady-state dosing interval was on the average 21-27% higher than the AUC after a single dose, indicating a slight decrease in the systemic clearance of l-propranolol during repetitive intravenous drug administration." | ( Pharmacokinetics of l-propranolol during repetitive dosing in normal and uranyl nitrate-induced renal failure rats. Shen, DD; Terao, N, 1984) | 0.77 |
" The mean concentration achieved in seminal plasma at 2 h after dosing was almost identical to that in blood serum." | ( Propranolol concentrations in blood serum, seminal plasma and saliva in man after a single oral dose. Grech, ED; Mahajan, P; Pearson, RM; Ridgway, EJ; Turner, P, 1984) | 1.71 |
" The degree of beta 1-blockade (reduction in exercise tachycardia) was much the same on both dosing regimens at trough concentrations." | ( Dynamics of propranolol dosing schedules. Coelho, JB; Dvornik, D; Kaufman, J; Krantz, KD; Lee, TY; Mullane, JF; Perdue, HS; Simon, J; Weidler, D, 1983) | 0.64 |
"To determine whether the depression of left ventricular pumping activity associated with beta-blockade alone could be offset by a substantial degree of partial agonist activity, the haemodynamic dose-response effects of intravenous propranolol and pindolol were compared in a randomised between-group saline controlled study in twenty patients with angiographically proven coronary artery disease." | ( Comparative haemodynamic dose-response effects of intravenous propranolol and pindolol in patients with coronary heart disease. Ahuja, RC; Nelson, GI; Okoli, RC; Silke, B; Taylor, SH, 1983) | 0.69 |
" The adrenaline-stimulated water flux exhibited a linear dose-response curve up to an adrenaline dosage of 750 micrograms kg-1; wt." | ( Cholinergic and adrenergic effects on diffusional water flux in the toadfish, Opsanus beta. Evans, DH; Oduleye, SO, 1983) | 0.27 |
" After an initial 2 week dosing period, all individuals additionally received 600 mg rifampicin daily for 3 weeks followed by a 4 week period during which again only the propranolol was given." | ( Induction of propranolol metabolism by rifampicin. Herman, RJ; Nakamura, K; Wilkinson, GR; Wood, AJ, 1983) | 0.83 |
" This dosage produced a minimal increase in heart rate and reduced the PR interval." | ( The search for a digitalis substitute II milrinone (Win 47203). Its action on the heart-lung preparation of the dog. Farah, A; Kabela, E; Mendez, R; Pastelin, G, 1983) | 0.27 |
" The dose-response curve for Phe was markedly shifted to the left by papaverine in 6W rats, but slightly in 7M rats." | ( Age-dependent differences in the positive inotropic effect of phenylephrine on rat isolated atria. Hashimoto, H; Nakashima, M; Sugino, N, 1983) | 0.27 |
" Propranolol (PROP) in sufficient dosage abolished the chemoreceptor response to NE and also markedly reduced the chemoreceptor response to hypoxia." | ( Interaction between norepinephrine and hypoxia on carotid body chemoreception in rabbits. Milsom, WK; Sadig, T, 1983) | 1.18 |
" Only the animals dosed with barbital exhibited severe withdrawal signs such as spontaneous withdrawal convulsions." | ( Effects of propranolol on barbital dependence formation and withdrawal signs. Hiramori, T; Nakao, K; Tagashira, E; Urano, T; Yanaura, S, 1983) | 0.66 |
" Dose-response curves were obtained one week prior to pretreatment and 24, 48, 72 and 168 hours after the last dose of propranolol." | ( Propranolol withdrawal-induced supersensitivity to the chronotropic effects of isoproterenol in the conscious rabbit. Tenner, TE, 1983) | 1.92 |
" Dosage was adjusted to achieve a standing heart rate of 60 beats/min unless adverse effects occurred." | ( Long-term medical management of hypertrophic cardiomyopathy: usefulness of propranolol. Abdulla, AM; Frank, MJ; Prisant, L; Stefadouros, MA; Watkins, LO, 1983) | 0.5 |
" Dosage was adjusted to a standing heart rate of 60 beats/min unless adverse drug effects developed." | ( Rhythm disturbances in hypertrophic cardiomyopathies: relationship to symptoms and the effect of 'complete' beta blockade. Abdulla, AM; Frank, MJ; Prisant, LM; Stefadouros, MA; Watkins, LO, 1983) | 0.27 |
" The dose-response curve for the stimulating effect of neostigmine on saliva production was shifted to the right in borderline hypertensive as compared with normotensive subjects." | ( Studies of salivary flow in borderline hypertension: effects of drugs acting on structures innervated by the autonomic nervous system. Rahn, KH; Schols, M; van Baak, MA; van Hooff, M, 1984) | 0.27 |
"The comparative haemodynamic dose-response effects of beta- (propranolol) or alpha- plus beta-blockade (labetalol) were evaluated in a randomised between-group study of 16 patients with an uncomplicated acute myocardial infarction." | ( Comparison of haemodynamic dose-response effects of beta- and alpha-beta-blockade in acute myocardial infarction. Ahuja, RC; Nelson, GI; Silke, B; Taylor, SH; Walker, C, 1984) | 0.51 |
" The dose-response curve describing LTD4-induced changes in dynamic lung compliance (CDYN) and pulmonary resistance (RL) [as reflective indices of bronchoconstriction] was shifted to the left by approximately 20-fold by propranolol." | ( Propranolol potentiates leukotriene D4-induced bronchoconstriction and enhances antagonism by FPL 55712. Kirchner, T; Weichman, BM, 1984) | 1.9 |
"To evaluate the possible influence of sympathetic activation on the haemodynamic response to intravenous beta-blockade, the dose-response characteristics of three boluses of propranolol were evaluated in 8 patients with uncomplicated infarction and compared in a similar number of patients with stable angina." | ( Enhanced haemodynamic effects of propranolol in acute myocardial infarction. Ahuja, RC; Hussain, M; Nelson, GI; Silke, B; Taylor, SH; Verma, SP; Walker, C, 1984) | 0.74 |
" Also during treatment, fewer patients receiving hydrochlorothiazide required termination as compared with those receiving propranolol; comparative dosage requirements were lower; additional titration during long-term treatment was required less often, and BP remained lower after withdrawal of the active drugs." | ( Comparison of propranolol and hydrochlorothiazide for the initial treatment of hypertension. II. Results of long-term therapy. Veterans Administration Cooperative Study Group on Antihypertensive Agents. , 1982) | 0.83 |
" Dosage was titrated for each patient to achieve normotensive levels and was in the range of 40 to 320 mg twice daily." | ( Comparison of antihypertensive efficacy: propranolol versus oxprenolol in accelerated hypertension. Fernandez, PG; Galway, AB; Granter, S; Kim, BK; Sharma, JN; Zachariah, PK, 1982) | 0.53 |
" A booster dosage of 5 to 20 mg of minoxidil was given at four hours if the diastolic BP exceeded 100 mm Hg." | ( Rapid control of severe hypertension with minoxidil. Alpert, MA; Bauer, JH, 1982) | 0.26 |
" Prior to study, 2 hours post dosing and coincident with immediate pre-exercise on treadmill, at graded increases of exercise and 2 hours post exercise (approximately 4 hours post dosing), blood was sampled for potassium, renin concentration, aldosterone and catecholamines." | ( Potassium disposition and neuroendocrine effects of propranolol, methyldopa and clonidine during dynamic exercise. Affrime, MB; Falkner, B; Hakki, H; Lowenthal, DT; Rosenthal, L; Saris, S, 1982) | 0.51 |
" Before the study, 2 hr after dosing and coincident with immediate preexercise on treadmill (at graded increases of exercise), and 2 hr after exercise, blood was sampled for determination of potassium, renin, aldosterone, and catecholamine levels." | ( Biochemical and dynamic responses to single and repeated doses of methyldopa and propranolol during dynamic physical activity. Affrime, MB; Falkner, B; Gould, AB; Lowenthal, DT; Rosenthal, L; Saris, S, 1982) | 0.49 |
" Long-acting propranolol in a once daily dosage of 160 mg proved to be effective over a 6-week period of treatment with no significant side-effects." | ( Comparison of sustained-release clonidine and long-acting propranolol in the treatment of hypertension. Lawson, AA; Rodrigues, E, 1982) | 0.88 |
" and may be preferred by some patients because of the simple dosage regimen." | ( Metoprolol in angina pectoris complicated by essential hypertension. A clinical comparison of the antianginal efficacy of metoprolol slow-release tablets (Durules) given once daily and propranolol tablets given twice daily. BLoem, TJ; Lindner, PC, 1981) | 0.45 |
" The dosage of each drug was adjusted at monthly clinic visits until satisfactory control of blood pressure was achieved (140/90 mm Hg or less by cuff) or the maximum dose in the study protocol was reached." | ( Ambulatory blood pressure during once-daily randomised double-blind administration of atenolol, metoprolol, pindolol, and slow-release propranolol. Floras, JS; Hassan, MO; Jones, JV; Sleight, P, 1982) | 0.47 |
" Each treatment was given for a period of 4 weeks at two different dosage regimens (150 and 300 mg daily for metoprolol, 120 and 240 mg daily for propranolol)." | ( Controlled study of metoprolol and propranolol during prolonged administration in patients with essential tremor. Calzetti, S; Findley, LJ; Perucca, E; Richens, A, 1982) | 0.74 |
" Each compound was administered by intravenous single dose injection, dosage being 1 mg/kg for propranolol, 10 mg/kg for phenytoin, and 3,5 mg/kg for lidocain." | ( [Pharmacokinetics of propranolol, phenytoin and lidocaine in hypercholesterolemic rabbits]. Albin, H; Pehourcq, F; Ploux, D; Vinçon, G, ) | 0.67 |
" 5 Clinically important changes in drug effect may be present acutely, within the dosing interval, as a result of altered drug binding." | ( Variations in drug free fraction during alcohol withdrawal. Khouw, V; Naranjo, CA; Sandor, P; Sellers, EM, 1983) | 0.27 |
"1 The effects on heart rate and blood pressure after single and multiple dosing (1 month) of a long acting formulation of propranolol 160 mg daily, and conventional propranolol, 80 mg twice daily, or 160 mg daily were compared in 11 moderately hypertensive subjects previously shown to respond to propranolol." | ( The pharmacodynamics and pharmacokinetics of conventional and long-acting propranolol in patients with moderate hypertension. Breckenridge, AM; Green, GJ; MacIver, M; Orme, ML; Serlin, MJ; Sibeon, RG, 1983) | 0.7 |
"3 mg/kg) or prazosin in high dosage (0." | ( Bronchopulmonary effects of clonidine on the bronchomotor responses of the guinea-pig. Advenier, C; Floch, A; Mallard, B, 1983) | 0.27 |
" Inhalation dose-response curves to PGE2 in doses from 10 to 400 micrograms were constructed on three separate occasions." | ( The effects of oral propranolol and indomethacin on the response to inhaled PGE2 in normal human subjects. Bevan, M; Davies, BH; Walters, EH, 1982) | 0.59 |
" The daily dosage of propranolol and clonidine was 160 mg and 100 microgram, respectively." | ( Propranolol (Inderal) and clonidine (Catapressan) in the prophylactic treatment of migraine. A comparative trial. Kåss, B; Nestvold, K, 1980) | 2.02 |
" When compared with previous work, these results indicate that propranolol attenuates nitroprusside-induced renin release, reduces the dosage of nitroprusside required to induce hypotension, suppresses reflex tachycardia, and prevents overshoot hypertension on discontinuation of nitroprusside." | ( Propranolol alters renin release during nitroprusside-induced hypotension and prevents hypertension on discontinuation of nitroprusside. Khambatta, HJ; Khan, E; Stone, JG, 1981) | 1.94 |
" 4 The synergistic effect was even more pronounced after reduction in propranolol dosage to 50% of the beta-adrenoceptor blocking dose, reflecting the myocardial depressant effects of beta-adrenoceptor blocking drugs in these patients with coronary heart disease, some of whom had poor left ventricular function." | ( The combination of nifedipine and propranolol in the management of patients with angina pectoris. Beattie, JM; Hutton, I; Murray, RG; Tweddel, AC, 1981) | 0.78 |
" Consequently, the insulin dose-response curve of SSBG apparently shifted rightwards in KK mice." | ( Determination of overall insulin sensitivity in diabetic mice, KK. Ikeda, H; Ishikawa, E; Iwatsuka, H; Taketomi, S, 1982) | 0.26 |
" Pindolol and propranolol lowered PRA comparably at equivalent dosages, although this effect was not consistently observed in all studies or at all dosage levels." | ( Pindolol: effects on blood pressure and plasma renin activity. Bennett, CM; Glassock, RJ; Gonasun, L; Hamilton, B; Kirkendall, W; Maxwell, M; Weitzman, RE; Winer, N, 1982) | 0.62 |
" Steady-state TCA plasma levels correlate well with tissue concentrations and permit adjustment of dosage to minimize the risk of iatrogenic poisoning." | ( Toxicity of tricyclic antidepressants--kinetics, mechanism, intervention: a review. Irwin, HA; Preskorn, SH, 1982) | 0.26 |
" Following infusion of propranolol to the mother, steady-state plasma concentrations were obtained at three dosage levels in each of the eight animals studied." | ( The developing liver: the steady-state disposition of propranolol in pregnant sheep. Hardy, KJ; Mihaly, GW; Morgan, DJ; Smallwood, R, ) | 0.69 |
"(1) The methods available for assessment of the regulatory features of dose-response relationships that do not conform to the Hill equation are considered, and the sensitisation index Si introduced (2) The value of determining Si is assessed using lipolytic dose-response relationships yielded by beta-adrenergic agonists both alone and in the presence of their specific antagonists [D." | ( Analysis of apparent co-operativity in the catecholamine-stimulated lipolysis of rat adipose tissue. Cooper, DM; Davies, JI; Everett, D, 1982) | 0.26 |
"Experiments have been carried out in dogs and man to determine the effect of hydrochlorothiazide (HCT) on the pharmacokinetics of propranolol and to evaluate the bioavailability of two dosage forms containing both propranolol and HCT (40/25 and 80/25 mg, respectively)." | ( Biopharmaceutical characteristics of a new propranolol/hydrochlorothiazide tablet combination. Dubuc, J; Dvornik, D; Kraml, M; Lee, TY; Mullane, J; Patterson-Kreuscher, S; Perdue, H, ) | 0.6 |
"Following oral dosing to steady state, the disposition of S(-)- and R(+)-propranolol and their corresponding glucuronide conjugates was studied in 4 healthy adults using doses from 40 to 320 mg/day of the racemate." | ( Stereoselective disposition and glucuronidation of propranolol in humans. Holford, NH; Riegelman, S; Silber, B, 1982) | 0.75 |
" During multiple oral dosage (80 mg every 12 h), observed steady state serum levels (47 +/- 5 ng/ml) tended to be less than those predicted based on the single oral dose (61 +/- 5 ng/ml), thus providing no evidence for reduced propranolol clearance at steady-state." | ( Kinetics and cardiac effects of propranolol in humans. Bodem, G; Greenblatt, DJ; Grube, E; Knüchel, M; Ochs, HR, 1982) | 0.73 |
" Incubation of tissues with papaverine (1 hr) changed the usual dose-response curve to isoproterenol into a low, monotonous effect, independent of the agonist dose." | ( Papaverine-induced changes on cardiac inotropism with special reference to a D-propranolol antagonism. Aramendía, P; Márquez, MT, 1982) | 0.49 |
" Preliminary results of prophylactic treatment with propranolol are encouraging; smaller dosage than those previously recommended sometimes can be effective." | ( Hemiplegic migraine in childhood: diagnostic and therapeutic aspects. Lai, CW; Lansky, LL; Torres, F; Ziegler, DK, 1982) | 0.51 |
"One hundred sixty-nine normal men received varying propranolol dosage regimens and placebo." | ( Propranolol dosage, plasma concentration, and beta blockade. Coelho, J; Dvornik, D; Kaufman, J; Mullane, JF, 1982) | 1.96 |
" Since concentrations which suppress the lymphocyte mitogen dose-response are much greater than the Kd for the binding site, it may be suggested that the suppression of the mitogen dose-response is a result of nonspecific effects of propranolol." | ( Use of fluorescent probes to monitor propranolol effects on the murine splenic lymphocyte. Audus, KL; Gordon, MA; Johnson, DL, ) | 0.59 |
" The combination was given in a dosage that produced values for systemic blood pressure, heart rate, and maximal positive left-ventricular dP/dt (LV dP/dt) that were similar to those produced by halothane." | ( Treatment of myocardial ischemia with halothane or nitroprusside-propranolol. Bainton, CR; Gerson, JI; Hickey, RF, 1982) | 0.5 |
" Additionally, EVI(+)S dose-response curves of classical signs of digitalis cardiac toxicity shifted to the left." | ( Chagasic sera alter the effects of ouabain on isolated rat atria. Participation of adrenergic mechanisms. Arana, R; Borda, E; Canga, L; Cossio, P; Diez, C; Gimeno, AL; Sterin-Borda, L, 1981) | 0.26 |
" The dosage can be sufficiently guided by clinical evaluation of effect." | ( Essential tremor treated with propranolol: lack of correlation between clinical effect and plasma propranolol levels. Jansen, EC; Paulson, OB; Steiness, E; Sørensen, PS, 1981) | 0.55 |
" It is concluded that in the doses used, slow release oxprenolol administered once daily does not exert as consistent a beneficial effect on exercise tolerance throughout the dosing schedule as does propranolol given four times daily." | ( Slow release oxprenolol in angina pectoris: study comparing oxprenolol, once daily, with propranolol, four times daily. Olowoyeye, JO; Parker, JO; Thadani, U, 1981) | 0.67 |
"Criteria for the choice of drug dosage are established." | ( [Determination of the criteria for selecting the optimal obsidan and hypothiazide treatment regimen in hypertension based on mathematical modelling data]. Churnosov, EV; Katiukhin, VN; Temirov, AA, 1981) | 0.26 |
" He responded to ventilator support, transvenous pacing, and massive dosage of isoprenaline." | ( Self-poisoning with propranolol. Fisher, MM; Ibels, LS; Tynan, RF, 1981) | 0.59 |
" In addition, in five patients the area under the plasma propranolol concentration versus time curve during a dosing interval increased significantly from 405 ng/ml/h when hyperthyroid to 778 ng/ml/h when euthyroid." | ( Plasma propranolol steady state concentrations in thyroid disorders. Crooks, J; Feely, J; Stevenson, IH, 1981) | 0.96 |
" Pyd action is modified only by the most active purine 2-Cl-adenosine, which displaces the dose-response curves to the right." | ( Interactions between hydralazine, propildazine and purines on arterial smooth muscle. Chevillard, C; Saiag, B; Worcel, M, 1981) | 0.26 |
" On rechallenge with 10 mg qid the patient displayed no problems; however, when the dosage was increased to 20 mg qid, the diarrhea returned." | ( Severe diarrhea secondary to propranolol. Burtner, DE; Robinson, JD, 1981) | 0.55 |
" However, a higher proportion of patients achieved satisfactory control (BP less than 160/95 mm Hg) on FUR than on HCT and, in addition, there was a more marked dose-response effect with FUR." | ( Controlled comparison of the effects of furosemide and hydrochlorothiazide added to propranolol in the treatment of hypertension. Dombey, SL; Lawrence, J; Vander Elst, E; Vlassak, W, 1981) | 0.49 |
" The amount of isoproterenol required to increase the heart rate by 25 beats/min was determined at each dosage level." | ( Beta adrenergic blockade with propranolol in conscious euthyroid and thyrotoxic calves: dosage requirements and effects on heart rate and left ventricular performance. Goldman, S; Mayersohn, M; Morkin, E; Olajos, M; Perrier, D; Pieniaszek, H, 1981) | 0.55 |
" Comparison of the systemic blood levels obtained after peripheral and portal dosage indicated that hepatic extraction was much more efficient in the adult." | ( Fetal hepatic function: the disposition of propranolol in the pregnant sheep. Hardy, KJ; Marshall, AW; Mihaly, GW; Morgan, DJ; Smallwood, RA, 1981) | 0.53 |
" 4 Forearm blood flow, at rest, was significantly reduced at 2 h after dosing with propranolol, but not after acebutolol." | ( The effects of oral acebutolol and propranolol on forearm blood flow in hypertensive patients. Ireland, MA; Littler, WA, 1981) | 0.76 |
" In aortic strip preparations, Wu-Chu-Yu caused the increase of contractile force, and the dose-response curve was parallel shift to the right in the presence of phentolamine." | ( In vivo and in vitro studies on the mechanism of cardiovascular effects of Wu-Chu-Yu (Evodiae fructus). Chen, CF; Chen, SM; Chow, SY; Lin, MT, 1981) | 0.26 |
" dosage the radioactivity was largely cleared via the kidneys." | ( Disposition of pranolium chloride in dogs, baboons and monkeys. Allan, L; Barrow, A; Haskins, NJ; Palmer, RF; Rogers, M; Rose, DA, 1981) | 0.26 |
" Conventional propranolol at a dosage of 160 mg/day was frequently insufficient to produce a high degree of beta-adrenergic blockade, particularly in severely thyrotoxic patients." | ( Propranolol in the surgical treatment of hyperthyroidism, including severely thyrotoxic patients. Crooks, J; Feely, J; Forrest, AL; Gunn, A; Hamilton, WF, 1981) | 2.07 |
" The chronotropic dose-response curves were made in both spontaneously beating atria while inotropic effects were derived from left atria driven at 1 Hz, 5 msec and voltage about 20 percent above threshold." | ( Interactions between sympathomimetic agonists and blocking agents: cardiac effects of phenylephrine and isoproterenol. Aramendía, P; Márquez, MT; Mikulić, LE, ) | 0.13 |
" Despite this, PGE2 caused bronchodilatation and reproducible dose-response curves were obtained, with a maximum increase in sGaw of 53%." | ( Effect of propranolol on the airway response to prostaglandin E2 in normal man. Clarke, VS; Lewis, RA; Seth, RV; Tattersfield, AE, 1981) | 0.67 |
" The variability in the areas under the concentration-time curves of propranolol appeared to be smaller after the 80-mg twice-a-day dosing schedule." | ( Comparative bioavailability of propranolol: twice-daily versus four times-daily administration. Dubuc, J; Dvornik, D; Kraml, M; Milosovich, G; Mullane, JF; Patterson-Kreuscher, S, ) | 0.65 |
" Once-daily propranolol dosage was well tolerated and possibly gave less rise to the troublesome side effect of vivid dreaming." | ( One and three doses of propranolol a day in hypertension. Boer, P; Dorhout Mees, EJ; Geyskes, GG; van Asten, P; van den Brink, G, 1980) | 0.95 |
"The effect of conventional propranolol and bendrofluazide tablets given twice daily has been compared with an equivalent dosage combined in a single capsule given twice daily in fourteen patients with essential hypertension." | ( Treatment of essential hypertension with a combination of propranolol and bendrofluazide. Dawes, PM; Solomon, LR, 1980) | 0.8 |
"The dose-response and time-action parameters for the prototype antiarrhythmic drugs lidocaine, propranolol and quinidine were established using a cardiac antiarrhythmic screening procedure in the rat." | ( A cardiac antiarrhythmic screening test in the rat: the effects of lidocaine, propranolol and quinidine. Baker, T; Erker, EF, 1980) | 0.71 |
" The areas under the plasma concentration curve at conversion of ventricular tachycardia to sinus rhythm were similar for both dosage groups with area under the plasma concentration curve proportional to myocardial UM-272 concentration." | ( Plasma and myocardial tissue concentrations of UM-272 (N,N-dimethylpropranolol) after oral administration in dogs. Lucchesi, BR; Patterson, E; Stetson, P, 1980) | 0.5 |
" In patients as well as in normal subjects, the data indicated considerable beta-blocking effects for both drugs at the end of a 12-hourly dosing schedule, suggesting that twice-daily timolol and propranolol may be clinically practical." | ( Plasma timolol levels and systolic time intervals. Chew, C; Collett, J; Singh, BN; Whitlock, RM; Williams, FM, 1980) | 0.45 |
" Steady-state daily dosage of propranolol averaged 225 +/- 36 mg (range, 80 to 400)." | ( Massive propranolol metabolite retention during maintenance hemodialysis. Stone, WJ; Walle, T, 1980) | 0.98 |
" In a group of 40 patients, including 10 severely thyrotoxic patients, who had the dosage of propranolol titrated objectively preoperatively to bring about a greater than 25% reduction in exercise heart rate at the end of a dosage interval, no case of thyroid storm was encountered." | ( Propranolol dosage in thyrotoxicosis. Crooks, J; Feely, J; Forrest, A; Gunn, A; Hamilton, W; Stevenson, I, 1980) | 1.92 |
" If the elimination of this drug is enhanced in thyrotoxic patients, one may consider necessary a modification of the dosage regimien when treating patients with this dysfunction." | ( No enhanced elimination of propranolol in patients with hyperthyroidism. Ishizaki, T; Masuno, M; Tawara, K, 1980) | 0.56 |
" The resting heart rate is faster with labetalol than with an equivalent dosage of propranolol." | ( Comparison of labetalol and propranolol in treatment of hypertension. Harvald, B, 1980) | 0.78 |
" Adequate beta-adrenoceptor blockade in hyperthyroid patients may require higher propranolol dosage than expected." | ( Effects of thyroid dysfunction on propranolol kinetics. Kelly, JG; McDevitt, DG; Neill, JD; Riddell, JG, 1980) | 0.77 |
" In addition, the findings support the assumption that therapeutic failure with beta-blockers in hyperthyroidism may be due to suboptimal treatment, and that individualized dosage is necessary." | ( Effects and plasma levels of propranolol and metoprolol in hyperthyroid patients. Melander, A; Nilsson, OR; Tegler, L, 1980) | 0.55 |
" In the dosage range studied, the amount of propranolol reaching the systemic circulation increased with dose, while half-lives remained unchanged." | ( Dose-dependent disposition of oral propranolol in normal subjects. Jusko, WJ; Mackichan, JJ; Pyszczynski, DR, ) | 0.67 |
" Dose-response curves for heart rate, cardiac output, arterial blood pressure and pulmonary artery pressure were obtained in 16 male patients after intravenous administration of three increasing doses of pindolol, propranolol or placebo." | ( A comparison of the acute haemodynamic effects of propranolol and pindolol at rest and during supine exercise in man. Carlsen, JE; Hartling, O; McNair, A; Svendsen, TL; Trap-Jensen, J, 1980) | 0.7 |
" Dose-response curves obtained for carbachol and isoproterenol indicated that the maximum response to carbachol is greater than that to isoproterenol but that the threshold for response to isoproterenol is much lower than that to carbachol." | ( Autonomic control of lacrimal protein secretion. Bromberg, BB, 1981) | 0.26 |
" 6 There is, therefore, no pharmacokinetic basis to adjust the dosage of propranolol in patients with renal failure." | ( Propranolol disposition in renal failure. Shand, DG; Spannuth, CL; Stone, WJ; Vestal, RE; Wilkinson, GR; Wood, AJ, 1980) | 1.94 |
" caused dose-dependent parallel rightward shifts of the dose-response curves (DBP and LVdP/dtmax) without altering the maximal responses to AII." | ( Effect of various angiotensin receptor antagonists on cardiovascular responses to angiotensin II in pithed rats. Pfaffendorf, M; van Zwieten, PA; Zhang, J, 1994) | 0.29 |
" Dose-response curves of the sedative effect of the alpha 2 adrenergic receptor agonist clonidine were established, a sedative effect being defined as a decrease in overall horizontal displacements, rearings and hole visits." | ( Novelty seeking behavior in the rat is dependent upon the integrity of the noradrenergic system. Dyon-Laurent, C; Hervé, A; Sara, SJ, 1995) | 0.29 |
" In nonfailing ventricular myocardium, both DL-sotalol and D-sotalol shifted the dose-response curve for isoproterenol to higher concentrations (P < ." | ( Positive and negative inotropic effects of DL-sotalol and D-sotalol in failing and nonfailing human myocardium under physiological experimental conditions. Fraedrich, G; Hasenfuss, G; Holubarsch, C; Just, H; Pieske, B; Posival, H; Ruf, T; Schneider, R, 1995) | 0.29 |
" Losartan, but not PD123177, shifted the dose-response curves for AII to the right in a parallel manner." | ( Hemodynamic effects of angiotensin II and the influence of angiotensin receptor antagonists in pithed rabbits. Pfaffendorf, M; van Zwieten, PA; Zhang, J, 1995) | 0.29 |
") was used in all experiments except the dose-response relationship study." | ( Role of the sympathoadrenal axis in the cardiovascular response to cocaine in conscious unrestrained rats. Chen, BX; Myles, J; Wilkerson, RD, 1995) | 0.29 |
" Therefore, this study was designed to determine whether differences in the disposition of S- and R-propranolol occur in humans when altering the input rate of propranolol by giving different dosage forms of the drug." | ( The effect of dosage release formulations on the pharmacokinetics of propranolol stereoisomers in humans. Amidon, GL; Bleske, BE; Rose, S; Shea, MJ; Welage, LS, 1995) | 0.74 |
" Though acute reversible psychosis has been appreciated after initiating or increasing propranolol dosage therapeutically, this association has not been reported in the literature regarding beta blocker overdose or intoxication." | ( Toxic psychosis: an unusual presentation of propranolol intoxication. Handler, JA; Love, JN, 1995) | 0.78 |
" alpha-Adrenoceptor blockade by dopexamine and fenoldopam was confirmed by the parallel displacement of dose-response curves for the vasopressor responses to noradrenaline." | ( Renal vasodilatation by dopexamine and fenoldopam due to alpha 1-adrenoceptor blockade. Broadley, KJ; Martin, SW, 1995) | 0.29 |
" Propranolol (4 mg) was dosed into the reservoir as a single bolus and perfusate and bile sampled over 150 min." | ( Fetal hepatic propranolol metabolism. Studies in the isolated perfused fetal sheep liver. Ching, MS; Ghabrial, H; Morgan, DJ; Ring, JA; Shulkes, A; Smallwood, RA, 1995) | 1.56 |
" Thirty-three patients were randomized to relaxation-biofeedback training alone (administered in a limited-contact treatment format), or to relaxation-biofeedback training accompanied by long-acting propranolol (with dosage individualized at 60, 120, or 180 mg/day)." | ( Enhancing the effectiveness of relaxation-thermal biofeedback training with propranolol hydrochloride. Cordingley, GE; France, JL; Holroyd, KA; Kvaal, SA; Lipchik, GL; McCool, HR; Rokicki, LA, 1995) | 0.71 |
"The intravenous and oral dose kinetics and metabolism of the enantiomers of propranolol were investigated in five dogs during steady-state oral racemic propranolol dosing (5 mg/kg, every 8 hr for 3 days)." | ( Effects of diltiazem on the disposition and metabolism of the enantiomers of propranolol in the dog during multiple oral dosing. Bai, SA; Lankford, SM; Maskasame, C, ) | 0.59 |
" Specificity of the method for 1045U85 was demonstrated using spiked plasma samples as well as plasma samples from dosed animals." | ( Development and validation of a chiral LC method for analysis of the four stereoisomers of 1045U85 in plasma. Deal, DL; McNulty, MJ; Page, TL, 1994) | 0.29 |
" Drugs were dosed cumulatively after the second, fourth and sixth exercise periods." | ( The haemodynamic actions of ZENECA ZD7288, a novel sino-atrial node function modulator, in the exercising beagle: a comparison with zatebradine and propranolol. Johnson, IR; Rouse, W; Stafford, PJ, 1994) | 0.49 |
" The pulmonary vascular dose-response relation to the sympathetic alpha-adrenoreceptor agonist phenylephrine also was investigated in conscious and isoflurane-anesthetized dogs (n = 6)." | ( Isoflurane and the pulmonary vascular pressure-flow relation at baseline and during sympathetic alpha- and beta-adrenoreceptor activation in chronically instrumented dogs. Lennon, PF; Murray, PA, 1995) | 0.29 |
"75, 10, and 30 mg) of cilazapril reduced diastolic blood pressure dose-dependently and shifted the angiotensin I dose-response curves to the right." | ( Review of studies on the clinical pharmacodynamics of cilazapril. Belz, GG; Breithaupt, K; Erb, K, 1994) | 0.29 |
" Activation of thermogenesis with the selective beta 3-agonist BRL 35135 (BRL) reduced heat influx by both obese and lean rats at doses between 2 and 10 micrograms/kg, but no dose-response effects were evident within this range." | ( Effects of beta-adrenoceptor agonists and antagonists on thermoregulation in the cold in lean and obese Zucker rats. Carlisle, HJ; Dubuc, PU; Stock, MJ, 1993) | 0.29 |
" Most antihypertensives can be given once or twice daily without the need for sustained-release dosage forms." | ( Selected factors that influence responses to antihypertensives. Choosing therapy for the uncomplicated patient. Carter, BL; Elliott, WJ; Frohlich, ED; Mann, RJ; Moore, MA; Roberts, RW, 1994) | 0.29 |
" A propranolol dose-response was studied for each strain: (1) saline solution controls (n = 18); (2) propranolol, 10 mg/kg subcutaneously (n = 18); (3) propranolol, 30 mg/kg (n = 14)." | ( Expansion of aortic aneurysms is reduced by propranolol in a hypertensive rat model. Gadowski, GR; Hendley, ED; Pilcher, DB; Ricci, MA; Slaiby, JM, 1994) | 1.17 |
"This study investigated the effects of isamoltane on the changes induced by cumulative doses of inhaled albuterol (salbutamol) on bronchomotor tone, skeletal muscle, circulatory system, and metabolism after single (day 1) and multiple dosing (day 7) in 15 healthy subjects." | ( Assessment of beta-adrenergic receptor blockade after isamoltane, a 5-HT1-receptor active compound, in healthy volunteers. Bauer, K; Dietersdorfer, F; Kaik, G, 1993) | 0.29 |
" The hypotensive action of NZ-105 were reproducible after repeated dosing for 12 weeks." | ( Effects of long-term oral administration of NZ-105, a novel calcium antagonist, with or without propranolol in spontaneously hypertensive rats. Kasuya, Y; Masuda, Y; Sakai, T; Shigenobu, K; Shudo, C; Tanaka, S, 1993) | 0.5 |
" On a dosage basis, the order of antifibrillatory potency of these compounds is: carazolol-FD > propranolol-FD > carazolol > propranolol > celiprolol-FD > celiprolol." | ( Synthesis and pharmacological evaluation of the antifibrillatory effect of fluorinated derivatives of carazolol and celiprolol: comparison with propranolol. Aboul-Enein, HY; Almotrefi, AA; Dzimiri, N; Premkumar, LS, 1993) | 0.7 |
" Dosage had no influence on the plasma binding of either enantiomer." | ( Contribution of differences in plasma binding of propranolol to ethnic differences in sensitivity. Comparison between Chinese and Caucasians. Shay, SD; Wood, AJ; Zhou, HH, 1993) | 0.54 |
" All patients took propranolol at a dosage of 10 mg, 3 times a day for 7 days." | ( Pharmacokinetics of propranolol used for suppressing tachycardia in hyperthyroidism. Masuda, H; Miyake, F; Motohashi, F; Murayama, M; Musha, H; Sugai, J; Takada, H, 1994) | 0.94 |
" In the rats dosed with propranolol and clenbuterol plus propranolol, no modifications occurred in estrogen receptor concentrations when compared with control values." | ( Regulation of uterine estrogen receptors (ER) by beta-adrenergic stimulation in immature rats. Badino, P; Dacasto, M; Di Carlo, F; Girardi, C; Re, G, 1993) | 0.59 |
" Drug interaction studies with fluvastatin and cholestyramine (CME) demonstrated a lower rate and extent of fluvastatin bioavailability; no impact on efficacy was demonstrated when CME was given 4 h before fluvastatin dosing in clinical trials." | ( Pharmacokinetics of fluvastatin and specific drug interactions. Hwang, DS; Jokubaitis, LA; Robinson, WT; Smith, HT; Troendle, AJ, 1993) | 0.29 |
" The overall increase in aggression observed following dosing with propranolol was not expected from a review of the clinical literature." | ( Propranolol-induced increases in target-biting attack. Matray-Devoti, J; Wagner, GC, 1993) | 1.96 |
" NA increased mucociliary activity at a dosage of 10(-5) mol/kg, the maximal increase being 16." | ( The effect of noradrenaline on mucociliary activity in the rabbit maxillary sinus. Cervin, A; Lindberg, S; Mercke, U, 1993) | 0.29 |
"Combined treatment with propranolol and reserpine enhanced acetylcholine-induced dose-response curves for bronchoconstriction in guinea pigs in vivo." | ( Pharmacological model for airway hypersensitivity produced by propranolol and reserpine in guinea pigs. Goto, S; Inagaki, N; Koda, A; Nagai, H, 1993) | 0.83 |
" These results suggest that propranolol is absorbed more rapidly after morning dosing than after night-time dosing in younger but not in older subjects." | ( The effect of age on diurnal variation in the pharmacokinetics of propranolol in hypertensive subjects. Ebihara, A; Fujimura, A; Ohashi, K; Shiga, T; Tateishi, T, 1993) | 0.82 |
"Prospective dose-response study with each animal serving as it own control." | ( Effects of dopexamine on hemodynamics and oxygen consumption after beta blockade in lambs. Rogers, BW; Sziszak, TJ; Sziszak, TL; Taylor, BJ, 1993) | 0.29 |
"Previous studies have shown that the absorption rate of a lipophilic, but not hydrophilic, agent is faster after the night dosage than after the morning dosage in nocturnal rodents." | ( Differences of chronopharmacokinetic profiles between propranolol and atenolol in hypertensive subjects. Ebihara, A; Fujimura, A; Ohashi, K; Shiga, T; Tateishi, T, 1993) | 0.53 |
" One capsule was taken for three days and then the dosage was doubled for the remainder of a four-week period." | ( Effect of hydrochlorothiazide, enalapril, and propranolol on quality of life and cognitive and motor function in hypertensive patients. Annett, MP; Culbert, JP; McCorvey, E; McKenney, JM; Proctor, JD; Wright, JT, 1993) | 0.54 |
"The effect of propranolol dosing rate on beta-blockade was studied in human volunteers after administration of a conventional tablet and a sustained release capsule." | ( Dosing rate-dependent relationship between propranolol plasma concentration and beta-blockade. Kashiwada, K; Ogata, H; Ohira, M; Someya, K; Takahashi, H, 1993) | 0.91 |
"04 mg/kg); oral quinidine was then administered at a daily dosage of 1,200 mg for 3 to 4 days, after which the QT duration was reassessed using the same method in a second study." | ( Direct and autonomically mediated effects of oral quinidine on RR/QT relation after an abrupt increase in heart rate. Alboni, P; Antonioli, GE; Cappato, R; Codecà, L; Guardigli, G; Toselli, T, 1993) | 0.29 |
" It was concluded that bethanechol and, less likely, neostigmine at the dosage used in this study may be suitable for medical treatment of cecal dilatation in cattle in which hypomotility of the cecum and proximal loop of the ascending colon has to be reversed." | ( Effect of bethanechol, neostigmine, metoclopramide, and propranolol on myoelectric activity of the ileocecocolic area in cows. Martig, J; Roussel, AJ; Steiner, A, 1995) | 0.54 |
" Analyses of dose-response relationships indicated that the degree of inhibition increased with increasing dose." | ( The inhibitory effects of propranolol on genital reflexes in male rats. Cetrulo, EJ; Clark, JT; Davidson, JM; Donahue, JP; Hoffman, BB; Smith, ER; Sparrow, H, 1995) | 0.59 |
" The fentanyl dose-response curve was unchanged by opioid receptor blockade with 10(-6)M naloxone and by alpha and beta adrenoceptor blockade produced by 10(-6)M prazosin and 10(-6)M propranolol." | ( Direct effects of fentanyl on canine coronary artery rings. Bridges, MT; Grover, TE; Introna, RP; Pruett, JK; Yodlowski, EH, 1995) | 0.48 |
" Rats dosed orally (100 mg/kg) were fully protected from VF." | ( Efficacy of the class III antiarrhythmic agent azimilide in rodent models of ventricular arrhythmia. Brooks, RR; Carpenter, JF; Maynard, AE; Miller, KE, 1996) | 0.29 |
" Spironolactone was administered during a 6-week period at a dosage of 100 mg/d." | ( The effect of long-term treatment with spironolactone on variceal pressure in patients with portal hypertension without ascites. Fevery, J; Lijnen, P; Nevens, F; VanBilloen, H, 1996) | 0.29 |
" With coadministration, the maximum peak concentration (Cmax) and area under the concentration-time curve over the dosing interval (AUC tau) of propranolol decreased 29% and 14%, respectively; Cmax and AUC tau of 4-hydroxy-propranolol decreased 15% and 21%, respectively." | ( Pharmacokinetic and pharmacodynamic evaluation during coadministration of nefazodone and propranolol in healthy men. Fulmor, IE; Lee, JS; Marathe, PH; Raymond, RH; Salazar, DE; Uderman, HD, 1995) | 0.71 |
" Dose-response curves to isoproterenol (10(-9)-10(-8) M) and phenylephrine (10(-9)-10(-6) M) were also obtained." | ( Ricin depresses cardiac function in the rabbit heart. Hsu, CH; Ma, L; Patterson, E; Robinson, CP; Thadani, U, 1996) | 0.29 |
" In nine other rats a lower dosage (5 mg kg-1) was used." | ( Haemodynamic and electrophysiological acute toxic effects of mercury in anaesthetized rats and in langendorff perfused rat hearts. Amaral, SM; Massaroni, L; Oliveira, EM; Rossoni, LV; Stefanon, I; Vassallo, DV, ) | 0.13 |
" At the end of each dosage level, serum electrolytes, catecholamines, and an electrocardiogram were recorded." | ( Epinephrine-induced changes in serum potassium and cardiac repolarization and effects of pretreatment with propranolol and diltiazem. Darbar, D; Mörike, K; Roden, DM; Smith, M, 1996) | 0.51 |
"Using an isolated, electrically stimulated rat left afrium model, the dose-response curves to the muscarinic agonist carbachol and the anesthetics ketamine and thiopental were compared under conditions of high (10(-6)M isoproterenol bath concentration) or low (10(-6)M propranolol) beta-adrenergic tone." | ( In vitro myocardial depression by ketamine or thiopental is dependent on the underlying beta-adrenergic tone. Mathew, BP; Thurston, TA, 1996) | 0.47 |
"3-1 mg/ml) also antagonized the dose-response curve of contractions induced by acetylcholine (0." | ( Mechanisms involved in the spasmolytic effect of extracts from Sabal serrulata fruit on smooth muscle. Cantabrana, B; García de Boto, MJ; Gutierrez, M; Hidalgo, A, 1996) | 0.29 |
"0 mg/kg) were administered to complete a dose-response curve." | ( Cardiovascular effects of the macrolide antibiotic tilmicosin, administered alone and in combination with propranolol or dobutamine, in conscious unrestrained dogs. Main, BW; Means, JR; Rinkema, LE; Sarazan, RD; Smith, WC, 1996) | 0.51 |
" Salmeterol and salbutamol produced the same maximal increase in sGAW and had the same area under the dose-response curves." | ( Airway effects of salmeterol in healthy individuals. Bake, B; Bergendal, A; Johansson, A; Löfdahl, CG; Lötvall, J; Skoogh, BE, 1995) | 0.29 |
" The dose-response curves of adenosine on AV nodal conduction were almost identical in the control state and after verapamil, propranolol, or procainamide injection." | ( Effects of verapamil, propranolol, and procainamide on adenosine-induced negative dromotropism in human beings. Lai, WT; Lee, CS; Sheu, SH; Wu, JC; Wu, SN, 1996) | 0.81 |
"3 mM), at approximately twice the equimolar dosage of cocaine, produced apneustic breathing that was indistinguishable from that produced by cocaine." | ( Cardiorespiratory effects of cocaine and procaine at the ventral brainstem. Dehkordi, O; Dennis, GC; Millis, RM; Trouth, CO, 1996) | 0.29 |
" Racial differences in propranolol enantiomer kinetics following oral dosing were previously documented in our laboratory." | ( Racial differences in propranolol enantiomer kinetics following simultaneous i.v. and oral administration. Burlew, BS; Johnson, JA; Lima, JJ; Massie, JD; Sowinski, KM, 1996) | 0.92 |
" S(-)-propranolol 10(-5) M also inhibited vasoconstriction induced by methoxamine, shifting the dose-response curves to the right, but did not affect pressor responses to arginine-vasopressin." | ( Propranolol stereoselectively inhibits alpha-adrenoceptor-mediated vasoconstriction in mesenteric arterial beds of rats. Heinemann, A; Stauber, RE, 1996) | 2.22 |
" The potentiation of the toxic effect of the enantiomers observed after dosing the racemate instead of the pure enantiomers could not be explained by a stereoselective difference in plasma propranolol concentration." | ( Toxic doses of rac-, (-)-(S)- and (+)-(R)-propranolol in rats and rabbits. Bode, W; de Wildt, DJ; Meulenbelt, J; Toet, AE; van de Kuil, A; Vleeming, W; Wemer, J, 1996) | 0.75 |
" A single-dose three-way crossover bioavailability study of two extended-release experimental formulations (80 mg), Inderal LA (80 mg) and an Inderal immediate-release dosage form (2 x 40 mg) was also conducted and a comparative analysis of pharmacokinetic parameters and the in-vitro release profiles was performed to assess in-vitro/in-vivo correlation." | ( Bioavailability and in-vitro/in-vivo correlation for propranolol hydrochloride extended-release bead products prepared using aqueous polymeric dispersions. Jambhekar, SS; Rekhi, GS, 1996) | 0.54 |
" Dose-response curves for dopexamine, isoprenaline, noradrenaline and impromidine on heart rate, blood pressure and myocardial contractility (dP/dt:integrated isometric tension) were obtained in untreated dogs and compared to those measured in dogs which had been pretreated with propranolol (8 mg kg-1 day-1), atenolol (6 mg kg-1 day-1), isoprenaline (0." | ( Changes in cardiovascular responsiveness to dopexamine and beta 1- and beta 2-adrenoceptor function after the chronic treatment of beta-adrenoceptor antagonists and agonists in anaesthetized dogs. Chang, DH; Einstein, R, 1996) | 0.47 |
" Furthermore, isoproterenol dose-response relationships of these contractile parameters were blunted in the hypothyroid animals and augmented in the hyperthyroid animals compared with euthyroid control animals." | ( Measurement of intraventricular pressure and cardiac performance in the intact closed-chest anesthetized mouse. Lorenz, JN; Robbins, J, 1997) | 0.3 |
" Mean arrival time after oral dosing was significantly lengthened by hyperthyroidism (100 +/- 38 minutes vs 157 +/- 71 minutes)." | ( Pharmacokinetics of propranolol in healthy cats during euthyroid and hyperthyroid states. Calvert, C; Ferguson, D; Jacobs, G; Sams, R; Whittem, T, 1997) | 0.62 |
" Response to beta-adrenergic stimulation showed a classic sigmoidal dose-response curve; however, there was very little tachycardiac response to vagal blockade, indicating low resting vagal tone." | ( Cardiovascular indexes in the mouse at rest and with exercise: new tools to study models of cardiac disease. Barsh, GS; Bernstein, D; Desai, KH; Kobilka, BK; Sato, R; Schauble, E, 1997) | 0.3 |
" Rings were exposed to increasing concentrations of triiodothyronine (4 x 10(-12) to 1 x 10(-4) mol/L) to obtain dose-response curves." | ( Direct effects of triiodothyronine on human internal mammary artery and saphenous veins. Carlsson, C; Chen, D; Cooper, SC; Eldridge, CJ; Hellmann, SK; Jeevanandam, V; Krasner, LJ; McClurken, JB; Wendling, WW, 1997) | 0.3 |
" Though glucagon was initiated more often than any other intervention in fatal intoxications (83%), optimal dosing and maintenance infusions appear to have been underutilized." | ( Characterization of fatal beta blocker ingestion: a review of the American Association of Poison Control Centers data from 1985 to 1995. Clancy, C; Howell, JM; Litovitz, TL; Love, JN, 1997) | 0.3 |
"The effect of rac-sotalol on QT interval duration was studied in 10 patients after single oral administration (160 mg) and after 6-day multiple oral dosing (80 mg two or three times daily)." | ( Tolerance to the repolarization effects of rac-sotalol during long-term treatment. Al Bunni, M; Ferrari, M; Gusella, M; Magnolfi, G; Maiolino, P; Padrini, R; Piovan, D; Zordan, R, 1997) | 0.3 |
"5%) in matched normal subjects, but had no effect on TLCO and KCO in EH patients prior to TS; and (2) subsequent inhalation of the beta 2-adrenoreceptor agonist salbutamol in a dosage suspected to cause alveolar beta-receptor stimulation had no effect on TLCO and KCO, neither in the normal subjects, nor in EH patients (before and after TS)." | ( Partial pulmonary sympathetic denervation by thoracoscopic D2-D3 sympathicolysis for essential hyperhidrosis: effect on the pulmonary diffusion capacity. Noppen, MM; Vincken, WG, 1997) | 0.3 |
" It is therefore unlikely that the pharmacokinetic changes will lead to clinically important changes in pharmacological effects and dosage adjustment of zolmitriptan is not required in patients taking propranolol for migraine prophylaxis." | ( The interaction between propranolol and the novel antimigraine agent zolmitriptan (311C90). Dixon, R; Gillotin, CG; Layton, G; Peck, RW; Posner, J; Seaber, EJ; Weatherley, BC, 1997) | 0.79 |
" Dose-response effects on HR with celiprolol were evident in the presence of atenolol, unlike those with propranolol that abolished the HR increase between celiprolol, 200 mg and 800 mg." | ( Effects of beta-adrenoceptor agonists and antagonists on heart-rate variability in normal subjects assessed using summary statistics and nonlinear procedures. Guy, S; Riddell, JG; Silke, B, 1997) | 0.51 |
" Measures of dosing interval--used-on-schedule rate and therapeutic coverage--averaged between 44% and 71%." | ( Noncompliance may render migraine prophylaxis useless, but once-daily regimens are better. Mulleners, WM; Steiner, TJ; Whitmarsh, TE, 1998) | 0.3 |
" The results obtained show that Adalat in dosage 60 mg daily during 7 days is most effective in cases with concomitant border-line hypertension." | ( [Premedication with different groups of hypotensive drugs in preparation of patients with concomitant arterial hypertension to planned surgical treatment]. Eliutin, DV; Mil'tsyn, AS; Sadchikov, DV, 1998) | 0.3 |
"The biphasic nature of the lipolytic dose-response curve of epinephrine in fat cells from "young" rats (40-45 days) was confirmed." | ( Hormone-stimulated lipolysis in isolated fat cells from "young" and "old" rats. Allen, DO; Miller, EA, 1973) | 0.25 |
" Male Sprague-Dawley rats were pretreated with either subcutaneous nicotine or equivolume saline and a dose-response curve for dopaminergic pulmonary vasodilation was constructed ex vivo in isolated, salt-perfused rat lungs preconstricted with the synthetic thromboxane analogue U-46619." | ( Acute nicotine pretreatment augments dopaminergic pulmonary vasodilation. Russ, RD, 1998) | 0.3 |
" Using a catheter placed through the auxiliary port of a flexible fiberoptic endoscope, liquid dosage formulations were consistently delivered to the canine stomach, duodenum, ileum, and colon." | ( Site-specific drug delivery in the dog using flexible fiberoptic endoscopy. Enever, RP; Heit, MC; Smith, DF, 1998) | 0.3 |
" When amiodarone was ineffective, propranolol was added at a dosage of 2-4 mg/kg/day." | ( Amiodarone used alone or in combination with propranolol: a very effective therapy for tachyarrhythmias in infants and children. Di Liso, G; Drago, F; Guccione, P; Mafrici, A; Mazza, A; Ragonese, P, ) | 0.67 |
" In general, it was considered that the duration and the extent of these reactions were dependent on the PRL dosage and application time." | ( Relationship between the skin permeation movement of propranolol and skin inflammatory reactions. Gemba, M; Hosaka, K; Kamiyama, M; Kobayashi, I; Konno, C; Maruo, H; Saeki, Y, 1998) | 0.55 |
" Pretreatment with atropine shifted the dose-response curve of acetylcholine to the right and the maximal response was reduced by 9%, 49% and 77% respectively with pretreatment with atropine 10(-8), 10(-7) and 10(-6) mole/kg." | ( Effects of atropine, isoproterenol and propranolol on the rabbit bladder contraction induced by intra-arterial administration of acetylcholine and ATP. Horan, P; Levin, RM; Liu, SP, 1998) | 0.57 |
" Dose-response curves for NE-induced perfusion pressure, VO2, and lactate production in SHR were shifted to the left compared with WKY." | ( Altered muscle metabolism associated with vasoconstriction in spontaneously hypertensive rats. Colquhoun, EQ; Ye, JM, 1998) | 0.3 |
" Therefore, retaining propranolol at the dosed site in the rectum by the addition of appropriate mucoadhesives to the formulation of liquid suppositories appears to be a very important factor in avoiding first-pass hepatic elimination and thereby increasing the bioavailability of the drug." | ( Increased bioavailability of propranolol in rats by retaining thermally gelling liquid suppositories in the rectum. Chung, SJ; Kim, CK; Lee, MH; Ryu, JM, 1999) | 0.91 |
" Adherence and adequacy of dosage (>1 mg/kg per day, more than twice daily dose frequency) are important determinants of efficacy." | ( Propranolol in prevention of portal hypertensive hemorrhage in children: a pilot study. Grand, RJ; Langhans, N; Shashidhar, H, 1999) | 1.75 |
" In acutely dosed rats, where protein synthesis is reduced, protein carbonyl concentrations (an index of oxidative damage to muscle) also decline slightly or are unaltered, contrary to the expected increase." | ( Oxidants, antioxidants and alcohol: implications for skeletal and cardiac muscle. Falkous, G; Mantle, D; Patel, VB; Preedy, VR; Reilly, ME; Richardson, PJ, 1999) | 0.3 |
"6 microgram/kg) and aminophylline (25 mg/kg), which were determined by the dose-response curves for inhibition of histamine-induced bronchoconstriction, were intravenously administered 5 minutes before the propranolol inhalation." | ( Difference in bronchoprotective effects of bronchodilators on postallergic propranolol-induced bronchoconstriction. Fujimura, M; Ishiura, Y; Matsuda, T; Mizuhashi, K; Myou, S, 1999) | 0.72 |
" At the lowest dose studied (20 microgram/kg iv), the inhibitory effects of candesartan were competitive, whereas at the highest dose (100 microgram/kg iv) the dose-response curve for angiotensin II was shifted to the right in a nonparallel manner with inhibitory effects that could not be surmounted." | ( Role of AT(1) receptors and autonomic nervous system in mediating acute pressor responses to ANG II in anesthetized mice. Bivalacqua, TJ; Champion, HC; Dalal, A; Kadowitz, PJ, 1999) | 0.3 |
" These data provide a potential mechanism to explain the paradoxical increase in asthma morbidity and mortality associated with the chronic use of scheduled dosing of short-acting beta-adrenergic agonists." | ( Beta-adrenergic modulation of human type-1/type-2 cytokine balance. Agarwal, SK; Marshall, GD, 2000) | 0.31 |
" This produced a dosage form with a high intraparticulate porosity in the dry state." | ( Tablet and capsule hydrophilic matrices based on heterodisperse polysaccharides having porosity-independent in vitro release profiles. Kelly, ML; Staniforth, JN; Tobyn, MJ, 2000) | 0.31 |
"An original dosage form for oral delivery based on the encapsulation of both, lipophilic and hydrophilic drugs, in poly(epsilon-caprolactone) (PCL) microparticles prepared either by the oil-in-water (o/w) or the water-in-oil-in-water (w/o/w) solvent evaporation method was developed." | ( The preparation and evaluation of poly(epsilon-caprolactone) microparticles containing both a lipophilic and a hydrophilic drug. Astier, A; Bodmeier, R; Hoffman, M; Hombreiro Pérez, M; Lamprecht, A; Maincent, P; Ubrich, N; Zinutti, C, 2000) | 0.31 |
" It is concluded that polymers of this type may have great potential in controlling, via means of formulation, the release of drug eutomer whilst enhancing retention of distomer in the dosage form." | ( Evaluation of matrices containing molecularly imprinted polymers in the enantioselective-controlled delivery of beta-blockers. Martin, GP; Srichana, T; Suedee, R, 2000) | 0.31 |
"A significant reduction in heart rate, in QT dispersion and in QTc dispersion was observed, as was also an increase in the PR interval and in the QT interval, after the use of propranolol in an average dosage of 100 mg/day." | ( Effects of propranolol on the QT dispersion in congestive heart failure. Cramer, H; de Deus, FC; dos Santos, PA; dos Santos, VB; Guedes, CR; Maia, ER; Mesquita, ET; Romeo, LJ; Subieta, CG; Villacorta, H, 1999) | 0.89 |
"5, 15, and 40 mg nadolol or propranolol (both beta1- and beta2-adrenergic receptor antagonists) at random, after which isoproterenol (beta1-, beta2-, and beta3-adrenergic receptor agonist) was infused in an individually determined dosage (range, 19 to 35 ng/kg x min) that increased energy expenditure by 25% without pretreatment." | ( In vivo beta3-adrenergic stimulation of human thermogenesis and lipid use. Blaak, EE; Saris, WH; Schiffelers, SL; van Baak, MA, 2000) | 0.6 |
" These data demonstrate that chronic dosing with propranolol can impair retention of spatial learning, which cannot be attributed to reduced arousal or motor function." | ( Chronic propranolol induces deficits in retention but not acquisition performance in the water maze in mice. Czech, DA; Laubmeier, KK; Nielson, KA, 2000) | 1 |
" The results showed that acute alcohol dosage reduced the fractional rates of cardiac protein synthesis (k(S), %/day)." | ( Inability of propranolol to prevent alcohol-induced reductions in cardiac protein synthesis in vivo. Patel, VB; Preedy, VR; Richardson, PJ, 2000) | 0.68 |
" The dose-response curve for L-750355-induced glycerolemia lies to the left of that for tachycardia." | ( L-750355, a human beta3-adrenoceptor agonist; in vitro pharmacology and profile of activity in vivo in the rhesus monkey. Bach, T; Candelore, MR; Cascieri, MA; Cioffe, C; Deng, L; Fisher, MH; Forrest, MJ; Hegarty-Friscino, B; Hom, G; MacIntyre, E; Marko, O; Ok, HO; Strader, C; Szumiloski, J; Tota, L; Vicario, P; Weber, AE; Wyvratt, M, 2000) | 0.31 |
" Therefore, it is quite possible that both drugs produce adverse immunological effects in vivo in cases of high dosage or obstruction of elimination." | ( [Effect of migraine medications on monocyte chemotaxis] . Krumholz, W; Menges, T; Ogal, H; Szalay, G, 2000) | 0.31 |
" Dosing of propranolol in the evening may be important for its role in preventing variceal bleeding." | ( Daily variation of azygos and portal blood flow and the effect of propranolol administration once an evening in cirrhotics. Ishii, K; Sasao, K; Sugano, S; Tanikawa, K; Watanabe, M; Yamamoto, K, 2001) | 0.94 |
" The dose-response relationships of the beta(3)-adrenoceptor agonists were challenged with the selective beta(3)-adrenoceptor antagonist 3-(2-ethylphenoxy)-1-[(1S)-1,2,3,4-tetrahydronapth-1-ylamino]-2S-2-propanol oxalate (SR59230A) or the beta(2)-adrenoceptor antagonist (-)propranolol." | ( Enhancement of memory consolidation in chicks by beta(3)-adrenoceptor agonists. Gibbs, ME; Summers, RJ, 2001) | 0.49 |
" Dose-response curves conducted at 30-min incubation time showed that chlorpromazine potently inhibited labelling of diacylglycerol and diacyglycerol-derived lipids (triacyglycerol and phosphatidylcholine) by the 3H-labelled precursors." | ( Chlorpromazine and human platelet glycerolipid metabolism: precursor specificity and significance of drug-platelet interaction time. Daasvatn, KO; Holmsen, H, 1999) | 0.3 |
" This study used a within-subject, dose-response design to determine whether prazosin (PRAZ), an alpha1-NA antagonist, or propranolol (PROP), a beta-NA antagonist, would continue to reinstate hemiplegia over time after recovery from weight-drop traumatic brain injury (TBI)." | ( Enduring vulnerability to transient reinstatement of hemiplegia by prazosin after traumatic brain injury. Feeney, DM; Stibick, DL, 2001) | 0.52 |
"To obtain a sustained-release dosage form with a lack of gastric unwanted effects, wax microspheres containing propranolol (I) were prepared by a congealable dispersion microencapsulation technique." | ( Development and evaluation of sustained-release propranolol wax microspheres. Keihanfar, M; Varshosaz, J, ) | 0.6 |
" In the present study, the plasma concentration profiles of propranolol obtained in human subjects following oral dosing were analyzed using the newly derived models based on mass balance and compared with the conventional models." | ( Time-dependent oral absorption models. Amidon, GL; Higaki, K; Yamashita, S, 2001) | 0.55 |
" In contrast, the low (4 mg/kg) and intermediate (7 mg/kg) doses of propranolol significantly decreased spontaneous CeA activity, with the suppressant effect of propranolol on CeA firing rates weakening as the dosage increased from 4 to 7 mg/kg." | ( Dose-sensitive excitation and inhibition of spontaneous amygdala activity by propranolol. Gibson, B; Levin, D; Naylor, JC; Schneider, AM; Simson, PE, ) | 0.6 |
", dosing rate or enantiomer-enantiomer interaction) or the patient (e." | ( Stereospecific pharmacokinetics and pharmacodynamics of beta-adrenergic blockers in humans. Brocks, DR; Mehvar, R, ) | 0.13 |
"Carbomers are carboxyvinylic derivatives that are widely used in the manufacture of hydrogel dosage forms." | ( Use of beta-cyclodextrins to prevent modifications of the properties of carbopol hydrogels due to carbopol-drug interactions. Blanco-Fuente, H; Blanco-Méndez, J; Esteban-Fernández, B; Otero-Espinar, FJ, 2002) | 0.31 |
" In contrast, the dose-response curve for substance P recorded 1 h after antigen challenge was not modified by pretreatment with silymarin." | ( Protective effect of silymarin in antigen challenge- and histamine-induced bronchoconstriction in in vivo guinea-pigs. Apostoliti, F; Breschi, MC; Martinotti, E; Nieri, P, 2002) | 0.31 |
"001), whereas glycopyrrolate increased peak HR to sea level values, 184 +/- 3 beats/min, confirming adequate dosing with each drug." | ( Role of the autonomic nervous system in the reduced maximal cardiac output at altitude. Bogaard, HJ; Hopkins, SR; Niizeki, K; Wagner, PD; Yamaya, Y; Ziegler, MG, 2002) | 0.31 |
" The proposed methods have been successfully applied to the determinations of PPH and PX in various dosage forms." | ( Indirect spectrophotometric determination of propranolol hydrochloride and piroxicam in pure and pharmaceutical formulations. Gowda, BG; Melwanki, MB; Seetharamappa, J, 2002) | 0.57 |
" Although it remains possible that with a different dosage or timing protocol a post-treatment effect of noradrenaline in humans can be found, this experiment could not find support for it." | ( The effect of beta-adrenergic blockade after encoding on memory of an emotional event. Everaerd, W; Gooren, LJ; van Stegeren, AH, 2002) | 0.31 |
" The method was applied for the determination of the drug in the tablet dosage form." | ( Polarographic determination of propranolol in pharmaceutical formulation. Abou-Sekkina, MM; El-Ries, MA; Wassel, AA, 2002) | 0.6 |
"H/L ratio may help in the selection of drug dosage (especially blood flow dependent drug) in pre-clinical studies for chronic liver disease during the drug development process." | ( [Relationship of propranolol pharmacokinetic parameters with portosystemic shunt in CCl4-induced cirrhotic rats]. Choi, HS; Choi, YY; Hahm, JS; Kang, JS; Kim, DU; Kim, JB; Kim, JM; Koh, DH; Lee, MH; Lee, SH; Park, GT; Yun, YS, 2002) | 0.65 |
"For clinical treatment, a smaller dosage of propranolol is often used among Chinese people." | ( Dose-response relationships of propranolol in Chinese subjects with different CYP2D6 genotypes. Huang, CW; Huang, JD; Lai, ML; Lee, HL; Lin, MS, 2003) | 0.87 |
"Despite therebeing higher S-propranolol plasma concentration in CYP2D6*10 subjects than in CYP2D6*1 subjects at 10- and 20-mg dosage, the dose-response relationship was not significantly different in these subjects." | ( Dose-response relationships of propranolol in Chinese subjects with different CYP2D6 genotypes. Huang, CW; Huang, JD; Lai, ML; Lee, HL; Lin, MS, 2003) | 0.9 |
" All three beta blockers were equally protective but the intermediate dosage of landiolol preserved LVP during the pre-ischemic period." | ( Landiolol, esmolol and propranolol protect from ischemia/reperfusion injury in isolated guinea pig hearts. Fujita, S; Kanaya, N; Kurosawa, S; Nakayama, M; Namiki, A; Niiyama, Y, 2003) | 0.63 |
" Current formulations and dosing of antihypertensive drugs do not provide maximum coverage during this vulnerable period." | ( Pharmacokinetics of propranolol after single and multiple dosing with sustained release propranolol or propranolol CR (innopran XL) , a new chronotherapeutic formulation. Frishman, WH; Manowitz, N; Sica, D, ) | 0.45 |
" A decline in mean arterial pressure was observed in both groups with increasing dosage of phentolamine." | ( Preserved alpha-adrenergic tone in the leg vascular bed of spinal cord-injured individuals. Hopman, MT; Kooijman, M; Rongen, GA; Smits, P, 2003) | 0.32 |
"Intravenous dosing was initially done via jugular cannula." | ( Iontophoretic in vivo transdermal delivery of beta-blockers in hairless rats and reduced skin irritation by liposomal formulation. Banga, AK; Betageri, GV; Chaturvedula, A; Conjeevaram, R; Sunkara, G, 2003) | 0.32 |
" Images showed that the seal between the shell and the tablet plug is a key route of water penetration in these dosage forms." | ( Investigating the coating-dependent release mechanism of a pulsatile capsule using NMR microscopy. Bowtell, RW; Köckenberger, W; MacRae, RJ; Melia, CD; Ross, AC; Stevens, HN; Sutch, JC, 2003) | 0.32 |
"A simple spectrophotometric method has been developed for the determination of propranolol hydrochloride in pure as well as in dosage forms." | ( Spectrophotometric determination of propranolol in formulations via oxidative coupling with 3-methylbenzothiazoline-2-one hydrazone. Belal, FF; El-Ashry, SM; El-Emam, AA; El-Sherbiny, DT; Hansen, SH; Moustafa, MA, 2003) | 0.82 |
" The dosage of beta-blockers should be modified in patients with an abnormal lipid profile in serum." | ( [Pharmacokinetic comparison of propranolol and atenolol in people with primary hypertension]. Telatyńska-Smieszek, B, 2002) | 0.6 |
" This system is quite useful to predict the oral absorption of poorly water-soluble drugs after administration as solid dosage forms." | ( In vitro system to evaluate oral absorption of poorly water-soluble drugs: simultaneous analysis on dissolution and permeation of drugs. Kataoka, M; Masaoka, Y; Sakane, T; Sezaki, H; Yamashita, S; Yamazaki, Y, 2003) | 0.32 |
" The analysis was then adjusted for mouse weight and intraperitoneal (-)-propranolol dosage using a logistic regression (LR) model." | ( Inhibition of (-)-propranolol hydrochloride by its enantiomer in white mice. Kuzeff, RM; Mecheva, RP; Topashka-Ancheva, MN, 2003) | 0.88 |
"In this article, we document how an interdisciplinary committee of health professionals led to an approximate 50% reduction in the incidence of postoperative atrial fibrillation (AF) following a cardiac surgery procedure by using preoperative loading and dosing of PO amiodarone and beta blockade." | ( National databases and clinical practice specialist: decreasing postoperative atrial fibrillation following cardiac surgery. Barnett, SD; Burton, NA; Halpin, LS, ) | 0.13 |
" To generate a ketoconazole dosing regimen, the pharmacokinetics of ketoconazole were first determined in the monkey and were found to be consistent with that previously described in the rat, dog, and human." | ( Development of an in vivo preclinical screen model to estimate absorption and first-pass hepatic extraction of xenobiotics. II. Use of ketoconazole to identify P-glycoprotein/CYP3A-limited bioavailability in the monkey. Azzarano, LM; Kehler, JR; McSurdy-Freed, JE; Morgan, JA; Proksch, JW; Smith, BR; Stelman, GJ; Ward, KW; Zeigler, KS, 2004) | 0.32 |
" Propranolol hydrochloride (propranolol HCl) is subjected to first-pass effect, therefore formulation of buccal-adhesive dosage form can circumvent this effect." | ( Development and evaluation of buccoadhesive propranolol hydrochloride tablet formulations: effect of fillers. Adrangui, M; Akbari, J; Farid, D; Nokhodchi, A; Saeedi, M; Siahi-Shadbad, MR, 2004) | 1.49 |
" The analysis was then adjusted for mouse weight and intraperitoneal (-)-propranolol dosage using a logistic regression (LR) model." | ( Inhibition of (-)-propranolol hydrochloride by its enantiomer in white mice--a placebo-controlled randomized study. Kuzeff, RM; Mecheva, RP; Topashka-Ancheva, MN, 2004) | 0.89 |
" In the light of the results obtained, the following conclusions were drawn: 1) hyperlipidemia affects pharmacodynamic properties of lipophilic propranolol and hydrophilic atenolol, 2) a modification of the drug dosage in hyperlipidemia is warranted." | ( [Effect of hyperlipidemia on pharmacodynamics of propranolol and atenolol]. Droździk, M; Gawrońska-Szklarz, B; Sterna, R; Sulzyc-Bielicka, V; Telatyńska-Smieszek, B; Wójcicki, J, 2004) | 0.78 |
"This study evaluated the antihypertensive efficacy and tolerability of a chronotherapeutic formulation of propranolol designed for nighttime dosing (propranolol controlled release [CR])." | ( The antihypertensive efficacy and safety of a chronotherapeutic formulation of propranolol in patients with hypertension. Manowitz, N; Neutel, JM; Sica, DA; Weber, MA, 2004) | 0.76 |
"To assess the strategy of titration for prescribing an efficient dosage of propranolol to reduce myocardial ischemia in the elderly." | ( Strategy for identifying an efficient dosage of beta-blocker for elderly patients with myocardial ischemia and preserved left ventricular function. Abe, R; Dal Bó, C; de Oliveira, MA; Gebara, O; Giorgi, MC; Meneghetti, JC; Nussbacher, A; Pierri, H; Serro-Azul, JB; Wajngarten, M, 2004) | 0.55 |
" Titration was performed to identify the dosage of propranolol that would cause a 15% reduction in heart rate at the end of a 50 W load (corresponding to normal daily activities in the elderly) in weekly exercise tests." | ( Strategy for identifying an efficient dosage of beta-blocker for elderly patients with myocardial ischemia and preserved left ventricular function. Abe, R; Dal Bó, C; de Oliveira, MA; Gebara, O; Giorgi, MC; Meneghetti, JC; Nussbacher, A; Pierri, H; Serro-Azul, JB; Wajngarten, M, 2004) | 0.58 |
" Dose-response curves were established for the noradrenaline-induced (10(-12) to 10(-7) mol/kg) increase of diastolic blood pressure in pithed rats treated with tubocurarine, propranolol, and atropine." | ( Reduction of vascular noradrenaline sensitivity by AT1 antagonists depends on functional sympathetic innervation. Dendorfer, A; Dominiak, P; Raasch, W; Ziegler, A, 2004) | 0.52 |
"The aim of this study was to investigate the importance of the type of plasticizer in polymer blends used for the coating of solid dosage forms, comparing a lipophilic and a hydrophilic plasticizer (dibutyl sebacate (DBS) and triethyl citrate (TEC))." | ( Polymer blends used for the aqueous coating of solid dosage forms: importance of the type of plasticizer. Bodmeier, R; Lecomte, F; MacRae, RJ; Siepmann, J; Walther, M, 2004) | 0.32 |
" Following a propranolol or placebo dose titration period of up to 9 days (per a dosing algorithm), subjects were maintained on maximum achieved dose for 6 weeks." | ( Propranolol for disruptive behaviors in nursing home residents with probable or possible Alzheimer disease: a placebo-controlled study. Bonner, LT; Pascualy, M; Peskind, ER; Raskind, MA; Riekse, RG; Snowden, MB; Thomas, R; Tsuang, DW, ) | 1.94 |
" In Gr I, incremental dosage of propranolol (sufficient to reduce heart rate to 55 beats/min or 25% reduction from baseline) was administered and continued after obliteration of varices." | ( Endoscopic variceal ligation plus propranolol versus endoscopic variceal ligation alone in primary prophylaxis of variceal bleeding. Agarwal, SR; Sarin, SK; Sharma, BC; Tyagi, P; Wadhawan, M, 2005) | 0.89 |
"An original dosage form for nasal delivery based on the encapsulation of hydrophilic drug in chitosan-poly(methyl vinyl ether-co-maleic anhydride) (CH-PVM/MA) microparticles prepared by spray-drying technique was developed." | ( Chitosan and poly(methyl vinyl ether-co-maleic anhydride) microparticles as nasal sustained delivery systems. Bigucci, F; Cerchiara, T; Chidichimo, G; Luppi, B; Zecchi, V, 2005) | 0.33 |
" The relative bioavailability of two FDA approved (Orange Book AB rating) solid oral dosage forms of metoprolol and propranolol/hydrochlorothiazide (combination tablets) was evaluated in human volunteers under fed conditions using a two-way crossover design." | ( The effect of food on the relative bioavailability of rapidly dissolving immediate-release solid oral products containing highly soluble drugs. Asafu-Adjaye, E; Ciavarella, AB; Conner, DP; Faustino, PJ; Hussain, AS; Lesko, LJ; Mehta, MU; Parekh, A; Straughn, AB; Yang, Y; Yu, LX, ) | 0.34 |
" The secondary outcome measures were the duration of labour, the required dosage of oxytocin, CTG readings, neonatal outcome and maternal and cord plasma levels of beta-adrenoceptor-binding component of propranolol." | ( A double blind, randomized trial on augmentation of labour with a combination of intravenous propranolol and oxytocin versus oxytocin only. Huhtala, H; Kaila, T; Lavapuro, M; Palomäki, O; Tammela, O; Tuimala, R; Uotila, J, 2006) | 0.74 |
" No differences in the required oxytocin dosage or CTG pathology were found between the groups." | ( A double blind, randomized trial on augmentation of labour with a combination of intravenous propranolol and oxytocin versus oxytocin only. Huhtala, H; Kaila, T; Lavapuro, M; Palomäki, O; Tammela, O; Tuimala, R; Uotila, J, 2006) | 0.55 |
" Using propranolol as a model compound the effect of formulation and dosing variables was explored as a means to characterize the limiting parameters of this model." | ( A rabbit model for sublingual drug delivery: comparison with human pharmacokinetic studies of propranolol, verapamil and captopril. Dali, MM; Heran, CL; Mathias, NR; Moench, PA; Smith, RL; Stetsko, PI, 2006) | 1.01 |
" Serial bleeding of mice is advantageous for the reduction of animal usage, dosing errors, and animal-to-animal variation." | ( Supercritical fluid chromatography-tandem mass spectrometry for the enantioselective determination of propranolol and pindolol in mouse blood by serial sampling. Chen, J; Cook, J; Hsieh, Y; Korfmacher, WA; Morrison, R, 2006) | 0.55 |
" In the propranolol group, the mean daily dosage of the drug was 68." | ( Endoscopic variceal ligation versus propranolol in prophylaxis of first variceal bleeding in patients with cirrhosis. Chen, CB; Lai, YL; Lay, CS; Lee, FY; Peng, CY; Tsai, YT; Yu, CJ, 2006) | 1.04 |
"6) suggested that the dissolution profile of the present two sustained-release oral dosage forms are similar." | ( Development and optimization of a novel sustained-release dextran tablet formulation for propranolol hydrochloride. Bataille, B; Colarte, AI; Gil, EC; Heinämäki, J; Pedraz, JL; Rodríguez, F, 2006) | 0.56 |
" Stability of optimized patches was performed in natural human saliva showed that both drug and dosage forms were stable in human saliva." | ( Physicochemical characterization and evaluation of buccal adhesive patches containing propranolol hydrochloride. Patel, JK; Patel, MM; Patel, VM; Prajapati, BG, 2006) | 0.56 |
", group III was treated with CCl4 for 6 weeks and received propranolol x2 at the same dosage as group I, while group VI was treated with CCl4 and the same drug dosage as group II." | ( H3 Propranolol serum levels following lidocaine administration in rats with CCL4 induced liver damage. Anagnostopoulou, S; Kotsiou, A; Tesseromatis, C; Tsamouri, M; Tzivras, M; Vairactaris, E, ) | 1 |
" The results obtained in this study demonstrate, that EPR is a powerful method to monitor the first steps of diffusion processes and the physicochemical state of coated dosage forms." | ( Mechanistic analysis of drug release from tablets with membrane controlled drug delivery. Mäder, K; Metz, H; Strübing, S, 2007) | 0.34 |
"The aim of our study was to develop an apparatus assessing in vitro permeation through Caco-2 monolayers of oral solid dosage forms as a possible tool to forecast in vivo performance." | ( Permeability assessment for solid oral drug formulations based on Caco-2 monolayer in combination with a flow through dissolution cell. Balbach, S; Eichinger, T; Lehr, CM; Motz, SA; Schaefer, UF, 2007) | 0.34 |
"The ILSI/HESI telemetry studies were conducted as a double Latin square design where eight dogs each received a vehicle control and three dose levels of a compound on four separate dosing days." | ( ILSI-HESI cardiovascular safety subcommittee dataset: an analysis of the statistical properties of QT interval and rate-corrected QT interval (QTc). Bass, AS; Chiang, AY; Cooper, MM; Engwall, MJ; Menton, RG; Thomas, K, ) | 0.13 |
" However, PB-93 was rapidly cleared, and dosing every 12 h failed to cure the rats." | ( Efficacy, pharmacokinetics, and metabolism of tetrahydroquinoline inhibitors of Plasmodium falciparum protein farnesyltransferase. Ankala, S; Barrett, LK; Bauer, KD; Bendale, P; Buckner, FS; Chakrabarti, D; Floyd, D; Gelb, MH; Hamilton, AD; Hornéy, C; Hucke, O; Lombardo, LJ; Nallan, L; Rivas, KL; Smart, BP; Strickland, C; Van Voorhis, WC; Verlinde, CL; Williams, DK; Yokoyama, K, 2007) | 0.34 |
" We randomized 54 healthy subjects double-blind to 5-day treatment with a single daily oral dosage of either 100 mg aspirin plus 80 mg propranolol combined, 100 mg of aspirin, 80 mg of propranolol, or placebo medication." | ( Effects of aspirin and propranolol on the acute psychological stress response in factor VIII coagulant activity: a randomized, double-blind, placebo-controlled experimental study. Cung, T; Fischer, JE; Haeberli, A; Helfricht, S; Kudielka, BM; Metzenthin, P; Preckel, D; von Känel, R, 2008) | 0.86 |
" Repetitive once daily oral dosing (0." | ( Backbone cyclic peptidomimetic melanocortin-4 receptor agonist as a novel orally administrated drug lead for treating obesity. Faier, A; Gabinet, Y; Gilon, C; Halbfinger, E; Haskell-Luevano, C; Hess, S; Hoffman, A; Lapidot, T; Linde, Y; Ovadia, O; Portillo, FP; Safrai, E; Shalev, DE; Swed, A; Winkler, I; Xiang, Z; Yarden, D, 2008) | 0.35 |
" Dose-response curves were constructed for NE with and without the addition of the alpha-adrenergic antagonist prazosin, EPI (after 20%-30% preconstruction with the thromboxane analog U46619) with and without the addition of the beta-adrenergic antagonist propranolol, and NE in the presence of 10(-8) M EPI." | ( The effect of maternal catecholamines on the caliber of gravid uterine microvessels. Segal, S; Wang, SY, 2008) | 0.53 |
" Additionally, they randomly received either placebo (N = 15) or irbesartan (step-up dosage titration up to 300 mg/d, N = 17)." | ( Irbesartan plus low-dose propranolol versus low-dose propranolol alone in cirrhosis: a placebo-controlled, double-blind study. Flacke, S; Ghauri, M; Heller, J; Herold, T; Sauerbruch, T; Schepke, M; Stoffel-Wagner, B; Wiest, R, 2008) | 0.65 |
"The release of propranolol hydrochloride from matrix tablets with hydroxy propyl methyl cellulose (HPMC K15M) or KollidonSR at different concentrations was investigated with a view to developing twice daily sustained release dosage form." | ( Comparative study of propranolol hydrochloride release from matrix tablets with KollidonSR or hydroxy propyl methyl cellulose. Biswal, S; Mahapatra, AK; Murthy, PN; Sahoo, J; Sahoo, SK, 2008) | 1.02 |
"Desorption electrospray ionization tandem mass spectrometry (DESI-MS/MS) and whole-body autoradiography (WBA) were used for chemical imaging of whole-body thin tissue sections of mice intravenously dosed with propranolol (7." | ( Comparison of drug distribution images from whole-body thin tissue sections obtained using desorption electrospray ionization tandem mass spectrometry and autoradiography. Covey, TR; Kertesz, V; Koeplinger, KA; Schneider, BB; Van Berkel, GJ; Vavrek, M, 2008) | 0.53 |
" Three dosage forms including commercial tablet, sustained-release tablet and the delayed-onset sustained-release tablet were administrated to six beagle dogs and the plasma levels of propranolol hydrochloride were measured with high-performance liquid chromatography." | ( Preparation and evaluation of a novel delayed-onset sustained-release system of propranolol hydrochloride. Chen, HZ; Fang, C; Feng, XM; Ren, Q; Rong, ZX; Shen, HF; Zhang, WZ, 2008) | 0.76 |
" The study indicates that locust bean gum and chitosan in a weight ratio of 2:3 (F1) not only releases the drug unidirectionally from the dosage form, but also gives buccal tablets which are sufficiently mucoadhesive for clinical applications." | ( In vitro and in vivo evaluation of locust bean gum and chitosan combination as a carrier for buccal drug delivery. Ramakrishnan, A; Vasanthakumar, S; Vijayaraghavan, C, 2008) | 0.35 |
" [14C]-propranolol, dosed intraperitoneally to rat at 25 mg kg(-1) and 200 microCi kg(-1) was used as a model compound for this evaluation." | ( Evaluation of the use of UPLC-TOFMS with simultaneous [14C]-radioflow detection for drug metabolite profiling: application to propranolol metabolites in rat urine. Athersuch, TJ; Clarkson-Jones, JA; Kenyon, AS; Sison, RL; Wilson, ID, 2008) | 1.01 |
" After oral dosing of moxifloxacin, a substantial, dose-dependent increase in the QT-interval duration could be shown, as anticipated for this agent." | ( Validation of the normal, freely moving Göttingen minipig for pharmacological safety testing. Guth, B; Klumpp, A; Markert, M; Mayer, K; Schuler-Metz, A; Schumacher, K; Stubhan, M; Trautmann, T, ) | 0.13 |
" Lowering propranolol dosage or switching to atenolol was less efficient to reduce cortisol levels." | ( Adrenal Cushing's syndrome due to bilateral macronodular adrenal hyperplasia: prediction of the efficacy of beta-blockade therapy and interest of unilateral adrenalectomy. Chabre, O; Chaffanjon, P; Martinie, M; Mazzuco, TL; Sturm, N, 2009) | 0.76 |
" This finding suggests that the PPN-MAS complexes obtained in this study are strong candidates for use as drug carriers in oral modified-release dosage forms." | ( Propranolol-magnesium aluminum silicate complex dispersions and particles: characterization and factors influencing drug release. Pongjanyakul, T; Rojtanatanya, S, 2010) | 1.8 |
" Analysis of whole-body mouse thin tissue sections from animals dosed with propranolol, adhered to an adhesive tape substrate, provided semiquantitative information for propranolol and its hydroxyproranolol glucuronide metabolite within specific organs of the tissue." | ( Application of a liquid extraction based sealing surface sampling probe for mass spectrometric analysis of dried blood spots and mouse whole-body thin tissue sections. Kertesz, V; Van Berkel, GJ, 2009) | 0.58 |
"3 x 10(-3) mol/L) produced a significant rightward shift in the phenylephrine dose-response curve, but had no effects on the potassium chloride-induced contraction." | ( Relaxant effects of matrine on aortic smooth muscles of guinea pigs. Dai, GD; Fu, XY; Yan, L; Zheng, J; Zheng, P; Zhou, R; Zhou, X, 2009) | 0.35 |
" Further studies are needed to determine the long-term effectiveness, dosing strategies, and side effect profile of propranolol treatment for hemangiomas." | ( Initial experience using propranolol as the sole treatment for infantile airway hemangiomas. Hartnick, C; Maturo, S, 2010) | 0.87 |
"A 27-day-old male infant with diffuse hemangiomatosis of the skin and liver was treated with oral propranolol at a dosage of 2 mg/kg per day." | ( Severe hypoglycemia during successful treatment of diffuse hemangiomatosis with propranolol. Acquafredda, A; Bonifazi, E; Laforgia, N; Milano, A; Montagna, O, ) | 0.58 |
"The Biopharmaceutical Classification System (BCS) guidance issued by the FDA allows waivers for in vivo bioavailability and bioequivalence studies for immediate-release (IR) solid oral dosage forms only for BCS class I drugs." | ( The biowaiver extension for BCS class III drugs: the effect of dissolution rate on the bioequivalence of BCS class III immediate-release drugs predicted by computer simulation. Amidon, GL; Tsume, Y, 2010) | 0.36 |
" To illustrate the utility of coupling a separation with this direct liquid extraction based surface sampling approach, four different organs (brain, lung, kidney, and liver) from whole-body thin tissue sections of propranolol dosed and control mice were examined." | ( Liquid microjunction surface sampling coupled with high-pressure liquid chromatography-electrospray ionization-mass spectrometry for analysis of drugs and metabolites in whole-body thin tissue sections. Kertesz, V; Van Berkel, GJ, 2010) | 0.55 |
" The propranolol dosage was adjusted to 2 mg/kg/day and the sodium valproate dosage to 15 mg/kg/day, after the first follow-up visit." | ( A randomized trial of propranolol versus sodium valproate for the prophylaxis of migraine in pediatric patients. Bidabadi, E; Mashouf, M, 2010) | 1.19 |
" The dosage was slowly increased to 2 mg/kg daily over the course of 1-2 weeks." | ( Outpatient treatment of periocular infantile hemangiomas with oral propranolol. Eikenberry, J; Haggstrom, A; Haider, KM; Neely, DE; Plager, DA, 2010) | 0.6 |
" However, the mechanism by which it causes this dramatic effect is unknown, the dosage empirical and the optimal duration of treatment unexplored." | ( Low-dose propranolol for infantile haemangioma. Itinteang, T; Leadbitter, P; Tan, ST, 2011) | 0.79 |
" We aimed to evaluate the dosing and tolerance of BBs achievable in a specialized, nurse-run BB titration clinic with non-trial participants." | ( A specialized, nurse-run titration clinic: a feasible option for optimizing beta-blockade in non-clinical trial patients. Abraldes, JG; Berzigotti, A; Bosch, J; Garcia-Pagan, JC; Saez, R; Tandon, P, 2010) | 0.36 |
"Three new, simple, sensitive, rapid and economical spectrophotometric methods (A, B and C) have been developed for the determination of propranolol hydrochloride (PRO) in bulk drug and dosage forms." | ( A sensitive spectrophotometric method for the determination of propranolol HCl based on oxidation bromination reactions. El-Didamony, AM, 2010) | 0.8 |
" In these two patients, the propranolol dosage had been tailed down rapidly and the therapy was of a shorter duration than in those without recurrence." | ( Use of propranolol in infantile haemangioma among Chinese children. Chan, HB; Chik, KK; Luk, CK; Tan, HY, 2010) | 1.11 |
"Matrix type, monolithic, dosage forms suitable for controlled release that exhibit pH-dependent behavior are considerably less common than similarly behaving multiparticulated, enterically coated dosage forms, although simpler and less expensive to make." | ( Formulations of zero-order, pH-dependent, sustained release matrix systems by ionotropic gelation of alginate-containing mixtures. Drefko, W; Moroni, A; Thone, G, 2011) | 0.37 |
"Evaluate the properties of alginates and alginate-containing systems to produce pH-sensitive, monolithic, controlled release dosage forms that perform acceptably and determine their limits of application in regard with stability, pH and Ca(++) sensitivity, and appropriated rate of release." | ( Formulations of zero-order, pH-dependent, sustained release matrix systems by ionotropic gelation of alginate-containing mixtures. Drefko, W; Moroni, A; Thone, G, 2011) | 0.37 |
") with other gel-forming gums such as propylene glycol alginate (PGA), xanthan, or hydroxypropyl methylcellulose have been evaluated for applicability in the manufacture of controlled release dosage forms with three drugs of different solubility and ionic character." | ( Formulations of zero-order, pH-dependent, sustained release matrix systems by ionotropic gelation of alginate-containing mixtures. Drefko, W; Moroni, A; Thone, G, 2011) | 0.37 |
" with a number of other gums have been demonstrated suitable to manufacture pH-sensitive, matrix-type solid dosage forms with release-controlling properties for up to 12 hours." | ( Formulations of zero-order, pH-dependent, sustained release matrix systems by ionotropic gelation of alginate-containing mixtures. Drefko, W; Moroni, A; Thone, G, 2011) | 0.37 |
" The latter steadily gain in importance as parenteral controlled release dosage forms, especially for acid-labile drugs." | ( Drug release mechanisms of compressed lipid implants. Kreye, F; Siepmann, F; Siepmann, J, 2011) | 0.37 |
" Pharmacokinetic studies showed that 4k is orally bioavailable, with an elimination half-life of 178 min following oral dosing in mice." | ( A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. Aboagye, EO; Ali, S; Alikian, M; Barbazanges, M; Barrett, AG; Blum, A; Brackow, J; Coombes, RC; Freemont, PS; Fuchter, MJ; Hazel, P; Heathcote, DA; Jogalekar, AS; Kanneganti, SK; Kroll, SH; Liotta, DC; Pace, RD; Patel, H; Periyasamy, M; Scheiper, B; Siwicka, A; Snyder, JP, 2010) | 0.36 |
" Known adverse effects of propranolol treatment include transient bradycardia, hypotension, hypoglycemia, and bronchospasm (in patients with underlying spastic respiratory illnesses), which led to a general recommendation to gradually increase propranolol dosage and closely monitor patients' hemodynamics at the onset of therapy." | ( Hyperkalemia complicating propranolol treatment of an infantile hemangioma. Kietz, S; Lakomek, M; Lauerer, P; Pavlakovic, H; Zutt, M, 2010) | 0.96 |
" The patients received oral propranolol, with dosage varying among study centers." | ( Propranolol for the treatment of orbital infantile hemangiomas. Bersani, T; Fridman, G; Grieser, E; Hill, R; Khuddus, N; Slonim, C, ) | 1.87 |
" Further studies are needed to determine the long-term effectiveness, dosing strategies, and side-effect profile of propranolol for treatment of recurrent respiratory papillomatosis." | ( Initial experience using propranolol as an adjunctive treatment in children with aggressive recurrent respiratory papillomatosis. Hartnick, CJ; Kinane, TB; Maturo, S; Tse, SM, 2011) | 0.88 |
" Further evaluation of propranolol therapy efficacy at the current dosing and duration of treatment continues." | ( Initial experience with a multidisciplinary strategy for initiation of propranolol therapy for infantile hemangiomas. Boucek, RJ; Cushing, SL; Manning, SC; Perkins, JA; Sidbury, R, 2011) | 0.91 |
" Questions remain about optimal dosing and age at treatment cessation." | ( Propranolol as first-line treatment of head and neck hemangiomas. Ayari-Khalfallah, S; Froehlich, P; Fuchsmann, C; Giguere, C; Guibaud, L; McCone, C; Powell, J; Quintal, MC, 2011) | 1.81 |
" The heart rate difference was analyzed by the logistic linear regression model with variables that included gender, age, body height, body weight, systolic blood pressure (SBP), diastolic blood pressure (DBP) and the dosage of propranolol." | ( Effects of propranolol on the left ventricular volume of normal subjects during CT coronary angiography. Jaw, FS; Jeng, CM; Mo, YH; Peng, SF; Wang, YC, ) | 0.71 |
" The difference of heart rate was negatively correlated with the dosage of propranolol." | ( Effects of propranolol on the left ventricular volume of normal subjects during CT coronary angiography. Jaw, FS; Jeng, CM; Mo, YH; Peng, SF; Wang, YC, ) | 0.75 |
"The difference of heart rate is significantly influenced by gender and the dosage of propranolol." | ( Effects of propranolol on the left ventricular volume of normal subjects during CT coronary angiography. Jaw, FS; Jeng, CM; Mo, YH; Peng, SF; Wang, YC, ) | 0.75 |
" We proposed a systematic classification scheme using FDA-approved drug labeling to assess the DILI potential of drugs, which yielded a benchmark dataset with 287 drugs representing a wide range of therapeutic categories and daily dosage amounts." | ( FDA-approved drug labeling for the study of drug-induced liver injury. Chen, M; Fang, H; Liu, Z; Shi, Q; Tong, W; Vijay, V, 2011) | 0.37 |
" An in vivo study, verapamil (25mg/kg, per oral) was administered 2h before phenytoin (30mg/kg, per oral) dosing in male Wistar rats." | ( Study on in situ and in vivo absorption kinetics of phenytoin by modulating P-glycoprotein with verapamil in rats. Bedada, SK; Ganji, D; Neerati, P, 2011) | 0.37 |
" The potential use of this synergistic interaction can be a design of new extended release pharmaceutical dosage forms with a more prolonged release (beyond 12 h) using lower polymer amount, which could be particularly beneficial for freely water-soluble drugs, preferably for once daily oral administration." | ( The influence of sodium carboxymethylcellulose on drug release from polyethylene oxide extended release matrices. Douroumis, D; Farrell, T; Levina, M; Nokhodchi, A; Palmer, D; Rajabi-Siahboomi, A, 2011) | 0.37 |
" A dosage of 2 mg/kg/d, is usually employed with a dosing interval of 8 hours." | ( [Propranolol in the treatment of infantile hemangioma: clinical effectiveness, risks, and recommendations]. López-Gutiérrez, JC; Ruiz-Rodriguez, R; Sánchez-Carpintero, I, 2011) | 1.28 |
"4 μg/g) at 1 h after dosing and generally undetectable at 8 h after dosing." | ( Distribution of propranolol in periocular tissues: a comparison of topical and systemic administration. Hao, J; Li, SK; Liu, H; Yang, MB, 2011) | 0.72 |
" The dosage was slowly increased to 2 mg/kg daily in divided doses for a mean duration of 16 weeks (range 4 weeks-41 weeks)." | ( [Oral propranolol in the management of periorbital proliferating phase infantile hemangioma]. Fu, HB; Guo, X; Huo, R; Lin, LL; Lü, RR; Wui, JC; Xu, GQ; Zhang, J; Zhao, ZF, 2011) | 0.85 |
" Propranolol was administered in a dosage of 2 mg/kg per day with initial monitoring of vital signs." | ( Propranolol therapy in 55 infants with infantile hemangioma: dosage, duration, adverse effects, and outcome. Günther, P; Holland-Cunz, S; Kleber, JB; Schupp, CJ, ) | 2.48 |
"The direct separation of isomeric glucuronide metabolites from propranolol dosed tissue extracts by differential mobility spectrometry-mass spectrometry (DMS-MS) with the use of the polar gas-phase chemical modifier acetonitrile was demonstrated." | ( Rapid analysis of isomeric exogenous metabolites by differential mobility spectrometry-mass spectrometry. Corr, JJ; Covey, TR; Kertesz, V; Parson, WB; Schneider, BB; Van Berkel, GJ, 2011) | 0.61 |
" This study utilises the methods of cassette dosing and the perfused ovine eye model - to reduce animal usage and therefore animal time - to show that for a series of beta adrenoreceptor antagonists, lipophilicity is a key physicochemical property that governs drug distribution within the eye." | ( A pharmacokinetic study of a combination of beta adrenoreceptor antagonists - in the isolated perfused ovine eye. Mains, J; Tan, LE; Urquhart, A; Wilson, C, 2012) | 0.38 |
" It is concluded that, at the dosage used, propranolol, unlike diazepam, does not affect the central mechanisms determining CNV magnitude or subjective anxiety." | ( A comparison of some physiological and psychological effects of propranolol and diazepam in normal subjects. Ashton, H; Millman, JE; Telford, R; Thompson, JW, 1976) | 0.76 |
" Normally, an increase in chlorine dosage and pH resulted in faster degradation of these pharmaceuticals." | ( Reaction of β-blockers and β-agonist pharmaceuticals with aqueous chlorine. Investigation of kinetics and by-products by liquid chromatography quadrupole time-of-flight mass spectrometry. Cela, R; Quintana, JB; Rodil, R, 2012) | 0.38 |
"To assess the effect of various levosimendan dosing regimens on hemodynamics in a rodent model of propranolol poisoning." | ( Levosimendan does not improve cardiac output or blood pressure in a rodent model of propranolol toxicity when administered using various dosing regimens. Graudins, A; Kalam, Y, 2012) | 0.82 |
" Levosimendan did not improve CO or BP with any dosing regimen." | ( Levosimendan does not improve cardiac output or blood pressure in a rodent model of propranolol toxicity when administered using various dosing regimens. Graudins, A; Kalam, Y, 2012) | 0.6 |
" The symptoms resolved after dosage tapering." | ( Treatment with propranolol for infantile hemangioma in 13 Taiwanese newborns and young infants. Chang, TK; Chen, CH; Chou, CM; Hsu, TC; Lin, HK; Wang, JD; Wang, TM, 2012) | 0.73 |
" Long exposures (24 h) in dose-response experiments with norepinephrine or epinephrine induced significant increases in DNA damage in treated cells compared to that of untreated controls as measured by the alkaline comet assay." | ( Chronic exposure to stress hormones promotes transformation and tumorigenicity of 3T3 mouse fibroblasts. Baum, A; Chambers, WH; Episcopo, B; Flint, MS; Jenkins, FJ; Knickelbein, KZ; Liegey Dougall, AJ, 2013) | 0.39 |
" The oral delivery of antihypertensive propranolol HCl was facilitated by preparing an effervescent floating dosage form which could increase its absorption in the stomach by increasing the drug's gastric residence time." | ( Design and in vitro evaluation of effervescent gastric floating drug delivery systems of propanolol HCl. Battu, JR; Kolapalli, VR; Meka, VS; Nali, SR; Songa, AS, 2012) | 0.65 |
" We will also review the current dosing recommendations as well as potential side effects of ILE as an antidote." | ( Intravenous lipid emulsion for the treatment of drug toxicity. Ozcan, MS; Weinberg, G, ) | 0.13 |
" The potencies and equipotent doses were determined for infiltrative cutaneous analgesia on the rat back by determination of dose-response curves for propranolol and lidocaine." | ( Propranolol elicits cutaneous analgesia against skin nociceptive stimuli in rats. Chen, YC; Chen, YW; Chu, CC; Hung, CH; Wang, JJ, 2012) | 2.02 |
" Verapamil-poisoned rats received the higher dosing regimen of FDP250." | ( The effects of fructose-1,6-diphosphate on haemodynamic parameters and survival in a rodent model of propranolol and verapamil poisoning. Graudins, A; Kalam, Y, 2012) | 0.59 |
" In addition, content uniformity and release profiles of the produced solid dosage forms before and after coating were studied." | ( Tailoring controlled-release oral dosage forms by combining inkjet and flexographic printing techniques. Ehlers, H; Fors, D; Genina, N; Haeggström, E; Ihalainen, P; Kassamakov, I; Peltonen, J; Pohjala, L; Sandler, N; Vakili, H; Vuorela, P, 2012) | 0.38 |
" Use of the lowest possible dosage, slow dosage titration, three times per day dosing to minimize abrupt changes in blood pressure, and close follow-up, including neurologic consultation as needed, are recommended." | ( Propranolol use in PHACE syndrome with cervical and intracranial arterial anomalies: collective experience in 32 infants. Baselga, E; Chamlin, S; Drolet, BA; Frieden, IJ; Garzon, M; Hess, C; Maheshwari, M; Mancini, AJ; Metry, D; Powell, J; Siegel, D, ) | 1.57 |
" In patients with life-saving use in suicide attempts important role in addition to medication dosage plays an elapsed time of their consumption and speed of action taken to remove and prevent absorbtion the poison", as well as close supervision in the intensive care unit." | ( [Drugs acting on the heart-conductive system in suicide attempts]. Dabek, J; Jakubowski, D; Rychlik, W; Stachoń, K, 2012) | 0.38 |
"The main objective of the present study is the physicochemical characterization of naturally available Terminalia catappa gum (Badam gum [BG]) as a novel pharmaceutical excipient and its suitability in the development of gastroretentive floating drug delivery systems (GRFDDS) to retard the drug for 12 h when the dosage form is exposed to gastrointestinal fluids in the gastric environment." | ( Characterization and in vitro drug release studies of a natural polysaccharide Terminalia catappa gum (Badam gum). Kolapalli, VR; Meka, VS; Nali, SR; Songa, AS, 2012) | 0.38 |
" In both dosing groups, elimination half-life was significantly longer (14." | ( Propranolol concentrations after oral administration in term and preterm neonates. Bagnoli, P; Cavallaro, G; Dal Monte, M; Della Bona, ML; Donzelli, G; Filippi, L; Fiorini, P; Giocaliere, E; la Marca, G; Malvagia, S; Mosca, F, 2013) | 1.83 |
" However, the effect and mechanism of dosage form pH upon skin permeation of these weak bases is not well understood." | ( Evaluation of skin permeation of β-blockers for topical drug delivery. Chantasart, D; Hao, J; Li, SK, 2013) | 0.39 |
" Propranolol hydrochloride is available as tablet, capsule, and oral liquid dosage forms in several strengths." | ( Stability of propranolol hydrochloride in SyrSpend SF. Geiger, CM; Sorenson, B; Voudrie, MA, ) | 1.41 |
" Updates will also need to be made as more is learned regarding the optimal dosing and safety monitoring when using propranolol for this indication." | ( Propranolol treatment of infantile hemangiomas: anticipatory guidance for parents and caretakers. Blei, F; Bleib, F; Boucek, RJ; Chamlin, SL; Chiu, YE; Drolet, BA; Frieden, IJ; Frommelt, PC; Garzon, MC; Kwon, EK; MacLellan-Tobert, S; Mancini, AJ; Martin, K; Seefeldt, M; Sidbury, R; Siegel, DH, ) | 1.78 |
"Laminar extrusion of wet masses was studied as a novel technology for the production of dosage forms for oral drug delivery." | ( Production of dosage forms for oral drug delivery by laminar extrusion of wet masses. Müllers, KC; Pinto, JF; Wahl, MA, 2013) | 0.39 |
" Cassette dosing method was used in the epithelium side of cornea in vitro to get the effect of penetrant, and the perfusate was collected in the side of endothelium." | ( [Simultaneous determination of eight derivatives of propranolol in cornea perfusate in vitro by high performance liquid chromatography]. Chen, C; Liao, N; Mi, S; Wang, N; Wu, H, 2012) | 0.63 |
" The starting dosage was 2 mg/kg per day, which had been for the remaining duration of treatment." | ( Propranolol therapy of infantile hemangiomas: efficacy, adverse effects, and recurrence. Li, Q; Xiao, Q; Yu, W; Zhang, B, 2013) | 1.83 |
" Standard recommendations for dosing of insulin vary and the optimal dose of HDI in PICS has not been established." | ( A blinded, randomized, controlled trial of three doses of high-dose insulin in poison-induced cardiogenic shock. Adams, AB; Anderson, CP; Cole, JB; Ellsworth, H; Engebretsen, KM; Holger, JS; Stellpflug, SJ, 2013) | 0.39 |
" In the series of patients in this study, oral propranolol at a dosage of 2 mg/kg/day was a well-tolerated and effective treatment for IHs." | ( Use of propranolol for the treatment infantile hemangiomas in the maxillofacial region. Kasimova, KR; Metellmann, HR; Podmelle, F; Sadykov, RA; Sadykov, RR, 2013) | 1.1 |
" The system operation was tested with the extraction, separation and detection of propranolol and associated metabolites from drug dosed tissues, caffeine from a coffee bean, cocaine from paper currency, and proteins from dried sheep blood spots on paper." | ( Continuous-flow liquid microjunction surface sampling probe connected on-line with high-performance liquid chromatography/mass spectrometry for spatially resolved analysis of small molecules and proteins. Kertesz, V; Van Berkel, GJ, 2013) | 0.62 |
" C and NGR received saline injections at an identical dosage regimen." | ( [Operational mechanism modification of bone mechanostat in an animal model of nutritional stress: effect of propranolol]. Boyer, PM; Bozzini, C; Friedman, SM; Lezón, CE; Pintos, PM, ) | 0.34 |
"Design of a new dosage form manufactured by laminar extrusion for oral administration of drugs." | ( Multilayer laminar co-extrudate as a novel controlled release dosage form. Müllers, KC; Pinto, JF; Wahl, MA, 2013) | 0.39 |
" Clinical trials are required to determine the optimal dosage and pharmaceutical form, method of use and treatment duration." | ( [Rapid regression of infantile haemangioma with 2% propranolol ointment]. Azoumah, KD; Kombaté, K; Mouhari-Toure, A; Pitche, P; Saka, B; Tchamdja, K; Tchangaï-Walla, K, ) | 0.38 |
"This work describes a simple and sensitive method for simultaneous determination of zolmitriptan, naproxen and propranolol in their dosage forms using HPLC." | ( A rapid and sensitive HPLC assay of some concomitant anti-migraine drugs. El-Kadi, AO; Lotfy, HM; Michael, AM; Rezk, MR; Shehata, MA, 2014) | 0.61 |
" Pharmacokinetic and pharmacodynamic changes depend on the nature and degree of hepatic impairment and on the characteristics of the dosed drug." | ( [Effect of liver cirrhosis on pharmacokinetics and pharmacodynamics of drugs]. Perlík, F, 2013) | 0.39 |
" Oral propranolol therapy was initiated with a daily dosage of 1 mg/kg body weight." | ( Periocular infantile haemangioma and the role of propranolol. Ahmad, K; Chaudhry, TA; Kamal, M, 2013) | 1.13 |
" We assessed the safety and tolerability of acute dosing with esmolol and propranolol in patients with asthma." | ( Effects of intravenous and oral β-blockade in persistent asthmatics controlled on inhaled corticosteroids. Anderson, WJ; Lipworth, BJ; Short, PM; Williamson, PA, 2014) | 0.63 |
" Tiotropium prevented propranolol induced bronchoconstriction after acute dosing during up-titration to 80 mg with no adverse impact on asthma control." | ( Effects of intravenous and oral β-blockade in persistent asthmatics controlled on inhaled corticosteroids. Anderson, WJ; Lipworth, BJ; Short, PM; Williamson, PA, 2014) | 0.72 |
" Furthermore, vascular endothelial growth factor (VEGF), metalloproteinase-2 (MMP-2), and metalloproteinase-9 (MMP-9) levels were significantly lower in the groups with propranolol treated dosage of 5 and 10 mg kg(-1)day(-1) than in the control group." | ( Antiangiogenic effect of propranolol on the growth of the neuroblastoma xenografts in nude mice. Ji, Y; Xiao, X; Xu, T; Yang, S; Zheng, J; Zheng, S; Zhu, H, 2013) | 0.89 |
" Simulations of carbamazepine dosing regimen based on the pharmacokinetic parameters of this patient were performed to allow individualization of drug therapy." | ( Slow carbamazepine clearance in a nonadherent Malay woman with epilepsy and thyrotoxicosis. Hui-Ping Khor, A; Lim, KS; Lo, YL; Ng, CC; Yeap, LL, 2014) | 0.4 |
" Therapy should begin early, continue with the target dosage of 2 mg/kg/day in three divided doses through the proliferative phase of infantile hemangioma, and be stopped gradually." | ( Treatment of infantile hemangiomas with propranolol: clinical guidelines. Anderson, W; Stewart, K; Szychta, P, 2014) | 0.67 |
" These candidates were subjected to a dose-response bioactivity assay, measuring an increase in α-tubulin K40 acetylation in two neuronal cell lines, which yielded five compounds bioactive in both cell lines and eight compounds bioactive in at least one of the cell lines tested." | ( Development and characterization of 3-(benzylsulfonamido)benzamides as potent and selective SIRT2 inhibitors. Choi, SH; Kazantsev, AG; Khanfar, MA; Quinti, L; Silverman, RB; Wang, H, 2014) | 0.4 |
" The dosage of propranolol was 1 mg/kg/day on the first day and 2 mg/kg/day from the second day." | ( Propranolol in infantile haemangioma: simplifying pretreatment monitoring. de Buys Roessingh, A; El Ezzi, O; Hohlfeld, J, 2014) | 2.2 |
"A three-times-daily dosing regimen of propranolol had no significant sustained effects on heart rates in subjects with IH." | ( Safety profile of a divided dose of propranolol for heart rate in children with infantile haemangioma during 16 weeks of treatment. Chen, W; Shi, H; Song, H; Wang, J; Yu, Y; Zhang, X; Zhou, H, 2015) | 0.96 |
" Drug withdrawal was usually made after dosing for 1 year or under when there was a total regression of hemandiomas." | ( [Clinical analysis for treatment of 1 080 cases of infantile hemangiomas with oral propranolol]. Ge, C; Li, K; Liu, X; Qin, Z; Tai, M, 2014) | 0.63 |
" The objective of this study was to investigate the effects of dosing protocol on the distribution of propranolol in the periocular tissues and plasma after topical ocular instillation." | ( Effects of dosing protocol on distribution of propranolol in periocular tissues after topical ocular instillation. Hao, J; Li, SK; Liu, H; Yang, MB, 2015) | 0.89 |
"5% ophthalmic solution using one of the following dosing protocols: three drops of 50 μL, one drop of 50 μL, or one drop of 25 μL." | ( Effects of dosing protocol on distribution of propranolol in periocular tissues after topical ocular instillation. Hao, J; Li, SK; Liu, H; Yang, MB, 2015) | 0.68 |
"5%), decreasing the number of eye drops during dosing (three drops to one drop), or decreasing the instilled volume (50 µL to 25 µL) generally lowered the concentration of propranolol in the periocular tissues." | ( Effects of dosing protocol on distribution of propranolol in periocular tissues after topical ocular instillation. Hao, J; Li, SK; Liu, H; Yang, MB, 2015) | 0.87 |
"The dosing protocol of topical ocular instillation can be tailored to achieve the desired therapeutic concentrations of propranolol in the periocular tissues while minimizing systemic exposure." | ( Effects of dosing protocol on distribution of propranolol in periocular tissues after topical ocular instillation. Hao, J; Li, SK; Liu, H; Yang, MB, 2015) | 0.88 |
"Propranolol, now the preferred treatment for problematic proliferating infantile haemangioma (IH), at an empirical cardiovascular dosage of 2-3 mg/kg/day is associated with variable complication rates." | ( Low-dose propranolol regimen for infantile haemangioma. Itinteang, T; Leadbitter, P; Marsh, R; Tan, CE; Tan, ST, 2015) | 2.28 |
"Our observations show that gradually increasing the dosage of propranolol up to 3 mg/kg and gradually weaning the dosage is safe and effective in treatment of problematic IH." | ( Treatment of problematic infantile hemangiomas with propranolol: a series of 40 cases and review of the literature. Dębek, W; Dzienis-Koronkiewicz, E; Hermanowicz, A; Matuszczak, E; Oksiuta, M; Tylicka, M, 2014) | 0.89 |
" Following optimization of the propranolol dosing regimen (study 1), we conducted a five-period crossover study (study 2) in which subjects received the following treatments: dry powder inhaler (DPI) GSK961081 400 µg + oral placebo, DPI GSK961081 1,200 µg + oral placebo, DPI GSK961081 400 µg + oral propranolol 80 mg, DPI GSK961081 1,200 µg + oral propranolol 80 mg and DPI and oral placebo." | ( Use of propranolol blockade to explore the pharmacology of GSK961081, a bi-functional bronchodilator, in healthy volunteers: results from two randomized trials. Ambery, C; Norris, V, 2014) | 1.14 |
" The dosage was increased up to a maximum of 2 mg/kg/d and was maintained until the lesion had involuted or showed good result." | ( Treatment of rapidly proliferating haemangiomas in newborns with propranolol and review of the literature. Debek, W; Dzienis-Koronkiewicz, E; Hermanowicz, A; Matuszczak, E; Oksiuta, M, 2016) | 0.67 |
" The objective of the study is to observe the effects of acute exposure to high altitude at 4,010 m on pharmacokinetics of propranolol in rats, and to provide basis and new ideas to adjust drug dosage and administration, so as to promote rational drug use in high altitude." | ( Effects on Pharmacokinetics of Propranolol and Other Factors in Rats After Acute Exposure to High Altitude at 4,010 m. Hua, X; Juanhong, Z; Rong, W; Wenbin, L; Xiaoyu, W; Zhengping, J, 2015) | 0.91 |
" However, constant drug release rates are difficult to achieve with this type of dosage forms if the drug is freely water-soluble." | ( How to easily provide zero order release of freely soluble drugs from coated pellets. Dekyndt, B; Neut, C; Siepmann, F; Siepmann, J; Verin, J, 2015) | 0.42 |
" Atenolol may be a preferred therapeutic option compared with propanolol, in view of its convenient once-a-day dosing and better side effect profile." | ( Idiopathic aquagenic pruritus: pathogenesis and effective treatment with atenolol. Cao, T; Tan, KB; Tey, HL; Yong, AA, ) | 0.13 |
" Co-administration of diosmin with fexofenadine can reduce the dosage and results in reduced side effects of fexofenadine." | ( Effect of diosmin on the intestinal absorption and pharmacokinetics of fexofenadine in rats. Bedada, SK; Neerati, P, 2015) | 0.42 |
" Chronic dosing of propranolol may be required for efficacy; therefore, we tested the efficacy of chronic treatment with either propranolol or phenytoin on RTT mice." | ( Treatment of cardiac arrhythmias in a mouse model of Rett syndrome with Na+-channel-blocking antiepileptic drugs. Glaze, DG; Herrera, JA; Kaufmann, WE; Neul, JL; Percy, AK; Pitcher, MR; Skinner, S; Ward, CS; Wehrens, XH, 2015) | 0.75 |
" The obtained new knowledge can be helpful for the development of novel coating materials (based on QPM-MAS blends) for controlled-release dosage forms." | ( Quaternary polymethacrylate-magnesium aluminum silicate films: Water uptake kinetics and film permeability. Pongjanyakul, T; Rongthong, T; Siepmann, F; Siepmann, J; Sungthongjeen, S, 2015) | 0.42 |
" Attrition was secondary to drug-induced side effects, no response, and dosing noncompliance." | ( Propranolol Therapy for Problematic Infantile Hemangioma. Knuth, C; Murthy, A; Ng, M; Weisbrod, C, 2016) | 1.88 |
" The dosage of Propranolol was increased over the course of treatment, which initiated three days." | ( Large Doses of Propranolol for the Treatment of Infantile Cephalic and Facial Hemangiomas: A Clinical Report of 38 Cases. Jianguo, K; Mingkun, Z; Qiaoling, C; Wenjin, L; Xichun, W, 2015) | 1.12 |
"Propranolol therapy for genital infantile hemangiomas was successfully initiated and the dosage increased in 9 young children without significant side effects and with marked improvement in all patients who continued on treatment." | ( Propranolol for Treatment of Genital Infantile Hemangioma. Golden, A; Rhee, A; Tamburro, J; Tran, C, 2016) | 3.32 |
" Radiolabelled (14)C-propranolol was dosed into both single (closed) and continuous (flow-through) simulations over 13 SBR cycles." | ( Evaluation of a sequencing batch reactor sewage treatment rig for investigating the fate of radioactively labelled pharmaceuticals: Case study of propranolol. May, E; Mills, GA; Oliver, R; Popple, T; Williams, JB, 2016) | 0.95 |
" Administration of early propranolol was dosed within 24 hours of admission at 1 mg intravenous every 6 hours." | ( Early propranolol after traumatic brain injury is associated with lower mortality. Alban, RF; Barmparas, G; Bloom, MB; Chung, R; Harada, MY; Ko, A; Ley, EJ; Margulies, DR; Melo, N; Thomsen, GM, 2016) | 1.22 |
" Future studies are needed to identify additional benefits and optimal dosing regimens." | ( Early propranolol after traumatic brain injury is associated with lower mortality. Alban, RF; Barmparas, G; Bloom, MB; Chung, R; Harada, MY; Ko, A; Ley, EJ; Margulies, DR; Melo, N; Thomsen, GM, 2016) | 0.92 |
"There is not enough evidence to support or discourage the use of beta-blockers in children with congestive heart failure, or to propose a paediatric dosing scheme." | ( Beta-blockers for congestive heart failure in children. Al Dakhoul, S; Alabed, S; Bdaiwi, Y; Frobel-Mercier, AK; Sabouni, A, 2016) | 0.43 |
" Intravenous dosing of propranolol was tolerated well in a critically ill neonate with multisystem complications of prematurity." | ( Use of intravenous propranolol for control of a large cervicofacial hemangioma in a critically ill neonate. Fernando, SJ; Krol, A; Leitenberger, S; MacArthur, CJ; Majerus, M, 2016) | 1.07 |
" A thin sweetener coating layer of saccharin was successfully included in the final dosage forms for palatability purposes using a casting knife." | ( Application of a colorimetric technique in quality control for printed pediatric orodispersible drug delivery systems containing propranolol hydrochloride. Genina, N; Nyman, JO; Preis, M; Sandler, N; Vakili, H, 2016) | 0.64 |
" A wide variation of practice patterns highlights the need for further study in regard to patient outcomes, duration of therapy, and dosing to drive consensus guidelines." | ( A survey of the use of propranolol in burn centers: Who, what, when, why. Kahn, SA; LeCompte, MT; Rae, L, 2017) | 0.77 |
" However, the appropriate drug dosage, dosing regimen, time for initiation, optimal duration, monitoring for side effects remains controversial." | ( [Chinese experts consensus on the use of oral propranolol for treatment of infantile hemangiomas]. Fan, XD; Huo, R; Li, K; Liu, SH; Qin, ZP; Wang, XK; Wang, XY; Yang, YW; Zhao, JH; Zheng, JW; Zhou, DK, 2016) | 0.69 |
" No evidence-based guidelines exist for proper dosing of propranolol." | ( The use of propranolol in the treatment of subglottic hemangiomas: A literature review and meta-analysis. Dodson, KM; Hardison, S; Wan, W, 2016) | 1.07 |
" In vivo studies showed that the antitumour efficacy of propranolol follows a U-shaped biphasic dose-response curve." | ( Biphasic effects of propranolol on tumour growth in B16F10 melanoma-bearing mice. Bearzi, C; Buoncervello, M; Catalano, L; Gabriele, L; Giordani, L; Maccari, S; Macchia, D; Marano, G; Rampin, A; Rizzi, R; Spada, M; Stati, T, 2017) | 1.02 |
"Hydrophilic matrix systems are currently some of the most widely used drug delivery systems for controlled-release oral dosage forms." | ( Evaluation of the drug solubility and rush ageing on drug release performance of various model drugs from the modified release polyethylene oxide matrix tablets. Maniruzzaman, M; Nokhodchi, A; Shojaee, S, 2017) | 0.46 |
" Dose-response analyses by number of prescriptions were also performed." | ( Propranolol and survival from breast cancer: a pooled analysis of European breast cancer cohorts. Bennett, K; Brown, C; Cardwell, CR; Cronin-Fenton, D; De Schutter, H; Friis, S; Garmo, H; Gavin, A; Lambe, M; Murray, LJ; O'Rorke, M; Pottegård, A; Powe, DG; Sharp, L; Vaes, E; van Herk-Sukel, MP; Vissers, PA; Visvanathan, K, 2016) | 1.88 |
" There was little evidence of a dose-response relationship." | ( Propranolol and survival from breast cancer: a pooled analysis of European breast cancer cohorts. Bennett, K; Brown, C; Cardwell, CR; Cronin-Fenton, D; De Schutter, H; Friis, S; Garmo, H; Gavin, A; Lambe, M; Murray, LJ; O'Rorke, M; Pottegård, A; Powe, DG; Sharp, L; Vaes, E; van Herk-Sukel, MP; Vissers, PA; Visvanathan, K, 2016) | 1.88 |
" Plasma propranolol concentrations were determined following two dosing strategies: Q6 (liquid formulation; n = 86) and Q24 (extended-release capsule; n = 22)." | ( Oxandrolone Coadministration Does Not Alter Plasma Propranolol Concentrations in Severely Burned Pediatric Patients. Andersen, CR; Finnerty, CC; Guillory, AN; Herndon, DN; Silva, MB; Suman, OE, ) | 0.82 |
" However, the appropriate indications, drug dosage, dosing regimen, time for initiation, optimal duration, monitoring for side effects still remains controversial." | ( [Chinese expert consensus on the use of topical timolol maleate treatment of infantile hemangiomas]. Fan, XD; Huo, R; Jiang, CH; Lei, SR; Liu, SH; Qin, ZP; Wang, XK; Wang, XY; Yang, YW; Zhao, JH; Zheng, JW; Zhou, DK, 2016) | 0.43 |
" During the involution phase, tapering propranolol dosage can be done to minimize side effects before discontinuing treatment." | ( Propranolol therapy for infantile hemangioma: our experience. Wu, HW; Yuan, W; Zhang, L; Zheng, JW, 2017) | 2.17 |
" Our SCAMP proposes guidelines for dosing and monitoring parameters." | ( Atenolol Versus Propranolol for Treatment of Infantile Hemangiomas During the Proliferative Phase: A Retrospective Noninferiority Study. Bayart, CB; Golden, AB; Tamburro, JE; Vidimos, AT; Wang, L, 2017) | 0.8 |
"The aim of this study was to determine the appropriate propranolol dosing strategy for reducing heart rate in severely burned adults." | ( Propranolol kinetics in plasma from severely burned adults. Andersen, CR; Edgu-Fry, E; Finnerty, CC; Guillory, AN; Herndon, DN; Silva, MB; Suman, OE, 2017) | 2.15 |
" Plasma propranolol concentrations were determined in a placebo group (n=10) or following one of three dosing strategies: Q6 (n=4), Q8 (n=6), and Q24 (n=6)." | ( Propranolol kinetics in plasma from severely burned adults. Andersen, CR; Edgu-Fry, E; Finnerty, CC; Guillory, AN; Herndon, DN; Silva, MB; Suman, OE, 2017) | 2.33 |
" Plasma propranolol concentrations were significantly higher in the Q6 dosing strategy than in the Q8 dosing strategy (p=0." | ( Propranolol kinetics in plasma from severely burned adults. Andersen, CR; Edgu-Fry, E; Finnerty, CC; Guillory, AN; Herndon, DN; Silva, MB; Suman, OE, 2017) | 2.33 |
"Heart rate can be decreased to a similar degree with Q6 and Q24 dosing strategies, with the Q8 dosing strategy being less effective." | ( Propranolol kinetics in plasma from severely burned adults. Andersen, CR; Edgu-Fry, E; Finnerty, CC; Guillory, AN; Herndon, DN; Silva, MB; Suman, OE, 2017) | 1.9 |
" Establishing the optimal dosage and treatment schedule is to date a crucial issue." | ( Study protocol: safety and efficacy of propranolol 0.2% eye drops in newborns with a precocious stage of retinopathy of prematurity (DROP-ROP-0.2%): a multicenter, open-label, single arm, phase II trial. Agosti, M; Araimo, G; Aversa, S; Bagnoli, P; Berti, E; Borsari, G; Bossi, A; Bozzetti, V; Buonocore, G; Calvani, AM; Cavallaro, G; Cavallotti, B; Chirico, G; Cortinovis, I; Dal Monte, M; De Angelis, C; Donati, S; Donzelli, G; Filippi, L; Forni, G; Fortunato, P; la Marca, G; Milani, S; Mosca, F; Nascimbeni, G; Osnaghi, S; Padrini, L; Pasqualetti, R; Pugi, A; Regiroli, G; Tagliabue, P; Tomasini, B; Vanni, M; Villamor, E, 2017) | 0.72 |
"Knowledge about the region-specific absorption profiles from the gastrointestinal tract of orally administered drugs is a critical factor guiding dosage form selection in drug development." | ( Mass Spectrometry Imaging proves differential absorption profiles of well-characterised permeability markers along the crypt-villus axis. Andrén, PE; Goodwin, RJA; Hayes, MA; Hilgendorf, C; Nilsson, A; Peric, A; Strimfors, M, 2017) | 0.46 |
" Among the different mucoadhesive dosage forms, buccal films are particularly addressed for paediatric population since they are thin, adaptable to the mucosal surface and able to offer an exact and flexible dose." | ( Bilayered buccal films as child-appropriate dosage form for systemic administration of propranolol. Abruzzo, A; Bigucci, F; Cerchiara, T; Dalena, F; Luppi, B; Nicoletta, FP, 2017) | 0.68 |
" In this patient, prophylactic treatment with low dosage of propranolol was successful." | ( Primary headache associated with sexual activity: A case report. İşcanlı, MD; Özcan, T; Yancar Demir, E, 2017) | 0.7 |
" Although meta-analysis did not indicate a significant effect of beta-blockers on arterial hypotension or bradycardia, propranolol dosage in one study was reduced by 50% in infants of less than 26 weeks' gestational age due to severe hypotension, bradycardia, and apnoea in several participants." | ( Beta-blockers for prevention and treatment of retinopathy of prematurity in preterm infants. Jost, K; Kaempfen, S; Neumann, RP; Schulzke, SM, 2018) | 0.69 |
" The method was used for quantitative analysis of the drugs in raw materials and pharmaceutical dosage form." | ( Simultaneous determination of rosuvastatin and propranolol in their binary mixture by synchronous spectrofluorimetry. Abdel-Fattah, A; Abo-Serie, AAM; Attia, KAM; El-Abasawi, NM; Morshedy, S, 2018) | 0.74 |
" This study was conducted to document a safe and effective dosing regimen for three different age groups." | ( The Safety and Efficacy of Propranolol in Reducing the Hypermetabolic Response in the Pediatric Burn Population. Andersen, CR; Blumenthal, E; Herndon, DN; Meyer, WJ; Ojeda, S; Robles, L; Stevens, P, 2018) | 0.78 |
" Dosing recommendations and optimal treatment duration vary among studies, and should be altered in patients with certain medical conditions such as Posterior fossa anomalies, Hemangioma, Arterial lesions, Cardiac abnormalities/coarctation of the aorta, Eye anomalies (PHACE) syndrome." | ( Infantile hemangiomas: what have we learned from propranolol? Ghareeb, E; Hagen, R; Jalali, O; Zinn, Z, 2018) | 0.74 |
" The efficacy of propranolol for infantile hemangiomas is clear, however questions pertaining to mechanism of action, pretreatment risk stratification, and optimal dosing remain unanswered." | ( Infantile hemangiomas: what have we learned from propranolol? Ghareeb, E; Hagen, R; Jalali, O; Zinn, Z, 2018) | 1.07 |
" Cumulative dose-response curves with isoproterenol were established in basal condition, and after fifteen minutes of pre-incubation with propranolol (1x10-6 M)." | ( Inotropic and chronotropic effects of propranolol in isolated atrium of rats with fructose-induced insulin-resistance Mago, N; Rodríguez, G, 2017) | 0.93 |
" As per the guideline, a preliminary paediatric assessment was performed and a 1 mg/kg test dose was administered, followed by definitive treatment at a dosage of 2 mg/kg in three divided doses." | ( Orbital infantile haemangioma: radiological features and treatment - case series and literature review. Albanese, G; Mohandas, P; Ravenscroft, J; Srinivasan, J; Tambe, K; Taylor, T; Thomas, S; Wells, L, 2019) | 0.51 |
" Additional research may confirm the best dosage and route of administration to maximize efficacy in reducing induced astigmatism and amblyopia associated with periocular hemangiomas while minimizing side effects." | ( The Use of β-Blockers for the Treatment of Periocular Hemangiomas in Infants: A Report by the American Academy of Ophthalmology. Galvin, JA; Hutchinson, AK; Kraker, RT; Lambert, SR; Pineles, SL; VanderVeen, DK; Wilson, LB, 2019) | 0.51 |
" Cell sensitivity was assessed based on the total area under and over the dose-response curves (AUOC) in relation to baselines." | ( Differentiated mitochondrial function in mouse 3T3 fibroblasts and human epithelial or endothelial cells in response to chemical exposure. Boncler, M; Dastych, J; Golanski, J; Lukasiak, M; Watala, C, 2019) | 0.51 |
" Higher PS concentration, nZVI dosage and ultrasound power as well as acidic pH favored the PRO degradation." | ( Ultrasound-assisted heterogeneous activation of persulfate by nano zero-valent iron (nZVI) for the propranolol degradation in water. Gao, NY; Gao, YQ; Kang, SF; Wang, W; Xiang, HM; Xu, JH; Yin, DQ, 2018) | 0.7 |
" This could be advantageous for maximizing local skin drug concentrations and improving dosing schedules for infantile hemangioma treatment." | ( In Vitro Skin Retention and Drug Permeation through Intact and Microneedle Pretreated Skin after Application of Propranolol Loaded Microemulsions. Brogden, NK; Kelchen, MN, 2018) | 0.69 |
" In contrast, in Study 2 in which the timing and dosage of propranolol (0." | ( Voluntary exercise or systemic propranolol ameliorates stress-related maladaptive behaviors in female rats. Aldrich, SJ; Cahill, MM; Christ, CC; Robinson, S; Taylor-Yeremeeva, E, 2019) | 1.04 |
" The dosage of propranolol was gradually increased from 1mg to 2mg/kg/day." | ( Effects of propranolol therapy in Moroccan children with infantile hemangioma. Baline, K; Chiheb, S; Fatoiki, FZE; Hali, F; Khadir, K; Lahrichi, A, 2018) | 1.22 |
" The inkjet-printed API was immediately released from the dosage forms upon contact with the dissolution medium." | ( Edible solid foams as porous substrates for inkjet-printable pharmaceuticals. Bar-Shalom, D; Edinger, M; Genina, N; Iftimi, LD; Rantanen, J, 2019) | 0.51 |
" Dosage was not adjusted to patients' weight gain." | ( EFFECTIVENESS OF FIXED DOSES OF PROPRANOLOL IN THE TREATMENT OF HEMANGIOMAS REGARDLESS OF CHILD'S WEIGHT GAIN: A CASE REPORT. Anger, J; Gabel, J; Oliveira, EM, 2019) | 0.8 |
"It is possible to treat patients with Propranolol 10 mg tablets, even though the dosage is not as precise as when calculated according to patients' weight." | ( EFFECTIVENESS OF FIXED DOSES OF PROPRANOLOL IN THE TREATMENT OF HEMANGIOMAS REGARDLESS OF CHILD'S WEIGHT GAIN: A CASE REPORT. Anger, J; Gabel, J; Oliveira, EM, 2019) | 1.07 |
"Floor effects in the delayed impact of the emotional scene could preclude observing differences as a function of propranolol, and propranolol dosage may need to be increased." | ( Encoding or consolidation? The effects of pre- and post-learning propranolol on the impact of an emotional scene. Bekker, TA; De Bree, AM; Elsey, JWB; Kindt, M, 2020) | 1.01 |
" Currently, oral propranolol is the treatment of choice for infantile hemangioma, but there is no consensus when it comes to its recommended dosage for this condition." | ( Individualized dosing of oral propranolol for treatment of infantile hemangioma: a prospective study. Kumar, B; Kumari, M; Prasad, A; Sinha, AK, 2019) | 1.14 |
" A dosage of 2 mg/kg/day propranolol orally may be a good choice for IH." | ( Efficacy and adverse effects of oral propranolol in infantile hemangioma: a meta-analysis of comparative studies. Guo, XD; Hu, DL; Shu, Q; Yang, H, 2019) | 1.09 |
"To evaluate the medical literature on the use of β-blockers, through different routes, for the treatment of periorbital infantile hemangiomas and to summarize the recommendations available on dosage and monitoring." | ( β-blockers in the treatment of periocular infantile hemangioma. Al-Haddad, C; El Moussawi, Z; El Salloukh, NA, 2019) | 0.51 |
"β-blockers have been shown to improve survival after traumatic brain injury (TBI); however, the impact of continuous dosage of β-blockers on cognitive function has not been elucidated." | ( Propranolol attenuates cognitive, learning, and memory deficits in a murine model of traumatic brain injury. Bae, EH; Friese, RS; Gries, L; Hamidi, M; Hanna, K; Joseph, B; Kulvatunyou, N; OʼKeeffe, T; Tang, A; Zakaria, ER; Zeeshan, M, 2019) | 1.96 |
" It is not possible to put a temporal period for each segment, as the hair growth at the age of 32 months is not the same as for an adult (difference in the duration of the anagen period), nor to put any quantitative dosage or frequency of exposure(s) when interpreting the data." | ( The Difficult Interpretation of a Hair Test Result from a 32-Month-Old Child: Administration of Propranolol and Quetiapine or Contamination? Ameline, A; Kintz, P; Raul, JS, 2020) | 0.78 |
" This dosing schedule caused daily drug-free periods of at least 6 h as evidenced by propranolol plasma concentrations and cardiac β-adrenergic responsiveness." | ( Intermittent β-adrenergic blockade downregulates the gene expression of β-myosin heavy chain in the mouse heart. Ambrosio, C; Barbagallo, F; Catalano, L; Grò, MC; Maccari, S; Marano, G; Matarrese, P; Molinari, P; Pace, V; Patrizio, M; Rizzi, R; Stati, T; Vezzi, V, 2020) | 0.78 |
" We review the indications, dosing regimens, duration of treatment, efficacy and adverse effects of propranolol, and therapeutic alternatives including oral atenolol, acebutolol, nadolol, intralesional propranolol injections, topical propranolol and timolol, and oral captopril." | ( β-blocker therapy for infantile hemangioma. Koh, SP; Leadbitter, P; Smithers, F; Tan, ST, 2020) | 0.77 |
" More research is required to understand the optimal dosing and duration, efficacy and safety of these alternative therapies." | ( β-blocker therapy for infantile hemangioma. Koh, SP; Leadbitter, P; Smithers, F; Tan, ST, 2020) | 0.56 |
"There is not enough evidence to support or discourage the use of beta-blockers in children with congestive heart failure, or to propose a paediatric dosing scheme." | ( Beta-blockers for congestive heart failure in children. Al Dakhoul, S; Alabed, S; Bdaiwi, Y; Sabouni, A, 2020) | 0.56 |
" Although oral propranolol is currently first-line therapy, optimal dosing for treatment of IH remains debated." | ( Retrospective case series of increased oral propranolol dosage for infantile hemangiomas. Aggarwal, P; Cohen, BA; Huang, AH; Mahon, M; Mannschreck, D, 2020) | 1.17 |
" Baseline characteristics were compared between patients who received increased propranolol dosing (≥2." | ( Retrospective case series of increased oral propranolol dosage for infantile hemangiomas. Aggarwal, P; Cohen, BA; Huang, AH; Mahon, M; Mannschreck, D, 2020) | 1.05 |
"Of 245 patients, 204 (83%) received standard 2 mg/kg/d propranolol dosing while 41 (17%) received a higher dose of ≥2." | ( Retrospective case series of increased oral propranolol dosage for infantile hemangiomas. Aggarwal, P; Cohen, BA; Huang, AH; Mahon, M; Mannschreck, D, 2020) | 1.07 |
" Patients had little improvement in HAS score with increased propranolol dosing implemented late in the treatment course with over one-fourth ultimately receiving surgical excision." | ( Retrospective case series of increased oral propranolol dosage for infantile hemangiomas. Aggarwal, P; Cohen, BA; Huang, AH; Mahon, M; Mannschreck, D, 2020) | 1.06 |
"These findings support that propranolol hydrochloride bucco-adhesive film can be considered as a proper effective dosage form for pediatric delivery." | ( Bucco-Adhesive Film as a Pediatric Proper Dosage Form for Systemic Delivery of Propranolol Hydrochloride: In-vitro and in-vivo Evaluation. Mansour, HF; Mohamad, SA; Salem, H; Yassin, HA, 2020) | 1.08 |
"Buccal matrices represent a widely accepted dosage form permitting a convenient, easy, reliable drug administration and reducing administration errors." | ( Freeze-Dried Matrices for Buccal Administration of Propranolol in Children: Physico-Chemical and Functional Characterization. Abruzzo, A; Adduci, R; Bigucci, F; Cerchiara, T; Crispini, A; Dalena, F; Luppi, B; Nicoletta, FP; Prata, C, 2021) | 0.87 |
" Two patients in the nadolol group required dosage reduction due to asymptomatic bradycardia." | ( Propranolol versus nadolol for treatment of pediatric subglottic hemangioma. Cushing, SL; Pope, E; Propst, EJ; Wolter, JK; Wolter, NE; Yang, W, 2021) | 2.06 |
" Ninety percent of women reached the target propranolol dosing of 80 mg ER daily, and 70% took the target propranolol dose until the night before surgery." | ( Phase II study of propranolol feasibility with neoadjuvant chemotherapy in patients with newly diagnosed breast cancer. Accordino, M; Crew, KD; Hershman, DL; Hopson, MB; Kalinsky, K; Lee, S; Maurer, M; Trivedi, M, 2021) | 1.22 |
" Propranolol can commence for most infants in the outpatient setting and the most frequently employed dosing regimen is 1 mg/kg twice daily." | ( Infantile hemangioma. Part 2: Management. Rodríguez Bandera, AL; Sebaratnam, DF; Wargon, O; Wong, LF, 2021) | 1.53 |
" Patient characteristics, location of hemangioma(s), weight at initiation of treatment, dosing information, side effects, response, and duration of treatment were documented." | ( Safety of propranolol for infantile hemangioma in infants less than five weeks corrected age. Check, JF; Gatts, JE; McLean, TW; Rush, MC; Samelak, DM, 2022) | 1.12 |
" However, a high level of heterogeneity, variation in propranolol dosage and inadequate sample sizes mean that these findings require cautious interpretation." | ( Effects of propranolol on the modification of trauma memory reconsolidation in PTSD patients: A systematic review and meta-analysis. Benedek, DM; Canales, JJ; Eri, R; Johnson, LR; Raut, SB; Ravindran, M; Ursano, RJ, 2022) | 1.36 |
" The dosage can be adjusted flexibly by the model shape and size." | ( Semisolid Extrusion 3D Printing of Propranolol Hydrochloride Gummy Chewable Tablets: an Innovative Approach to Prepare Personalized Medicine for Pediatrics. Gao, X; Han, X; Liu, N; Sun, Y; Tian, Y; Wang, Z; Zhang, E; Zhang, H; Zheng, A; Zhu, C, 2022) | 1 |
" The majority of our cases made some change in their daily medication dosage during the course of the study - 73." | ( Prospective, longitudinal analysis of medication use in a cohort of elderly essential tremor cases. Berry, DS; Delgado, N; Hernandez, DI; Louis, ED, 2022) | 0.72 |
" nonuse and daily dosage of both primidone and propranolol fluctuated across time for a sizable proportion of ET cases." | ( Prospective, longitudinal analysis of medication use in a cohort of elderly essential tremor cases. Berry, DS; Delgado, N; Hernandez, DI; Louis, ED, 2022) | 0.98 |
" There are no established recommendations for the dosage of sirolimus for this particular indication." | ( Severe consumptive hypothyroidism in hepatic hemangioendothelioma. Dubinski, I; Häberle, B; Küppers, J; Lurz, E; Schmid, I; Schmidt, H; Walther, A, 2022) | 0.72 |
" Since 2020, twice-daily dosage was more frequently prescribed than three times daily (p = 0." | ( Management of infantile hemangiomas-experience of a tertiary hospital. Álvares, S; Banquart Leitão, J; Barbosa-Sequeira, J; Correia, MR; Fernandes, A; Fraga, C; Gomes, R; Paiva Coelho, M; Salazar, L, 2023) | 0.91 |
" A propranolol dosage level of less than 3 mg/kg/day protected against early relapse [OR = 0." | ( Factors associated with early relapse of infantile haemangioma in children treated for at least six months with oral propranolol: A case-control study using the 2014-2021 French Ouest DataHub. Abasq, C; Adamski, H; Barbarot, S; Beuchée, A; Bouzillé, G; Chrétien, JM; Descatha, A; Droitcourt, C; Dupuy, A; Goronflot, T; Gourraud, PA; Happe, A; Herbert, J; Martin, L; Maruani, A; Mauguen, C; Oger, E, 2023) | 1.74 |
"This study showed that propranolol decreased the PI of the aorta and PI and RI of the caudal vena cava in healthy normal cats 2 h post-propranolol ingestion at the dosage of 1 mg/kg." | ( Effects of oral propranolol on the resistive and pulsatility indices of major abdominal vasculatures in domestic short-haired cats. Amini Masouleh, S; Bokaie, S; Nasrollahzadeh Masouleh, M; Vazir, B, 2023) | 1.57 |
" Tests related to adsorption kinetics, equilibrium isotherms and adsorbent reuse were studied, and optimization parameters related to the initial pH of the solution and the adsorbent dosage were defined." | ( Adsorption of chloroquine, propranolol, and metformin in aqueous solutions using magnetic graphene oxide nanocomposite. Cavalcanti, JVFL; da Motta Sobrinho, MA; de Araújo, CMB; Del Carmen Pinto Osorio, D; do Nascimento, BF; Dotto, GL; Silva, LFO, 2023) | 1.21 |
Role | Description |
---|---|
beta-adrenergic antagonist | An agent that binds to but does not activate beta-adrenergic receptors thereby blocking the actions of endogenous or exogenous beta-adrenergic agonists. beta-Adrenergic antagonists are used for treatment of hypertension, cardiac arrhythmias, angina pectoris, glaucoma, migraine headaches and anxiety. |
anxiolytic drug | Anxiolytic drugs are agents that alleviate anxiety, tension, and anxiety disorders, promote sedation, and have a calming effect without affecting clarity of consciousness or neurologic conditions. |
anti-arrhythmia drug | A drug used for the treatment or prevention of cardiac arrhythmias. Anti-arrhythmia drugs may affect the polarisation-repolarisation phase of the action potential, its excitability or refractoriness, or impulse conduction or membrane responsiveness within cardiac fibres. |
vasodilator agent | A drug used to cause dilation of the blood vessels. |
antihypertensive agent | Any drug used in the treatment of acute or chronic vascular hypertension regardless of pharmacological mechanism. |
xenobiotic | A xenobiotic (Greek, xenos "foreign"; bios "life") is a compound that is foreign to a living organism. Principal xenobiotics include: drugs, carcinogens and various compounds that have been introduced into the environment by artificial means. |
environmental contaminant | Any minor or unwanted substance introduced into the environment that can have undesired effects. |
human blood serum metabolite | Any metabolite (endogenous or exogenous) found in human blood serum samples. |
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] |
Class | Description |
---|---|
secondary amine | A compound formally derived from ammonia by replacing two hydrogen atoms by hydrocarbyl groups. |
propanolamine | |
naphthalenes | Any benzenoid aromatic compound having a skeleton composed of two ortho-fused benzene rings. |
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] |
Pathway | Proteins | Compounds |
---|---|---|
Propranolol Action Pathway | 47 | 8 |
Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
thioredoxin reductase | Rattus norvegicus (Norway rat) | Potency | 42.2395 | 0.1000 | 20.8793 | 79.4328 | AID588453; AID588456 |
TDP1 protein | Homo sapiens (human) | Potency | 16.3601 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
arylsulfatase A | Homo sapiens (human) | Potency | 2.1331 | 1.0691 | 13.9551 | 37.9330 | AID720538 |
euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 3.1623 | 0.0355 | 20.9770 | 89.1251 | AID504332 |
D(1A) dopamine receptor | Homo sapiens (human) | Potency | 14.1254 | 0.0224 | 5.9449 | 22.3872 | AID488981 |
Ataxin-2 | Homo sapiens (human) | Potency | 14.1254 | 0.0119 | 12.2221 | 68.7989 | AID588378 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Beta-1 adrenergic receptor | Cavia porcellus (domestic guinea pig) | IC50 (µMol) | 0.0347 | 0.0347 | 0.0747 | 0.1148 | AID42036 |
Gamma-aminobutyric acid receptor subunit pi | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0288 | 0.0001 | 0.5075 | 10.0000 | AID40713 |
Solute carrier family 22 member 1 | Homo sapiens (human) | IC50 (µMol) | 63.2000 | 0.2100 | 5.5537 | 10.0000 | AID386625 |
ATP-binding cassette sub-family C member 3 | Homo sapiens (human) | IC50 (µMol) | 133.0000 | 0.6315 | 4.4531 | 9.3000 | AID1473740 |
Multidrug resistance-associated protein 4 | Homo sapiens (human) | IC50 (µMol) | 133.0000 | 0.2000 | 5.6774 | 10.0000 | AID1473741 |
Voltage-dependent L-type calcium channel subunit alpha-1C | Cavia porcellus (domestic guinea pig) | IC50 (µMol) | 21.0000 | 0.0220 | 1.6422 | 8.9000 | AID1207691 |
Bile salt export pump | Rattus norvegicus (Norway rat) | IC50 (µMol) | 1,000.0000 | 0.4000 | 2.7500 | 8.6000 | AID1209456 |
5-hydroxytryptamine receptor 4 | Cavia porcellus (domestic guinea pig) | IC50 (µMol) | 2.2940 | 0.0001 | 1.0076 | 8.7800 | AID625218 |
5-hydroxytryptamine receptor 4 | Cavia porcellus (domestic guinea pig) | Ki | 1.2020 | 0.0000 | 0.8871 | 10.0000 | AID625218 |
Bile salt export pump | Homo sapiens (human) | IC50 (µMol) | 567.0000 | 0.1100 | 7.1903 | 10.0000 | AID1209455; AID1443980; AID1449628; AID1473738 |
Cytochrome P450 1A2 | Homo sapiens (human) | IC50 (µMol) | 7.0000 | 0.0001 | 1.7740 | 10.0000 | AID1262929; AID625245 |
Beta-2 adrenergic receptor | Homo sapiens (human) | IC50 (µMol) | 0.0114 | 0.0002 | 0.9326 | 7.2000 | AID1262864; AID1669462; AID1669463; AID41136; AID41152; AID625205 |
Beta-2 adrenergic receptor | Homo sapiens (human) | Ki | 0.0014 | 0.0000 | 0.6635 | 9.5499 | AID1061255; AID1061256; AID1350481; AID1603579; AID625205 |
Muscarinic acetylcholine receptor M2 | Homo sapiens (human) | IC50 (µMol) | 5.0119 | 0.0000 | 1.2326 | 7.7930 | AID1262892 |
ATP-dependent translocase ABCB1 | Homo sapiens (human) | IC50 (µMol) | 573.0000 | 0.0002 | 2.3185 | 10.0000 | AID150618 |
ATP-dependent translocase ABCB1 | Homo sapiens (human) | Ki | 48.0000 | 0.0200 | 2.3594 | 8.5900 | AID150735 |
Beta-1 adrenergic receptor | Homo sapiens (human) | IC50 (µMol) | 0.0575 | 0.0002 | 1.4681 | 9.0000 | AID1262865; AID41136; AID41152; AID42031; AID625204 |
Beta-1 adrenergic receptor | Homo sapiens (human) | Ki | 0.0042 | 0.0001 | 1.3391 | 9.9840 | AID1350482; AID1603580; AID218718; AID625204 |
Cytochrome P450 3A4 | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0001 | 1.7536 | 10.0000 | AID1262927 |
5-hydroxytryptamine receptor 1A | Homo sapiens (human) | IC50 (µMol) | 3.9811 | 0.0001 | 0.6664 | 10.0000 | AID1262875 |
Alpha-2A adrenergic receptor | Homo sapiens (human) | IC50 (µMol) | 5.0119 | 0.0000 | 1.4421 | 7.3470 | AID1262885 |
Adenosine receptor A3 | Homo sapiens (human) | IC50 (µMol) | 5.0119 | 0.0000 | 1.8940 | 8.5470 | AID1262883 |
Beta-2 adrenergic receptor | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0120 | 0.0030 | 1.1783 | 9.7724 | AID41607; AID41610 |
Beta-2 adrenergic receptor | Rattus norvegicus (Norway rat) | Ki | 1.6000 | 0.0005 | 0.3546 | 1.6000 | AID41752 |
Cytochrome P450 2C8 | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0008 | 1.8848 | 7.9000 | AID1262931 |
Cytochrome P450 2D6 | Homo sapiens (human) | IC50 (µMol) | 2.9706 | 0.0000 | 2.0151 | 10.0000 | AID1262928; AID241889; AID625249 |
Muscarinic acetylcholine receptor M1 | Homo sapiens (human) | IC50 (µMol) | 5.0119 | 0.0000 | 1.4039 | 10.0000 | AID1262891 |
Cytochrome P450 2C9 | Homo sapiens (human) | IC50 (µMol) | 30.0000 | 0.0000 | 2.8005 | 10.0000 | AID1210069; AID1262932 |
Beta-3 adrenergic receptor | Homo sapiens (human) | IC50 (µMol) | 0.0493 | 0.0023 | 3.2415 | 8.0600 | AID41136; AID41152; AID625206 |
Beta-3 adrenergic receptor | Homo sapiens (human) | Ki | 0.0990 | 0.0030 | 2.3098 | 6.0450 | AID625206 |
D(2) dopamine receptor | Homo sapiens (human) | IC50 (µMol) | 5.0119 | 0.0000 | 0.7472 | 8.0000 | AID1262894 |
Gamma-aminobutyric acid receptor subunit beta-1 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0288 | 0.0001 | 0.5075 | 10.0000 | AID40713 |
Alpha-1B adrenergic receptor | Rattus norvegicus (Norway rat) | IC50 (µMol) | 100.0000 | 0.0002 | 1.8742 | 10.0000 | AID37016 |
Beta-1 adrenergic receptor | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0120 | 0.0030 | 0.0787 | 0.3250 | AID41607; AID41610 |
Beta-1 adrenergic receptor | Rattus norvegicus (Norway rat) | Ki | 0.2713 | 0.0000 | 0.6673 | 10.0000 | AID1353525; AID266006; AID266007; AID266008; AID266009; AID266010; AID41752 |
Gamma-aminobutyric acid receptor subunit delta | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0288 | 0.0001 | 0.5075 | 10.0000 | AID40713 |
Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0288 | 0.0001 | 0.5057 | 10.0000 | AID40713 |
Alpha-2C adrenergic receptor | Homo sapiens (human) | IC50 (µMol) | 5.0119 | 0.0000 | 1.4725 | 7.8980 | AID1262886 |
D(3) dopamine receptor | Rattus norvegicus (Norway rat) | Ki | 5.0000 | 0.0001 | 0.2567 | 5.8000 | AID65625 |
5-hydroxytryptamine receptor 1A | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0827 | 0.0003 | 1.3833 | 8.4000 | AID40713; AID41607; AID625190 |
5-hydroxytryptamine receptor 1A | Rattus norvegicus (Norway rat) | Ki | 0.1390 | 0.0001 | 0.7396 | 10.0000 | AID625190 |
Gamma-aminobutyric acid receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0288 | 0.0001 | 0.4973 | 10.0000 | AID40713 |
Gamma-aminobutyric acid receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0288 | 0.0001 | 0.5075 | 10.0000 | AID40713 |
Muscarinic acetylcholine receptor M3 | Homo sapiens (human) | IC50 (µMol) | 5.0119 | 0.0001 | 1.0104 | 9.9280 | AID1262890 |
D(1A) dopamine receptor | Homo sapiens (human) | IC50 (µMol) | 5.0119 | 0.0003 | 1.8473 | 9.2250 | AID1262893 |
Voltage-dependent L-type calcium channel subunit alpha-1C | Rattus norvegicus (Norway rat) | IC50 (µMol) | 21.0000 | 0.0013 | 2.2495 | 6.9000 | AID1207691 |
Gamma-aminobutyric acid receptor subunit gamma-1 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0288 | 0.0001 | 0.4988 | 10.0000 | AID40713 |
Gamma-aminobutyric acid receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0288 | 0.0001 | 0.5046 | 10.0000 | AID40713 |
Alpha-1D adrenergic receptor | Rattus norvegicus (Norway rat) | IC50 (µMol) | 100.0000 | 0.0002 | 1.2704 | 10.0000 | AID37016 |
Endothelin-1 receptor | Homo sapiens (human) | IC50 (µMol) | 5.0119 | 0.0000 | 0.7647 | 9.9000 | AID1262895 |
Beta-3 adrenergic receptor | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0120 | 0.0030 | 0.0787 | 0.3250 | AID41607; AID41610 |
Beta-3 adrenergic receptor | Rattus norvegicus (Norway rat) | Ki | 1.6000 | 0.0005 | 0.3367 | 1.6000 | AID41752 |
5-hydroxytryptamine receptor 1B | Homo sapiens (human) | IC50 (µMol) | 5.0119 | 0.0005 | 0.3975 | 6.5000 | AID1262876 |
5-hydroxytryptamine receptor 1B | Homo sapiens (human) | Ki | 10.0000 | 0.0001 | 0.5485 | 9.2100 | AID4253 |
5-hydroxytryptamine receptor 2A | Homo sapiens (human) | IC50 (µMol) | 3.2389 | 0.0001 | 0.8801 | 8.8500 | AID1262877; AID625192 |
5-hydroxytryptamine receptor 2A | Homo sapiens (human) | Ki | 0.4190 | 0.0000 | 0.3855 | 10.0000 | AID625192 |
5-hydroxytryptamine receptor 2C | Homo sapiens (human) | IC50 (µMol) | 3.6529 | 0.0001 | 1.0302 | 9.0000 | AID1262879; AID625218 |
5-hydroxytryptamine receptor 2C | Homo sapiens (human) | Ki | 1.2020 | 0.0001 | 0.9549 | 10.0000 | AID625218 |
Gamma-aminobutyric acid receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0288 | 0.0001 | 0.5075 | 10.0000 | AID40713 |
Gamma-aminobutyric acid receptor subunit gamma-3 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0288 | 0.0001 | 0.5075 | 10.0000 | AID40713 |
5-hydroxytryptamine receptor 1B | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.2430 | 0.0005 | 1.4835 | 7.8000 | AID625190 |
5-hydroxytryptamine receptor 1B | Rattus norvegicus (Norway rat) | Ki | 0.0945 | 0.0003 | 1.2967 | 9.2440 | AID3616; AID625190 |
Adenosine receptor A2a | Homo sapiens (human) | IC50 (µMol) | 5.0119 | 0.0007 | 1.5594 | 10.0000 | AID1262882 |
Gamma-aminobutyric acid receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0288 | 0.0001 | 0.5075 | 10.0000 | AID40713 |
Type-1 angiotensin II receptor | Homo sapiens (human) | IC50 (µMol) | 5.0119 | 0.0002 | 0.0932 | 3.6000 | AID1262887 |
Sodium-dependent serotonin transporter | Homo sapiens (human) | IC50 (µMol) | 0.3800 | 0.0001 | 0.8645 | 8.7096 | AID625222 |
Sodium-dependent serotonin transporter | Homo sapiens (human) | Ki | 0.2020 | 0.0000 | 0.7048 | 8.1930 | AID625222 |
Cholecystokinin receptor type A | Homo sapiens (human) | IC50 (µMol) | 5.0119 | 0.0001 | 0.3038 | 1.9000 | AID1262889 |
Cytochrome P450 2C19 | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0000 | 2.3983 | 10.0000 | AID1262930 |
5-hydroxytryptamine receptor 7 | Homo sapiens (human) | IC50 (µMol) | 5.0119 | 0.0005 | 0.4546 | 4.7640 | AID1262881 |
Beta-1 adrenergic receptor | Mus musculus (house mouse) | Ki | 0.0024 | 0.0001 | 0.1310 | 0.5500 | AID1603578 |
Alpha-1A adrenergic receptor | Homo sapiens (human) | IC50 (µMol) | 5.0119 | 0.0002 | 0.5614 | 5.4000 | AID1262884 |
Mu-type opioid receptor | Homo sapiens (human) | IC50 (µMol) | 5.0119 | 0.0001 | 0.8133 | 10.0000 | AID1262898 |
Vasopressin V1a receptor | Homo sapiens (human) | IC50 (µMol) | 5.0119 | 0.0006 | 0.3835 | 2.0000 | AID1262888 |
Delta-type opioid receptor | Homo sapiens (human) | IC50 (µMol) | 5.0119 | 0.0002 | 0.7521 | 8.0140 | AID1262896 |
Kappa-type opioid receptor | Homo sapiens (human) | IC50 (µMol) | 5.0119 | 0.0000 | 1.2011 | 10.0000 | AID1262897 |
5-hydroxytryptamine receptor 2B | Homo sapiens (human) | IC50 (µMol) | 2.6769 | 0.0001 | 1.1873 | 8.9125 | AID1262878; AID625217 |
5-hydroxytryptamine receptor 2B | Homo sapiens (human) | Ki | 0.2180 | 0.0003 | 0.7693 | 10.0000 | AID625217 |
Alpha-1A adrenergic receptor | Rattus norvegicus (Norway rat) | IC50 (µMol) | 100.0000 | 0.0000 | 1.8194 | 10.0000 | AID37016 |
5-hydroxytryptamine receptor 6 | Homo sapiens (human) | IC50 (µMol) | 4.0384 | 0.0017 | 0.8381 | 5.4200 | AID1262880; AID625221 |
5-hydroxytryptamine receptor 6 | Homo sapiens (human) | Ki | 1.4230 | 0.0002 | 0.5229 | 10.0000 | AID625221 |
5-hydroxytryptamine receptor 7 | Cavia porcellus (domestic guinea pig) | IC50 (µMol) | 63.2000 | 2.0300 | 5.5313 | 9.9000 | AID386625 |
Cytochrome P450 2J2 | Homo sapiens (human) | IC50 (µMol) | 50.0000 | 0.0120 | 2.5312 | 9.4700 | AID1210069 |
Beta-2 adrenergic receptor | Canis lupus familiaris (dog) | IC50 (µMol) | 0.0170 | 0.0001 | 2.4596 | 5.2000 | AID40703 |
Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0288 | 0.0001 | 0.5065 | 10.0000 | AID40713 |
Gamma-aminobutyric acid receptor subunit beta-3 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0288 | 0.0001 | 0.5057 | 10.0000 | AID40713 |
Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0288 | 0.0001 | 0.5075 | 10.0000 | AID40713 |
Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) | IC50 (µMol) | 2.8280 | 0.0009 | 1.9014 | 10.0000 | AID1207227 |
Voltage-dependent L-type calcium channel subunit alpha-1C | Homo sapiens (human) | IC50 (µMol) | 21.0000 | 0.0003 | 2.2545 | 9.6000 | AID1207691 |
Sodium channel protein type 5 subunit alpha | Homo sapiens (human) | IC50 (µMol) | 2.1000 | 0.0003 | 3.6484 | 9.2000 | AID1207168 |
Sodium/bile acid cotransporter | Homo sapiens (human) | IC50 (µMol) | 5.5000 | 1.0000 | 5.9267 | 9.6000 | AID681378 |
Beta-2 adrenergic receptor | Cavia porcellus (domestic guinea pig) | IC50 (µMol) | 0.0288 | 0.0004 | 0.1680 | 0.9772 | AID40713 |
GABA theta subunit | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0288 | 0.0001 | 0.5075 | 10.0000 | AID40713 |
Canalicular multispecific organic anion transporter 1 | Homo sapiens (human) | IC50 (µMol) | 133.0000 | 2.4100 | 6.3433 | 10.0000 | AID1473739 |
Sigma non-opioid intracellular receptor 1 | Homo sapiens (human) | IC50 (µMol) | 2.8700 | 0.0003 | 0.7028 | 5.3660 | AID625223 |
Sigma non-opioid intracellular receptor 1 | Homo sapiens (human) | Ki | 1.2060 | 0.0000 | 0.4901 | 10.0000 | AID625223 |
Gamma-aminobutyric acid receptor subunit epsilon | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0288 | 0.0001 | 0.5075 | 10.0000 | AID40713 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Beta-1 adrenergic receptor | Cavia porcellus (domestic guinea pig) | Kd | 0.0359 | 0.0000 | 0.5358 | 8.3176 | AID1135965; AID39943; AID39950; AID42020; AID42040; AID42209; AID42210; AID42211; AID79325; AID79651; AID79652 |
Gamma-aminobutyric acid receptor subunit pi | Rattus norvegicus (Norway rat) | Kd | 0.0030 | 0.0002 | 0.5629 | 4.4668 | AID40869 |
Albumin | Homo sapiens (human) | Kd | 520.3425 | 0.0893 | 3.3135 | 8.0000 | AID327170; AID327176; AID327177; AID327178; AID327179; AID327180 |
Beta-2 adrenergic receptor | Homo sapiens (human) | Kd | 0.0223 | 0.0000 | 0.6288 | 8.9130 | AID1626022; AID1626023; AID1798580; AID41154; AID41305; AID41306; AID426242; AID620387; AID620391 |
Muscarinic acetylcholine receptor M2 | Homo sapiens (human) | EC50 (µMol) | 5.0119 | 0.0000 | 0.7378 | 10.0000 | AID1262915 |
Beta-1 adrenergic receptor | Homo sapiens (human) | Kd | 0.0314 | 0.0001 | 0.8039 | 10.0000 | AID1798580; AID41154; AID41305; AID41306; AID620386; AID620389; AID620390 |
Alpha-2A adrenergic receptor | Homo sapiens (human) | EC50 (µMol) | 5.0119 | 0.0008 | 0.3733 | 6.7100 | AID1262908 |
Alpha-2A adrenergic receptor | Homo sapiens (human) | Kd | 100.0000 | 0.0037 | 0.1675 | 0.5754 | AID33124 |
Adenosine receptor A3 | Homo sapiens (human) | EC50 (µMol) | 5.0119 | 0.0001 | 0.4258 | 7.9800 | AID1262906 |
Muscarinic acetylcholine receptor M1 | Homo sapiens (human) | EC50 (µMol) | 5.0119 | 0.0016 | 1.3043 | 10.0000 | AID1262914 |
Beta-3 adrenergic receptor | Homo sapiens (human) | Kd | 0.0514 | 0.0001 | 0.7631 | 8.9130 | AID1798580; AID41154; AID41305; AID41306; AID620388; AID620392 |
D(2) dopamine receptor | Homo sapiens (human) | EC50 (µMol) | 5.0119 | 0.0000 | 0.1874 | 3.9000 | AID1262917 |
Gamma-aminobutyric acid receptor subunit beta-1 | Rattus norvegicus (Norway rat) | Kd | 0.0030 | 0.0002 | 0.5629 | 4.4668 | AID40869 |
Alpha-1B adrenergic receptor | Rattus norvegicus (Norway rat) | Kd | 0.0148 | 0.0002 | 0.5266 | 7.5858 | AID1123429 |
Alpha-2B adrenergic receptor | Homo sapiens (human) | Kd | 100.0000 | 0.0037 | 0.1675 | 0.5754 | AID33124 |
Beta-1 adrenergic receptor | Rattus norvegicus (Norway rat) | Kd | 0.0044 | 0.0014 | 0.0601 | 0.3910 | AID40420; AID40527 |
Gamma-aminobutyric acid receptor subunit delta | Rattus norvegicus (Norway rat) | Kd | 0.0030 | 0.0002 | 0.5629 | 4.4668 | AID40869 |
Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) | Kd | 0.0030 | 0.0002 | 0.5629 | 4.4668 | AID40869 |
Alpha-2C adrenergic receptor | Homo sapiens (human) | EC50 (µMol) | 5.0119 | 0.0005 | 0.5541 | 6.7100 | AID1262909 |
Alpha-2C adrenergic receptor | Homo sapiens (human) | Kd | 100.0000 | 0.0037 | 0.1675 | 0.5754 | AID33124 |
5-hydroxytryptamine receptor 1A | Rattus norvegicus (Norway rat) | Kd | 0.0031 | 0.0001 | 2.2933 | 8.5114 | AID40869; AID40873 |
Alpha-2B adrenergic receptor | Rattus norvegicus (Norway rat) | Kd | 0.0148 | 0.0002 | 0.6277 | 9.3325 | AID1123429 |
Gamma-aminobutyric acid receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | Kd | 0.0030 | 0.0002 | 0.5629 | 4.4668 | AID40869 |
Gamma-aminobutyric acid receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | Kd | 0.0030 | 0.0002 | 0.5629 | 4.4668 | AID40869 |
Muscarinic acetylcholine receptor M3 | Homo sapiens (human) | EC50 (µMol) | 5.0119 | 0.0004 | 0.9935 | 5.9000 | AID1262913 |
D(1A) dopamine receptor | Homo sapiens (human) | EC50 (µMol) | 5.0119 | 0.0002 | 0.4795 | 9.5000 | AID1262916 |
Alpha-2C adrenergic receptor | Rattus norvegicus (Norway rat) | Kd | 0.0148 | 0.0002 | 0.6277 | 9.3325 | AID1123429 |
Alpha-2A adrenergic receptor | Rattus norvegicus (Norway rat) | Kd | 0.0148 | 0.0002 | 0.6277 | 9.3325 | AID1123429 |
Gamma-aminobutyric acid receptor subunit gamma-1 | Rattus norvegicus (Norway rat) | Kd | 0.0030 | 0.0002 | 0.5629 | 4.4668 | AID40869 |
Gamma-aminobutyric acid receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | Kd | 0.0030 | 0.0002 | 0.5629 | 4.4668 | AID40869 |
Alpha-1D adrenergic receptor | Rattus norvegicus (Norway rat) | Kd | 0.0148 | 0.0002 | 0.8962 | 7.5858 | AID1123429 |
Alpha-1D adrenergic receptor | Homo sapiens (human) | Kd | 100.0000 | 0.0000 | 0.1945 | 1.2882 | AID33124 |
5-hydroxytryptamine receptor 1B | Homo sapiens (human) | EC50 (µMol) | 5.0119 | 0.0116 | 0.1388 | 0.4300 | AID1262899 |
5-hydroxytryptamine receptor 2A | Homo sapiens (human) | EC50 (µMol) | 5.0119 | 0.0000 | 0.2276 | 3.4750 | AID1262900 |
5-hydroxytryptamine receptor 2C | Homo sapiens (human) | EC50 (µMol) | 5.0119 | 0.0001 | 0.1008 | 2.4500 | AID1262902 |
Gamma-aminobutyric acid receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Kd | 0.0030 | 0.0002 | 0.5629 | 4.4668 | AID40869 |
Gamma-aminobutyric acid receptor subunit gamma-3 | Rattus norvegicus (Norway rat) | Kd | 0.0030 | 0.0002 | 0.5629 | 4.4668 | AID40869 |
Adenosine receptor A2a | Homo sapiens (human) | EC50 (µMol) | 5.0119 | 0.0003 | 0.7081 | 10.0000 | AID1262905 |
Neuromedin-K receptor | Cavia porcellus (domestic guinea pig) | Kd | 0.0024 | 0.0001 | 0.0056 | 0.0155 | AID79325 |
Gamma-aminobutyric acid receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | Kd | 0.0030 | 0.0002 | 0.5629 | 4.4668 | AID40869 |
Type-1 angiotensin II receptor | Homo sapiens (human) | EC50 (µMol) | 5.0119 | 0.0005 | 0.0135 | 0.0676 | AID1262910 |
Cholecystokinin receptor type A | Homo sapiens (human) | EC50 (µMol) | 5.0119 | 0.0000 | 0.0505 | 0.2691 | AID1262912 |
5-hydroxytryptamine receptor 7 | Homo sapiens (human) | EC50 (µMol) | 5.0119 | 0.0006 | 0.0356 | 0.0832 | AID1262904 |
Alpha-1A adrenergic receptor | Homo sapiens (human) | EC50 (µMol) | 5.0119 | 0.0001 | 0.5098 | 7.1000 | AID1262907 |
Alpha-1A adrenergic receptor | Homo sapiens (human) | Kd | 100.0000 | 0.0000 | 0.2048 | 1.2882 | AID33124 |
Alpha-1B adrenergic receptor | Homo sapiens (human) | Kd | 100.0000 | 0.0000 | 0.1199 | 1.2882 | AID33124 |
Mu-type opioid receptor | Homo sapiens (human) | EC50 (µMol) | 5.0119 | 0.0000 | 0.3263 | 9.4000 | AID1262921 |
Vasopressin V1a receptor | Homo sapiens (human) | EC50 (µMol) | 5.0119 | 0.0000 | 0.1971 | 3.2000 | AID1262911 |
Delta-type opioid receptor | Homo sapiens (human) | EC50 (µMol) | 5.0119 | 0.0000 | 0.4332 | 8.3000 | AID1262919 |
Kappa-type opioid receptor | Homo sapiens (human) | EC50 (µMol) | 5.0119 | 0.0000 | 0.2244 | 8.9900 | AID1262920 |
5-hydroxytryptamine receptor 2B | Homo sapiens (human) | EC50 (µMol) | 5.0119 | 0.0004 | 0.2061 | 1.0000 | AID1262901 |
Alpha-1A adrenergic receptor | Rattus norvegicus (Norway rat) | Kd | 0.0148 | 0.0002 | 0.5139 | 7.5858 | AID1123429 |
5-hydroxytryptamine receptor 6 | Homo sapiens (human) | EC50 (µMol) | 5.0119 | 0.0001 | 0.0096 | 0.0448 | AID1262903 |
Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | Kd | 0.0030 | 0.0002 | 0.5629 | 4.4668 | AID40869 |
Gamma-aminobutyric acid receptor subunit beta-3 | Rattus norvegicus (Norway rat) | Kd | 0.0030 | 0.0002 | 0.5629 | 4.4668 | AID40869 |
Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Kd | 0.0030 | 0.0002 | 0.5629 | 4.4668 | AID40869 |
Beta-2 adrenergic receptor | Cavia porcellus (domestic guinea pig) | Kd | 0.0045 | 0.0002 | 0.5477 | 4.4668 | AID1123429; AID1495599; AID40869; AID40870; AID40873 |
GABA theta subunit | Rattus norvegicus (Norway rat) | Kd | 0.0030 | 0.0002 | 0.5629 | 4.4668 | AID40869 |
Gamma-aminobutyric acid receptor subunit epsilon | Rattus norvegicus (Norway rat) | Kd | 0.0030 | 0.0002 | 0.5629 | 4.4668 | AID40869 |
Nuclear receptor subfamily 2 group E member 1 | Homo sapiens (human) | EC50 (µMol) | 33.6667 | 5.0000 | 5.0000 | 5.0000 | AID1810681; AID1810684; AID1810686 |
Nuclear receptor subfamily 2 group E member 1 | Homo sapiens (human) | Kd | 0.5000 | 0.5000 | 0.5000 | 0.5000 | AID1810687 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Beta-1 adrenergic receptor | Cavia porcellus (domestic guinea pig) | Affinity constant | 0.0130 | 0.0130 | 0.0130 | 0.0130 | AID42039 |
Alpha-2A adrenergic receptor | Homo sapiens (human) | Kapp | 0.0180 | 0.0170 | 0.0370 | 0.0930 | AID1123537 |
Beta-2 adrenergic receptor | Rattus norvegicus (Norway rat) | Kapp | 0.0180 | 0.0170 | 0.0370 | 0.0930 | AID1123537 |
Alpha-2B adrenergic receptor | Homo sapiens (human) | Kapp | 0.0180 | 0.0170 | 0.0370 | 0.0930 | AID1123537 |
Beta-1 adrenergic receptor | Rattus norvegicus (Norway rat) | Kapp | 0.0110 | 0.0077 | 0.0119 | 0.0150 | AID1123536 |
Alpha-2C adrenergic receptor | Homo sapiens (human) | Kapp | 0.0180 | 0.0170 | 0.0370 | 0.0930 | AID1123537 |
5-hydroxytryptamine receptor 1A | Rattus norvegicus (Norway rat) | Affinity constant | 0.0130 | 0.0130 | 0.0130 | 0.0130 | AID42039 |
Alpha-1D adrenergic receptor | Homo sapiens (human) | Kapp | 0.0180 | 0.0170 | 0.0370 | 0.0930 | AID1123537 |
Alpha-1A adrenergic receptor | Homo sapiens (human) | Kapp | 0.0180 | 0.0170 | 0.0370 | 0.0930 | AID1123537 |
Alpha-1B adrenergic receptor | Homo sapiens (human) | Kapp | 0.0180 | 0.0170 | 0.0370 | 0.0930 | AID1123537 |
Beta-2 adrenergic receptor | Cavia porcellus (domestic guinea pig) | Affinity constant | 0.0006 | 0.0006 | 0.0006 | 0.0006 | AID40716 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID327180 | Binding affinity to 100 uM human serum albumin at 50 uM by PAMPA method | 2008 | Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7 | New approach to measure protein binding based on a parallel artificial membrane assay and human serum albumin. |
AID1407668 | Apparent permeability of the compound from apical to basolateral side in human Caco2 cells assessed as drug recovery after 120 mins by LC-MS/MS analysis | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Hedgehog pathway inhibitors of the acylthiourea and acylguanidine class show antitumor activity on colon cancer in vitro and in vivo. |
AID1262873 | Chemical stability of compound in buffer at pH 7.4 assessed as compound remaining at 10 mg/ml after 2 days | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
AID744882 | Toxicity in rat spontaneous hypertensive model assessed as heart rate at 20 mg/kg, po measured at 6 hrs by tail-cuff method (Rvb = 405.1 +/- 24 bpm) | 2013 | Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9 | Novel hybrids of natural isochroman-4-one bearing N-substituted isopropanolamine as potential antihypertensive candidates. |
AID58778 | Duration of ischemic arrhythmias in dogs determined in minutes. | 1984 | Journal of medicinal chemistry, Sep, Volume: 27, Issue:9 | Synthesis and antiarrhythmic activity of new 1-[1-[2-[3-(alkylamino)-2-hydroxypropoxy]phenyl]vinyl]-1 H-imidazoles and related compounds. |
AID636075 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum D10 after 48 hrs by lactate dehydrogenase assay | 2012 | Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2 | Synthesis, biological evaluation and mechanistic studies of totarol amino alcohol derivatives as potential antimalarial agents. |
AID327169 | Apparent permeability across parallel artificial membrane | 2008 | Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7 | New approach to measure protein binding based on a parallel artificial membrane assay and human serum albumin. |
AID1262926 | Intrinsic clearance in rat liver microsomes at 1 uM by HPLC/MS/MS analysis | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
AID42036 | Inhibitory activity against beta-1 adrenergic receptor in guinea pig atria is determined | 1993 | Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21 | Conformationally restrained analogs of sympathomimetic catecholamines. Synthesis, conformational analysis, and adrenergic activity of isochroman derivatives. |
AID386623 | Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells at 100 uM by confocal microscopy | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19 | Structural requirements for drug inhibition of the liver specific human organic cation transport protein 1. |
AID23271 | Partition coefficient (logD7.4) | 1990 | Journal of medicinal chemistry, Jul, Volume: 33, Issue:7 | Structure-activity relationships of antineoplastic agents in multidrug resistance. |
AID37016 | Inhibition of alpha-1 adrenergic receptor isolated from rat ventricle homogenates | 1998 | Journal of medicinal chemistry, May-07, Volume: 41, Issue:10 | Synthesis and adrenergic activity of a new series of N-aryl dicyclopropyl ketone oxime ethers: SAR and stereochemical aspects. |
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AID496824 | Antimicrobial activity against Toxoplasma gondii | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID1209457 | Unbound Cmax in human plasma | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1 | In vitro inhibition of the bile salt export pump correlates with risk of cholestatic drug-induced liver injury in humans. |
AID21234 | Partition coefficient of compound in to octanol/buffer | 1991 | Journal of medicinal chemistry, Mar, Volume: 34, Issue:3 | Reevaluating equilibrium and kinetic binding parameters for lipophilic drugs based on a structural model for drug interaction with biological membranes. |
AID62114 | Evaluated for the heart rate at dose 1.0 mg/kg in 4 animals by aminophylline-induced sinus tachycardia test | 1983 | Journal of medicinal chemistry, Feb, Volume: 26, Issue:2 | Cardiac-slowing amidines containing the 3-thioindone group. Potential antianginal agents. |
AID1079939 | Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source] | |||
AID1171974 | Hepatic extraction ratio in CD-1 mouse liver microsomes at 0.75 uM incubated for 5 mins prior to NADPH addition measured after 30 mins by LC/MS/MS analysis relative to control | 2014 | Journal of medicinal chemistry, Dec-26, Volume: 57, Issue:24 | Discovery of a phosphodiesterase 9A inhibitor as a potential hypoglycemic agent. |
AID744902 | Antihypertensive activity in rat spontaneous hypertensive model assessed as mean arterial blood pressure at 20 mg/kg, po measured at 0.5 hrs by tail-cuff method (Rvb = 156.2 +/- 7.21 mmHg) | 2013 | Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9 | Novel hybrids of natural isochroman-4-one bearing N-substituted isopropanolamine as potential antihypertensive candidates. |
AID350217 | Octanol-water partition coefficient, log P of the cationic form of the compound | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10 | Lipophilicity of basic drugs measured by hydrophilic interaction chromatography. |
AID1262892 | Antagonist activity at human wild-type M2 receptor expressed in CHO-K1 cells assessed as acetylcholine-induced cAMP by HTRF assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
AID166005 | Cerebral biodistribution pattern of [123I]- ligand was evaluated in hypothalamus of anesthetized rabbit after Intravenous injection of 50 uCi after 2 hr | 1996 | Journal of medicinal chemistry, Aug-16, Volume: 39, Issue:17 | Synthesis and in vitro and in vivo characteristics of an iodinated analogue of the beta-adrenoceptor antagonist carazolol. |
AID1125254 | Antihypertensive activity in Wistar rat assessed as mean arterial pressure at 10 mg/kg, ip measured immediately at 30 mins (Rvb = 194.72 +/- 1.002 mmHg) | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Synthesis and pharmacological screening of some novel anti-hypertensive agents possessing 5-Benzylidene-2-(phenylimino)-thiazolidin-4-one ring. |
AID737837 | Selectivity ratio of GI50 for human MRC5 cells to GI50 for human SHEP cells | 2013 | Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7 | Synthesis of novel isoflavene-propranolol hybrids as anti-tumor agents. |
AID1212333 | Drug uptake in lysosomes of human Fa2N-4 cells assessed as cellular partitioning at 1 uM after 5 mins by LC-MS analysis in presence of diclofenac | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4 | Lysosomal sequestration (trapping) of lipophilic amine (cationic amphiphilic) drugs in immortalized human hepatocytes (Fa2N-4 cells). |
AID62115 | Evaluated for the heart rate at dose 1.0 mg/kg in 4 animals by glucagon-induced tachycardia test | 1983 | Journal of medicinal chemistry, Feb, Volume: 26, Issue:2 | Cardiac-slowing amidines containing the 3-thioindone group. Potential antianginal agents. |
AID61087 | Compound was tested for its ability to block isoproterenol-induced contractile force in anesthetized dogs. | 1981 | Journal of medicinal chemistry, Mar, Volume: 24, Issue:3 | Ring-hydroxylated propranolol: synthesis and beta-receptor antagonist and vasodilating activities of the seven isomers. |
AID42024 | Apparent pA2 value for myocardial contractile force (beta-1) evaluated against beta-1 adrenergic receptor in anesthetized dogs | 1985 | Journal of medicinal chemistry, Jun, Volume: 28, Issue:6 | Synthesis of 4'-hydroxypropranolol sulfate, a major non-beta-blocking propranolol metabolite in man. |
AID22764 | T1/2 in canine blood | 1984 | Journal of medicinal chemistry, Aug, Volume: 27, Issue:8 | [(Arylcarbonyl)oxy]propanolamines. 1. Novel beta-blockers with ultrashort duration of action. |
AID1207022 | Permeability of the compound at pH 5 by PAMPA | 2015 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 25, Issue:12 | Novel natural-product-like caged xanthones with improved druglike properties and in vivo antitumor potency. |
AID744906 | Antihypertensive activity in rat spontaneous hypertensive model assessed as diastolic arterial blood pressure at 20 mg/kg, po measured at 6 hrs by tail-cuff method (Rvb = 141.2 +/- 7.34 mmHg) | 2013 | Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9 | Novel hybrids of natural isochroman-4-one bearing N-substituted isopropanolamine as potential antihypertensive candidates. |
AID1212325 | Drug uptake in lysosomes of human Fa2N-4 cells assessed as cellular partitioning at 1 uM after 5 mins by LC-MS analysis in presence of ammonium chloride | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4 | Lysosomal sequestration (trapping) of lipophilic amine (cationic amphiphilic) drugs in immortalized human hepatocytes (Fa2N-4 cells). |
AID1510596 | Metabolic stability in Sprague-Dawley rat liver microsomes at 10 uM preincubated for 5 mins followed by NADPH addition and measured for 60 mins by HPLC analysis | 2019 | ACS medicinal chemistry letters, Jun-13, Volume: 10, Issue:6 | Computer-Aided Selective Optimization of Side Activities of Talinolol. |
AID1810682 | Agonist activity at in human TLX LBD expressed in human HEK293T cells coexpressing Gal4-VP 16 assessed as remaining activity measured after 14 hrs by luciferase reporter gene assay relative to control | 2021 | Journal of medicinal chemistry, 06-24, Volume: 64, Issue:12 | Propranolol Activates the Orphan Nuclear Receptor TLX to Counteract Proliferation and Migration of Glioblastoma Cells. |
AID1262903 | Agonist activity at human 5-HT6 receptor expressed in 1321N1 cells assessed as cAMP by HTRF assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
AID1262872 | Chemical stability of compound in buffer at pH 7.4 assessed as compound remaining at 10 mg/ml after 1 day | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
AID26292 | Partition coefficient (logD7.4) | 1981 | Journal of medicinal chemistry, Mar, Volume: 24, Issue:3 | Ring-hydroxylated propranolol: synthesis and beta-receptor antagonist and vasodilating activities of the seven isomers. |
AID165693 | Biodistribution pattern of [123I]- ligand was evaluated in left atrial muscle of anesthetized rabbit after Intravenous injection of 50 uCi after 2 hr | 1996 | Journal of medicinal chemistry, Aug-16, Volume: 39, Issue:17 | Synthesis and in vitro and in vivo characteristics of an iodinated analogue of the beta-adrenoceptor antagonist carazolol. |
AID625286 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID1585795 | Apparent permeability across basolateral to apical side in human Caco2 cells assessed as mean drug recovery at 2 uM after 2 hrs by lucifer yellow dye-based LC-MS/MS analysis | 2018 | Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24 | Design, Synthesis, and Biological Evaluation of 2-Nitroimidazopyrazin-one/-es with Antitubercular and Antiparasitic Activity. |
AID28925 | Highest effective permeability across hexadecane membrane (pH 4-8) | 2001 | Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6 | High-throughput permeability pH profile and high-throughput alkane/water log P with artificial membranes. |
AID232339 | Ratio of Beta-2(trachea) to Beta-1(Atria) adrenoceptor affinity constants from guinea pig | 1983 | Journal of medicinal chemistry, Nov, Volume: 26, Issue:11 | beta 1-selective adrenoceptor antagonists. 1. Synthesis and beta-adrenergic blocking activity of a series of binary (aryloxy)propanolamines. |
AID395324 | Lipophilicity, log D at pH 7.4 by liquid chromatography | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6 | Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs. |
AID220928 | Beta-adrenoceptor blocking activity after intravenous dose as inhibition of isiprenaline-induced tachycardia in rats | 1993 | Journal of medicinal chemistry, Jan-08, Volume: 36, Issue:1 | o-Chlorobenzenesulfonamidic derivatives of (aryloxy)propanolamines as beta-blocking/diuretic agents. |
AID48537 | Percent inhibition of vasopressor response | 1981 | Journal of medicinal chemistry, Nov, Volume: 24, Issue:11 | Beta-adrenergic blocking agents. 21. threo-1-(Aryloxy)-3-(alkylamino)butan-2-ols. |
AID1262889 | Antagonist activity at human wild-type CCKA receptor expressed in CHO-K1 cells assessed as CCK8-induced calcium by FDSS assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
AID1603581 | Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor I2.64C mutant expressed in HEK293T cell membranes | |||
AID1217712 | Time dependent inhibition of CYP2C8 (unknown origin) at 100 uM by LC/MS system | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
AID60112 | Number of dogs used ouabain induced arrhythmia | 1980 | Journal of medicinal chemistry, Feb, Volume: 23, Issue:2 | Mono- and diaryl-2-quinuclidinylcarbinols with local anesthetic and antiarrhythmic activity. |
AID165796 | Percentage change of IOP in rabbits after 0 min administration (1%) of compound | 1988 | Journal of medicinal chemistry, Jan, Volume: 31, Issue:1 | Improved delivery through biological membranes. 26. Design, synthesis, and pharmacological activity of a novel chemical delivery system for beta-adrenergic blocking agents. |
AID218718 | Inhibition of [3H]dihydroalprenolol binding to beta 1 adrenoceptor from turkey erythrocyte membranes. | 1993 | Journal of medicinal chemistry, Jan-08, Volume: 36, Issue:1 | o-Chlorobenzenesulfonamidic derivatives of (aryloxy)propanolamines as beta-blocking/diuretic agents. |
AID29925 | Volume of distribution in man (IV dose) | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13 | Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data. |
AID1262932 | Inhibition of human CYP2C9 by LC-MS analysis | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
AID1429806 | Apparent permeability of the compound at 10 mM at pH 6.5 after 4 hrs by PAMPA | 2017 | Journal of medicinal chemistry, 02-23, Volume: 60, Issue:4 | Antimalarial Pyrido[1,2-a]benzimidazoles: Lead Optimization, Parasite Life Cycle Stage Profile, Mechanistic Evaluation, Killing Kinetics, and in Vivo Oral Efficacy in a Mouse Model. |
AID1456599 | Apparent permeability of compound at 20 uM at pH 7.4 after 16 hrs by PAMPA | 2017 | Bioorganic & medicinal chemistry letters, 05-15, Volume: 27, Issue:10 | Y-shaped bis-arylethenesulfonic acid esters: Potential potent and membrane permeable protein tyrosine phosphatase 1B inhibitors. |
AID1146372 | Inhibition of isoproterenol-induced decrease in diastolic blood pressure in bilaterally vagotomized open chest mongrel dog model at 0.03 mg/kg, iv administered 10 to 20 mins prior to and following isoproterenol challenge | 1978 | Journal of medicinal chemistry, Jan, Volume: 21, Issue:1 | Synthesis of heteroaromatic potential beta-adrenergic antagonists by the glycidol route. |
AID636077 | Resistance index, ratio of IC50 for chloroquine-resistant Plasmodium falciparum K1 to IC50 for chloroquine-sensitive Plasmodium falciparum D10 | 2012 | Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2 | Synthesis, biological evaluation and mechanistic studies of totarol amino alcohol derivatives as potential antimalarial agents. |
AID237685 | Lipophilicity determined as logarithm of the partition coefficient in the alkane/water system | 2005 | Journal of medicinal chemistry, May-05, Volume: 48, Issue:9 | Calculating virtual log P in the alkane/water system (log P(N)(alk)) and its derived parameters deltalog P(N)(oct-alk) and log D(pH)(alk). |
AID737301 | Permeability of the compound | 2013 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 23, Issue:7 | Triazolopyridazine LRRK2 kinase inhibitors. |
AID1207258 | Effective free therapeutic plasma concentration (EFTPC): the concentration of unbound compund in the blood plasma at therapeutic dose (mean of range) | 2011 | Cardiovascular research, Jul-01, Volume: 91, Issue:1 | Simulation of multiple ion channel block provides improved early prediction of compounds' clinical torsadogenic risk. |
AID1221009 | Apparent distribution ratio of the compound in perfused liver of high-fat emulsion-induced nonalcoholic steatohepatitis Wistar rat at 8 mM after 10 mins | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4 | Hepatic pharmacokinetics of cationic drugs in a high-fat emulsion-induced rat model of nonalcoholic steatohepatitis. |
AID174556 | Change in systolic blood pressure after 33 mg/kg oral administration in spontaneous hypertensive rats after 24 hr | 1981 | Journal of medicinal chemistry, Dec, Volume: 24, Issue:12 | Antihypertensive pyrrolo[1,2-c]quinazolines and pyrrolo[1,2-c]quinazolinones. |
AID643383 | Induction of phospholipidosis in bovine corneal fibroblasts assessed as lamellar inclusion bodies after 72 hrs by light microscopy | 2012 | Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1 | In silico assay for assessing phospholipidosis potential of small druglike molecules: training, validation, and refinement using several data sets. |
AID604825 | Metabolic stability in human liver microsomes as compound remaining at 1 uM | 2010 | Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24 | A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. |
AID1137403 | In vivo beta-adrenergic receptor blockade in iv dosed anesthetized dog assessed as inhibition of isoproterenol-induced tachycardia | 1979 | Journal of medicinal chemistry, Nov, Volume: 22, Issue:11 | Symbiotic approach to drug design: antihypertensive beta-adrenergic blocking agents. |
AID48524 | In vivo beta-adrenoceptor blocking potency in cat (expressed as total dose infused over a period of 30 minutes causing 50% inhibition of the tachycardia by iv administration) | 1980 | Journal of medicinal chemistry, Oct, Volume: 23, Issue:10 | Beta-adrenergic blocking agents. 20. (3-Hydroxyprop-1-enyl)-substituted 1-(aryloxy)-3-(alkylamino)propan-2-ols. |
AID150735 | High affinity constant at binding site of human P-Glycoprotein (P-gp) in two-affinity model | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26 | Pharmacophore model of drugs involved in P-glycoprotein multidrug resistance: explanation of structural variety (hypothesis). |
AID1702309 | Intrinsic clearance in human liver microsomes at 0.1 uM | |||
AID48535 | In vivo beta adrenergic blocking potency was determined by inhibition of depressor response produced by isoproterenol (0.2 mg/kg iv) in cat preparation | 1982 | Journal of medicinal chemistry, Nov, Volume: 25, Issue:11 | Beta-adrenergic blocking agents. 22. 1-Phenoxy-3-[[(substituted-amido) alkyl]amino]-2-propanols. |
AID1572362 | Intrinsic clearance in human liver microsomes at 2 uM by LC-MS/MS analysis | 2019 | Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3 | Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors. |
AID59472 | Beta adrenergic blockade activity was measured in anesthetized dogs by blockade of isoproterenol induced hypotension after iv administration | 1980 | Journal of medicinal chemistry, Jan, Volume: 23, Issue:1 | Heterocyclic analogues of the antihypertensive beta-adrenergic blocking agent (S)-2-[3-(ter-butylamino)-2-hydroxypropoxy]-3-cyanopyridine. |
AID1305711 | Half life in mouse liver microsomes at 0.1 uM | 2016 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 26, Issue:14 | Coumarin carboxylic acids as monocarboxylate transporter 1 inhibitors: In vitro and in vivo studies as potential anticancer agents. |
AID165849 | Biodistribution pattern of [123I]- ligand was evaluated in muscle of anesthetized rabbit after Intravenous injection of 50 uCi after 2 hr | 1996 | Journal of medicinal chemistry, Aug-16, Volume: 39, Issue:17 | Synthesis and in vitro and in vivo characteristics of an iodinated analogue of the beta-adrenoceptor antagonist carazolol. |
AID1667044 | Half life in human liver microsomes in presence of NADPH | 2020 | Bioorganic & medicinal chemistry letters, 04-01, Volume: 30, Issue:7 | Discovery and optimization of 4-oxo-2-thioxo-thiazolidinones as NOD-like receptor (NLR) family, pyrin domain-containing protein 3 (NLRP3) inhibitors. |
AID1708323 | Inhibition of NE-induced lipolysis in adipocytes (unknown origin) assessed as reduction in glycerol release at 1 uM pre-incubated for 30 mins before NE stimulation for 90 mins by glycerol reagent based assay relative to control | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2 | Structure-Activity Relationship and Biological Investigation of SR18292 ( |
AID1466761 | Half life in human liver S9 fractions at 1 uM measured pretreated up to 45 mins followed by NADPH addition by LC/MS/MS analysis | 2017 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 27, Issue:12 | Drug-like property-driven optimization of 4-substituted 1,5-diarylanilines as potent HIV-1 non-nucleoside reverse transcriptase inhibitors against rilpivirine-resistant mutant virus. |
AID165817 | Percentage change of IOP in rabbits after 6 hr administration (1%) of compound | 1988 | Journal of medicinal chemistry, Jan, Volume: 31, Issue:1 | Improved delivery through biological membranes. 26. Design, synthesis, and pharmacological activity of a novel chemical delivery system for beta-adrenergic blocking agents. |
AID624627 | Ratio of apparent permeability from basolateral to apical side over apical to basolateral side determined in MDR1-MDCKII cells in the presence of inhibitor (2uM GF120919) | 2001 | The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2 | Rational use of in vitro P-glycoprotein assays in drug discovery. |
AID166137 | Cerebral biodistribution pattern of [123I]- ligand was evaluated in striatum of anesthetized rabbit after Intravenous injection of 50 uCi after 2 hr | 1996 | Journal of medicinal chemistry, Aug-16, Volume: 39, Issue:17 | Synthesis and in vitro and in vivo characteristics of an iodinated analogue of the beta-adrenoceptor antagonist carazolol. |
AID194405 | Vasodilator activity in ganglion blocked rats. Values denote percent change in mean arterial blood pressure 30 minutes after dosing rats at 3 mg/kg intravenously | 1980 | Journal of medicinal chemistry, Mar, Volume: 23, Issue:3 | Antihypertensive indole derivatives of phenoxypropanolamines with beta-adrenergic receptor antagonist and vasodilating activity. |
AID327172 | Apparent permeability across parallel artificial membrane at 10 uM in presence of 100 uM human serum albumin | 2008 | Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7 | New approach to measure protein binding based on a parallel artificial membrane assay and human serum albumin. |
AID3616 | Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand. | 1989 | Journal of medicinal chemistry, Apr, Volume: 32, Issue:4 | Design and synthesis of propranolol analogues as serotonergic agents. |
AID1136407 | Myocardial depressant activity in guinea pig atrial muscle assessed as maximal non-depressant dose by measuring contractility | 1978 | Journal of medicinal chemistry, Sep, Volume: 21, Issue:9 | Nondepressant beta-adrenergic blocking agents. 1. Substituted 3-amino-1-(5,6,7,8-tetrahydro-1-naphthoxy)-2-propanols. |
AID1146366 | Inhibition of isoproterenol-induced decrease in diastolic blood pressure in iv dosed bilaterally vagotomized open chest mongrel dog model administered 10 to 20 mins prior to and following isoproterenol challenge | 1978 | Journal of medicinal chemistry, Jan, Volume: 21, Issue:1 | Synthesis of heteroaromatic potential beta-adrenergic antagonists by the glycidol route. |
AID625277 | FDA Liver Toxicity Knowledge Base Benchmark Dataset (LTKB-BD) drugs of less concern for DILI | 2011 | Drug discovery today, Aug, Volume: 16, Issue:15-16 | FDA-approved drug labeling for the study of drug-induced liver injury. |
AID166127 | Cerebral biodistribution pattern of [123I]- ligand was evaluated in kidney of anesthetized rabbit after Intravenous injection of 50 uCi after 2 hr | 1996 | Journal of medicinal chemistry, Aug-16, Volume: 39, Issue:17 | Synthesis and in vitro and in vivo characteristics of an iodinated analogue of the beta-adrenoceptor antagonist carazolol. |
AID1667047 | Clearance in mouse liver microsomes in presence of NADPH | 2020 | Bioorganic & medicinal chemistry letters, 04-01, Volume: 30, Issue:7 | Discovery and optimization of 4-oxo-2-thioxo-thiazolidinones as NOD-like receptor (NLR) family, pyrin domain-containing protein 3 (NLRP3) inhibitors. |
AID330907 | Displacement of quinaldine red from human AAG by fluorescence method | 2008 | Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7 | Selective plasma protein binding of antimalarial drugs to alpha1-acid glycoprotein. |
AID1733545 | Efflux ratio of apparent permeability across basolateral to apical membrane over apical to basolateral membrane in human Caco2 cells at 20 uM after 2 hrs by LC-MS analysis | 2021 | Bioorganic & medicinal chemistry, 05-01, Volume: 37 | Systematic evaluation of structure-property relationships and pharmacokinetics in 6-(hetero)aryl-substituted matched pair analogs of amiloride and 5-(N,N-hexamethylene)amiloride. |
AID1636372 | Drug activation in human Hep3B cells assessed as human CYP3A4-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 53.7 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of N | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16 | Development of a cell viability assay to assess drug metabolite structure-toxicity relationships. |
AID1895164 | Permeability across apical to basal side in human Caco-2 cells preincubated with verapamil for 30 mins followed by compound addition measured at 0.5 to 2 hrs by LC-MS analysis | 2021 | Journal of medicinal chemistry, 06-24, Volume: 64, Issue:12 | Interplay among Conformation, Intramolecular Hydrogen Bonds, and Chameleonicity in the Membrane Permeability and Cyclophilin A Binding of Macrocyclic Peptide Cyclosporin O Derivatives. |
AID61088 | Compound was tested for its ability to block isoproterenol-induced increases in heart rate(HR) in anesthetized dogs. | 1981 | Journal of medicinal chemistry, Mar, Volume: 24, Issue:3 | Ring-hydroxylated propranolol: synthesis and beta-receptor antagonist and vasodilating activities of the seven isomers. |
AID7804 | In vitro metabolic potential in human liver microsomes | 2003 | Bioorganic & medicinal chemistry letters, Apr-17, Volume: 13, Issue:8 | Oxyguanidines: application to non-peptidic phenyl-based thrombin inhibitors. |
AID481442 | Transcellular permeability at pH 6.5 calculated from in vitro P app values in Caco-2 and/or MDCK cells | 2010 | Journal of medicinal chemistry, May-13, Volume: 53, Issue:9 | How well can the Caco-2/Madin-Darby canine kidney models predict effective human jejunal permeability? |
AID1212330 | Drug uptake in lysosomes of human Fa2N-4 cells assessed as cellular partitioning at 1 uM after 5 mins by LC-MS analysis in presence of chloroquine | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4 | Lysosomal sequestration (trapping) of lipophilic amine (cationic amphiphilic) drugs in immortalized human hepatocytes (Fa2N-4 cells). |
AID678715 | Inhibition of human CYP2D6 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 4-methylaminoethyl-7-methoxycoumarin as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
AID1626024 | Binding affinity to inactive/G protein-uncoupled human beta2-AR by immobilized artificial membrane HPLC analysis | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Uncoupling the Structure-Activity Relationships of β2 Adrenergic Receptor Ligands from Membrane Binding. |
AID1669462 | Antagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under dark conditions by FRET assay | 2020 | Journal of medicinal chemistry, 08-13, Volume: 63, Issue:15 | Photoswitchable Antagonists for a Precise Spatiotemporal Control of β |
AID1262923 | Kinetic solubility of compound in phosphate buffer at pH 7.4 for 4 hrs by UPLC/UV analysis | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
AID1220981 | Extraction ratio of the compound in healthy Wistar rat perfused liver at 8 mM after 10 mins | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4 | Hepatic pharmacokinetics of cationic drugs in a high-fat emulsion-induced rat model of nonalcoholic steatohepatitis. |
AID1123536 | Displacement of [3H]DHA from beta1 adrenergic receptor in rat ventricular muscle by competitive binding assay | 1979 | Journal of medicinal chemistry, Jun, Volume: 22, Issue:6 | Cardioselectivity of beta-adrenoceptor blocking agents 1. 1-[(4-Hydroxyphenethyl)amino]-3-(aryloxy)propan-2-ols. |
AID1221001 | Permeability surface area product in perfused liver of high-fat emulsion-induced nonalcoholic steatohepatitis Wistar rat assessed per gm of liver at 8 mM after 10 mins | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4 | Hepatic pharmacokinetics of cationic drugs in a high-fat emulsion-induced rat model of nonalcoholic steatohepatitis. |
AID62112 | Evaluated for the heart rate at dose 0.5 mg/kg in 4 animals by poldine tachycardia test | 1983 | Journal of medicinal chemistry, Feb, Volume: 26, Issue:2 | Cardiac-slowing amidines containing the 3-thioindone group. Potential antianginal agents. |
AID658937 | Apparent permeability from basolateral to apical side of human Caco2 cells at 100 uM up to 90 mins | 2012 | European journal of medicinal chemistry, Jun, Volume: 52 | Exploring the interplay of physicochemical properties, membrane permeability and giardicidal activity of some benzimidazole derivatives. |
AID1810687 | Binding affinity to TLX LBD expressed in His6-tagged Escherichia coli Rosetta assessed as binding constant measured after 300 sec at 200 mM by isothermal titration calorimetry | 2021 | Journal of medicinal chemistry, 06-24, Volume: 64, Issue:12 | Propranolol Activates the Orphan Nuclear Receptor TLX to Counteract Proliferation and Migration of Glioblastoma Cells. |
AID1430075 | Permeability of the compound at pH 7.4 | 2017 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5 | Identification of novel ROS inducer by merging the fragments of piperlongumine and dicoumarol. |
AID79651 | Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparation at a duration of 3h | 1982 | Journal of medicinal chemistry, Dec, Volume: 25, Issue:12 | Ultra-short-acting beta-adrenergic receptor blocking agents. 2. (Aryloxy)propanolamines containing esters on the aryl function. |
AID1262888 | Antagonist activity at human wild-type AVPR1A receptor expressed in CHO-K1 cells assessed as vassopressin-induced calcium by FDSS assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
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AID1915898 | Metabolic stability in human liver microsomes assessed as parent compound remaining at 2 uM incubated for 40 mins in presence of NADPH by LC-MS/MS analysis | |||
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AID1368592 | Apparent permeability from apical to basolateral side in MDCK2-MDR1 cells at 2 uM incubated over 150 mins at 37 degC by LC-MS/MS method | 2018 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 28, Issue:2 | Assessment of a pretomanid analogue library for African trypanosomiasis: Hit-to-lead studies on 6-substituted 2-nitro-6,7-dihydro-5H-imidazo[2,1-b][1,3]thiazine 8-oxides. |
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AID462613 | Permeability across artificial membrane assessed as membrane retention at 200 uM by PAMPA using HPLC/MS method | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6 | N-methyl phenylalanine-rich peptides as highly versatile blood-brain barrier shuttles. |
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AID1262921 | Agonist activity at human wild-type opioid-mu receptor expressed in CHO-K1 cells assessed as cAMP level by HTRF assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
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AID681378 | TP_TRANSPORTER: inhibition of Taurocholate uptake in NTCP-expressing HeLa cells | 1999 | The Journal of pharmacology and experimental therapeutics, Dec, Volume: 291, Issue:3 | Modulation by drugs of human hepatic sodium-dependent bile acid transporter (sodium taurocholate cotransporting polypeptide) activity. |
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AID165992 | Cerebral biodistribution pattern of [123I]- ligand was evaluated in cerebellum of anesthetized rabbit after Intravenous injection of 50 uCi after 2 hr | 1996 | Journal of medicinal chemistry, Aug-16, Volume: 39, Issue:17 | Synthesis and in vitro and in vivo characteristics of an iodinated analogue of the beta-adrenoceptor antagonist carazolol. |
AID1415057 | Aqueous solubility of the compound in simulated intestinal fluid | 2018 | Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23 | Application of Sequential Palladium Catalysis for the Discovery of Janus Kinase Inhibitors in the Benzo[ c]pyrrolo[2,3- h][1,6]naphthyridin-5-one (BPN) Series. |
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AID737840 | Antiproliferative activity against human SHEP cells by measuring metabolic activity of cells after 72 hrs by spectrophotometric analysis | 2013 | Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7 | Synthesis of novel isoflavene-propranolol hybrids as anti-tumor agents. |
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AID1810684 | Agonist activity at full length TLX activating element expressed in human HEK293T cells coexpressing human full-length TLX/Gal4-VP 16 assessed as decrease in reporter activity at 100 uM by luciferase reporter gene assay relative to control | 2021 | Journal of medicinal chemistry, 06-24, Volume: 64, Issue:12 | Propranolol Activates the Orphan Nuclear Receptor TLX to Counteract Proliferation and Migration of Glioblastoma Cells. |
AID737839 | Antiproliferative activity against human MRC5 cells by measuring metabolic activity of cells after 72 hrs by spectrophotometric analysis | 2013 | Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7 | Synthesis of novel isoflavene-propranolol hybrids as anti-tumor agents. |
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AID765484 | Half life in human liver microsomes at 1 uM by LC-MS analysis | 2013 | European journal of medicinal chemistry, Sep, Volume: 67 | N-aryl-6-methoxy-1,2,3,4-tetrahydroquinolines: a novel class of antitumor agents targeting the colchicine site on tubulin. |
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AID166130 | Cerebral biodistribution pattern of [123I]- ligand was evaluated in pituitary gland of anesthetized rabbit after Intravenous injection of 50 uCi after 2 hr | 1996 | Journal of medicinal chemistry, Aug-16, Volume: 39, Issue:17 | Synthesis and in vitro and in vivo characteristics of an iodinated analogue of the beta-adrenoceptor antagonist carazolol. |
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AID1895162 | Permeability across basal to apical side in human Caco-2 cells assessed as drug recovery measured at 0.5 to 2 hrs by LC-MS analysis relative to control | 2021 | Journal of medicinal chemistry, 06-24, Volume: 64, Issue:12 | Interplay among Conformation, Intramolecular Hydrogen Bonds, and Chameleonicity in the Membrane Permeability and Cyclophilin A Binding of Macrocyclic Peptide Cyclosporin O Derivatives. |
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AID166300 | Effect on IOP of rabbits 4 hr after administration (1%) | 1988 | Journal of medicinal chemistry, Jan, Volume: 31, Issue:1 | Improved delivery through biological membranes. 26. Design, synthesis, and pharmacological activity of a novel chemical delivery system for beta-adrenergic blocking agents. |
AID1407667 | Apparent permeability of the compound from apical to basolateral side in human Caco2 cells after 120 mins by LC-MS/MS analysis | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Hedgehog pathway inhibitors of the acylthiourea and acylguanidine class show antitumor activity on colon cancer in vitro and in vivo. |
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AID426242 | Binding affinity to human adrenergic beta2 receptor | 2009 | European journal of medicinal chemistry, Jul, Volume: 44, Issue:7 | Synthesis, pharmacological and in silico evaluation of 1-(4-di-hydroxy-3,5-dioxa-4-borabicyclo[4.4.0]deca-7,9,11-trien-9-yl)-2-(tert-butylamino)ethanol, a compound designed to act as a beta2 adrenoceptor agonist. |
AID1285114 | Half life in human liver microsomes at 0.1 uM up to 60 mins by HPLC-MS/MS analysis | 2016 | European journal of medicinal chemistry, Apr-13, Volume: 112 | Three stories on Eph kinase inhibitors: From in silico discovery to in vivo validation. |
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AID1171961 | Apparent clearance in CD-1 mouse liver microsomes at 0.75 uM incubated for 5 mins prior to NADPH addition measured after 30 mins by LC/MS/MS analysis | 2014 | Journal of medicinal chemistry, Dec-26, Volume: 57, Issue:24 | Discovery of a phosphodiesterase 9A inhibitor as a potential hypoglycemic agent. |
AID1365713 | Protein binding in human plasma at 5 uM after 4 hrs by LC-MS/MS analysis | 2017 | Bioorganic & medicinal chemistry, 11-01, Volume: 25, Issue:21 | The antitubercular activity of various nitro(triazole/imidazole)-based compounds. |
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AID404304 | Effect on human MRP2-mediated estradiol-17-beta-glucuronide transport in Sf9 cells inverted membrane vesicles relative to control | 2008 | Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11 | Prediction and identification of drug interactions with the human ATP-binding cassette transporter multidrug-resistance associated protein 2 (MRP2; ABCC2). |
AID1750324 | Intrinsic clearance in human liver microsomes at 1 uM measured up to 60 mins in presence of NADPH by HPLC-MS/MS analysis | 2021 | Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8 | From Celecoxib to a Novel Class of Phosphodiesterase 5 Inhibitors: Trisubstituted Pyrazolines as Novel Phosphodiesterase 5 Inhibitors with Extremely High Potency and Phosphodiesterase Isozyme Selectivity. |
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AID1443980 | Inhibition of human BSEP expressed in fall armyworm sf9 cell plasma membrane vesicles assessed as reduction in vesicle-associated [3H]-taurocholate transport preincubated for 10 mins prior to ATP addition measured after 15 mins in presence of [3H]-tauroch | 2010 | Toxicological sciences : an official journal of the Society of Toxicology, Dec, Volume: 118, Issue:2 | Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development. |
AID1350706 | Apparent permeability cross basolateral to apical side in MDCK-MDR1 cells at 5 uM after 90 mins by LC-MS/MS analysis | 2018 | Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14 | Optimization of Isothiazolo[4,3- b]pyridine-Based Inhibitors of Cyclin G Associated Kinase (GAK) with Broad-Spectrum Antiviral Activity. |
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AID1587288 | Protein binding in mouse plasma | 2019 | Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8 | Discovery of Potent, Selective, and Orally Bioavailable Inhibitors against Phosphodiesterase-9, a Novel Target for the Treatment of Vascular Dementia. |
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AID1529184 | Protein binding in immobilized human serum albumin by HPLC analysis | 2020 | Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4 | Human Serum Albumin Binding in a Vial: A Novel UV-pH Titration Method To Assist Drug Design. |
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AID232998 | Degree of Selectivity measured as the antilog of pA2 atria-pA2 trachea | 1987 | Journal of medicinal chemistry, Jun, Volume: 30, Issue:6 | Synthesis of a series of compounds related to betaxolol, a new beta 1-adrenoceptor antagonist with a pharmacological and pharmacokinetic profile optimized for the treatment of chronic cardiovascular diseases. |
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AID1810689 | Effect on TLX regulated gene expression in human T98G cells assessed as induction of SIRT1 mRNA expression at 50 uM after 8 hrs by qRT-PCR analysis | 2021 | Journal of medicinal chemistry, 06-24, Volume: 64, Issue:12 | Propranolol Activates the Orphan Nuclear Receptor TLX to Counteract Proliferation and Migration of Glioblastoma Cells. |
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AID1215121 | Fraction unbound in Wistar rat brain homogenate at 5 uM after 5 hrs by equilibrium dialysis method | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Brain tissue binding of drugs: evaluation and validation of solid supported porcine brain membrane vesicles (TRANSIL) as a novel high-throughput method. |
AID28236 | Unbound fraction (tissues) | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13 | Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data. |
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AID59381 | Myocardial depression in conscious dog; Moderate activity. | 1983 | Journal of medicinal chemistry, Feb, Volume: 26, Issue:2 | Cardiac-slowing amidines containing the 3-thioindone group. Potential antianginal agents. |
AID1262906 | Agonist activity at human wild-type A3 receptor expressed in CHO-K1 cells assessed as cAMP level by HTRF assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
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AID45741 | Collateral sensitivity of CHRC5 cells to local anesthetics/steroids as log of ratio of molar concentration of drug inducing 50% growth inhibition in CHO AUXB1 cells to that of CHRC5 cells | 1990 | Journal of medicinal chemistry, Jul, Volume: 33, Issue:7 | Structure-activity relationships of antineoplastic agents in multidrug resistance. |
AID604020 | Unbound drug concentration in Sprague-Dawley rat plasma administered in casettes of 2/3 drugs at 4 hr constant rate intravenous infusions using flow rate of 1 (ml/kg)/hr corresponding to dosage rate of 2 (umol/kg)/hr by LC-MS/MS method | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20 | Structure-brain exposure relationships in rat and human using a novel data set of unbound drug concentrations in brain interstitial and cerebrospinal fluids. |
AID1211295 | Unbound fraction in plasma (unknown origin) at pH 7.63 after 6 hrs by equilibrium dialysis method in presence of 5% CO2 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3 | Control and measurement of plasma pH in equilibrium dialysis: influence on drug plasma protein binding. |
AID503306 | Antiproliferative activity against human PC3 cells at 2 uM after 120 hrs by MTT assay relative to DMSO | 2006 | Nature chemical biology, Jun, Volume: 2, Issue:6 | Identifying off-target effects and hidden phenotypes of drugs in human cells. |
AID1495599 | Antagonist activity at adrenergic beta2 receptor in isolated guinea pig trachea assessed as inhibition of isoprenaline-induced bronchodilation incubated for 20 mins | 2018 | Bioorganic & medicinal chemistry, 07-30, Volume: 26, Issue:13 | Design, synthesis and cardiovascular evaluation of some aminoisopropanoloxy derivatives of xanthone. |
AID1262933 | Permeability across apical to basolateral in MDCK expressing human MDR1 at 5 uM by LC-MS/MS method | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
AID1215672 | Drug metabolism in pooled human hepatocytes assessed as aldehyde oxidase-mediated drug metabolism at 10 uM up to 120 mins by HPLC analysis in presence of 50 uM of hydralazine | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 40, Issue:7 | Hydralazine as a selective probe inactivator of aldehyde oxidase in human hepatocytes: estimation of the contribution of aldehyde oxidase to metabolic clearance. |
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AID368064 | Antiarrhythmic activity in anaesthetized iv dosed Wistar rat assessed as decrease in adrenaline-induced cardiac rhythm disturbance administered 15 mins before adrenaline challenge | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3 | Preliminary evaluation of pharmacological properties of some xanthone derivatives. |
AID1217705 | Time dependent inhibition of CYP2B6 (unknown origin) at 100 uM by LC/MS system | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
AID1322296 | Displacement of [3H]prazosin from alpha1 adrenergic receptor in rat brain cerebral cortex at 50 uM after 30 mins by microbeta scintillation counting method | |||
AID298035 | Fraction unbound ligand in rat lung after 20 hrs | 2007 | Journal of medicinal chemistry, Sep-20, Volume: 50, Issue:19 | High-throughput screening of drug-brain tissue binding and in silico prediction for assessment of central nervous system drug delivery. |
AID1733544 | Apparent permeability across basolateral to apical side in human Caco2 cells at 20 uM after 2 hrs by LC-MS analysis | 2021 | Bioorganic & medicinal chemistry, 05-01, Volume: 37 | Systematic evaluation of structure-property relationships and pharmacokinetics in 6-(hetero)aryl-substituted matched pair analogs of amiloride and 5-(N,N-hexamethylene)amiloride. |
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AID1530048 | Inhibition of Streptococcus pyogenes SrtA deltaN81 mutant expressed in Escherichia coli BL21(DE3) at 100 uM using Abz-LPETA-Dap(Dnp) as substrate preincubated for 10 mins followed by substrate addition measured every min for 2.5 hrs by fluorimetric assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Identification of potential antivirulence agents by substitution-oriented screening for inhibitors of Streptococcus pyogenes sortase A. |
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AID643279 | Half life in CD-1 mouse liver microsomes at 1 uM by LC-MS/MS analysis | 2012 | Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1 | Ethionamide boosters. 2. Combining bioisosteric replacement and structure-based drug design to solve pharmacokinetic issues in a series of potent 1,2,4-oxadiazole EthR inhibitors. |
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AID1135972 | Anesthetic effect in guinea pig at 0.1 % by intradermal wheal method | 1978 | Journal of medicinal chemistry, Jan, Volume: 21, Issue:1 | Adrenoceptor blocking agents. 2. 2-(alpha-Hydroxyarylmethyl)-3,3-dimethylaziridines, a new class of selective beta2-adrenoceptor antagonists. |
AID462611 | Effective permeability across artificial membrane at 200 uM by PAMPA using HPLC/MS method | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6 | N-methyl phenylalanine-rich peptides as highly versatile blood-brain barrier shuttles. |
AID1563156 | Metabolic stability in human liver microsomes assessed as compound remaining after 30 mins | 2019 | Journal of medicinal chemistry, 07-11, Volume: 62, Issue:13 | ( |
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AID80626 | Inhibition of isoproterenol-induced responses in guinea pig trachea. | 1983 | Journal of medicinal chemistry, Aug, Volume: 26, Issue:8 | Ultra-short-acting beta-adrenergic receptor blocking agents. 3. Ethylenediamine derivatives of (aryloxy)propanolamines having esters on the aryl function. |
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AID62237 | Evaluated for the heart rate at dose 2.5 mg/kg in 4 animals by glucagon-induced tachycardia test | 1983 | Journal of medicinal chemistry, Feb, Volume: 26, Issue:2 | Cardiac-slowing amidines containing the 3-thioindone group. Potential antianginal agents. |
AID62116 | Evaluated for the heart rate at dose 1.0 mg/kg in 4 animals by poldine tachycardia test | 1983 | Journal of medicinal chemistry, Feb, Volume: 26, Issue:2 | Cardiac-slowing amidines containing the 3-thioindone group. Potential antianginal agents. |
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AID41305 | Beta adrenergic receptor blocking activity measured by the chronotropic effect was determined 1 hr after pretreatment of the right atria in guinea pig | 1984 | Journal of medicinal chemistry, Sep, Volume: 27, Issue:9 | Synthesis and antiarrhythmic activity of new 1-[1-[2-[3-(alkylamino)-2-hydroxypropoxy]phenyl]vinyl]-1 H-imidazoles and related compounds. |
AID643280 | Intrinsic clearance in CD-1 mouse liver microsomes at 1 uM by LC-MS/MS analysis | 2012 | Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1 | Ethionamide boosters. 2. Combining bioisosteric replacement and structure-based drug design to solve pharmacokinetic issues in a series of potent 1,2,4-oxadiazole EthR inhibitors. |
AID171500 | Blood pressure of the urethane-anesthetized normotensive Wistar rat was tested 10 min after inducing the compound on dose of 1.0 mg/kg | 1994 | Journal of medicinal chemistry, Apr-01, Volume: 37, Issue:7 | Guaiacoxypropanolamine derivatives of capsaicin: a new family of beta-adrenoceptor blockers with intrinsic cardiotonic properties. |
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AID1765570 | Metabolic stability in human liver microsomes assessed as half life at 80 uM by HPLC analysis | 2021 | European journal of medicinal chemistry, Oct-15, Volume: 222 | Effects of substituent pattern on the intracellular target of antiproliferative benzo[b]thiophenyl chromone derivatives. |
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AID1379470 | Protein binding in Swiss Webster mouse plasma at 2 uM after 8 hrs by microdialysis based liquid chromatography/tandem mass spectrometric analysis | 2017 | ACS medicinal chemistry letters, Aug-10, Volume: 8, Issue:8 | 1-Benzyl-3-aryl-2-thiohydantoin Derivatives as New Anti- |
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AID1262875 | Antagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as seretonin-induced cAMP level by HTRF assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
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AID60896 | Percent inhibition of isoproterenol induced tachycardia at a dose of 1.3 microg (3-h infusion period) | 1984 | Journal of medicinal chemistry, Aug, Volume: 27, Issue:8 | [(Arylcarbonyl)oxy]propanolamines. 1. Novel beta-blockers with ultrashort duration of action. |
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AID1262893 | Antagonist activity at human wild-type D1 receptor expressed in CHO cells assessed as dopamine-induced cAMP by HTRF assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
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AID1526018 | Apparent permeability from apical to basolateral side in MDCK-MDR1 cells | 2019 | Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18 | Heteroaryl Phosphonates as Noncovalent Inhibitors of Both Serine- and Metallocarbapenemases. |
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AID168626 | Compound was tested for oral salidiuretic activity (control/drug treatment value) in rats expressed as urinary output. at a dose of 32 mg/kg; 9.05/10.98 | 1986 | Journal of medicinal chemistry, Jan, Volume: 29, Issue:1 | [p-[(Thienylcarbonyl)amino]phenoxy]propanolamines derivatives as diuretic and beta-adrenergic receptor blocking agents. |
AID1220975 | Drug distribution in perfused liver of high-fat emulsion-induced nonalcoholic steatohepatitis Wistar rat assessed as equilibrium amount ratio charactering slow binding process at 8 mM after 10 mins | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4 | Hepatic pharmacokinetics of cationic drugs in a high-fat emulsion-induced rat model of nonalcoholic steatohepatitis. |
AID496818 | Antimicrobial activity against Trypanosoma brucei brucei | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID624612 | Specific activity of expressed human recombinant UGT1A9 | 2000 | Annual review of pharmacology and toxicology, , Volume: 40 | Human UDP-glucuronosyltransferases: metabolism, expression, and disease. |
AID1212321 | Drug uptake in lysosomes of human Fa2N-4 cells assessed as cellular partitioning at 1 uM co-incubated with chloroquine for 5 mins by LC-MS analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4 | Lysosomal sequestration (trapping) of lipophilic amine (cationic amphiphilic) drugs in immortalized human hepatocytes (Fa2N-4 cells). |
AID234826 | Slope value of the compound | 1982 | Journal of medicinal chemistry, Jun, Volume: 25, Issue:6 | Arylethanolamines derived from salicylamide with alpha- and beta-adrenoceptor blocking activities. Preparation of labetalol, its enantiomers, and related salicylamides. |
AID1079937 | Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source] | |||
AID1703748 | Intrinsic clearance in human liver microsomes at 0.1 uM in presence of NADPH measured upto 60 mins by LC/MS/MS analysis | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | Evaluation of N-phenyl-2-aminothiazoles for treatment of multi-drug resistant and intracellular Staphylococcus aureus infections. |
AID1209584 | Drug uptake in Sprague-Dawley rat brain slices in presence of 50 pM to 50 nM of monensin | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3 | Measurement of unbound drug exposure in brain: modeling of pH partitioning explains diverging results between the brain slice and brain homogenate methods. |
AID1473741 | Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
AID171502 | Blood pressure of the urethane-anesthetized normotensive Wistar rat was tested 30 min after inducing the compound on dose of 1.0 mg/kg | 1994 | Journal of medicinal chemistry, Apr-01, Volume: 37, Issue:7 | Guaiacoxypropanolamine derivatives of capsaicin: a new family of beta-adrenoceptor blockers with intrinsic cardiotonic properties. |
AID40537 | Selectivity for beta-1 adrenergic receptor | 1988 | Journal of medicinal chemistry, Nov, Volume: 31, Issue:11 | Modeling of beta-adrenoceptors based on molecular electrostatic potential studies of agonists and antagonists. |
AID174558 | Change in systolic blood pressure after 33 mg/kg oral administration in spontaneous hypertensive rats after 4 hr | 1981 | Journal of medicinal chemistry, Dec, Volume: 24, Issue:12 | Antihypertensive pyrrolo[1,2-c]quinazolines and pyrrolo[1,2-c]quinazolinones. |
AID1545657 | Intrinsic clearance in CD1 mouse liver microsomes by HPLC analysis | 2019 | Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18 | Novel multitarget 5-arylidenehydantoins with arylpiperazinealkyl fragment: Pharmacological evaluation and investigation of cytotoxicity and metabolic stability. |
AID1211294 | Unbound fraction in plasma (unknown origin) at pH 7.4 after 6 hrs by equilibrium dialysis method in presence of 5% CO2 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3 | Control and measurement of plasma pH in equilibrium dialysis: influence on drug plasma protein binding. |
AID468627 | Apparent permeability from apical to basolateral side in human Caco-2 cells | 2009 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20 | Phenylaminopyrimidines as inhibitors of Janus kinases (JAKs). |
AID59158 | Heart rate of the dog was measured after drug administration to dogs | 1980 | Journal of medicinal chemistry, Feb, Volume: 23, Issue:2 | Mono- and diaryl-2-quinuclidinylcarbinols with local anesthetic and antiarrhythmic activity. |
AID636085 | Antiplasmodial activity against Plasmodium falciparum schizonts assessed as change in parasitemia at IC50 concentration treated until all schizonts had burst and invasion was assumed to have occurred by Giemsa staining-based microscopy relative to control | 2012 | Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2 | Synthesis, biological evaluation and mechanistic studies of totarol amino alcohol derivatives as potential antimalarial agents. |
AID1123429 | Competitive antagonist activity at beta-2 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced tracheal relaxation | 1979 | Journal of medicinal chemistry, Feb, Volume: 22, Issue:2 | Synthesis and preliminary biological studies of 4- and 5-[2-hydroxy-3-(isopropylamino)propoxy]benzimidazoles: selective beta2 adrenergic blocking agents. |
AID1211297 | Drug recovery in plasma (unknown origin) | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3 | Control and measurement of plasma pH in equilibrium dialysis: influence on drug plasma protein binding. |
AID1262868 | Chemical stability of compound in 0.1N HCL assessed as compound remaining at 10 mg/ml after 1 day | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
AID21859 | In vivo clearance in rat. | 1999 | Journal of medicinal chemistry, Dec-16, Volume: 42, Issue:25 | Combining in vitro and in vivo pharmacokinetic data for prediction of hepatic drug clearance in humans by artificial neural networks and multivariate statistical techniques. |
AID1211793 | Lipophilicity, log P of the compound | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1 | Comparison of cryopreserved HepaRG cells with cryopreserved human hepatocytes for prediction of clearance for 26 drugs. |
AID540221 | Volume of distribution at steady state in human after iv administration | 2005 | Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7 | Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure. |
AID1393541 | Apparent permeability from apical to basolateral side in human Caco2 cells in absence of P-gp inhibitor by LC-MS/MS analysis | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Effects of rigidity on the selectivity of protein kinase inhibitors. |
AID231957 | Ratio of dissociation constant KD' of rat lung to KD' of rat heart | 1987 | Journal of medicinal chemistry, Apr, Volume: 30, Issue:4 | Beta-adrenoceptor antagonist activity of bivalent ligands. 1. Diamide analogues of practolol. |
AID79647 | The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig | 1980 | Journal of medicinal chemistry, Jun, Volume: 23, Issue:6 | Synthesis and beta-adrenergic blocking activity of new aliphatic oxime ethers. |
AID1602438 | Apparent permeability of the compound after 24 hrs by PAMPA | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5 | Discovery of a Novel Chemotype of Histone Lysine Methyltransferase EHMT1/2 (GLP/G9a) Inhibitors: Rational Design, Synthesis, Biological Evaluation, and Co-crystal Structure. |
AID165815 | Percentage change of IOP in rabbits after 60 min administration (1%) of compound | 1988 | Journal of medicinal chemistry, Jan, Volume: 31, Issue:1 | Improved delivery through biological membranes. 26. Design, synthesis, and pharmacological activity of a novel chemical delivery system for beta-adrenergic blocking agents. |
AID438775 | Apparent permeability from apical to basolateral side of human Caco-2 cells | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20 | Structure mechanism insights and the role of nitric oxide donation guide the development of oxadiazole-2-oxides as therapeutic agents against schistosomiasis. |
AID266009 | Antagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cells | 2006 | Journal of medicinal chemistry, Jun-15, Volume: 49, Issue:12 | Role of Tyr(356(7.43)) and Ser(190(4.57)) in antagonist binding in the rat beta1-adrenergic receptor. |
AID695707 | Apparent permeability across human Caco2 cells at 200 uM by LC/MS analysis | 2012 | Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12 | Synthesis and biological evaluation of an orally active glycosylated endomorphin-1. |
AID1262882 | Antagonist activity at human wild-type A2A receptor expressed in CHO-K1 cells assessed as NECA-induced cAMP by HTRF assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
AID1207023 | Permeability of the compound at pH 6.2 by PAMPA | 2015 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 25, Issue:12 | Novel natural-product-like caged xanthones with improved druglike properties and in vivo antitumor potency. |
AID588213 | Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents | 2010 | Chemical research in toxicology, Jan, Volume: 23, Issue:1 | Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species. |
AID165820 | Percentage change of IOP in rabbits after 8 hr administration (1%) of compound | 1988 | Journal of medicinal chemistry, Jan, Volume: 31, Issue:1 | Improved delivery through biological membranes. 26. Design, synthesis, and pharmacological activity of a novel chemical delivery system for beta-adrenergic blocking agents. |
AID1466759 | Octanol-water partition coefficient, log P of the compound at pH 7.4 after 24 hrs by HPLC method | 2017 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 27, Issue:12 | Drug-like property-driven optimization of 4-substituted 1,5-diarylanilines as potent HIV-1 non-nucleoside reverse transcriptase inhibitors against rilpivirine-resistant mutant virus. |
AID21233 | Partition coefficient of compound in to biological membranes | 1991 | Journal of medicinal chemistry, Mar, Volume: 34, Issue:3 | Reevaluating equilibrium and kinetic binding parameters for lipophilic drugs based on a structural model for drug interaction with biological membranes. |
AID58438 | Percent decrease from initial heart rate (percent delta HR50/HR0 x 100) in dogs | 1983 | Journal of medicinal chemistry, Feb, Volume: 26, Issue:2 | Cardiac-slowing amidines containing the 3-thioindone group. Potential antianginal agents. |
AID1262922 | Log D of compound at pH 7.4 by chromotography | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
AID1123428 | Competitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial contractile force | 1979 | Journal of medicinal chemistry, Feb, Volume: 22, Issue:2 | Synthesis and preliminary biological studies of 4- and 5-[2-hydroxy-3-(isopropylamino)propoxy]benzimidazoles: selective beta2 adrenergic blocking agents. |
AID1079938 | Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source] | |||
AID42197 | Ratio of EC50 of test to control evaluated in guinea pig atria (beta-1) | 1981 | Journal of medicinal chemistry, Oct, Volume: 24, Issue:10 | beta-Adrenergic blocking agents. alpha- and gamma-methyl(aryloxy)propanolamines. |
AID1633503 | Permeability of the compound in pH 7.4 at 250 uM incubated for 24 hrs by UV spectroscopic assay based PAMPA | 2019 | ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4 | Investigation around the Oxadiazole Core in the Discovery of a New Chemotype of Potent and Selective FXR Antagonists. |
AID165835 | Biodistribution pattern of [123I]- ligand was evaluated in liver of anesthetized rabbit after Intravenous injection of 50 uCi after 2 hr | 1996 | Journal of medicinal chemistry, Aug-16, Volume: 39, Issue:17 | Synthesis and in vitro and in vivo characteristics of an iodinated analogue of the beta-adrenoceptor antagonist carazolol. |
AID298032 | Acid dissociation constant, pKa of the compound | 2007 | Journal of medicinal chemistry, Sep-20, Volume: 50, Issue:19 | High-throughput screening of drug-brain tissue binding and in silico prediction for assessment of central nervous system drug delivery. |
AID680283 | TP_TRANSPORTER: increase in Calcein-AM intracellular accumulation (Calcein-AM: 0.5 uM, Propranolol: 500 uM) in MDR1-expressing NIH-3T3 cells | 2004 | Biochemical and biophysical research communications, Mar-19, Volume: 315, Issue:4 | Distinct groups of multidrug resistance modulating agents are distinguished by competition of P-glycoprotein-specific antibodies. |
AID455986 | Permeability across human Caco-2 cells | 2009 | Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19 | Computational modeling of novel inhibitors targeting the Akt pleckstrin homology domain. |
AID1146371 | Inhibition of isoproterenol-induced increase in heart rate in bilaterally vagotomized open chest mongrel dog model at 4.61 mg/kg, iv administered 10 to 20 mins prior to and following isoproterenol challenge | 1978 | Journal of medicinal chemistry, Jan, Volume: 21, Issue:1 | Synthesis of heteroaromatic potential beta-adrenergic antagonists by the glycidol route. |
AID1137402 | In vivo beta-adrenergic receptor blockade in iv dosed anesthetized dog assessed as inhibition of isoproterenol-induced hypotension | 1979 | Journal of medicinal chemistry, Nov, Volume: 22, Issue:11 | Symbiotic approach to drug design: antihypertensive beta-adrenergic blocking agents. |
AID1322295 | Displacement of [3H]CGP-12177 from beta1 adrenergic receptor in rat brain cerebral cortex after 60 mins by microbeta scintillation counting method | |||
AID1449628 | Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12 | Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification. |
AID1810694 | Antiproliferation activity against human T98G cells measured after 72 hrs by crystal violet staining based assay | 2021 | Journal of medicinal chemistry, 06-24, Volume: 64, Issue:12 | Propranolol Activates the Orphan Nuclear Receptor TLX to Counteract Proliferation and Migration of Glioblastoma Cells. |
AID730927 | Permeability of the compound at pH 7.4 by PAMPA | 2013 | Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1 | Garcinia xanthones as orally active antitumor agents. |
AID1262912 | Agonist activity at human wild-type CCKA receptor expressed in CHO-K1 cells assessed as calcium level by FDSS assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
AID1135368 | In vivo inhibition of beta-adrenoceptor in cat assessed as inhibition of isoproterenol-induced hypotension at 0.1 mg/kg, iv relative to control | 1977 | Journal of medicinal chemistry, Jul, Volume: 20, Issue:7 | beta-Adrenoceptor blocking activity of halogenated thienylethanolamine derivatives. |
AID7625 | In vitro metabolic potential in mouse liver microsomes | 2003 | Bioorganic & medicinal chemistry letters, Apr-17, Volume: 13, Issue:8 | Oxyguanidines: application to non-peptidic phenyl-based thrombin inhibitors. |
AID1406275 | Effective permeability of the compound at 50 uM after 16 hrs by PAMPA | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Multi-target-directed ligands for treating Alzheimer's disease: Butyrylcholinesterase inhibitors displaying antioxidant and neuroprotective activities. |
AID1061256 | Displacement of [3H]-CGP-12177 from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1 | Comparative molecular field analysis of fenoterol derivatives interacting with an agonist-stabilized form of the β₂-adrenergic receptor. |
AID444057 | Fraction escaping hepatic elimination in human | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination. |
AID41607 | Inhibitory concentration required for displacement of Beta adrenergic receptor specific ligand [3H]dihydroalprenolol from rat brain cerebral cortical membranes | 1982 | Journal of medicinal chemistry, Jun, Volume: 25, Issue:6 | Syntheses and adrenergic agonist properties of ring-fluorinated isoproterenols. |
AID1262870 | Chemical stability of compound in 0.1N NaOH assessed as compound remaining at 10 mg/ml after 1 day | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
AID171501 | Blood pressure of the urethane-anesthetized normotensive Wistar rat was tested 15 min after inducing the compound on dose of 1.0 mg/kg | 1994 | Journal of medicinal chemistry, Apr-01, Volume: 37, Issue:7 | Guaiacoxypropanolamine derivatives of capsaicin: a new family of beta-adrenoceptor blockers with intrinsic cardiotonic properties. |
AID21849 | In vitro clearance in dog in 1000000 cells | 1999 | Journal of medicinal chemistry, Dec-16, Volume: 42, Issue:25 | Combining in vitro and in vivo pharmacokinetic data for prediction of hepatic drug clearance in humans by artificial neural networks and multivariate statistical techniques. |
AID1217707 | Time dependent inhibition of CYP2C19 in human liver microsomes at 100 uM by LC/MS system | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
AID187178 | Inhibition constant of compound on R-(+)-125[I]-8 radioligand binding to rat striatal membranes | 1991 | Journal of medicinal chemistry, Mar, Volume: 34, Issue:3 | Synthesis and resolution of (+-)-7-chloro-8-hydroxy-1-(3'-iodophenyl)-3-methyl-2,3,4,5-tetrahydro- 1H-3- benzazepine (TISCH): a high affinity and selective iodinated ligand for CNS D1 dopamine receptor. |
AID624624 | Apparent permeability (Papp) from apical to basolateral side determined in MDR1-MDCKII cells in the presence of inhibitor (2uM GF120919) | 2001 | The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2 | Rational use of in vitro P-glycoprotein assays in drug discovery. |
AID1585793 | Apparent permeability across basolateral to apical side in human Caco2 cells at 2 uM after 2 hrs by lucifer yellow dye-based LC-MS/MS analysis | 2018 | Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24 | Design, Synthesis, and Biological Evaluation of 2-Nitroimidazopyrazin-one/-es with Antitubercular and Antiparasitic Activity. |
AID168612 | Compound was tested for oral salidiuretic activity (control/drug treatment value) in rats expressed as urinary output. at a dose of 128 mg/kg; 9.05/12.83 | 1986 | Journal of medicinal chemistry, Jan, Volume: 29, Issue:1 | [p-[(Thienylcarbonyl)amino]phenoxy]propanolamines derivatives as diuretic and beta-adrenergic receptor blocking agents. |
AID1212314 | Drug uptake in lysosomes of human Fa2N-4 cells assessed as inhibition of LysoTracker Red fluorescence after 30 mins | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4 | Lysosomal sequestration (trapping) of lipophilic amine (cationic amphiphilic) drugs in immortalized human hepatocytes (Fa2N-4 cells). |
AID1772562 | n-Octanol/PBS buffer distribution coefficient, logD of the compound at pH 7.4 | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Non-carboxylic acid inhibitors of aldose reductase based on N-substituted thiazolidinedione derivatives. |
AID1415056 | Aqueous solubility of the compound in PBS buffer at pH 7.4 after 2 hrs | 2018 | Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23 | Application of Sequential Palladium Catalysis for the Discovery of Janus Kinase Inhibitors in the Benzo[ c]pyrrolo[2,3- h][1,6]naphthyridin-5-one (BPN) Series. |
AID694016 | Permeability across MDCK2-MDR1 cells expressing MDR1 at 3 uM in presence of 2 uM P-gp inhibitor Elacridal by mass spectroscopy | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14 | Urea-based inhibitors of Trypanosoma brucei methionyl-tRNA synthetase: selectivity and in vivo characterization. |
AID1513922 | Efflux ratio of apparent permeability in human Caco2 cells at 10 uM after 120 mins by LC-MS/MS analysis | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 | Alkyl-guanidine Compounds as Potent Broad-Spectrum Antibacterial Agents: Chemical Library Extension and Biological Characterization. |
AID1382491 | Apparent permeability from apical to basolateral side in human Caco2 cells at 10 uM after 60 mins by LC-MS/MS analysis | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Alkynyl-containing phenylthiazoles: Systemically active antibacterial agents effective against methicillin-resistant Staphylococcus aureus (MRSA). |
AID166291 | Effect on IOP of rabbits 0 min after administration (1%) | 1988 | Journal of medicinal chemistry, Jan, Volume: 31, Issue:1 | Improved delivery through biological membranes. 26. Design, synthesis, and pharmacological activity of a novel chemical delivery system for beta-adrenergic blocking agents. |
AID40718 | Antagonist activity of compound against Beta-2 adrenergic receptor in isolated guinea pig trachea | 1981 | Journal of medicinal chemistry, Aug, Volume: 24, Issue:8 | 2-Benzodioxinylaminoethanols: a new class of beta-adrenergic blocking and antihypertensive agents. |
AID1429805 | Apparent permeability of the compound at 10 mM at pH 4 after 4 hrs by PAMPA | 2017 | Journal of medicinal chemistry, 02-23, Volume: 60, Issue:4 | Antimalarial Pyrido[1,2-a]benzimidazoles: Lead Optimization, Parasite Life Cycle Stage Profile, Mechanistic Evaluation, Killing Kinetics, and in Vivo Oral Efficacy in a Mouse Model. |
AID1211296 | Unbound fraction in plasma (unknown origin) under normal atmospheric condition at pH 7.72 after 6 hrs by equilibrium dialysis method | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3 | Control and measurement of plasma pH in equilibrium dialysis: influence on drug plasma protein binding. |
AID60485 | Relative adrenoceptor blocking activity (DR10) was recorded for the antagonism of Isoproterenol-induced responses in Positive chronotropy in beta1-Adrenoceptor blockade | 1982 | Journal of medicinal chemistry, Jun, Volume: 25, Issue:6 | Arylethanolamines derived from salicylamide with alpha- and beta-adrenoceptor blocking activities. Preparation of labetalol, its enantiomers, and related salicylamides. |
AID1529186 | Binding affinity to human serum albumin assessed as change in dissociation constant pKa1 of compound in aqueous medium to presence of human serum albumin by UV-pH titration based spectrophotometric analysis | 2020 | Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4 | Human Serum Albumin Binding in a Vial: A Novel UV-pH Titration Method To Assist Drug Design. |
AID1911470 | Apparent permeability across apical to basolateral side in human Caco-2 cells | 2022 | Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11 | Design, Synthesis, and Biological Evaluations of DOT1L Peptide Mimetics Targeting the Protein-Protein Interactions between DOT1L and MLL-AF9/MLL-ENL. |
AID28235 | Unbound fraction (plasma) | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13 | Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data. |
AID40404 | Apparent dissociation constant towards beta-1 adrenergic receptor in rat heart membranes using (2-6)x10E-9M of [3AH]-DHA in the presence or absence of 10e-5 M (+/-) propranolol. | 1987 | Journal of medicinal chemistry, Apr, Volume: 30, Issue:4 | Beta-adrenoceptor antagonist activity of bivalent ligands. 1. Diamide analogues of practolol. |
AID1320616 | Permeability of the compound after 4 hrs by PAMPA | 2016 | Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22 | Structure-based design of ester compounds to inhibit MLL complex catalytic activity by targeting mixed lineage leukemia 1 (MLL1)-WDR5 interaction. |
AID1668033 | Antiproliferative activity against human SK-MEL-5 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay | 2020 | Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9 | Drug repurposing and rediscovery: Design, synthesis and preliminary biological evaluation of 1-arylamino-3-aryloxypropan-2-ols as anti-melanoma agents. |
AID1262938 | Fraction unbound in rat plasma at 5 uM after 4.5 hrs by LC-MS/MS analysis | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
AID737835 | Antiangiogenic activity in human HMEC1 cells at 10 uM after 8 hrs by matrigel assay | 2013 | Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7 | Synthesis of novel isoflavene-propranolol hybrids as anti-tumor agents. |
AID288184 | Permeability coefficient through artificial membrane in presence of unstirred water layer by PAMPA | 2007 | Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11 | QSAR study on permeability of hydrophobic compounds with artificial membranes. |
AID193033 | Antihypertensive activity as percent maximum (0-6 hr) decrease in blood pressure at 135 umol/kg po (~40-50 mg/kg) in 5 spontaneously hypertensive rats (SHR); NA denotes no data | 1987 | Journal of medicinal chemistry, Apr, Volume: 30, Issue:4 | Substituted 1,2,3,4-tetrahydroaminonaphthols: antihypertensive agents, calcium channel blockers, and adrenergic receptor blockers with catecholamine-depleting effects. |
AID20062 | Compound was evaluated for pKa by titration of the compounds in 1:2 methyl alcohol and water. | 1986 | Journal of medicinal chemistry, Nov, Volume: 29, Issue:11 | 6,7-Dichloro-1-(3,4,5-trimethoxybenzyl)-1,2,3,4-tetrahydroisoquinoline . A structurally novel beta-adrenergic receptor blocking agent. |
AID1262877 | Antagonist activity at human 5-HT2A receptor expressed in CHO-K1 cells assessed as seretonin-induced calcium level by FDSS assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
AID166310 | Effect on IOP of rabbits 8 hr min after administration (1%) | 1988 | Journal of medicinal chemistry, Jan, Volume: 31, Issue:1 | Improved delivery through biological membranes. 26. Design, synthesis, and pharmacological activity of a novel chemical delivery system for beta-adrenergic blocking agents. |
AID737838 | Selectivity ratio of GI50 for human MRC5 cells to GI50 for human HMEC1 cells | 2013 | Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7 | Synthesis of novel isoflavene-propranolol hybrids as anti-tumor agents. |
AID1212318 | Drug uptake in lysosomes of human Fa2N-4 cells assessed as cellular partitioning at 1 uM up to 10 mins by LC-MS analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4 | Lysosomal sequestration (trapping) of lipophilic amine (cationic amphiphilic) drugs in immortalized human hepatocytes (Fa2N-4 cells). |
AID496826 | Antimicrobial activity against Entamoeba histolytica | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID181812 | Percentage of fall in systolic blood pressure (SBP) at the following hours after dosing at 75 mg/kg (po) at 24 hr in spontaneously hypertensive rats(SHR); NS means not significant | 1987 | Journal of medicinal chemistry, May, Volume: 30, Issue:5 | Flavones. 1. Synthesis and antihypertensive activity of (3-phenylflavonoxy)propanolamines without beta-adrenoceptor antagonism. |
AID1245599 | Efflux ratio of apparent permeability across basolateral to apical side over apical to basolateral side in human Caco2 cells after 2 hrs | 2015 | Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19 | Discovery of potent nitrotriazole-based antitrypanosomal agents: In vitro and in vivo evaluation. |
AID1262943 | Cmax in Swiss mouse brain at 5 mg/kg, sc | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
AID41482 | Compound was evaluated for competitive antagonism of beta-2 adrenergic receptor in rat uterus measured as pA2 (-log KB) | 1984 | Journal of medicinal chemistry, Jul, Volume: 27, Issue:7 | The 3,4-catechol derivative of propranolol, a minor dihydroxylated metabolite. |
AID744914 | Antihypertensive activity in rat spontaneous hypertensive model assessed as diastolic arterial blood pressure at 20 mg/kg, po measured at 0.5 hrs by tail-cuff method (Rvb = 138.7 +/- 9.2 mmHg) | 2013 | Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9 | Novel hybrids of natural isochroman-4-one bearing N-substituted isopropanolamine as potential antihypertensive candidates. |
AID1393790 | Apparent permeability from basolateral to apical side in human Caco2 cells in presence of P-gp inhibitor by LC-MS/MS analysis | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Effects of rigidity on the selectivity of protein kinase inhibitors. |
AID625285 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID1533478 | Apparent permeability from basolateral to apical side in MDCK cells | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Second generation of diazachrysenes: Protection of Ebola virus infected mice and mechanism of action. |
AID1676993 | Apparent permeability across basolateral to apical side in human Caco-2 cells | |||
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AID168827 | Compound was tested for oral salidiuretic activity (control/drug treatment value) in rats expressed in Na+, mequiv/6 hr at a dose of 64 mg/kg; 0.216/0.097 | 1986 | Journal of medicinal chemistry, Jan, Volume: 29, Issue:1 | [p-[(Thienylcarbonyl)amino]phenoxy]propanolamines derivatives as diuretic and beta-adrenergic receptor blocking agents. |
AID540219 | Volume of distribution at steady state in monkey after iv administration | 2005 | Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7 | Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure. |
AID1382495 | Half life in human liver microsomes at 0.1 uM preincubated for 5 mins followed by NDAPH addition measured up to 60 mins by HPLC-MS/MS analysis | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Alkynyl-containing phenylthiazoles: Systemically active antibacterial agents effective against methicillin-resistant Staphylococcus aureus (MRSA). |
AID165863 | Biodistribution pattern of [123I]- ligand was evaluated in right ventricular muscle of anesthetized rabbit after Intravenous injection of 50 uCi after 2 hr | 1996 | Journal of medicinal chemistry, Aug-16, Volume: 39, Issue:17 | Synthesis and in vitro and in vivo characteristics of an iodinated analogue of the beta-adrenoceptor antagonist carazolol. |
AID79518 | Positive chronotropic effect was evaluated on atrial muscles of the guinea pig | 1994 | Journal of medicinal chemistry, Apr-01, Volume: 37, Issue:7 | Guaiacoxypropanolamine derivatives of capsaicin: a new family of beta-adrenoceptor blockers with intrinsic cardiotonic properties. |
AID1203210 | Apparent permeability across basolateral to apical side in human Caco2 cells in presence of 0.1% bovine serum albumin | 2015 | Journal of medicinal chemistry, Apr-09, Volume: 58, Issue:7 | Discovery and optimization of novel antagonists to the human neurokinin-3 receptor for the treatment of sex-hormone disorders (Part I). |
AID1146369 | Inhibition of isoproterenol-induced increase in heart rate in bilaterally vagotomized open chest mongrel dog model at 0.45 mg/kg, iv administered 10 to 20 mins prior to and following isoproterenol challenge | 1978 | Journal of medicinal chemistry, Jan, Volume: 21, Issue:1 | Synthesis of heteroaromatic potential beta-adrenergic antagonists by the glycidol route. |
AID1211293 | Unbound fraction in plasma (unknown origin) under normal atmospheric condition at pH 7.22 after 6 hrs by equilibrium dialysis method | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3 | Control and measurement of plasma pH in equilibrium dialysis: influence on drug plasma protein binding. |
AID1207691 | Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in human embryonic kidney cells heterologically expressing alpha-1C subunit | 2012 | Journal of applied toxicology : JAT, Oct, Volume: 32, Issue:10 | Predictive model for L-type channel inhibition: multichannel block in QT prolongation risk assessment. |
AID62242 | Evaluated for the heart rate at dose 5.0 mg/kg in 4 animals by aminophylline-induced sinus tachycardia test | 1983 | Journal of medicinal chemistry, Feb, Volume: 26, Issue:2 | Cardiac-slowing amidines containing the 3-thioindone group. Potential antianginal agents. |
AID588209 | Literature-mined public compounds from Greene et al multi-species hepatotoxicity modelling dataset | 2010 | Chemical research in toxicology, Jul-19, Volume: 23, Issue:7 | Developing structure-activity relationships for the prediction of hepatotoxicity. |
AID658932 | Apparent permeability from apical to basolateral side of human Caco2 cells at 100 uM up to 90 mins | 2012 | European journal of medicinal chemistry, Jun, Volume: 52 | Exploring the interplay of physicochemical properties, membrane permeability and giardicidal activity of some benzimidazole derivatives. |
AID744904 | Antihypertensive activity in rat spontaneous hypertensive model assessed as diastolic arterial blood pressure at 20 mg/kg, po measured at 8 hrs by tail-cuff method (Rvb = 135.3 +/- 8.21 mmHg) | 2013 | Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9 | Novel hybrids of natural isochroman-4-one bearing N-substituted isopropanolamine as potential antihypertensive candidates. |
AID41151 | Apparent pA2 value for blockade of isoproterenol-induced increase in heart rate evaluated against beta adrenergic receptor in anesthetized dogs | 1985 | Journal of medicinal chemistry, Jun, Volume: 28, Issue:6 | Synthesis of 4'-hydroxypropranolol sulfate, a major non-beta-blocking propranolol metabolite in man. |
AID343619 | Apparent permeability across human Caco-2 cells | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14 | Structure-based design, synthesis, and biological evaluation of 1,1-dioxoisothiazole and benzo[b]thiophene-1,1-dioxide derivatives as novel inhibitors of hepatitis C virus NS5B polymerase. |
AID25356 | Compound was evaluated for pKa value by potentiometric titration | 1984 | Journal of medicinal chemistry, Oct, Volume: 27, Issue:10 | Synthesis and beta-adrenergic blocking activity of new aliphatic and alicyclic oxime ethers. |
AID47781 | Duration of hypotensive activity in cat following i.v. administration of 1 mg/kg | 2004 | Bioorganic & medicinal chemistry letters, Jun-07, Volume: 14, Issue:11 | 1- and 2-substituted naphthalenes: a new class of potential hypotensive agents. |
AID373867 | Hepatic clearance in human hepatocytes in absence of fetal calf serum | 2009 | European journal of medicinal chemistry, Apr, Volume: 44, Issue:4 | First-principle, structure-based prediction of hepatic metabolic clearance values in human. |
AID1602439 | Apparent permeability of the compound after 24 hrs by BBB-PAMPA | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5 | Discovery of a Novel Chemotype of Histone Lysine Methyltransferase EHMT1/2 (GLP/G9a) Inhibitors: Rational Design, Synthesis, Biological Evaluation, and Co-crystal Structure. |
AID1091956 | Apparent hydrophobicity, log D of the compound in Octanol-buffer | 2011 | Journal of agricultural and food chemistry, Apr-13, Volume: 59, Issue:7 | Importance of physicochemical properties for the design of new pesticides. |
AID184270 | The compound was tested for percent increase in heart rate with respect to that measured after isoprenaline in 5-10 animals. | 1998 | Journal of medicinal chemistry, May-07, Volume: 41, Issue:10 | Synthesis and adrenergic activity of a new series of N-aryl dicyclopropyl ketone oxime ethers: SAR and stereochemical aspects. |
AID1733543 | Apparent permeability across apical to basolateral side in human Caco2 cells at 20 uM after 2 hrs by LC-MS analysis | 2021 | Bioorganic & medicinal chemistry, 05-01, Volume: 37 | Systematic evaluation of structure-property relationships and pharmacokinetics in 6-(hetero)aryl-substituted matched pair analogs of amiloride and 5-(N,N-hexamethylene)amiloride. |
AID165810 | Percentage change of IOP in rabbits after 4 hr administration (1%) of compound | 1988 | Journal of medicinal chemistry, Jan, Volume: 31, Issue:1 | Improved delivery through biological membranes. 26. Design, synthesis, and pharmacological activity of a novel chemical delivery system for beta-adrenergic blocking agents. |
AID1136326 | Antagonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of isoproterenol-induced response after 20 mins | 1978 | Journal of medicinal chemistry, Oct, Volume: 21, Issue:10 | 2-Methoxyphenylethanolamines, potential beta-adrenergic blocking agents. |
AID1262901 | Agonist activity at human 5-HT2B receptor expressed in CHO-K1 cells assessed as calcium level by FDSS assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
AID47972 | In vivo beta adrenergic blocking potency was determined by inhibition of tachycardia produced by isoproterenol (0.2 mg/kg iv) in cat preparation | 1982 | Journal of medicinal chemistry, Nov, Volume: 25, Issue:11 | Beta-adrenergic blocking agents. 22. 1-Phenoxy-3-[[(substituted-amido) alkyl]amino]-2-propanols. |
AID361981 | Membrane permeability by PAMPA in presence of 20% 1-propanol | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16 | Toward an optimal blood-brain barrier shuttle by synthesis and evaluation of peptide libraries. |
AID1079949 | Proposed mechanism(s) of liver damage. [column 'MEC' in source] | |||
AID620386 | Displacement of [3H]-CGP 12177 from human beta-1 adrenergic receptor expressed in CHOK1 cells | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19 | Synthesis and characterization of high-affinity 4,4-difluoro-4-bora-3a,4a-diaza-s-indacene-labeled fluorescent ligands for human β-adrenoceptors. |
AID1146373 | Inhibition of isoproterenol-induced decrease in diastolic blood pressure in bilaterally vagotomized open chest mongrel dog model at 0.13 mg/kg, iv administered 10 to 20 mins prior to and following isoproterenol challenge | 1978 | Journal of medicinal chemistry, Jan, Volume: 21, Issue:1 | Synthesis of heteroaromatic potential beta-adrenergic antagonists by the glycidol route. |
AID41348 | Beta-2 adrenergic receptor blockade measured as inhibition of depressor response caused by isoprenaline in anesthetized rats when administered intravenously | 1983 | Journal of medicinal chemistry, Nov, Volume: 26, Issue:11 | beta 1-selective adrenoceptor antagonists. 1. Synthesis and beta-adrenergic blocking activity of a series of binary (aryloxy)propanolamines. |
AID1900032 | Apparent permeability across basolateral to apical side in human Caco-2 cells assessed as drug recovery at 10 uM measured after 2 hrs by LC-MS/MS analysis | 2022 | Journal of medicinal chemistry, 01-13, Volume: 65, Issue:1 | Design, Synthesis, and Biological Evaluation of 1-(Indolizin-3-yl)ethan-1-ones as CBP Bromodomain Inhibitors for the Treatment of Prostate Cancer. |
AID190411 | Antihypertensive activity expressed as percentage of base-line systolic blood pressure of base-line values in spontaneously hypertensive rats (SHR) was reported after 2 hr | 1987 | Journal of medicinal chemistry, Jun, Volume: 30, Issue:6 | Synthesis of a series of compounds related to betaxolol, a new beta 1-adrenoceptor antagonist with a pharmacological and pharmacokinetic profile optimized for the treatment of chronic cardiovascular diseases. |
AID1262865 | Antagonist activity at human beta1 receptor expressed in CHO-K1 cells assessed as isoproterenol-induced cAMP level by HTRF assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
AID16351 | Percent diffusion through fuzzy rat skin after 48 h of incubation | 1988 | Journal of medicinal chemistry, Feb, Volume: 31, Issue:2 | (Acyloxy)alkyl carbamates as novel bioreversible prodrugs for amines: increased permeation through biological membranes. |
AID1215126 | Ratio of fraction unbound in Wistar rat brain homogenate at 5 uM after 5 hrs by equilibrium dialysis method to fraction unbound in solid supported porcine brain membrane vesicles at 5 uM by TRANSIL assay | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Brain tissue binding of drugs: evaluation and validation of solid supported porcine brain membrane vesicles (TRANSIL) as a novel high-throughput method. |
AID744888 | Toxicity in rat spontaneous hypertensive model assessed as heart rate at 20 mg/kg, po measured at 1 hr by tail-cuff method (Rvb = 403.9 +/- 12.41 bpm) | 2013 | Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9 | Novel hybrids of natural isochroman-4-one bearing N-substituted isopropanolamine as potential antihypertensive candidates. |
AID193030 | Antihypertensive activity as percent average (over 24 hr) decrease in blood pressure at 135 umol/kg po (~40-50 mg/kg) in 5 spontaneously hypertensive rats (SHR); NA denotes no data | 1987 | Journal of medicinal chemistry, Apr, Volume: 30, Issue:4 | Substituted 1,2,3,4-tetrahydroaminonaphthols: antihypertensive agents, calcium channel blockers, and adrenergic receptor blockers with catecholamine-depleting effects. |
AID236917 | Apparent permeability of the compound was determined inCaco-2 (human colon carcinoma) cells; Activity = Papp 10E-6 | 2005 | Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3 | In silico prediction of membrane permeability from calculated molecular parameters. |
AID1217710 | Covalent binding in human liver microsomes measured per mg of protein using radiolabelled compound at 10 uM after 1 hr incubation by liquid scintillation counting | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
AID1137384 | Antihypertensive activity in spontaneously hypertensive Wistar-Okamoto rat assessed as duration of action at 5 mg/kg, po | 1979 | Journal of medicinal chemistry, Nov, Volume: 22, Issue:11 | Symbiotic approach to drug design: antihypertensive beta-adrenergic blocking agents. |
AID699540 | Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake at 20 uM incubated for 5 mins by scintillation counting | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10 | Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions. |
AID610065 | Apparent permeability from basolateral to apical side of human Caco2 cells at 10 uM by LC/MS/MS analysis | 2011 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16 | Effects of C7 substitutions in a high affinity microtubule-binding taxane on antitumor activity and drug transport. |
AID41752 | Inhibition constant from beta adrenergic receptor binding assay | 1989 | Journal of medicinal chemistry, Jan, Volume: 32, Issue:1 | Flavones. 2. Synthesis and structure-activity relationship of flavodilol and its analogues, a novel class of antihypertensive agents with catecholamine depleting properties. |
AID1262925 | Intrinsic clearance in mouse liver microsomes at 1 uM by HPLC/MS/MS analysis | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
AID1510597 | Permeability of the compound in PBS at 100 uM incubated for 16 hrs by artificial membrane permeability assay based UPLS-MS analysis | 2019 | ACS medicinal chemistry letters, Jun-13, Volume: 10, Issue:6 | Computer-Aided Selective Optimization of Side Activities of Talinolol. |
AID288194 | Intrinsic artificial membrane permeability coefficient, log P0 of the compound | 2007 | Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11 | QSAR study on permeability of hydrophobic compounds with artificial membranes. |
AID1262895 | Antagonist activity at human wild-type ETA receptor expressed in CHO-K1 cells assessed as endothelin-1-induced calcium by HTRF assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
AID1810691 | Effect on TLX regulated gene expression in human T98G cells assessed as decrease in TET3 mRNA expression at 50 uM after 8 hrs by qRT-PCR analysis | 2021 | Journal of medicinal chemistry, 06-24, Volume: 64, Issue:12 | Propranolol Activates the Orphan Nuclear Receptor TLX to Counteract Proliferation and Migration of Glioblastoma Cells. |
AID737841 | Antiproliferative activity against human MDA-MB-231 cells by measuring metabolic activity of cells after 72 hrs by spectrophotometric analysis | 2013 | Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7 | Synthesis of novel isoflavene-propranolol hybrids as anti-tumor agents. |
AID288185 | Permeability coefficient through artificial membrane in presence of stirred water layer | 2007 | Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11 | QSAR study on permeability of hydrophobic compounds with artificial membranes. |
AID1079935 | Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source] | |||
AID361986 | Lipophilicity, log D of compound at pH 7.4 by shake flask method | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16 | Determination of log D via automated microfluidic liquid-liquid extraction. |
AID1302020 | Passive permeability of compound assessed as drug transport at 500 uM after 4 hrs by BBB-PAMPA | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8 | Bifunctional Peptide-Based Opioid Agonist-Nociceptin Antagonist Ligands for Dual Treatment of Acute and Neuropathic Pain. |
AID1585796 | Efflux ratio of apparent permeability in human Caco2 cells at 2 uM after 2 hrs by lucifer yellow dye-based LC-MS/MS analysis | 2018 | Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24 | Design, Synthesis, and Biological Evaluation of 2-Nitroimidazopyrazin-one/-es with Antitubercular and Antiparasitic Activity. |
AID4036 | Binding affinity towards 5-hydroxytryptamine 1A receptor by the displacement of [125I]trans-8-OH-PIPAT in membrane homogenates of hippocampal tissue of rat brain | 1993 | Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21 | Synthesis of (R,S)-trans-8-hydroxy-2-[N-n-propyl-N-(3'-iodo-2'-propenyl)amino]tetral in (trans-8-OH-PIPAT): a new 5-HT1A receptor ligand. |
AID1510595 | Inhibition of recombinant human full length soluble epoxide hydrolase (1 to 555 residues) expressed in Escherichia coli BL21(DE3) using non-fluorescent PHOME as substrate preincubated for 30 mins followed by substrate addition and measured after 30 mins b | 2019 | ACS medicinal chemistry letters, Jun-13, Volume: 10, Issue:6 | Computer-Aided Selective Optimization of Side Activities of Talinolol. |
AID1135366 | In vivo inhibition of beta-adrenoceptor in cat assessed as inhibition of isoproterenol-induced tachycardia at 0.1 mg/kg, iv relative to control | 1977 | Journal of medicinal chemistry, Jul, Volume: 20, Issue:7 | beta-Adrenoceptor blocking activity of halogenated thienylethanolamine derivatives. |
AID1123427 | Competitive antagonist activity at beta-1 adrenergic receptor in guinea pig assessed as inhibition of isoproterenol-induced atrial beat rate | 1979 | Journal of medicinal chemistry, Feb, Volume: 22, Issue:2 | Synthesis and preliminary biological studies of 4- and 5-[2-hydroxy-3-(isopropylamino)propoxy]benzimidazoles: selective beta2 adrenergic blocking agents. |
AID1209583 | Unbound drug partitioning coefficient, Kp of the compound assessed as ratio of unbound concentration in Sprague-Dawley rat brain to unbound concentration in plasma | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3 | Measurement of unbound drug exposure in brain: modeling of pH partitioning explains diverging results between the brain slice and brain homogenate methods. |
AID59159 | Heart rate of the dog was measured after ouabain administration to dogs | 1980 | Journal of medicinal chemistry, Feb, Volume: 23, Issue:2 | Mono- and diaryl-2-quinuclidinylcarbinols with local anesthetic and antiarrhythmic activity. |
AID166308 | Effect on IOP of rabbits 6 hr min after administration (2.5%) | 1988 | Journal of medicinal chemistry, Jan, Volume: 31, Issue:1 | Improved delivery through biological membranes. 26. Design, synthesis, and pharmacological activity of a novel chemical delivery system for beta-adrenergic blocking agents. |
AID1262936 | Fraction unbound in human plasma at 5 uM after 4.5 hrs by LC-MS/MS analysis | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
AID40867 | Beta-2 adrenergic receptor blocking activity in trachea of guinea pig. | 1984 | Journal of medicinal chemistry, Oct, Volume: 27, Issue:10 | Synthesis and beta-adrenergic blocking activity of new aliphatic and alicyclic oxime ethers. |
AID679346 | TP_TRANSPORTER: transepithelial transport in Caco2 cells | 2004 | Journal of controlled release : official journal of the Controlled Release Society, Mar-24, Volume: 95, Issue:3 | The use of a dendrimer-propranolol prodrug to bypass efflux transporters and enhance oral bioavailability. |
AID79325 | Antagonism of the isoprenaline-induced positive chronotropic effect on the atria of guinea pig | 1980 | Journal of medicinal chemistry, Jun, Volume: 23, Issue:6 | Synthesis and beta-adrenergic blocking activity of new aliphatic oxime ethers. |
AID1407669 | Apparent permeability of the compound from basolateral to apical side in human Caco2 cells after 120 mins by LC-MS/MS analysis | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Hedgehog pathway inhibitors of the acylthiourea and acylguanidine class show antitumor activity on colon cancer in vitro and in vivo. |
AID1262897 | Antagonist activity at human wild-type opioid-kappa 1 receptor expressed in CHO-K1 cells assessed as U50488-induced cAMP by HTRF assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
AID42211 | Compound was evaluated for competitive antagonism of beta-1 adrenergic receptor in guinea pig atria measured as pA2 (-log KB) | 1984 | Journal of medicinal chemistry, Jul, Volume: 27, Issue:7 | The 3,4-catechol derivative of propranolol, a minor dihydroxylated metabolite. |
AID327177 | Binding affinity to 100 uM human serum albumin at 10 uM by PAMPA method | 2008 | Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7 | New approach to measure protein binding based on a parallel artificial membrane assay and human serum albumin. |
AID41136 | Tested for Beta Adrenergic receptor binding inhibition from canine ventricular tissue, using [3H]dihydroalprenolol as the radioligand in anesthetized dogs | 1990 | Journal of medicinal chemistry, Oct, Volume: 33, Issue:10 | Synthesis of novel (aryloxy)propanolamines and related compounds possessing both class II and class III antiarrhythmic activity. |
AID1137304 | Negative inotropic activity in New Zealand White rabbit isolated atria assessed as reduction of tissue contractility after 15 mins | 1979 | Journal of medicinal chemistry, Jan, Volume: 22, Issue:1 | Relationship of nonspecific antiarrhythmic and negative inotropic activity with physicochemical parameters of propranolol analogues. |
AID1360443 | Metabolic stability in CD1 mouse liver microsomes at 40 mins by LC-MS method | 2018 | European journal of medicinal chemistry, Jul-15, Volume: 155 | Novel 8-nitroquinolin-2(1H)-ones as NTR-bioactivated antikinetoplastid molecules: Synthesis, electrochemical and SAR study. |
AID620391 | Antagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19 | Synthesis and characterization of high-affinity 4,4-difluoro-4-bora-3a,4a-diaza-s-indacene-labeled fluorescent ligands for human β-adrenoceptors. |
AID60471 | Evaluated for the dose required to achieve 50 % of the maximal cardiac slowing in the triazine tachycardia test. | 1983 | Journal of medicinal chemistry, Feb, Volume: 26, Issue:2 | Cardiac-slowing amidines containing the 3-thioindone group. Potential antianginal agents. |
AID21857 | In vivo clearance in human. | 1999 | Journal of medicinal chemistry, Dec-16, Volume: 42, Issue:25 | Combining in vitro and in vivo pharmacokinetic data for prediction of hepatic drug clearance in humans by artificial neural networks and multivariate statistical techniques. |
AID625288 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID1212317 | Drug uptake in lysosomes of human Fa2N-4 cells assessed as cellular partitioning measured per 10'6 cells at 1 uM after 5 mins by LC-MS analysis in presence of ammonium chloride | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4 | Lysosomal sequestration (trapping) of lipophilic amine (cationic amphiphilic) drugs in immortalized human hepatocytes (Fa2N-4 cells). |
AID718837 | Permeability of the compound by PAMPA | 2012 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23 | Inhibition of monoamine oxidase by derivatives of piperine, an alkaloid from the pepper plant Piper nigrum, for possible use in Parkinson's disease. |
AID174418 | Change in systolic blood pressure after 100 mg/kg oral administration in spontaneous hypertensive rats after 4 hr | 1981 | Journal of medicinal chemistry, Dec, Volume: 24, Issue:12 | Antihypertensive pyrrolo[1,2-c]quinazolines and pyrrolo[1,2-c]quinazolinones. |
AID266006 | Antagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cells | 2006 | Journal of medicinal chemistry, Jun-15, Volume: 49, Issue:12 | Role of Tyr(356(7.43)) and Ser(190(4.57)) in antagonist binding in the rat beta1-adrenergic receptor. |
AID624623 | Apparent permeability (Papp) from basolateral to apical side determined in MDR1-MDCKII cells | 2001 | The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2 | Rational use of in vitro P-glycoprotein assays in drug discovery. |
AID28924 | Effective permeability (Pe) across a hexadecane membrane (pH 6.8) | 2001 | Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6 | High-throughput permeability pH profile and high-throughput alkane/water log P with artificial membranes. |
AID1669463 | Antagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under constant violet light conditions by FRET assay | 2020 | Journal of medicinal chemistry, 08-13, Volume: 63, Issue:15 | Photoswitchable Antagonists for a Precise Spatiotemporal Control of β |
AID40870 | In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea | 1986 | Journal of medicinal chemistry, Jun, Volume: 29, Issue:6 | Beta 1-selective adrenoceptor antagonists: examples of the 2-[4-[3-(substituted amino)-2-hydroxypropoxy]phenyl]imidazole class. 2. |
AID29139 | Calculated dissociation constant (pKa, calculated with ACD/pKa) | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26 | Pharmacophore model of drugs involved in P-glycoprotein multidrug resistance: explanation of structural variety (hypothesis). |
AID1545656 | Half-life in CD1 mouse liver microsomes by HPLC analysis | 2019 | Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18 | Novel multitarget 5-arylidenehydantoins with arylpiperazinealkyl fragment: Pharmacological evaluation and investigation of cytotoxicity and metabolic stability. |
AID1079932 | Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source] | |||
AID1603577 | Selectivity index, ratio of Ki for displacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranes to Ki for displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranes | |||
AID368076 | Displacement of [3H]CGP12177 from beta-1 adrenergic receptor in rat cerebral cortex by liquid scintillation counting | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3 | Preliminary evaluation of pharmacological properties of some xanthone derivatives. |
AID1079942 | Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source] | |||
AID1365714 | Apparent permeability of the compound across apical side to basolateral side in human Caco2 cells monolayer at 10 uM after 2 hrs by LC-MS/MS analysis | 2017 | Bioorganic & medicinal chemistry, 11-01, Volume: 25, Issue:21 | The antitubercular activity of various nitro(triazole/imidazole)-based compounds. |
AID1262879 | Antagonist activity at human 5-HT2C receptor expressed in CHO-K1 cells assessed as seretonin-induced calcium level by FDSS assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
AID481440 | Dissociation constant, pKa of the compound | 2010 | Journal of medicinal chemistry, May-13, Volume: 53, Issue:9 | How well can the Caco-2/Madin-Darby canine kidney models predict effective human jejunal permeability? |
AID636078 | Cytotoxicity against CHO cells after 48 hrs by MTT assay | 2012 | Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2 | Synthesis, biological evaluation and mechanistic studies of totarol amino alcohol derivatives as potential antimalarial agents. |
AID1883092 | Apparent permeability of the compound in phosphate buffer at pH 7.4 measured after 24 hrs by PAMPA assay | 2022 | Journal of medicinal chemistry, 09-08, Volume: 65, Issue:17 | Turning Nonselective Inhibitors of Type I Protein Arginine Methyltransferases into Potent and Selective Inhibitors of Protein Arginine Methyltransferase 4 through a Deconstruction-Reconstruction and Fragment-Growing Approach. |
AID165964 | Concentration in iris-ciliary body of rabbit after 30 min administration of compound | 1988 | Journal of medicinal chemistry, Jan, Volume: 31, Issue:1 | Improved delivery through biological membranes. 26. Design, synthesis, and pharmacological activity of a novel chemical delivery system for beta-adrenergic blocking agents. |
AID47782 | Duration of hypotensive activity in cat following i.v. administration of 5 mg/kg | 2004 | Bioorganic & medicinal chemistry letters, Jun-07, Volume: 14, Issue:11 | 1- and 2-substituted naphthalenes: a new class of potential hypotensive agents. |
AID1454616 | Protein binding in Swiss Webster mouse plasma assessed as drug recovery at 2 uM by LC-MS/MS analysis | 2017 | ACS medicinal chemistry letters, Jul-13, Volume: 8, Issue:7 | New Class of Antitrypanosomal Agents Based on Imidazopyridines. |
AID1473740 | Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
AID1305710 | Half life in human liver microsomes at 0.1 uM | 2016 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 26, Issue:14 | Coumarin carboxylic acids as monocarboxylate transporter 1 inhibitors: In vitro and in vivo studies as potential anticancer agents. |
AID595744 | Half life in CD1 mouse liver microsomes by LC-MS-MS analysis | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8 | Ethionamide boosters: synthesis, biological activity, and structure-activity relationships of a series of 1,2,4-oxadiazole EthR inhibitors. |
AID1322297 | Displacement of [3H]clonidine from alpha2 adrenergic receptor in rat brain cerebral cortex at 50 uM after 25 mins by microbeta scintillation counting method | |||
AID127068 | Compound was evaluated for ventricular extrasystole activity, 3 min before aconitine infusion, at a dose of 10 mg/kg, intravenously administered in mice; S=significant antiarrhythmic effect | 1984 | Journal of medicinal chemistry, Sep, Volume: 27, Issue:9 | Synthesis and antiarrhythmic activity of new 1-[1-[2-[3-(alkylamino)-2-hydroxypropoxy]phenyl]vinyl]-1 H-imidazoles and related compounds. |
AID496825 | Antimicrobial activity against Leishmania mexicana | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID4253 | Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptor | 1997 | Journal of medicinal chemistry, Dec-19, Volume: 40, Issue:26 | 2-(1-Naphthyloxy)ethylamines with enhanced affinity for human 5-HT1D beta (h5-HT1B) serotonin receptors. |
AID1851459 | Half-life in human liver microsomes at 1 uM preincubated for 10 mins and measured up to 60 mins by LC-MS/MS analysis | 2022 | European journal of medicinal chemistry, Nov-05, Volume: 241 | Novel analgesic/anti-inflammatory agents: 1,5-Diarylpyrrole nitrooxyethyl sulfides and related compounds as Cyclooxygenase-2 inhibitors containing a nitric oxide donor moiety endowed with vasorelaxant properties. |
AID1262937 | Fraction unbound in mouse plasma at 5 uM after 4.5 hrs by LC-MS/MS analysis | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
AID165842 | Biodistribution pattern of [123I]- ligand was evaluated in lung of anesthetized rabbit after Intravenous injection of 50 uCi after 2 hr | 1996 | Journal of medicinal chemistry, Aug-16, Volume: 39, Issue:17 | Synthesis and in vitro and in vivo characteristics of an iodinated analogue of the beta-adrenoceptor antagonist carazolol. |
AID744894 | Antihypertensive activity in rat spontaneous hypertensive model assessed as mean arterial blood pressure at 20 mg/kg, po measured at 6 hrs by tail-cuff method (Rvb = 155.8 +/- 7.97 mmHg) | 2013 | Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9 | Novel hybrids of natural isochroman-4-one bearing N-substituted isopropanolamine as potential antihypertensive candidates. |
AID444054 | Oral bioavailability in human | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination. |
AID1220980 | Dissociation constant, pKa of the compound | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4 | Hepatic pharmacokinetics of cationic drugs in a high-fat emulsion-induced rat model of nonalcoholic steatohepatitis. |
AID61089 | Compound was tested for its ability to block isoproterenol-induced vasodilation in anesthetized dogs. | 1981 | Journal of medicinal chemistry, Mar, Volume: 24, Issue:3 | Ring-hydroxylated propranolol: synthesis and beta-receptor antagonist and vasodilating activities of the seven isomers. |
AID48145 | Hypotensive activity in cat following i.v. administration of 5 mg/kg expressed as fall in blood pressure | 2004 | Bioorganic & medicinal chemistry letters, Jun-07, Volume: 14, Issue:11 | 1- and 2-substituted naphthalenes: a new class of potential hypotensive agents. |
AID1262907 | Agonist activity at human wild-type alpha 1A receptor expressed in CHO cells assessed as calcium level by HTRF assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
AID1602586 | Apparent permeability across apical to basolateral side in human Caco2 cells at 5 uM by LC-MS/MS analysis | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5 | Identification and Characterization of AES-135, a Hydroxamic Acid-Based HDAC Inhibitor That Prolongs Survival in an Orthotopic Mouse Model of Pancreatic Cancer. |
AID40704 | The compound was tested for beta-2 adrenergic receptor blocking activity in dogs | 1986 | Journal of medicinal chemistry, Jan, Volume: 29, Issue:1 | [p-[(Thienylcarbonyl)amino]phenoxy]propanolamines derivatives as diuretic and beta-adrenergic receptor blocking agents. |
AID1451409 | Metabolic stability in dog liver microsomes assessed as compound remaining after 30 mins | 2017 | Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17 | 5-(4,6-Dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine (PQR309), a Potent, Brain-Penetrant, Orally Bioavailable, Pan-Class I PI3K/mTOR Inhibitor as Clinical Candidate in Oncology. |
AID29423 | HPLC capacity factor (k') | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13 | Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data. |
AID540215 | Volume of distribution at steady state in rat after iv administration | 2005 | Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7 | Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure. |
AID170444 | Antihypertensive activity in spontaneously hypertensive rats after peroral administration | 1980 | Journal of medicinal chemistry, Mar, Volume: 23, Issue:3 | Antihypertensive indole derivatives of phenoxypropanolamines with beta-adrenergic receptor antagonist and vasodilating activity. |
AID540209 | Volume of distribution at steady state in human after iv administration | 2008 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7 | Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds. |
AID1851460 | Intrinsic clearance in mouse liver microsomes at 1 uM preincubated for 10 mins and measured up to 60 mins by LC-MS/MS analysis | 2022 | European journal of medicinal chemistry, Nov-05, Volume: 241 | Novel analgesic/anti-inflammatory agents: 1,5-Diarylpyrrole nitrooxyethyl sulfides and related compounds as Cyclooxygenase-2 inhibitors containing a nitric oxide donor moiety endowed with vasorelaxant properties. |
AID625284 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID1207197 | Inhibition of calcium current (ICaL) measured using whole-cell patch clamp experiments in isolated guinea pig ventricular myocytes | 2011 | Cardiovascular research, Jul-01, Volume: 91, Issue:1 | Simulation of multiple ion channel block provides improved early prediction of compounds' clinical torsadogenic risk. |
AID1262940 | Metabolic stability in human liver microsomes assessed as CN adduct formation at 40 uM for 1 hr by LC/MS analysis | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
AID1135965 | Inhibition of beta1-adrenergic receptor in guinea pig auricle assessed as reversal of isoproterenol-induced effect | 1978 | Journal of medicinal chemistry, Jan, Volume: 21, Issue:1 | Adrenoceptor blocking agents. 2. 2-(alpha-Hydroxyarylmethyl)-3,3-dimethylaziridines, a new class of selective beta2-adrenoceptor antagonists. |
AID1217728 | Intrinsic clearance for reactive metabolites formation per mg of protein based on cytochrome P450 (unknown origin) inactivation rate by TDI assay | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
AID1415059 | Apparent permeability across apical to basolateral side in human Caco2 cells at pH 6.5 to 7.5 after 2 hrs by LC/MS/MS analysis | 2018 | Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23 | Application of Sequential Palladium Catalysis for the Discovery of Janus Kinase Inhibitors in the Benzo[ c]pyrrolo[2,3- h][1,6]naphthyridin-5-one (BPN) Series. |
AID1212323 | Drug uptake in lysosomes of human Fa2N-4 cells assessed as cellular partitioning at 1 uM preincubated with ammonium chloride for 5 mins followed by media washout and compound treatment measured after 5 mins by LC-MS analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4 | Lysosomal sequestration (trapping) of lipophilic amine (cationic amphiphilic) drugs in immortalized human hepatocytes (Fa2N-4 cells). |
AID737836 | Selectivity ratio of GI50 for human MRC5 cells to GI50 for human MDA-MB-231 cells | 2013 | Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7 | Synthesis of novel isoflavene-propranolol hybrids as anti-tumor agents. |
AID227718 | Binding energy by using the equation deltaG obsd = -RT ln KD | 1984 | Journal of medicinal chemistry, Dec, Volume: 27, Issue:12 | Functional group contributions to drug-receptor interactions. |
AID1262910 | Agonist activity at human wild-type AGTR1 receptor expressed in CHO-K1 cells assessed as calcium level by FDSS assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
AID1262935 | Fraction unbound in rat brain at 5 uM after 5 hrs by LC-MS/MS analysis | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
AID1125245 | Toxicity in DOCA-induced normotensive Wistar rat assessed as mean arterial pressure at 10 mg/kg, ip after 45 mins (Rvb = 94.83 +/- 0.943 mmHg) | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Synthesis and pharmacological screening of some novel anti-hypertensive agents possessing 5-Benzylidene-2-(phenylimino)-thiazolidin-4-one ring. |
AID1217729 | Intrinsic clearance for reactive metabolites formation assessed as summation of [3H]GSH adduct formation rate-based reactive metabolites formation and cytochrome P450 (unknown origin) inactivation rate-based reactive metabolites formation | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
AID759362 | Displacement of [3H]CGP-12177 from beta1-adrenergic receptor in rat cerebral cortex after 60 mins by scintillation counting | 2013 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15 | Synthesis and evaluation of pharmacological properties of some new xanthone derivatives with piperazine moiety. |
AID1262900 | Agonist activity at human 5-HT2A receptor expressed in CHO-K1 cells assessed as calcium level by FDSS assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
AID319635 | Apparent permeability from apical to basolateral side in human Caco-2 cells at 10 uM | 2008 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 18, Issue:11 | Novel HCV NS5B polymerase inhibitors derived from 4-(1',1'-dioxo-1',4'-dihydro-1'lambda(6)-benzo[1',2',4']thiadiazin-3'-yl)-5-hydroxy-2H-pyridazin-3-ones. Part 3: Further optimization of the 2-, 6-, and 7'-substituents and initial pharmacokinetic assessme |
AID177960 | Antagonistic activity against beta-1 adrenergic receptor to inhibit tachycardia in rats | 1985 | Journal of medicinal chemistry, Nov, Volume: 28, Issue:11 | Beta-adrenoceptor activity of the stereoisomers of the bufuralol alcohol and ketone metabolites. |
AID165984 | Biodistribution pattern of [123I]- ligand was evaluated in spleen of anesthetized rabbit after Intravenous injection of 50 uCi after 2 hr | 1996 | Journal of medicinal chemistry, Aug-16, Volume: 39, Issue:17 | Synthesis and in vitro and in vivo characteristics of an iodinated analogue of the beta-adrenoceptor antagonist carazolol. |
AID174417 | Change in systolic blood pressure after 100 mg/kg oral administration in spontaneous hypertensive rats after 2 hr | 1981 | Journal of medicinal chemistry, Dec, Volume: 24, Issue:12 | Antihypertensive pyrrolo[1,2-c]quinazolines and pyrrolo[1,2-c]quinazolinones. |
AID311367 | Permeability coefficient in human skin | 2007 | Bioorganic & medicinal chemistry, Nov-15, Volume: 15, Issue:22 | Transdermal penetration behaviour of drugs: CART-clustering, QSPR and selection of model compounds. |
AID1262939 | Metabolic stability in human liver microsomes assessed as GSH adduct formation at 40 uM for 1 hr by LC/MS analysis | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
AID361985 | Lipophilicity, log D of compound at pH 7.4 by microfluidic liquid-liquid extraction method | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16 | Determination of log D via automated microfluidic liquid-liquid extraction. |
AID721850 | Metabolic stability in mouse liver microsomes assessed as compound remaining after 30 mins by LC-MS/MS assay | 2013 | Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1 | Toward highly potent cancer agents by modulating the C-2 group of the arylthioindole class of tubulin polymerization inhibitors. |
AID42040 | Antagonist activity of compound against Beta-1 adrenergic receptor in isolated guinea pig left atria | 1981 | Journal of medicinal chemistry, Aug, Volume: 24, Issue:8 | 2-Benzodioxinylaminoethanols: a new class of beta-adrenergic blocking and antihypertensive agents. |
AID1810695 | Inhibition of cell migration in human T98G cells at 75 uM incubated for 24 hrs by crystal violet staining based by Boyden chamber method | 2021 | Journal of medicinal chemistry, 06-24, Volume: 64, Issue:12 | Propranolol Activates the Orphan Nuclear Receptor TLX to Counteract Proliferation and Migration of Glioblastoma Cells. |
AID540232 | Dose normalised AUC in monkey after po administration | 2005 | Xenobiotica; the fate of foreign compounds in biological systems, Feb, Volume: 35, Issue:2 | Comparative evaluation of oral systemic exposure of 56 xenobiotics in rat, dog, monkey and human. |
AID587815 | Metabolic stability of the compound in human liver microsome assessed as compound remaining | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5 | Potent farnesyltransferase inhibitors with 1,4-diazepane scaffolds as novel destabilizing microtubule agents in hormone-resistant prostate cancer. |
AID1123538 | Cardio selectivity ratio of Kapp for beta2 adrenergic receptor in rat lung muscle to Kapp for beta1 adrenergic receptor in rat ventricular muscle | 1979 | Journal of medicinal chemistry, Jun, Volume: 22, Issue:6 | Cardioselectivity of beta-adrenoceptor blocking agents 1. 1-[(4-Hydroxyphenethyl)amino]-3-(aryloxy)propan-2-ols. |
AID1146365 | Inhibition of isoproterenol-induced increase in heart rate in iv dosed bilaterally vagotomized open chest mongrel dog model administered 10 to 20 mins prior to and following isoproterenol challenge | 1978 | Journal of medicinal chemistry, Jan, Volume: 21, Issue:1 | Synthesis of heteroaromatic potential beta-adrenergic antagonists by the glycidol route. |
AID444050 | Fraction unbound in human plasma | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination. |
AID386625 | Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19 | Structural requirements for drug inhibition of the liver specific human organic cation transport protein 1. |
AID1221017 | Intrinsic elimination clearance in perfused liver of high-fat emulsion-induced nonalcoholic steatohepatitis Wistar rat assessed per gm of liver at 8 mM after 10 mins | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4 | Hepatic pharmacokinetics of cationic drugs in a high-fat emulsion-induced rat model of nonalcoholic steatohepatitis. |
AID444058 | Volume of distribution at steady state in human | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination. |
AID1603580 | Displacement of [3H]CGP12177 from human beta1 adrenoceptor expressed in HEK293T cell membranes | |||
AID165821 | Percentage change of IOP in rabbits after 8 hr administration (2.5%) of compound | 1988 | Journal of medicinal chemistry, Jan, Volume: 31, Issue:1 | Improved delivery through biological membranes. 26. Design, synthesis, and pharmacological activity of a novel chemical delivery system for beta-adrenergic blocking agents. |
AID1635248 | Efflux ratio of apparent permeability from basolateral to apical side over apical to basolateral side in human Caco2 cells at 10 uM incubated for 120 mins by LC-MS/MS analysis | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer. |
AID395325 | Lipophilicity, log P by microemulsion electrokinetic chromatography | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6 | Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs. |
AID395328 | Lipophilicity, log P of the compound | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6 | Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs. |
AID1125252 | Antihypertensive activity in Wistar rat assessed as mean arterial pressure at 10 mg/kg, ip measured immediately at 0 min (Rvb = 194.08 +/- 1.962 mmHg) | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Synthesis and pharmacological screening of some novel anti-hypertensive agents possessing 5-Benzylidene-2-(phenylimino)-thiazolidin-4-one ring. |
AID42039 | In vitro affinity constant against beta-1 adrenergic receptor from guinea pig artia | 1983 | Journal of medicinal chemistry, Nov, Volume: 26, Issue:11 | beta 1-selective adrenoceptor antagonists. 1. Synthesis and beta-adrenergic blocking activity of a series of binary (aryloxy)propanolamines. |
AID496823 | Antimicrobial activity against Trichomonas vaginalis | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID310933 | Permeability across PAMPA membrane after 7 hrs | 2007 | Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4 | In silico and in vitro filters for the fast estimation of skin permeation and distribution of new chemical entities. |
AID1626023 | Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Uncoupling the Structure-Activity Relationships of β2 Adrenergic Receptor Ligands from Membrane Binding. |
AID187013 | Tested for maximum fall in mean arterial pressure in Spontaneously hypertensive rats after peroral administration by using 1% methyl cellulose as vehicle at 1.25 mg/kg | 1980 | Journal of medicinal chemistry, Jan, Volume: 23, Issue:1 | Heterocyclic analogues of the antihypertensive beta-adrenergic blocking agent (S)-2-[3-(ter-butylamino)-2-hydroxypropoxy]-3-cyanopyridine. |
AID223361 | Inhibition of the isoproterenol response at a dose of 1 x 10e -4M in guinea pig; slight inhibition was found. | 1989 | Journal of medicinal chemistry, Jan, Volume: 32, Issue:1 | Flavones. 2. Synthesis and structure-activity relationship of flavodilol and its analogues, a novel class of antihypertensive agents with catecholamine depleting properties. |
AID186642 | Evaluated for its positive inotropic effect by the beta-adrenergic stimulation on cyclic AMP concentrations in rat left atria at 10E-7 concentration | 1984 | Journal of medicinal chemistry, Feb, Volume: 27, Issue:2 | Synthesis of imidazo[1,2-a]pyrazine derivatives with uterine-relaxing, antibronchospastic, and cardiac-stimulating properties. |
AID444055 | Fraction absorbed in human | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination. |
AID20050 | Human absorption A (%) | 1998 | Journal of medicinal chemistry, Mar-26, Volume: 41, Issue:7 | Physicochemical high throughput screening: parallel artificial membrane permeation assay in the description of passive absorption processes. |
AID625291 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID40420 | Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria | 1987 | Journal of medicinal chemistry, Jun, Volume: 30, Issue:6 | Synthesis of a series of compounds related to betaxolol, a new beta 1-adrenoceptor antagonist with a pharmacological and pharmacokinetic profile optimized for the treatment of chronic cardiovascular diseases. |
AID1365729 | Fraction unbound in human plasma at 5 uM after 4 hrs by LC-MS/MS analysis | 2017 | Bioorganic & medicinal chemistry, 11-01, Volume: 25, Issue:21 | The antitubercular activity of various nitro(triazole/imidazole)-based compounds. |
AID7779 | Oral bioavailability in human | 2002 | Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2 | Graphical model for estimating oral bioavailability of drugs in humans and other species from their Caco-2 permeability and in vitro liver enzyme metabolic stability rates. |
AID1750279 | Apparent permeability of the compound across basolateral to apical side in human Caco-2 cells at 20 uM | |||
AID165960 | Concentration in iris -ciliary body of rabbit after 120 min administration of compound; Below detection limit | 1988 | Journal of medicinal chemistry, Jan, Volume: 31, Issue:1 | Improved delivery through biological membranes. 26. Design, synthesis, and pharmacological activity of a novel chemical delivery system for beta-adrenergic blocking agents. |
AID21271 | Mean apparent permeability through fuzzy rat skin | 1988 | Journal of medicinal chemistry, Feb, Volume: 31, Issue:2 | (Acyloxy)alkyl carbamates as novel bioreversible prodrugs for amines: increased permeation through biological membranes. |
AID165805 | Percentage change of IOP in rabbits after 30 min administration (2.5%) of compound | 1988 | Journal of medicinal chemistry, Jan, Volume: 31, Issue:1 | Improved delivery through biological membranes. 26. Design, synthesis, and pharmacological activity of a novel chemical delivery system for beta-adrenergic blocking agents. |
AID41150 | Beta adrenergic receptor antagonist potency relative to propranolol. | 1981 | Journal of medicinal chemistry, Mar, Volume: 24, Issue:3 | Ring-hydroxylated propranolol: synthesis and beta-receptor antagonist and vasodilating activities of the seven isomers. |
AID1212328 | Drug uptake in lysosomes of human Fa2N-4 cells assessed as cellular partitioning at 1 uM after 5 mins by LC-MS analysis in presence of astemizole | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4 | Lysosomal sequestration (trapping) of lipophilic amine (cationic amphiphilic) drugs in immortalized human hepatocytes (Fa2N-4 cells). |
AID1209455 | Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1 | In vitro inhibition of the bile salt export pump correlates with risk of cholestatic drug-induced liver injury in humans. |
AID40396 | Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for S-enantiomer) | 1998 | Journal of medicinal chemistry, May-07, Volume: 41, Issue:10 | Synthesis and adrenergic activity of a new series of N-aryl dicyclopropyl ketone oxime ethers: SAR and stereochemical aspects. |
AID540216 | Clearance in dog after iv administration | 2005 | Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7 | Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure. |
AID41754 | Inhibitory activity against beta adrenergic receptor of rat frontal cortex homogenate using (1.0 nM) [3H]- dihydroalprenolol | 1989 | Journal of medicinal chemistry, Apr, Volume: 32, Issue:4 | Design and synthesis of propranolol analogues as serotonergic agents. |
AID1220979 | Octanol-water apparent partition coefficient, logD of the compound at pH 7.4 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4 | Hepatic pharmacokinetics of cationic drugs in a high-fat emulsion-induced rat model of nonalcoholic steatohepatitis. |
AID1393542 | Efflux ratio in human Caco2 cells in absence of P-gp inhibitor by LC-MS/MS analysis | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Effects of rigidity on the selectivity of protein kinase inhibitors. |
AID1302019 | Passive permeability of compound at 500 uM after 4 hrs by BBB-PAMPA | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8 | Bifunctional Peptide-Based Opioid Agonist-Nociceptin Antagonist Ligands for Dual Treatment of Acute and Neuropathic Pain. |
AID1907153 | Apparent permeability of the compound across basolateral to apical side in human Caco-2 cells at 10 uM incubated for 120 mins and measured by LC-MS/MS analysis | 2022 | European journal of medicinal chemistry, Jun-05, Volume: 236 | Discovery, optimization and evaluation of 1-(indolin-1-yl)ethan-1-ones as novel selective TRIM24/BRPF1 bromodomain inhibitors. |
AID41610 | The compound was tested for the concentration to inhibit 50% of Beta adrenergic receptor isolated from rat ventricle homogenates | 1998 | Journal of medicinal chemistry, May-07, Volume: 41, Issue:10 | Synthesis and adrenergic activity of a new series of N-aryl dicyclopropyl ketone oxime ethers: SAR and stereochemical aspects. |
AID194448 | Evaluated for the percentage inhibition of the depressor response of isoproterenol (0.25 mg/kg, iv) by propranolol hydrochloride at dose of 10 mg/kg | 1987 | Journal of medicinal chemistry, May, Volume: 30, Issue:5 | Flavones. 1. Synthesis and antihypertensive activity of (3-phenylflavonoxy)propanolamines without beta-adrenoceptor antagonism. |
AID468628 | Apparent permeability from basolateral to apical side in human Caco-2 cells | 2009 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20 | Phenylaminopyrimidines as inhibitors of Janus kinases (JAKs). |
AID1393788 | Efflux ratio in human Caco2 cells in presence of P-gp inhibitor by LC-MS/MS analysis | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Effects of rigidity on the selectivity of protein kinase inhibitors. |
AID33124 | Evaluated for norepinephrine as agonist. | 1982 | Journal of medicinal chemistry, Jun, Volume: 25, Issue:6 | Arylethanolamines derived from salicylamide with alpha- and beta-adrenoceptor blocking activities. Preparation of labetalol, its enantiomers, and related salicylamides. |
AID193105 | Beta-adrenergic receptor blockade activity in conscious normotensive rats at a dose of 1.25 mg/kg | 1980 | Journal of medicinal chemistry, Mar, Volume: 23, Issue:3 | Antihypertensive indole derivatives of phenoxypropanolamines with beta-adrenergic receptor antagonist and vasodilating activity. |
AID351392 | Activity of Bacillus megaterium CYP450 D6H10 mutant assessed as conversion of propranolol to 5-hydroxypropranolol at 5 mM in presence of 1 mM H2O2 and 4 mM ascorbic acid | 2009 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11 | Regioselective preparation of 5-hydroxypropranolol and 4'-hydroxydiclofenac with a fungal peroxygenase. |
AID744928 | Antagonist activity at beta1 adrenoreceptor in Sprague-Dawley rat left atrium assessed as inhibition of isoprenaline-induced contraction at 0.1 uM incubated for 5 mins prior to isoprenaline-induction | 2013 | Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9 | Novel hybrids of natural isochroman-4-one bearing N-substituted isopropanolamine as potential antihypertensive candidates. |
AID28234 | % absorbed in human GI-tract | 2001 | Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6 | High-throughput permeability pH profile and high-throughput alkane/water log P with artificial membranes. |
AID1079943 | Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source] | |||
AID1900031 | Apparent permeability across apical to basolateral side in human Caco-2 cells assessed as drug recovery at 10 uM measured after 2 hrs by LC-MS/MS analysis | 2022 | Journal of medicinal chemistry, 01-13, Volume: 65, Issue:1 | Design, Synthesis, and Biological Evaluation of 1-(Indolizin-3-yl)ethan-1-ones as CBP Bromodomain Inhibitors for the Treatment of Prostate Cancer. |
AID1900029 | Apparent permeability across basolateral to apical side in human Caco-2 cells at 10 uM measured after 2 hrs by LC-MS/MS analysis | 2022 | Journal of medicinal chemistry, 01-13, Volume: 65, Issue:1 | Design, Synthesis, and Biological Evaluation of 1-(Indolizin-3-yl)ethan-1-ones as CBP Bromodomain Inhibitors for the Treatment of Prostate Cancer. |
AID1874536 | Apparent permeability across apical to basolateral side in human Caco-2 cells measured after 120 mins by LC-MS/MS analysis | 2022 | Journal of medicinal chemistry, 09-08, Volume: 65, Issue:17 | Development, Optimization, and In Vivo Validation of New Imidazopyridine Chemotypes as Dual TLR7/TLR9 Antagonists through Activity-Directed Sequential Incorporation of Relevant Structural Subunits. |
AID79652 | Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparation at a duration of 40 min | 1982 | Journal of medicinal chemistry, Dec, Volume: 25, Issue:12 | Ultra-short-acting beta-adrenergic receptor blocking agents. 2. (Aryloxy)propanolamines containing esters on the aryl function. |
AID1702307 | Permeability of compound across apical to basolateral side in human Caco-2 cells at pH 6.5 | |||
AID678716 | Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using diethoxyfluorescein as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
AID588220 | Literature-mined public compounds from Kruhlak et al phospholipidosis modelling dataset | 2008 | Toxicology mechanisms and methods, , Volume: 18, Issue:2-3 | Development of a phospholipidosis database and predictive quantitative structure-activity relationship (QSAR) models. |
AID29812 | Oral bioavailability in human | 2000 | Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13 | QSAR model for drug human oral bioavailability. |
AID236268 | Fraction absorbed in human intestine after oral administration compound was measured | 2005 | Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2 | Exploring the role of different drug transport routes in permeability screening. |
AID62986 | Effect on ischemic arrhythmias was studied in dogs, by glass bead method. 60 mg/kg was administered perorally and percent sinus beats after compound administration, was reported. | 1984 | Journal of medicinal chemistry, Sep, Volume: 27, Issue:9 | Synthesis and antiarrhythmic activity of new 1-[1-[2-[3-(alkylamino)-2-hydroxypropoxy]phenyl]vinyl]-1 H-imidazoles and related compounds. |
AID166299 | Effect on IOP of rabbits 3h after administration (2.5%) | 1988 | Journal of medicinal chemistry, Jan, Volume: 31, Issue:1 | Improved delivery through biological membranes. 26. Design, synthesis, and pharmacological activity of a novel chemical delivery system for beta-adrenergic blocking agents. |
AID41760 | In vitro inhibitory specificity for Beta adrenergic receptor was evaluated | 1998 | Journal of medicinal chemistry, May-07, Volume: 41, Issue:10 | Synthesis and adrenergic activity of a new series of N-aryl dicyclopropyl ketone oxime ethers: SAR and stereochemical aspects. |
AID165560 | Biodistribution pattern of [123I]- ligand was evaluated in blood of anesthetized rabbit after Intravenous injection of 50 uCi after 2 hr | 1996 | Journal of medicinal chemistry, Aug-16, Volume: 39, Issue:17 | Synthesis and in vitro and in vivo characteristics of an iodinated analogue of the beta-adrenoceptor antagonist carazolol. |
AID1752935 | Intrinsic clearance in human liver microsomes measured upto 40 mins by LC-MS/MS analysis | |||
AID1220997 | Permeability surface area product in healthy Wistar rat perfused liver assessed per gm of liver at 8 mM after 10 mins | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4 | Hepatic pharmacokinetics of cationic drugs in a high-fat emulsion-induced rat model of nonalcoholic steatohepatitis. |
AID1223490 | Apparent permeability across human differentiated Caco2 cells | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2 | Predicting phenolic acid absorption in Caco-2 cells: a theoretical permeability model and mechanistic study. |
AID298036 | Fraction unbound ligand in rat brown fat tissue after 20 hrs | 2007 | Journal of medicinal chemistry, Sep-20, Volume: 50, Issue:19 | High-throughput screening of drug-brain tissue binding and in silico prediction for assessment of central nervous system drug delivery. |
AID350784 | Permeability from basolateral to apical side in human Caco-2 cells | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Efficacy, pharmacokinetics, and metabolism of tetrahydroquinoline inhibitors of Plasmodium falciparum protein farnesyltransferase. |
AID40877 | Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparation | 1982 | Journal of medicinal chemistry, Dec, Volume: 25, Issue:12 | Ultra-short-acting beta-adrenergic receptor blocking agents. 2. (Aryloxy)propanolamines containing esters on the aryl function. |
AID1215122 | Percentage unbound in solid supported porcine brain membrane vesicles at 5 uM by TRANSIL assay | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Brain tissue binding of drugs: evaluation and validation of solid supported porcine brain membrane vesicles (TRANSIL) as a novel high-throughput method. |
AID1211797 | Intrinsic clearance in cryopreserved human hepatocytes cells assessed per 10'6 cells by LC-MS/MS method | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1 | Comparison of cryopreserved HepaRG cells with cryopreserved human hepatocytes for prediction of clearance for 26 drugs. |
AID1137374 | Antihypertensive activity in spontaneously hypertensive Wistar-Okamoto rat assessed as maximal fall in mean arterial pressure at 20 mg/kg, po | 1979 | Journal of medicinal chemistry, Nov, Volume: 22, Issue:11 | Symbiotic approach to drug design: antihypertensive beta-adrenergic blocking agents. |
AID678721 | Metabolic stability in human liver microsomes assessed as GSH adduct formation at 100 uM after 90 mins by HPLC-MS analysis | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
AID1217704 | Time dependent inhibition of CYP1A2 (unknown origin) at 100 uM by LC/MS system | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
AID166298 | Effect on IOP of rabbits 3h after administration (1%) | 1988 | Journal of medicinal chemistry, Jan, Volume: 31, Issue:1 | Improved delivery through biological membranes. 26. Design, synthesis, and pharmacological activity of a novel chemical delivery system for beta-adrenergic blocking agents. |
AID233866 | Selectivity determined by expression 10[pA2(atria) - pA2 (trachea)] in guinea pig | 1984 | Journal of medicinal chemistry, Aug, Volume: 27, Issue:8 | [(Arylcarbonyl)oxy]propanolamines. 1. Novel beta-blockers with ultrashort duration of action. |
AID604026 | Unbound CSF to plasma concentration ratio in human | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20 | Structure-brain exposure relationships in rat and human using a novel data set of unbound drug concentrations in brain interstitial and cerebrospinal fluids. |
AID39943 | In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria | 1986 | Journal of medicinal chemistry, Jun, Volume: 29, Issue:6 | Beta 1-selective adrenoceptor antagonists: examples of the 2-[4-[3-(substituted amino)-2-hydroxypropoxy]phenyl]imidazole class. 2. |
AID1752934 | Intrinsic clearance in mouse liver microsomes measured upto 40 mins by LC-MS/MS analysis | |||
AID241889 | Inhibitory activity against recombinant human Cytochrome P450 2D6 (CYP2D6) after incubated for 45 minutes | 2005 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 15, Issue:17 | A 3D-QSAR model for CYP2D6 inhibition in the aryloxypropanolamine series. |
AID1832395 | Apparent permeability across basolateral to apical side in human Caco2 cells at 10 uM | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Discovery of Novel Acetamide-Based Heme Oxygenase-1 Inhibitors with Potent |
AID288192 | Partition coefficient, log P of the compound | 2007 | Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11 | QSAR study on permeability of hydrophobic compounds with artificial membranes. |
AID127205 | Compound was evaluated for ventricular extrasystole, 30 min before aconitine infusion, at a dose of 30 mg/kg, perorally administered in mice; S=significant antiarrhythmic effect | 1984 | Journal of medicinal chemistry, Sep, Volume: 27, Issue:9 | Synthesis and antiarrhythmic activity of new 1-[1-[2-[3-(alkylamino)-2-hydroxypropoxy]phenyl]vinyl]-1 H-imidazoles and related compounds. |
AID411793 | Metabolic stability in human liver microsomes assessed as intrinsic clearance per mg of protein | 2009 | Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2 | Metabolic soft spot identification and compound optimization in early discovery phases using MetaSite and LC-MS/MS validation. |
AID79324 | Antagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbachol | 1988 | Journal of medicinal chemistry, Nov, Volume: 31, Issue:11 | Synthesis and beta-adrenergic antagonism of 2-(aryloxy)-1-(2-piperidyl)ethanols. |
AID1222768 | Systemic clearance in human | 2013 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5 | Which metabolites circulate? |
AID361980 | Membrane permeability assessed as passive transport after 4 hrs by PAMPA | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16 | Toward an optimal blood-brain barrier shuttle by synthesis and evaluation of peptide libraries. |
AID1230989 | Permeability of the compound at pH 7.4 by PAMPA | 2015 | Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14 | Discovery and Modification of in Vivo Active Nrf2 Activators with 1,2,4-Oxadiazole Core: Hits Identification and Structure-Activity Relationship Study. |
AID1331468 | Intrinsic permeability of compound at 50 uM at pH 7.4 after 16 hrs by PAMPA assay | 2017 | Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1 | Rational design, synthesis, and structure-activity relationships of 5-amino-1H-pyrazole-4-carboxylic acid derivatives as protein tyrosine phosphatase 1B inhibitors. |
AID592681 | Apparent permeability across human Caco2 cell membrane after 2 hrs by LC-MS/MS analysis | 2011 | Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8 | QSAR-based permeability model for drug-like compounds. |
AID1212316 | Drug uptake in lysosomes of human Fa2N-4 cells assessed as cellular partitioning measured per 10'6 cells at 1 uM after 5 mins by LC-MS analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4 | Lysosomal sequestration (trapping) of lipophilic amine (cationic amphiphilic) drugs in immortalized human hepatocytes (Fa2N-4 cells). |
AID1262866 | Chemical stability of compound in DMSO assessed as compound remaining at 10 mg/ml after 2 days at room temperature | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
AID165975 | Concentration of propranolone oxime in aqueous humor of rabbit after 30 min administration of compound; N/A= no oxime can be present after administration of propranolone hydrochloride | 1988 | Journal of medicinal chemistry, Jan, Volume: 31, Issue:1 | Improved delivery through biological membranes. 26. Design, synthesis, and pharmacological activity of a novel chemical delivery system for beta-adrenergic blocking agents. |
AID186078 | Compound was tested for effect on arterial pressure in spontaneously hypertensive rats (SHR) at 5 mg/kg, po | 1981 | Journal of medicinal chemistry, May, Volume: 24, Issue:5 | Approaches to vasodilating/beta-adrenergic blocking agents: examples of the dihydrolutidine type. |
AID1415343 | Anticonvulsant activity in ip dosed mouse assessed as protection against maximal electroshock-induced seizures | 2017 | MedChemComm, Jan-01, Volume: 8, Issue:1 | Design, synthesis and anticonvulsant-analgesic activity of new |
AID28679 | Partition coefficient (logD6.8) | 2001 | Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6 | High-throughput permeability pH profile and high-throughput alkane/water log P with artificial membranes. |
AID1733542 | Permeability across basolateral to apical side in human Caco2 cells assessed as mass balance at 20 uM after 2 hrs by LC-MS analysis | 2021 | Bioorganic & medicinal chemistry, 05-01, Volume: 37 | Systematic evaluation of structure-property relationships and pharmacokinetics in 6-(hetero)aryl-substituted matched pair analogs of amiloride and 5-(N,N-hexamethylene)amiloride. |
AID588210 | Human drug-induced liver injury (DILI) modelling dataset from Ekins et al | 2010 | Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 38, Issue:12 | A predictive ligand-based Bayesian model for human drug-induced liver injury. |
AID666540 | Antiarrhythmic activity in iv dosed Wistar rat assessed as protection against adrenaline-induced arrhythmia administered 15 mins prior to adrenaline-challenge | 2012 | Bioorganic & medicinal chemistry, Apr-01, Volume: 20, Issue:7 | Antiarrhythmic properties of phenylpiperazine derivatives of phenytoin with α₁-adrenoceptor affinities. |
AID540218 | Clearance in monkey after iv administration | 2005 | Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7 | Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure. |
AID1454617 | Fraction unbound in Swiss Webster mouse plasma at 2 uM by LC-MS/MS analysis | 2017 | ACS medicinal chemistry letters, Jul-13, Volume: 8, Issue:7 | New Class of Antitrypanosomal Agents Based on Imidazopyridines. |
AID1305708 | Permeability across basolateral side at pH 6.5 to apical side at pH 7.4 in human Caco2 cells assessed as compound recovery at 10 uM | 2016 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 26, Issue:14 | Coumarin carboxylic acids as monocarboxylate transporter 1 inhibitors: In vitro and in vivo studies as potential anticancer agents. |
AID1466760 | Half life in human liver microsomes at 1 uM pretreated up to 45 mins followed by NADPH addition by LC/MS/MS analysis | 2017 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 27, Issue:12 | Drug-like property-driven optimization of 4-substituted 1,5-diarylanilines as potent HIV-1 non-nucleoside reverse transcriptase inhibitors against rilpivirine-resistant mutant virus. |
AID744884 | Toxicity in rat spontaneous hypertensive model assessed as heart rate at 20 mg/kg, po measured at 4 hrs by tail-cuff method (Rvb = 403.1 +/- 15.92 bpm) | 2013 | Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9 | Novel hybrids of natural isochroman-4-one bearing N-substituted isopropanolamine as potential antihypertensive candidates. |
AID1776036 | Metabolic stability in CD1 mouse liver microsomes assessed as half life at 10 uM incubated for 4 hr by LC-MS analysis | 2021 | Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8 | Deconstructing Noncovalent Kelch-like ECH-Associated Protein 1 (Keap1) Inhibitors into Fragments to Reconstruct New Potent Compounds. |
AID1668034 | Antiproliferative activity against human SK-MEL-28 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay | 2020 | Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9 | Drug repurposing and rediscovery: Design, synthesis and preliminary biological evaluation of 1-arylamino-3-aryloxypropan-2-ols as anti-melanoma agents. |
AID1135371 | In vivo inhibition of beta-adrenoceptor in histamine-treated guinea pig assessed as inhibition of isoproterenol-induced bronchodilator effect at 0.1 mg/kg, iv administered 3 mins prior to histamine/isoproterenol challenge relative to control | 1977 | Journal of medicinal chemistry, Jul, Volume: 20, Issue:7 | beta-Adrenoceptor blocking activity of halogenated thienylethanolamine derivatives. |
AID193107 | The compound was tested for beta-adrenergic receptor blockade activity in conscious normotensive rats at a dose of 5 mg/kg | 1980 | Journal of medicinal chemistry, Mar, Volume: 23, Issue:3 | Antihypertensive indole derivatives of phenoxypropanolamines with beta-adrenergic receptor antagonist and vasodilating activity. |
AID48541 | The compound was evaluated for inhibition of depressor response. | 1982 | Journal of medicinal chemistry, Dec, Volume: 25, Issue:12 | beta-adrenergic blocking agents. 24. Heterocyclic substituted 1-(aryloxy)-3-[[(amido)alkyl]amino]propan-2-ols. |
AID58612 | Concentration required to reverse ouabain induced arrhythmia in dogs | 1980 | Journal of medicinal chemistry, Feb, Volume: 23, Issue:2 | Mono- and diaryl-2-quinuclidinylcarbinols with local anesthetic and antiarrhythmic activity. |
AID165973 | Concentration of propranolone oxime in aqueous humor of rabbit after 120 min administration of compound; N/A= no oxime can be present after administration of propranolone hydrochloride | 1988 | Journal of medicinal chemistry, Jan, Volume: 31, Issue:1 | Improved delivery through biological membranes. 26. Design, synthesis, and pharmacological activity of a novel chemical delivery system for beta-adrenergic blocking agents. |
AID40869 | In vitro beta-2 adrenergic receptor activity was determined by measuring inhibition of the isoproterenol induced relaxation in isolated guinea pig tracheal chains contracted with PGF2-alpha | 1983 | Journal of medicinal chemistry, Jul, Volume: 26, Issue:7 | Beta 1-selective adrenoceptor antagonists: examples of the 2-[4-[3-(substituted-amino)-2-hydroxypropoxy]phenyl]imidazole class. |
AID1079933 | Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is | |||
AID168635 | Compound was tested for oral salidiuretic activity (control/drug treatment value) in rats expressed as urinary output. at a dose of 64 mg/kg; 9.05/11.67 | 1986 | Journal of medicinal chemistry, Jan, Volume: 29, Issue:1 | [p-[(Thienylcarbonyl)amino]phenoxy]propanolamines derivatives as diuretic and beta-adrenergic receptor blocking agents. |
AID1262942 | Mutagenicity in Salmonella typhimurium by Ames test | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
AID625289 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID1365727 | Apparent permeability of the compound across basolateral side to apical side in human Caco2 cells monolayer at 10 uM after 1 hr by LC-MS/MS analysis | 2017 | Bioorganic & medicinal chemistry, 11-01, Volume: 25, Issue:21 | The antitubercular activity of various nitro(triazole/imidazole)-based compounds. |
AID1226792 | Permeability of the compound at 10 uM after 5 hrs by LC-MS detection based PAMPA method | 2015 | Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11 | Probing the Physicochemical Boundaries of Cell Permeability and Oral Bioavailability in Lipophilic Macrocycles Inspired by Natural Products. |
AID1211791 | Fraction unbound in human hepatocytes | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1 | Comparison of cryopreserved HepaRG cells with cryopreserved human hepatocytes for prediction of clearance for 26 drugs. |
AID1135375 | Acute toxicity in iv dosed mouse | 1977 | Journal of medicinal chemistry, Jul, Volume: 20, Issue:7 | beta-Adrenoceptor blocking activity of halogenated thienylethanolamine derivatives. |
AID476929 | Human intestinal absorption in po dosed human | 2010 | European journal of medicinal chemistry, Mar, Volume: 45, Issue:3 | Neural computational prediction of oral drug absorption based on CODES 2D descriptors. |
AID1135962 | Reversal of epinephrine-induced increase in mean arterial blood pressure in cat at 2.5 mg/kg, iv | 1978 | Journal of medicinal chemistry, Jan, Volume: 21, Issue:1 | Adrenoceptor blocking agents. 2. 2-(alpha-Hydroxyarylmethyl)-3,3-dimethylaziridines, a new class of selective beta2-adrenoceptor antagonists. |
AID1220971 | Drug distribution in healthy Wistar rat perfused liver assessed as equilibrium amount ratio charactering slow binding process at 8 mM after 10 mins | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4 | Hepatic pharmacokinetics of cationic drugs in a high-fat emulsion-induced rat model of nonalcoholic steatohepatitis. |
AID1350482 | Displacement of [3H]-CGP12177 from human beta1 ADR expressed in HEK293T cell membranes after 90 mins by scintillation counting | 2018 | Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12 | Discovery of β-Adrenergic Receptors Blocker-Carbonic Anhydrase Inhibitor Hybrids for Multitargeted Antiglaucoma Therapy. |
AID230146 | The cardioselectivity ratio was obtained by taking the antilog (pA2 beta1-pA2 beta2) | 1986 | Journal of medicinal chemistry, Jun, Volume: 29, Issue:6 | Beta 1-selective adrenoceptor antagonists: examples of the 2-[4-[3-(substituted amino)-2-hydroxypropoxy]phenyl]imidazole class. 2. |
AID1262930 | Inhibition of human CYP2C19 by LC-MS analysis | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
AID1074028 | Efflux ratio of permeability in pig LLC-PK1 cells transfected with human MDR1 at 1 uM by LC-MS/MS analysis | 2014 | Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3 | Discovery of 7-tetrahydropyran-2-yl chromans: β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors that reduce amyloid β-protein (Aβ) in the central nervous system. |
AID1766988 | Permeability of the compound at pH 7.4 by PAMPA | |||
AID1382494 | Intrinsic clearance in human liver microsomes at 0.1 uM preincubated for 5 mins followed by NDAPH addition measured up to 60 mins by HPLC-MS/MS analysis | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Alkynyl-containing phenylthiazoles: Systemically active antibacterial agents effective against methicillin-resistant Staphylococcus aureus (MRSA). |
AID1350707 | Apparent permeability cross apical to basolateral side in MDCK-MDR1 cells at 5 uM after 90 mins by LC-MS/MS analysis | 2018 | Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14 | Optimization of Isothiazolo[4,3- b]pyridine-Based Inhibitors of Cyclin G Associated Kinase (GAK) with Broad-Spectrum Antiviral Activity. |
AID79515 | Negative log concentration effecting 50% blockade of isoproterenol-induced rate responses in vitro in guinea pig right atria. | 1983 | Journal of medicinal chemistry, Aug, Volume: 26, Issue:8 | Ultra-short-acting beta-adrenergic receptor blocking agents. 3. Ethylenediamine derivatives of (aryloxy)propanolamines having esters on the aryl function. |
AID395327 | Dissociation constant, pKa by capillary electrophoresis | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6 | Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs. |
AID1720724 | Anticonvulsant activity in ip dosed albino mouse assessed as protection against 50 mA current-induced seizure by maximal electroshock seizure test | |||
AID1135145 | Antagonist activity at guinea pig atrial beta adrenergic receptor assessed as isometric contractions by force displacement transducer | 1977 | Journal of medicinal chemistry, Mar, Volume: 20, Issue:3 | Synthesis and adrenergic beta-blocking activity of some 1,3-benzodioxole derivatives. |
AID165949 | Concentration in aqueous humor of rabbit after 120 min administration of compound; Below detection limit | 1988 | Journal of medicinal chemistry, Jan, Volume: 31, Issue:1 | Improved delivery through biological membranes. 26. Design, synthesis, and pharmacological activity of a novel chemical delivery system for beta-adrenergic blocking agents. |
AID1137372 | Antihypertensive activity in spontaneously hypertensive Wistar-Okamoto rat assessed as maximal fall in mean arterial pressure at 1.25 mg/kg, po | 1979 | Journal of medicinal chemistry, Nov, Volume: 22, Issue:11 | Symbiotic approach to drug design: antihypertensive beta-adrenergic blocking agents. |
AID1752938 | Half life in mouse liver microsomes measured upto 40 mins by LC-MS/MS analysis | |||
AID1136404 | Inhibition of beta-adrenergic receptor in isoproterenol-stimulated guinea pig atrial muscle | 1978 | Journal of medicinal chemistry, Sep, Volume: 21, Issue:9 | Nondepressant beta-adrenergic blocking agents. 1. Substituted 3-amino-1-(5,6,7,8-tetrahydro-1-naphthoxy)-2-propanols. |
AID1262928 | Inhibition of human CYP2D6 by LC-MS analysis | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
AID702960 | Half life in human liver microsomes | 2012 | Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12 | Identification, synthesis, and biological evaluation of the metabolites of 3-amino-6-(3'-aminopropyl)-5H-indeno[1,2-c]isoquinoline-5,11-(6H)dione (AM6-36), a promising rexinoid lead compound for the development of cancer chemotherapeutic and chemopreventi |
AID625282 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID1424874 | Protein binding in mouse plasma at 1 uM after 16 hrs by LC-MS/MS analysis | 2018 | European journal of medicinal chemistry, Jun-25, Volume: 154 | From hit to lead: Structure-based discovery of naphthalene-1-sulfonamide derivatives as potent and selective inhibitors of fatty acid binding protein 4. |
AID1472091 | Apparent permeability of compound at 1 uM at pH 6.5 after 4 hrs by PAMPA | 2017 | Journal of medicinal chemistry, 12-28, Volume: 60, Issue:24 | 4-Aminoquinoline Antimalarials Containing a Benzylmethylpyridylmethylamine Group Are Active against Drug Resistant Plasmodium falciparum and Exhibit Oral Activity in Mice. |
AID744886 | Toxicity in rat spontaneous hypertensive model assessed as heart rate at 20 mg/kg, po measured at 2 hrs by tail-cuff method (Rvb = 399.5 +/- 19.68 bpm) | 2013 | Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9 | Novel hybrids of natural isochroman-4-one bearing N-substituted isopropanolamine as potential antihypertensive candidates. |
AID636084 | Antiplasmodial activity against Plasmodium falciparum schizonts assessed as parasitemia at IC50 concentration treated until all schizonts had burst and invasion was assumed to have occurred by Giemsa staining-based microscopy (Rvb = 8.83%) | 2012 | Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2 | Synthesis, biological evaluation and mechanistic studies of totarol amino alcohol derivatives as potential antimalarial agents. |
AID298033 | Fraction unbound ligand in rat adrenal gland after 20 hrs | 2007 | Journal of medicinal chemistry, Sep-20, Volume: 50, Issue:19 | High-throughput screening of drug-brain tissue binding and in silico prediction for assessment of central nervous system drug delivery. |
AID48734 | Percent of maximum effect in anaesthetized cat at a dose of 1 mg/kg intravenously | 2004 | Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12 | Potential hypotensive agents: synthesis and hypotensive activity of oxime ethers derived from 1-naphthoxepines and related compounds. |
AID193870 | Change in diastolic blood pressure in anesthetized spontaneous hypertensive rats when 5 mg/kg of compound was administered intravenously | 1981 | Journal of medicinal chemistry, Aug, Volume: 24, Issue:8 | 2-Benzodioxinylaminoethanols: a new class of beta-adrenergic blocking and antihypertensive agents. |
AID39950 | Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparation | 1982 | Journal of medicinal chemistry, Dec, Volume: 25, Issue:12 | Ultra-short-acting beta-adrenergic receptor blocking agents. 2. (Aryloxy)propanolamines containing esters on the aryl function. |
AID1222769 | Fraction unbound in human | 2013 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5 | Which metabolites circulate? |
AID678722 | Covalent binding affinity to human liver microsomes assessed per mg of protein at 10 uM after 60 mins presence of NADPH | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
AID1145698 | Negative inotropic activity in guinea pig right atrium assessed as contractile force at MEC after 30 mins | 1977 | Journal of medicinal chemistry, Apr, Volume: 20, Issue:4 | Beta-adrenoceptor studies. 2. Effects of alkyl substitution on beta-adrenoceptor blocking, antiarrhythmic, and local anesthetic activities of 1,1'-(o-phenylenedioxy)bis(3-isopropylamino-2-propanol). |
AID744908 | Antihypertensive activity in rat spontaneous hypertensive model assessed as diastolic arterial blood pressure at 20 mg/kg, po measured at 4 hrs by tail-cuff method (Rvb = 141.4 +/- 7.11 mmHg) | 2013 | Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9 | Novel hybrids of natural isochroman-4-one bearing N-substituted isopropanolamine as potential antihypertensive candidates. |
AID1472090 | Apparent permeability of compound at 1 uM at pH 4 after 4 hrs by PAMPA | 2017 | Journal of medicinal chemistry, 12-28, Volume: 60, Issue:24 | 4-Aminoquinoline Antimalarials Containing a Benzylmethylpyridylmethylamine Group Are Active against Drug Resistant Plasmodium falciparum and Exhibit Oral Activity in Mice. |
AID1415058 | Aqueous solubility of the compound in simulated gastric fluid | 2018 | Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23 | Application of Sequential Palladium Catalysis for the Discovery of Janus Kinase Inhibitors in the Benzo[ c]pyrrolo[2,3- h][1,6]naphthyridin-5-one (BPN) Series. |
AID496827 | Antimicrobial activity against Leishmania amazonensis | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID42209 | Beta-1 adrenergic receptor blocking activity in atria of guinea pig. | 1984 | Journal of medicinal chemistry, Oct, Volume: 27, Issue:10 | Synthesis and beta-adrenergic blocking activity of new aliphatic and alicyclic oxime ethers. |
AID193881 | Change in systolic blood pressure in anesthetized spontaneous hypertensive rats when 5 mg/kg of compound was administered intravenously | 1981 | Journal of medicinal chemistry, Aug, Volume: 24, Issue:8 | 2-Benzodioxinylaminoethanols: a new class of beta-adrenergic blocking and antihypertensive agents. |
AID1907152 | Apparent permeability of the compound across apical to basolateral side in human Caco-2 cells at 10 uM incubated for 120 mins and measured by LC-MS/MS analysis | 2022 | European journal of medicinal chemistry, Jun-05, Volume: 236 | Discovery, optimization and evaluation of 1-(indolin-1-yl)ethan-1-ones as novel selective TRIM24/BRPF1 bromodomain inhibitors. |
AID1217706 | Time dependent inhibition of CYP2C9 (unknown origin) at 100 uM by LC/MS system | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
AID1810681 | Agonist activity at in human TLX LBD expressed in human HEK293T cells coexpressing Gal4-VP 16 assessed as increase in reporter activity measured after 14 hrs by luciferase reporter gene assay relative to control | 2021 | Journal of medicinal chemistry, 06-24, Volume: 64, Issue:12 | Propranolol Activates the Orphan Nuclear Receptor TLX to Counteract Proliferation and Migration of Glioblastoma Cells. |
AID187017 | Tested for maximum fall in mean arterial pressure in Spontaneously hypertensive rats after peroral administration by using 1% methyl cellulose as vehicle at 5 mg/kg | 1980 | Journal of medicinal chemistry, Jan, Volume: 23, Issue:1 | Heterocyclic analogues of the antihypertensive beta-adrenergic blocking agent (S)-2-[3-(ter-butylamino)-2-hydroxypropoxy]-3-cyanopyridine. |
AID1171962 | Hepatic clearance in CD-1 mouse liver microsomes at 0.75 uM incubated for 5 mins prior to NADPH addition measured after 30 mins by LC/MS/MS analysis | 2014 | Journal of medicinal chemistry, Dec-26, Volume: 57, Issue:24 | Discovery of a phosphodiesterase 9A inhibitor as a potential hypoglycemic agent. |
AID1473738 | Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
AID40716 | In vitro affinity constant against beta-2 adrenergic receptor from guinea pig trachea | 1983 | Journal of medicinal chemistry, Nov, Volume: 26, Issue:11 | beta 1-selective adrenoceptor antagonists. 1. Synthesis and beta-adrenergic blocking activity of a series of binary (aryloxy)propanolamines. |
AID744890 | Toxicity in rat spontaneous hypertensive model assessed as heart rate at 20 mg/kg, po measured at 0.5 hrs by tail-cuff method (Rvb = 406.5 +/- 13.15 bpm) | 2013 | Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9 | Novel hybrids of natural isochroman-4-one bearing N-substituted isopropanolamine as potential antihypertensive candidates. |
AID755840 | Passive permebility in wild-type MDCK cells | 2013 | Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13 | Discovery of (R)-4-cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro-1H-pyrazolo[4,3-c]quinoline (ELND006) and (R)-4-cyclopropyl-8-fluoro-5-(6-(trifluoromethyl)pyridin-3-ylsulfonyl)-4,5-dihydro-2H-pyrazolo[4,3-c]quinoline (ELND007 |
AID1571402 | Intrinsic clearance in rat liver microsomes at 2 uM preincubated for 5 mins followed by NADPH addition and measured up to 30 mins by LC-MS/MS analysis | |||
AID1262883 | Antagonist activity at human wild-type A3 receptor expressed in CHO-K1 cells assessed as IB MECA-induced cAMP by HTRF assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
AID1262880 | Antagonist activity at human 5-HT6 receptor expressed in 1321N1 cells assessed as seretonin-induced cAMP by HTRF assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
AID1667046 | Half life in mouse liver microsomes in presence of NADPH | 2020 | Bioorganic & medicinal chemistry letters, 04-01, Volume: 30, Issue:7 | Discovery and optimization of 4-oxo-2-thioxo-thiazolidinones as NOD-like receptor (NLR) family, pyrin domain-containing protein 3 (NLRP3) inhibitors. |
AID42031 | Tested for Beta-1 adrenergic receptor selectivity in canine cardiac tissue in anesthetized dogs | 1990 | Journal of medicinal chemistry, Oct, Volume: 33, Issue:10 | Synthesis of novel (aryloxy)propanolamines and related compounds possessing both class II and class III antiarrhythmic activity. |
AID781328 | pKa (acid-base dissociation constant) as determined by Luan ref: Pharm. Res. 2005 | 2014 | Pharmaceutical research, Apr, Volume: 31, Issue:4 | Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds. |
AID744880 | Toxicity in rat spontaneous hypertensive model assessed as heart rate at 20 mg/kg, po measured at 8 hrs by tail-cuff method (Rvb = 397.2 +/- 24.87 bpm) | 2013 | Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9 | Novel hybrids of natural isochroman-4-one bearing N-substituted isopropanolamine as potential antihypertensive candidates. |
AID28923 | Effective permeability measured with Caco-2 cells | 2001 | Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6 | High-throughput permeability pH profile and high-throughput alkane/water log P with artificial membranes. |
AID350216 | Dissociation constant, pKa of the compound | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10 | Lipophilicity of basic drugs measured by hydrophilic interaction chromatography. |
AID620389 | Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19 | Synthesis and characterization of high-affinity 4,4-difluoro-4-bora-3a,4a-diaza-s-indacene-labeled fluorescent ligands for human β-adrenoceptors. |
AID624625 | Apparent permeability (Papp) from basolateral to apical side determined in MDR1-MDCKII cells in the presence of inhibitor (2uM GF120919) | 2001 | The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2 | Rational use of in vitro P-glycoprotein assays in drug discovery. |
AID165816 | Percentage change of IOP in rabbits after 60 min administration (2.5%) of compound | 1988 | Journal of medicinal chemistry, Jan, Volume: 31, Issue:1 | Improved delivery through biological membranes. 26. Design, synthesis, and pharmacological activity of a novel chemical delivery system for beta-adrenergic blocking agents. |
AID50194 | Ability to lower arterial blood pressure in cat at 200 ug/kg; reversed | 1983 | Journal of medicinal chemistry, Jun, Volume: 26, Issue:6 | 1-(Aminomethyl)-6,7-dihydroxytetralin derivatives: synthesis and assessment of dopamine-like effects. |
AID192643 | Dose required to induce at least 50% inhibition of the isoprenaline-induced effect, administered intravenously | 1981 | Journal of medicinal chemistry, Aug, Volume: 24, Issue:8 | 2-Benzodioxinylaminoethanols: a new class of beta-adrenergic blocking and antihypertensive agents. |
AID20866 | Compound was determined for partition coefficient | 1984 | Journal of medicinal chemistry, Oct, Volume: 27, Issue:10 | Synthesis and beta-adrenergic blocking activity of new aliphatic and alicyclic oxime ethers. |
AID468629 | Ratio of permeability from apical to basolateral side over basolateral to apical side in human Caco-2 cells | 2009 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 19, Issue:20 | Phenylaminopyrimidines as inhibitors of Janus kinases (JAKs). |
AID444052 | Hepatic clearance in human | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination. |
AID1473739 | Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
AID165952 | Concentration in aqueous humor of rabbit after 60 min administration of compound | 1988 | Journal of medicinal chemistry, Jan, Volume: 31, Issue:1 | Improved delivery through biological membranes. 26. Design, synthesis, and pharmacological activity of a novel chemical delivery system for beta-adrenergic blocking agents. |
AID610064 | Apparent permeability from apical to basolateral side of human Caco2 cells at 10 uM by LC/MS/MS analysis | 2011 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16 | Effects of C7 substitutions in a high affinity microtubule-binding taxane on antitumor activity and drug transport. |
AID40707 | Apparent pA2 value for isoproterenol-induced vasodilation (beta2) evaluated against beta-2 adrenergic receptor in anesthetized dogs | 1985 | Journal of medicinal chemistry, Jun, Volume: 28, Issue:6 | Synthesis of 4'-hydroxypropranolol sulfate, a major non-beta-blocking propranolol metabolite in man. |
AID166144 | Cerebral biodistribution pattern of [123I]- ligand was evaluated in thalamus of anesthetized rabbit after Intravenous injection of 50 uCi after 2 hr | 1996 | Journal of medicinal chemistry, Aug-16, Volume: 39, Issue:17 | Synthesis and in vitro and in vivo characteristics of an iodinated analogue of the beta-adrenoceptor antagonist carazolol. |
AID1635247 | Apparent permeability from basolateral to apical side in human Caco2 cells at 10 uM incubated for 120 mins by LC-MS/MS analysis | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer. |
AID1061889 | Displacement of [3H]BTX-B from neuronal voltage-gated sodium channel in rat cerebral cortex synaptoneurosomes after 60 mins by scintillation counting | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1 | A highly predictive 3D-QSAR model for binding to the voltage-gated sodium channel: design of potent new ligands. |
AID1212331 | Drug uptake in lysosomes of human Fa2N-4 cells assessed as cellular partitioning at 1 uM after 5 mins by LC-MS analysis in presence of imipramine | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4 | Lysosomal sequestration (trapping) of lipophilic amine (cationic amphiphilic) drugs in immortalized human hepatocytes (Fa2N-4 cells). |
AID185135 | Beta blocking effect as percent inhibition of increased heart frequency induced by isoprenaline in 5-10 animals. | 1998 | Journal of medicinal chemistry, May-07, Volume: 41, Issue:10 | Synthesis and adrenergic activity of a new series of N-aryl dicyclopropyl ketone oxime ethers: SAR and stereochemical aspects. |
AID190410 | Antihypertensive activity expressed as percentage of base-line systolic blood pressure of base-line values in spontaneously hypertensive rats (SHR) was reported after 24 hr | 1987 | Journal of medicinal chemistry, Jun, Volume: 30, Issue:6 | Synthesis of a series of compounds related to betaxolol, a new beta 1-adrenoceptor antagonist with a pharmacological and pharmacokinetic profile optimized for the treatment of chronic cardiovascular diseases. |
AID1125256 | Antihypertensive activity in Wistar rat assessed as mean arterial pressure at 10 mg/kg, ip measured immediately at 60 mins (Rvb = 195.11 +/- 0.531 mmHg) | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Synthesis and pharmacological screening of some novel anti-hypertensive agents possessing 5-Benzylidene-2-(phenylimino)-thiazolidin-4-one ring. |
AID41488 | Selectivity for beta-2 adrenergic receptor | 1988 | Journal of medicinal chemistry, Nov, Volume: 31, Issue:11 | Modeling of beta-adrenoceptors based on molecular electrostatic potential studies of agonists and antagonists. |
AID327176 | Binding affinity to 50 uM human serum albumin at 10 uM by PAMPA method | 2008 | Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7 | New approach to measure protein binding based on a parallel artificial membrane assay and human serum albumin. |
AID1215128 | Ratio, ratio of fraction unbound in solid supported porcine brain membrane vesicles at 5 uM dosed as discrete compounds after 5 hrs by TRANSIL assay to fraction unbound in solid supported porcine brain membrane vesicles at 5 uM using four compound cocktai | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Brain tissue binding of drugs: evaluation and validation of solid supported porcine brain membrane vesicles (TRANSIL) as a novel high-throughput method. |
AID625280 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID42218 | In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations | 1983 | Journal of medicinal chemistry, Jul, Volume: 26, Issue:7 | Beta 1-selective adrenoceptor antagonists: examples of the 2-[4-[3-(substituted-amino)-2-hydroxypropoxy]phenyl]imidazole class. |
AID165681 | Biodistribution pattern of [123I]- ligand was evaluated in intestine of anesthetized rabbit after Intravenous injection of 50 uCi after 2 hr | 1996 | Journal of medicinal chemistry, Aug-16, Volume: 39, Issue:17 | Synthesis and in vitro and in vivo characteristics of an iodinated analogue of the beta-adrenoceptor antagonist carazolol. |
AID695938 | Apparent permeability across human Caco2 cells st 200 uM measured over 150 mins by LC/MS analysis | 2012 | Bioorganic & medicinal chemistry, Nov-01, Volume: 20, Issue:21 | Synthesis, biological activity and structure-activity relationship of endomorphin-1/substance P derivatives. |
AID1415060 | Apparent permeability across basolateral to apical side in human Caco2 cells at pH 6.5 to 7.5 after 2 hrs by LC/MS/MS analysis | 2018 | Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23 | Application of Sequential Palladium Catalysis for the Discovery of Janus Kinase Inhibitors in the Benzo[ c]pyrrolo[2,3- h][1,6]naphthyridin-5-one (BPN) Series. |
AID361719 | Apparent permeability from apical to basolateral side in human Caco-2 cells at 10 uM | 2008 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 18, Issue:16 | 4-(1,1-Dioxo-1,4-dihydro-1lambda6-benzo[1,4]thiazin-3-yl)-5-hydroxy-2H-pyridazin-3-ones as potent inhibitors of HCV NS5B polymerase. |
AID1212319 | Drug uptake in lysosomes of human Fa2N-4 cells assessed as cellular partitioning at 1 uM measured at 10 mins by LC-MS analysis in presence of ammonium chloride | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4 | Lysosomal sequestration (trapping) of lipophilic amine (cationic amphiphilic) drugs in immortalized human hepatocytes (Fa2N-4 cells). |
AID1668035 | Antiproliferative activity against human A375 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay | 2020 | Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9 | Drug repurposing and rediscovery: Design, synthesis and preliminary biological evaluation of 1-arylamino-3-aryloxypropan-2-ols as anti-melanoma agents. |
AID1365726 | Apparent permeability of the compound across apical side to basolateral side in human Caco2 cells monolayer at 10 uM after 1 hr by LC-MS/MS analysis | 2017 | Bioorganic & medicinal chemistry, 11-01, Volume: 25, Issue:21 | The antitubercular activity of various nitro(triazole/imidazole)-based compounds. |
AID26250 | Compound was evaluated for distribution coefficient | 1986 | Journal of medicinal chemistry, Nov, Volume: 29, Issue:11 | 6,7-Dichloro-1-(3,4,5-trimethoxybenzyl)-1,2,3,4-tetrahydroisoquinoline . A structurally novel beta-adrenergic receptor blocking agent. |
AID165802 | Percentage change of IOP in rabbits after 2 hr administration (2.5%) of compound | 1988 | Journal of medicinal chemistry, Jan, Volume: 31, Issue:1 | Improved delivery through biological membranes. 26. Design, synthesis, and pharmacological activity of a novel chemical delivery system for beta-adrenergic blocking agents. |
AID48727 | Hypotensive activity in cat following i.v. administration of 1 mg/kg expressed as fall in blood pressure | 2004 | Bioorganic & medicinal chemistry letters, Jun-07, Volume: 14, Issue:11 | 1- and 2-substituted naphthalenes: a new class of potential hypotensive agents. |
AID1135374 | Local anesthetic activity in ICR Swiss mouse assessed as inhibition of pain reflex response at 1%, id relative to control | 1977 | Journal of medicinal chemistry, Jul, Volume: 20, Issue:7 | beta-Adrenoceptor blocking activity of halogenated thienylethanolamine derivatives. |
AID7812 | In vitro rate of absorption observed as Caco-2 permeability in humans | 2002 | Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2 | Graphical model for estimating oral bioavailability of drugs in humans and other species from their Caco-2 permeability and in vitro liver enzyme metabolic stability rates. |
AID1262881 | Antagonist activity at human wild-type 5-HT7 receptor expressed in HEK cells assessed as seretonin-induced cAMP by HTRF assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
AID1053287 | Fraction unbound in rat plasma at 5 uM after 4 hrs by equilibrium dialysis method | 2013 | Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21 | Design, synthesis and discovery of picomolar selective α4β2 nicotinic acetylcholine receptor ligands. |
AID625287 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID168803 | Compound was tested for oral salidiuretic activity (control/drug treatment value) in rats expressed in Na+, mequiv/6 hr at a dose of 128 mg/kg; 0.216/0.263 | 1986 | Journal of medicinal chemistry, Jan, Volume: 29, Issue:1 | [p-[(Thienylcarbonyl)amino]phenoxy]propanolamines derivatives as diuretic and beta-adrenergic receptor blocking agents. |
AID1079940 | Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source] | |||
AID1526020 | Permeability in MDCK-MDR1 cells assessed as drug recovery | 2019 | Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18 | Heteroaryl Phosphonates as Noncovalent Inhibitors of Both Serine- and Metallocarbapenemases. |
AID1262905 | Agonist activity at human wild-type A2A receptor expressed in CHO-K1 cells assessed as cAMP level by HTRF assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
AID620390 | Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19 | Synthesis and characterization of high-affinity 4,4-difluoro-4-bora-3a,4a-diaza-s-indacene-labeled fluorescent ligands for human β-adrenoceptors. |
AID48143 | Hypotensive activity in cat following i.v. administration of 1 mg/kg expressed as fall in blood pressure | 2004 | Bioorganic & medicinal chemistry letters, Jun-07, Volume: 14, Issue:11 | 1- and 2-substituted naphthalenes: a new class of potential hypotensive agents. |
AID1585794 | Apparent permeability across apical to basolateral side in human Caco2 cells assessed as mean drug recovery at 2 uM after 2 hrs by lucifer yellow dye-based LC-MS/MS analysis | 2018 | Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24 | Design, Synthesis, and Biological Evaluation of 2-Nitroimidazopyrazin-one/-es with Antitubercular and Antiparasitic Activity. |
AID58409 | Time taken for 80% recovery at a dose of 1.3 microg (3-h infusion period) | 1984 | Journal of medicinal chemistry, Aug, Volume: 27, Issue:8 | [(Arylcarbonyl)oxy]propanolamines. 1. Novel beta-blockers with ultrashort duration of action. |
AID678712 | Inhibition of human CYP1A2 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using ethoxyresorufin as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
AID1203236 | Ratio of apparent permeability across apical to basolateral over basolateral to apical side in human Caco2 cells in presence of 0.1% bovine serum albumin | 2015 | Journal of medicinal chemistry, Apr-09, Volume: 58, Issue:7 | Discovery and optimization of novel antagonists to the human neurokinin-3 receptor for the treatment of sex-hormone disorders (Part I). |
AID19006 | Calculated membrane partition coefficient (Kmemb) | 2004 | Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7 | Surface activity profiling of drugs applied to the prediction of blood-brain barrier permeability. |
AID744926 | Antihypertensive activity in rat spontaneous hypertensive model assessed as systolic arterial blood pressure at 20 mg/kg, po measured at 0.5 hrs by tail-cuff method (Rvb = 178.5 +/- 10.13 mmHg) | 2013 | Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9 | Novel hybrids of natural isochroman-4-one bearing N-substituted isopropanolamine as potential antihypertensive candidates. |
AID1212327 | Drug uptake in lysosomes of human Fa2N-4 cells assessed as cellular partitioning at 1 uM after 5 mins by LC-MS analysis in presence of ammonium chloride, nigericin and monensin | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4 | Lysosomal sequestration (trapping) of lipophilic amine (cationic amphiphilic) drugs in immortalized human hepatocytes (Fa2N-4 cells). |
AID42210 | Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated guinea pig trachea | 1987 | Journal of medicinal chemistry, Jun, Volume: 30, Issue:6 | Synthesis of a series of compounds related to betaxolol, a new beta 1-adrenoceptor antagonist with a pharmacological and pharmacokinetic profile optimized for the treatment of chronic cardiovascular diseases. |
AID65751 | Competitive binding assay against Dopamine receptor D2 in rat striatal membranes and [125I]-IBF radioligand | 1990 | Journal of medicinal chemistry, Jan, Volume: 33, Issue:1 | Synthesis and characterization of iodobenzamide analogues: potential D-2 dopamine receptor imaging agents. |
AID1895165 | Permeability across apical to basal side in human Caco-2 cells assessed as drug recovery preincubated with verapamil for 30 mins followed by compound addition measured at 0.5 to 2 hrs by LC-MS analysis relative to control | 2021 | Journal of medicinal chemistry, 06-24, Volume: 64, Issue:12 | Interplay among Conformation, Intramolecular Hydrogen Bonds, and Chameleonicity in the Membrane Permeability and Cyclophilin A Binding of Macrocyclic Peptide Cyclosporin O Derivatives. |
AID678717 | Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-benzyloxyquinoline as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
AID1203133 | Apparent permeability of the compound at RT after 24 hrs by PAMPA | 2015 | Journal of medicinal chemistry, Mar-26, Volume: 58, Issue:6 | A novel cell-permeable, selective, and noncompetitive inhibitor of KAT3 histone acetyltransferases from a combined molecular pruning/classical isosterism approach. |
AID1212329 | Drug uptake in lysosomes of human Fa2N-4 cells assessed as cellular partitioning at 1 uM after 5 mins by LC-MS analysis in presence of dextromethorphan | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4 | Lysosomal sequestration (trapping) of lipophilic amine (cationic amphiphilic) drugs in immortalized human hepatocytes (Fa2N-4 cells). |
AID625290 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID1135963 | Reversal of isoproterenol-induced increase in mean arterial blood pressure in cat assessed as depressor phase at 2.5 mg/kg, iv | 1978 | Journal of medicinal chemistry, Jan, Volume: 21, Issue:1 | Adrenoceptor blocking agents. 2. 2-(alpha-Hydroxyarylmethyl)-3,3-dimethylaziridines, a new class of selective beta2-adrenoceptor antagonists. |
AID1221021 | Drug distribution in healthy Wistar rat perfused liver assessed as equilibrium amount ratio charactering fast binding process at 8 mM after 10 mins | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4 | Hepatic pharmacokinetics of cationic drugs in a high-fat emulsion-induced rat model of nonalcoholic steatohepatitis. |
AID29845 | Estimation of fraction absorbed (Fa) in the human intestine using biosensor technology. | 2000 | Journal of medicinal chemistry, Jun-01, Volume: 43, Issue:11 | SPR biosensor studies of the direct interaction between 27 drugs and a liposome surface: correlation with fraction absorbed in humans. |
AID1262898 | Antagonist activity at human wild-type opioid-mu receptor expressed in CHO-K1 cells assessed as DAMGO-induced cAMP by HTRF assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
AID1222767 | Unbound renal clearance in human | 2013 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5 | Which metabolites circulate? |
AID166296 | Effect on IOP of rabbits 30 mins after administration (1%) | 1988 | Journal of medicinal chemistry, Jan, Volume: 31, Issue:1 | Improved delivery through biological membranes. 26. Design, synthesis, and pharmacological activity of a novel chemical delivery system for beta-adrenergic blocking agents. |
AID218533 | beta-adrenoceptor blocking activity of the perorally administered compound was evaluated by inhibition of isiprenaline-induced tachycardia in rats | 1993 | Journal of medicinal chemistry, Jan-08, Volume: 36, Issue:1 | o-Chlorobenzenesulfonamidic derivatives of (aryloxy)propanolamines as beta-blocking/diuretic agents. |
AID1135151 | Hypotensive activity at guinea pig assessed as decrease in blood pressure at 50 mg/kg, po after 5 hrs (Rvb = 112 +/- 2.6 to 122 +/- 2.7 mmHg) | 1977 | Journal of medicinal chemistry, Mar, Volume: 20, Issue:3 | Synthesis and adrenergic beta-blocking activity of some 1,3-benzodioxole derivatives. |
AID171503 | Blood pressure of the urethane-anesthetized normotensive Wistar rat was tested 5 min after inducing the compound on dose of 1.0 mg/kg | 1994 | Journal of medicinal chemistry, Apr-01, Volume: 37, Issue:7 | Guaiacoxypropanolamine derivatives of capsaicin: a new family of beta-adrenoceptor blockers with intrinsic cardiotonic properties. |
AID332086 | Apparent permeability from apical to basolateral side of human Caco-2 cells at 10 uM | 2008 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 18, Issue:11 | Novel HCV NS5B polymerase inhibitors derived from 4-(1',1'-dioxo-1',4'-dihydro-1'lambda6-benzo[1',2',4']thiadiazin-3'-yl)-5-hydroxy-2H-pyridazin-3-ones: Part 4. Optimization of DMPK properties. |
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AID394756 | Inhibition of [3H]norepinephrine binding to Escherichia coli Qsec by liposome-based scintillation counting assay | 2008 | Science (New York, N.Y.), Aug-22, Volume: 321, Issue:5892 | Targeting QseC signaling and virulence for antibiotic development. |
AID41152 | Concentration effective against displacing [3H]dihydroalprenolol from beta adrenergic receptor from canine ventricular tissue | 1987 | Journal of medicinal chemistry, Apr, Volume: 30, Issue:4 | Synthesis and antiarrhythmic activity of novel 3-alkyl-1-[omega-[4-[(alkylsulfonyl)amino]phenyl]-omega- hydroxyalkyl]-1H-imidazolium salts and related compounds. |
AID1874537 | Apparent permeability across basolateral to apical side in human Caco-2 cells measured after 120 mins by LC-MS/MS analysis | 2022 | Journal of medicinal chemistry, 09-08, Volume: 65, Issue:17 | Development, Optimization, and In Vivo Validation of New Imidazopyridine Chemotypes as Dual TLR7/TLR9 Antagonists through Activity-Directed Sequential Incorporation of Relevant Structural Subunits. |
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AID1509218 | Otoprotective activity against gentamicin-induced outer hair cell death in CD-1 mouse cochlea at 20 uM after 48 hrs by TRITC-phalloidin staining-based microscopic analysis relative to control | 2019 | Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11 | Design, Synthesis, and Biological Evaluation of a New Series of Carvedilol Derivatives That Protect Sensory Hair Cells from Aminoglycoside-Induced Damage by Blocking the Mechanoelectrical Transducer Channel. |
AID312896 | Partition coefficient, log P by UPLC method | 2008 | Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3 | High-throughput log P determination by ultraperformance liquid chromatography: a convenient tool for medicinal chemists. |
AID1335249 | Effective permeability of the compound incubated for 2 hrs by PAMPA-BBB assay | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | Novel multi-target-directed ligands for Alzheimer's disease: Combining cholinesterase inhibitors and 5-HT |
AID1217709 | Time dependent inhibition of CYP3A4 (unknown origin) at 100 uM by LC/MS system | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
AID1563154 | Metabolic stability in dog liver microsomes assessed as compound remaining after 30 mins | 2019 | Journal of medicinal chemistry, 07-11, Volume: 62, Issue:13 | ( |
AID1368448 | Apparent permeability in MDCK2-MDR1 cells at 3 uM incubated over 150 mins at 37 degC by LC-MS/MS method | 2018 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 28, Issue:2 | Assessment of a pretomanid analogue library for African trypanosomiasis: Hit-to-lead studies on 6-substituted 2-nitro-6,7-dihydro-5H-imidazo[2,1-b][1,3]thiazine 8-oxides. |
AID604023 | Ratio of total drug level in brain to plasma in Sprague-Dawley rat administered in casettes of 2/3 drugs at 4 hr constant rate intravenous infusions using flow rate of 1 (ml/kg)/hr corresponding to dosage rate of 2 (umol/kg)/hr by LC-MS/MS method | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20 | Structure-brain exposure relationships in rat and human using a novel data set of unbound drug concentrations in brain interstitial and cerebrospinal fluids. |
AID451155 | Permeability by PAMPA | 2009 | Bioorganic & medicinal chemistry, Sep-01, Volume: 17, Issue:17 | Fluorinated pyridinium oximes as potential reactivators for acetylcholinesterases inhibited by paraoxon organophosphorus agent. |
AID744920 | Antihypertensive activity in rat spontaneous hypertensive model assessed as systolic arterial blood pressure at 20 mg/kg, po measured at 4 hrs by tail-cuff method (Rvb = 172.9 +/- 10.21 mmHg) | 2013 | Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9 | Novel hybrids of natural isochroman-4-one bearing N-substituted isopropanolamine as potential antihypertensive candidates. |
AID1668036 | Inhibition of colony formation in human SK-MEL-28 cells at 5 to 100 uM supplemented with fresh medium containing compound every 72 hrs for 2 weeks by crystal violet staining based assay | 2020 | Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9 | Drug repurposing and rediscovery: Design, synthesis and preliminary biological evaluation of 1-arylamino-3-aryloxypropan-2-ols as anti-melanoma agents. |
AID1137383 | Antihypertensive activity in spontaneously hypertensive Wistar-Okamoto rat assessed as duration of action at 1.25 mg/kg, po | 1979 | Journal of medicinal chemistry, Nov, Volume: 22, Issue:11 | Symbiotic approach to drug design: antihypertensive beta-adrenergic blocking agents. |
AID1262896 | Antagonist activity at human wild-type opioid-delta 1 receptor expressed in CHO-K1 cells assessed as DPDPE-induced cAMP by HTRF assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
AID165797 | Percentage change of IOP in rabbits after 0 min administration (2.5%) of compound | 1988 | Journal of medicinal chemistry, Jan, Volume: 31, Issue:1 | Improved delivery through biological membranes. 26. Design, synthesis, and pharmacological activity of a novel chemical delivery system for beta-adrenergic blocking agents. |
AID21277 | Permeability through isolated albino rabbit cornea | 1988 | Journal of medicinal chemistry, Feb, Volume: 31, Issue:2 | (Acyloxy)alkyl carbamates as novel bioreversible prodrugs for amines: increased permeation through biological membranes. |
AID1079931 | Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source] | |||
AID432063 | Apparent permeability at pH 7.4 after 24 hrs by PAMPA method | 2009 | European journal of medicinal chemistry, Sep, Volume: 44, Issue:9 | Determination of permeability and lipophilicity of pyrazolo-pyrimidine tyrosine kinase inhibitors and correlation with biological data. |
AID781326 | pKa (acid-base dissociation constant) as determined by Avdeef ref: DOI: 10.1002/047145026X | 2014 | Pharmaceutical research, Apr, Volume: 31, Issue:4 | Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds. |
AID26362 | Ionization constant (pKa) | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5 | Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics. |
AID1350727 | Aqueous solubility in PBS buffer at pH 7.4 at 100 uM after 1 hr by LC-MS/MS analysis | 2018 | Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14 | Optimization of Isothiazolo[4,3- b]pyridine-Based Inhibitors of Cyclin G Associated Kinase (GAK) with Broad-Spectrum Antiviral Activity. |
AID1510594 | Binding affinity to recombinant human C-terminal soluble epoxide hydrolase-hydrolase domain (222 to 555 residues) expressed in Escherichia coli BL21(DE3) assessed as change in melting temperature at 200 uM by SYPRO orange dye-based differential scanning f | 2019 | ACS medicinal chemistry letters, Jun-13, Volume: 10, Issue:6 | Computer-Aided Selective Optimization of Side Activities of Talinolol. |
AID1365728 | Efflux ratio of apparent permeability from basolateral to apical over apical to basolateral side in human Caco2 cells monolayer at 10 uM after 1 hr by LC-MS/MS analysis | 2017 | Bioorganic & medicinal chemistry, 11-01, Volume: 25, Issue:21 | The antitubercular activity of various nitro(triazole/imidazole)-based compounds. |
AID232338 | Ratio of rat Beta-2 to Beta-1 adrenoceptor antagonism | 1983 | Journal of medicinal chemistry, Nov, Volume: 26, Issue:11 | beta 1-selective adrenoceptor antagonists. 1. Synthesis and beta-adrenergic blocking activity of a series of binary (aryloxy)propanolamines. |
AID1212311 | Drug uptake in lysosomes of human Fa2N-4 cells assessed as cellular partitioning at 1 uM preincubated with chloroquine followed by compound treatment measured after 5 mins by LC-MS analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4 | Lysosomal sequestration (trapping) of lipophilic amine (cationic amphiphilic) drugs in immortalized human hepatocytes (Fa2N-4 cells). |
AID361982 | Membrane permeability assessed as passive transport after 4 hrs by PAMPA in presence of 20% 1-propanol | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16 | Toward an optimal blood-brain barrier shuttle by synthesis and evaluation of peptide libraries. |
AID620387 | Displacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cells | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19 | Synthesis and characterization of high-affinity 4,4-difluoro-4-bora-3a,4a-diaza-s-indacene-labeled fluorescent ligands for human β-adrenoceptors. |
AID1221013 | Intrinsic elimination clearance in healthy Wistar rat perfused liver assessed per gm of liver at 8 mM after 10 mins | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4 | Hepatic pharmacokinetics of cationic drugs in a high-fat emulsion-induced rat model of nonalcoholic steatohepatitis. |
AID624615 | Specific activity of expressed human recombinant UGT2B10 | 2000 | Annual review of pharmacology and toxicology, , Volume: 40 | Human UDP-glucuronosyltransferases: metabolism, expression, and disease. |
AID266007 | Antagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cells | 2006 | Journal of medicinal chemistry, Jun-15, Volume: 49, Issue:12 | Role of Tyr(356(7.43)) and Ser(190(4.57)) in antagonist binding in the rat beta1-adrenergic receptor. |
AID1135372 | In vivo inhibition of beta-adrenoceptor in histamine-treated guinea pig assessed as inhibition of isoproterenol-induced bronchodilator effect at 0.01 mg/kg, iv administered 3 mins prior to histamine/isoproterenol challenge relative to control | 1977 | Journal of medicinal chemistry, Jul, Volume: 20, Issue:7 | beta-Adrenoceptor blocking activity of halogenated thienylethanolamine derivatives. |
AID1135149 | Hypotensive activity at guinea pig assessed as decrease in blood pressure at 50 mg/kg, po after 1 hr (Rvb = 112 +/- 2.6 to 122 +/- 2.7 mmHg) | 1977 | Journal of medicinal chemistry, Mar, Volume: 20, Issue:3 | Synthesis and adrenergic beta-blocking activity of some 1,3-benzodioxole derivatives. |
AID1623705 | Apparent permeability of compound at 10 uM at pH 7.4 after 12 hrs by PAMPA | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Investigation of stereoisomeric bisarylethenesulfonic acid esters for discovering potent and selective PTP1B inhibitors. |
AID266008 | Antagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cells | 2006 | Journal of medicinal chemistry, Jun-15, Volume: 49, Issue:12 | Role of Tyr(356(7.43)) and Ser(190(4.57)) in antagonist binding in the rat beta1-adrenergic receptor. |
AID134406 | Lethal dose in mice (LD50) (following i.v. dosing) | 1984 | Journal of medicinal chemistry, Sep, Volume: 27, Issue:9 | Synthesis and antiarrhythmic activity of new 1-[1-[2-[3-(alkylamino)-2-hydroxypropoxy]phenyl]vinyl]-1 H-imidazoles and related compounds. |
AID1223488 | 1-Octanol-water distribution coefficient, log D of the compound at pH 7.4 | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2 | Predicting phenolic acid absorption in Caco-2 cells: a theoretical permeability model and mechanistic study. |
AID467613 | Volume of distribution at steady state in human | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Prediction of volume of distribution values in human using immobilized artificial membrane partitioning coefficients, the fraction of compound ionized and plasma protein binding data. |
AID481441 | Aqueous diffusivity at 37C | 2010 | Journal of medicinal chemistry, May-13, Volume: 53, Issue:9 | How well can the Caco-2/Madin-Darby canine kidney models predict effective human jejunal permeability? |
AID681961 | TP_TRANSPORTER: inhibition of cimetidine uptake (Cimetidine: 100 uM, Propranolol: 1000 uM) in OCT2-expressing mIMCD3 cells | 2000 | British journal of pharmacology, Sep, Volume: 131, Issue:1 | The organic cation transporter OCT2 mediates the uptake of beta-adrenoceptor antagonists across the apical membrane of renal LLC-PK(1) cell monolayers. |
AID29337 | Ionisation constant (pKa) | 2002 | Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13 | Prediction of volume of distribution values in humans for neutral and basic drugs using physicochemical measurements and plasma protein binding data. |
AID1262913 | Agonist activity at human wild-type M3 receptor expressed in CHO-K1 cells assessed as calcium level by FDSS assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
AID1302321 | Metabolic stability in human liver microsomes assessed as parent compound remaining at 1 uM incubated for 30 mins in presence of NADPH by LC-MS analysis | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8 | Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitor Agents: Optimization of Diarylanilines with High Potency against Wild-Type and Rilpivirine-Resistant E138K Mutant Virus. |
AID65625 | Tested for binding affinity against dopamine receptor D3 expressed in Sf9 cells. | 1993 | Journal of medicinal chemistry, May-14, Volume: 36, Issue:10 | Synthesis of (R,S)-2'-trans-7-hydroxy-2-[N-n-propyl-N-(3'-iodo-2'- propenyl)-amino]tetralin (trans-7-OH-PIPAT): a new D3 dopamine receptor ligand. |
AID192444 | Systolic blood pressure (SBP) in anesthetized spontaneously hypertensive rats (SHR) before administration of 75 mg/kg dose perorally. | 1989 | Journal of medicinal chemistry, Jan, Volume: 32, Issue:1 | Flavones. 2. Synthesis and structure-activity relationship of flavodilol and its analogues, a novel class of antihypertensive agents with catecholamine depleting properties. |
AID229400 | Selectivity of inhibition at beta-1 versus beta-2 adrenergic receptors, ratio of pA2 values | 1988 | Journal of medicinal chemistry, Nov, Volume: 31, Issue:11 | Synthesis and beta-adrenergic antagonism of 2-(aryloxy)-1-(2-piperidyl)ethanols. |
AID1510598 | Inhibition of soluble epoxide hydrolase in human HepG2 cells assessed as reduction in conversion of EET to DHET up to 1 uM using (+/-)14(15)-EET-d11 as substrate preincubated for 15 mins followed by substrate addition and measured after 10 mins by LC-MS/M | 2019 | ACS medicinal chemistry letters, Jun-13, Volume: 10, Issue:6 | Computer-Aided Selective Optimization of Side Activities of Talinolol. |
AID1207690 | Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes | 2012 | Journal of applied toxicology : JAT, Oct, Volume: 32, Issue:10 | Predictive model for L-type channel inhibition: multichannel block in QT prolongation risk assessment. |
AID1262917 | Agonist activity at human wild-type D2 receptor expressed in CHO-K1 cells assessed as cAMP level by HTRF assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
AID699539 | Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake at 20 uM by scintillation counting | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10 | Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions. |
AID127207 | Compound was evaluated for ventricular tachycardia activity in intravenously administered mice, 3 min before aconitine infusion, at a dose of 10 mg/kg; S=significant antiarrhythmic effect | 1984 | Journal of medicinal chemistry, Sep, Volume: 27, Issue:9 | Synthesis and antiarrhythmic activity of new 1-[1-[2-[3-(alkylamino)-2-hydroxypropoxy]phenyl]vinyl]-1 H-imidazoles and related compounds. |
AID21854 | In vivo clearance in dog. | 1999 | Journal of medicinal chemistry, Dec-16, Volume: 42, Issue:25 | Combining in vitro and in vivo pharmacokinetic data for prediction of hepatic drug clearance in humans by artificial neural networks and multivariate statistical techniques. |
AID387875 | Apparent permeability across human Caco-2 cell membrane | 2008 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20 | Novel HCV NS5B polymerase inhibitors derived from 4-(1',1'-dioxo-1',4'-dihydro-1'lambda(6)-benzo[1',2',4']thiadiazin-3'-yl)-5-hydroxy-2H-pyridazin-3-ones. Part 5: Exploration of pyridazinones containing 6-amino-substituents. |
AID166085 | Concentration of propranolone oxime in cornea of rabbit after 120 min administration of compound; N/A= no oxime can be present after administration of propranolone hydrochloride | 1988 | Journal of medicinal chemistry, Jan, Volume: 31, Issue:1 | Improved delivery through biological membranes. 26. Design, synthesis, and pharmacological activity of a novel chemical delivery system for beta-adrenergic blocking agents. |
AID33116 | Relative adrenoceptor blocking activity (DR10) was recorded for the antagonism of Phenylephrine-induced vasopressor responses in Alpha adrenergic receptor blockade the anesthetized dog | 1982 | Journal of medicinal chemistry, Jun, Volume: 25, Issue:6 | Arylethanolamines derived from salicylamide with alpha- and beta-adrenoceptor blocking activities. Preparation of labetalol, its enantiomers, and related salicylamides. |
AID165956 | Concentration in cornea of rabbit after 30 min administration of compound | 1988 | Journal of medicinal chemistry, Jan, Volume: 31, Issue:1 | Improved delivery through biological membranes. 26. Design, synthesis, and pharmacological activity of a novel chemical delivery system for beta-adrenergic blocking agents. |
AID1669464 | Ratio of IC50 for antagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under constant violet light conditions by FRET assay | 2020 | Journal of medicinal chemistry, 08-13, Volume: 63, Issue:15 | Photoswitchable Antagonists for a Precise Spatiotemporal Control of β |
AID624606 | Specific activity of expressed human recombinant UGT1A1 | 2000 | Annual review of pharmacology and toxicology, , Volume: 40 | Human UDP-glucuronosyltransferases: metabolism, expression, and disease. |
AID1365715 | Apparent permeability of the compound across basolateral side to apical side in human Caco2 cells monolayer at 10 uM after 2 hrs by LC-MS/MS analysis | 2017 | Bioorganic & medicinal chemistry, 11-01, Volume: 25, Issue:21 | The antitubercular activity of various nitro(triazole/imidazole)-based compounds. |
AID624622 | Apparent permeability (Papp) from apical to basolateral side determined in MDR1-MDCKII cells | 2001 | The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2 | Rational use of in vitro P-glycoprotein assays in drug discovery. |
AID63503 | Concentration that causes a 20% increase in APD95 (action potential duration at 95% repolarization) from control value in anesthetized dogs; (-)1.0, (-)3.5, (-)2.5 | 1990 | Journal of medicinal chemistry, Oct, Volume: 33, Issue:10 | Synthesis of novel (aryloxy)propanolamines and related compounds possessing both class II and class III antiarrhythmic activity. |
AID1365716 | Efflux ratio of apparent permeability from basolateral to apical over apical to basolateral side in human Caco2 cells monolayer at 10 uM after 2 hrs by LC-MS/MS analysis | 2017 | Bioorganic & medicinal chemistry, 11-01, Volume: 25, Issue:21 | The antitubercular activity of various nitro(triazole/imidazole)-based compounds. |
AID166293 | Effect on IOP of rabbits 2 hr after administration (1%) | 1988 | Journal of medicinal chemistry, Jan, Volume: 31, Issue:1 | Improved delivery through biological membranes. 26. Design, synthesis, and pharmacological activity of a novel chemical delivery system for beta-adrenergic blocking agents. |
AID91481 | Binding constant against human serum albumin (HSA) | 2001 | Journal of medicinal chemistry, Dec-06, Volume: 44, Issue:25 | Cheminformatic models to predict binding affinities to human serum albumin. |
AID41890 | Tested for intrinsic sympathomimetic activity (ISA); Pure antagonist | 1988 | Journal of medicinal chemistry, Nov, Volume: 31, Issue:11 | Modeling of beta-adrenoceptors based on molecular electrostatic potential studies of agonists and antagonists. |
AID1733541 | Permeability across apical to basolateral side in human Caco2 cells assessed as mass balance at 20 uM after 2 hrs by LC-MS analysis | 2021 | Bioorganic & medicinal chemistry, 05-01, Volume: 37 | Systematic evaluation of structure-property relationships and pharmacokinetics in 6-(hetero)aryl-substituted matched pair analogs of amiloride and 5-(N,N-hexamethylene)amiloride. |
AID467612 | Fraction unbound in human plasma | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Prediction of volume of distribution values in human using immobilized artificial membrane partitioning coefficients, the fraction of compound ionized and plasma protein binding data. |
AID1810693 | Induction of apoptosis in human T98G cells assessed as viable cells at 100 nM measured after 72 hrs by propidium iodide staining based flow cytometry | 2021 | Journal of medicinal chemistry, 06-24, Volume: 64, Issue:12 | Propranolol Activates the Orphan Nuclear Receptor TLX to Counteract Proliferation and Migration of Glioblastoma Cells. |
AID604024 | Unbound brain to plasma concentration ratio in Sprague-Dawley rat administered in casettes of 2/3 drugs at 4 hr constant rate intravenous infusions using flow rate of 1 (ml/kg)/hr corresponding to dosage rate of 2 (umol/kg)/hr | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20 | Structure-brain exposure relationships in rat and human using a novel data set of unbound drug concentrations in brain interstitial and cerebrospinal fluids. |
AID604025 | Unbound CSF to plasma concentration ratio in Sprague-Dawley rat administered in casettes of 2/3 drugs at 4 hr constant rate intravenous infusions using flow rate of 1 (ml/kg)/hr corresponding to dosage rate of 2 (umol/kg)/hr by LC-MS/MS method | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20 | Structure-brain exposure relationships in rat and human using a novel data set of unbound drug concentrations in brain interstitial and cerebrospinal fluids. |
AID327171 | Apparent permeability across parallel artificial membrane at 10 uM in presence of 50 uM human serum albumin | 2008 | Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7 | New approach to measure protein binding based on a parallel artificial membrane assay and human serum albumin. |
AID41347 | Antagonistic activity against beta-2 adrenergic receptor as inhibition of vasopressor response in rats | 1985 | Journal of medicinal chemistry, Nov, Volume: 28, Issue:11 | Beta-adrenoceptor activity of the stereoisomers of the bufuralol alcohol and ketone metabolites. |
AID1382492 | Apparent permeability from basolateral to apical side in human Caco2 cells at 10 uM after 60 mins by LC-MS/MS analysis | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Alkynyl-containing phenylthiazoles: Systemically active antibacterial agents effective against methicillin-resistant Staphylococcus aureus (MRSA). |
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AID540231 | Dose normalised AUC in dog after po administration | 2005 | Xenobiotica; the fate of foreign compounds in biological systems, Feb, Volume: 35, Issue:2 | Comparative evaluation of oral systemic exposure of 56 xenobiotics in rat, dog, monkey and human. |
AID79519 | Positive inotropic effect was evaluated on atrial muscles of the guinea pig | 1994 | Journal of medicinal chemistry, Apr-01, Volume: 37, Issue:7 | Guaiacoxypropanolamine derivatives of capsaicin: a new family of beta-adrenoceptor blockers with intrinsic cardiotonic properties. |
AID1135311 | In vivo inhibition of beta-2 adrenergic receptor in cat assessed as inhibition of isoproterenol-induced vasodepressor response at ED50 administered as 30 mins of infusion measured at 30 mins relative to control | 1977 | Journal of medicinal chemistry, May, Volume: 20, Issue:5 | Beta-Adrenergic blocking agents. 15. 1-Substituted ureidophenoxy-3-amino-2-propanols. |
AID1407671 | Efflux ratio of apparent permeability from basolateral to apical over apical to basolateral side in human Caco2 cells after 120 mins by LC-MS/MS analysis | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Hedgehog pathway inhibitors of the acylthiourea and acylguanidine class show antitumor activity on colon cancer in vitro and in vivo. |
AID1810688 | Effect on TLX regulated gene expression in human T98G cells assessed as induction of mRNA expression at 50 uM after 8 hrs by qRT-PCR analysis | 2021 | Journal of medicinal chemistry, 06-24, Volume: 64, Issue:12 | Propranolol Activates the Orphan Nuclear Receptor TLX to Counteract Proliferation and Migration of Glioblastoma Cells. |
AID1738187 | Effective permeability of compound at 200 uM measured after 4 hrs by PAMPA-BBB assay | |||
AID462612 | Permeability across artificial membrane assessed as compound transport at 200 uM after 4 hrs by PAMPA using HPLC/MS method | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6 | N-methyl phenylalanine-rich peptides as highly versatile blood-brain barrier shuttles. |
AID744927 | Antagonist activity at beta1 adrenoreceptor in Sprague-Dawley rat left atrium assessed as inhibition of isoprenaline-induced contraction at 1 uM incubated for 5 mins prior to isoprenaline-induction | 2013 | Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9 | Novel hybrids of natural isochroman-4-one bearing N-substituted isopropanolamine as potential antihypertensive candidates. |
AID1262874 | Chemical stability of compound in DMSO assessed as compound remaining at 10 mg/ml after 1 day at room temperature | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
AID1262944 | Ratio of drug level in brain to plasma in Swiss mouse at 5 mg/kg, sc | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
AID40703 | Tested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogs | 1990 | Journal of medicinal chemistry, Oct, Volume: 33, Issue:10 | Synthesis of novel (aryloxy)propanolamines and related compounds possessing both class II and class III antiarrhythmic activity. |
AID625281 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID227878 | Broncho-selectivity for beta-2 and beta-1 adrenergic receptor (difference between the tracheal and atrial pA2 values) | 1984 | Journal of medicinal chemistry, Oct, Volume: 27, Issue:10 | Synthesis and beta-adrenergic blocking activity of new aliphatic and alicyclic oxime ethers. |
AID1220985 | Extraction ratio of the compound in perfused liver of high-fat emulsion-induced nonalcoholic steatohepatitis Wistar rat at 8 mM after 10 mins | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4 | Hepatic pharmacokinetics of cationic drugs in a high-fat emulsion-induced rat model of nonalcoholic steatohepatitis. |
AID1075746 | Half life in human liver microsomes at 1 uM by LC-MS analysis | 2014 | Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4 | Optimization of 4-(N-cycloamino)phenylquinazolines as a novel class of tubulin-polymerization inhibitors targeting the colchicine site. |
AID1212334 | Drug uptake in lysosomes of human Fa2N-4 cells assessed as cellular partitioning at 1 uM after 5 mins by LC-MS analysis in presence of rifampin | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4 | Lysosomal sequestration (trapping) of lipophilic amine (cationic amphiphilic) drugs in immortalized human hepatocytes (Fa2N-4 cells). |
AID180098 | Heart rate of the urethane-anesthetized normotensive Wistar rat was tested 5 min after inducing the compound on dose of 1.0 mg/kg | 1994 | Journal of medicinal chemistry, Apr-01, Volume: 37, Issue:7 | Guaiacoxypropanolamine derivatives of capsaicin: a new family of beta-adrenoceptor blockers with intrinsic cardiotonic properties. |
AID327175 | Apparent permeability across parallel artificial membrane at 50 uM in presence of 100 uM human serum albumin | 2008 | Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7 | New approach to measure protein binding based on a parallel artificial membrane assay and human serum albumin. |
AID166089 | Concentration of propranolone oxime in cornea of rabbit after 60 min administration of compound; N/A= no oxime can be present after administration of propranolone hydrochloride | 1988 | Journal of medicinal chemistry, Jan, Volume: 31, Issue:1 | Improved delivery through biological membranes. 26. Design, synthesis, and pharmacological activity of a novel chemical delivery system for beta-adrenergic blocking agents. |
AID327173 | Apparent permeability across parallel artificial membrane at 10 uM in presence of 300 uM human serum albumin | 2008 | Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7 | New approach to measure protein binding based on a parallel artificial membrane assay and human serum albumin. |
AID327170 | Binding affinity to human serum albumin by PAMPA method | 2008 | Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7 | New approach to measure protein binding based on a parallel artificial membrane assay and human serum albumin. |
AID288193 | Flux ionization constant, pKa of the membrane permeability coefficient of the compound | 2007 | Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11 | QSAR study on permeability of hydrophobic compounds with artificial membranes. |
AID1226796 | Apparent permeability from apical to basolateral side in low-efflux MDCK cells expressing low levels of endogenous P-glycoprotein at 2 mM incubated for 2 hrs by LC-MS/MS method | 2015 | Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11 | Probing the Physicochemical Boundaries of Cell Permeability and Oral Bioavailability in Lipophilic Macrocycles Inspired by Natural Products. |
AID1603579 | Displacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranes | |||
AID1211794 | Fraction unbound in blood (not specified) | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1 | Comparison of cryopreserved HepaRG cells with cryopreserved human hepatocytes for prediction of clearance for 26 drugs. |
AID1262886 | Antagonist activity at human wild-type alpha 2C receptor expressed in CHO-K1 cells assessed as epinephrine-induced cAMP by HTRF assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
AID744912 | Antihypertensive activity in rat spontaneous hypertensive model assessed as diastolic arterial blood pressure at 20 mg/kg, po measured at 1 hr by tail-cuff method (Rvb = 146.2 +/- 13.19 mmHg) | 2013 | Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9 | Novel hybrids of natural isochroman-4-one bearing N-substituted isopropanolamine as potential antihypertensive candidates. |
AID1125242 | Toxicity in DOCA-induced normotensive Wistar rat assessed as mean arterial pressure at 10 mg/kg, ip measured immediately at 0 min (Rvb = 94.21 +/- 2.065 mmHg) | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Synthesis and pharmacological screening of some novel anti-hypertensive agents possessing 5-Benzylidene-2-(phenylimino)-thiazolidin-4-one ring. |
AID625292 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID1911471 | Stability in human plasma assessed as compound remaining measured upto 1440 mins by HPLC analysis | 2022 | Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11 | Design, Synthesis, and Biological Evaluations of DOT1L Peptide Mimetics Targeting the Protein-Protein Interactions between DOT1L and MLL-AF9/MLL-ENL. |
AID1752939 | Half life in human liver microsomes measured upto 40 mins by LC-MS/MS analysis | |||
AID1374480 | Apparent intrinsic permeability in human Caco2 cells from basolateral to apical side after 120 mins by mass spectrometry | 2018 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 28, Issue:5 | Pharmacology and in vivo efficacy of pyridine-pyrimidine amides that inhibit microtubule polymerization. |
AID702975 | Clearance in human hepatocytes in the presence of fetal calf serum | 2012 | Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12 | Identification, synthesis, and biological evaluation of the metabolites of 3-amino-6-(3'-aminopropyl)-5H-indeno[1,2-c]isoquinoline-5,11-(6H)dione (AM6-36), a promising rexinoid lead compound for the development of cancer chemotherapeutic and chemopreventi |
AID1079946 | Presence of at least one case with successful reintroduction. [column 'REINT' in source] | |||
AID496831 | Antimicrobial activity against Cryptosporidium parvum | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID40860 | Ratio of EC50 of test to control evaluated in guinea pig tracheal strips (beta2) | 1981 | Journal of medicinal chemistry, Oct, Volume: 24, Issue:10 | beta-Adrenergic blocking agents. alpha- and gamma-methyl(aryloxy)propanolamines. |
AID462614 | Apparent permeability in BBMEC | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6 | N-methyl phenylalanine-rich peptides as highly versatile blood-brain barrier shuttles. |
AID1513921 | Apparent permeability across apical to basolateral side in human Caco2 cells at 10 uM after 120 mins by LC-MS/MS analysis | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 | Alkyl-guanidine Compounds as Potent Broad-Spectrum Antibacterial Agents: Chemical Library Extension and Biological Characterization. |
AID298031 | Lipophilicity, log D at pH7.4 | 2007 | Journal of medicinal chemistry, Sep-20, Volume: 50, Issue:19 | High-throughput screening of drug-brain tissue binding and in silico prediction for assessment of central nervous system drug delivery. |
AID1703749 | Half life in human liver microsomes at 0.1 uM in presence of NADPH by LC/MS/MS analysis | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | Evaluation of N-phenyl-2-aminothiazoles for treatment of multi-drug resistant and intracellular Staphylococcus aureus infections. |
AID1851458 | Intrinsic clearance in human liver microsomes at 1 uM preincubated for 10 mins and measured up to 60 mins by LC-MS/MS analysis | 2022 | European journal of medicinal chemistry, Nov-05, Volume: 241 | Novel analgesic/anti-inflammatory agents: 1,5-Diarylpyrrole nitrooxyethyl sulfides and related compounds as Cyclooxygenase-2 inhibitors containing a nitric oxide donor moiety endowed with vasorelaxant properties. |
AID331213 | Apparent permeability from apical to basolateral side in human Caco-2 cells at 10 uM | 2008 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 18, Issue:12 | Pyrrolo[1,2-b]pyridazin-2-ones as potent inhibitors of HCV NS5B polymerase. |
AID180099 | Heart rate of the urethane-anesthetized normotensive Wistar rat was tested 60 min after inducing the compound on dose of 1.0 mg/kg | 1994 | Journal of medicinal chemistry, Apr-01, Volume: 37, Issue:7 | Guaiacoxypropanolamine derivatives of capsaicin: a new family of beta-adrenoceptor blockers with intrinsic cardiotonic properties. |
AID166304 | Effect on IOP of rabbits 60 mins after administration (2.5%) | 1988 | Journal of medicinal chemistry, Jan, Volume: 31, Issue:1 | Improved delivery through biological membranes. 26. Design, synthesis, and pharmacological activity of a novel chemical delivery system for beta-adrenergic blocking agents. |
AID1450161 | Apparent permeability of the compound in phosphate buffer at pH 7.4 by PAMPA | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | One drug for two targets: Biological evaluation of antiretroviral agents endowed with antiproliferative activity. |
AID150736 | Fraction of high affinity at binding site of human P-Glycoprotein (P-gp) in two-affinity model | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26 | Pharmacophore model of drugs involved in P-glycoprotein multidrug resistance: explanation of structural variety (hypothesis). |
AID496820 | Antimicrobial activity against Trypanosoma brucei | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID41306 | Beta adrenergic receptor blocking activity measured by the inotropic effect was determined 1 hr after pretreament of the right atria in guinea pig | 1984 | Journal of medicinal chemistry, Sep, Volume: 27, Issue:9 | Synthesis and antiarrhythmic activity of new 1-[1-[2-[3-(alkylamino)-2-hydroxypropoxy]phenyl]vinyl]-1 H-imidazoles and related compounds. |
AID467611 | Dissociation constant, pKa of the compound | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Prediction of volume of distribution values in human using immobilized artificial membrane partitioning coefficients, the fraction of compound ionized and plasma protein binding data. |
AID165999 | Cerebral biodistribution pattern of [123I]- ligand was evaluated in frontal cortex of anesthetized rabbit after Intravenous injection of 50 uCi after 2 hr | 1996 | Journal of medicinal chemistry, Aug-16, Volume: 39, Issue:17 | Synthesis and in vitro and in vivo characteristics of an iodinated analogue of the beta-adrenoceptor antagonist carazolol. |
AID1217711 | Metabolic activation in human liver microsomes assessed as [3H]GSH adduct formation rate measured per mg of protein at 100 uM by [3H]GSH trapping assay | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
AID1874538 | Efflux ratio of apparent permeability across basolateral to apical side to apical to basolateral side in human Caco-2 cells measured after 120 mins by LC-MS/MS analysis | 2022 | Journal of medicinal chemistry, 09-08, Volume: 65, Issue:17 | Development, Optimization, and In Vivo Validation of New Imidazopyridine Chemotypes as Dual TLR7/TLR9 Antagonists through Activity-Directed Sequential Incorporation of Relevant Structural Subunits. |
AID176311 | Beta-1-adrenoceptor blockade measured as inhibition of tachycardia caused by isoprenaline in anesthetized rats when administered intravenously | 1983 | Journal of medicinal chemistry, Nov, Volume: 26, Issue:11 | beta 1-selective adrenoceptor antagonists. 1. Synthesis and beta-adrenergic blocking activity of a series of binary (aryloxy)propanolamines. |
AID1137373 | Antihypertensive activity in spontaneously hypertensive Wistar-Okamoto rat assessed as maximal fall in mean arterial pressure at 5 mg/kg, po | 1979 | Journal of medicinal chemistry, Nov, Volume: 22, Issue:11 | Symbiotic approach to drug design: antihypertensive beta-adrenergic blocking agents. |
AID156204 | Binding to POPC/GMI liposomes using biosensor system | 2000 | Journal of medicinal chemistry, Jun-01, Volume: 43, Issue:11 | SPR biosensor studies of the direct interaction between 27 drugs and a liposome surface: correlation with fraction absorbed in humans. |
AID1067808 | Apparent permeability across MDCK2 cells expressing human MDR1 in presence of GF120918 | 2014 | Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3 | Substituted 2-phenylimidazopyridines: a new class of drug leads for human African trypanosomiasis. |
AID1135964 | Inhibition of beta2-adrenergic receptor in guinea pig tracheal chain assessed as reversal of isoproterenol-induced effect after 15 mins | 1978 | Journal of medicinal chemistry, Jan, Volume: 21, Issue:1 | Adrenoceptor blocking agents. 2. 2-(alpha-Hydroxyarylmethyl)-3,3-dimethylaziridines, a new class of selective beta2-adrenoceptor antagonists. |
AID76043 | Less than 80% recovery from 50% blockade levels after 1-h infusions of drug(in vivo) | 1983 | Journal of medicinal chemistry, Aug, Volume: 26, Issue:8 | Ultra-short-acting beta-adrenergic receptor blocking agents. 3. Ethylenediamine derivatives of (aryloxy)propanolamines having esters on the aryl function. |
AID1211298 | Dissociation constant, pKa of the compound | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3 | Control and measurement of plasma pH in equilibrium dialysis: influence on drug plasma protein binding. |
AID1212341 | Cytotoxicity against human Fa2N-4 cells by lactate dehydrogenase assay | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4 | Lysosomal sequestration (trapping) of lipophilic amine (cationic amphiphilic) drugs in immortalized human hepatocytes (Fa2N-4 cells). |
AID462616 | Apparent permeability in BBMEC assessed as membrane retention | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6 | N-methyl phenylalanine-rich peptides as highly versatile blood-brain barrier shuttles. |
AID181815 | Percentage of fall in systolic blood pressure (SBP) at the following hours after dosing at 75 mg/kg (po) at 2 hr in spontaneously hypertensive rats(SHR); NS means not significant | 1987 | Journal of medicinal chemistry, May, Volume: 30, Issue:5 | Flavones. 1. Synthesis and antihypertensive activity of (3-phenylflavonoxy)propanolamines without beta-adrenoceptor antagonism. |
AID1810690 | Effect on TLX regulated gene expression in human T98G cells assessed as decrease in PTEN mRNA expression at 50 uM after 8 hrs by qRT-PCR analysis | 2021 | Journal of medicinal chemistry, 06-24, Volume: 64, Issue:12 | Propranolol Activates the Orphan Nuclear Receptor TLX to Counteract Proliferation and Migration of Glioblastoma Cells. |
AID1262918 | Agonist activity at human wild-type ETA receptor expressed in CHO-K1 cells assessed as calcium level by HTRF assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
AID47944 | Beta-adrenergic blocking potency to inhibit tachycardia in anesthetized cats | 1983 | Journal of medicinal chemistry, Mar, Volume: 26, Issue:3 | beta-Adrenergic blocking agents. 23. 1-[Substituted-amido)phenoxy]-3-[[(substituted-amido)alkyl]amino] propan-2-ols. |
AID1067798 | Apparent permeability across MDCK2 cells expressing human MDR1 | 2014 | Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3 | Substituted 2-phenylimidazopyridines: a new class of drug leads for human African trypanosomiasis. |
AID694133 | Binding affinity to MDR1 expressed in MDCK2 cells assessed as absorptive quotient at at 3 uM in absence of 2 uM by mass spectroscopy | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14 | Urea-based inhibitors of Trypanosoma brucei methionyl-tRNA synthetase: selectivity and in vivo characterization. |
AID1145697 | Negative chronotropic activity in guinea pig right atrium assessed as atrial rate at MEC after 30 mins | 1977 | Journal of medicinal chemistry, Apr, Volume: 20, Issue:4 | Beta-adrenoceptor studies. 2. Effects of alkyl substitution on beta-adrenoceptor blocking, antiarrhythmic, and local anesthetic activities of 1,1'-(o-phenylenedioxy)bis(3-isopropylamino-2-propanol). |
AID1900028 | Apparent permeability across apical to basolateral side in human Caco-2 cells at 10 uM measured after 2 hrs by LC-MS/MS analysis | 2022 | Journal of medicinal chemistry, 01-13, Volume: 65, Issue:1 | Design, Synthesis, and Biological Evaluation of 1-(Indolizin-3-yl)ethan-1-ones as CBP Bromodomain Inhibitors for the Treatment of Prostate Cancer. |
AID1262884 | Antagonist activity at human wild-type alpha 1A receptor expressed in CHO cells assessed as EP-induced calcium by HTRF assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
AID298034 | Fraction unbound ligand in rat brain after 20 hrs | 2007 | Journal of medicinal chemistry, Sep-20, Volume: 50, Issue:19 | High-throughput screening of drug-brain tissue binding and in silico prediction for assessment of central nervous system drug delivery. |
AID60615 | Relative adrenoceptor blocking activity (DR10) was recorded for the antagonism of Isoproterenol-induced responses in Vasodepression in beta2-Adrenoceptor blockade. | 1982 | Journal of medicinal chemistry, Jun, Volume: 25, Issue:6 | Arylethanolamines derived from salicylamide with alpha- and beta-adrenoceptor blocking activities. Preparation of labetalol, its enantiomers, and related salicylamides. |
AID1262916 | Agonist activity at human wild-type D1 receptor expressed in CHO cells assessed as cAMP level by HTRF assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
AID1563153 | Metabolic stability in mouse liver microsomes assessed as compound remaining after 30 mins | 2019 | Journal of medicinal chemistry, 07-11, Volume: 62, Issue:13 | ( |
AID1906942 | Relaxant activity in guinea pig smooth muscle cells assessed as decrease in intracellular calcium level at 10 umol/L incubated for 5 mins by Flura2AM staining based fluorescence assay | |||
AID62988 | Effect on ischemic arrhythmias was studied in dogs. 10 mg/kg was injected intravenously and percent sinus beats after compound administration, was reported. | 1984 | Journal of medicinal chemistry, Sep, Volume: 27, Issue:9 | Synthesis and antiarrhythmic activity of new 1-[1-[2-[3-(alkylamino)-2-hydroxypropoxy]phenyl]vinyl]-1 H-imidazoles and related compounds. |
AID1832396 | Apparent permeability across apical to basolateral side in human Caco2 cells at 10 uM | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Discovery of Novel Acetamide-Based Heme Oxygenase-1 Inhibitors with Potent |
AID1262915 | Agonist activity at human wild-type M2 receptor expressed in CHO-K1 cells assessed as cAMP level by HTRF assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
AID1262924 | Intrinsic clearance in human liver microsomes at 1 uM by HPLC/MS/MS analysis | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
AID1221005 | Apparent distribution ratio of the compound in healthy Wistar rat perfused liver at 8 mM after 10 mins | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4 | Hepatic pharmacokinetics of cationic drugs in a high-fat emulsion-induced rat model of nonalcoholic steatohepatitis. |
AID496819 | Antimicrobial activity against Plasmodium falciparum | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID1374481 | Efflux ratio of apparent intrinsic permeability in human Caco2 cells after 120 mins by mass spectrometry | 2018 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 28, Issue:5 | Pharmacology and in vivo efficacy of pyridine-pyrimidine amides that inhibit microtubule polymerization. |
AID1079947 | Comments (NB not yet translated). [column 'COMMENTAIRES' in source] | |||
AID187015 | Tested for maximum fall in mean arterial pressure in Spontaneously hypertensive rats after peroral administration by using 1% methyl cellulose as vehicle at 20 mg/kg | 1980 | Journal of medicinal chemistry, Jan, Volume: 23, Issue:1 | Heterocyclic analogues of the antihypertensive beta-adrenergic blocking agent (S)-2-[3-(ter-butylamino)-2-hydroxypropoxy]-3-cyanopyridine. |
AID1146374 | Inhibition of isoproterenol-induced decrease in diastolic blood pressure in bilaterally vagotomized open chest mongrel dog model at 0.45 mg/kg, iv administered 10 to 20 mins prior to and following isoproterenol challenge | 1978 | Journal of medicinal chemistry, Jan, Volume: 21, Issue:1 | Synthesis of heteroaromatic potential beta-adrenergic antagonists by the glycidol route. |
AID58964 | Duration of the reversal of ouabain induced arrhythmia was measured | 1980 | Journal of medicinal chemistry, Feb, Volume: 23, Issue:2 | Mono- and diaryl-2-quinuclidinylcarbinols with local anesthetic and antiarrhythmic activity. |
AID40873 | In vitro inhibitory activity against beta-2 adrenergic receptor determined as pA2 in guinea pig trachea | 1985 | Journal of medicinal chemistry, Jul, Volume: 28, Issue:7 | New chiral and isomeric cyclopropyl ketoxime propanolamine derivatives with potent beta-adrenergic blocking properties. |
AID77095 | In vitro evaluation on guinea pig trachea. EC50 which is the molar concentration required to give 50% inhibition of the isoproterenol response (1x10E-6M) was determined. | 1984 | Journal of medicinal chemistry, Jun, Volume: 27, Issue:6 | Synthesis of a novel series of (aryloxy)propanolamines: new selective beta 2-blocking agents. |
AID1526019 | Apparent permeability from basolateral to apical side in MDCK-MDR1 cells | 2019 | Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18 | Heteroaryl Phosphonates as Noncovalent Inhibitors of Both Serine- and Metallocarbapenemases. |
AID1125255 | Antihypertensive activity in Wistar rat assessed as mean arterial pressure at 10 mg/kg, ip measured immediately at 45 mins (Rvb = 193.96 +/- 0.865 mmHg) | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Synthesis and pharmacological screening of some novel anti-hypertensive agents possessing 5-Benzylidene-2-(phenylimino)-thiazolidin-4-one ring. |
AID1079941 | Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source] | |||
AID48147 | Fall of blood pressure in anaesthetized cat at a dose of 1 mg/kg intravenously | 2004 | Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12 | Potential hypotensive agents: synthesis and hypotensive activity of oxime ethers derived from 1-naphthoxepines and related compounds. |
AID48148 | Fall of blood pressure in anaesthetized cat at a dose of 5 mg/kg intravenously | 2004 | Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12 | Potential hypotensive agents: synthesis and hypotensive activity of oxime ethers derived from 1-naphthoxepines and related compounds. |
AID496828 | Antimicrobial activity against Leishmania donovani | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID1851461 | Half-life in mouse liver microsomes at 1 uM preincubated for 10 mins and measured up to 60 mins by LC-MS/MS analysis | 2022 | European journal of medicinal chemistry, Nov-05, Volume: 241 | Novel analgesic/anti-inflammatory agents: 1,5-Diarylpyrrole nitrooxyethyl sulfides and related compounds as Cyclooxygenase-2 inhibitors containing a nitric oxide donor moiety endowed with vasorelaxant properties. |
AID1278102 | Inhibition of 5-HT-induced contraction in Sprague-Dawley rat ileum at 1 uM incubated for 10 mins | 2016 | European journal of medicinal chemistry, Mar-03, Volume: 110 | Synthesis, in vitro and in vivo pharmacological evaluation of serotoninergic ligands containing an isonicotinic nucleus. |
AID180095 | Heart rate of the urethane-anesthetized normotensive Wistar rat was tested 10 min after inducing the compound on dose of 1.0 mg/kg | 1994 | Journal of medicinal chemistry, Apr-01, Volume: 37, Issue:7 | Guaiacoxypropanolamine derivatives of capsaicin: a new family of beta-adrenoceptor blockers with intrinsic cardiotonic properties. |
AID1209582 | Unbound volume of distribution in Sprague-Dawley rat brain slices at 100 nM after 5 hrs | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3 | Measurement of unbound drug exposure in brain: modeling of pH partitioning explains diverging results between the brain slice and brain homogenate methods. |
AID1702310 | Metabolic stability in human liver microsomes assessed as half-life at 0.1 uM | |||
AID1451408 | Metabolic stability in rat liver microsomes assessed as compound remaining after 30 mins | 2017 | Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17 | 5-(4,6-Dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine (PQR309), a Potent, Brain-Penetrant, Orally Bioavailable, Pan-Class I PI3K/mTOR Inhibitor as Clinical Candidate in Oncology. |
AID1262927 | Inhibition of human CYP3A4 by LC-MS analysis | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
AID165955 | Concentration in cornea of rabbit after 120 min administration of compound; Below detection limit | 1988 | Journal of medicinal chemistry, Jan, Volume: 31, Issue:1 | Improved delivery through biological membranes. 26. Design, synthesis, and pharmacological activity of a novel chemical delivery system for beta-adrenergic blocking agents. |
AID171630 | Blood pressure of the urethane-anesthetized normotensive Wistar rat was tested 60 min after inducing the compound on dose of 1.0 mg/kg | 1994 | Journal of medicinal chemistry, Apr-01, Volume: 37, Issue:7 | Guaiacoxypropanolamine derivatives of capsaicin: a new family of beta-adrenoceptor blockers with intrinsic cardiotonic properties. |
AID4330 | Inhibitory activity against 5-hydroxytryptamine 1A receptor of rat hippocampal tissue using [3H]OH-DPAT as radioligand. | 1989 | Journal of medicinal chemistry, Apr, Volume: 32, Issue:4 | Design and synthesis of propranolol analogues as serotonergic agents. |
AID166301 | Effect on IOP of rabbits 4 hr after administration (2.5%) | 1988 | Journal of medicinal chemistry, Jan, Volume: 31, Issue:1 | Improved delivery through biological membranes. 26. Design, synthesis, and pharmacological activity of a novel chemical delivery system for beta-adrenergic blocking agents. |
AID1135369 | In vivo inhibition of beta-adrenoceptor in cat assessed as inhibition of isoproterenol-induced hypotension at 1 mg/kg, iv relative to control | 1977 | Journal of medicinal chemistry, Jul, Volume: 20, Issue:7 | beta-Adrenoceptor blocking activity of halogenated thienylethanolamine derivatives. |
AID1589933 | Half life in rat S9 fraction | 2019 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 29, Issue:12 | Lead generation of 1,2-dithiolanes as exon 19 and exon 21 mutant EGFR tyrosine kinase inhibitors. |
AID7974 | Metabolic stability observed at 30 min after administration in human liver microsomes | 2002 | Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2 | Graphical model for estimating oral bioavailability of drugs in humans and other species from their Caco-2 permeability and in vitro liver enzyme metabolic stability rates. |
AID1262911 | Agonist activity at human wild-type AVPR1A receptor expressed in CHO-K1 cells assessed as calcium level by FDSS assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
AID1074030 | Apparent permeability from apical to basolateral side in pig LLC-PK1 cells by LC-MS/MS analysis | 2014 | Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3 | Discovery of 7-tetrahydropyran-2-yl chromans: β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors that reduce amyloid β-protein (Aβ) in the central nervous system. |
AID327179 | Binding affinity to 600 uM human serum albumin at 10 uM by PAMPA method | 2008 | Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7 | New approach to measure protein binding based on a parallel artificial membrane assay and human serum albumin. |
AID41299 | Antagonist activity for blockade of beta adrenergic receptor of isolated guinea pig atrial pairs | 1986 | Journal of medicinal chemistry, Nov, Volume: 29, Issue:11 | 6,7-Dichloro-1-(3,4,5-trimethoxybenzyl)-1,2,3,4-tetrahydroisoquinoline . A structurally novel beta-adrenergic receptor blocking agent. |
AID1388323 | Passive permeability of the compound in pH 7.4 PBS at 10 uM after 5 hrs by UPLC-MS/MS method based PAMPA | 2018 | Journal of medicinal chemistry, 01-25, Volume: 61, Issue:2 | Group-Based Optimization of Potent and Cell-Active Inhibitors of the von Hippel-Lindau (VHL) E3 Ubiquitin Ligase: Structure-Activity Relationships Leading to the Chemical Probe (2S,4R)-1-((S)-2-(1-Cyanocyclopropanecarboxamido)-3,3-dimethylbutanoyl)-4-hydr |
AID1407670 | Apparent permeability of the compound from basolateral to apical side in human Caco2 cells assessed as drug recovery after 120 mins by LC-MS/MS analysis | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Hedgehog pathway inhibitors of the acylthiourea and acylguanidine class show antitumor activity on colon cancer in vitro and in vivo. |
AID666536 | Antiarrhythmic activity in iv dosed adrenaline-induced Wistar rat arrhythmia model assessed as protection against mortality administered 15 mins prior to barium chloride-challenge | 2012 | Bioorganic & medicinal chemistry, Apr-01, Volume: 20, Issue:7 | Antiarrhythmic properties of phenylpiperazine derivatives of phenytoin with α₁-adrenoceptor affinities. |
AID60110 | Number of dogs reverted ouabain induced arrhythmia | 1980 | Journal of medicinal chemistry, Feb, Volume: 23, Issue:2 | Mono- and diaryl-2-quinuclidinylcarbinols with local anesthetic and antiarrhythmic activity. |
AID180096 | Heart rate of the urethane-anesthetized normotensive Wistar rat was tested 15 min after inducing the compound on dose of 1.0 mg/kg | 1994 | Journal of medicinal chemistry, Apr-01, Volume: 37, Issue:7 | Guaiacoxypropanolamine derivatives of capsaicin: a new family of beta-adrenoceptor blockers with intrinsic cardiotonic properties. |
AID344616 | Apparent permeability from apical to basolateral side in human Caco-2 cell membrane at 10 uM | 2008 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18 | Hexahydro-pyrrolo- and hexahydro-1H-pyrido[1,2-b]pyridazin-2-ones as potent inhibitors of HCV NS5B polymerase. |
AID1212335 | Drug uptake in lysosomes of human Fa2N-4 cells assessed as cellular partitioning at 1 uM after 5 mins by LC-MS analysis in presence of atorvastatin | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4 | Lysosomal sequestration (trapping) of lipophilic amine (cationic amphiphilic) drugs in immortalized human hepatocytes (Fa2N-4 cells). |
AID48729 | Hypotensive activity in cat following i.v. administration of 5 mg/kg expressed as fall in blood pressure | 2004 | Bioorganic & medicinal chemistry letters, Jun-07, Volume: 14, Issue:11 | 1- and 2-substituted naphthalenes: a new class of potential hypotensive agents. |
AID1079936 | Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source] | |||
AID176761 | In vivo beta adrenergic receptor blocking potency was determined by inhibition of tachycardia in rat | 1982 | Journal of medicinal chemistry, Dec, Volume: 25, Issue:12 | beta-adrenergic blocking agents. 24. Heterocyclic substituted 1-(aryloxy)-3-[[(amido)alkyl]amino]propan-2-ols. |
AID337597 | Inhibition of acetylcholine-induced contraction in guinea pig ileum at 0.2 ug/ml | 1994 | Journal of natural products, Sep, Volume: 57, Issue:9 | (+/-)-Gelliusines A and B, two diastereomeric brominated tris-indole alkaloids from a deep water new caledonian marine sponge (Gellius or Orina sp.). |
AID13443 | In vitro metabolic potential in rat liver microsomes | 2003 | Bioorganic & medicinal chemistry letters, Apr-17, Volume: 13, Issue:8 | Oxyguanidines: application to non-peptidic phenyl-based thrombin inhibitors. |
AID1603582 | Displacement of [3H]CGP12177 from human beta2 adrenoceptor H2.64C mutant expressed in HEK293T cell membranes | |||
AID1475282 | Apparent permeability in human Caco2 cells at 10 uM | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Discovery of N-{4-[5-(4-Fluorophenyl)-3-methyl-2-methylsulfanyl-3H-imidazol-4-yl]-pyridin-2-yl}-acetamide (CBS-3595), a Dual p38α MAPK/PDE-4 Inhibitor with Activity against TNFα-Related Diseases. |
AID1667045 | Clearance in human liver microsomes in presence of NADPH | 2020 | Bioorganic & medicinal chemistry letters, 04-01, Volume: 30, Issue:7 | Discovery and optimization of 4-oxo-2-thioxo-thiazolidinones as NOD-like receptor (NLR) family, pyrin domain-containing protein 3 (NLRP3) inhibitors. |
AID1572361 | Half life in human liver microsomes at 2 uM by LC-MS/MS analysis | 2019 | Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3 | Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors. |
AID190412 | Antihypertensive activity expressed as percentage of base-line systolic blood pressure of base-line values in spontaneously hypertensive rats (SHR) was reported after 4 hr | 1987 | Journal of medicinal chemistry, Jun, Volume: 30, Issue:6 | Synthesis of a series of compounds related to betaxolol, a new beta 1-adrenoceptor antagonist with a pharmacological and pharmacokinetic profile optimized for the treatment of chronic cardiovascular diseases. |
AID166311 | Effect on IOP of rabbits 8 hr min after administration (2.5%) | 1988 | Journal of medicinal chemistry, Jan, Volume: 31, Issue:1 | Improved delivery through biological membranes. 26. Design, synthesis, and pharmacological activity of a novel chemical delivery system for beta-adrenergic blocking agents. |
AID1220993 | Mean transit time of the compound in perfused liver of high-fat emulsion-induced nonalcoholic steatohepatitis Wistar rat at 8 mM after 10 mins | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 39, Issue:4 | Hepatic pharmacokinetics of cationic drugs in a high-fat emulsion-induced rat model of nonalcoholic steatohepatitis. |
AID1895159 | Permeability across apical to basal side in human Caco-2 cells measured at 0.5 to 2 hrs by LC-MS analysis | 2021 | Journal of medicinal chemistry, 06-24, Volume: 64, Issue:12 | Interplay among Conformation, Intramolecular Hydrogen Bonds, and Chameleonicity in the Membrane Permeability and Cyclophilin A Binding of Macrocyclic Peptide Cyclosporin O Derivatives. |
AID1237774 | Intrinsic clearance in human liver microsomes assessed per mg of protein preincubated for 10 mins followed by NADP/Glc6P/G6P-DH addition by LC-MS/MS analysis | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15 | New Indole Tubulin Assembly Inhibitors Cause Stable Arrest of Mitotic Progression, Enhanced Stimulation of Natural Killer Cell Cytotoxic Activity, and Repression of Hedgehog-Dependent Cancer. |
AID321772 | Permeability across human Caco-2 cells | 2008 | Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4 | Backbone cyclic peptidomimetic melanocortin-4 receptor agonist as a novel orally administrated drug lead for treating obesity. |
AID41903 | Beta adrenoceptor blocking potency was estimated by inhibition of 50% of the tachycardia produced by a submaximal dose of the isoproterenol (0.2ug/kg, intravenously) | 1981 | Journal of medicinal chemistry, Nov, Volume: 24, Issue:11 | Beta-adrenergic blocking agents. 21. threo-1-(Aryloxy)-3-(alkylamino)butan-2-ols. |
AID327174 | Apparent permeability across parallel artificial membrane at 10 uM in presence of 600 uM human serum albumin | 2008 | Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7 | New approach to measure protein binding based on a parallel artificial membrane assay and human serum albumin. |
AID1137306 | Selectivity index, ratio of pED40 for tissue contractility to pED40 for maximum driving response in New Zealand White rabbit isolated atria | 1979 | Journal of medicinal chemistry, Jan, Volume: 22, Issue:1 | Relationship of nonspecific antiarrhythmic and negative inotropic activity with physicochemical parameters of propranolol analogues. |
AID744924 | Antihypertensive activity in rat spontaneous hypertensive model assessed as systolic arterial blood pressure at 20 mg/kg, po measured at 1 hr by tail-cuff method (Rvb = 181.2 +/- 16.37 mmHg) | 2013 | Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9 | Novel hybrids of natural isochroman-4-one bearing N-substituted isopropanolamine as potential antihypertensive candidates. |
AID1262891 | Antagonist activity at human wild-type M1 receptor expressed in CHO-K1 cells assessed as acetylcholine-induced calcium by FDSS assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
AID1079944 | Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source] | |||
AID1262904 | Agonist activity at human wild-type 5-HT7 receptor expressed in HEK cells assessed as cAMP by HTRF assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
AID1810685 | Effect on Gal4-VP16 plasmid transfected in human HEK293T cells assessed as reporter activity incubated for 14 hrs by luciferase assay | 2021 | Journal of medicinal chemistry, 06-24, Volume: 64, Issue:12 | Propranolol Activates the Orphan Nuclear Receptor TLX to Counteract Proliferation and Migration of Glioblastoma Cells. |
AID1123537 | Displacement of [3H]DHA from beta2 adrenergic receptor in rat lung muscle by competitive binding assay | 1979 | Journal of medicinal chemistry, Jun, Volume: 22, Issue:6 | Cardioselectivity of beta-adrenoceptor blocking agents 1. 1-[(4-Hydroxyphenethyl)amino]-3-(aryloxy)propan-2-ols. |
AID444056 | Fraction escaping gut-wall elimination in human | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination. |
AID1810692 | Cytotoxicity against human T98G cells assessed as cell viability by WST-1 assay | 2021 | Journal of medicinal chemistry, 06-24, Volume: 64, Issue:12 | Propranolol Activates the Orphan Nuclear Receptor TLX to Counteract Proliferation and Migration of Glioblastoma Cells. |
AID1529182 | Protein binding in plasma (unknown origin) | 2020 | Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4 | Human Serum Albumin Binding in a Vial: A Novel UV-pH Titration Method To Assist Drug Design. |
AID1305707 | Permeability across apical side at pH 6.5 to basolateral side at pH 7.4 in human Caco2 cells assessed as compound recovery at 10 uM | 2016 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 26, Issue:14 | Coumarin carboxylic acids as monocarboxylate transporter 1 inhibitors: In vitro and in vivo studies as potential anticancer agents. |
AID42032 | Compound was tested for beta-1 adrenergic receptor blocking activity in dogs | 1986 | Journal of medicinal chemistry, Jan, Volume: 29, Issue:1 | [p-[(Thienylcarbonyl)amino]phenoxy]propanolamines derivatives as diuretic and beta-adrenergic receptor blocking agents. |
AID1393789 | Apparent permeability from basolateral to apical side in human Caco2 cells in absence of P-gp inhibitor by LC-MS/MS analysis | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Effects of rigidity on the selectivity of protein kinase inhibitors. |
AID462615 | Apparent permeability in BBMEC assessed as compound transport after 2 hrs | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6 | N-methyl phenylalanine-rich peptides as highly versatile blood-brain barrier shuttles. |
AID28926 | Effective permeability corrected for ionization | 2001 | Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6 | High-throughput permeability pH profile and high-throughput alkane/water log P with artificial membranes. |
AID159425 | Tested for beta-2 adrenoceptor blocking activity in anesthetized pigs (n=2) challenged with intravenous injections of isoproterenol. | 1987 | Journal of medicinal chemistry, Apr, Volume: 30, Issue:4 | Substituted 1,2,3,4-tetrahydroaminonaphthols: antihypertensive agents, calcium channel blockers, and adrenergic receptor blockers with catecholamine-depleting effects. |
AID350783 | Permeability from apical to basolateral side in human Caco-2 cells | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Efficacy, pharmacokinetics, and metabolism of tetrahydroquinoline inhibitors of Plasmodium falciparum protein farnesyltransferase. |
AID92844 | Concentration required to inhibit ADP-induced platelet aggregation by 50% | 1992 | Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16 | Molecular determinants of the platelet aggregation inhibitory activity of carbamoylpiperidines. |
AID27167 | Delta logD (logD6.5 - logD7.4) | 2000 | Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13 | QSAR model for drug human oral bioavailability. |
AID310931 | Partition coefficient, log P of the compound | 2007 | Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4 | In silico and in vitro filters for the fast estimation of skin permeation and distribution of new chemical entities. |
AID165958 | Concentration in cornea of rabbit after 60 min administration of compound | 1988 | Journal of medicinal chemistry, Jan, Volume: 31, Issue:1 | Improved delivery through biological membranes. 26. Design, synthesis, and pharmacological activity of a novel chemical delivery system for beta-adrenergic blocking agents. |
AID19419 | Partition coefficient (logD7.4) | 1998 | Journal of medicinal chemistry, Mar-26, Volume: 41, Issue:7 | Physicochemical high throughput screening: parallel artificial membrane permeation assay in the description of passive absorption processes. |
AID1209593 | Dissociation constant, pKa of the acidic compound by capillary electrophoresis-mass spectrometry analysis | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3 | Measurement of unbound drug exposure in brain: modeling of pH partitioning explains diverging results between the brain slice and brain homogenate methods. |
AID1262934 | Efflux ratio of permeability across basolateral to apical side over apical to basolateral side in MDCK cells expressing human MDR1 at 5 uM by LC-MS/MS method | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
AID1708567 | Stability in mouse hepatic microsomes assessed as half life for compound degradation at 5 mM in presence of NADPH by UPLC analysis | 2021 | Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3 | A High-Affinity Peptide Ligand Targeting Syntenin Inhibits Glioblastoma. |
AID1212322 | Drug uptake in lysosomes of human Fa2N-4 cells assessed as cellular partitioning at 1 uM preincubated with ammonium chloride followed by compound treatment measured after 5 mins by LC-MS analysis | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4 | Lysosomal sequestration (trapping) of lipophilic amine (cationic amphiphilic) drugs in immortalized human hepatocytes (Fa2N-4 cells). |
AID159424 | Tested for beta-1 adrenoceptor blocking activity in anesthetized pigs (n=2) challenged with intravenous injections of isoproterenol. | 1987 | Journal of medicinal chemistry, Apr, Volume: 30, Issue:4 | Substituted 1,2,3,4-tetrahydroaminonaphthols: antihypertensive agents, calcium channel blockers, and adrenergic receptor blockers with catecholamine-depleting effects. |
AID48346 | Beta-1-adrenoceptor antagonsim of compound expressed as inhibition of isoprenaline-induced tachycardia in the ganglion-blocked anesthetized cat | 1988 | Journal of medicinal chemistry, Feb, Volume: 31, Issue:2 | Design and synthesis of a series of combined vasodilator/beta-adrenoceptor antagonists based on 6-arylpyridazinones. |
AID666534 | Antiarrhythmic activity in iv dosed Wistar rat assessed as protection against adrenaline-induced extrasystoles administered 15 mins prior to adrenaline-challenge | 2012 | Bioorganic & medicinal chemistry, Apr-01, Volume: 20, Issue:7 | Antiarrhythmic properties of phenylpiperazine derivatives of phenytoin with α₁-adrenoceptor affinities. |
AID624619 | Specific activity of expressed human recombinant UGT2B7 | 2000 | Annual review of pharmacology and toxicology, , Volume: 40 | Human UDP-glucuronosyltransferases: metabolism, expression, and disease. |
AID63494 | Evaluated for Adrenoceptor from guinea pig trachea by using isoproterenol as agonist. | 1982 | Journal of medicinal chemistry, Jun, Volume: 25, Issue:6 | Arylethanolamines derived from salicylamide with alpha- and beta-adrenoceptor blocking activities. Preparation of labetalol, its enantiomers, and related salicylamides. |
AID1256760 | Permeability of the compound at 10 mM after 4 hrs by PAMPA | 2015 | European journal of medicinal chemistry, Nov-13, Volume: 105 | Novel 5-carboxy-8-HQ based histone demethylase JMJD2A inhibitors: introduction of an additional carboxyl group at the C-2 position of quinoline. |
AID1895163 | Efflux ratio of permeability from apical to basolateral side over basolateral to apical side in human Caco2 cells measured at 0.5 to 2 hrs by LC-MS analysis | 2021 | Journal of medicinal chemistry, 06-24, Volume: 64, Issue:12 | Interplay among Conformation, Intramolecular Hydrogen Bonds, and Chameleonicity in the Membrane Permeability and Cyclophilin A Binding of Macrocyclic Peptide Cyclosporin O Derivatives. |
AID624629 | Inhibition of Pgp expressed in MDR1-MDCKII cells measured by calcein-AM assay | 2001 | The Journal of pharmacology and experimental therapeutics, Nov, Volume: 299, Issue:2 | Rational use of in vitro P-glycoprotein assays in drug discovery. |
AID477503 | Apparent permeability from apical to basolateral side of the human Caco-2 cells at 10 uM after 2 hrs by LC-MS/MS analysis | 2009 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 19, Issue:21 | Pyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione derivatives: their cytoprotection effect from rotenone toxicity and preliminary DMPK properties. |
AID1374479 | Apparent intrinsic permeability in human Caco2 cells from apical to basolateral side after 120 mins by mass spectrometry | 2018 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 28, Issue:5 | Pharmacology and in vivo efficacy of pyridine-pyrimidine amides that inhibit microtubule polymerization. |
AID79687 | Ionotropic effect in electrically driven left atrial preparation (Atria isolated from guinea pig) and is expressed in pA2. | 1998 | Journal of medicinal chemistry, May-07, Volume: 41, Issue:10 | Synthesis and adrenergic activity of a new series of N-aryl dicyclopropyl ketone oxime ethers: SAR and stereochemical aspects. |
AID1203209 | Apparent permeability across apical to basolateral side in human Caco2 cells in presence of 0.1% bovine serum albumin | 2015 | Journal of medicinal chemistry, Apr-09, Volume: 58, Issue:7 | Discovery and optimization of novel antagonists to the human neurokinin-3 receptor for the treatment of sex-hormone disorders (Part I). |
AID1765571 | Metabolic stability in human liver microsomes assessed as intrinsic clearance at 80 uM by HPLC analysis | 2021 | European journal of medicinal chemistry, Oct-15, Volume: 222 | Effects of substituent pattern on the intracellular target of antiproliferative benzo[b]thiophenyl chromone derivatives. |
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AID1222793 | Dissociation constant, pKa of the compound | 2013 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5 | Which metabolites circulate? |
AID444053 | Renal clearance in human | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination. |
AID62238 | Evaluated for the heart rate at dose 2.5 mg/kg in 4 animals by poldine tachycardia test | 1983 | Journal of medicinal chemistry, Feb, Volume: 26, Issue:2 | Cardiac-slowing amidines containing the 3-thioindone group. Potential antianginal agents. |
AID744922 | Antihypertensive activity in rat spontaneous hypertensive model assessed as systolic arterial blood pressure at 20 mg/kg, po measured at 2 hrs by tail-cuff method (Rvb = 172.6 +/- 17.3 mmHg) | 2013 | Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9 | Novel hybrids of natural isochroman-4-one bearing N-substituted isopropanolamine as potential antihypertensive candidates. |
AID1350481 | Displacement of [3H]-CGP12177 from human beta2 ADR expressed in HEK293T cell membrane after 90 mins by scintillation counting | 2018 | Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12 | Discovery of β-Adrenergic Receptors Blocker-Carbonic Anhydrase Inhibitor Hybrids for Multitargeted Antiglaucoma Therapy. |
AID42020 | In vitro inhibitory activity against beta-1 adrenergic receptor determined as pA2 in guinea pig atria | 1985 | Journal of medicinal chemistry, Jul, Volume: 28, Issue:7 | New chiral and isomeric cyclopropyl ketoxime propanolamine derivatives with potent beta-adrenergic blocking properties. |
AID744892 | Antihypertensive activity in rat spontaneous hypertensive model assessed as mean arterial blood pressure at 20 mg/kg, po measured at 8 hrs by tail-cuff method (Rvb = 155.8 +/- 11.54 mmHg) | 2013 | Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9 | Novel hybrids of natural isochroman-4-one bearing N-substituted isopropanolamine as potential antihypertensive candidates. |
AID497005 | Antimicrobial activity against Pneumocystis carinii | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID1663579 | Lipophilicity, log D of the compound in 1-Octanol-phosphate buffer at pH 7.4 | 2020 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14 | Synthesis, in vitro ADME profiling and in vivo pharmacological evaluation of novel glycogen phosphorylase inhibitors. |
AID1262902 | Agonist activity at human 5-HT2C receptor expressed in CHO-K1 cells assessed as calcium level by FDSS assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
AID588212 | Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents | 2010 | Chemical research in toxicology, Jan, Volume: 23, Issue:1 | Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species. |
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AID267570 | Stability in human liver microsomes at 1 M at pH 7.4 | 2006 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13 | Synthesis and biological evaluation of lisofylline (LSF) analogs as a potential treatment for Type 1 diabetes. |
AID41154 | In Vitro inhibition of the beta adrenergic receptor in guinea pig atria | 1984 | Journal of medicinal chemistry, Aug, Volume: 27, Issue:8 | [(Arylcarbonyl)oxy]propanolamines. 1. Novel beta-blockers with ultrashort duration of action. |
AID24180 | Permeability coefficient reported; (Expressed as Permeability coefficient x 10 e 4 cm/s) | 1996 | Journal of medicinal chemistry, Nov-22, Volume: 39, Issue:24 | Computation of brain-blood partitioning of organic solutes via free energy calculations. |
AID174416 | Change in systolic blood pressure after 100 mg/kg oral administration in spontaneous hypertensive rats after 24 hr | 1981 | Journal of medicinal chemistry, Dec, Volume: 24, Issue:12 | Antihypertensive pyrrolo[1,2-c]quinazolines and pyrrolo[1,2-c]quinazolinones. |
AID1262887 | Antagonist activity at human wild-type AGTR1 receptor expressed in CHO-K1 cells assessed as angiotensin-2-induced calcium by FDSS assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
AID620392 | Antagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19 | Synthesis and characterization of high-affinity 4,4-difluoro-4-bora-3a,4a-diaza-s-indacene-labeled fluorescent ligands for human β-adrenoceptors. |
AID1129458 | Protein binding in plasma (unknown origin) at 5 uM after 4 hrs | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Development and characterization of 3-(benzylsulfonamido)benzamides as potent and selective SIRT2 inhibitors. |
AID181817 | Percentage of fall in systolic blood pressure (SBP) at the following hours after dosing at 75 mg/kg (po) at 5 hr in spontaneously hypertensive rats(SHR); NS means not significant | 1987 | Journal of medicinal chemistry, May, Volume: 30, Issue:5 | Flavones. 1. Synthesis and antihypertensive activity of (3-phenylflavonoxy)propanolamines without beta-adrenoceptor antagonism. |
AID1146370 | Inhibition of isoproterenol-induced increase in heart rate in bilaterally vagotomized open chest mongrel dog model at 1.45 mg/kg, iv administered 10 to 20 mins prior to and following isoproterenol challenge | 1978 | Journal of medicinal chemistry, Jan, Volume: 21, Issue:1 | Synthesis of heteroaromatic potential beta-adrenergic antagonists by the glycidol route. |
AID1171959 | Half life in CD-1 mouse liver microsomes at 0.75 uM incubated for 5 mins prior to NADPH addition measured after 30 mins by LC/MS/MS analysis | 2014 | Journal of medicinal chemistry, Dec-26, Volume: 57, Issue:24 | Discovery of a phosphodiesterase 9A inhibitor as a potential hypoglycemic agent. |
AID185196 | Tested for MED (smallest dose giving maximum effect) evaluated by dose-response curve, from 0.1 to 5 mg/kg in 5-10 animals on iv administration. | 1998 | Journal of medicinal chemistry, May-07, Volume: 41, Issue:10 | Synthesis and adrenergic activity of a new series of N-aryl dicyclopropyl ketone oxime ethers: SAR and stereochemical aspects. |
AID1262899 | Agonist activity at human 5-HT1B receptor expressed in CHO-K1 cells assessed as cAMP level by HTRF assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
AID1135310 | In vivo inhibition of beta-1 adrenergic receptor in cat assessed as inhibition of isoproterenol-induced tachycardia administered as 30 mins of infusion measured at 30 mins by cardiotachometer | 1977 | Journal of medicinal chemistry, May, Volume: 20, Issue:5 | Beta-Adrenergic blocking agents. 15. 1-Substituted ureidophenoxy-3-amino-2-propanols. |
AID78357 | Effect on maximal follow rate showing the contractile frequencies of atria to electrical stimulation 10 min after incubating compound with right atria of guinea pig | 1984 | Journal of medicinal chemistry, Sep, Volume: 27, Issue:9 | Synthesis and antiarrhythmic activity of new 1-[1-[2-[3-(alkylamino)-2-hydroxypropoxy]phenyl]vinyl]-1 H-imidazoles and related compounds. |
AID722794 | Antiarrhythmic activity in iv dosed Wistar rat adrenaline-induced arrhythmia model assessed as reduction of heart-rhythm disturbance administered 15 mins adrenaline-challenge | 2013 | Bioorganic & medicinal chemistry, Jan-15, Volume: 21, Issue:2 | Synthesis and preliminary evaluation of pharmacological properties of some piperazine derivatives of xanthone. |
AID1137385 | Antihypertensive activity in spontaneously hypertensive Wistar-Okamoto rat assessed as duration of action at 20 mg/kg, po | 1979 | Journal of medicinal chemistry, Nov, Volume: 22, Issue:11 | Symbiotic approach to drug design: antihypertensive beta-adrenergic blocking agents. |
AID19424 | Partition coefficient (logD7.4) | 2001 | Journal of medicinal chemistry, Jul-19, Volume: 44, Issue:15 | ElogD(oct): a tool for lipophilicity determination in drug discovery. 2. Basic and neutral compounds. |
AID1211795 | Dissociation constant, pKa of the compound | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1 | Comparison of cryopreserved HepaRG cells with cryopreserved human hepatocytes for prediction of clearance for 26 drugs. |
AID1146354 | Inhibition of isoproterenol-induced decrease in diastolic blood pressure in bilaterally vagotomized open chest mongrel dog model at 4.61 mg/kg, iv administered 10 to 20 mins prior to and following isoproterenol challenge | 1978 | Journal of medicinal chemistry, Jan, Volume: 21, Issue:1 | Synthesis of heteroaromatic potential beta-adrenergic antagonists by the glycidol route. |
AID744898 | Antihypertensive activity in rat spontaneous hypertensive model assessed as mean arterial blood pressure at 20 mg/kg, po measured at 2 hrs by tail-cuff method (Rvb = 157.41 +/- 9.62 mmHg) | 2013 | Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9 | Novel hybrids of natural isochroman-4-one bearing N-substituted isopropanolamine as potential antihypertensive candidates. |
AID625279 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID327178 | Binding affinity to 300 uM human serum albumin at 10 uM by PAMPA method | 2008 | Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7 | New approach to measure protein binding based on a parallel artificial membrane assay and human serum albumin. |
AID174557 | Change in systolic blood pressure after 33 mg/kg oral administration in spontaneous hypertensive rats after 2 hr | 1981 | Journal of medicinal chemistry, Dec, Volume: 24, Issue:12 | Antihypertensive pyrrolo[1,2-c]quinazolines and pyrrolo[1,2-c]quinazolinones. |
AID40527 | Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atria | 1987 | Journal of medicinal chemistry, Jun, Volume: 30, Issue:6 | Synthesis of a series of compounds related to betaxolol, a new beta 1-adrenoceptor antagonist with a pharmacological and pharmacokinetic profile optimized for the treatment of chronic cardiovascular diseases. |
AID351393 | Activity of Agrocybe aegerita peroxygenase assessed as conversion of propranolol to 5-hydroxypropranolol at 5 mM in presence of 5 mM H2O2 and 4 mM ascorbic acid | 2009 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11 | Regioselective preparation of 5-hydroxypropranolol and 4'-hydroxydiclofenac with a fungal peroxygenase. |
AID165818 | Percentage change of IOP in rabbits after 6 hr administration (2.5%) of compound | 1988 | Journal of medicinal chemistry, Jan, Volume: 31, Issue:1 | Improved delivery through biological membranes. 26. Design, synthesis, and pharmacological activity of a novel chemical delivery system for beta-adrenergic blocking agents. |
AID1136327 | Intrinsic activity at beta2 adrenoceptor in guinea pig trachea after 20 mins | 1978 | Journal of medicinal chemistry, Oct, Volume: 21, Issue:10 | 2-Methoxyphenylethanolamines, potential beta-adrenergic blocking agents. |
AID7783 | Unbound fraction (plasma) | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5 | Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics. |
AID1262929 | Inhibition of human CYP1A2 by LC-MS analysis | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
AID772976 | Half life in human liver microsomes at 1 uM after 1 to 60 mins by UHPLC-MS/MS analysis | 2013 | European journal of medicinal chemistry, Oct, Volume: 68 | Chemopreventive and antioxidant activity of 6-substituted imidazo[2,1-b]thiazoles. |
AID1209581 | Fraction unbound in Sprague-Dawley rat brain homogenates at 5 uM by equilibrium dialysis analysis | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3 | Measurement of unbound drug exposure in brain: modeling of pH partitioning explains diverging results between the brain slice and brain homogenate methods. |
AID77257 | Mean increase in the heart rate in anesthetized guinea pigs induced with urethane. | 1984 | Journal of medicinal chemistry, Jun, Volume: 27, Issue:6 | Synthesis of a novel series of (aryloxy)propanolamines: new selective beta 2-blocking agents. |
AID1563155 | Metabolic stability in rat liver microsomes assessed as compound remaining after 30 mins | 2019 | Journal of medicinal chemistry, 07-11, Volume: 62, Issue:13 | ( |
AID1135150 | Hypotensive activity at guinea pig assessed as decrease in blood pressure at 50 mg/kg, po after 3 hrs (Rvb = 112 +/- 2.6 to 122 +/- 2.7 mmHg) | 1977 | Journal of medicinal chemistry, Mar, Volume: 20, Issue:3 | Synthesis and adrenergic beta-blocking activity of some 1,3-benzodioxole derivatives. |
AID8002 | Observed volume of distribution | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5 | Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics. |
AID1636428 | Drug activation in human Hep3B cells assessed as human CYP2D6-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 2.1 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of NA | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16 | Development of a cell viability assay to assess drug metabolite structure-toxicity relationships. |
AID384955 | Intrinsic aqueous solubility at pH 10 by shake-flask method | 2008 | Journal of medicinal chemistry, May-22, Volume: 51, Issue:10 | Molecular characteristics for solid-state limited solubility. |
AID165950 | Concentration in aqueous humor of rabbit after 30 min administration of compound | 1988 | Journal of medicinal chemistry, Jan, Volume: 31, Issue:1 | Improved delivery through biological membranes. 26. Design, synthesis, and pharmacological activity of a novel chemical delivery system for beta-adrenergic blocking agents. |
AID1605678 | Microsomal stability of compound in BALB/c mouse liver microsomes assessed as parent compound remaining at 2 uM after 40 mins by HPLC-MS/MS analysis | 2020 | Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7 | Structure-Activity Relationship Studies of Tetrahydroquinolone Free Fatty Acid Receptor 3 Modulators. |
AID165811 | Percentage change of IOP in rabbits after 4 hr administration (2.5%) of compound | 1988 | Journal of medicinal chemistry, Jan, Volume: 31, Issue:1 | Improved delivery through biological membranes. 26. Design, synthesis, and pharmacological activity of a novel chemical delivery system for beta-adrenergic blocking agents. |
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AID180097 | Heart rate of the urethane-anesthetized normotensive Wistar rat was tested 30 min after inducing the compound on dose of 1.0 mg/kg | 1994 | Journal of medicinal chemistry, Apr-01, Volume: 37, Issue:7 | Guaiacoxypropanolamine derivatives of capsaicin: a new family of beta-adrenoceptor blockers with intrinsic cardiotonic properties. |
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AID1635246 | Apparent permeability from apical to basolateral side in human Caco2 cells at 10 uM incubated for 120 mins by LC-MS/MS analysis | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer. |
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AID496817 | Antimicrobial activity against Trypanosoma cruzi | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID42208 | Beta-1 adrenergic receptor activation measured by isoprenaline-induced positive inotropic effect in guinea pig left atrium | 1988 | Journal of medicinal chemistry, Nov, Volume: 31, Issue:11 | Synthesis and beta-adrenergic antagonism of 2-(aryloxy)-1-(2-piperidyl)ethanols. |
AID166094 | Concentration of propranolone oxime in iris-ciliary body of rabbit after 60 min administration of compound; N/A= no oxime can be present after administration of propranolone hydrochloride | 1988 | Journal of medicinal chemistry, Jan, Volume: 31, Issue:1 | Improved delivery through biological membranes. 26. Design, synthesis, and pharmacological activity of a novel chemical delivery system for beta-adrenergic blocking agents. |
AID1262885 | Antagonist activity at human wild-type alpha 2A receptor expressed in CHO-K1 cells assessed as epinephrine-induced cAMP by HTRF assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
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AID1383763 | Effective permeability of the compound at pH 7.4 at 200 uM after 4 hrs by PAMPA-BBB assay | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Metallomics for Alzheimer's disease treatment: Use of new generation of chelators combining metal-cation binding and transport properties. |
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AID62120 | Evaluated for the heart rate at dose 2.5 mg/kg in 4 animals by aminophylline-induced sinus tachycardia test | 1983 | Journal of medicinal chemistry, Feb, Volume: 26, Issue:2 | Cardiac-slowing amidines containing the 3-thioindone group. Potential antianginal agents. |
AID165674 | Biodistribution pattern of [123I]- ligand was evaluated in fat of anesthetized rabbit after Intravenous injection of 50 uCi after 2 hr | 1996 | Journal of medicinal chemistry, Aug-16, Volume: 39, Issue:17 | Synthesis and in vitro and in vivo characteristics of an iodinated analogue of the beta-adrenoceptor antagonist carazolol. |
AID642116 | Metabolic stability in mouse liver microsomes assessed as compound remaining after 30 mins by LC-Ms/Ms analysis | 2011 | Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24 | Design and synthesis of 2-heterocyclyl-3-arylthio-1H-indoles as potent tubulin polymerization and cell growth inhibitors with improved metabolic stability. |
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AID1764461 | Protein binding in human plasma at 10 uM measured after 4 hrs by LC-MS/MS analysis | 2021 | Journal of medicinal chemistry, 03-25, Volume: 64, Issue:6 | Pyrazole Agonist of the Apelin Receptor Improves Symptoms of Metabolic Syndrome in Mice. |
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AID1810686 | Agonist activity at TAE expressed in human HEK293T cells coexpressing human full-length TLX/Gal4-VP 16 assessed as renilla luciferase reporter activity incubated for 14 hrs by Dual-glo luciferase | 2021 | Journal of medicinal chemistry, 06-24, Volume: 64, Issue:12 | Propranolol Activates the Orphan Nuclear Receptor TLX to Counteract Proliferation and Migration of Glioblastoma Cells. |
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AID55922 | Cardiac slowing index was measured for potency and efficacy | 1983 | Journal of medicinal chemistry, Feb, Volume: 26, Issue:2 | Cardiac-slowing amidines containing the 3-thioindone group. Potential antianginal agents. |
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AID568395 | Antihypertensive activity against methyl prednisolone acetate-induced hypertension in albino rat assessed as reduction in mean arterial pressure at 14 mg/kg, ip after 1 hr by tail-cuff method | 2011 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 21, Issue:3 | Triazole incorporated pyridazinones as a new class of antihypertensive agents: design, synthesis and in vivo screening. |
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AID1262871 | Chemical stability of compound in 0.1N NaOH assessed as compound remaining at 10 mg/ml after 2 days | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
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AID1740490 | Apparent permeability in MDCK-MDR1 cells at 10 uM after 30 mins by LC-MS/MS analysis | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | Design, synthesis, and biological evaluation of aryl piperazines with potential as antidiabetic agents via the stimulation of glucose uptake and inhibition of NADH:ubiquinone oxidoreductase. |
AID1146367 | Inhibition of isoproterenol-induced increase in heart rate in bilaterally vagotomized open chest mongrel dog model at 0.03 mg/kg, iv administered 10 to 20 mins prior to and following isoproterenol challenge | 1978 | Journal of medicinal chemistry, Jan, Volume: 21, Issue:1 | Synthesis of heteroaromatic potential beta-adrenergic antagonists by the glycidol route. |
AID1533477 | Apparent permeability from apical to basolateral side in MDCK cells | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Second generation of diazachrysenes: Protection of Ebola virus infected mice and mechanism of action. |
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AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347049 | Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500 | Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
AID504836 | Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation | 2002 | The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16 | Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells. |
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AID1347045 | Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500 | Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
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AID504812 | Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID588349 | qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay | |||
AID1347050 | Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500 | Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
AID504810 | Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
AID1159607 | Screen for inhibitors of RMI FANCM (MM2) intereaction | 2016 | Journal of biomolecular screening, Jul, Volume: 21, Issue:6 | A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway. |
AID1347154 | Primary screen GU AMC qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1745855 | NCATS anti-infectives library activity on the primary C. elegans qHTS viability assay | 2023 | Disease models & mechanisms, 03-01, Volume: 16, Issue:3 | In vivo quantitative high-throughput screening for drug discovery and comparative toxicology. |
AID1745854 | NCATS anti-infectives library activity on HEK293 viability as a counter-qHTS vs the C. elegans viability qHTS | 2023 | Disease models & mechanisms, 03-01, Volume: 16, Issue:3 | In vivo quantitative high-throughput screening for drug discovery and comparative toxicology. |
AID1346250 | Human beta2-adrenoceptor (Adrenoceptors) | 2003 | Molecular pharmacology, Sep, Volume: 64, Issue:3 | Influence of agonist efficacy and receptor phosphorylation on antagonist affinity measurements: differences between second messenger and reporter gene responses. |
AID1347018 | Rat beta3-adrenoceptor (Adrenoceptors) | 2004 | European journal of pharmacology, Jan-26, Volume: 484, Issue:2-3 | Stereoselectivity for interactions of agonists and antagonists at mouse, rat and human beta3-adrenoceptors. |
AID1346250 | Human beta2-adrenoceptor (Adrenoceptors) | 2005 | British journal of pharmacology, Feb, Volume: 144, Issue:3 | The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors. |
AID1346297 | Human beta3-adrenoceptor (Adrenoceptors) | 1999 | European journal of pharmacology, Feb-19, Volume: 367, Issue:2-3 | LK 204-545, a highly selective beta1-adrenoceptor antagonist at human beta-adrenoceptors. |
AID1346312 | Mouse beta3-adrenoceptor (Adrenoceptors) | 2004 | European journal of pharmacology, Jan-26, Volume: 484, Issue:2-3 | Stereoselectivity for interactions of agonists and antagonists at mouse, rat and human beta3-adrenoceptors. |
AID1346250 | Human beta2-adrenoceptor (Adrenoceptors) | 1999 | European journal of pharmacology, Feb-19, Volume: 367, Issue:2-3 | LK 204-545, a highly selective beta1-adrenoceptor antagonist at human beta-adrenoceptors. |
AID1346250 | Human beta2-adrenoceptor (Adrenoceptors) | 1999 | Molecular pharmacology, Nov, Volume: 56, Issue:5 | Binding pockets of the beta(1)- and beta(2)-adrenergic receptors for subtype-selective agonists. |
AID1346297 | Human beta3-adrenoceptor (Adrenoceptors) | 2004 | European journal of pharmacology, Jan-26, Volume: 484, Issue:2-3 | Stereoselectivity for interactions of agonists and antagonists at mouse, rat and human beta3-adrenoceptors. |
AID1798580 | 3H-CGP 12177 Whole Cell Binding Assay from Article 10.1038/sj.bjp.0706048: \\The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors.\\ | 2005 | British journal of pharmacology, Feb, Volume: 144, Issue:3 | The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 20315 (65.57) | 18.7374 |
1990's | 4614 (14.89) | 18.2507 |
2000's | 2522 (8.14) | 29.6817 |
2010's | 2820 (9.10) | 24.3611 |
2020's | 713 (2.30) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.
| This Compound (131.46) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 3,406 (10.23%) | 5.53% |
Reviews | 1,327 (3.98%) | 6.00% |
Case Studies | 1,978 (5.94%) | 4.05% |
Observational | 34 (0.10%) | 0.25% |
Other | 26,565 (79.75%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Trial | Phase | Enrollment | Study Type | Start Date | Status | ||
---|---|---|---|---|---|---|---|
Endoscopic Variceal Ligation Plus Propranolol And Isosorbide Mononitrate Versus Endoscopic Variceal Ligation Alone For Secondary Prophylaxis Of Variceal Bleeding: A Randomized Controlled Trial [NCT00766805] | 177 participants (Actual) | Interventional | 2002-10-31 | Completed | |||
Endoscopic Variceal Ligation as Primary Prophylaxis for Upper Gastrointestinal Bleeding in Children [NCT03943784] | 60 participants (Actual) | Observational | 2014-01-01 | Completed | |||
COMPARATIVE STUDY OF NORFLOXACIN AND PROBIOTICS ON PORTAL PRESSURE IN PATIENTS WITH CIRRHOSIS AND LARGE VARICES WHO HAVE NEVER BLED IN THE PAST [NCT01134692] | Phase 3 | 0 participants | Interventional | Recruiting | |||
A Randomized, Double Blind, Placebo Controlled, Multicenter Phase 2 Study of VT-122 in Combination With Sorafenib Compared to Sorafenib With Placebo in Patients With Hepatocellular Carcinoma and Systemic Inflammation at Risk for Cachexia [NCT01265576] | Phase 2 | 20 participants (Actual) | Interventional | 2010-12-31 | Active, not recruiting | ||
Effects of a Low-dose Propranolol on a Stress Induced Autonomic Response and on Muscle Pain [NCT01333150] | 16 participants (Anticipated) | Interventional | 2011-08-31 | Recruiting | |||
Reversal of Acute β-Blocker Induced Bronchoconstriction [NCT01070225] | Phase 4 | 14 participants (Actual) | Interventional | 2010-03-31 | Completed | ||
Feasibility Study: Therapeutic Targeting of Stress Factors in Ovarian Cancer Patients [NCT01308944] | Phase 1 | 24 participants (Actual) | Interventional | 2010-08-31 | Completed | ||
Comparison of Efficacy Between Combination of Amitriptyline-propranolol and Pizotifen for Migraine Prophylaxis: A Single-blind Randomized Controlled Trial [NCT06158230] | Phase 2 | 140 participants (Actual) | Interventional | 2023-03-19 | Active, not recruiting | ||
A Novel Treatment For Chronic Posttraumatic Stress Disorder (PTSD) Using Post-Reactivation Propranolol [NCT01127568] | Phase 2/Phase 3 | 50 participants (Anticipated) | Interventional | 2010-02-28 | Recruiting | ||
Impact of Post-Traumatic Stress Disorder Treatment by Reconsolidation Therapy on Fibromyalgia Syndrome [NCT04950426] | Phase 2 | 25 participants (Anticipated) | Interventional | 2021-08-13 | Recruiting | ||
Perioperative Use of a β-adrenergic Blocker, Propranolol, and a COX2 Inhibitor, Etodolac, in Patients Undergoing Resection With Curative Intent for Primary Colon and Rectal Cancer: Effect on Tumor Recurrence and Survival [NCT03919461] | Phase 2 | 200 participants (Anticipated) | Interventional | 2019-02-28 | Recruiting | ||
A Randomized, Double-blind, Parallel-group, 2-period, Placebo-controlled, Phase 1 Study to Investigate the Effects on Heart Rate, Blood Pressure, and Pharmacokinetic Interactions of the Up-titration Regimen of Ponesimod in Healthy Adult Subjects Receiving [NCT03882255] | Phase 1 | 52 participants (Actual) | Interventional | 2019-03-20 | Completed | ||
Propranolol Rescue of Prolonged Labor (PROPEL): A Randomized, Double-blind, Placebo-controlled Multicenter Investigation of Propranolol's Effect on Cesarean Delivery Rate Among Women With Prolonged Labor [NCT04299438] | Phase 3 | 164 participants (Actual) | Interventional | 2020-07-14 | Terminated(stopped due to Stopped at interim analysis) | ||
Perioperative Use of a Beta-adrenergic Blocker and a COX-2 Inhibitor in Patients Undergoing Surgery With Primary Pancreatic Cancer: Intervention Aiming to Reduce Pro-metastatic Processes [NCT03838029] | Phase 2 | 210 participants (Anticipated) | Interventional | 2019-11-20 | Recruiting | ||
Primary Prevention of Gastric Variceal Bleeding : Endoscopic Treatment Versus Non-selective Beta-blocker [NCT01298271] | Phase 4 | 120 participants (Anticipated) | Interventional | 2010-04-30 | Recruiting | ||
Reconsolidation as a Treatment Target for Cocaine Addiction [NCT01319214] | 60 participants (Anticipated) | Interventional | 2011-03-31 | Not yet recruiting | |||
N-of-1 Trials for Deprescribing Beta-blockers in HFpEF [NCT04767061] | Phase 4 | 9 participants (Actual) | Interventional | 2021-04-01 | Completed | ||
Reduction of the Reconsolidation of the Trauma Memory With Propranolol [NCT01349439] | Phase 2 | 76 participants (Anticipated) | Interventional | 2011-03-31 | Recruiting | ||
Clinical Research on Teratment of Gastrointestinal Cancer in the Preoperative by Propranolol [NCT03245554] | Early Phase 1 | 80 participants (Anticipated) | Interventional | 2018-05-01 | Not yet recruiting | ||
EUS-guided Therapy vs Non-selective Beta Blocker for the Primary Prophylaxis of Gastric Varices Bleed: a Randomized Controlled Trial [NCT05859009] | 0 participants (Actual) | Interventional | 2023-07-01 | Withdrawn(stopped due to No study oversight due to changes in study personnel.) | |||
Neurobehavioral Substrates of Propranolol's Effects on Drug Cue Reactivity [NCT03309943] | Phase 4 | 44 participants (Actual) | Interventional | 2018-01-16 | Completed | ||
Efficacy Evaluation of Propranolol Treatment of Hepatic Hemangioma [NCT03633747] | Phase 1/Phase 2 | 25 participants (Anticipated) | Interventional | 2018-07-01 | Recruiting | ||
Effect of Lasmiditan on Heart Rate and Blood Pressure in Healthy Subjects Receiving Oral Doses of Propranolol [NCT03270644] | Phase 1 | 44 participants (Actual) | Interventional | 2017-08-31 | Completed | ||
Controlling Hyperadrenergic Activity in Neurologic Injury [NCT01343329] | Phase 1/Phase 2 | 0 participants (Actual) | Interventional | 2011-07-31 | Withdrawn(stopped due to Unable to enroll subjects that fit study criteria.) | ||
A Study to Investigate Continuous Blood Pressure Monitoring Using Traditional Device (ABPM) Versus Novel Devices (Biobeat and Aktiia) [NCT05692869] | 24 participants (Actual) | Interventional | 2023-01-31 | Completed | |||
The Mechanism of Tremor Modulating Properties of Propranolol and Primidone in Essential Tremor: A Study With Transcranial Magnetic Stimulation and Eye Blink Classical Conditioning Paradigm [NCT04692844] | 61 participants (Actual) | Observational | 2017-08-28 | Completed | |||
Study of the Efficacy of Propranolol for the Management of Epistaxis in Hereditary Hemorrhagic Telangiectasia Patients [NCT04113187] | Phase 3 | 15 participants (Actual) | Interventional | 2020-06-23 | Completed | ||
An Exploratory Study Into the Mechanism of Mirabegron-induced Cardiovascular Effects in Healthy Male Subjects. [NCT01284868] | Phase 1 | 12 participants (Actual) | Interventional | 2009-07-31 | Completed | ||
Prophylaxis of Posttraumatic Stress Disorder With Post-Trauma Propranolol [NCT00158262] | Phase 4 | 43 participants (Actual) | Interventional | 2004-09-30 | Completed | ||
Endoscopic Treatment Alone Versus Combined Propranolol and Endoscopic Treatment of Acute Variceal Hemorrhage in Patients With HCC:a Randomized Trial [NCT01298284] | Phase 4 | 60 participants (Anticipated) | Interventional | 2009-10-31 | Recruiting | ||
¹³C-Methacetin Breath Test (MBT) Methodology Study [NCT01205074] | Phase 2/Phase 3 | 0 participants | Interventional | 2010-09-30 | Active, not recruiting | ||
Effects of Nabilone on Trauma Related Cue Reactivity in Cannabis Users With PTSD [NCT03251326] | Phase 1/Phase 2 | 4 participants (Actual) | Interventional | 2015-10-31 | Terminated(stopped due to Recruitment difficulties) | ||
Safety and Efficacy of Treatment With Propranolol in Newborns With Retinopathy of Prematurity: a Pilot Study [NCT01079715] | Phase 2/Phase 3 | 52 participants (Actual) | Interventional | 2010-01-31 | Completed | ||
Pharmacokinetic Study of Propranolol, Losartan, and Eprosartan in Healthy Volunteers and Patients With Chronic Kidney Disease [NCT01087749] | Phase 1 | 24 participants (Actual) | Interventional | 2010-03-31 | Completed | ||
Reconsolidation Therapy With Propranolol as a Novel Treatment for Chronic Pain : a Placebo-controlled Feasibility Study [NCT05085782] | Phase 2 | 48 participants (Anticipated) | Interventional | 2022-02-07 | Recruiting | ||
Sex Differences in Sympathetic Vascular Reactivity at High Altitude [NCT05525416] | 17 participants (Actual) | Interventional | 2022-07-28 | Completed | |||
Population Pharmacokinetics of Propafenone and Propranolol in Children Patients [NCT05463614] | 500 participants (Anticipated) | Observational | 2019-02-01 | Recruiting | |||
Role of Propranolol as Compared to Bleomycin in Management of Hemangioma [NCT05327309] | 90 participants (Actual) | Interventional | 2015-05-08 | Completed | |||
Examining the Impact of Propranolol on Preoperative Anxiety and on Tumorigenic Changes in Patients With Pancreatic Ductal Adenocarcinomas: a Randomized, Triple-blinded, Placebo-controlled Pilot Trial [NCT06145074] | Phase 2 | 30 participants (Anticipated) | Interventional | 2024-01-01 | Not yet recruiting | ||
Propranolol With Standard Chemoradiation for Esophageal Adenocarcinoma A Phase II Study [NCT04682158] | Phase 2 | 106 participants (Anticipated) | Interventional | 2021-04-01 | Recruiting | ||
Neoadjuvant Trial on the Efficacy of Propranolol Monotherapy in Cutaneous Angiosarcoma [NCT04518124] | Phase 2 | 14 participants (Actual) | Interventional | 2019-12-27 | Completed | ||
Dose Response and Receptor Selectivity of Beta-blocker Effects on Bone Metabolism [NCT02467400] | Early Phase 1 | 165 participants (Actual) | Interventional | 2015-07-01 | Completed | ||
Effects of Propranolol on Fear of Dental Extraction: Study Protocol for a Randomized Placebo-controlled Trial. [NCT02268357] | Phase 2/Phase 3 | 36 participants (Actual) | Interventional | 2014-11-30 | Completed | ||
Safety and Efficacy of Propranolol in the Treatment of Tardive Dyskinesia [NCT03254186] | Phase 2/Phase 3 | 0 participants (Actual) | Interventional | 2017-09-18 | Withdrawn(stopped due to No participants) | ||
The Effect of Carvedilol Vs Propranolol in Patients With Cirrhosis Related Esophagogastric Varices After Multiple Endoscopic Treatments For Secondary Prophylaxis:A Randomized Controlled Trial [NCT02385422] | Phase 4 | 480 participants (Anticipated) | Interventional | 2015-03-31 | Recruiting | ||
Adequate Therapy of Topiramate in Migraine [NCT01060111] | Phase 4 | 250 participants (Actual) | Interventional | 2006-07-31 | Completed | ||
Comparison of Treatment Response to Intravitreal Injection of Combined Propranolol and Bevacizumab Versus Bevacizumab Monotherapy in Patients With Wet Age Related Macular Degeneration :A Clinical Trial [NCT03609307] | Phase 2/Phase 3 | 40 participants (Anticipated) | Interventional | 2018-09-30 | Recruiting | ||
Evaluating the Effect of ADRB2 Blockers on PKA/BAD/CREB Signaling in Patients Undergoing Prostatectomy [NCT03152786] | Phase 2 | 46 participants (Actual) | Interventional | 2019-01-15 | Terminated(stopped due to PIs not interested in continuing with the trial.) | ||
A Randomised, Open Label, Four-way Crossover Phase I Trial to Investigate the in Vivo Specificity of a Single Oral Dose of 320 mg KUC 7483 CL Co-administered With Bisoprolol (10 mg Daily), Propranolol (160 mg Daily), and Acipimox (500 mg Daily) Over 5 Day [NCT02256722] | Phase 1 | 12 participants (Actual) | Interventional | 2005-10-31 | Completed | ||
Efficacy and Safety of Propranolol Versus Atenolol on the Proliferative Phase of Infantile Hemangioma [NCT02342275] | Phase 3 | 377 participants (Actual) | Interventional | 2013-10-31 | Completed | ||
Randomised Trial of 8mm Transjugular Intrahepatic Portosystemic Shunt Versus Endoscopic Variceal Ligation Plus Propranolol for Prevention of Variceal Rebleeding [NCT02477384] | 100 participants (Actual) | Interventional | 2015-06-30 | Completed | |||
The Efficacy of Traumatic Memory Modification Using a Memory Reconsolidation Procedure Under Propranolol Among Adolescents With Post-traumatic Stress Disorder [NCT04921982] | Phase 2 | 74 participants (Anticipated) | Interventional | 2023-05-31 | Not yet recruiting | ||
8mm-TIPS Versus Endoscopic Variceal Ligation (EVL) Plus Propranolol for Prevention of Variceal Rebleeding in Patients With Child A Cirrhosis [NCT03094234] | 72 participants (Anticipated) | Interventional | 2017-04-28 | Recruiting | |||
Beta-Adrenergic Blockade for Suppression of Catecholamine Surge Following Traumatic Brain Injury: A Randomized Trial [NCT02957331] | Phase 4 | 26 participants (Actual) | Interventional | 2016-01-31 | Completed | ||
Mechanistic Clinical Trial of Beta-Blocker Administration For Reactivating Cardiomyocyte Division In Tetrology of Fallot [NCT04713657] | Phase 1 | 40 participants (Anticipated) | Interventional | 2022-12-16 | Recruiting | ||
Multicenter Study of Antiarrhythmic Medications for Treatment of Infants With Supraventricular Tachycardia [NCT00390546] | Phase 3 | 72 participants (Actual) | Interventional | 2006-10-31 | Completed | ||
Comparison of Effect of Propranolol, Bisoprolol, Pyridosgitmine in Postural Orthostatic Tachycardia Syndrome (POTS) and Prognosis After Medical Treatment [NCT02171988] | Phase 4 | 150 participants (Actual) | Interventional | 2014-03-31 | Completed | ||
Effect of Oral Propranolol on mRNA Expression in Symptomatice Caavernous Malformation [NCT03474614] | Phase 2 | 20 participants (Anticipated) | Interventional | 2018-01-24 | Active, not recruiting | ||
Beta Blocker Use In Traumatic Brain Injury Based On The High-Sensitive Troponin T Status: A Randomized Controlled Trial (BBTBBT) [NCT04508244] | Phase 4 | 771 participants (Anticipated) | Interventional | 2020-12-29 | Recruiting | ||
Safety and Efficacy of Lacosamide Versus Propranolol in Migraine [NCT05851781] | Phase 3 | 600 participants (Actual) | Interventional | 2022-06-01 | Completed | ||
Effect of Prophylactic, Perioperative Propranolol on Peri- and Postoperative Complications in Patients With Post Traumatic Stress Disorder [NCT01555554] | 59 participants (Actual) | Interventional | 2012-05-31 | Terminated(stopped due to Unable to meet enrollment goals.) | |||
Short Term Effects of Propanolol on Heart Rate Variability of Hyperthyroidism [NCT03393728] | Phase 4 | 10 participants (Actual) | Interventional | 2008-09-01 | Completed | ||
Treatment of Renal Angiomyolipomas in Tuberous Sclerosis by Beta-blockers: Pilot Trial [NCT02104011] | Phase 2 | 2 participants (Actual) | Interventional | 2015-05-22 | Completed | ||
Oral Propanolol for Surgically Inaccessible Cerebral and Spinal Cavernous Malformations [NCT03523650] | Phase 1 | 346 participants (Anticipated) | Interventional | 2018-02-07 | Enrolling by invitation | ||
Open-label, Uncontrolled Study of the Off Label Use of Propranolol for Infancy Hemangiomas to Identify Side Effects [NCT01211080] | 72 participants (Actual) | Observational | 2008-08-31 | Completed | |||
Management of Supraventricular Tachycardia of Children Admitted to Assiut University Children Hospital(Clinical Audit) [NCT03528616] | 50 participants (Anticipated) | Observational [Patient Registry] | 2018-05-15 | Not yet recruiting | |||
Study of Propranolol Hydrochloride in Combination With Sintilimab and Platinum-based Chemotherapy for Treatment of Advanced Non-small Cell Lung Cancer (BRIO) [NCT05979818] | Phase 1 | 6 participants (Anticipated) | Interventional | 2023-12-31 | Not yet recruiting | ||
Reliving the Traumatic Event in Posttraumatic Stress Disorder: An Emotional Memory Reactivation Pathology? An fMRI Study [NCT01239173] | Phase 3 | 5 participants (Actual) | Interventional | 2010-09-30 | Terminated(stopped due to Study stopped by promoter for lack of inclusion) | ||
Safety and Efficacy of Propranolol 0.2% Eye Drops in Treating Newborn With Retinopathy of Premature: A Pilot Study (DROP-ROP-0.2%) [NCT02504944] | Phase 2 | 98 participants (Actual) | Interventional | 2015-07-31 | Completed | ||
A Phase II Study of Propranolol Plus Sunitinib in First-line Treatment of Metastatic Renal Cell Carcinoma (ProSun Study) [NCT03323710] | Phase 2 | 0 participants (Actual) | Interventional | 2018-09-30 | Withdrawn(stopped due to Poor patient recruitment.) | ||
Propranolol, Carvedilol and Rosuvastatin in the Prevention of Recurrent Variceal Haemorrhage in Patients With Cirrhotic Portal Hypertension [NCT03720067] | Phase 2/Phase 3 | 80 participants (Anticipated) | Interventional | 2019-01-25 | Recruiting | ||
HVPG-guided Laparoscopic Versus Endoscopic Therapy for Variceal Rebleeding in Portal Hypertension: A Multicenter Randomized Controlled Trial (CHESS1803) [NCT03783065] | 40 participants (Anticipated) | Interventional | 2019-01-02 | Recruiting | |||
The Efficacy of Early Propranolol Administration at Preventing/Reducing PTSD Symptoms in Child Trauma Victims: Pilot. [NCT00597389] | 29 participants (Actual) | Interventional | 2004-02-29 | Completed | |||
Trial of Propranolol in Children and Youth With Autism Spectrum Disorder and Predictors of Response [NCT02871349] | Early Phase 1 | 69 participants (Actual) | Interventional | 2016-08-31 | Completed | ||
Safety and Efficacy of Propranolol Eye Drops in Newborns With Retinopathy of Premature (DROP-PROP) [NCT02014454] | Phase 2 | 23 participants (Actual) | Interventional | 2013-11-30 | Completed | ||
A Randomised, Controlled, Multidose, Multicentre, Adaptive Phase II/III Study in Infants With Proliferating Infantile Hemangiomas (IHs) Requiring Systemic Therapy to Compare 4 Regimens of Propranolol (1 or 3 mg/kg/Day for 3 or 6 Months) to Placebo (Double [NCT01056341] | Phase 2/Phase 3 | 512 participants (Actual) | Interventional | 2010-01-31 | Completed | ||
Biopsychosocial Influence on Shoulder Pain: a Randomized, Pre-clinical Trial [NCT02620579] | Phase 2 | 264 participants (Actual) | Interventional | 2016-01-31 | Completed | ||
Evaluation of the Efficacy of Captopril Versus Propranolol and Timolol as a Treatment of Infantile Capillary Hemangioma [NCT04288700] | Phase 4 | 100 participants (Anticipated) | Interventional | 2019-10-01 | Recruiting | ||
Propranolol vs Prednisolone for Infant Hemangiomas-A Clinical and Molecular Study [NCT00967226] | Phase 2 | 19 participants (Actual) | Interventional | 2009-07-31 | Terminated(stopped due to Serious adverse events with prednisolone, primarily temporary growth retardation, <5th percentile.) | ||
Early Primary Prophylaxis With Beta-Blockers In Prevention Of Growth Of Small Esophageal Varices In Cirrhosis: A Randomized Controlled Trial [NCT00772057] | 164 participants (Actual) | Interventional | 2004-10-31 | Completed | |||
Does Oral Propranolol Accelerate Labor Induction/Augmentation With Oxytocin in Nulliparous Women in Abakaliki? [NCT05251610] | 110 participants (Actual) | Interventional | 2020-11-02 | Completed | |||
Misophonia-Related Memory Modification Using Reconsolidation Mechanisms: Pharmacological and Behavioral Manipulation [NCT05928689] | Early Phase 1 | 150 participants (Anticipated) | Interventional | 2023-06-02 | Recruiting | ||
"Comparison of Effectiveness of Sekanjabin e Safarjali (Quince Oxymel), Propranolol and Placebo in the Prevention of Migraine Attacks in Patients With Simultaneous Upper Gastrointestinal Dysfunction" [NCT02179775] | 45 participants (Anticipated) | Interventional | 2014-07-31 | Recruiting | |||
To Study the Effect of Nonselective Beta Blockers in Advanced Stage Liver Disease With Ascites [NCT02649335] | Phase 3 | 190 participants (Actual) | Interventional | 2015-07-01 | Completed | ||
Contribution of COMT Haplotypes in Propranolol Analgesic Efficacy for Treating Post-surgical Pain After Laparoscopic Hemicolectomy [NCT02511483] | Phase 2 | 10 participants (Actual) | Interventional | 2015-05-18 | Terminated(stopped due to Difficulty with recruitment) | ||
A Randomized, Blank-controlled, Open Label Study of the Safety and Efficacy of Propranolol in Reducing Stroke Associated Pneumonia and Urinary Tract Infection [NCT05375240] | Phase 2 | 45 participants (Anticipated) | Interventional | 2022-06-30 | Not yet recruiting | ||
Evaluation of Intestinal Permeability in Cirrhotic Patients Before and After Treatment With Non-selective Beta Blocker (Propranolol) [NCT02484573] | 39 participants (Anticipated) | Interventional | 2015-05-31 | Recruiting | |||
Impact of Beta-2 Adrenergic Blockade With Checkpoint Inhibition in Checkpoint Inhibitor Refractory Metastatic Triple Negative Breast Cancer [NCT05741164] | Phase 2 | 25 participants (Anticipated) | Interventional | 2023-12-15 | Not yet recruiting | ||
Improving Host Factors in Patients With Monoclonal Gammopathies [NCT05312255] | 150 participants (Anticipated) | Interventional | 2022-06-28 | Recruiting | |||
Propranolol Versus Propranolol and Clonidine in Sympathetic Hyperactivity After Moderate Traumatic Brain Injury [NCT04833218] | Early Phase 1 | 90 participants (Anticipated) | Interventional | 2020-01-31 | Active, not recruiting | ||
Trial of Propranolol in Adults and Adolescents With Autism Spectrum Disorder (ASD) and Predictors of Response [NCT02414451] | 0 participants (Actual) | Interventional | 2016-09-30 | Withdrawn(stopped due to No need for a pilot study. New study will be opened.) | |||
A Randomized Controlled Trial Comparing Cyanoacrylate Injection Versus Beta-Blockers Versus No Treatment for Primary Prophylaxis of Gastric Variceal Bleed [NCT00905996] | 74 participants (Actual) | Interventional | 2006-08-31 | Completed | |||
Evaluation of Beta Blockers for the Treatment of Asthma. A Randomised Controlled Trial of Propranolol [NCT01074853] | Phase 2 | 18 participants (Actual) | Interventional | 2010-05-31 | Completed | ||
Double Blind, Randomised, Placebo-controlled Study of Propranolol in Infantile Capillary Hemangiomas [NCT00744185] | Phase 2/Phase 3 | 14 participants (Actual) | Interventional | 2008-10-31 | Terminated(stopped due to Study halted prematurely due to some difficulties in recruitment of patients) | ||
Randomized Controlled Trial Comparing Propranolol, Endoscopic Banding Ligation, and Combined Treatment to Prevent First Variceal Hemorrhage in Patients With Liver Cirrhosis [NCT00965900] | Phase 4 | 288 participants (Anticipated) | Interventional | 2006-09-30 | Recruiting | ||
[NCT00759005] | 0 participants | Interventional | 2007-03-31 | Completed | |||
Association Between Angiotensin Converting Enzyme Inhibitor or Angiotensin Receptor Blocker Use and COVID-19 Severity and Mortality Among US Veterans [NCT04467931] | 22,213 participants (Actual) | Observational | 2020-01-19 | Completed | |||
The Use of Propranolol to Block Memory Reconsolidation in Post Traumatic Stress Disorders (PTSD) [NCT00611871] | Phase 2 | 12 participants (Actual) | Interventional | 2007-09-30 | Terminated(stopped due to Low enrollment, grant term expired) | ||
Memory Reconsolidation Blockade as a Novel Intervention for Nicotine Dependence [NCT00916721] | Phase 3 | 113 participants (Actual) | Interventional | 2008-04-30 | Completed | ||
Banding Ligation Plus Propranolol Versus Banding Ligation to Prevent Rebleeding of Esophageal Varices [NCT02740166] | Phase 4 | 212 participants (Anticipated) | Interventional | 2013-06-30 | Recruiting | ||
[NCT02732678] | Phase 1/Phase 2 | 24 participants (Anticipated) | Interventional | 2016-05-31 | Not yet recruiting | ||
Efficacy of Ivabradine Versus Propranolol Premedication During Hypotensive Anesthesia in Endoscopic Sinus Surgery [NCT04208594] | 50 participants (Anticipated) | Interventional | 2019-12-11 | Recruiting | |||
Konditionerende Smertestimuli - Sammenligning af Forskellige Test og Konditioneringsmodaliteter [NCT02808611] | 25 participants (Actual) | Interventional | 2016-07-31 | Completed | |||
RCT Comparing the Efficacies of Endoscopic Variceal Ligation (EBL) and Combined Treatment of Beta-blocker and EBL for the Prevention of Esophageal Variceal Rebleeding [NCT00966121] | Phase 4 | 180 participants (Anticipated) | Interventional | 2008-08-31 | Recruiting | ||
Single-Dose Fasting Bioequivalence Study of Propranolol Hydrochloride Extended-Release Capsules (160 mg; Mylan) and Inderal® LA Capsules (160 mg; Wyeth) in Healthy Volunteers [NCT00647816] | Phase 1 | 100 participants (Actual) | Interventional | 2005-09-30 | Completed | ||
Comparative, Randomized, Single-Dose, 2 Way Cross Over Bioavailability Study of Par Propranolol 160 mg With That of Inderal-LA Propranolol 160 mg in Healthy Subjects Under Fasting Conditions. [NCT00653120] | Phase 2 | 48 participants (Actual) | Interventional | 2005-05-31 | Completed | ||
Phase IIB Study: TRAUMA HELP: Healing and Analgesia With Propranolol [NCT01007084] | Phase 2 | 0 participants (Actual) | Interventional | 2009-10-31 | Withdrawn(stopped due to Lack of eligible patient recruits/feasibility considerations.) | ||
How Does the Brain Learn About Positive and Negative Things? [NCT06014606] | 150 participants (Actual) | Interventional | 2021-03-01 | Completed | |||
Treatment of Pediatric Post-traumatic Stress Disorder With Memory Reactivation Under the Influence of Propranolol: A Randomized Placebo-controlled Trial. PPP [NCT04985344] | Phase 3 | 92 participants (Anticipated) | Interventional | 2023-02-01 | Recruiting | ||
Perioperative β-adrenergic Blocker and a COX2 Inhibitor in Patients Undergoing Resection for Primary Colon and Rectal Cancer: Effect on Tumor Recurrence and Postoperative Immune Perturbations. A Multicenter Randomized Prospective Trial. [NCT00888797] | Phase 3 | 400 participants (Anticipated) | Interventional | 2010-01-31 | Recruiting | ||
Candesartan vs Propranolol for Migraine Prevention: A Double Blind, Placebo Controlled, Double Dummy, Triple Cross-over Study [NCT00884663] | Phase 2/Phase 3 | 72 participants (Actual) | Interventional | 2009-04-30 | Completed | ||
A Phase 2 Trial of Chemotherapy, Pembrolizumab, and Propranolol in Advanced Esophageal/Gastroesophageal Junction Adenocarcinoma Patients [NCT05651594] | Phase 2 | 40 participants (Anticipated) | Interventional | 2023-03-07 | Recruiting | ||
Does Propranolol, a Beta Blocker, Attenuate Stress-Induced Drinking? [NCT03588754] | Phase 2 | 20 participants (Anticipated) | Interventional | 2018-09-15 | Recruiting | ||
Treatment of Orthostatic Intolerance [NCT00262470] | Phase 1/Phase 2 | 150 participants (Anticipated) | Interventional | 1997-04-30 | Active, not recruiting | ||
Efficacy and Safety of Propranolol Combined With Neoadjuvant Chemotherapy in Stage III-IV Gastric Cancer: an Open-lable, Single-arm Study [NCT04005365] | Phase 2 | 78 participants (Anticipated) | Interventional | 2019-11-20 | Recruiting | ||
Efficacy of SCH 420814 to Reduce the Frequency or Severity of Neuroleptic Induced Akathisia [NCT00693472] | Phase 2 | 46 participants (Actual) | Interventional | 2007-08-15 | Terminated | ||
Effects of Exercise in Orthostatic Intolerance [NCT00770484] | 12 participants (Actual) | Interventional | 2008-11-30 | Completed | |||
Cold Induced Changes in Human Subcutaneous White Adipose [NCT02596776] | Early Phase 1 | 26 participants (Actual) | Interventional | 2016-03-31 | Completed | ||
Effects of Propranolol on Responses to Drug-Related Imagery Scripts [NCT00688805] | Phase 1 | 40 participants (Actual) | Interventional | 2007-12-12 | Terminated | ||
The Pathophysiology of Orthostatic Hypotension [NCT00748059] | Phase 1 | 10 participants (Actual) | Interventional | 1996-12-31 | Completed | ||
NINDS Clinical Research Collaboration Chronic Migraine Treatment Trial [NCT00772031] | Phase 3 | 191 participants (Actual) | Interventional | 2008-10-31 | Completed | ||
A Randomized, Open-label, Active Control Trial to Evaluate the Effect of LOSARTAN Therapy on the Progression of Aortic Root Dilation in Patients With Marfan Syndrome [NCT00651235] | Phase 2 | 44 participants (Anticipated) | Interventional | 2007-02-28 | Recruiting | ||
Effects of Propranolol on the Encoding and Retrieval of Emotional Material After Single Dose Administration in Healthy Young Subjects [NCT00889096] | Phase 1 | 46 participants (Anticipated) | Interventional | Completed | |||
Serum Betatrophin Levels and Its Influencing Factors in Patients With Hyperthyroidism [NCT02812888] | 240 participants (Anticipated) | Observational [Patient Registry] | 2016-07-31 | Recruiting | |||
The BURN HELP Trial: BURN Healing and AnaLgesia With Propranolol [NCT00934947] | Phase 2 | 45 participants (Actual) | Interventional | 2009-07-31 | Completed | ||
Propranolol for Syncope With Sympathoadrenal Imbalance [NCT00060866] | Phase 4 | 24 participants | Interventional | 2003-05-31 | Completed | ||
Targeting Fear Memory by Disrupting the Process of Reconsolidating: A New Intervention for Panic Disorder [NCT02631694] | Phase 2 | 60 participants (Anticipated) | Interventional | 2016-04-30 | Not yet recruiting | ||
Using Reconsolidation Blockade to Treat Trauma Related Disorders After Paris Attacks: an Effectiveness Study [NCT02789982] | Phase 3 | 364 participants (Actual) | Interventional | 2016-05-27 | Completed | ||
Drug and Non-Drug Treatment of Severe Migraine [NCT00910689] | Phase 4 | 232 participants (Actual) | Interventional | 2001-07-31 | Completed | ||
A Randomized Controlled Trial of Medical Therapies for Chronic Post-Traumatic Headaches [NCT00862095] | Phase 4 | 64 participants (Actual) | Interventional | 2008-06-30 | Terminated(stopped due to inadequate enrollment, insufficient funds to continue enrollment) | ||
A Relative Bioavailability Study of 160 mg Propranolol Hydrochloride Extended Release Capsules Under Fasting Conditions [NCT00865215] | Phase 1 | 60 participants (Actual) | Interventional | 2005-04-30 | Completed | ||
"'' Efficacy of Propranolol in the Treatment of Infantile Hemangioma" [NCT04684667] | Phase 2 | 100 participants (Anticipated) | Interventional | 2021-01-01 | Not yet recruiting | ||
Effectiveness of Pre-surgical Hand Washing in Reducing Bacterial Load, Using an Alcoholic Solution of Chlorhexidine Digluconate and Potassium Sorbate [NCT04683146] | Phase 4 | 24 participants (Anticipated) | Interventional | 2021-03-10 | Not yet recruiting | ||
A Relative Bioavailability Study of 160 mg Propranolol Hydrochloride Extended Release Capsules Under Non-Fasting Conditions [NCT00864747] | Phase 1 | 60 participants (Actual) | Interventional | 2005-05-31 | Completed | ||
RCT Comparing the Efficacies of Endoscopic Band Ligation (EBL) and Combined Treatment of Beta-blocker and EBL for the Prevention of Esophageal Variceal Rebleeding in Patients With Previous Endoscopic Variceal Treatment [NCT00966082] | Phase 4 | 180 participants (Anticipated) | Interventional | 2008-08-31 | Recruiting | ||
Comparison of Endoscopic Variceal Ligation (EVL) and Propranolol in Secondary Prophylaxis of Variceal Bleeding in Patients With Non Cirrhotic Portal Hypertension (NCPH): A Prospective Randomized Controlled Trial [NCT01000779] | Phase 3 | 100 participants (Anticipated) | Interventional | 2005-01-31 | Completed | ||
Impact of Nonselective Beta-blocker on Acute Kidney Injury in Cirrhotic Patients With Esophageal Varices [NCT04074473] | Phase 4 | 170 participants (Anticipated) | Interventional | 2015-04-13 | Recruiting | ||
A Study to Investigate the Relative Pharmacological Activity of Aninhaled B2-agonist/Anticholinergic Dual Pharmacophore Inhealthy Volunteers [NCT00687700] | Phase 1 | 23 participants (Actual) | Interventional | 2008-03-10 | Completed | ||
Propranolol Administration in Pediatric Patients With Recurrent Respiratory Papillomatosis [NCT01058317] | Phase 2/Phase 3 | 0 participants (Actual) | Interventional | 2010-01-31 | Withdrawn(stopped due to No participants enrolled) | ||
Clinical and Molecular Effects of Catecholamine Blockade Post-burn [NCT01299753] | 80 participants (Anticipated) | Interventional | 2011-02-28 | Active, not recruiting | |||
Cognitive Side Effects of Commonly Prescribed Medications in Pediatric Migraine [NCT00777218] | 0 participants (Actual) | Interventional | 2007-08-31 | Withdrawn(stopped due to Enrollment criteria was too challenging and Investigators changed Institutions) | |||
Beta Blocker Effects on Patients With Traumatic Brain Injury [NCT05195996] | Phase 4 | 40 participants (Actual) | Interventional | 2021-10-01 | Completed | ||
N-of-1 Trials for Deprescribing Beta-blockers in HFpEF [NCT04757584] | Phase 4 | 9 participants (Actual) | Interventional | 2021-04-01 | Completed | ||
Hemodynamic Response of Rifaximin and Non-selective β-blocker Combination Therapy Versus Non-selective β-blocker Monotherapy in Cirrhotic Patients With Esophageal Varices [NCT01897051] | Phase 2/Phase 3 | 140 participants (Anticipated) | Interventional | 2013-07-31 | Recruiting | ||
Propranolol Treatment of Traumatic Memories (PTTM) [NCT01069159] | 66 participants (Anticipated) | Interventional | 2010-02-28 | Recruiting | |||
[NCT00000492] | Phase 3 | 0 participants | Interventional | 1977-09-30 | Completed | ||
Secondary Prophylaxis of Gastrointestinal Bleeding in Cirrhotic Patients Using Thalidomide [NCT00787436] | Phase 3 | 0 participants (Actual) | Interventional | 2006-05-31 | Withdrawn | ||
Treatment of Winter Depression With Pharmacological Suppression of Melatonin Secretion [NCT00016666] | Phase 2 | 70 participants | Interventional | 2001-05-21 | Completed | ||
Opioid Induced Hyperalgesia (OIH) Modulation With Propranolol, in Laparoscopic Abdominal Surgery [NCT02934763] | Phase 4 | 80 participants (Anticipated) | Interventional | 2016-10-31 | Not yet recruiting | ||
A Comparative Study of the Use of Beta Blocker and Oral Corticosteroid in the Treatment of Proliferative and Involuting Cutaneous Infantile Hemangioma [NCT01072045] | Phase 2 | 50 participants (Actual) | Interventional | 2010-01-31 | Completed | ||
Evaluation of Gastrointestinal Transite in Cirrhotic Patient Pre and Post Treatment With Non Selective Betablockers (Propanolol) [NCT02923336] | 10 participants (Anticipated) | Interventional | 2015-05-31 | Recruiting | |||
A Double-Blind, Placebo Controlled Trial of Propranolol and Amantadine for the Treatment of Cocaine Dependent Subjects With Severe Cocaine Withdrawal Symptoms [NCT00158132] | Phase 2 | 199 participants (Actual) | Interventional | 1999-09-30 | Completed | ||
Multicenter, Randomized, Double-blind, Placebo-controlled Study on the Effectiveness of Treatment With Beta-blockers to Prevent Decompensation of Cirrhosis With Portal Hypertension [NCT01059396] | Phase 4 | 201 participants (Actual) | Interventional | 2010-01-28 | Completed | ||
Beta-Blocker in Acute Ischemic Stroke - a Prospective, Randomized, Double-blinded, Placebo-controlled Safety and Efficacy Trial of Early Treatment [NCT01061190] | Phase 2/Phase 3 | 20 participants (Actual) | Interventional | 2010-01-31 | Completed | ||
Efficacy of Propranolol for the Treatment of Central Nervous System Hemangioblastomas in Von Hippel-Lindau Disease: a Randomized Controlled Clinical Trial [NCT05424016] | 85 participants (Anticipated) | Interventional | 2023-01-16 | Recruiting | |||
A Comparison Between the Effect of Oxytocin Only and Oxytocin Plus Propranolol on Induction of Labor in Term Pregnancy [NCT03533699] | 202 participants (Anticipated) | Interventional | 2016-10-01 | Recruiting | |||
Protective Effects of Propranolol in Adults Following Major Burn Injury: A Safety and Efficacy Trial [NCT01902810] | Phase 2/Phase 3 | 47 participants (Actual) | Interventional | 2013-07-31 | Terminated(stopped due to At the request of the study site, this study has been closed and access to study-related data is unavailable. We are unable to submit the results-data.) | ||
Placebo-Controlled Randomized Trial of Oxytocin Alone Versus Oxytocin and Propranolol for the Treatment of Dysfunctional Labor [NCT00315913] | Phase 2 | 0 participants (Actual) | Interventional | 2004-01-31 | Withdrawn(stopped due to Lack of feasibility) | ||
Immune Checkpoint Inhibitors With or Without Propranolol Hydrochloride In Patients With Urothelial Carcinoma [NCT04848519] | Phase 2 | 24 participants (Anticipated) | Interventional | 2021-05-20 | Recruiting | ||
Safety and Efficacy of Propranolol in Severely Burned Children [NCT01957449] | Phase 2/Phase 3 | 63 participants (Actual) | Interventional | 2013-12-31 | Terminated(stopped due to At the request of the study site, this study has been closed and access to study-related data is unavailable. We are unable to submit the results-data.) | ||
Endoscopic Treatment Versus Propranolol for Primary Prevention of Patients With Hepatocellular Carcinoma and Concomitant Esophageal Varices [NCT01970748] | Phase 4 | 200 participants (Anticipated) | Interventional | 2009-08-31 | Recruiting | ||
Phase 2 Prospective Study of the Efficacy of Propranolol on Malignant Melanoma Progression. A Randomized Placebo-controlled,Single Blind Trial [NCT01988831] | Phase 2 | 450 participants (Anticipated) | Interventional | 2016-06-30 | Suspended(stopped due to We must delay the study for some financial reasons) | ||
Assessment of Mechanisms of Improved Wound Healing of Anabolic Agents and Diet in Severely Burned Patients [NCT00673309] | Phase 2/Phase 3 | 644 participants (Actual) | Interventional | 2000-07-31 | Completed | ||
Propanolol Effect on Red Cell Adhesion in Non-Asthmatic Children With Sickle Cell Disease: A Dose Finding Study [NCT02012777] | Phase 1 | 9 participants (Actual) | Interventional | 2010-06-30 | Terminated(stopped due to Inability to recruit patients into the study.) | ||
[NCT00000493] | Phase 3 | 0 participants | Interventional | 1977-09-30 | Completed | ||
Comparative Study Between Oral Ivabradine Versus Oral Propranolol for Induced Hypotension in Functional Endoscopic Sinus Surgery [NCT04580342] | Phase 2 | 60 participants (Anticipated) | Interventional | 2020-10-15 | Recruiting | ||
Molecular Basis of Loss Aversion [NCT06034158] | 60 participants (Anticipated) | Interventional | 2023-09-18 | Recruiting | |||
Pathophysiology of Orthostatic Intolerance [NCT00608725] | 100 participants (Anticipated) | Interventional | 1996-12-31 | Recruiting | |||
Establishing and Eliminating Cue-drug Associations in Human Cocaine Addiction [NCT01978457] | Phase 1 | 6 participants (Actual) | Interventional | 2012-10-31 | Terminated(stopped due to Not funded) | ||
Endoscopic Cyanoacrylate Injection Versus Beta-Blockers for Secondary Prophylaxis of Gastric Variceal Bleed [NCT00888784] | 64 participants (Actual) | Interventional | 2006-08-31 | Completed | |||
ANALYSIS OF THE EFFECTIVENESS OF A STAGED MANAGEMENT PROGRAM AIMED AT CONTROLLING BLOOD PRESSURE AND BLOOD GLUCOSE OF TYPE 2 DIABETIC PATIENTS USING EXCLUSIVELY THE RESOURCES AVAILABLE IN A PRIMARY CARE SETTING IN BRAZIL [NCT00935805] | 124 participants (Anticipated) | Observational | 2006-07-31 | Active, not recruiting | |||
Assessment of the Treatment of the Severely Burned With Anabolic Agents on Clinical Outcomes, Recovery and Rehabilitation [NCT00675714] | Phase 2/Phase 3 | 1,126 participants (Actual) | Interventional | 2004-01-31 | Terminated(stopped due to At the request of the study site, this study has been closed and access to study-related data is unavailable. We are unable to submit the results-data.) | ||
Effect of Prophylaxy of Amiodarone and Propranolol and Amiodarone With Propranolol in Prevention of Atrial Fibrillation Post Coronary Artery Bypass Graft, A Prospective Double-Blind Randomized Study [NCT00654290] | 240 participants (Actual) | Interventional | 2007-03-31 | Completed | |||
Treating Adjustment Disorders Stemming From Romantic Betrayals: An Open-label Trial of Impairing Memory Reconsolidation Using Propranolol [NCT03151681] | Phase 2/Phase 3 | 84 participants (Actual) | Interventional | 2015-11-01 | Completed | ||
The Effect of Coadministration of Oral Propranolol to Oxytocin on Induction of Labor [NCT02702674] | Phase 3 | 242 participants (Anticipated) | Interventional | 2015-12-31 | Recruiting | ||
"Efficacy of Combination of Midodrine With Propranolol in Preventing First Bleed in Decompensated Cirrhotics With Severe Ascites: A Randomized Controlled Trial" [NCT04208776] | 120 participants (Anticipated) | Interventional | 2020-02-04 | Recruiting | |||
Single-Dose Fed Bioequivalence Study of Propranolol Hydrochloride Extended-Release Capsules (160 mg; Mylan) and Inderal® LA Capsules (160 mg; Wyeth) in Healthy Volunteers [NCT00647608] | Phase 1 | 98 participants (Actual) | Interventional | 2005-09-30 | Completed | ||
Comparative, Randomized, Single-Dose, 2 Way Cross Over Bioavailability Study of Par Propranolol 160 mg With That of Inderal-LA Propranolol 160 mg in Healthy Subjects Under Fed Conditions. [NCT00652600] | Phase 1 | 46 participants (Actual) | Interventional | 2005-09-30 | Completed | ||
Transjugular Intrahepatic Portosystemic Shunt (TIPS) for Variceal Rebleeding in Cirrhotic Patients With Occlusive Portal Vein Thrombosis (PVT) and Cavernous Transformation of the Portal Vein (CTPV) [NCT02853526] | Phase 3 | 100 participants (Anticipated) | Interventional | 2015-07-31 | Recruiting | ||
Cognitive vs. Emotional Psycho-Pharmacological Manipulations of Fear vs. Anxiety [NCT02153944] | Phase 4 | 142 participants (Actual) | Interventional | 2014-06-16 | Completed | ||
The Effect of Beta-Blockers, Aspirin, and Natural Habituation on Procoagulant Activity, Expression of Cellular Adhesion Molecules, and Endothelial Activation in Response to Acute Mental Stress: a Randomized Controlled Trial. [NCT00174902] | Phase 1/Phase 2 | 80 participants | Interventional | 2003-10-31 | Active, not recruiting | ||
A Randomized, Placebo Controlled, Multicenter Phase 2 Study of Etodolac and Propranolol in Patients With Clinically Progressive Prostate Cancer [NCT01857817] | Phase 2 | 35 participants (Actual) | Interventional | 2013-06-30 | Terminated(stopped due to Low patient recruitment) | ||
Mismatch vs. Standard Intervention During Memory Reconsolidation Blockade With Propranolol: Effect on Psychophysiological Reactivity During Traumatic Imagery [NCT05853627] | Phase 4 | 80 participants (Anticipated) | Interventional | 2023-08-31 | Not yet recruiting | ||
Phase II Study of Propranolol as Anti-Adhesive Therapy for Sickle Cell Disease [NCT01077921] | Phase 2 | 31 participants (Actual) | Interventional | 2010-06-30 | Completed | ||
TIPS Versus Endoscopic Therapy for the Prevention of Variceal Rebleeding in Cirrhotic Patients With Portal Vein Thrombosis: A Randomized Controlled Trial [NCT02485184] | 120 participants (Anticipated) | Interventional | 2017-07-09 | Recruiting | |||
Propranolol as a Treatment for Impaired Awareness of Hypoglycemia in Type 1 Diabetes [NCT03161964] | Phase 2 | 2 participants (Actual) | Interventional | 2017-10-19 | Terminated(stopped due to Statistical power could not be achieved due to low enrollment.) | ||
An Intra-patient Dose Escalation Study of Propranolol in Patients With Lymphedema [NCT02595996] | Phase 2 | 1 participants (Actual) | Interventional | 2017-06-07 | Terminated(stopped due to Lack of funding) | ||
Reduction of the Traumatic Memory by Reconsolidation Blockade: A Pilot Study [NCT00465608] | Phase 2 | 20 participants (Anticipated) | Interventional | 2007-04-30 | Completed | ||
The Surrogate Marker of Rate Control in Patients With Atrial Fibrillation [NCT04513509] | 50 participants (Anticipated) | Interventional | 2020-08-07 | Not yet recruiting | |||
Endoscopic Treatment Alone Versus Combined Propranolol and Endoscopic Treatment of Acute Variceal Hemorrhage in Patients With Hepatocellular Carcinoma [NCT01451658] | Phase 4 | 100 participants (Anticipated) | Interventional | 2009-12-31 | Recruiting | ||
A Study to Optimise the Propranolol Block Model for Assessment of the Pharmacological Activity of Bronchodilators in Healthy Volunteers. [NCT00549120] | Phase 1 | 18 participants (Actual) | Interventional | 2007-08-15 | Completed | ||
Testing a Novel Therapeutic Strategy for Comorbid Post-Traumatic Stress Disorder and Alcohol Use Disorder [NCT05692271] | Phase 2 | 48 participants (Anticipated) | Interventional | 2023-07-15 | Recruiting | ||
Influence of Systemic Propranolol Treatment on the Physical Development of Paediatric Patients With Infantile Hemangiomas [NCT04651049] | 128 participants (Actual) | Observational | 2010-07-15 | Completed | |||
A Study to Investigate Continuous Heart Rate Monitoring Using a Chest-worn Biosensor on the Background of Drug-induced Positive and Negative Heart Rate Changes [NCT04682184] | 21 participants (Actual) | Interventional | 2021-01-27 | Completed | |||
Wavelet Transform and Pharmacodynamic Analysis of Atropine and Propranolol Induced Changes in Human Heart Rate Variability [NCT00251602] | Phase 1 | 24 participants (Actual) | Interventional | 2003-03-31 | Completed | ||
A Phase 2, Randomized, Open-Label Study to Assess the Safety and Efficacy of GPC 100 and Propranolol With and Without G-CSF for the Mobilization of Stem Cells in Patients With Multiple Myeloma Undergoing Autologous Stem Cell Transplant [NCT05561751] | Phase 2 | 40 participants (Anticipated) | Interventional | 2023-02-13 | Recruiting | ||
Data Analysis for Drug Repurposing for Effective Alzheimer's Medicines (DREAM)- Propranolol/Carvedilol Versus Atenolol/Bisoprolol/Sotalol [NCT05794997] | 817,337 participants (Actual) | Observational | 2022-11-30 | Active, not recruiting | |||
Propranolol for Syncope With Sympathoadrenal Imbalance in Children [NCT00093860] | Phase 2 | 50 participants | Interventional | 2004-10-31 | Completed | ||
Mechanisms of Choroidal Blood Flow Changes During Dark/Light Transitions [NCT00431392] | Phase 2 | 42 participants | Interventional | 2001-09-30 | Completed | ||
Danish Carvedilol Study in Portal Hypertension. Carvedilol in the Prevention of Bleeding in Portal Hypertension and Esophageal Varices [NCT00493480] | Phase 3 | 40 participants (Anticipated) | Interventional | 2003-09-30 | Completed | ||
Perioperative Administration of COX 2 Inhibitors and Beta Blockers in Women Undergoing Breast Cancer Surgery: an Intervention to Decrease Immune Suppression, Metastatic Potential and Cancer Recurrence [NCT00502684] | 32 participants (Anticipated) | Interventional | 2014-06-30 | Recruiting | |||
Phase 2 Trial of Metronomic Treatment in Children and Adolescents With Recurrent or Progressive Neuroblastoma (NB) [NCT02641314] | Phase 2 | 26 participants (Anticipated) | Interventional | 2016-12-22 | Recruiting | ||
PTSD Symptom Reduction by Propranolol Given After Memory Activation [NCT00645450] | Phase 4 | 9 participants (Actual) | Interventional | 2008-04-30 | Terminated(stopped due to Difficulty recruiting subjects and loss of study physician for new job) | ||
Reduction of Nocturnal Hypertension in Pediatric Renal Transplant Recipients [NCT01007994] | Phase 2/Phase 3 | 33 participants (Actual) | Interventional | 2009-11-30 | Completed | ||
Investigation of Analgesic and Anti-inflammatory Effects of Beta-adrenergic Antagonist Propranolol [NCT01094574] | 10 participants (Actual) | Interventional | 2010-01-31 | Completed | |||
Sympathetic Neurovascular Transduction: Role of Adrenergic Receptors and Sex Differences [NCT05997732] | Phase 4 | 30 participants (Anticipated) | Interventional | 2023-10-31 | Recruiting | ||
[NCT02897986] | Phase 1 | 54 participants (Anticipated) | Interventional | 2017-01-31 | Not yet recruiting | ||
Melablock: A Multicentre Randomized, Double---blinded and Placebo---controlled Clinical Trial on the Efficacy and Safety of Once Daily Propranolol 80 mg Retard for the Prevention of Cutaneous Malignant Melanoma Recurrence [NCT02962947] | Phase 2/Phase 3 | 546 participants (Anticipated) | Interventional | 2017-06-30 | Not yet recruiting | ||
Hemodynamic Effects of Chronic Administration of Spironolactone, Propranolol and Their Association in Alcoholic Cirrhotic Patients [NCT00188045] | Phase 4 | 54 participants | Interventional | 1995-04-30 | Terminated | ||
Effect of LY2216684 on Heart Rate and Blood Pressure in Healthy Subjects Receiving Oral Doses of Albuterol or Propranolol [NCT01263197] | Phase 1 | 48 participants (Actual) | Interventional | 2010-12-31 | Completed | ||
A Randomised, Double Blind, Controlled, Multicentre Study in Infants With Infantile Hemangioma to Compare Propranolol Gel to Placebo. [NCT01512173] | Phase 2 | 82 participants (Actual) | Interventional | 2012-01-31 | Completed | ||
Randomized Controlled Pilot Study Using Propranolol to Decrease Gene Expression of Stress-Mediated Beta-Adrenergic Pathways in Hematopoietic Stem Cell Transplant (HCT) Recipients [NCT02420223] | Phase 2 | 25 participants (Actual) | Interventional | 2015-07-17 | Completed | ||
Propranolol for Diabetic Retinopathy [NCT01535495] | Phase 1 | 9 participants (Actual) | Interventional | 2012-02-29 | Completed | ||
Evaluation of Any Steroid Sparing Effect of Beta Blocker Therapy on Airway Hyper-responsiveness in Stable, Mild to Moderate Asthmatics [NCT01544634] | Phase 2 | 16 participants (Actual) | Interventional | 2012-04-04 | Completed | ||
A Pilot Study of Beta-Blockers in Patients With Advanced Cancer [NCT02013492] | Early Phase 1 | 1 participants (Actual) | Interventional | 2014-01-21 | Completed | ||
A Study to Evaluate the Efficacy of Propranolol in Boosting Immunotherapy in Hepatocellular Carcinoma, Cholangiocarcinoma and Pancreatic Adenocarcinoma [NCT05451043] | Phase 2 | 62 participants (Anticipated) | Interventional | 2023-03-01 | Not yet recruiting | ||
Propranolol For the Treatment of Acute Stress Disorder [NCT00069355] | Phase 2 | 50 participants | Interventional | 2003-09-30 | Completed | ||
Propranolol as an Anxiolytic to Reduce the Use of Sedatives From Critically-ill Adults Receiving Mechanical Ventilation: An Open-label Randomized Controlled Trial (PROACTIVE) [NCT04467086] | Phase 3 | 72 participants (Actual) | Interventional | 2021-01-08 | Completed | ||
Post-traumatic Stress Disorders in Police, Correctional Service Officers, and 911 Operators: A Cost-effectiveness and Efficacy Comparison of Treatment as Usual and a Novel Intervention [NCT03152175] | Phase 2 | 64 participants (Anticipated) | Interventional | 2017-03-30 | Recruiting | ||
Effectivity of Propranolol and Venlafaxine in Treatment of Vestibular Migraine: A Randomized Controlled Clinical Trial [NCT02350985] | Phase 4 | 73 participants (Actual) | Interventional | 2014-01-31 | Completed | ||
Sirolimus in the Treatment for Propranolol-resistant Infantile Hepatic Hemangioendothelioma [NCT04406870] | Phase 4 | 36 participants (Anticipated) | Interventional | 2020-07-31 | Not yet recruiting | ||
A Pilot/Feasibility Study of the Use of High Dose Propranolol to Treat Severe and Chronic Challenging Behaviors in Adolescents and Adults With Autism Spectrum Disorders [NCT04047355] | Phase 2 | 6 participants (Actual) | Interventional | 2021-01-01 | Active, not recruiting | ||
Effect of Beta-blocker Therapy on QTc Response in Exercise and Recovery in Normal Subjects [NCT00588965] | 36 participants (Actual) | Interventional | 2007-08-31 | Completed | |||
Combined Effects of Early Behavioral Intervention and Propranolol on ASD [NCT02428205] | 10 participants (Actual) | Interventional | 2015-04-30 | Completed | |||
A Double-Blind, Randomized, Placebo-Controlled, Single-Dose Crossover Study to Assess the Safety and Tolerability of MK0893 Coadministered With Propranolol Hydrochloride in Patients With Type 2 Diabetes [NCT00902161] | Phase 1 | 22 participants (Actual) | Interventional | 2009-05-31 | Completed | ||
Psychophysiology of Delayed Extinction and Reconsolidation in Humans [NCT01631682] | Phase 4 | 186 participants (Actual) | Interventional | 2010-11-30 | Completed | ||
The Safety and Efficiency of Propranolol as an Initial Treatment for Pediatric Hemangioma [NCT01908972] | Phase 4 | 34 participants (Actual) | Interventional | 2013-06-30 | Completed | ||
Golfer's Cramp: Correlation of Wrist Movements and Surface EMG With Putter Movements [NCT02032758] | Phase 4 | 38 participants (Actual) | Interventional | 2014-01-31 | Completed | ||
A Randomized, Double-Blind, Parallel-Group, Dose-Response Study to Evaluate the Efficacy and Safety of Two Doses of Topiramate Compared to Placebo and Propranolol in the Prophylaxis of Migraine [NCT00236561] | Phase 3 | 786 participants (Actual) | Interventional | 2001-04-30 | Completed | ||
Effect on the Reduction of Bacterial Load in Surgical Antisepsis of Hands After Washing With Triclosan 0.5% Compared to Propan-1-ol 60% Used as Reference Disinfectant [NCT04538365] | Phase 4 | 24 participants (Actual) | Interventional | 2020-10-01 | Completed | ||
Effect of Betablocker or Aldosterone Antagonist Therapy on Oxygenation, Peripheral and Cardiac Hemodynamics and Humoral Systems [NCT00332904] | Phase 4 | 22 participants (Actual) | Interventional | 2006-08-31 | Active, not recruiting | ||
Randomized Study Comparing Ligation With Propranolol for Primary Prophylaxis of Variceal Bleeding in Candidates for Liver Transplantation [NCT00337740] | Phase 3 | 120 participants (Anticipated) | Interventional | Terminated(stopped due to From the interim analysis resulted that more than 1000 patients were required to demonstrate a significant difference between the 2 treatments.) | |||
Assessing the Impact of Dosage Frequency of Propranolol on Sleep Patterns in Patients With Infantile Hemangiomas [NCT05479123] | Phase 4 | 174 participants (Anticipated) | Interventional | 2022-06-23 | Recruiting | ||
Randomized Double-Blind Study to Evaluate the Dose-Related Efficacy and Safety of Caffeine/Propranolol in the Treatment of Acute Migraine [NCT01080677] | Phase 2 | 60 participants (Actual) | Interventional | 2007-01-31 | Completed | ||
Feasibility Study: Therapeutic Targeting of Stress Factors in Ovarian Cancer Patients [NCT01504126] | Early Phase 1 | 32 participants (Actual) | Interventional | 2012-03-09 | Completed | ||
A Multi-center Randomized Controlled Study of Primary Prevention of Esophageal Variceal Bleeding in Cirrhotic Patients Treated With HVPG-guided Beta- Blocker Therapy or Standard Heart Rate-guided Beta-blocker Therapy [NCT01618890] | Phase 3 | 78 participants (Anticipated) | Interventional | 2012-09-30 | Recruiting | ||
Memory Reconsolidation Blockade for Treating Drug Addiction: a Feasibility Study [NCT01634347] | Phase 2 | 17 participants (Actual) | Interventional | 2012-01-31 | Completed | ||
Effect of COMT (Catecholamine-O-methyltransferase) Genetic Polymorphisms on Response to Propranolol Therapy in Temporomandibular Disorder [NCT02437383] | Phase 2 | 200 participants (Actual) | Interventional | 2015-08-20 | Completed | ||
Oral Propranolol, Diltiazem, Metoprolol and Verapamil in Atrial Fibrillation Rate Control in Patients With Stable Hemodynamic Status [NCT01655303] | Phase 4 | 90 participants (Actual) | Interventional | 2011-02-28 | Completed | ||
Sex Disparities in Hypoxic Vasodilation and Impact of Obesity [NCT05219799] | Early Phase 1 | 72 participants (Anticipated) | Interventional | 2023-03-14 | Recruiting | ||
A Randomized Phase II Trial Comparing Bevacizumab Monotherapy With Dacarbazine (DTIC) in Treatment of Malignant Melanoma, Focusing on Angiogenic Markers and Prevention of Hypertension. [NCT01705392] | Phase 2 | 2 participants (Actual) | Interventional | 2013-01-31 | Terminated(stopped due to Lack of financing of the study drug. Not sufficient financial support.) | ||
Treatment of PTSD by Reduction of Traumatic Memory Reconsolidation by Propranolol : a Multisite Trial [NCT01713556] | Phase 2 | 87 participants (Actual) | Interventional | 2012-11-30 | Completed | ||
Efficacy and Safety of Propranolol Versus Acebutolol on the Proliferative Phase of Infantile Hemangioma [NCT01743885] | Phase 3 | 55 participants (Actual) | Interventional | 2012-11-30 | Terminated | ||
The Mechanism of Human Non-Shivering Thermogenesis and Basal Metabolic Rate [NCT01950520] | Phase 2 | 134 participants (Anticipated) | Interventional | 2014-02-07 | Recruiting | ||
Treatment Implications of Beta-blockade Effects on Memory for Cocaine Craving [NCT00830362] | Phase 2 | 50 participants (Actual) | Interventional | 2009-02-28 | Completed | ||
Efficacy of Clonidine and Propranolol Versus Placebo for the Control of Anxiety During Surgical Procedures in Dentistry [NCT01784250] | Phase 2 | 60 participants (Anticipated) | Interventional | 2012-08-31 | Recruiting | ||
DASH After TBI Study: Decreasing Adrenergic or Sympathetic Hyperactivity After Severe Traumatic Brain Injury, A Pilot Randomized Clinical Trial Using Propranolol and Clonidine [NCT01322048] | Phase 2 | 48 participants (Actual) | Interventional | 2011-08-31 | Completed | ||
Beta-blockade Reduces Catabolism in Severely Injured Trauma Patients [NCT00356187] | Phase 2 | 15 participants (Actual) | Interventional | 2006-02-15 | Terminated(stopped due to Slow enrollment, end of funding) | ||
Role of Anabolic Steroid and Propranolol in Paediatric Burn- A Randomized Controlled Trial [NCT05805553] | 114 participants (Anticipated) | Interventional | 2020-12-01 | Recruiting | |||
An Open Label Phase 2 Study on Propranolol and Pembrolizumab in Advanced Angiosarcoma and Undifferentiated Pleomorphic Sarcoma - a Scandinavian Sarcoma Group Collaboration [NCT05961761] | Phase 2 | 80 participants (Anticipated) | Interventional | 2021-08-17 | Recruiting | ||
Beta-Blockers and Inflammatory Responses to Acute Psychosocial Stress [NCT02972554] | Phase 4 | 92 participants (Actual) | Interventional | 2016-01-26 | Completed | ||
Adrenergic Contribution to Glucose Counterregulation in Islet Transplantation [NCT03079921] | Early Phase 1 | 11 participants (Actual) | Interventional | 2017-01-20 | Active, not recruiting | ||
A Phase II, Dose Escalation, Single Center Study on the Effects of Early Propranolol on Heart Rate, Blood Pressure, and Cerebral Perfusion Pressure in Subjects Who Present With Moderate to Severe Traumatic Brain Injury. [NCT01202110] | Phase 2 | 10 participants (Actual) | Interventional | 2010-06-30 | Terminated | ||
Efficacy and Safety of Propranolol for the Post-Stroke Pneumonia [NCT05419193] | Phase 2 | 168 participants (Anticipated) | Interventional | 2023-02-21 | Recruiting | ||
Treatment Implications of Trauma Memory Modulation for PTSD & Alcohol Dependence [NCT01055171] | Phase 2 | 44 participants (Actual) | Interventional | 2010-01-31 | Completed | ||
PROPRANOLOL ASSOCIATED WITH ENDOSCOPIC BAND LIGATION REDUCES RECURRENCE OF ESOPHAGEAL VARICES FOR PRIMARY PROPHYLAXIS OF VARICEAL BLEEDING?: A RANDOMIZED CONTROLLED TRIAL [NCT01893541] | Phase 4 | 100 participants (Actual) | Interventional | 2008-06-30 | Completed | ||
Treat_CCM Clinical Trial A Multicenter Randomized Clinical Trial on Propranolol in Familial Cerebral Cavernous Malformation [NCT03589014] | Phase 2 | 71 participants (Actual) | Interventional | 2018-04-11 | Completed | ||
Safety and Efficacy of Propranolol Treatment in Newborns With Retinopathy of Prematurity:a Prospective Cohort Study [NCT03038295] | Phase 2 | 100 participants (Anticipated) | Interventional | 2017-03-31 | Not yet recruiting | ||
Department of Neonatology, Children's Hospital of Zhengzhou [NCT02977000] | 100 participants (Anticipated) | Interventional | 2016-05-31 | Recruiting | |||
A Study of the Beta-blocker Propranolol Alone and With Chemotherapy in Patients Receiving Neoadjuvant Treatment for Newly Diagnosed Breast Cancer [NCT01847001] | Phase 2 | 10 participants (Actual) | Interventional | 2012-10-31 | Completed | ||
Brief Stresses and DNA Integrity: An Experimental Analysis [NCT03893617] | Phase 1 | 239 participants (Actual) | Interventional | 2017-10-05 | Terminated(stopped due to Due to challenges associated with the Covid-19 pandemic, we were unable to complete recruitment as planned during the period we had funding to do so.) | ||
Functional Imaging of Tremor Circuits and Mechanisms of Treatment Response [NCT02495883] | Phase 4 | 56 participants (Actual) | Interventional | 2013-12-31 | Completed | ||
Shortening Duration of Antiarrhythmic Medication for SVT in Infants [NCT04837261] | 70 participants (Anticipated) | Observational | 2021-04-15 | Recruiting | |||
Using Propranolol in Traumatic Brain Injury to Reduce Sympathetic Storm Phenomenon: A Prospective Randomized Clinical Trial Injury to Reduce Sympathetic Storm Phenomenon: A Prospective Randomized Clinical Trial [NCT03401515] | Phase 4 | 60 participants (Actual) | Interventional | 2016-10-01 | Completed | ||
In Vitro Optimization of Oxytocin-induced Myometrial Contractility by Propranolol - Potential Applications in Induction of Labour and Treatment of Postpartum Hemorrhage [NCT03434444] | 57 participants (Actual) | Interventional | 2017-09-08 | Completed | |||
Sex-related Differences in Sympathetic Vascular Transduction in the Setting of Hypoxemia [NCT05256069] | Early Phase 1 | 35 participants (Anticipated) | Interventional | 2023-04-26 | Recruiting | ||
Adjuvant Treatment of Graves´ Ophthalmopathy With NSAID (aGO Study) [NCT01458600] | Phase 4 | 65 participants (Actual) | Interventional | 2006-09-30 | Completed | ||
[NCT01791114] | 39 participants (Actual) | Interventional | 2012-01-31 | Completed | |||
Oral Propranolol for Prevention of Threshold Retinopathy of Prematurity [NCT03083431] | Phase 2 | 276 participants (Anticipated) | Interventional | 2022-09-22 | Recruiting | ||
A Phase 1, Open-label, Fixed-sequence, Cross-over Trial to Assess the Effects of a Single Dose of Prazosin or Propranolol in the Presence of Brexpiprazole/Sertraline at Steady-state on Blood Pressure [NCT05189977] | Phase 1 | 24 participants (Anticipated) | Interventional | 2022-08-22 | Recruiting | ||
Analgesic Effects of Perioperative Propranolol Administration for Spine Surgery [NCT04421209] | Phase 2 | 0 participants (Actual) | Interventional | 2020-12-31 | Withdrawn(stopped due to No funding source) | ||
Propranolol for Prolonged Labor: A Randomized Controlled Trial (PRO-Labor Trial) [NCT04741698] | Phase 1 | 80 participants (Actual) | Interventional | 2021-07-27 | Completed | ||
A Phase II, Randomized, Double-Blind Comparison of Corticosteroid and Corticosteroids With Propranolol Treatment of Infantile Hemangiomas (IH) [NCT01074437] | Phase 2 | 9 participants (Actual) | Interventional | 2010-02-28 | Terminated(stopped due to Insufficient enrollment) | ||
Beta-Adrenergic Modulation of Drug Cue Reactivity: Neural and Behavioral Mechanisms [NCT05587361] | Phase 4 | 80 participants (Anticipated) | Interventional | 2024-01-15 | Not yet recruiting | ||
Propranolol for Treating Fibromyalgia Pain: Pilot Study [NCT03029845] | Phase 1 | 15 participants (Actual) | Interventional | 2017-01-31 | Terminated(stopped due to The funding ended.) | ||
Propranolol and Misoprostol Versus Misoprostol Alone for Induction of Labor In Primigravidas [NCT04533841] | Phase 2 | 128 participants (Actual) | Interventional | 2020-02-01 | Completed | ||
Propranolol Versus Placebo for Induction of Labor in Nulliparous Patients: a Double-blind Randomized Controlled Trial [NCT03348683] | Phase 2 | 240 participants (Actual) | Interventional | 2017-12-11 | Completed | ||
Perioperative Propranolol in Robotic Assisted Laparoscopic Prostatectomy- A Feasibility Study of Propranolol to Target Perioperative Stress Induced Cancer Progression [NCT05679193] | Phase 2 | 40 participants (Anticipated) | Interventional | 2023-01-02 | Recruiting | ||
A Randomized Crossover Study of Propranolol Versus Ivabradine in Postural Tachycardia Syndrome (POTS) [NCT04186286] | Phase 2 | 20 participants (Anticipated) | Interventional | 2021-02-01 | Recruiting | ||
"Pilot Window of Opportunity Neoadjuvant Study of Propranolol in Breast Cancer" [NCT02596867] | Phase 2 | 2 participants (Actual) | Interventional | 2015-09-01 | Terminated(stopped due to poor accrual) | ||
Propranolol Adjuvant Treatment of Bladder Cancer: a Randomized Phase II Clinical Trial [NCT04493489] | Phase 2 | 242 participants (Anticipated) | Interventional | 2020-09-06 | Not yet recruiting | ||
Mechanisms of Fenofibrate and Propranolol Alone or Combined in Burn Patients [NCT02452255] | Phase 2/Phase 3 | 18 participants (Actual) | Interventional | 2015-11-30 | Terminated(stopped due to Shriner's Burn Hospital closed the study and access to study-related data is unavailable. We are unable to submit the additional information or results-data) | ||
Comparing Standard vs. Modified Reconsolidation Blockade for the Treatment of Psychological Trauma: A Randomized Controlled Trial [NCT04982211] | Phase 2 | 150 participants (Anticipated) | Interventional | 2021-08-01 | Not yet recruiting | ||
Nadolol Versus Propranolol in Children With Infantile Hemangiomas: a Randomized, Controlled, Double-blinded Trial [NCT02505971] | Phase 3 | 74 participants (Actual) | Interventional | 2015-09-30 | Completed | ||
The Efficacy and Safety of Beta-blockers Drugs in Adults With Spinal Hemangioma: a Prospective Cohort Study [NCT05106179] | Phase 4 | 1,000 participants (Anticipated) | Interventional | 2021-12-31 | Enrolling by invitation | ||
Propranolol for Treatment of Cocaine Addiction [NCT00000197] | Phase 2 | 0 participants | Interventional | 1987-01-31 | Completed | ||
Efficacy of Propanolol for Treatment of Posttraumatic Stress Disorder [NCT00648375] | Phase 4 | 12 participants (Actual) | Interventional | 2003-12-31 | Terminated(stopped due to inadequate recruitment) | ||
Reducing Total Cardiovascular Risk in an Urban Community [NCT00241904] | Phase 4 | 525 participants (Actual) | Interventional | 2006-05-31 | Completed | ||
Effect of Beta Blockade on Opioid-Induced Hyperalgesia in Humans [NCT01222091] | Phase 2 | 10 participants (Actual) | Interventional | 2009-02-28 | Completed | ||
Brief Intervention to Reduce Fear of Public Speaking [NCT02790736] | Phase 4 | 6 participants (Actual) | Interventional | 2016-06-30 | Terminated(stopped due to COVID-19 restrictions) | ||
Propranolol for Sleep Apnea Therapy [NCT03049306] | Phase 2 | 36 participants (Anticipated) | Interventional | 2017-02-15 | Enrolling by invitation | ||
A Phase II Study of Propranolol for the Treatment of Kaposi Sarcoma in Children and Adults [NCT05797662] | Phase 2 | 25 participants (Anticipated) | Interventional | 2024-07-01 | Not yet recruiting | ||
Brief Intervention for OCD Fears [NCT02790710] | Phase 4 | 0 participants (Actual) | Interventional | 2016-06-30 | Withdrawn(stopped due to Study has been withdrawn due to reconsideration of study design.) | ||
A Phase I Study to Evaluate the Safety of Naltrexone and Propranolol in Combination With Standard of Care Ipilimumab and Nivolumab in Patients With Advanced Melanoma [NCT05968690] | Phase 1 | 12 participants (Anticipated) | Interventional | 2023-09-11 | Recruiting | ||
Proton Pump Inhibitor Plus Propranolol Versus Proton Pump Inhibitor Alone on Peptic Ulcer Healing in Patients With Liver Cirrhosis: a Randomized Trail [NCT04140591] | Phase 2/Phase 3 | 10 participants (Actual) | Interventional | 2016-12-26 | Terminated(stopped due to 1. Most patients with liver cirrhosis already use PPI and NSBB 2. 90 % Peptic ulcer size is smaller than 5cm) | ||
Modafinil and Cognitive Function in Postural Tachycardia Syndrome [NCT01988883] | Early Phase 1 | 20 participants (Actual) | Interventional | 2014-10-31 | Active, not recruiting | ||
A Phase Ib/II Study of Propranolol With Fixed-Dose Pembrolizumab in Patients With Unresectable Stage III and Stage IV Melanoma [NCT03384836] | Phase 1/Phase 2 | 47 participants (Anticipated) | Interventional | 2018-01-31 | Recruiting | ||
Post-balloon Occluded Retrograde Transvenous Obliteration Use of Propranolol for the Prevention of Worsening of Esophageal Varices in Patients With Isolated Gastric Varices [NCT03171805] | 74 participants (Anticipated) | Interventional | 2017-06-01 | Recruiting | |||
Effect of a Beta Adrenergic Blockade Combined With Relaxation/Guided Imagery Audio Intervention on Symptom Distress in Women With Advanced, Recurrent Incurable Cervical Cancer - Feasibility Study [NCT01902966] | 6 participants (Actual) | Interventional | 2013-09-11 | Terminated(stopped due to low accrual and lack of funding) | |||
Role of Combined Therapy of Propranolol and Gabapentin in Paroxysmal Sympathetic Hyperactivity in Traumatic Brain Injury at Emergency Intensive Care Unit [NCT05427474] | Phase 3 | 90 participants (Anticipated) | Interventional | 2022-12-01 | Recruiting | ||
Oral Propranolol Versus Placebo for Early Stages of Retinopathy of Prematurity (ROP): A Pilot, Randomized and Prospective Study. [NCT01238471] | Phase 1/Phase 2 | 20 participants (Actual) | Interventional | 2010-05-31 | Completed | ||
The Use of Propranolol Hydrochloride Combined With Anthracyclin Based Chemotherapy in the Treatment of Metastatic Soft Tissue Sarcoma [NCT03108300] | Phase 2 | 50 participants (Anticipated) | Interventional | 2019-08-30 | Not yet recruiting | ||
Trial of Propranolol in Older Adults With Primary Progressive Aphasia [NCT06066710] | Early Phase 1 | 20 participants (Anticipated) | Interventional | 2024-01-31 | Recruiting | ||
Genetic Variants Associated With the Occurrence of Localized Low Back Pain or Low Back Pain With Widespread Pain Symptoms, and Their Response to Treatment With Duloxetine or Propranolol [NCT03364075] | Phase 2 | 10 participants (Actual) | Interventional | 2017-09-01 | Terminated(stopped due to Recruitment issue) | ||
Effects on the Airway Lumen of Single Oral Doses of Talsaclidine (12, 24, 48 and 60 mg) in Combination With a Single Oral Doses of 160 mg Propranolol in Comparison to the Effects of the Monosubstances (60 mg Talsaclidine and 160 mg Propranolol) in Healthy [NCT02264093] | Phase 1 | 12 participants (Actual) | Interventional | 1999-11-30 | Completed | ||
Surgical Hand Antisepsis With Propan-ol-1 60% Per Rubbing and Scrubbing in Accordance With European Norm Regulation 12791 [NCT04446923] | Phase 4 | 24 participants (Actual) | Interventional | 2020-06-28 | Completed | ||
Evaluating of Oral Propranolol Effect on Managing Anxiety of Dental Extractions in Children: A Randomized Controlled Clinical Trial [NCT03388957] | 60 participants (Actual) | Interventional | 2018-07-30 | Completed | |||
Thermogenesis in Hyperthyroidism and Effect of Anti-Adrenergic Therapy [NCT03379181] | Phase 4 | 19 participants (Actual) | Interventional | 2017-07-18 | Completed | ||
A Psychophysiologic Study of Weakening Traumatic Combat Memories With Post-Reactivation Propranolol [NCT00709735] | Phase 4 | 23 participants (Actual) | Interventional | 2007-05-31 | Completed | ||
Enhancing Disrupted Reconsolidation: Impact on Cocaine Craving, Reactivity and Use [NCT01822587] | Phase 2 | 181 participants (Actual) | Interventional | 2013-09-30 | Completed | ||
Propranolol and Botulinum Toxin for Essential Vocal Tremor [NCT02111369] | Phase 4 | 18 participants (Actual) | Interventional | 2014-05-31 | Completed | ||
Propanolol for Primary Prophylaxis for Variceal Bleed in Biliary Atresia - An Open Label Randomized Controlled Study [NCT04494763] | 92 participants (Anticipated) | Interventional | 2020-08-15 | Recruiting | |||
Comparative Study to Evaluate the Effectiveness of Atenolol and Propranolol in the Treatment of Infantile Hemangiomas [NCT03237637] | Phase 3 | 60 participants (Anticipated) | Interventional | 2017-03-24 | Recruiting | ||
Effects of Propranolol (vs. Placebo) on Information Processing During Presentation of Emotionally Arousing Pictures After Single Dose (80 mg) Administration and Relationships Between ß1- and ß2-adrenoreceptors Genotype and Both the Information Processing [NCT02509559] | Phase 1 | 8 participants (Actual) | Interventional | 2013-10-31 | Completed | ||
Randomized Controlled Trial on the Effectiveness and Safety of Carvedilol vs. Propranolol Combined With Endoscopic Treatment in Second Prophylaxis of Variceal Bleeding in Cirrhosis [NCT05651789] | 160 participants (Anticipated) | Interventional | 2023-01-31 | Not yet recruiting | |||
[information is prepared from clinicaltrials.gov, extracted Sep-2024] |