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oxprenolol

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Description

Oxprenolol is a beta blocker that was first synthesized in the 1960s. It is a racemic mixture of two enantiomers, with the S-enantiomer being the more potent. Oxprenolol is used to treat a variety of cardiovascular conditions, including hypertension, angina pectoris, and arrhythmias. It works by blocking the effects of adrenaline and noradrenaline on the heart and blood vessels. Oxprenolol is also being studied for its potential to treat other conditions, such as migraine headaches and essential tremor. It is generally well-tolerated, but can cause side effects such as fatigue, dizziness, and bradycardia. Oxprenolol is typically taken orally. It is metabolized by the liver and excreted in the urine. Oxprenolol has been a subject of significant research due to its versatility and potential benefits for various health conditions. Its effects on the cardiovascular system, specifically its ability to decrease heart rate and blood pressure, make it a valuable tool in managing hypertension and related disorders. Ongoing studies explore its effectiveness in treating other ailments, further solidifying its importance in medical research. '

Oxprenolol: A beta-adrenergic antagonist used in the treatment of hypertension, angina pectoris, arrhythmias, and anxiety. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID4631
CHEMBL ID546
CHEBI ID91704
SCHEMBL ID16310
MeSH IDM0015659

Synonyms (77)

Synonym
BRD-A43671941-003-03-6
2-propanol, 1-[(1-methylethyl)amino]-3-[2-(2-propenyloxy)phenoxy]-
2-propanol, 1-(2-allyloxyphenoxy)-3-(isopropylamino)-
oxprenolol, dl-
1-(isopropylamino)-2-hydroxy-3-(o-(allyloxy)phenoxy)propane
osprenololo [dcit]
(1)-1-(o-(allyloxy)phenoxy)-3-(isopropylamino)propan-2-ol
oxprenololum [inn-latin]
1-((1-methylethyl)amino)-3-(2-(2-propenyloxy)phenoxy)-2-propanol
einecs 245-359-6
einecs 229-257-9
2-propanol, 1-((1-methylethyl)amino)-3-(2-(2-propenyloxy)phenoxy)-
ccris 4201
coretal
oxprenolol [inn:ban]
(+-)-oxprenolol
1-(o-(allyloxy)phenoxy)-3-(isopropylamino)-2-propanol
BSPBIO_001014
PRESTWICK2_001057
PRESTWICK3_001057
2-propanol, 1-[(1-methylethyl)amino]-3-[2-(2-propenyloxy)phenoxy]-, (+/-)
1-(2-allyloxyphenoxy)-3-(isopropylamino)propan-2-ol
trasicor (*hydrochloride*)
6452-71-7
1-[(1-methylethyl)amino]-3-[2-(2-propenyloxy)phenoxy]-2-propanol
coretal (*hydrochloride*)
trasicor 80
dl-oxprenolol
laracor (*hydrochloride*)
slow-pren (*hydrochloride*)
trasacor (*hydrochloride*)
oxprenolol ba 39089 (*hydrochloride*)
AB00514712
oxprenolol
DB01580
BPBIO1_001116
PRESTWICK1_001057
SPBIO_002937
PRESTWICK0_001057
L013416
bdbm50240370
1-(2-allyloxy-phenoxy)-3-isopropylamino-propan-2-ol (oxprenolol)
1-(2-allyloxy-phenoxy)-3-isopropylamino-propan-2-ol
1-(2-allyloxy-phenoxy)-3-isopropylamino-propan-2-ol(oxprenolol)
1-(2-(allyloxy)phenoxy)-3-(isopropylamino)propan-2-ol
CHEMBL546 ,
oxprenolol (inn)
D08318
oxprenolol (tn)
1-(propan-2-ylamino)-3-(2-prop-2-enoxyphenoxy)propan-2-ol
osprenololo
oxprenololum
519mxn9yzr ,
unii-519mxn9yzr
1-[2-(allyloxy)phenoxy]-3-(isopropylamino)-2-propanol
trasacor
{2-hydroxy-3-[2-(prop-2-en-1-yloxy)phenoxy]propyl}(propan-2-yl)amine
gtpl7255
oxprenolol [mi]
2-propanol, 1-(o-allyloxyphenoxy)-3-isopropylamino-
oxprenolol [who-dd]
oxprenolol [inn]
SCHEMBL16310
1-(2-allyloxyphenoxy)-3-(iso-propylamino)-2-propanol
DTXSID1043835
1-[2-(allyloxy)phenoxy]-3-(isopropylamino)-2-propanol #
(+/-)-oxprenolol
AB00514712_07
1-(propan-2-ylamino)-3-(2-prop-2-enoxyphenoxy)-2-propanol
CHEBI:91704
Q425963
1-(isopropylamino)-2-hydroxy-3-[o-(allyloxy)phenoxy]propane
()-oxprenolol
1-[2-(prop-2-en-1-yloxy)phenoxy]-3-[(propan-2-yl)amino]propan-2-ol
EN300-18552821
HY-B1486A
CS-0013720

Research Excerpts

Overview

Oxprenolol is a potent noncardioselective beta-adrenoceptor blocking drug with partial agonist activity of proved efficacy and high tolerability in patients at risk of various cardiovascular disease syndromes. Oxprenlol is an experimental beta adrenergic blocker with intrinsic sympathomimetic activity.

ExcerptReferenceRelevance
"Oxprenolol (OX) is a nonselective, beta-adrenergic blocking agent with intrinsic sympathomimetic activity. "( Slow-release oxprenolol compared with oxprenolol in hypertensive patients: a multicenter clinical trial.
Friedman, BA; Glazer, N; Gray, JM; Gross, S; Hla, KM; Materson, BJ; Neidorf, BS, 1983
)
2.08
"Oxprenolol is a nonselective beta-adrenergic blocking agent that also possesses intrinsic sympathomimetic activity (ISA) and membrane stabilizing effects. "( Oxprenolol hydrochloride: pharmacology, pharmacokinetics, adverse effects and clinical efficacy.
Covinsky, JO; Russo, ME,
)
3.02
"Oxprenolol is a potent noncardioselective beta-adrenoceptor blocking drug with partial agonist activity of proved efficacy and high tolerability in patients at risk of various cardiovascular disease syndromes. "( Oxprenolol in clinical practice.
Taylor, SH, 1983
)
3.15
"Oxprenolol is an experimental beta adrenergic blocker with intrinsic sympathomimetic activity. "( Antihypertensive and hemodynamic effects of oxprenolol versus propranolol.
Aronow, WS; Easthope, JL; Ferlinz, J; Hughes, D; Siegel, J; Tobis, J, 1980
)
1.97
"Oxprenolol is a non-selective adrenergic beta-receptor antagonist displaying beta-mimetic activity. "( Oxprenolol and the circulation during anaesthesia in the dog: influence of intrinsic sympathomimetic activity.
Bennett, MJ; Foëx, P; Roberts, JG; Saner, CA, 1981
)
3.15
"Oxprenolol is a beta-adrenergic blocker with intrinsic sympathomimetic activity. "( Hemodynamic effects of oxprenolol and propranolol in hypertension.
Franciosa, JA; Johnson, SM; Tobian, LJ, 1979
)
2.01
"Oxprenolol is a new beta-adrenergic blocking drug, whose effectiveness in the treatment of various forms of glaucoma has been evaluated. "( [Topical oxpernolol in the treatment of various forms of glaucoma (author's transl)].
Bietti, GB; Bucci, MG; Pescosolido, N, 1977
)
1.7
"Oxprenolol is a non-selective beta-blocker with moderate intrinsic sympathomimetic activity (ISA), given by the Oros delivery system."( An interactive computer program for randomization analysis of response curves with facilities for multiple comparisons.
Does, RJ; Roos, JM; Tan, ES; Van Baak, MA; Volovics, A, 1992
)
1

Effects

Oxprenolol has less negative inotropic and chronotropic effects than propranolol. It has substantial benefit in the alleviation of many of the somatic sequelae of psychic stress and anxiety.

ExcerptReferenceRelevance
"Oxprenolol has less negative inotropic and chronotropic effects than propranolol."( Oxprenolol hydrochloride: pharmacology, pharmacokinetics, adverse effects and clinical efficacy.
Covinsky, JO; Russo, ME,
)
2.3
"Oxprenolol has substantial benefit in the alleviation of many of the somatic sequelae of psychic stress and anxiety."( Oxprenolol in clinical practice.
Taylor, SH, 1983
)
2.43

Actions

ExcerptReferenceRelevance
"Oxprenolol may increase the hypotensive effect of chlorthalidone by counteracting the hypokalemic effect of the diuretic and by attenuating the diuretic-induced increase in plasma renin activity."( Effects of chlorthalidone, oxprenolol, and their combination in hypertensive blacks: a randomized double-blind crossover study.
Obel, AO, 1989
)
1.3

Treatment

Treatment with oxprenolol (0.5 mg.kg-1 iv) preserved both basic heart activity and cardiac heat emission at levels which were comparable to the control state. Oxprenlol treatment did not modify the blood pressure levels in the renal hypertensive rats nor in the spontaneously hypertensive turkeys.

ExcerptReferenceRelevance
"Oxprenolol treatment did not modify the blood pressure levels in the renal hypertensive rats nor in the spontaneously hypertensive turkeys."( Cardioprotection by beta-blockers: molecular and structural aspects in experimental hypertension.
Dal Palù, C; Pauletto, P; Pessina, AC; Scannapieco, G; Vescovo, G, 1990
)
1
"Oxprenolol-treated patients had a significantly lower daytime heart rate as compared with the placebo group, whereas no difference was found at night."( Effect of oxprenolol on ventricular arrhythmias: the European Infarction Study experience.
Andresen, D; Bethge, KP; Boissel, JP; Peyrieux, JC; Schröder, R; Tietze, U; von Leitner, ER, 1985
)
1.39
"Oxprenolol treatment continuously applied from the 4th day postburn (2 X 0.5 mg/kg) prevented the development of myocardial damage, while the electron dense complexes containing Ni were still detectable."( The effect of alpha and beta adrenergic blockade on Ni induced coronary spasm in scalded rats.
Balogh, I; Faragó, M; Gergely, A; Kovách, AG; Rubányi, G; Szabó, K, 1986
)
0.99
"3. Treatment with oxprenolol (taken during the day) reduces daytime blood pressure but is less effective during the night and early morning."( Blood pressure circadian rhythm in essential hypertension.
Balasubramanian, V; Mann, S; Millar Craig, MW; Raftery, EB, 1978
)
0.58
"Pretreatment with oxprenolol (0.5 mg.kg-1 iv) preserved both basic heart activity and cardiac heat emission at levels which were comparable to the control state, but prevented DA mediated excitation of cardiac and coronary beta-adrenoceptors."( The dopamine-induced coronary vasoconstrictor response is potentiated by adenosine administration in the dog heart.
Juhász-Nagy, A; Kékesi, V; Kollár, A, 1989
)
0.6

Toxicity

ExcerptReferenceRelevance
" Oxprenolol produced no serious adverse effects."( Oxprenolol hydrochloride: a long-term study of efficacy, safety, and tolerability.
Tarpley, EL,
)
2.48

Pharmacokinetics

Higher AUC and Cmax values were obtained for metoprolol, oxprenolol and propranolol in groups receiving the low-dose oestrogen-ethinyl oestradiol oral contraceptive. The 16/260 Oros system gave smoother pharmacokinetic and pharmacodynamic profiles.

ExcerptReferenceRelevance
" Using the fitted pharmacokinetic curve, the drug effect was related to its plasma concentration using the Emax model."( Pharmacokinetic-pharmacodynamic modelling of oxprenolol in man using continuous non-invasive blood pressure monitoring.
Karemaker, JM; Koopmans, R; Oosterhuis, B; van Boxtel, CJ; Wemer, J, 1988
)
0.53
" The absolute bioavailabilities for prototype and clinical trial systems were shown to be similar, at approximately 42%, and no significant differences in plasma profiles or pharmacokinetic constants were detected between the two Oros forms."( Pharmacokinetic investigation of the absorption of oxprenolol from Oros delivery systems in healthy volunteers: comparison of in vivo and in vitro drug release.
Bradbrook, ID; John, VA; Morrison, PJ; Rogers, HJ; Spector, RG, 1985
)
0.52
" The 16/260 Oros system gave smoother pharmacokinetic and pharmacodynamic profiles, and on repeated dosing a higher mean pre-dose plasma oxprenolol concentration than Slow Trasicor."( A multiple dose comparative study of the pharmacodynamic and pharmacokinetic behaviour of polymer-matrix and Oros dosage forms of oxprenolol in healthy volunteers.
Halsey, A; Jack, DB; John, VA; Kendall, MJ; O'Donnell, ML; Warrington, SJ; Woods, KL, 1985
)
0.68
"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
)
0.72
"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
)
0.51
" 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
)
0.29

Compound-Compound Interactions

Study was a comparison of the effects on respiratory function produced by four antihypertensive agents. Oxprenolol was administered in combination with clortalidone in group B and with phentolamine in group C.

ExcerptReferenceRelevance
"The study was a comparison of the effects on respiratory function produced by four antihypertensive agents with receptor-blocking properties (atenolol, oxprenolol, labetalol, metoprolol), when used in combination with a diuretic (chlorthalidone) in four homogeneous groups of hypertensive patients also suffering from chronic obstructive lung disease."( Respiratory effects of four adrenergic blocking agents combined with a diuretic in treating hypertension with concurrent chronic obstructive lung disease.
Dal Negro, RW; Pomari, C; Trevisan, F; Turco, P; Zoccatelli, O, 1986
)
0.47

Bioavailability

Oxprenolol was well absorbed from the rectum while the system was present in this segment of the gut.

ExcerptReferenceRelevance
"The relative bioavailability of a test sustained-release (SR) oxprenolol tablet against an approved regular-release (RR) tablet has been investigated at steady-state."( Relative bioavailability of oral sustained-release and regular-release oxprenolol tablets at steady-state.
Gupta, PK; Hung, CT; Lam, FC; Lim, JK; Zoest, AR, 1991
)
0.75
" Oxprenolol was well absorbed from the rectum while the system was present in this segment of the gut."( The pharmacokinetics of oxprenolol following oral and rectal dosing--a comparison of delivery systems and routes of administration.
Gregg, MR; Jack, DB; Kendall, MJ; Smith, SR, 1987
)
1.49
" The intestinal absorption rate was markedly increased in the presence of nutrients (mean amount absorbed 96% for C)."( Jejunal and ileal absorption of oxprenolol in man: influence of nutrients and digestive secretions on jejunal absorption and systemic availability.
Bernier, JJ; Bovet, M; Franchisseur, C; Godbillon, J; Gosset, G; Hirtz, J; Palma, R; Pfeiffer, A; Vidon, N, 1987
)
0.56
" Initially, the in vivo absorption rate was similar to the in vitro release rate but after 5-6 h it slowed perceptibly."( Pharmacokinetic investigation of the absorption of oxprenolol from Oros delivery systems in healthy volunteers: comparison of in vivo and in vitro drug release.
Bradbrook, ID; John, VA; Morrison, PJ; Rogers, HJ; Spector, RG, 1985
)
0.52
" The technique was applied in a study of the bioavailability of metoprolol after oral administration to man; mean plasma concentrations are reported."( Gas chromatographic determination of metoprolol in human plasma.
Leroux, F; Sandrenan, N; Sioufi, A, 1983
)
0.27
" Methods to increase ocular bioavailability include (a) the development of drug delivery devices designed to release drugs at controlled rates, (b) the use of various vehicles that retard precorneal drug loss, and (c) the conversion of drugs to biologically reversible derivatives (prodrugs) with increased corneal penetration properties, from which the active drugs are released by enzymatic hydrolysis."( A study of the relationship between the structure and physicochemical parameters of a homologous series of oxprenolol esters at various pH values and temperatures.
Jordan, CG, 1997
)
0.51
" Therefore, some methods have been employed to increase ocular bioavailability such as (a) the development of drug delivery devices designed to release drugs at controlled rates, (b) the use of various vehicles that retard precorneal drug loss, and (c) the conversion of drugs to biologically reversible derivatives (prodrugs) with increased corneal penetration properties, from which the active drugs are released by enzymatic hydrolysis."( How an increase in the carbon chain length of the ester moiety affects the stability of a homologous series of oxprenolol esters in the presence of biological enzymes.
Jordan, CG, 1998
)
0.51
" Pharmacokinetic parameters which describe bioavailability and general kinetic behavior of the drug were calculated from individual serum profiles."( Relative bioavailability of different oral sustained release oxprenolol tablets.
Capalneanu, R; Follidis, M; Leucuta, SE; Mocan, A,
)
0.37
"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 new methodology may, therefore, be used for fast bioavailability screening of virtual libraries having millions of molecules."( Fast calculation of molecular polar surface area as a sum of fragment-based contributions and its application to the prediction of drug transport properties.
Ertl, P; Rohde, B; Selzer, P, 2000
)
0.31
" This was also suggested by the bioavailability of the model drug after intragastric and intranasal administration of the microspheres."( Oxprenolol-loaded bioadhesive microspheres: preparation and in vitro/in vivo characterization.
Leucuta, SE; Preda, M,
)
1.57
" 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

Dosage Studied

The results of this study support the concept of extending the duration of oxprenolol release from a rate-controlled dosage form to permit once-daily administration with this short elimination half-life drug. Repeated dosing significantly reduced supine systolic and diastolic blood pressures, and pulse rate at 24 h after dosing.

ExcerptRelevanceReference
" 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
)
0.26
" 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
" In 14 patients who showed no response whatever, further treatment, with bromocriptine in doses raised gradually to a final daily dosage of 15 mg, was effective in four cases, though the improvement was generally only moderate."( Therapy of extrapyramidal side effects, with particular reference to persistent dyskinesia and lithium tremor.
Pöldinger, W, 1978
)
0.26
" 4) In the management of essential moderate or severe hypertension is preferable to employ a mild dosage of betablockers and diuretics, rather than use higher doses of a single agent."( [The role of renin after betablocking diuretic and vasodilator treatment in essential hypertension (author's transl)].
Fusco, M; Lombardo, M; Valente, D, 1979
)
0.26
" Half the patients responded will to low dosage (oxprenolol less than or equal to 320 mg, methyldopa less than or equal to 1 g, a day) and 9 of 11 such patients responded satisfactorily to each drug."( Comparison of oxprenolol and methyldopa in hypertension. A within-patient double-blind trial.
Barritt, DW; Heaton, S; Marshall, AJ, 1976
)
0.87
" As 77 percent of the patients considered the once daily dose in a calendar pack to be helpful, simplification of dosage was thought to be an important factor in improving patient compliance, which resulted in better blood pressure control without an increase in unwanted effects."( Once daily administration of a beta-blocker in hypertension.
Duncan, TD; Watt, M, 1978
)
0.26
" The dosage was 80 mg three times a day."( Oxprenolol in the treatment of migraine.
Ekbom, K; Zetterman, M, 1977
)
1.7
" Blood pressure readings 24 h post-dose were lower following morning dosing than following evening dosing, although pulse rates showed the opposite trend."( A comparison of slow release oxprenolol with conventional oxprenolol in the treatment of hypertension.
Havard, CW; Resnekov, EB, 1978
)
0.55
"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
)
0.69
" 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
)
0.57
" However, patient compliance might be considerably improved with the once-daily dosage schedule of the fixed combination."( Antihypertensive effect of oxprenolol and chlorthalidone in fixed combination, given once daily.
Buoninconti, R; Motolese, M; Rubegni, M, 1979
)
0.56
" 3 Slow-release oxprenolol is, under the conditions of this study, a reliable and convenient dosage form, providing similar plasma-drug profiles in fasted and nonfasted individuals."( Bioavailability of conventional and slow-release oxprenolol in fasted and nonfasted individuals.
Dawes, CP; Kendall, MJ; Welling, PG, 1979
)
0.86
" 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
)
0.26
" Preference for once daily therapy, enthusiasm for the calendar pack, and a net increase in the mean daily dosage of a beta-receptor antagonist were the probable factors contributing to the improvement recorded."( A multicentre evaluation of sustained release oxprenolol in the management of hypertension in hospital out-patient practice.
Forrest, WA, 1978
)
0.52
" The maximum plasma levels and the area beneath the plasma concentration curves increased roughly in proportion to the dosage increment."( Relation between plasma concentrations and cardiovascular effects of oral oxprenolol in man.
Brunner, L; Imhof, P; Jack, D, 1975
)
0.49
"Patients with moderate to severe hypertension were studied during a 12-week period, during which they were given a slow release formulation of oxprenolol once daily, in a dosage equal to their previous total daily dose of oxprenolol given in divided doses."( Comparison of a slow release formulation of oxprenolol with conventional oxprenolol in the treatment of hypertension.
O'Brien, KP; Stephens, EJ, 1976
)
0.72
" Once-daily dosage offers advantages of patient compliance."( Comparison of a slow-release formulation of oxprenolol with conventional oxprenolol in the treatment of hypertension.
O'Brien, KP; Stephens, EJ, 1976
)
0.52
" The drugs could be given in a twice-daily dosage and had a much higher degree of patient acceptance."( Oxprenolol and hydrallazine in the treatment of hypertension.
Freeman, JW; Knight, LW, 1975
)
1.7
" From the third week of treatment onwards, the Esidrix dosage was maintained; the dosage of Trasicor 80 was either maintained, increased, or later decreased, according to the results obtained."( [Ambulatory treatment of arterial hypertension urinary the new combination "saluretic and beta-sympatholytic"].
Dannhorn, R; Müller, AA, 1975
)
0.25
" Possible increases in the dosage of trasicor in the pediatric practice are deemed permissible."( [Characteristics of the reaction of the renal tissue adenylic system to the beta-adrenoblockader, trasicor (oxprenolol), in early postnatal ontogeny].
Chekman, IS; Chernomorets, SG; Viktorov, AP,
)
0.34
" The results obtained are reproducible and hence the method is suitable for the determination of oxprenolol hydrochloride in pharmaceutical dosage forms."( Spectrophotometric determination of oxprenolol hydrochloride as its Fe (III) complex.
Agatonović-Kustrin, S; Pećanac, D; Radulović, D; Zivanović, L, 1990
)
0.77
" This was most apparent in standing systolic and diastolic and post-exercise systolic blood pressures between 1 and 2 h after dosing and was dose-related."( A comparison of single doses of bucindolol and oxprenolol in hypertensive patients.
Jamieson, M; Petrie, JC; Robb, OJ; Verschueren, J; Webster, J, 1985
)
0.53
" Individual plasma values were simulated using a lest squares procedure and the results were applied to evaluate individual release patterns following dosage with the sustained release preparation."( The pharmacokinetics and dynamics of oxprenolol: a simulation study with six subjects.
Ingram, D; Saunders, L; Warrington, SJ, 1985
)
0.54
" 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
" These observations suggest that both oxprenolol OROS systems display sustained drug release and on once daily dosing provide 24 h beta-blockade and control of blood pressure at rest and following exercise."( Evaluation of two oxprenolol oral osmotic (OROS) delivery systems in patients with essential hypertension.
Brodie, MJ; McInnes, GT, 1988
)
0.88
" As judged from the relative areas under the plasma concentration-time curve, however, the availability of the drug from the two dosage forms was comparable."( The pharmacokinetics of oxprenolol following oral and rectal dosing--a comparison of delivery systems and routes of administration.
Gregg, MR; Jack, DB; Kendall, MJ; Smith, SR, 1987
)
0.58
" The results of this study support the concept of extending the duration of oxprenolol release from a rate-controlled dosage form to permit once-daily administration with this short elimination half-life drug."( Oxprenolol absorption in man after single bolus dosing into two segments of the colon compared with that after oral dosing.
Antonin, KH; Bieck, P; Jedrychowski, M; Malchow, H; Scheurlen, M, 1985
)
1.94
" In the analysis of the first study, the plasma profile following intravenous dosing was used as the reference function, allowing the combined release/absorption process to be calculated; for the second, an oral bolus was used, the result of the deconvolution therefore indicating the in vivo dissolution rate of the Oros systems."( In vitro and in vivo deconvolution assessment of drug release kinetics from oxprenolol Oros preparations.
Langenbucher, F; Mysicka, J, 1985
)
0.5
"The absorption kinetics of oxprenolol have been investigated in eight healthy volunteers after single dosing with 16/260 Oros drug delivery systems."( Pharmacokinetic investigation of the absorption of oxprenolol from Oros delivery systems in healthy volunteers: comparison of in vivo and in vitro drug release.
Bradbrook, ID; John, VA; Morrison, PJ; Rogers, HJ; Spector, RG, 1985
)
0.82
" The 16/260 Oros system gave smoother pharmacokinetic and pharmacodynamic profiles, and on repeated dosing a higher mean pre-dose plasma oxprenolol concentration than Slow Trasicor."( A multiple dose comparative study of the pharmacodynamic and pharmacokinetic behaviour of polymer-matrix and Oros dosage forms of oxprenolol in healthy volunteers.
Halsey, A; Jack, DB; John, VA; Kendall, MJ; O'Donnell, ML; Warrington, SJ; Woods, KL, 1985
)
0.68
"Plasma oxprenolol concentrations were measured in six young healthy female volunteers after single oral dosing with a 16/260 oxprenolol Oros system on three separate occasions."( Reproducibility of oxprenolol plasma concentrations in young female volunteers following oral administration of an oxprenolol Oros dosage form.
Jack, DB; Kendall, MJ; Laugher, SJ; Smith, SR, 1985
)
1.05
"Plasma concentrations of oxprenolol have been measured in six healthy volunteers following single-dose oral administration of the drug in conventional and Oros dosage forms in fasting and postprandial states."( Influence of food intake on plasma oxprenolol concentrations following oral administration of conventional and Oros preparations.
John, VA; Smith, SE, 1985
)
0.85
" Repeated dosing with both Oros and SR oxprenolol preparations, in comparison with placebo, significantly reduced supine systolic and diastolic blood pressures, and pulse rate at 24 h after dosing."( Exercise and resting blood pressure and heart rate changes 24 h after dosing in patients with essential hypertension receiving 16/260 oxprenolol Oros once daily.
Allsopp, LF; Bolli, P; Bühler, FR; Cooper, GL; Frei, P; Glaus, L; Müller, FB; Ritz, R, 1985
)
0.74
" These results provide some justification for the development of oral dosage forms with extended durations of release even for drugs which undergo significant first-pass metabolism."( Evaluation of oxprenolol and metoprolol Oros systems in the dog: comparison of in vivo and in vitro drug release, and of drug absorption from duodenal and colonic infusion sites.
Fara, JW; Myrback, RE; Swanson, DR, 1985
)
0.63
"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
" Results obtained show that the fixed combination oxprenolol 80 mg plus chlorthalidone 10 mg can be safely administered also in the elderly hypertensive patients, without risk of cardiovascular complications, allowing satisfactory blood pressure control, with a simple dosage schedule, thus improving patient compliance to the therapy."( [Effectiveness of treatment with beta-blocking agents and diuretics in fixed combination, in aged hypertensive patients].
Andreoni, A; Paciaroni, E; Quattrini, L; Saccomanno, G, 1980
)
0.51
" 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
)
0.5
"The haemodynamic dose-response effects of intravenous oxprenolol over the range of 2--64 mg were measured in 28 patients with coronary heart disease."( Haemodynamic dose-response effects of intravenous oxprenolol in coronary heart disease.
Hilal, A; Silke, B; Taylor, SH,
)
0.63
" 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 a pilot study, the presented method was used to investigate the metabolic fate of the enantiomers in two dogs dosed orally with racemic [14C]oxprenolol hydrochloride (3 mg/kg)."( Multiple inverse isotope dilution assay for the stereospecific determination of R(+)- and S(-)-oxprenolol in biological fluids.
Dieterle, W; Faigle, JW, 1983
)
0.68
" A comparison of mean standing diastolic blood pressure and supine systolic and diastolic blood presses showed no significant difference between groups during the fixed dosage period."( A double-blind study of oxprenolol once and twice daily in hypertensive patients.
Friedman, B; Gerlings, E; Glazer, N; Gross, S; Lowney, C; Solomon, R, 1983
)
0.57
" All study designs but 1 called for dosage to be increased to a maximum of 480 mg/day."( Clinical responses to oxprenolol in the elderly.
Ellis, RA, 1983
)
0.58
" 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
)
0.51
"25 mg cyclopenthiazide during the first 4 weeks of each treatment period, after which the dosage was doubled."( Lipids and lipoprotein fractions after cyclopenthiazide and oxprenolol: a double-blind crossover study.
Carruthers, M; Crisp, AJ; Ebbutt, AF; Hoffbrand, BI; Kennedy, PG, 1980
)
0.5
" The results from this study suggest that these compounds in their standard dosage range are useful and safe antihypertensive agents in older patients."( The treatment of hypertension in older patients: a double-blind, between-patient study, in previously treated patients comparing a diuretic, a beta-receptor antagonist, and their fixed combination.
Forrest, WA, 1981
)
0.26
" It has been shown that multiple dosing does not result in oxprenolol accumulation in either group and that age has no effect on the pharmacokinetics of this drug."( The effect of age on the pharmacokinetics of oxprenolol.
Kendall, MJ; Quarterman, CP, 1982
)
0.77
" 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
)
0.88
" The remaining patients of both groups double the corresponding dosage after the first 4 weeks."( A fixed combination of oxprenolol slow-release and chlorthalidone once daily in treatment of mild to moderate hypertension.
Agabiti-Rosei, E; Buoninconti, R; Carotti, A; Fariello, R; Innocenti, P; Motolese, M; Muiesan, G; Toso, M; Valori, C, 1981
)
0.57
" throughout the study; the remaining doubled the corresponding dosage after the first 2 weeks."( Antihypertensive activity of a fixed combination of oxprenolol and chlorthalidone in mild to moderate arterial hypertension.
Agabiti-Rosei, E; Carotti, A; Innocenti, P; Montervino, C; Motolese, M; Muiesan, G; Solinas, E; Toso, M, 1980
)
0.51
"We have studied the effect of dosage time of oxprenolol (Trasicor) on its pharmacokinetics and pharmacodynamics in six healthy volunteers."( The effect of oxprenolol dosage time on its pharmacokinetics and haemodynamic effects during exercise in man.
Karemaker, JM; Koopmans, R; Oosterhuis, B; van Boxtel, CJ; Wemer, J, 1993
)
0.91
"The purpose of this work was to study solute (drug and protein)/polymer interactions that affect solute diffusion in and subsequent release from swellable dosage forms based on environmentally responsive, pH-sensitive polymer networks."( Analysis of drug distribution in hydrogels using fourier transform infrared microscopy.
am Ende, MT; Peppas, NA, 1995
)
0.29
"The bioequivalence of oral dosage forms of oxprenolol was assessed in a triple crossover study on two groups of 12 volunteers each."( Relative bioavailability of different oral sustained release oxprenolol tablets.
Capalneanu, R; Follidis, M; Leucuta, SE; Mocan, A,
)
0.64
"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
" The work suggests the potential of this pharmaceutical delivery system as an alternative controlled-release dosage form, either for oral or nasal administration."( Oxprenolol-loaded bioadhesive microspheres: preparation and in vitro/in vivo characterization.
Leucuta, SE; Preda, M,
)
1.57
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
aromatic etherAny ether in which the oxygen is attached to at least one aryl substituent.
[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]

Pathways (1)

PathwayProteinsCompounds
Oxprenolol Action Pathway478

Protein Targets (4)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Solute carrier family 22 member 1 Homo sapiens (human)IC50 (µMol)28.60000.21005.553710.0000AID386625
Bile salt export pumpHomo sapiens (human)IC50 (µMol)1,000.00000.11007.190310.0000AID1449628
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Ki0.09330.00010.739610.0000AID4411
5-hydroxytryptamine receptor 7Cavia porcellus (domestic guinea pig)IC50 (µMol)28.60002.03005.53139.9000AID386625
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (50)

Processvia Protein(s)Taxonomy
xenobiotic metabolic processSolute carrier family 22 member 1 Homo sapiens (human)
neurotransmitter transportSolute carrier family 22 member 1 Homo sapiens (human)
serotonin transportSolute carrier family 22 member 1 Homo sapiens (human)
establishment or maintenance of transmembrane electrochemical gradientSolute carrier family 22 member 1 Homo sapiens (human)
organic cation transportSolute carrier family 22 member 1 Homo sapiens (human)
quaternary ammonium group transportSolute carrier family 22 member 1 Homo sapiens (human)
prostaglandin transportSolute carrier family 22 member 1 Homo sapiens (human)
monoamine transportSolute carrier family 22 member 1 Homo sapiens (human)
putrescine transportSolute carrier family 22 member 1 Homo sapiens (human)
spermidine transportSolute carrier family 22 member 1 Homo sapiens (human)
acetylcholine transportSolute carrier family 22 member 1 Homo sapiens (human)
dopamine transportSolute carrier family 22 member 1 Homo sapiens (human)
norepinephrine transportSolute carrier family 22 member 1 Homo sapiens (human)
thiamine transportSolute carrier family 22 member 1 Homo sapiens (human)
xenobiotic transportSolute carrier family 22 member 1 Homo sapiens (human)
epinephrine transportSolute carrier family 22 member 1 Homo sapiens (human)
serotonin uptakeSolute carrier family 22 member 1 Homo sapiens (human)
norepinephrine uptakeSolute carrier family 22 member 1 Homo sapiens (human)
thiamine transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
metanephric proximal tubule developmentSolute carrier family 22 member 1 Homo sapiens (human)
purine-containing compound transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
dopamine uptakeSolute carrier family 22 member 1 Homo sapiens (human)
monoatomic cation transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
transport across blood-brain barrierSolute carrier family 22 member 1 Homo sapiens (human)
(R)-carnitine transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
acyl carnitine transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
spermidine transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
cellular detoxificationSolute carrier family 22 member 1 Homo sapiens (human)
xenobiotic transport across blood-brain barrierSolute carrier family 22 member 1 Homo sapiens (human)
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (26)

Processvia Protein(s)Taxonomy
acetylcholine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
neurotransmitter transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
dopamine:sodium symporter activitySolute carrier family 22 member 1 Homo sapiens (human)
norepinephrine:sodium symporter activitySolute carrier family 22 member 1 Homo sapiens (human)
protein bindingSolute carrier family 22 member 1 Homo sapiens (human)
monoamine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
secondary active organic cation transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
organic anion transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
organic cation transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
prostaglandin transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
pyrimidine nucleoside transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
thiamine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
putrescine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
spermidine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
quaternary ammonium group transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
toxin transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
identical protein bindingSolute carrier family 22 member 1 Homo sapiens (human)
xenobiotic transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
(R)-carnitine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (15)

Processvia Protein(s)Taxonomy
plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
basal plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
membraneSolute carrier family 22 member 1 Homo sapiens (human)
basolateral plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
apical plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
lateral plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
presynapseSolute carrier family 22 member 1 Homo sapiens (human)
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (123)

Assay IDTitleYearJournalArticle
AID1131360Antagonist activity at beta adrenergic receptor in guinea pig tracheal strips assessed as inhibition of 10'-7 M isoproterenol-induced tracheal relaxation incubated 1 hr prior to testing1979Journal of medicinal chemistry, Dec, Volume: 22, Issue:12
Synthesis of 4'- and 5'-hydroxyoxprenolol:pharmacologically active ring-hydroxylated metabolites of oxprenolol.
AID1449628Inhibition 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 method2012Drug 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.
AID1133114Drug excretion in Sprague-Dawley rat urine assessed as 6-methoxyoxprenolol formation at 20 mg/kg, ip after 24 hrs by GC-CIMS analysis in presence of beta-glucuronidase and CH2N21978Journal of medicinal chemistry, Dec, Volume: 21, Issue:12
Aromatic hydroxylation of beta-adrenergic antagonists. 4- and 5-hydroxylation of 1-(isopropylamino)-3-[2-(allyloxy)phenoxy]-2-propanol (oxprenolol).
AID288192Partition coefficient, log P of the compound2007Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11
QSAR study on permeability of hydrophobic compounds with artificial membranes.
AID312895Partition coefficient, log P of the compound2008Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
High-throughput log P determination by ultraperformance liquid chromatography: a convenient tool for medicinal chemists.
AID1079936Choleostatic 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]
AID1131361Antagonist activity at beta adrenergic receptor in guinea pig tracheal strips assessed as inhibition of 10'-6 M isoproterenol-induced tracheal relaxation incubated 1 hr prior to testing1979Journal of medicinal chemistry, Dec, Volume: 22, Issue:12
Synthesis of 4'- and 5'-hydroxyoxprenolol:pharmacologically active ring-hydroxylated metabolites of oxprenolol.
AID1079935Cytolytic 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]
AID48346Beta-1-adrenoceptor antagonsim of compound expressed as inhibition of isoprenaline-induced tachycardia in the ganglion-blocked anesthetized cat1988Journal of medicinal chemistry, Feb, Volume: 31, Issue:2
Design and synthesis of a series of combined vasodilator/beta-adrenoceptor antagonists based on 6-arylpyridazinones.
AID681962TP_TRANSPORTER: inhibition of cimetidine uptake (Cimetidine: 100 uM, Oxprenolol: 1000 uM) in OCT2-expressing mIMCD3 cells2000British 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.
AID1130716Drug excretion in Sprague-Dawley rat urine assessed as 3'-methoxyoxprenolol at 20 mg/kg, ip measured after 24 hrs by GC-CIMS analysis in presence of beta-glucuronidase and CH2N21979Journal of medicinal chemistry, Sep, Volume: 22, Issue:9
Aromatic hydroxylation of beta-adrenergic antagonists. Formation of 4'- and 5'-hydroxy-1-(isopropylamino)-3-[2'-allyloxy)phenoxy]-2-propanol from oxprenolol.
AID1209593Dissociation constant, pKa of the acidic compound by capillary electrophoresis-mass spectrometry analysis2011Drug 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.
AID496828Antimicrobial activity against Leishmania donovani2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID496817Antimicrobial activity against Trypanosoma cruzi2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID15120Percent of the drug absorbed after administration to humans was determined1999Journal of medicinal chemistry, May-20, Volume: 42, Issue:10
Molecular hashkeys: a novel method for molecular characterization and its application for predicting important pharmaceutical properties of molecules.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1131359Antagonist activity at beta adrenergic receptor in guinea pig tracheal strips assessed as inhibition of 10'-8 M isoproterenol-induced tracheal relaxation incubated 1 hr prior to testing1979Journal of medicinal chemistry, Dec, Volume: 22, Issue:12
Synthesis of 4'- and 5'-hydroxyoxprenolol:pharmacologically active ring-hydroxylated metabolites of oxprenolol.
AID496831Antimicrobial activity against Cryptosporidium parvum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID18847Percent of drug absorbed by human intestine after oral administration2000Journal of medicinal chemistry, Oct-05, Volume: 43, Issue:20
Fast calculation of molecular polar surface area as a sum of fragment-based contributions and its application to the prediction of drug transport properties.
AID237585Tested for fraction of oral dose absorbed orally in humans2005Journal 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).
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID496827Antimicrobial activity against Leishmania amazonensis2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID29359Ionization constant (pKa)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID1209582Unbound volume of distribution in Sprague-Dawley rat brain slices at 100 nM after 5 hrs2011Drug 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.
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID25049pK value is evaluated1984Journal of medicinal chemistry, Jul, Volume: 27, Issue:7
Beta-adrenergic blocking agents: substituted phenylalkanolamines. Effect of side-chain length on beta-blocking potency in vitro.
AID496824Antimicrobial activity against Toxoplasma gondii2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID496829Antimicrobial activity against Leishmania infantum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1133105Drug excretion in Sprague-Dawley rat urine assessed as 5-hydroxyoxprenolol formation at 20 mg/kg, ip after 24 hrs by GC-CIMS analysis1978Journal of medicinal chemistry, Dec, Volume: 21, Issue:12
Aromatic hydroxylation of beta-adrenergic antagonists. 4- and 5-hydroxylation of 1-(isopropylamino)-3-[2-(allyloxy)phenoxy]-2-propanol (oxprenolol).
AID604021Unbound volume of distribution in Sprague-Dawley rat brain measured per gram of brain tissue 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 b2009Journal 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.
AID48526Beta-adrenoceptor blocking potency in cat, measured as the degree (percent) of blockade of the vasopressor response at the dose level1980Journal 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.
AID496823Antimicrobial activity against Trichomonas vaginalis2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID41903Beta adrenoceptor blocking potency was estimated by inhibition of 50% of the tachycardia produced by a submaximal dose of the isoproterenol (0.2ug/kg, intravenously)1981Journal of medicinal chemistry, Nov, Volume: 24, Issue:11
Beta-adrenergic blocking agents. 21. threo-1-(Aryloxy)-3-(alkylamino)butan-2-ols.
AID496832Antimicrobial activity against Trypanosoma brucei rhodesiense2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID311367Permeability coefficient in human skin2007Bioorganic & medicinal chemistry, Nov-15, Volume: 15, Issue:22
Transdermal penetration behaviour of drugs: CART-clustering, QSPR and selection of model compounds.
AID350216Dissociation constant, pKa of the compound2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Lipophilicity of basic drugs measured by hydrophilic interaction chromatography.
AID604024Unbound 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)/hr2009Journal 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.
AID48368Intrinsic Sympathomimetic Activity (ISA) determined from the ratio of the maximal compound and isoprenaline induced tachycardia in anesthetized ganglion blocked cats following intravenous administration1988Journal of medicinal chemistry, Feb, Volume: 31, Issue:2
Design and synthesis of a series of combined vasodilator/beta-adrenoceptor antagonists based on 6-arylpyridazinones.
AID78664Beta-adrenoceptor blocking potency in the isolated guinea pig heart, giving 50% inhibition of isoproterenol-induced tachycardia relative to oxprenolol1984Journal of medicinal chemistry, Jul, Volume: 27, Issue:7
Beta-adrenergic blocking agents: substituted phenylalkanolamines. Effect of side-chain length on beta-blocking potency in vitro.
AID386623Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells at 100 uM by confocal microscopy2008Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
Structural requirements for drug inhibition of the liver specific human organic cation transport protein 1.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID1209583Unbound drug partitioning coefficient, Kp of the compound assessed as ratio of unbound concentration in Sprague-Dawley rat brain to unbound concentration in plasma2011Drug 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.
AID1130717Drug excretion in Sprague-Dawley rat urine assessed as 6'-methoxyoxprenolol at 20 mg/kg, ip measured after 24 hrs by GC-CIMS analysis in presence of beta-glucuronidase and CH2N21979Journal of medicinal chemistry, Sep, Volume: 22, Issue:9
Aromatic hydroxylation of beta-adrenergic antagonists. Formation of 4'- and 5'-hydroxy-1-(isopropylamino)-3-[2'-allyloxy)phenoxy]-2-propanol from oxprenolol.
AID1130714Drug excretion in Sprague-Dawley rat urine assessed as 5'-methoxyoxprenolol at 20 mg/kg, ip measured after 24 hrs by GC-CIMS analysis in presence of beta-glucuronidase and CH2N21979Journal of medicinal chemistry, Sep, Volume: 22, Issue:9
Aromatic hydroxylation of beta-adrenergic antagonists. Formation of 4'- and 5'-hydroxy-1-(isopropylamino)-3-[2'-allyloxy)phenoxy]-2-propanol from oxprenolol.
AID26525Distribution coefficient measured in Octanol/buffer (0.15 M KCl)1998Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27
Evaluation of dynamic polar molecular surface area as predictor of drug absorption: comparison with other computational and experimental predictors.
AID1131363Antagonist activity at beta adrenergic receptor in guinea pig tracheal strips assessed as inhibition of isoproterenol-induced tracheal relaxation incubated 1 hr prior to testing1979Journal of medicinal chemistry, Dec, Volume: 22, Issue:12
Synthesis of 4'- and 5'-hydroxyoxprenolol:pharmacologically active ring-hydroxylated metabolites of oxprenolol.
AID496819Antimicrobial activity against Plasmodium falciparum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID288184Permeability coefficient through artificial membrane in presence of unstirred water layer by PAMPA2007Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11
QSAR study on permeability of hydrophobic compounds with artificial membranes.
AID28392Apparent permeability coefficient (Papp) (Caco-2 cell monolayer)2001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
Experimental and computational screening models for the prediction of intestinal drug absorption.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID496826Antimicrobial activity against Entamoeba histolytica2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID603954In-vivo blood/plasma to lung partition coefficients of the compound, logP(lung) in rat2008European journal of medicinal chemistry, Mar, Volume: 43, Issue:3
Air to lung partition coefficients for volatile organic compounds and blood to lung partition coefficients for volatile organic compounds and drugs.
AID1091955Dissociation constant, pKa of the compound at pH 7.32011Journal of agricultural and food chemistry, Apr-13, Volume: 59, Issue:7
Importance of physicochemical properties for the design of new pesticides.
AID156202Binding to POPC (palmitoyl-oleolyl-phosphatidyl-choline) liposomes using biosensor system2000Journal 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.
AID496820Antimicrobial activity against Trypanosoma brucei2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID78651Beta-adrenoceptor blocking potency in the isolated guinea pig heart, giving 50% inhibition of isoproterenol-induced tachycardia1984Journal of medicinal chemistry, Jul, Volume: 27, Issue:7
Beta-adrenergic blocking agents: substituted phenylalkanolamines. Effect of side-chain length on beta-blocking potency in vitro.
AID604023Ratio 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 method2009Journal 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.
AID25572Dissociation constant of the compound1998Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27
Evaluation of dynamic polar molecular surface area as predictor of drug absorption: comparison with other computational and experimental predictors.
AID21254Mono layer permeability of human intestinal Caco-2 cells1998Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27
Evaluation of dynamic polar molecular surface area as predictor of drug absorption: comparison with other computational and experimental predictors.
AID604025Unbound 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 method2009Journal 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.
AID4411Binding affinity of a compound to rat brain 5-hydroxytryptamine 1A (serotonin) receptor assayed by radiolabeled [3H]-8-OH-DPAT ligand displacement1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
Binding of arylpiperazines, (aryloxy)propanolamines, and tetrahydropyridylindoles to the 5-HT1A receptor: contribution of the molecular lipophilicity potential to three-dimensional quantitative structure-affinity relationship models.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID91481Binding constant against human serum albumin (HSA)2001Journal of medicinal chemistry, Dec-06, Volume: 44, Issue:25
Cheminformatic models to predict binding affinities to human serum albumin.
AID29845Estimation of fraction absorbed (Fa) in the human intestine using biosensor technology.2000Journal 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.
AID497005Antimicrobial activity against Pneumocystis carinii2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID231333Ratio of [(apical to basal)/(basal to apical)] (Caco-2 cell monolayer)2001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
Experimental and computational screening models for the prediction of intestinal drug absorption.
AID28399Cellular permeability (Pc) (Caco-2 cell monolayer)2001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
Experimental and computational screening models for the prediction of intestinal drug absorption.
AID1133113Drug excretion in Sprague-Dawley rat urine assessed as 3-methoxyoxprenolol formation at 20 mg/kg, ip after 24 hrs by GC-CIMS analysis in presence of beta-glucuronidase and CH2N21978Journal of medicinal chemistry, Dec, Volume: 21, Issue:12
Aromatic hydroxylation of beta-adrenergic antagonists. 4- and 5-hydroxylation of 1-(isopropylamino)-3-[2-(allyloxy)phenoxy]-2-propanol (oxprenolol).
AID476929Human intestinal absorption in po dosed human2010European journal of medicinal chemistry, Mar, Volume: 45, Issue:3
Neural computational prediction of oral drug absorption based on CODES 2D descriptors.
AID1209581Fraction unbound in Sprague-Dawley rat brain homogenates at 5 uM by equilibrium dialysis analysis2011Drug 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.
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID288185Permeability coefficient through artificial membrane in presence of stirred water layer2007Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11
QSAR study on permeability of hydrophobic compounds with artificial membranes.
AID1079938Chronic 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]
AID350217Octanol-water partition coefficient, log P of the cationic form of the compound2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Lipophilicity of basic drugs measured by hydrophilic interaction chromatography.
AID1130712Drug excretion in Sprague-Dawley rat urine assessed as 6'-hydroxyoxprenolol at 20 mg/kg, ip measured after 24 hrs by GC-CIMS analysis1979Journal of medicinal chemistry, Sep, Volume: 22, Issue:9
Aromatic hydroxylation of beta-adrenergic antagonists. Formation of 4'- and 5'-hydroxy-1-(isopropylamino)-3-[2'-allyloxy)phenoxy]-2-propanol from oxprenolol.
AID386625Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy2008Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
Structural requirements for drug inhibition of the liver specific human organic cation transport protein 1.
AID29812Oral bioavailability in human2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID604022Fraction unbound 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 method2009Journal 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.
AID592681Apparent permeability across human Caco2 cell membrane after 2 hrs by LC-MS/MS analysis2011Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8
QSAR-based permeability model for drug-like compounds.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID1133112Drug excretion in Sprague-Dawley rat urine assessed as 6-hydroxyoxprenolol formation at 20 mg/kg, ip after 24 hrs by GC-CIMS analysis1978Journal of medicinal chemistry, Dec, Volume: 21, Issue:12
Aromatic hydroxylation of beta-adrenergic antagonists. 4- and 5-hydroxylation of 1-(isopropylamino)-3-[2-(allyloxy)phenoxy]-2-propanol (oxprenolol).
AID455986Permeability across human Caco-2 cells2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
Computational modeling of novel inhibitors targeting the Akt pleckstrin homology domain.
AID496821Antimicrobial activity against Leishmania2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID496825Antimicrobial activity against Leishmania mexicana2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID29844Fraction absorbed after oral administration in humans2001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
Experimental and computational screening models for the prediction of intestinal drug absorption.
AID48524In 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)1980Journal 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.
AID350220Lipophilicity, log K at pH 2 by by hydrophilic interaction chromatography using 100% water as mobile phase2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Lipophilicity of basic drugs measured by hydrophilic interaction chromatography.
AID27167Delta logD (logD6.5 - logD7.4)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID156204Binding to POPC/GMI liposomes using biosensor system2000Journal 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.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1091956Apparent hydrophobicity, log D of the compound in Octanol-buffer2011Journal of agricultural and food chemistry, Apr-13, Volume: 59, Issue:7
Importance of physicochemical properties for the design of new pesticides.
AID1133108Drug excretion in Sprague-Dawley rat urine assessed as 4-methoxyoxprenolol formation at 20 mg/kg, ip after 24 hrs by GC-CIMS analysis in presence of beta-glucuronidase and CH2N21978Journal of medicinal chemistry, Dec, Volume: 21, Issue:12
Aromatic hydroxylation of beta-adrenergic antagonists. 4- and 5-hydroxylation of 1-(isopropylamino)-3-[2-(allyloxy)phenoxy]-2-propanol (oxprenolol).
AID496830Antimicrobial activity against Leishmania major2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1091957Apparent permeability of the compound by PAMPA2011Journal of agricultural and food chemistry, Apr-13, Volume: 59, Issue:7
Importance of physicochemical properties for the design of new pesticides.
AID23471Partition coefficient (logP)1984Journal of medicinal chemistry, Jul, Volume: 27, Issue:7
Beta-adrenergic blocking agents: substituted phenylalkanolamines. Effect of side-chain length on beta-blocking potency in vitro.
AID1133106Drug excretion in Sprague-Dawley rat urine assessed as 4-hydroxyoxprenolol formation at 20 mg/kg, ip after 24 hrs by GC-CIMS analysis1978Journal of medicinal chemistry, Dec, Volume: 21, Issue:12
Aromatic hydroxylation of beta-adrenergic antagonists. 4- and 5-hydroxylation of 1-(isopropylamino)-3-[2-(allyloxy)phenoxy]-2-propanol (oxprenolol).
AID1130709Drug excretion in Sprague-Dawley rat urine assessed as 5'-hydroxyoxprenolol at 20 mg/kg, ip measured after 24 hrs by GC-CIMS analysis1979Journal of medicinal chemistry, Sep, Volume: 22, Issue:9
Aromatic hydroxylation of beta-adrenergic antagonists. Formation of 4'- and 5'-hydroxy-1-(isopropylamino)-3-[2'-allyloxy)phenoxy]-2-propanol from oxprenolol.
AID350218Octanol-water partition coefficient, log PC of the compound2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Lipophilicity of basic drugs measured by hydrophilic interaction chromatography.
AID1130708Drug excretion in Sprague-Dawley rat urine assessed as 4'-hydroxyoxprenolol at 20 mg/kg, ip measured after 24 hrs by GC-CIMS analysis1979Journal of medicinal chemistry, Sep, Volume: 22, Issue:9
Aromatic hydroxylation of beta-adrenergic antagonists. Formation of 4'- and 5'-hydroxy-1-(isopropylamino)-3-[2'-allyloxy)phenoxy]-2-propanol from oxprenolol.
AID1130711Drug excretion in Sprague-Dawley rat urine assessed as 3'-hydroxyoxprenolol at 20 mg/kg, ip measured after 24 hrs by GC-CIMS analysis1979Journal of medicinal chemistry, Sep, Volume: 22, Issue:9
Aromatic hydroxylation of beta-adrenergic antagonists. Formation of 4'- and 5'-hydroxy-1-(isopropylamino)-3-[2'-allyloxy)phenoxy]-2-propanol from oxprenolol.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID409954Inhibition of mouse brain MAOA2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
AID1091958Hydrophobicity, log P of the compound in octanol-water by shaking-flask method2011Journal of agricultural and food chemistry, Apr-13, Volume: 59, Issue:7
Importance of physicochemical properties for the design of new pesticides.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID781326pKa (acid-base dissociation constant) as determined by Avdeef ref: DOI: 10.1002/047145026X2014Pharmaceutical research, Apr, Volume: 31, Issue:4
Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds.
AID350219Lipophilicity, log K at pH 2 by by hydrophilic interaction chromatography using 95% acetonitrile as mobile phase2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Lipophilicity of basic drugs measured by hydrophilic interaction chromatography.
AID1130713Drug excretion in Sprague-Dawley rat urine assessed as 4'-methoxyoxprenolol at 20 mg/kg, ip measured after 24 hrs by GC-CIMS analysis in presence of beta-glucuronidase and CH2N21979Journal of medicinal chemistry, Sep, Volume: 22, Issue:9
Aromatic hydroxylation of beta-adrenergic antagonists. Formation of 4'- and 5'-hydroxy-1-(isopropylamino)-3-[2'-allyloxy)phenoxy]-2-propanol from oxprenolol.
AID1133111Drug excretion in Sprague-Dawley rat urine assessed as 3-hydroxyoxprenolol formation at 20 mg/kg, ip after 24 hrs by GC-CIMS analysis1978Journal of medicinal chemistry, Dec, Volume: 21, Issue:12
Aromatic hydroxylation of beta-adrenergic antagonists. 4- and 5-hydroxylation of 1-(isopropylamino)-3-[2-(allyloxy)phenoxy]-2-propanol (oxprenolol).
AID312896Partition coefficient, log P by UPLC method2008Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
High-throughput log P determination by ultraperformance liquid chromatography: a convenient tool for medicinal chemists.
AID1079933Acute 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
AID1133109Drug excretion in Sprague-Dawley rat urine assessed as 5-methoxyoxprenolol formation at 20 mg/kg, ip after 24 hrs by GC-CIMS analysis in presence of beta-glucuronidase and CH2N21978Journal of medicinal chemistry, Dec, Volume: 21, Issue:12
Aromatic hydroxylation of beta-adrenergic antagonists. 4- and 5-hydroxylation of 1-(isopropylamino)-3-[2-(allyloxy)phenoxy]-2-propanol (oxprenolol).
AID1079931Moderate 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]
AID496818Antimicrobial activity against Trypanosoma brucei brucei2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID48537Percent inhibition of vasopressor response1981Journal of medicinal chemistry, Nov, Volume: 24, Issue:11
Beta-adrenergic blocking agents. 21. threo-1-(Aryloxy)-3-(alkylamino)butan-2-ols.
AID604020Unbound 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 method2009Journal 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.
AID28681Partition coefficient (logD6.5)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal 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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (983)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990851 (86.57)18.7374
1990's76 (7.73)18.2507
2000's34 (3.46)29.6817
2010's19 (1.93)24.3611
2020's3 (0.31)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 39.80

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 strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index39.80 (24.57)
Research Supply Index7.19 (2.92)
Research Growth Index4.11 (4.65)
Search Engine Demand Index65.76 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (39.80)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials285 (27.38%)5.53%
Reviews49 (4.71%)6.00%
Case Studies55 (5.28%)4.05%
Observational0 (0.00%)0.25%
Other652 (62.63%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]