Page last updated: 2024-12-04

betaxolol

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Cross-References

ID SourceID
PubMed CID2369
CHEMBL ID423
CHEBI ID3082
SCHEMBL ID23530
MeSH IDM0024177

Synonyms (99)

Synonym
betaxololum
1-{4-[2-(cyclopropylmethoxy)ethyl]phenoxy}-3-(propan-2-ylamino)propan-2-ol
AC-1115
BRD-A02759312-003-03-9
gtpl549
AKOS015841671
1-[(4-{2-[(cyclopropylmethyl)oxy]ethyl}phenyl)oxy]-3-[(1-methylethyl)amino]propan-2-ol
PRESTWICK3_000382
BSPBIO_000563
kerledex
2-propanol, 1-(4-(2-(cyclopropylmethoxy)ethyl)phenoxy)-3-((1-methylethyl)amino)-
sl 75212
betaxolol [inn:ban]
betaxololum [inn-latin]
BPBIO1_000621
D07526
betaxolol (inn)
betaxolol (tn)
LOPAC0_000193
PRESTWICK2_000382
63659-18-7
C06849
betaxolol ,
1-(isopropylamino)-3-[p-(cyclopropylmethoxyethyl)phenoxy]-2-propanol
DB00195
1-(4-(2-(cyclopropylmethoxy)ethyl)phenoxy)-3-((1-methylethyl)amino)-2-propanol
NCGC00024863-04
PRESTWICK0_000382
PRESTWICK1_000382
SPBIO_002484
NCGC00024863-03
HMS2089I07
NCGC00015159-08
sl-75212-10
L000125
chebi:3082 ,
alo-140102 free base
sl-7521210 free base
CHEMBL423
1-[4-[2-(cyclopropylmethoxy)ethyl]phenoxy]-3-(propan-2-ylamino)propan-2-ol
NCGC00015159-06
A834454
1-[4-[2-(cyclopropylmethoxy)ethyl]phenoxy]-3-(isopropylamino)propan-2-ol;betaxolol
108008-51-1
dtxcid102674
tox21_110091
cas-63659-18-7
dtxsid2022674 ,
CCG-204288
NCGC00015159-09
NCGC00015159-04
NCGC00015159-05
bdbm50405521
o0zr1r6rz2 ,
unii-o0zr1r6rz2
betaxolol s
S2091
betaxolol [inn]
betaxolol [who-dd]
betaxolol [mi]
betaxolol [vandf]
HY-B0381
SCHEMBL23530
tox21_110091_1
NCGC00015159-11
(.+/-.)-1-[p-[2-(cyclopropylmethoxy)ethyl]phenoxy]-3-(isopropylamino)-2-propanol
1-(4-[2-(cyclopropylmethoxy)ethyl]phenoxy)-3-(isopropylamino)-2-propanol #
Q-200713
dextrobetaxolol
1-(4-(2-(cyclopropylmethoxy)ethyl)phenoxy)-3-(isopropylamino)propan-2-ol
HMS3655P17
MRF-0000336
SW196917-5
FT-0773524
betaxolol (betoptic)
AS-14125
Q794162
(r)-betaxolol; (+)-betaxolol
BRD-A02759312-003-11-2
SDCCGSBI-0050181.P002
NCGC00015159-23
HMS3884L05
NCGC00015159-13
C75987
NCGC00015159-14
1-[4-(2-(cyclopropylmethyloxy)ethyl]-phenoxy]-3-[(1-methylethyl)amino]-2-propanol
(+/-)-1-(isopropylamino)-3-[p-(cyclopropylmethoxyethyl)phenoxy]-2-propanol
(r)-1-[4-(2-cyclopropylmethoxy-ethyl)-phenoxy]-3-isopropylamino-propan-2-ol
cobalt,[(1,2,5,6-h)-1,5-cyclooctadiene][(1,2,3,4,5-h)-1-(trifluoroacetyl)-2,4-cyclopentadien-1-yl]-
2-propanol, 1-[4-[2-(cyclopropylmethoxy)ethyl]phenoxy]-3-[(1-methylethyl)amino]-
EN300-18552812
1-{4-[2-(cyclopropylmethoxy)ethyl]phenoxy}-3-[(propan-2-yl)amino]propan-2-ol
s01ed02
c07ab05
1-(4-(2-(cyclopropylmethoxy)ethyl)phenoxy)-3-((1-methylethyl)amino)-propanol
betaxololum (inn-latin)
1-(isopropylamino)-3-(p-(cyclopropylmethoxyethyl)phenoxy)-2-propanol
betaxololo
1-(4-(2-(cyclopropylmethoxy)ethyl)phenoxy)-3-(propan-2-ylamino)propan-2-ol

Research Excerpts

Overview

Betaxolol hydrochloride is a beta1-selective antagonist that produces vasodilation in patients with hypertension and ischemic heart disease. It has a bioavailability of 90% and a T 1/2 of 20 h.

ExcerptReferenceRelevance
"Betaxolol is a relatively cardioselective β-adrenoceptor blocking drug, with no partial agonist (intrinsic sympathomimetic) activity and weak membrane-stabilizing (local anesthetic) activity. "( Betaxolol: A comprehensive profile.
Abdel-Aziz, AA; Al-Wadei, MJ; Bakheit, AH; Wani, TA, 2021
)
3.51
"Betaxolol is a selective beta(1) receptor blocker used in the treatment of hypertension and glaucoma. "( The structure of betaxolol studied by infrared spectroscopy and natural bond orbital theory.
Canotilho, J; Castro, RA, 2010
)
2.14
"Betaxolol is a beta-adrenergic blocker but its neuroprotective action is generally thought to be due to its calcium channel blocking properties. "( Nitric oxide synthase expression in the transient ischemic rat retina: neuroprotection of betaxolol.
Cheon, EW; Cho, GJ; Choi, WS; Kang, SS; Park, CH; Song, JK; Yoo, JM, 2002
)
1.98
"Betaxolol is a compound that has beta(1)-adrenergic receptor blocking and voltage-dependent calcium channel blocking properties."( Effect of betaxolol on aspartate aminotransferase activity in hypoxic rat retina in vitro.
Endo, S; Ishiguro, S; Tamai, M; Tomita, H, 2002
)
1.44
"Betaxolol hydrochloride is a beta1-selective antagonist that produces vasodilation in patients with hypertension and ischemic heart disease. "( Effect of betaxolol hydrochloride on heart rate variability indices during exercise stress testing in patients with hypertension.
Abe, Y; Hattori, H; Ishihara, M; Kurita, A; Matsui, T; Nagata, M; Ohsuzu, F; Takase, B, 2005
)
2.17
"Betaxolol is a selective antagonist of beta(1)-adrenergic receptors. "( Association of CYP2D6 and ADRB1 genes with hypotensive and antichronotropic action of betaxolol in patients with arterial hypertension.
Brovkin, AN; Manchaeva, BB; Minushkina, LO; Nikitin, AG; Nosikov, VV; Savel'eva, EG; Sidorenko, BA; Zateyshchikov, DA; Zateyshchikova, AA, 2007
)
2.01
"3. Betaxolol proved to be a potent and long-lasting beta-adrenoceptor blocking drug, devoid of intrinsic beta-sympathomimetic activity."( 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
)
1.02
"Betaxolol is a cardioselective beta-blocker, which has a bioavailability of 90% and a T 1/2 of 20 h. "( Comparison of two doses of betaxolol and placebo in hypertension: a randomized, double-blind cross-over trial.
Palminteri, R; Salonen, JT, 1982
)
2
"Betaxolol appears to be an effective and well tolerated ocular hypotensive agent in a typical glaucoma population, which includes many patients with cardiopulmonary disease. "( Betaxolol eye drops. A clinical trial of safety and efficacy.
Goldberg, H; Goldberg, I, 1995
)
3.18
"Betaxolol is a beta(1)-adrenergic blocker but its neuroprotective action is generally thought to be due to its calcium channel blocking properties."( Topically applied betaxolol attenuates NMDA-induced toxicity to ganglion cells and the effects of ischaemia to the retina.
Bae, JH; Chidlow, G; DeSantis, L; Nash, MS; Osborne, NN; Ugarte, M; Wood, JP, 1999
)
1.36
"Betaxolol is a useful tool to characterize presynaptic beta 1-adrenoceptors."( Coexistence of presynaptic beta 1- and beta 2-adrenoceptors in splenic strips from young rats and betaxolol-induced beta 1-stereoselective antagonism.
Goshima, Y; Kuwahara, M; Misu, Y; Sato, K,
)
1.07
"Betaxolol is a new beta-blocker that has been reported to have beta 1-selectivity, and it is devoid of both membrane stabilizing action and intrinsic sympathomimetic action. "( Regional hemodynamic effects of betaxolol, a new selective beta 1-blocker, and atenolol in conscious spontaneously hypertensive rats.
Abe, Y; Aki, Y; Fujisawa, Y; He, H; Horiuchi, K; Iwao, H; Kiyomoto, H; Nishiyama, A; Shoji, T; Tamaki, T, 1992
)
2.01
"Betaxolol is a cardioselective beta-adrenergic antagonist effective in the treatment of hypertension. "( Human pharmacokinetics of betaxolol enantiomers.
Davis, PJ; Ludden, TM; Stagni, G, 1991
)
2.02
"Betaxolol is a highly selective beta 1-adrenoceptor antagonist without intrinsic sympathomimetic activity. "( [Antihypertensive effect of betaxolol, a cardioselective beta-adrenoceptor antagonist, in experimental hypertensive rats].
Bessho, H; Narimatsu, A; Suzuki, J; Tobe, A, 1990
)
2.02
"Betaxolol is a new, highly cardioselective, once-a-day beta blocker with a long half-life (mean 16 hours). "( Double-blind comparison of once daily betaxolol versus propranolol four times daily in stable angina pectoris. Betaxolol Investigators Group.
Narahara, KA, 1990
)
1.99
"Betaxolol is a lipophilic beta-adrenoceptor antagonist relatively selective for beta 1-adrenoceptors with only weak beta 2-blocking activity. "( Ocular betaxolol. A review of its pharmacological properties, and therapeutic efficacy in glaucoma and ocular hypertension.
Buckley, MM; Clissold, SP; Goa, KL, 1990
)
2.18
"Betaxolol is a relatively selective beta-1 blocker which in most patients is almost as effective as timolol in lowering intraocular pressure, and may be partly additive with dipivefrin."( Betaxolol.
Goldberg, I, 1989
)
2.44
"Betaxolol is a new antiglaucomatous drug which is blocking solely the beta 1 receptors and in contrast to Timolol may be applied in persons with spastic conditions of the bronchi. "( [Use of Betaxolol in patients with glaucoma and chronic nonspecific diseases of the respiratory system].
Rojek, A; Sempińska-Szewczyk, J; Swietliczko, I; Toczyska-Rozentryt, E, 1989
)
2.15
"Betaxolol is a relatively cardioselective beta-adrenoceptor blocking drug, with no partial agonist (intrinsic sympathomimetic) activity and weak membrane-stabilising (local anaesthetic) activity. "( Betaxolol. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in hypertension.
Beresford, R; Heel, RC, 1986
)
3.16
"Betaxolol hydrochloride is a topical beta 1-blocking agent that has been found to be safe and effective in lowering intraocular pressure (IOP) in patients with glaucoma. "( Additive effect of betaxolol and epinephrine in primary open angle glaucoma.
Allen, RC; Epstein, DL, 1986
)
2.04
"Betaxolol is a new cardioselective beta-blocker without any intrinsic sympathomimetic activity. "( [Study of electrophysiological effects of betaxolol].
Citron, B; Gras, H; Ponsonnaille, J; Serignat, B; Trolese, JF, 1987
)
1.98
"Betaxolol is a relatively cardioselective beta-adrenergic blocker, while levobunolol is a nonselective beta-adrenergic blocking agent."( Comparison of ophthalmic beta-blocking agents.
Lesar, TS, 1987
)
0.99
"Betaxolol is a new beta-adrenergic receptor blocker that preferentially blocks beta 1 receptors."( Aphakic cystoid macular edema secondary to betaxolol therapy.
Hesse, RJ; Swan, JL, 1988
)
1.26
"Betaxolol appears to be a clinically effective and safe agent in the treatment of open-angle glaucoma."( A double-masked comparison of betaxolol vs timolol in the treatment of open-angle glaucoma.
Allen, RC; Epstein, DL; Hertzmark, E; Walker, AM, 1986
)
1.28

Effects

Betaxolol has an effect comparable to timolol in lowering IOP, but is less effective in some patients.

Betaxolol has negligible local anaesthetic activity, so that corneal desensitisation does not occur with its use. It was recently approved for clinical use in the United States for this indication.

ExcerptReferenceRelevance
"Betaxolol has a good hypotensive effect in the absence of adverse effects on lipid and carbohydrate metabolism. "( [Betaxolol treatment of hypertension in postmenopausal women].
Britov, AN; Bystrova, MM; Eliseeva, NA; Gorbunov, VM; Lebedev, AV; Metel'skaia, VA, 1999
)
2.66
"Betaxolol has an effect comparable to timolol in lowering IOP, but is less effective in some patients."( Ocular beta-blockers in glaucoma management. Clinical pharmacological aspects.
Brooks, AM; Gillies, WE,
)
0.85
"Betaxolol has a good hypotensive effect in the absence of adverse effects on lipid and carbohydrate metabolism. "( [Betaxolol treatment of hypertension in postmenopausal women].
Britov, AN; Bystrova, MM; Eliseeva, NA; Gorbunov, VM; Lebedev, AV; Metel'skaia, VA, 1999
)
2.66
"Betaxolol has an effect comparable to timolol in lowering IOP, but is less effective in some patients."( Ocular beta-blockers in glaucoma management. Clinical pharmacological aspects.
Brooks, AM; Gillies, WE,
)
0.85
"Betaxolol has negligible local anaesthetic activity, so that corneal desensitisation does not occur with its use."( Ocular betaxolol. A review of its pharmacological properties, and therapeutic efficacy in glaucoma and ocular hypertension.
Buckley, MM; Clissold, SP; Goa, KL, 1990
)
1.46
"Betaxolol has been proven to be a safe and effective antihypertensive agent, and was recently approved for clinical use in the United States for this indication."( Betaxolol: a new long-acting beta 1-selective adrenergic blocker.
Behrman, D; Frishman, WH; Lazar, EJ; Tepper, D, 1990
)
2.44
"Betaxolol has been well tolerated in most patients."( Betaxolol. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in hypertension.
Beresford, R; Heel, RC, 1986
)
2.44

Actions

Betaxolol may cause small changes in the cardiovascular system. Blood pressure and pulse rates should be checked before prescribing it for the elderly.

ExcerptReferenceRelevance
"Betaxolol may cause small changes in the cardiovascular system, suggesting that blood pressure and pulse rates should be checked before and in regular intervals after prescribing it for the elderly."( Effects of latanoprost and betaxolol on cardiovascular and respiratory status of newly diagnosed glaucoma patients.
Celik, P; Deveci, HM; Erkin, EF; Kayikçioğlu, O; Sakar, A, 2006
)
1.35
"Betaxolol inhibited the increase in Ca(2+)-induced contraction by calmodulin, and this effect of betaxolol was observed even at the concentration that had no effect when given alone."( Betaxolol, a beta 1-adrenoceptor antagonist, inhibits Ca(2+)-induced contraction in skinned renal artery of the dog.
Kitada, Y, 1996
)
2.46
"Betaxolol did not suppress the elevation induced by an EP4 agonist (ONO-AE1-392)."( Effect of topical betaxolol on the acute rise of aqueous flare induced by highly selective agonists for prostaglandin E2 receptor subtypes in pigmented rabbits.
Hayasaka, S; Hayasaka, Y; Kitagawa, K; Nagaki, Y; Yanagisawa, S; Zhang, XY,
)
1.19

Treatment

Betaxolol treatment is associated with a beneficial effect on retinal arteries width. Timolol does not yield the same amplitude of benefit. Retinal blood flow did not change significantly after 90 min, but increased significantly (14 +/- 9%; p = 0.02) after 2 weeks.

ExcerptReferenceRelevance
"The betaxolol-treated group, despite a slight decrease in IOP, had a decreased POBF."( Effect of treatment by medicine or surgery on intraocular pressure and pulsatile ocular blood flow in normal-pressure glaucoma.
Bunce, C; Garway-Heath, DF; Hitchings, RA; Indar, A; Poinoosawmy, D, 2002
)
0.8
"The betaxolol-treated group had significantly lower post-treatment IOP values."( Results of the betaxolol versus placebo treatment trial in ocular hypertension.
Bunce, C; Franks, W; Garway-Heath, D; Hitchings, R; Kamal, D; O'Sullivan, F; Ruben, S; Viswanathan, A, 2003
)
1.15
"Betaxolol treatment is associated with a beneficial effect on retinal arteries width whereas Timolol does not yield the same amplitude of benefit."( Effect of topical betablockers on human retinal vessels diameters.
Collignon, NJ; Collignon-Brach, JD,
)
1.57
"In betaxolol-treated eyes, retinal blood flow did not change significantly after 90 min, but increased significantly (14 +/- 9%; p = 0.02) compared with baseline after 2 weeks."( Comparison of short- and long-term effects of betaxolol and timolol on human retinal circulation.
Fujio, N; Hirokawa, H; Ishiko, S; Kagokawa, H; Kitaya, N; Konno, S; Nagaoka, T; Ogasawara, H; Yoshida, A, 1998
)
1.07
"In betaxolol treated patients diurnal variations in heart rate were definitely changed."( Effects of betaxolol on heart rate in patients with a recent transmural myocardial infarction.
Coupez, R; De Geest, H; Ector, H; Kesteloot, H; Yang, XS, 1987
)
1.18
"Pretreatment with betaxolol (1.5-4 mg/kg s.c.) did not modify the hypothermia following administration of MSO, but potentiation of hypothermia was recorded in rats pretreated with ICI 118,551 (2.26 mg/kg i.p.) then i.p."( Involvement of serotonin receptors in methionine sulfoximine-induced hypothermia in the rat.
Gayet, J; Ginefri-Gayet, M, 1992
)
0.61
"Treatment with betaxolol apparently inhibited the incidence of hypertensive lesions such as cardiac fibrosis, mesenteric vasculitis, proliferative and/or necrotic vasculitis and glomeruli showing collapse or vasculitis in the kidneys."( [Antihypertensive effects of betaxolol, a cardioselective beta-adrenoceptor antagonist, in stroke-prone spontaneously hypertensive rats (SHRSP)].
Fujimoto, M; Itoh, M; Niwa, M; Ozaki, M; Sekine, I; Uchida, S; Yamashita, K, 1990
)
0.91

Toxicity

Brinzolamide combined with Betaxolol has significant IOP lowering effect and few side effect for the Chinese people. The only serious adverse effect associated with betaxlol treatment was syncope, seen in 2 patients.

ExcerptReferenceRelevance
" Betaxolol was well tolerated by all patients with no adverse symptoms."( Betaxolol eye drops as a safe medication to lower intraocular pressure.
Brooks, AM; Gillies, WE; West, RH, 1987
)
2.63
"Thirty-one patients with poor control of elevated IOP were selected on the basis of coexistent respiratory disease which could be exacerbated by beta-antagonist administration and/or who had past adverse reactions to topical timolol."( Betaxolol eye drops. A clinical trial of safety and efficacy.
Goldberg, H; Goldberg, I, 1995
)
1.73
" The only serious adverse effect associated with betaxolol treatment was syncope, seen in 2 patients."( Safety and compatibility of betaxolol hydrochloride combined with diltiazem or nifedipine therapy in stable angina pectoris.
Friedman, R; Glasser, SP; Smith, LK; Talibi, T; Weir, EK, 1994
)
0.84
"While adverse effects are uncommon in patients who are otherwise fit and well, doctors should be aware of the implications of the systemic effects of these drugs, particularly the non-selective types, and particularly in the elderly."( The safety of topical beta-blockers in glaucoma treatment.
Goldberg, I, 1996
)
0.29
"In patients requiring more than one ocular hypotensive agent, the combination of betaxolol and pilocarpine in a single formulation appears to be an effective and relatively safe agent."( Ocular hypotensive efficacy and safety of a combined formulation of betaxolol and pilocarpine.
Robin, AL, 1996
)
0.76
" Very mild eye irritation, which was less than that of betaxolol hydrochloride, was observed particularly with BMO maleate, which is an excellent candidate for safe treatment of glaucoma."( Ocular-specific chemical delivery systems of betaxolol for safe local treatment of glaucoma.
Barros, MD; Bodor, N; Farag, HH; Prokai, L; Somogyi, G; Wu, WM, 1997
)
0.8
" The ocular adverse experience (AE) most frequently reported by patients was ocular burning and/or stinging, and the most frequently reported nonocular AEs were taste perversion, upper respiratory infection, and headache."( Comparison of the efficacy and safety of 2% dorzolamide and 0.5% betaxolol in the treatment of elevated intraocular pressure. Dorzolamide Comparison Study Group.
Adamsons, I; Laurence, J; Polis, A; Rusk, C; Sharpe, E,
)
0.37
" The side effect profile of unoprostone appears to be comparable to other established IOP-lowering agents."( A double-masked randomized comparison of the efficacy and safety of unoprostone with timolol and betaxolol in patients with primary open-angle glaucoma including pseudoexfoliation glaucoma or ocular hypertension. 6 month data.
Kapik, B; Mertz, B; Nordmann, JP; Schwenninger, C; Shams, N; Yannoulis, NC, 2002
)
0.53
"Data on office blood pressure (BP) and pulse rate as well as information on adverse effects were collected from 148 patients with mild and moderate hypertension during 12 week treatment with long acting lipophilic selective beta-adrenoreceptor blocker betaxolol (20 mg/day)."( [Confirmation of safety and therapeutic effect of betaxolol in the treatment of mild and moderate hypertension in general medical practice].
Ageev, FT; Belousov, IuB; Egorova, NA; Ivleva, AIu; Oleĭnikov, VE; Sidorenko, BA, 2005
)
0.76
"5 million adverse drug reaction (ADR) reports for 8620 drugs/biologics that are listed for 1191 Coding Symbols for Thesaurus of Adverse Reaction (COSTAR) terms of adverse effects."( Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
Benz, RD; Contrera, JF; Kruhlak, NL; Matthews, EJ; Weaver, JL, 2004
)
0.32
" The IOP and the side effect before and after the administration of the eyedrops were observed."( [Clinical investigation: the intraocular pressure-lowering efficacy and safety of brinzolamide combined with betaxolol].
Fang, M; Ge, J; Huang, S; Minbin, Y, 2005
)
0.54
"Brinzolamide combined with Betaxolol has significant IOP lowering effect and few side effect for the Chinese people."( [Clinical investigation: the intraocular pressure-lowering efficacy and safety of brinzolamide combined with betaxolol].
Fang, M; Ge, J; Huang, S; Minbin, Y, 2005
)
0.84
"Case/non-case analyses were performed in the FDA Adverse Events Reporting System (FAERS) using data from 2010-2020 to examine the reporting odds ratio (ROR) signal for OPP for all classes of antiglaucoma medications under multiple conditions: (i) comparison to all other drugs in FAERs, (ii) comparison to other antiglaucoma medications, (iii) comparison to vehicle/hydrating eye drops with cases of OPP and (iv) comparison to vehicle/hydrating eyedrops with and without cases of OPP to control for topical irritant and preservative effects."( Topical ophthalmic beta-blockers are associated with ocular pseudopemphigoid: A pharmacovigilance study of antiglaucoma medications utilising the FDA adverse event reporting system.
Jedlowski, MF; Jedlowski, PM, 2022
)
0.72

Pharmacokinetics

Betaxolol (Kerlon, 8) was found to exhibit an appropriate preclinical pharmacological and human pharmacokinetic profile. It could be used for the treatment of chronic cardiovascular diseases such as hypertension and angina.

ExcerptReferenceRelevance
" The pharmacokinetic behavior of betaxolol enantiomers in healthy male subjects is reported."( Human pharmacokinetics of betaxolol enantiomers.
Davis, PJ; Ludden, TM; Stagni, G, 1991
)
0.86
" Its pharmacokinetic properties of most interest include high bioavailability after oral administration, and a long elimination half-life."( Betaxolol. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in hypertension.
Beresford, R; Heel, RC, 1986
)
1.71
"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
)
0.49
" 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
)
1.44
" This method was used to evaluate the pharmacokinetic profile of the betaxolol enantiomers in three subjects following one single oral dose (20 mg) of racemic betaxolol."( Determination of betaxolol enantiomers by high-performance liquid chromatography. Application to pharmacokinetic studies.
Darmon, A; Thenot, JP, 1986
)
0.85
" 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
)
0.8
" The half-life for betaxolol was 24."( Observation on the efficacy and pharmacokinetics of betaxolol (SL 75212), a cardioselective beta-adrenoceptor blocking drug.
Balnave, K; Harron, DW; Leahey, WJ; Neill, JD; Russell, CJ; Shanks, RG; Wilson, R, 1981
)
0.84
" Its pharmacokinetic profile obtained following administration of a 20 mg oral dose was characterized by a half-life of 22 h and a bioavailability of 85%."( Determination of betaxolol, a new beta-blocker, by gas chromatography mass spectrometry: application to pharmacokinetic studies.
Allen, J; Fraisse, J; Hermann, P; Morselli, PL; Thenot, JP, 1984
)
0.61
" 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
" 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
"Volume of distribution is one of the most important pharmacokinetic properties of a drug candidate."( Volume of Distribution in Drug Design.
Beaumont, K; Di, L; Maurer, TS; Smith, DA, 2015
)
0.42
" Pharmacokinetic parameters were obtained using a compartmental fitting approach, and the estimated clearance, volume of distribution, and half-life values were the following: atenolol (6."( Ocular Intracameral Pharmacokinetics for a Cocktail of Timolol, Betaxolol, and Atenolol in Rabbits.
Del Amo, EM; Fayyaz, A; Gardner, I; Heikkinen, EM; Jamei, M; Ranta, VP; Reinisalo, M; Ricci, GD; Toropainen, E; Urtti, A; Vellonen, KS, 2020
)
0.8
"Ocular bioavailability after eye drops administration is an important, but rarely determined, pharmacokinetic parameter."( Topical ocular pharmacokinetics and bioavailability for a cocktail of atenolol, timolol and betaxolol in rabbits.
Del Amo, EM; Fayyaz, A; Gardner, I; Jamei, M; Puranen, J; Ranta, VP; Ruponen, M; Toropainen, E; Urtti, A; Valtari, A; Vellonen, KS, 2020
)
0.78

Compound-Compound Interactions

Brinzolamide combined with Betaxolol has significant IOP lowering effect and few side effect for the Chinese people.

ExcerptReferenceRelevance
"To evaluate the intraocular pressure (IOP) lowering efficacy and safety of Brinzolamide combined with Betaxolol for the Chinese glaucomatous patients."( [Clinical investigation: the intraocular pressure-lowering efficacy and safety of brinzolamide combined with betaxolol].
Fang, M; Ge, J; Huang, S; Minbin, Y, 2005
)
0.76
"Brinzolamide combined with Betaxolol has significant IOP lowering effect and few side effect for the Chinese people."( [Clinical investigation: the intraocular pressure-lowering efficacy and safety of brinzolamide combined with betaxolol].
Fang, M; Ge, J; Huang, S; Minbin, Y, 2005
)
0.84

Bioavailability

Betaxolol (Kerlon, 8) was found to exhibit an appropriate preclinical pharmacological and human pharmacokinetic profile for the treatment of chronic cardiovascular diseases such as hypertension and angina.

ExcerptReferenceRelevance
" Likewise, after the oral dose, there were no differences in the maximum concentration, time of maximum concentration, bioavailability, or apparent absorption rate constant (41."( Human pharmacokinetics of betaxolol enantiomers.
Davis, PJ; Ludden, TM; Stagni, G, 1991
)
0.58
" Its pharmacokinetic properties of most interest include high bioavailability after oral administration, and a long elimination half-life."( Betaxolol. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in hypertension.
Beresford, R; Heel, RC, 1986
)
1.71
" 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
)
0.49
" 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
)
1.44
"The absolute bioavailability and dose proportionality of betaxolol [(+/-)-1-(p-[2-cyclopropylmethoxy)ethyl]phenoxy]-3- (isopropylamino)-2-propanol hydrochloride], a cardioselective beta-adrenergic antagonist effective in the treatment of angina and hypertension, was studied in 12 healthy male subjects using a four-way crossover Latin Square design."( Absolute bioavailability and dose proportionality of betaxolol in normal healthy subjects.
Boyle, DA; Clementi, WA; Crawford, MH; Gieseker, D; Kennedy, GT; Ludden, LK; Ludden, TM, 1988
)
0.77
" 4 The absolute bioavailability of betaxolol was 89 +/- 5%."( Blood concentrations and pharmacodynamic effects of betaxolol (SL 75212) a new beta-adrenoceptor antagonist after oral and intravenous administration.
Bianchetti, G; Kilborn, JR; Morselli, PL; Turner, P; Warrington, SJ, 1980
)
0.79
" Its pharmacokinetic profile obtained following administration of a 20 mg oral dose was characterized by a half-life of 22 h and a bioavailability of 85%."( Determination of betaxolol, a new beta-blocker, by gas chromatography mass spectrometry: application to pharmacokinetic studies.
Allen, J; Fraisse, J; Hermann, P; Morselli, PL; Thenot, JP, 1984
)
0.61
"The kinetic and clinical profile of betaxolol--a beta 1-selective blocker with 80% to 90% bioavailability and a 16 to 20 hr t1/2--were studied in ten children aged 5 to 13 yr with chronic renal hypertension and mild to severe renal failure."( Betaxolol kinetics in hypertensive children with normal and abnormal renal function.
Assael, BM; Bianchetti, G; Claris-Appiani, A; Edefonti, A; Gomeni, R; Morselli, PL; Palminteri, R, 1984
)
1.99
" The systemic bioavailability ranged from 61% for atenolol to 100% for timolol."( Systemic absorption pathways of topically applied beta adrenergic antagonists in the pigmented rabbit.
Kompella, UB; Lee, VH; Lee, YH, 1993
)
0.29
"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
"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
"Poor bioavailability and therapeutic response of conventional therapy due to many pre-corneal constraints necessitate the development of novel controlled and sustained ocular drug delivery to become a standard one in modern pharmaceutical era."( Long acting betaxolol ocular inserts based on polymer composite.
Gevariya, HB; Patel, JK, 2013
)
0.77
" In vivo pharmacokinetics and pharmacodynamics studies indicated that the BH-HG formulation resulted in an improved bioavailability and a significantly lower intraocular pressure (IOP)."( Preparation, pharmacokinetics and pharmacodynamics of ophthalmic thermosensitive in situ hydrogel of betaxolol hydrochloride.
Fu, L; Hua, H; Huang, W; Liu, T; Ma, X; Tang, Y; Yang, Y; Zhang, N; Zhao, Y, 2016
)
0.65
" Unfortunately, effective treatments are limited by poor bioavailability of antiglaucoma medicine due to short residence time on the preocular surface."( Controlled drug delivery for glaucoma therapy using montmorillonite/Eudragit microspheres as an ion-exchange carrier.
Chen, Y; Duan, H; Hou, D; Li, J; Lv, Z; Tao, Q; Tian, S; Yang, F; Zhao, Y; Zhou, Q, 2018
)
0.48
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
"Ocular bioavailability after eye drops administration is an important, but rarely determined, pharmacokinetic parameter."( Topical ocular pharmacokinetics and bioavailability for a cocktail of atenolol, timolol and betaxolol in rabbits.
Del Amo, EM; Fayyaz, A; Gardner, I; Jamei, M; Puranen, J; Ranta, VP; Ruponen, M; Toropainen, E; Urtti, A; Valtari, A; Vellonen, KS, 2020
)
0.78
" Upon instillation of the betaxolol-loaded niosomal gel into rabbits' eyes, a prolonged intraocular pressure reduction and significant enhancement in the relative bioavailability of betaxolol (280 and 254."( Betaxolol-loaded niosomes integrated within pH-sensitive in situ forming gel for management of glaucoma.
Allam, A; El Badry, M; Eleraky, NE; Elsabahy, M, 2021
)
2.36
" Topical application of conventional eye drops results in substantial drug loss due to rapid tear turnover, with poor drug bioavailability being a major challenge for efficient glaucoma treatment."( Critical Evaluation of Multifunctional Betaxolol Hydrochloride Nanoformulations for Effective Sustained Intraocular Pressure Reduction.
Han, X; Hou, D; Hu, J; Ke, Y; Li, H; Li, W; Lin, H; Liu, H; Rupenthal, ID; Yang, F; Ye, J; Zhao, Y, 2022
)
0.99

Dosage Studied

The long acting highly selective beta1-blocker betaxolol in an adequate dosage is not inferior to carvedilol in terms of exercise tolerance, safety and effects on left ventricular function. Demecarium bromide in combination with a topical corticosteroid may be preferable to betaxlol in preventing PCAG in dogs.

ExcerptRelevanceReference
" Twenty-four-hour ambulatory HR recording demonstrated that this difference existed for the last 6 h of the dosage cycle."( Twenty-four-hour beta-blockade in stable angina pectoris: a study of atenolol and betaxolol.
Dargie, HJ; Findlay, IN; McLenachan, JM; Wilson, JT, 1992
)
0.51
"This study determined the dose-response relationship among three doses of betaxolol compared with placebo in patients with mild-to-moderate hypertension."( Dose-dependent effects of betaxolol in hypertension: a double-blind, multicenter study.
Goyle, KK; Herman, TS; Hogan, LB; Rofman, BA; Ruoff, GE; Williams, RL, 1992
)
0.81
" This new pharmaceutical dosage form produces very interesting therapeutic effects with much lower drug concentrations than that commonly used in aqueous commercial eye drops; thus, systemic and local side effects could be minimized."( [Nanocapsules of beta-blocking agents: a new drug carrier in ophthalmology. Application to medical treatment of glaucoma in rabbits].
Hoffman, M; Maincent, P; Marchal-Heussler, L; Sirbat, D, 1991
)
0.28
"The dose-response curves of betaxolol and atenolol were compared in 140 patients with mild to moderate essential hypertension."( Population dose versus response of betaxolol and atenolol: a comparison of potency and variability.
Sambol, NC; Sheiner, LB, 1991
)
0.85
"The isoproterenol dose-response curve was used to assess quantitatively the degree of systemic beta-adrenoceptor blockade induced by metipranolol (Bétanol) and betaxolol (Bétoptic) eye drops."( [Comparison in healthy volunteers of the systemic beta adrenergic receptor blockade by beta blockader eye drops].
de Dieuleveult, C; Pinaud, M; Queinnec, MC; Souron, R, 1989
)
0.47
"In a double-masked crossover study, the dose-response relationship for aqueous flow was determined for four concentrations of betaxolol hydrochloride and levobunolol hydrochloride in 19 normal subjects."( Comparison of a noncardioselective beta-adrenoceptor blocker and a cardioselective blocker in reducing aqueous flow in humans.
Brubaker, RF; Gaul, GR; Will, NJ, 1989
)
0.48
" These factors would be expected to provide a more consistent therapeutic response and more dependable dosage adjustment."( Steady-state fluctuation and variability of betaxolol and atenolol plasma levels.
Andersen, RL; Haack, DG; Kunka, RL; Wong, YY, 1989
)
0.54
" 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
)
0.66
" It has a narrow dose-response range, which obviates the need for dose titration, with 10 to 20 mg once daily being the usual dosage."( Betaxolol. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in hypertension.
Beresford, R; Heel, RC, 1986
)
1.71
" 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 between the 3rd and 14th day after the onset of AMI with either a single oral dosage of 20 mg betaxolol or placebo."( Effects of betaxolol on heart rate in patients with a recent transmural myocardial infarction.
Coupez, R; De Geest, H; Ector, H; Kesteloot, H; Yang, XS, 1987
)
0.87
"Glaucoma is described, and the chemistry, pharmacology, pharmacokinetics, clinical efficacy, adverse effects, and dosage and administration of betaxolol and levobunolol in comparison with timolol are reviewed."( Comparison of ophthalmic beta-blocking agents.
Lesar, TS, 1987
)
0.47
" The pharmacokinetics were studied during dosing and in the washout period."( Pharmacokinetics of the new beta-adrenoceptor blocking agent betaxolol (SL 75212) in man after repeated oral administration.
Bianchetti, G; Blatrix, C; Gomeni, R; Kilborn, JR; Larribaud, J; Lücker, PW; Morselli, PL; Thebault, JJ; Trocherie, S, 1980
)
0.5
"Betaxolol, a new beta-receptor blocking drug administered as a single dosage of 40 mg given orally, causes a maximal reduction of heart rate at rest of 30%, during a submaximal exercise of 28% and at rest after exercise of 33%."( Effect of betaxolol on heart rate at rest and during exercise.
Coupez-Lopinot, R; Kesteloot, H; Missotten, A; Sluyts, R, 1982
)
2.11
" 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
)
0.5
"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
" Its cardioselectivity, ease of dosing and complete absence of side effects makes BTX an attractive choice as antianginal agent for chronic use."( Dose related efficacy of betaxolol in combination with nitroglycerin in patients with angina pectoris: a double blind cross-over study.
Kesteloot, H; Stroobandt, R, 1984
)
0.57
"5% Sterile Ophthalmic Solution dosage form."( Ion exchange resins for ophthalmic delivery.
Ali, Y; Gan, O; Hancock, S; Jani, R; Rodstrom, R, 1994
)
0.29
"01) twelve hours after dosing at each observation times."( [Clinical evaluation of betaxolol in ophthalmic suspension with or without preservative agent in patients with glaucoma or ocular hypertension].
Demailly, P; Denis, P; Saraux, H, 1993
)
0.59
"), the heart rate dose-response curves to isoprenaline were shifted to the right of those determined in matched groups of vehicle-pretreated animals."( Celiprolol: agonist and antagonist effects at cardiac beta 1- and vascular beta 2-adrenoceptors determined under in vivo conditions in the rat.
Alda, O; Alvarez-Guerra, M; Garay, RP, 1997
)
0.3
" In patients under long-term therapy, the periocular tissue can accumulate a greater quantity of beta-antagonist than is present in a daily dosage of applied eyedrops, manyfold higher than the maximal intraocular concentration."( Periocular accumulation of timolol and betaxolol in glaucoma patients under long-term therapy.
Frenzel, H; Khuu, HD; Lam, KW; Sponsel, WE; Terry, S, 1999
)
0.57
"Phenylephrine dose-dependently contracted ciliary artery smooth muscle, and bunazosin (1 microM) shifted this dose-response curve to the right."( Effects of beta antagonists on mechanical properties in rabbit ciliary artery.
Hayashi, E; Hayashi-Morimoto, R; Ishikawa, H; Sato, Y; Yoshitomi, T, 1999
)
0.3
" Although DB/GB and betaxolol equally delayed or prevented the onset of glaucoma in the second eye, a less frequent dosing schedule for DB/GB suggests demecarium bromide in combination with a topical corticosteroid may be preferable to betaxolol in preventing PCAG in dogs."( The efficacy of topical prophylactic antiglaucoma therapy in primary closed angle glaucoma in dogs: a multicenter clinical trial.
Herrmann, MK; Miller, PE; Schmidt, GM; Swanson, JF; Vainisi, SJ,
)
0.45
" Among the 8 subjects in whom doxazosin dosage was increased to the maximum of 4 mg, the mean blood pressure achieved at 4 mg did not differ from that achieved at 2 mg (136/87 v 136/88 mm Hg)."( Low-dose alpha/beta blockade in the treatment of essential hypertension.
Gerber, LM; Mann, SJ, 2001
)
0.31
"Our aim was to study the concentration of betaxolol in plasma after its topical ocular use during the normal 12 hr dosing interval."( Plasma concentration of topically applied betaxolol in elderly glaucoma patients.
Huupponen, R; Pyykkö, K; Vainio-Jylhä, E; Vuori, ML, 2001
)
0.84
" The dose-response curves of these compounds were not significantly different."( Vasorelaxant effects of racemic betaxolol and its R- and S- isomers on bovine retinal vessels.
DeSantis, L; Kulkarni, PS, 2001
)
0.59
" Rats were dosed (IP) with vehicle or levobetaxolol (10 and 20 mg kg(-1)) 48, 24 and 0 hr prior to exposure for 6 hr to fluorescent blue light."( Levobetaxolol-induced Up-regulation of retinal bFGF and CNTF mRNAs and preservation of retinal function against a photic-induced retinopathy.
Agarwal, N; Collier, RJ; Kapin, MA; Krishnamoorthy, RR; Krueger, S; Landers, R; Martin, E; Wen, R, 2002
)
1.14
" Betaxolol compressed the dose-response curve of glutamate."( Effects of beta-adrenergic blockers on glutamate-induced calcium signals in adult mouse retinal ganglion cells.
Gross, RL; Wu, SM; Zhang, J, 2003
)
1.23
"The long acting highly selective beta1-blocker betaxolol in an adequate dosage is not inferior to carvedilol in terms of exercise tolerance, safety and effects on left ventricular function."( Betaxolol is equivalent to carvedilol in patients with heart failure NYHA II or III: result of a randomized multicenter trial (BETACAR Trial).
Chochola, J; Figulla, HR; Fridl, P; Kalmbach, C; Krzeminska-Pakula, M; Wrabec, K, 2006
)
2.03
"A randomized, controlled trial was conducted in an outpatient setting to examine the effect of beta-blocker dosing frequency on patient compliance, clinical outcome, and health-related quality of life in patients with stable angina pectoris."( Compliance, clinical outcome, and quality of life of patients with stable angina pectoris receiving once-daily betaxolol versus twice daily metoprolol: a randomized controlled trial.
Kardas, P, 2007
)
0.55
"5%, both dosed twice daily."( Efficacy of brinzolamide and levobetaxolol in pediatric glaucomas: a randomized clinical trial.
Bergamini, MV; Dickerson, JE; Gross, RD; Hua, SY; Landry, TA; Roarty, JD; Robin, AL; Scheib, SA; Scott, H; Vijaya, L; Whitson, JT; Woodside, AM, 2008
)
0.63
" 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
" It is a major determinant of half-life and dosing frequency of a drug."( Volume of Distribution in Drug Design.
Beaumont, K; Di, L; Maurer, TS; Smith, DA, 2015
)
0.42
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (3)

RoleDescription
beta-adrenergic antagonistAn 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.
antihypertensive agentAny drug used in the treatment of acute or chronic vascular hypertension regardless of pharmacological mechanism.
sympatholytic agentAny compound which inhibits the postganglionic functioning of the sympathetic nervous system (SNS).
[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]

Drug Classes (1)

ClassDescription
propanolamine
[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
Betaxolol Action Pathway478

Protein Targets (32)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency37.90830.01237.983543.2770AID1645841
EWS/FLI fusion proteinHomo sapiens (human)Potency18.65480.001310.157742.8575AID1259255
cytochrome P450 2D6Homo sapiens (human)Potency18.99910.00108.379861.1304AID1645840
arylsulfatase AHomo sapiens (human)Potency37.93301.069113.955137.9330AID720538
hexokinase-4 isoform 1Homo sapiens (human)Potency19.95262.511913.800328.1838AID743207
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency29.01450.000323.4451159.6830AID743065; AID743067
glucokinase regulatory proteinHomo sapiens (human)Potency19.95262.511913.800328.1838AID743207
lamin isoform A-delta10Homo sapiens (human)Potency35.48130.891312.067628.1838AID1487
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Bile salt export pumpHomo sapiens (human)IC50 (µMol)1,000.00000.11007.190310.0000AID1449628
Beta-1 adrenergic receptorHomo sapiens (human)IC50 (µMol)0.03710.00021.46819.0000AID42028
Cytochrome P450 2D6Homo sapiens (human)IC50 (µMol)66.00000.00002.015110.0000AID241889
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Beta-1 adrenergic receptor Cavia porcellus (domestic guinea pig)Kd0.02080.00000.53588.3176AID39943; AID42216
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Kd0.10470.00020.56294.4668AID40869
Beta-1 adrenergic receptorHomo sapiens (human)Kd0.00160.00010.803910.0000AID1232324
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Kd0.10470.00020.56294.4668AID40869
Beta-1 adrenergic receptorRattus norvegicus (Norway rat)Kd0.06440.00140.06010.3910AID1318766; AID40420
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Kd0.10470.00020.56294.4668AID40869
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Kd0.10470.00020.56294.4668AID40869
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Kd0.10470.00012.29338.5114AID40869
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Kd0.10470.00020.56294.4668AID40869
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Kd0.10470.00020.56294.4668AID40869
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Kd0.10470.00020.56294.4668AID40869
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Kd0.10470.00020.56294.4668AID40869
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Kd0.10470.00020.56294.4668AID40869
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Kd0.10470.00020.56294.4668AID40869
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Kd0.10470.00020.56294.4668AID40869
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Kd0.10470.00020.56294.4668AID40869
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Kd0.10470.00020.56294.4668AID40869
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Kd0.10470.00020.56294.4668AID40869
Beta-2 adrenergic receptor Bos taurus (cattle)Kd186.21000.00061.47759.1200AID40694
Beta-2 adrenergic receptorCavia porcellus (domestic guinea pig)Kd0.10470.00020.54774.4668AID40869; AID40870
GABA theta subunitRattus norvegicus (Norway rat)Kd0.10470.00020.56294.4668AID40869
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Kd0.10470.00020.56294.4668AID40869
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (56)

Processvia Protein(s)Taxonomy
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)
positive regulation of heart rate by epinephrine-norepinephrineBeta-1 adrenergic receptorHomo sapiens (human)
positive regulation of the force of heart contraction by epinephrine-norepinephrineBeta-1 adrenergic receptorHomo sapiens (human)
diet induced thermogenesisBeta-1 adrenergic receptorHomo sapiens (human)
response to coldBeta-1 adrenergic receptorHomo sapiens (human)
heat generationBeta-1 adrenergic receptorHomo sapiens (human)
negative regulation of multicellular organism growthBeta-1 adrenergic receptorHomo sapiens (human)
fear responseBeta-1 adrenergic receptorHomo sapiens (human)
regulation of circadian sleep/wake cycle, sleepBeta-1 adrenergic receptorHomo sapiens (human)
brown fat cell differentiationBeta-1 adrenergic receptorHomo sapiens (human)
regulation of postsynaptic membrane potentialBeta-1 adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayBeta-1 adrenergic receptorHomo sapiens (human)
positive regulation of cold-induced thermogenesisBeta-1 adrenergic receptorHomo sapiens (human)
norepinephrine-epinephrine-mediated vasodilation involved in regulation of systemic arterial blood pressureBeta-1 adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeBeta-1 adrenergic receptorHomo sapiens (human)
xenobiotic metabolic processCytochrome P450 2D6Homo sapiens (human)
steroid metabolic processCytochrome P450 2D6Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2D6Homo sapiens (human)
estrogen metabolic processCytochrome P450 2D6Homo sapiens (human)
coumarin metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid catabolic processCytochrome P450 2D6Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2D6Homo sapiens (human)
isoquinoline alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2D6Homo sapiens (human)
retinol metabolic processCytochrome P450 2D6Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2D6Homo sapiens (human)
negative regulation of bindingCytochrome P450 2D6Homo sapiens (human)
oxidative demethylationCytochrome P450 2D6Homo sapiens (human)
negative regulation of cellular organofluorine metabolic processCytochrome P450 2D6Homo sapiens (human)
arachidonic acid metabolic processCytochrome P450 2D6Homo sapiens (human)
receptor-mediated endocytosisBeta-2 adrenergic receptor Bos taurus (cattle)
regulation of smooth muscle contractionBeta-2 adrenergic receptor Bos taurus (cattle)
positive regulation of MAPK cascadeBeta-2 adrenergic receptor Bos taurus (cattle)
negative regulation of G protein-coupled receptor signaling pathwayBeta-2 adrenergic receptor Bos taurus (cattle)
adenylate cyclase-activating adrenergic receptor signaling pathwayBeta-2 adrenergic receptor Bos taurus (cattle)
positive regulation of autophagosome maturationBeta-2 adrenergic receptor Bos taurus (cattle)
positive regulation of lipophagyBeta-2 adrenergic receptor Bos taurus (cattle)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (25)

Processvia Protein(s)Taxonomy
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)
beta-adrenergic receptor activityBeta-1 adrenergic receptorHomo sapiens (human)
beta1-adrenergic receptor activityBeta-1 adrenergic receptorHomo sapiens (human)
protein bindingBeta-1 adrenergic receptorHomo sapiens (human)
PDZ domain bindingBeta-1 adrenergic receptorHomo sapiens (human)
alpha-2A adrenergic receptor bindingBeta-1 adrenergic receptorHomo sapiens (human)
protein heterodimerization activityBeta-1 adrenergic receptorHomo sapiens (human)
G protein-coupled neurotransmitter receptor activity involved in regulation of postsynaptic membrane potentialBeta-1 adrenergic receptorHomo sapiens (human)
monooxygenase activityCytochrome P450 2D6Homo sapiens (human)
iron ion bindingCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activityCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2D6Homo sapiens (human)
heme bindingCytochrome P450 2D6Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
beta2-adrenergic receptor activityBeta-2 adrenergic receptor Bos taurus (cattle)
protein homodimerization activityBeta-2 adrenergic receptor Bos taurus (cattle)
norepinephrine bindingBeta-2 adrenergic receptor Bos taurus (cattle)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (22)

Processvia Protein(s)Taxonomy
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)
early endosomeBeta-1 adrenergic receptorHomo sapiens (human)
plasma membraneBeta-1 adrenergic receptorHomo sapiens (human)
Schaffer collateral - CA1 synapseBeta-1 adrenergic receptorHomo sapiens (human)
neuronal dense core vesicleBeta-1 adrenergic receptorHomo sapiens (human)
plasma membraneBeta-1 adrenergic receptorHomo sapiens (human)
mitochondrionCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulumCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2D6Homo sapiens (human)
cytoplasmCytochrome P450 2D6Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2D6Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
early endosomeBeta-2 adrenergic receptor Bos taurus (cattle)
Golgi apparatusBeta-2 adrenergic receptor Bos taurus (cattle)
receptor complexBeta-2 adrenergic receptor Bos taurus (cattle)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (134)

Assay IDTitleYearJournalArticle
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings 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.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The 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.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID588214FDA HLAED, liver enzyme composite activity2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
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.
AID540209Volume of distribution at steady state in human after iv administration2008Drug 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.
AID1232324Antagonist activity against beta-1 adrenergic receptor (unknown origin)2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Volume of Distribution in Drug Design.
AID1318767Half life in human2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
The "Cyclopropyl Fragment" is a Versatile Player that Frequently Appears in Preclinical/Clinical Drug Molecules.
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1232311Unbound volume of distribution at steady state in human2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Volume of Distribution in Drug Design.
AID190411Antihypertensive activity expressed as percentage of base-line systolic blood pressure of base-line values in spontaneously hypertensive rats (SHR) was reported after 2 hr1987Journal 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.
AID444057Fraction escaping hepatic elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID444054Oral bioavailability in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID588217FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID540213Half life in human after iv administration2008Drug 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.
AID42216Compound was tested for the biological activity at the Beta-1 adrenergic receptor1992Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25
Computer-aided mapping of the beta-adrenoceptor. 1. Explanation for effect of para substitution on blocking activity at the beta-1-adrenoceptor.
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID540211Fraction unbound in human after iv administration2008Drug 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.
AID40869In 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-alpha1983Journal 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.
AID588215FDA HLAED, alkaline phosphatase increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID40694Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)1985Journal of medicinal chemistry, Sep, Volume: 28, Issue:9
Quantitative evaluation of the beta 2-adrenoceptor affinity of phenoxypropanolamines and phenylethanolamines.
AID425653Renal clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID540212Mean residence time in human after iv administration2008Drug 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.
AID42218In vitro beta-1 adrenergic receptor activity was determined via inhibition of the positive chronotropic actions of isoproterenol in isolated guinea pig atrial preparations1983Journal 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.
AID29359Ionization constant (pKa)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID425652Total body clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID40870In vitro inhibitory activity against beta-2 adrenergic receptor was measured by the inhibition of isoproterenol-induced relaxation of PGF2-alpha contracted guinea pig trachea1986Journal 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.
AID241889Inhibitory activity against recombinant human Cytochrome P450 2D6 (CYP2D6) after incubated for 45 minutes2005Bioorganic & medicinal chemistry letters, Sep-01, Volume: 15, Issue:17
A 3D-QSAR model for CYP2D6 inhibition in the aryloxypropanolamine series.
AID781328pKa (acid-base dissociation constant) as determined by Luan ref: Pharm. Res. 20052014Pharmaceutical research, Apr, Volume: 31, Issue:4
Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds.
AID444052Hepatic clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID40693Ratio between the IC50 values of beta-2 of calf lung and beta-1 receptor of dog heart1982Journal of medicinal chemistry, Aug, Volume: 25, Issue:8
Use of (S)-(trifloxymethyl)oxirane in the synthesis of a chiral beta-adrenoceptor antagonist, (R)- and (S)-9-[[3-(tert-butylamino)-2-hydroxypropyl]oximino]fluorene.
AID588219FDA HLAED, gamma-glutamyl transferase (GGT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID40686Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA)1985Journal of medicinal chemistry, Sep, Volume: 28, Issue:9
Quantitative evaluation of the beta 2-adrenoceptor affinity of phenoxypropanolamines and phenylethanolamines.
AID588216FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID29811Oral bioavailability in human2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID7783Unbound fraction (plasma)2004Journal 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.
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.
AID567091Drug absorption in human assessed as human intestinal absorption rate2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Prediction of drug intestinal absorption by new linear and non-linear QSPR.
AID588218FDA HLAED, lactate dehydrogenase (LDH) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID444056Fraction escaping gut-wall elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID190412Antihypertensive activity expressed as percentage of base-line systolic blood pressure of base-line values in spontaneously hypertensive rats (SHR) was reported after 4 hr1987Journal 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.
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1232308Distribution coefficient, log D of the compound2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Volume of Distribution in Drug Design.
AID26304Partition coefficient (logD6.5)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID8002Observed volume of distribution2004Journal 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.
AID40689Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-2 adrenergic receptor in calf lung membranes.1982Journal of medicinal chemistry, Aug, Volume: 25, Issue:8
Use of (S)-(trifloxymethyl)oxirane in the synthesis of a chiral beta-adrenoceptor antagonist, (R)- and (S)-9-[[3-(tert-butylamino)-2-hydroxypropyl]oximino]fluorene.
AID40537Selectivity for beta-1 adrenergic receptor1988Journal of medicinal chemistry, Nov, Volume: 31, Issue:11
Modeling of beta-adrenoceptors based on molecular electrostatic potential studies of agonists and antagonists.
AID230147The cardioselectivity ratio was obtained by taking the antilog of (pA2(beta-1)-pA2(beta2))1983Journal 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.
AID444053Renal clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID41487Selectivity towards beta-2 adrenergic receptor; Nonselective towards beta-2 adrenergic receptor1988Journal of medicinal chemistry, Nov, Volume: 31, Issue:11
Modeling of beta-adrenoceptors based on molecular electrostatic potential studies of agonists and antagonists.
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID444051Total clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID540210Clearance in human after iv administration2008Drug 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.
AID230146The cardioselectivity ratio was obtained by taking the antilog (pA2 beta1-pA2 beta2)1986Journal 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.
AID190410Antihypertensive activity expressed as percentage of base-line systolic blood pressure of base-line values in spontaneously hypertensive rats (SHR) was reported after 24 hr1987Journal 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.
AID588220Literature-mined public compounds from Kruhlak et al phospholipidosis modelling dataset2008Toxicology mechanisms and methods, , Volume: 18, Issue:2-3
Development of a phospholipidosis database and predictive quantitative structure-activity relationship (QSAR) models.
AID1318766Antagonist activity at rat beta1 adrenoceptor2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
The "Cyclopropyl Fragment" is a Versatile Player that Frequently Appears in Preclinical/Clinical Drug Molecules.
AID165494compound was evaluated for ocular hypotensive effects (intraocular pressure, IOP) by administering 0.5% of the drug twice daily1997Journal of medicinal chemistry, Aug-29, Volume: 40, Issue:18
New approaches to antiglaucoma therapy.
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID41890Tested for intrinsic sympathomimetic activity (ISA); Pure antagonist1988Journal of medicinal chemistry, Nov, Volume: 31, Issue:11
Modeling of beta-adrenoceptors based on molecular electrostatic potential studies of agonists and antagonists.
AID1232310Volume of distribution at steady state in human2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Volume of Distribution in Drug Design.
AID1232313Elimination half life in human2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Volume of Distribution in Drug Design.
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1232314Unbound intrinsic clearance in human2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Volume of Distribution in Drug Design.
AID444055Fraction absorbed in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
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.
AID42028Compound was tested for inhibition of [3H]dihydroalprenolol radioligand binding to Beta-1 adrenergic receptor in dog heart1982Journal of medicinal chemistry, Aug, Volume: 25, Issue:8
Use of (S)-(trifloxymethyl)oxirane in the synthesis of a chiral beta-adrenoceptor antagonist, (R)- and (S)-9-[[3-(tert-butylamino)-2-hydroxypropyl]oximino]fluorene.
AID1232312Clearance in human2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Volume of Distribution in Drug Design.
AID603953In-vivo 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.
AID39943In vitro inhibitory activity against beta-1 adrenergic receptor measured by inhibition of positive chronotropic effect of isoproterenolin in isolated guinea pig atria1986Journal 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.
AID444058Volume of distribution at steady state in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID444050Fraction unbound in human plasma2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID26362Ionization constant (pKa)2004Journal 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.
AID22293Delta logD (logD6.5 - logD7.4)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID40420Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria1987Journal 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.
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings 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.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
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.
AID1346260Human beta1-adrenoceptor (Adrenoceptors)1999European journal of pharmacology, Feb-19, Volume: 367, Issue:2-3
LK 204-545, a highly selective beta1-adrenoceptor antagonist at human beta-adrenoceptors.
AID1346250Human beta2-adrenoceptor (Adrenoceptors)1999European journal of pharmacology, Feb-19, Volume: 367, Issue:2-3
LK 204-545, a highly selective beta1-adrenoceptor antagonist at human beta-adrenoceptors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (672)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990184 (27.38)18.7374
1990's226 (33.63)18.2507
2000's168 (25.00)29.6817
2010's63 (9.38)24.3611
2020's31 (4.61)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 64.73

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.

MetricThis Compound (vs All)
Research Demand Index64.73 (24.57)
Research Supply Index6.85 (2.92)
Research Growth Index4.45 (4.65)
Search Engine Demand Index112.90 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (64.73)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials227 (31.66%)5.53%
Reviews29 (4.04%)6.00%
Case Studies46 (6.42%)4.05%
Observational1 (0.14%)0.25%
Other414 (57.74%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (8)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
N-of-1 Trials for Deprescribing Beta-blockers in HFpEF [NCT04767061]Phase 49 participants (Actual)Interventional2021-04-01Completed
Acute Management of Paroxysmal Atrial Fibrillation With Beta Blockers Plus Intravenous Flecainide: a Real-world Chios Registry (BETAFLEC-CHIOS) [NCT04991896]81 participants (Actual)Observational [Patient Registry]2020-01-01Completed
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)Observational2020-01-19Completed
A Multicenter, Randomized, Open-label, Positive-controlled, Parallel-group Clinical Trial of Levobetaxolol Hydrochloride Eye Drops in Patients With Primary Open-angle Glaucoma or Ocular Hypertension [NCT02617459]Phase 3366 participants (Actual)Interventional2019-01-04Completed
N-of-1 Trials for Deprescribing Beta-blockers in HFpEF [NCT04757584]Phase 49 participants (Actual)Interventional2021-04-01Completed
[NCT00000132]Phase 30 participants Interventional1992-10-31Active, not recruiting
Safety and Efficacy Study of BETOPTIC S 0.25% and Timolol Gel-forming Solution 0.25% and 0.5% in Pediatric Patients With Glaucoma or Ocular Hypertension [NCT00061542]Phase 3105 participants (Actual)Interventional2003-01-31Completed
Topical Betaxolol for the Prevention of Retinopathy of Prematurity [NCT01660620]Phase 123 participants (Actual)Interventional2011-04-30Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT04767061 (10) [back to overview]Change in Exercise Capacity When on Beta-blocker Versus When Off Beta-blocker, as Measured by Peak Oxygen Consumption (VO2) During Cardiopulmonary Exercise Test (CPET)
NCT04767061 (10) [back to overview]Change in Lower Extremity Function When on Beta-blocker Versus When Off Beta-blocker, as Measured by the Balance Portion of a Modified Version of the Short Physical Performance Battery.
NCT04767061 (10) [back to overview]Change in Lower Extremity Function When on Beta-blocker Versus When Off Beta-blocker, as Measured by the Chair Rise Portion of a Modified Version of the Short Physical Performance Battery.
NCT04767061 (10) [back to overview]Change in Lower Extremity Function When on Beta-blocker Versus When Off Beta-blocker, as Measured by the Gait Speed Portion of a Modified Version of the Short Physical Performance Battery.
NCT04767061 (10) [back to overview]Change in Patient-reported Cognitive Function When on Beta-blocker Versus When Off Beta-blocker, as Measured by Patient-Reported Outcome Measurement Information System-Short Form 6a (PROMIS SF-6a)
NCT04767061 (10) [back to overview]Change in Patient-reported Health Status When on Beta-blocker Versus When Off Beta-blocker, as Measured by Kansas City Cardiomyopathy Questionnaire (KCCQ-12)
NCT04767061 (10) [back to overview]Change in Patient-reported Health When on Beta-blocker Versus When Off Beta-blocker, as Measured by the EuroQol-5D Visual Analogue System (EQ-5D VAS)
NCT04767061 (10) [back to overview]Change in Patient-reported Sexual Function When on Beta-blocker Versus When Off Beta-blocker, as Measured by Patient-Reported Outcome Measurement Information System-Sexual Function (PROMIS-Sexual Function)
NCT04767061 (10) [back to overview]Change in Physical Activity When on Beta-blocker Versus When Off Beta-blocker, as Measured by Step Count on Wearable Activity Monitoring Device
NCT04767061 (10) [back to overview]Change in Patient-reported Quality of Life When on Beta-blocker Versus When Off Beta-blocker, as Measured by Patient-Reported Outcome Measurement Information System-29 (PROMIS-29)

Change in Exercise Capacity When on Beta-blocker Versus When Off Beta-blocker, as Measured by Peak Oxygen Consumption (VO2) During Cardiopulmonary Exercise Test (CPET)

"Cardiopulmonary exercise testing (CPET) measures breath-by-breath oxygen production during symptom-limited exercise on a stationary bike. This permits the calculation of peak oxygen consumption (VO2). Percent predicted peak VO2 for body weight will also be calculated. Due to the nature of N-of-1 trials, the duration of a subject's period varies based on the subject's home dose of beta-blocker prior to enrollment, therefore, each subject's respective time period for the OFF and ON periods could range between 3 - 6 weeks. The outcome measure data is the mean of the data collected during the span of the outcome measure time frame." (NCT04767061)
Timeframe: The maximum amount of time a subject could have been assessed for this outcome measure is 6-weeks. This outcome was measured at the end of the first and second visit.

Interventionml/kg/min (Mean)
ON Beta Blockers10.0
OFF Beta Blockers11.4

[back to top]

Change in Lower Extremity Function When on Beta-blocker Versus When Off Beta-blocker, as Measured by the Balance Portion of a Modified Version of the Short Physical Performance Battery.

"The Short Physical Performance Battery assesses gait speed, core strength when rising from a chair without using the upper extremities, and balance while standing without a cane or walker. The balance test portion of the SPPB assesses the subject's ability to stand unassisted without the use of a cane or walker. Balance test scores range from 0 - 4 with higher scores indicating better ability to stand unassisted. Our research team conducted the balance test according to SPPB standards. Due to the nature of N-of-1 trials, the duration of a subject's period varies based on the subject's home dose of beta-blocker prior to enrollment, therefore, each subject's respective time period for the OFF and ON periods could range between 3 - 6 weeks. The outcome measure data is the mean of the data collected during the span of the outcome measure time frame." (NCT04767061)
Timeframe: The maximum amount of time a subject could have been assessed for this outcome measure is 24-weeks. This outcome was measured at baseline and at each end of period visit.

Interventionscore on a scale (Mean)
ON Beta Blockers3.9
OFF Beta Blockers3.6

[back to top]

Change in Lower Extremity Function When on Beta-blocker Versus When Off Beta-blocker, as Measured by the Chair Rise Portion of a Modified Version of the Short Physical Performance Battery.

"The Short Physical Performance Battery assesses gait speed, core strength when rising from a chair without using the upper extremities, and balance while standing without a cane or walker. The chair rise portion of the SPPB assesses core strength. When comparing the number of seconds it takes to complete 5 chair rises, quicker speeds indicate better core strength. Our research team has chosen on comparing the speed at which subjects were able to complete the test. Due to the nature of N-of-1 trials, the duration of a subject's period varies based on the subject's home dose of beta-blocker prior to enrollment, therefore, each subject's respective time period for the OFF and ON periods could range between 3 - 6 weeks. The outcome measure data is the mean of the data collected during the outcome measure time frame." (NCT04767061)
Timeframe: The maximum amount of time a subject could have been assessed for this outcome measure is 24-weeks. This outcome was measured at baseline and at each end of period visit.

Interventionseconds (Mean)
ON Beta Blockers16
OFF Beta Blockers15.1

[back to top]

Change in Lower Extremity Function When on Beta-blocker Versus When Off Beta-blocker, as Measured by the Gait Speed Portion of a Modified Version of the Short Physical Performance Battery.

"The Short Physical Performance Battery assesses gait speed, core strength when rising from a chair without using the upper extremities, and balance while standing without a cane or walker. The gait speed portion of the SPPB assesses the subject's lower extremity function. When comparing the number of seconds it takes to complete the 4-meter gait speed test, quicker speeds indicate better lower extremity function. Our research team conducted the 4-meter gait speed test according to SPPB standards, but have chosen on comparing the speed at which subjects were able to complete the test. Due to the nature of N-of-1 trials, the duration of a subject's period varies based on the subject's home dose of beta-blocker prior to enrollment, therefore, each subject's respective time period for the OFF and ON periods could range between 3 - 6 weeks. The outcome measure data is the mean of the data collected during the span of the outcome measure time frame." (NCT04767061)
Timeframe: The maximum amount of time a subject could have been assessed for this outcome measure is 24-weeks. This outcome was measured at baseline and at each end of period visit.

Interventionseconds (Mean)
ON Beta Blockers4.3
OFF Beta Blockers4.6

[back to top]

Change in Patient-reported Cognitive Function When on Beta-blocker Versus When Off Beta-blocker, as Measured by Patient-Reported Outcome Measurement Information System-Short Form 6a (PROMIS SF-6a)

"Patient-Reported Outcome Measurement Information System-Short Form 6a (PROMIS SF-6a) is a survey of patient-perceived cognitive deficits. Questions are ranked on a 5-point Likert scale, with higher scores indicating better cognitive function. Scores are mapped so the values follow a normal distribution with a population mean T-score of 50 and an SD of 10. Instead of having a min or max, the raw scores have been transformed into t-scores for comparison to a reference population (the US general population) with a mean of 50 and SD of 10. Scores lower than 50 indicate worse cognitive function compared to the US general population. Due to the nature of N-of-1 trials, the duration of a subject's period varies based on the subject's home dose of beta-blocker prior to enrollment, therefore, each subject's respective time period for the OFF and ON periods could range between 3-6 weeks. The outcome measure data is the mean of the data collected during the span of the measured time points." (NCT04767061)
Timeframe: The maximum amount of time a subject could have been assessed for this measure is 76-weeks (24-week max intervention phase,1-year follow-up phase). This outcome was measured at baseline, weekly, end of period and intervention visits, and during follow-up.

Interventionscore on a scale (Mean)
ON Beta Blockers53.8
OFF Beta Blockers52.4

[back to top]

Change in Patient-reported Health Status When on Beta-blocker Versus When Off Beta-blocker, as Measured by Kansas City Cardiomyopathy Questionnaire (KCCQ-12)

"The Kansas City Cardiomyopathy Questionnaire (KCCQ-12) is a heart failure-specific health status survey. Questions are ranked on 5- to 7-point Likert scales, with higher scores indicating better health status. KCCQ scores are scaled from 0 to 100 and frequently summarized in 25-point ranges, where scores represent health status as follows: 0 to 24: very poor to poor; 25 to 49: poor to fair; 50 to 74: fair to good; and 75 to 100: good to excellent. Due to the nature of N-of-1 trials, the duration of a subject's period varies based on the subject's home dose of beta-blocker prior to enrollment, therefore, each subject's respective time period for the OFF and ON periods could range between 3 - 6 weeks. The outcome measure data is the mean of the data collected during the span of the outcome measure time frame." (NCT04767061)
Timeframe: The max amount of time a subject could have been assessed for this measure is 76-weeks (24-week max intervention phase,1-year follow-up phase). This outcome was measured at baseline, bi-weekly, end of period and intervention visits, and during follow-up.

Interventionscore on a scale (Mean)
ON Beta Blockers58.7
OFF Beta Blockers66.0

[back to top]

Change in Patient-reported Health When on Beta-blocker Versus When Off Beta-blocker, as Measured by the EuroQol-5D Visual Analogue System (EQ-5D VAS)

"The EuroQol-5D Visual Analogue System (EQ-5D VAS) indicates patient-perceived health on a vertical visual analogue scale. The scale ranges from 0, indicating poorest health, to 100, indicating the best health. Due to the nature of N-of-1 trials, the duration of a subject's period varies based on the subject's home dose of beta-blocker prior to enrollment, therefore, each subject's respective time period for the OFF and ON periods could range between 3 - 6 weeks. The outcome measure data is the mean of the data collected during the span of the outcome measure time frame." (NCT04767061)
Timeframe: The maximum amount of time a subject could have been assessed for this outcome measure is 24-weeks. This outcome was measured at baseline and at each end of period visit.

Interventionscore on a scale (Mean)
ON Beta Blockers68.9
OFF Beta Blockers67.8

[back to top]

Change in Patient-reported Sexual Function When on Beta-blocker Versus When Off Beta-blocker, as Measured by Patient-Reported Outcome Measurement Information System-Sexual Function (PROMIS-Sexual Function)

"Patient-Reported Outcome Measurement Information System-Sexual Function (PROMIS-Sexual Function) measures self-reported sexual function and satisfaction. Questions are ranked on a 6-point Likert scale, with higher scores indicating poorer sexual function and satisfaction. Due to the nature of N-of-1 trials, the duration of a subject's period varies based on the subject's home dose of beta-blocker prior to enrollment, therefore, each subject's respective time period for the OFF and ON periods could range between 3 - 6 weeks. The outcome measure data is the mean of the data collected during the span of the outcome measure time frame. The score ranges from 0-10 with higher scores meaning worsened sexual function." (NCT04767061)
Timeframe: The maximum amount of time a subject could have been assessed for this measure is 76-weeks (24-week max intervention phase,1-year follow-up phase). This outcome was measured at baseline, end of period and intervention visits, and during follow-up.

Interventionscore on a scale (Mean)
ON Beta Blockers1.8
OFF Beta Blockers2.1

[back to top]

Change in Physical Activity When on Beta-blocker Versus When Off Beta-blocker, as Measured by Step Count on Wearable Activity Monitoring Device

"The wearable activity monitoring device measures daily step count. Due to the nature of N-of-1 trials, the duration of a subject's periods varies based on the subject's home dose of beta-blocker prior to enrollment, therefore, each subject's respective time period for the OFF and ON periods could range between 3 and 6 weeks. We will compare average step counts over 2-week periods, which will be the final 2 weeks of each period when subjects are either on their home (ON Beta Blockers) or minimally tolerated (OFF Beta Blockers) dose. The outcome measure data is the mean collected during the outcome measure time frame." (NCT04767061)
Timeframe: The maximum amount of time a subject could have been assessed for this outcome measure is 8-weeks (last 2 weeks of each period for up to 4 periods).

InterventionCount of Steps (Mean)
ON Beta Blockers2790.5
OFF Beta Blockers3167.3

[back to top]

Change in Patient-reported Quality of Life When on Beta-blocker Versus When Off Beta-blocker, as Measured by Patient-Reported Outcome Measurement Information System-29 (PROMIS-29)

"The PROMIS-29 assesses 7 domains with 4 questions with an additional pain intensity numeric rating scale. The patients' answers to the PROMIS-29 are scored from 1-5 (except for the pain numeric rating scale). The sum of the PROMIS-29 is the raw score transformed into a final T-score metric. Scores are mapped so that the values follow a normal distribution with a population mean T-score of 50 and an SD of 10. Instead of having a min or max, the PROMIS-29 raw scores have been transformed into t-scores for comparison to a reference population (the US general population) with a mean of 50 and SD of 10. Scores lower than 50 indicate worse health compared to the US general population. Due to the nature of N-of-1 trials, the duration of a subject's period varies based on the subject's home dose of beta-blocker before enrollment, therefore, each subject's respective period for the OFF and ON periods could range between 3 - 6 weeks. The values measured over the time points were averaged." (NCT04767061)
Timeframe: The maximum amount of time a subject could have been assessed for this measure is 76-weeks (24-week max intervention phase,1-year follow-up phase). This outcome was measured at baseline, weekly, end of period and intervention visits, and during follow-up.

,
Interventionscore on a scale (Mean)
Physical Health ComponentMental Health Component
OFF Beta Blockers40.047.9
ON Beta Blockers39.846.8

[back to top]