Page last updated: 2024-11-04

bunazosin

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

bunazosin: structure [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID2472
CHEMBL ID188185
CHEBI ID135576
SCHEMBL ID49348
MeSH IDM0069474

Synonyms (43)

Synonym
2-(4-butanoyl-1,4-diazepan-1-yl)-6,7-bis(methyloxy)quinazolin-4-amine
80755-51-7
D07550
bunazosin (inn)
bunazosin
bunazosinum [latin]
1h-1,4-diazepine, 1-(4-amino-6,7-dimethoxy-2-quinazolinyl)hexahydro-4-(1-oxobutyl)-, monohydrochloride
bunazosina [spanish]
bunazosine [french]
bunazosin [inn]
1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-butyrylhexahydro-1h-1,4-diazepine
4-amino-2-(4-butyryl-1,4-diazepan-1-yl)-6,7-dimethoxychinazolin
L013380
CHEBI:135576
CHEMBL188185
1-[4-(4-amino-6,7-dimethoxyquinazolin-2-yl)-1,4-diazepan-1-yl]butan-1-one
9uuw4v7g2h ,
unii-9uuw4v7g2h
bunazosine
bunazosinum
bunazosina
bunazosin [who-dd]
bunazosin [mi]
SCHEMBL49348
smr004703272
MLS006011493
bdbm50088386
DTXSID7022700
dibenzo[1,2]oxathiin6-oxide
1-[4-(4-amino-6,7-dimethoxy-2-quinazolinyl)hexahydro-1h-1,4-diazepin-1-yl]-
sr-01000945226
SR-01000945226-1
SR-01000945226-2
AKOS030228613
AS-73224
4-amino-2-(4-butyrylhexahydro-1h-1,4-diazepin-1-yl)-6,7-dimethoxy-quinazoline
Z1172912933
DB12230
Q4997419
1-(4-(4-amino-6,7-dimethoxyquinazolin-2-yl)-1,4-diazepan-1-yl)butan-1-one
CS-0028147
HY-107326
EN300-6492965

Research Excerpts

Overview

Bunazosin hydrochloride is a potent and selective alpha1-adrenoceptor antagonist. It has been clinically used both as a systemic antihypertensive as well as an ocular hypotensive drug.

ExcerptReferenceRelevance
"Bunazosin hydrochloride is a potent and selective alpha1-adrenoceptor antagonist that has been clinically used both as a systemic antihypertensive as well as an ocular hypotensive drug. "( Bunazosin, a selective alpha1-adrenoceptor antagonist, as an anti-glaucoma drug: effects on ocular circulation and retinal neuronal damage.
Araie, M; Hara, H; Ichikawa, M; Oku, H; Shimazawa, M, 2005
)
3.21

Effects

Bunazosin has an additive effect on lowering IOP when topically added to latanoprost treatment in glaucoma patients. It has an antagonistic action on this receptor.

Bunazosin retard has Cmax and area underthe concentration curve (AUC) to be linearly related to the dose between 3 and 18 mg (r = 0.8) It has an antagonistic action on this receptor.

ExcerptReferenceRelevance
"Bunazosin has an additive effect on lowering IOP when topically added to latanoprost treatment in glaucoma patients."( Additive effect of bunazosin on intraocular pressure when topically added to treatment with latanoprost in patients with glaucoma.
Jian, K; Mishima, HK; Mukai, S; Okada, K; Takamatsu, M; Tsukamoto, H; Tsumamoto, Y,
)
1.9
"Bunazosin has an antagonistic action on this receptor."( Actions of the alpha-1 adrenoceptor blocker bunazosin on the norepinephrine-induced contraction of smooth muscles in the rabbit proximal urethra.
Itoh, T; Kimoto, Y; Nozaki, M, 1987
)
1.26
"Bunazosin has an additive effect on lowering IOP when topically added to latanoprost treatment in glaucoma patients."( Additive effect of bunazosin on intraocular pressure when topically added to treatment with latanoprost in patients with glaucoma.
Jian, K; Mishima, HK; Mukai, S; Okada, K; Takamatsu, M; Tsukamoto, H; Tsumamoto, Y,
)
1.9
"Bunazosin retard has Cmax and area underthe concentration curve (AUC) to be linearly related to the dose between 3 and 18 mg (r = 0.8)."( Pharmacokinetic and pharmacodynamic properties and therapeutic use of bunazosin in hypertension. A review.
Weidinger, G, 1995
)
1.25
"Bunazosin has an antagonistic action on this receptor."( Actions of the alpha-1 adrenoceptor blocker bunazosin on the norepinephrine-induced contraction of smooth muscles in the rabbit proximal urethra.
Itoh, T; Kimoto, Y; Nozaki, M, 1987
)
1.26

Actions

ExcerptReferenceRelevance
"Bunazosin appears to produce a decrease in urethral resistance and to be useful for the treatment of the failure of bladder emptying due to high urethral resistance."( [Effect of bunazosin on lower urinary tract function in the decerebrated dog].
Ebina, K; Fukuda, T; Nakamura, H; Nishizawa, O; Noto, H; Suzuki, K; Tsuchida, S, 1987
)
1.38

Treatment

Bunazosin appears to be associated with a slightly higher insulin sensitivity than is atenolol. Pretreatment with bunazos in inhibited the decrease in ATP and the increase in AMP caused by ischemia.

ExcerptReferenceRelevance
"Bunazosin retard treatment in hypertensive non-insulin-dependent diabetes mellitus patients appears to be associated with a slightly higher insulin sensitivity than is atenolol."( Insulin sensitivity following treatment with the alpha 1-blocker bunazosin retard and the beta 1-blocker atenolol in hypertensive non-insulin-dependent diabetes mellitus patients.
Eriksson, JW; Foley, K; Jansson, PA; Lithell, H, 1996
)
1.97
"Treatment with bunazosin was started when the animals were 7 weeks of age."( Prevention of cardiac hypertrophy by a sub-antihypertensive dose of the alpha 1-adrenergic antagonist bunazosin in Dahl salt-sensitive rats.
Fukuda, N; Izumi, Y; Kanmatsuse, K; Kubo, A; Matsuoka, M; Nakayama, T; Soma, M; Watanabe, Y, 1996
)
0.85
"Treatment with bunazosin ameliorated this ischemia-related shortening of refractory periods at both the endo- and epicardial sites, with a greater effect seen epicardially (p < 0.05), resulting in values similar to those in the nonischemic tissue."( Differences in refractory-period response of canine subendocardium and subepicardium to bunazosin, an alpha1-adrenoceptor antagonist, and propranolol during myocardial ischemia.
Handa, S; Iwamoto, T; Kusuzaki, S; Takigawa, O; Tanabe, T; Usui, K; Yoshitake, M, 1997
)
0.86
"Pretreatment with bunazosin inhibited the decrease in ATP and the increase in AMP caused by ischemia, resulting in the high value of ECP in the ischemic myocardium."( Effects of bunazosin, a selective alpha 1-adrenergic blocking agent, on myocardial energy metabolism in ischemic dog heart.
Abiko, Y; Ichihara, K; Yoshida, R, 1990
)
0.99
"Pretreatment with bunazosin, an alpha 1-"blocker," effectively prevented the increase in mitochondrial Ca2+ content, and reduced the arrhythmia ratio."( Effects of bunazosin and propranolol on ventricular arrhythmias in dogs with hypokalemia.
Ozawa, T; Sugiyama, S; Takamura, T, 1987
)
0.99
"pretreatment with bunazosin abolished the vasopressor responses to i.c.v."( Sympatholytic effects of the intravenously injected alpha 1-adrenergic blocker, bunazosin, in anaesthetized rats.
Ikegaki, I; Matsuzawa, M; Okabayashi, H; Suga, K; Takahashi, H; Yoshimura, M, 1987
)
0.82

Toxicity

ExcerptReferenceRelevance
" Stomatitis was observed in only one case as a side effect of this drug."( [Usefulness and safety of bunazosin hydrochloride in neurogenic bladder after prolonged administration].
Gotoh, S; Hiraga, S; Hosoda, K; Kakehi, R; Kaneoya, F; Kojima, S; Mizuo, T; Satoh, T; Tanizawa, A; Yokokawa, M, 1992
)
0.58

Pharmacokinetics

New ocular pharmacokinetic pharmacodynamic (PK/PD) model for anti-glaucoma drugs to describe ocular hypotensive effects.

ExcerptReferenceRelevance
" There were, however, neither prolongation of apparent elimination half-life (t1/2), nor increase in Cmax, nor area under the plasma concentration-time curve (AUC0-24) after consecutive dosing in both groups."( Pharmacokinetics and pharmacodynamics of the alpha 1-adrenergic antagonist bunazosin retard in hypertensives.
Gotoh, E; Ishii, M; Minamisawa, K; Minamisawa, M; Shionoiri, H; Sugimoto, K; Takasaki, I; Takizawa, T; Ueda, S, 1994
)
0.52
" In the present study, we have investigated the pharmacokinetic and pharmacodynamic characteristics of ibopamine after ocular application."( Ocular pharmacokinetics and pharmacodynamics in rabbits of ibopamine, a new mydriatic agent.
Galbiati, I; Gazzaniga, A; Gianesello, V; Soldati, L; Virno, M, 1993
)
0.29
" Pharmacokinetic studies in normotensive volunteers showed that plasma peak concentration (Cmax) of bunazosin retard and bioavailability were approximately 50% and 81%, respectively, of the values of the standard non-retarded formulation."( Pharmacokinetic and pharmacodynamic properties and therapeutic use of bunazosin in hypertension. A review.
Weidinger, G, 1995
)
0.74
" The pharmacokinetic parameters of bunazosin elimination half-life and time to peak level were not statistically significantly affected by renal insufficiency."( Pharmacokinetics and pharmacodynamics of bunazosin in patients with renal insufficiency.
Koike, Y; Mineshita, S; Mizoguchi, H; Nomura, Y, 1999
)
0.85
" 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
"We have constructed a new ocular pharmacokinetic pharmacodynamic (PK/PD) model for anti-glaucoma drugs to describe ocular hypotensive effects on intraocular pressure (IOP) after instillation of a combination of an alpha(1)-adrenergic antagonist, bunazosin, and a beta-adrenergic antagonist, timolol, into rabbits."( Ocular pharmacokinetic/pharmacodynamic modeling for multiple anti-glaucoma drugs.
Higuchi, S; Kawazu, K; Kitahara, T; Nakamura, J; Nakashima, M; Nishida, K; Sakanaka, K; Sasaki, H; Tomonari, M, 2008
)
0.53

Bioavailability

ExcerptReferenceRelevance
" Ibopamine is well absorbed through the cornea, it is rapidly hydrolysed by esterases to epinine and the mydriatic effect is correlated with the concentration of epinine in the aqueous humor."( Ocular pharmacokinetics and pharmacodynamics in rabbits of ibopamine, a new mydriatic agent.
Galbiati, I; Gazzaniga, A; Gianesello, V; Soldati, L; Virno, M, 1993
)
0.29
" Pharmacokinetic studies in normotensive volunteers showed that plasma peak concentration (Cmax) of bunazosin retard and bioavailability were approximately 50% and 81%, respectively, of the values of the standard non-retarded formulation."( Pharmacokinetic and pharmacodynamic properties and therapeutic use of bunazosin in hypertension. A review.
Weidinger, G, 1995
)
0.74

Dosage Studied

Bunazosin (10(-7) M) blocked norepinephrine-induced contraction with a parallel shift of the dose-response curve in both directions. A significant decrease in both systolic and diastolic BP was observed after consecutive dosing of bunazosins.

ExcerptRelevanceReference
" Thus, these improvements were not correlated with the dosage of drug."( [The evaluation of the effects of bunazosin hydrochloride in the treatment of prostatic hyperplasia].
Asano, H; Fujita, T; Hirabayashi, S; Kato, N; Kinukawa, T; Ohshima, S; Ono, Y, 1992
)
0.56
" At the late stage (within 8-11 hours of the perfusion period), the dose-response curve for guanabenz was shifted to the left and the maximum response became approximately 3-fold larger than that in the early stage."( Perfusion-time dependent enhancements of guanabenz- and KCl-induced vasoconstrictions in isolated and perfused dog pulmonary veins.
Chiba, S; Haniuda, M, 1990
)
0.28
" A dosage of 12 mg/day did not improve subjective symptoms more than did the 9 mg/day dose."( [Clinical study of bunazosin hydrochloride, an alpha 1-adrenergic blocker, in benign prostatic obstruction and neurogenic bladder dysfunction].
Kondo, A; Mitsuya, H; Otani, T; Takita, T, 1987
)
0.6
" An intraluminal injection of serotonin (5-HT) produced a marked vasoconstriction and the dose-response curve was bell-shaped."( Pharmacological analysis of 5-HT-induced vasoconstriction in isolated, perfused dog skeletal muscle arteries.
Chiba, S; Sinanović, O, 1987
)
0.27
" In the isolated rabbit aorta, E-643 blocked noradrenaline-induced contraction of the aorta with a parallel shift of the dose-response curve to the right."( alpha-Adrenoceptor blocking properties of a new antihypertensive agent, 2-[4-(n-butyryl)-homopiperazine-1-yl]-4-amino-6,7-dimethoxyquinazoline (E-643).
Daiku, Y; Igarashi, T; Shoji, T, 1980
)
0.26
" The order of affinity (pA2) for presynaptic alpha-receptors, as assessed from parallel shift of the dose-response curve to clonidine, was: phentolamine greater than yohimbine greater than tolazoline greater than E-643 greater than or equal to prazosin."( Comparison of pre- and postsynaptic alpha-adrenoceptor blocking effects of E-643 in the isolated vas deferens of the rat.
Shoji, T, 1981
)
0.26
" A significant decrease in both systolic and diastolic BP was observed after consecutive dosing of bunazosin compared to baseline values over 24 h in the NRF and for 8 h in the IRF."( Pharmacokinetics and pharmacodynamics of the alpha 1-adrenergic antagonist bunazosin retard in hypertensives.
Gotoh, E; Ishii, M; Minamisawa, K; Minamisawa, M; Shionoiri, H; Sugimoto, K; Takasaki, I; Takizawa, T; Ueda, S, 1994
)
0.74
" Dosage was of 3 and 6 mg/day per os; after 2 weeks' treatment, if DBP in clinostatism > or = 95 mmHg, the dose was doubled."( [Dose-response study of bunazosin in the treatment of light-to-moderate arterial hypertension].
De Luca, N; Fontana, D; Lamenza, F; Marchegiano, R; Sarno, D; Tozzi, N, 1993
)
0.59
" In fact, this range of daily dosage led to a fall in pressure values, without causing clinically significant alterations of heart rate, electrocardiograph traces and laboratory parameters."( [Dose-response study of bunazosin in the treatment of light-to-moderate arterial hypertension].
De Luca, N; Fontana, D; Lamenza, F; Marchegiano, R; Sarno, D; Tozzi, N, 1993
)
0.59
"In conclusions, in mild/moderate arterial hypertension, bunazosin in monotherapy at the dosage of 3-6 mg/day, is an effective and safe treatment."( [Dose-response study of bunazosin in the treatment of light-to-moderate arterial hypertension].
De Luca, N; Fontana, D; Lamenza, F; Marchegiano, R; Sarno, D; Tozzi, N, 1993
)
0.84
" As there was a close correlation between plasma levels and antihypertensive activity of bunazosin in the present study, dosage adjustment of the alpha 1-receptor blocker in patients with impaired liver and kidney function appears to be mandatory."( Bunazosin in patients with impaired hepatic or renal function.
Halabi, A; Kirch, W; Nokhodian, A,
)
1.8
" The dose-response curves for clonidine and NA were shifted to the right by bunazosin (a selective alpha 1-adrenoceptor antagonist), but were not affected by midaglizole (a selective alpha 2-adrenoceptor antagonist)."( Characteristics of the responses of isolated and perfused canine splenic arteries to vasoactive substances and to periarterially electrical stimulation.
Chiba, S; Nakane, T; Ren, LM, 1994
)
0.52
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
quinazolinesAny organic heterobicyclic compound based on a quinazoline skeleton and its substituted derivatives.
[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]

Protein Targets (3)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Alpha-1D adrenergic receptorHomo sapiens (human)IC50 (µMol)0.00120.00020.75688.8970AID1915707
Alpha-1A adrenergic receptorHomo sapiens (human)IC50 (µMol)0.00120.00020.56145.4000AID1915707
Alpha-1B adrenergic receptorHomo sapiens (human)IC50 (µMol)0.00120.00020.65268.3300AID1915707
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (37)

Processvia Protein(s)Taxonomy
G protein-coupled receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of cell population proliferationAlpha-1D adrenergic receptorHomo sapiens (human)
neuron-glial cell signalingAlpha-1D adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-1D adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of vasoconstrictionAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-1D adrenergic receptorHomo sapiens (human)
MAPK cascadeAlpha-1A adrenergic receptorHomo sapiens (human)
negative regulation of heart rate involved in baroreceptor response to increased systemic arterial blood pressureAlpha-1A adrenergic receptorHomo sapiens (human)
norepinephrine-epinephrine vasoconstriction involved in regulation of systemic arterial blood pressureAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of heart rate by epinephrine-norepinephrineAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of the force of heart contraction by epinephrine-norepinephrineAlpha-1A adrenergic receptorHomo sapiens (human)
apoptotic processAlpha-1A adrenergic receptorHomo sapiens (human)
smooth muscle contractionAlpha-1A adrenergic receptorHomo sapiens (human)
signal transductionAlpha-1A adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-1A adrenergic receptorHomo sapiens (human)
activation of phospholipase C activityAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationAlpha-1A adrenergic receptorHomo sapiens (human)
adult heart developmentAlpha-1A adrenergic receptorHomo sapiens (human)
negative regulation of cell population proliferationAlpha-1A adrenergic receptorHomo sapiens (human)
response to xenobiotic stimulusAlpha-1A adrenergic receptorHomo sapiens (human)
response to hormoneAlpha-1A adrenergic receptorHomo sapiens (human)
negative regulation of autophagyAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of cardiac muscle hypertrophyAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of synaptic transmission, GABAergicAlpha-1A adrenergic receptorHomo sapiens (human)
intracellular signal transductionAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of action potentialAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of vasoconstrictionAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of smooth muscle contractionAlpha-1A adrenergic receptorHomo sapiens (human)
calcium ion transport into cytosolAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of cardiac muscle contractionAlpha-1A adrenergic receptorHomo sapiens (human)
cell growth involved in cardiac muscle cell developmentAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of protein kinase C signalingAlpha-1A adrenergic receptorHomo sapiens (human)
pilomotor reflexAlpha-1A adrenergic receptorHomo sapiens (human)
neuron-glial cell signalingAlpha-1A adrenergic receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayAlpha-1A adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-1A adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-1A adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
regulation of vasoconstrictionAlpha-1B adrenergic receptorHomo sapiens (human)
intracellular signal transductionAlpha-1B adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-1B adrenergic receptorHomo sapiens (human)
regulation of cardiac muscle contractionAlpha-1B adrenergic receptorHomo sapiens (human)
neuron-glial cell signalingAlpha-1B adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-1B adrenergic receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationAlpha-1B adrenergic receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (4)

Processvia Protein(s)Taxonomy
protein bindingAlpha-1D adrenergic receptorHomo sapiens (human)
identical protein bindingAlpha-1D adrenergic receptorHomo sapiens (human)
alpha1-adrenergic receptor activityAlpha-1D adrenergic receptorHomo sapiens (human)
alpha1-adrenergic receptor activityAlpha-1A adrenergic receptorHomo sapiens (human)
protein bindingAlpha-1A adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-1A adrenergic receptorHomo sapiens (human)
protein bindingAlpha-1B adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-1B adrenergic receptorHomo sapiens (human)
alpha1-adrenergic receptor activityAlpha-1B adrenergic receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (8)

Processvia Protein(s)Taxonomy
plasma membraneAlpha-1D adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1D adrenergic receptorHomo sapiens (human)
nucleusAlpha-1A adrenergic receptorHomo sapiens (human)
nucleoplasmAlpha-1A adrenergic receptorHomo sapiens (human)
cytoplasmAlpha-1A adrenergic receptorHomo sapiens (human)
cytosolAlpha-1A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1A adrenergic receptorHomo sapiens (human)
caveolaAlpha-1A adrenergic receptorHomo sapiens (human)
nuclear membraneAlpha-1A adrenergic receptorHomo sapiens (human)
intracellular membrane-bounded organelleAlpha-1A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1A adrenergic receptorHomo sapiens (human)
nucleusAlpha-1B adrenergic receptorHomo sapiens (human)
cytoplasmAlpha-1B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1B adrenergic receptorHomo sapiens (human)
caveolaAlpha-1B adrenergic receptorHomo sapiens (human)
nuclear membraneAlpha-1B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1B adrenergic receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (10)

Assay IDTitleYearJournalArticle
AID1915707Antagonist activity at Adrenergic alpha-1 receptor (unknown origin)2021European journal of medicinal chemistry, Feb-05, Volume: 211Therapeutic progression of quinazolines as targeted chemotherapeutic agents.
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.
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.
AID239799Binding affinity for alpha 1a adrenoceptor2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Range and sensitivity as descriptors of molecular property spaces in dynamic QSAR analyses.
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.
AID239801Binding affinity for alpha 1d adrenoceptor2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Range and sensitivity as descriptors of molecular property spaces in dynamic QSAR analyses.
AID1207620Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes2012Journal of applied toxicology : JAT, Oct, Volume: 32, Issue:10
Predictive model for L-type channel inhibition: multichannel block in QT prolongation risk assessment.
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.
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.
AID239800Binding affinity for alpha 1b adrenoceptor2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Range and sensitivity as descriptors of molecular property spaces in dynamic QSAR analyses.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (230)

TimeframeStudies, This Drug (%)All Drugs %
pre-199083 (36.09)18.7374
1990's110 (47.83)18.2507
2000's33 (14.35)29.6817
2010's1 (0.43)24.3611
2020's3 (1.30)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 27.90

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

MetricThis Compound (vs All)
Research Demand Index27.90 (24.57)
Research Supply Index5.63 (2.92)
Research Growth Index5.04 (4.65)
Search Engine Demand Index33.17 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (27.90)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials33 (13.47%)5.53%
Reviews7 (2.86%)6.00%
Case Studies10 (4.08%)4.05%
Observational0 (0.00%)0.25%
Other195 (79.59%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (1)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Effects of Combination Therapy With an α1-blocker (Sustained-release Preparation of Bunazosin or Doxazosin) in Inadequate Responders to an Angiotensin II Antagonist (Valsartan) in the Treatment of Patients With Mild to Moderate Essential Hypertension [NCT00130156]Phase 493 participants (Actual)Interventional2005-10-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]