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terazosin

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Description

Terazosin: induces decreased blood pressure; used in the treatment of benign prostatic hyperplasia [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID5401
CHEMBL ID611
CHEBI ID9445
SCHEMBL ID6528
MeSH IDM0528343
PubMed CID969465
CHEMBL ID1554413
SCHEMBL ID5424458
MeSH IDM0528343

Synonyms (125)

Synonym
LS-14728
CHEBI:9445 ,
6,7-dimethoxy-2-[4-(tetrahydrofuran-2-ylcarbonyl)piperazin-1-yl]quinazolin-4-amine
terazosina
terazosinum
bdbm50033111
BRD-A22256192-003-03-7
LOPAC0_001138
vasomet
6,7-bis(methyloxy)-2-[4-(tetrahydrofuran-2-ylcarbonyl)piperazin-1-yl]quinazolin-4-amine
PRESTWICK3_000751
BPBIO1_000840
PRESTWICK2_000751
BSPBIO_000762
c19h25n5o4
terazosin [inn:ban]
terazosina [inn-spanish]
terazosine [inn-french]
piperazine, 1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-((tetrahydro-2-furanyl)carbonyl)-
flumarc
terazosinum [inn-latin]
C07127
terazosin
terazosine
63590-64-7
DB01162
1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-((tetrahydro-2-furanyl)carbonyl)piperazine
MLS000069703 ,
smr000058309
SPBIO_002701
PRESTWICK0_000751
PRESTWICK1_000751
NCGC00025191-03
MLS001201836
AC-11120
HMS2090P21
NCGC00016026-08
terazosabb
CHEMBL611 ,
L000692
D08569
terazosin (inn)
terazosabb (tn)
[4-(4-amino-6,7-dimethoxyquinazolin-2-yl)piperazin-1-yl]-(oxolan-2-yl)methanone
A834201
1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-[(tetrahydro-2-furanyl)carbonyl]-piperazinehydrochloride
AKOS005266642
HMS3259F04
[4-(4-amino-6,7-dimethoxyquinazolin-2-yl)piperazin-1-yl](tetrahydrofuran-2-yl)methanone
STK567029
BBL010743
CCG-205212
HMS2232N21
NCGC00016026-05
NCGC00016026-04
8l5014xet7 ,
unii-8l5014xet7
6,7-dimethoxy-2-[4-(oxolane-2-carbonyl)piperazin-1-yl]quinazolin-4-amine
abbott 45975
FT-0630739
NCGC00016026-11
gtpl7302
HMS3371E20
6,7-dimethoxy-2-[4-(oxolane-2-carbonyl)piperazin-1-yl]-3,4-dihydroquinazolin-4-imine
HMS3369P14
1-(4-amino-6,7-dimethoxy-2-quinazolinyl)4-[(tetrahydro-2-furanyl)carbonyl]piperazine hydrochloride
1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-(2-tetrahydrofuroyl)piperazine
1-(4-amino-6,7-dimethoxyquinazolin-2-yl)-4-[[(2rs)-2,3,4,5-tetrahydrofuran-2-yl]carbonyl]piperazine
1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-(tetrahydro-2-furoyl)piperazine
1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-(2-tetrahydrofuroyl)-piperazine
terazocin
terazosin [vandf]
terazosin [who-dd]
terazosin [mi]
terazosin [inn]
HY-B0371
NC00689
1-(4-amino-6,7-dimethoxy-2-quinazolinyl)4-[(tetrahydro-2-furanyl)carbonyl]piperazine
SCHEMBL6528
REGID_FOR_CID_5401
terazosin a
141269-45-6
terazosinhydrochloride
MLS006011889
6,7-dimethoxy-2-[4-(tetrahydro-2-furanylcarbonyl)-1-piperazinyl]-4-quinazolinamine #
OPERA_ID_1910
DTXSID3023639 ,
6,7-dimethoxy-2-{4-[(oxolan-2-yl)carbonyl]piperazin-1-yl}quinazolin-4-amine
(4-(4-amino-6,7-dimethoxyquinazolin-2-yl)piperazin-1-yl)(tetrahydrofuran-2-yl)methanone
1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-[(tetrahydro-2-furanyl)carbonyl]piperazine
Z1172269406
141269-44-5
Q280786
6,7-dimethoxy-2-[4-(tetrahydrofuran-2-ylcarbonyl)piperazin-1-yl]quinazolin-4-amine hydrochloride
BRD-A22256192-003-14-4
1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-{(tetnaphydro-2-furanyl)carbonyl}piperazine
SDCCGSBI-0051105.P002
HMS3742I09
terazosina (inn-spanish)
dtxcid003639
terazosinum (inn-latin)
g04ca03
terazosine (inn-french)
6,7-dimethoxy-2-(4-(tetrahydrofuran-2-ylcarbonyl)piperazin-1-yl)quinazolin-4-amine
EN300-119614
BIDD:GT0682
cas-63590-64-7
smr000550495
MLS001165675
A834431
[4-(4-azanyl-6,7-dimethoxy-quinazolin-2-yl)piperazin-1-yl]-[(2s)-oxolan-2-yl]methanone
[4-(4-amino-6,7-dimethoxy-2-quinazolinyl)-1-piperazinyl]-[(2s)-2-oxolanyl]methanone
[4-(4-amino-6,7-dimethoxyquinazolin-2-yl)piperazin-1-yl]-[(2s)-oxolan-2-yl]methanone
HMS2233L04
SCHEMBL5424458
(s)-terazosin
CHEMBL1554413
HY-B0371D
109351-33-9
(s)-(4-(4-amino-6,7-dimethoxyquinazolin-2-yl)piperazin-1-yl)(tetrahydrofuran-2-yl)methanone
CS-0096555
MS-26410
6,7-dimethoxy-2-{4-[(2s)-oxolane-2-carbonyl]piperazin-1-yl}quinazolin-4-amine
EN300-7438962
AKOS040737253

Research Excerpts

Overview

Terazosin is an alpha1-selective adrenoceptor blocking agent that has been reported in many clinical trials to be an effective choice for the treatment of benign prostatic hyperplasia (BPH)

ExcerptReferenceRelevance
"Terazosin is a safe and effective treatment for lower ureteral stones. "( Efficacy of terazosin as a facilitator agent for expulsion of the lower ureteral stones.
Alizadeh, F; Hosseini, SR; Mohseni, MG, 2006
)
2.16
"Terazosin is an alpha1-selective adrenoceptor blocking agent that has been reported in many clinical trials to be an effective choice for the treatment of benign prostatic hyperplasia (BPH). "( Effects of branded versus generic terazosin hydrochloride in adults with benign prostatic hyperplasia: a randomized, open-label, crossover study in Taiwan.
Lan, SK; Ou, JH; Tsai, YS; Tzai, TS, 2007
)
2.06
"Terazosin is a selective alpha1-adrenoceptor antagonist. "( Effects of oral and intravenous terazosin and head-up tilt on blood pressure responses in patients with hypertension.
Achari, R; Baroldi, P; Cavanaugh, J; Cohen, A; Hosmane, B; Linnen, P, 1998
)
2.03
"Terazosin is a safe treatment for BPH in normotensive and hypertensive men, including men who are already taking additional antihypertensive drugs."( Terazosin in benign prostatic hyperplasia: effects on blood pressure in normotensive and hypertensive men.
Kirby, RS, 1998
)
3.19
"Terazosin is an alpha 1 receptor antagonist which has been shown in placebo-controlled trials to significantly improve American Urology Association (AUA) symptom and quality-of-life scores and symptom problem index ('bother' score), as well as increase peak urinary flow rate, in men with BPH."( Terazosin. A pharmacoeconomic evaluation of its use in benign prostatic hyperplasia.
Goa, KL; Plosker, GL, 1997
)
2.46
"Terazosin is an alpha 1 receptor-blocking agent with a long half-life permitting once-daily dosing."( Terazosin in the treatment of benign prostatic hyperplasia: a multicentre, placebo-controlled trial.
Buckley, JF; Chilton, CP; Ibrahim, I; Kaisary, AV; Kirk, D; Lloyd, SN, 1992
)
2.45
"Terazosin is a selective alpha 1 adrenoceptor antagonist that is currently under clinical investigation for the treatment of clinical BPH."( Terazosin in the treatment of benign prostatic hyperplasia: the United States experience.
Laddu, A; Lepor, H, 1992
)
2.45
"Terazosin is a selective alpha 1-adrenoceptor antagonist; its actions on the serum lipoprotein profile were compared with those of the cardioselective beta-adrenoceptor antagonist atenolol in 40 patients with mild to moderate hypertension. "( Comparison of antihypertensive and lipid actions of terazosin and atenolol in essential hypertension.
Guy, S; Humphreys, JE; Silke, B, 1992
)
1.98
"Terazosin is a new, long-acting, selective, postsynaptic alpha 1-adrenergic receptor antagonist with a chemical structure similar to that of prazosin. "( Terazosin: pharmacokinetics and the effect of age and dose on the incidence of adverse events.
Achari, R; Laddu, AR; Somberg, JC, 1991
)
3.17
"Terazosin is a selective alpha 1-adrenergic-blocking agent indicated for the treatment of hypertension. "( Antihypertensive dose-response relationships: studies with the selective alpha 1-blocking agent terazosin.
Cheung, DG; Laddu, AR; Luther, RR; Weber, MA, 1991
)
1.94
"Terazosin was judged to be a safe and effective long-term medication for the treatment of hypertension."( Long-term efficacy and safety of terazosin alone and in combination with other antihypertensive agents.
Cohen, JD, 1991
)
1.28
"Terazosin is a potent and selective alpha 1 adrenergic blocking agent structurally similar to prazosin."( The alpha adrenergic binding properties of terazosin in the human prostate adenoma and canine brain.
Baumann, M; Lepor, H; Shapiro, E, 1988
)
1.26
"Terazosin is an alpha-1 adrenergic blocking agent currently marketed as an antihypertensive."( Clinical experience: symptomatic management of BPH with terazosin.
Dunzendorfer, U, 1988
)
1.24
"Terazosin is a new, selective, alpha 1-adrenoceptor antagonist which is structurally similar to prazosin and of similar therapeutic efficacy in the treatment of mild-to-moderate essential hypertension. "( Terazosin: a new antihypertensive agent with favorable effects on lipids.
Luther, RR, 1989
)
3.16
"Terazosin is a quinazoline antihypertensive agent that is chemically similar to prazosin. "( Pharmacology of terazosin.
Kyncl, JJ, 1986
)
2.06
"Terazosin is a post-synaptic alpha 1-adrenoceptor antagonist with a similar pharmacodynamic profile to prazosin. "( Terazosin. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in essential hypertension.
Monk, JP; Titmarsh, S, 1987
)
3.16
"Terazosin is a new long-acting, selective alpha 1-adrenergic antagonist. "( Terazosin: a new long-acting alpha 1-adrenergic antagonist for hypertension.
Eisen, G; Frishman, WH; Lapsker, J, 1988
)
3.16

Effects

Terazosin hydrochloride has been found to exist at room temperature in four solvent-free forms that can be isolated directly. The drug has been evaluated alone and in combination with other drugs for the treatment of mild to moderate hypertension.

ExcerptReferenceRelevance
"Terazosin has proved to be safe and results in significant improvement in bladder emptying in our patients with posterior urethral valves. "( Role of alpha adrenergic blocker in the management of posterior urethral valves.
Abraham, MK; Damisetti, KR; Kedari, PM; Narayanan, T; Nasir, AR; Puzhankara, R; Sudarsanan, B; Unnithan, GR, 2009
)
1.8
"Terazosin hydrochloride has been found to exist at room temperature in four solvent-free forms that can be isolated directly, one solvent-free form that can be prepared by desolvation of a methanolate, a methanol solvate, and a dihydrate."( Identification, preparation, and characterization of several polymorphs and solvates of terazosin hydrochloride.
Bauer, J; Dziki, W; Heitmann, W; Henry, R; Hollis, S; Leusen, FJ; Mannino, A; Morley, J; Quick, J; Spanton, S, 2006
)
1.28
"Terazosin has generally been well tolerated in short-term and long-term studies."( Terazosin: a new antihypertensive agent with favorable effects on lipids.
Luther, RR, 1989
)
2.44
"Terazosin has been studied in a variety of clinical trials conducted in hypertensive patients with supine diastolic blood pressures of 95 mm Hg or greater before treatment. "( Clinical trials with terazosin. General methods.
Glassman, HN; Luther, RR; Sperzel, WD, 1986
)
2.03
"Terazosin has been evaluated alone and in combination with other drugs for the treatment of mild to moderate hypertension."( Terazosin: a new long-acting alpha 1-adrenergic antagonist for hypertension.
Eisen, G; Frishman, WH; Lapsker, J, 1988
)
2.44

Actions

Terazosin was found to produce a dose-dependent, virtually complete cessation of behavioral activity that was reversed by coinfusion of phenylephrine. It had lower affinity at various subtypes than tamsulosin, but showed relatively high selectivity to the alpha1D-subtype.

ExcerptReferenceRelevance
"Terazosin promotes the expression of HSP90 and reduces the activity of iNOS."( Terazosin reduces steroidogenic factor 1 and upregulates heat shock protein 90 expression in LH-induced bovine ovarian theca cells.
Deng, SL; Lian, ZX; Tang, ZR; Yu, K, 2021
)
2.79
"Terazosin was found to produce a dose-dependent, virtually complete cessation of behavioral activity that was reversed by coinfusion of phenylephrine."( Immobility from administration of the alpha1-adrenergic antagonist, terazosin, in the IVth ventricle in rats.
Lin, Y; Quartermain, D; Stone, EA, 2003
)
1.28
"Terazosin had lower affinity at various subtypes than tamsulosin, but showed relatively high selectivity to the alpha1D-subtype."( Tamsulosin: alpha1-adrenoceptor subtype-selectivity and comparison with terazosin.
Muramatsu, I; Okada, K; Taniguchi, T, 1998
)
1.25

Treatment

Terazosin treatment resulted in significant changes in flow rate and residual urine. Changes in flow rates were not influenced by prostate size, while a marked decrease in residual urine was found in patients with large prostates. TerazosIn is a safe treatment for BPH in normotensive and hypertensive men, including men who are already taking a drug.

ExcerptReferenceRelevance
"Terazosin treatment extended survival, improved motor phenotypes and increased motor neuron number in Thy1-hTDP-43 mice."( Targeting phosphoglycerate kinase 1 with terazosin improves motor neuron phenotypes in multiple models of amyotrophic lateral sclerosis.
Becker, CG; Becker, T; Carroll, E; Chaytow, H; Faller, KME; Gillingwater, TH; Gordon, D; Huang, YT; Smith, HL; Talbot, K; van der Hoorn, D, 2022
)
1.71
"Terazosin or genistein treatment inhibited the growth of DU-145 cells in a dose-dependent manner, whereas had no effect on normal prostate epithelial cells."( Combined effects of terazosin and genistein on a metastatic, hormone-independent human prostate cancer cell line.
Chang, KL; Cheng, HL; Chih, TT; Hsieh, BS; Hu, YC; Huang, LW; Shyu, HW; Su, SJ, 2009
)
1.4
"Terazosin treatment did not affect prostate weight or histomorphology. "( Terazosin treatment suppresses basic fibroblast growth factor expression in the rat ventral prostate.
Christelli, E; Karayannacos, P; Kyroudi-Voulgari, A; Mitropoulos, D; Zervas, A, 2009
)
3.24
"In terazosin pretreated animals, the venom-induced cardiorespiratory changes were attenuated significantly."( Buthus tamulus venom-induced vasosensory reflexes are mediated through efferent pathways in sympathetic and vagal parasympathetics.
Deshpande, SB; Singh, SK, 2009
)
0.87
"Terazosin treatment however, 24 hours prior to, or 24 hours post-irradiation resulted in a significant enhancement of radiation-induced loss of clonogenic survival compared to radiation alone (p<0.05)."( Alpha1-adrenoceptor antagonists radiosensitize prostate cancer cells via apoptosis induction.
Cuellar, DC; Kyprianou, N; Rhee, J,
)
0.85
"Terazosin treatment did not affect the weight of the ventral prostate gland. "( Terazosin modifies the content of glycosaminoglycans and the activity of matrix metalloproteinase 2 in the rat ventral prostate.
Aletras, AJ; Hatzichristou, D; Kalinderis, N; Karakiulakis, G; Mitropoulos, D; Papakonstantinou, E; Zervas, A, 2007
)
3.23
"In terazosin treated patients, improvement after 3 months were as follows, IPSS 3.93 +/- .74 points reduction, Qmax 2.13 +/- .68 ml/s increase, post-voided residual urine volume (PVR) 20.67 +/- 10.56 ml reduction (significant, p<0.001) and prostate volume 0.57 +/- 1.54 ml reduction (not significant)."( Efficacy of terazosin and finasteride in symptomatic benign prostatic hyperplasia: A comparative study.
Anwarul Islam, AK; Kashem, MA; Kibria, SA; Shameem, IA, 2005
)
1.22
"Terazosin-treated patients had decreases in Boyarsky obstructive, irritative, and total scores of 3.3 (52%), 1.3 (29%), and 4.6 (42%), respectively, compared with decreases of 0.7 (12%), 0.4 (9%), and 1.1 (11%), respectively, in the placebo group (P < .05). "( Terazosin in the treatment of benign prostatic hyperplasia. Terazosin Benign Prostatic Hyperplasia Study Group.
Adams, G; Brawer, MK; Epstein, H, 1993
)
3.17
"Terazosin treatment results in symptomatic relief and improved urinary flow in patients with and without bladder outlet obstruction, and in significant improvement in patients with urodynamically proved obstruction."( Urodynamic and clinical effects of terazosin therapy in patients with symptomatic benign prostatic hyperplasia.
de La Rosette, JJ; de Wildt, MJ; Debruyne, FM; Rosier, FW; van Iersel, MP; Witjes, WP, 1996
)
2.01
"Terazosin treatment resulted in significant changes in flow rate and residual urine, however, changes in flow rates were not influenced by prostate size, while a marked decrease in residual urine was found in patients with large prostates."( Influence of prostate size on terazosin efficacy.
Becopoulos, T; Christofis, I; Mitropoulos, D, 1997
)
1.31
"The terazosin treatment groups received 1.5 mg of terazosin hydrochloride twice daily either orally or subcutaneously while the rest received a saline solution placebo either orally or subcutaneously for the last 4 weeks of the study."( Terazosin blockade of nicotine-induced skin flap necrosis in the rat.
Karien, RG; Maisel, RH, 1997
)
2.22
"Terazosin treatment did not show consistent decrease of casual BP, but was associated with a transient decrease of systolic BP and an increase of pulse rate after standing, and enhanced postprandial decrease in BP."( Comparative efficacies of a calcium antagonist and an alpha1 blocker in elderly hypertensive patients with stroke.
Abe, I; Fujishima, M; Hasuo, Y; Nishino, Y; Onaka, U; Setoguchi, M, 1998
)
1.02
"Terazosin is a safe treatment for BPH in normotensive and hypertensive men, including men who are already taking additional antihypertensive drugs."( Terazosin in benign prostatic hyperplasia: effects on blood pressure in normotensive and hypertensive men.
Kirby, RS, 1998
)
3.19
"Terazosin treatment was associated with an increase in the peak flow rate of 1.4 mL/s (95% confidence interval [1.0, 1.7]) compared with placebo."( Meta-analysis of randomized trials of terazosin in the treatment of benign prostatic hyperplasia.
Boyle, P; Manski, R; Padley, RJ; Robertson, C; Roehrborn, CG, 2001
)
1.3
"Terazosin treatment, even 2 mg. "( Urodynamic effects of terazosin treatment for Japanese patients with symptomatic benign prostatic hyperplasia.
Furuya, S; Itoh, N; Masumori, N; Ogura, H; Sato, Y; Takahashi, A; Tanaka, Y; Tsukamoto, T, 2002
)
2.07
"All terazosin treatment groups exhibited significantly greater decreases in total Boyarsky symptom score than the placebo group."( A randomized, placebo-controlled multicenter study of the efficacy and safety of terazosin in the treatment of benign prostatic hyperplasia.
Auerbach, S; Leifer, G; Lepor, H; Lowe, F; Madsen, P; Moon, T; Narayan, P; Puras-Baez, A; Soloway, M, 1992
)
0.99
"All terazosin treatment groups showed dramatic improvement in obstructive symptoms when compared with the placebo group, but these differences were not statistically significant because of the small numbers of patients in each group."( Terazosin in the treatment of benign prostatic hyperplasia: a multicentre, placebo-controlled trial.
Buckley, JF; Chilton, CP; Ibrahim, I; Kaisary, AV; Kirk, D; Lloyd, SN, 1992
)
2.21
"Terazosin-treated patients (n = 43) had significant mean decreases from the baseline in supine BP (systolic/diastolic = -8.8/-8.5 mm Hg) and standing BP (-10.9/-9.5 mm Hg), whereas the decreases in BP in the placebo-treated patients (n = 49; supine, -2.3/-2.6 mm Hg; standing, -1.4/-1.3 mm Hg) were not significant."( Concomitant administration of terazosin and atenolol for the treatment of essential hypertension.
Holtzman, JL; Kaihlanen, PM; Lewin, AJ; Oberlin, JA; Rider, JA; Spindler, JS, 1988
)
1.28
"Treatment with terazosin, an FDA-approved compound with a known non-canonical action of increasing PGK1 activity, also improved these phenotypes."( Targeting phosphoglycerate kinase 1 with terazosin improves motor neuron phenotypes in multiple models of amyotrophic lateral sclerosis.
Becker, CG; Becker, T; Carroll, E; Chaytow, H; Faller, KME; Gillingwater, TH; Gordon, D; Huang, YT; Smith, HL; Talbot, K; van der Hoorn, D, 2022
)
1.33
"Mice treated with terazosin had a significant decrease in serum creatinine, urinary Kim-1 levels, HIF-1α, apoptosis, and downstream Adrab1 genes including Ece1, Edn1, pMAPK14 with increased cell proliferation."( Identification of novel therapeutic targets for contrast induced acute kidney injury (CI-AKI): alpha blockers as a therapeutic strategy for CI-AKI.
Cai, C; Kilari, S; Misra, S; Sharma, A; Simeon, M; Singh, A; van Wijnen, AJ; Zhao, C, 2021
)
0.94
"Co-treatment with terazosin resulted in the genistein-induced arrest of DU-145 cells in G2/M phase being overridden and an increase in apoptotic cells, as evidenced by procaspase-3 activation and PARP cleavage."( Combined effects of terazosin and genistein on a metastatic, hormone-independent human prostate cancer cell line.
Chang, KL; Cheng, HL; Chih, TT; Hsieh, BS; Hu, YC; Huang, LW; Shyu, HW; Su, SJ, 2009
)
1
"Pre-treatment with terazosin blocked vasoconstrictor responses to increasing doses of methoxamine, and also blocked vasodilatation several mm from the site of terazosin and methoxamine administration."( Alpha-1 adrenoceptor stimulation triggers axon-reflex vasodilatation in human skin.
Drummond, PD, 2009
)
0.67
"Pretreatment with terazosin (10 mg/kg ip) significantly reduced the initial increase in MAP to 12 +/- 6 mmHg, whereas MAP for the last 45 min was superimposable on control values."( Sympathetic and angiotensin-dependent hypertension during cage-switch stress in mice.
Brands, MW; Lee, DL; Webb, RC, 2004
)
0.65
"Treatment with terazosin can reduce patients' episodes of nocturia both subjectively and objectively in some men with LUTS. "( alpha-blocker monotherapy in the treatment of nocturia in men with lower urinary tract symptoms: a prospective study of response prediction.
Kim, SW; Ku, JH; Paick, JS; Shin, JW; Yang, JH, 2006
)
0.69
"Treatment with terazosin was initiated with 1 mg daily for 3 days, followed by 2 mg daily for 25 days."( The Hytrin Community Assessment Trial study: a one-year study of terazosin versus placebo in the treatment of men with symptomatic benign prostatic hyperplasia. HYCAT Investigator Group.
Auerbach, S; Kaplan, SA; Lloyd, LK; Milam, DE; Oesterling, JE; Padley, RJ; Roehrborn, CG, 1996
)
0.87
"Treatment with terazosin has a beneficial effect on BPH, continuing for at least 12 months, and can be safely considered for medium- to long-term use in those who benefit."( The international terazosin trial: a multicentre study of the long-term efficacy and safety of terazosin in the treatment of benign prostatic hyperplasia. The ITT Group.
Debruyne, FM; Fitzpatrick, J; Kirby, R; Kirk, D; Prezioso, D; Witjes, WP, 1996
)
0.98

Toxicity

The dose of terazosin was titrated to 5 mg/day over a one-month interval, provided significant adverse drug reactions were not observed. Dizziness, headache, and asthenia were the most commonly reported adverse experiences. The incidence of headache in placebo-controlled trials was not significantly different between the terzosin and placebo groups.

ExcerptReferenceRelevance
" during a 1-month period provided adverse reactions and orthostatic hypotension were not observed."( The safety, efficacy and compliance of terazosin therapy for benign prostatic hyperplasia.
Knapp-Maloney, G; Lepor, H; Meretyk, S, 1992
)
0.55
"Selected adverse events were evaluated from the combined randomized placebo-controlled clinical trials (once-a-day or twice-a-day; monotherapy or combination therapy) of terazosin in hypertensive patients."( Effect of age and dose on the incidence of adverse events in the treatment of hypertension in patients receiving terazosin.
Hosmane, BS; Jordan, DC; Laddu, A; Maurath, CJ, 1992
)
0.69
" Once daily administration of terazosin proved to be safe and effective in reducing the blood pressure of patients with mild-moderate essential hypertension and favourably reduced the total plasma cholesterol level."( A multicentre, hospital study of the efficacy and safety of terazosin and its effects on the plasma cholesterol levels of patients with untreated essential hypertension.
Coles, S; Lytle, T; Waite, MA, 1991
)
0.81
" In this article the pharmacokinetics of terazosin are reviewed, and the incidence of adverse events in a dose-response study and a meta-analysis of 20 placebo-controlled trials involving a total of 1814 patients is presented."( Terazosin: pharmacokinetics and the effect of age and dose on the incidence of adverse events.
Achari, R; Laddu, AR; Somberg, JC, 1991
)
1.99
" Most adverse events were mild or moderate in severity."( Long-term efficacy and safety of terazosin alone and in combination with other antihypertensive agents.
Cohen, JD, 1991
)
0.56
" Once daily administration of terazosin, either as monotherapy or in combination with other antihypertensive agents, proved to be safe and effective in reducing the blood pressure of patients with uncontrolled mild-moderate essential hypertension and favourably reduced the total plasma cholesterol level."( A multicentre, hospital study of the efficacy and safety of terazosin and its effects on the plasma cholesterol levels of patients with essential hypertension.
Coles, SJ; Lytle, TB; Waite, MA, 1991
)
0.81
" The present review of terazosin in males with symptomatic BPH supports the following conclusions: (1) the dose of terazosin can be safely titrated to 10 mg in normotensive and hypertensive patients with symptomatic BPH; (2) the adverse events associated with doses of terazosin up to 10 mg are relatively mild and reversible; and (3) the improvements in the outcome parameters (symptom scores and urinary flow rates) are clinically and statistically significant."( The efficacy and safety of terazosin for the treatment of symptomatic BPH.
Henry, D; Laddu, AR; Lepor, H, 1991
)
0.89
" The dose of terazosin was titrated to 5 mg/day over a one-month interval, provided significant adverse drug reactions were not observed."( The safety and efficacy of terazosin for the treatment of benign prostatic hyperplasia.
Knapp-Maloney, G; Lepor, H; Wozniak-Petrofsky, J, 1989
)
0.94
" Similar numbers of patients in all three groups reported adverse experiences of a subjective nature."( Comparison of the safety and efficacy of once-daily terazosin versus twice-daily prazosin for the treatment of mild to moderate hypertension.
Deger, G, 1986
)
0.52
" Dizziness, headache, and asthenia were the most commonly reported adverse experiences among all terazosin-treated patients, although the incidence of headache in placebo-controlled trials was not significantly different between the terazosin and placebo groups."( Overall safety of terazosin as an antihypertensive agent.
Glassman, HN; Jordan, DC; Luther, RR; Sperzel, WD, 1986
)
0.82
" Adverse effects were mild."( Efficacy and safety of intravenous terazosin in hypertensive patients. A preliminary report.
Cohen, A, 1986
)
0.55
" Under these conditions the LD50 was 277 mg/kg for males and 293 mg/kg for females."( Terazosin: intravenous safety evaluation in rats.
Cusick, PK; Fort, FL; Heyman, IA; Kesterson, JW; Majors, K; Tekeli, S, 1984
)
1.71
" The most common adverse events resulting in premature termination from the study were dizziness (6."( Long-term efficacy and safety of terazosin in patients with benign prostatic hyperplasia. Terazosin Research Group.
Lepor, H, 1995
)
0.57
" Parameters evaluated included Boyarsky symptom score (Sx), peak uroflow (Qmax), blood pressure and occurrence of adverse events."( Terazosin and doxazosin in normotensive men with symptomatic prostatism: a pilot study to determine the effect of dosing regimen on efficacy and safety.
Kaplan, SA; Olsson, CA; Soldo, KA, 1995
)
1.73
" Only 11 patients withdrew because of an adverse event, 7 in the terazosin and 4 in the placebo group."( A multicenter, randomized, double-blind, placebo-controlled study to evaluate the safety and efficacy of terazosin in the treatment of benign prostatic hyperplasia.
Barkin, J; Beland, G; Boake, RC; Casey, RW; Elhilali, MM; Fradet, Y; Klotz, LH; Orovan, WL; Ramsey, EW; Schick, E; Trachtenberg, J, 1996
)
0.75
"Overall, this study showed terazosin to be safe and effective in relieving the signs and symptoms of BPH and should be considered as a treatment alternative."( A multicenter, randomized, double-blind, placebo-controlled study to evaluate the safety and efficacy of terazosin in the treatment of benign prostatic hyperplasia.
Barkin, J; Beland, G; Boake, RC; Casey, RW; Elhilali, MM; Fradet, Y; Klotz, LH; Orovan, WL; Ramsey, EW; Schick, E; Trachtenberg, J, 1996
)
0.8
" The most common adverse event resulting in premature termination from the study was dizziness."( The international terazosin trial: a multicentre study of the long-term efficacy and safety of terazosin in the treatment of benign prostatic hyperplasia. The ITT Group.
Debruyne, FM; Fitzpatrick, J; Kirby, R; Kirk, D; Prezioso, D; Witjes, WP, 1996
)
0.63
"We determined the mechanism of adverse events associated with alpha1-blockers for treating benign prostatic hyperplasia (BPH)."( The mechanism of adverse events associated with terazosin: an analysis of the Veterans Affairs cooperative study.
Jones, K; Lepor, H; Williford, W, 2000
)
0.56
" Adverse events were captured at all study visits during our 1-year study."( The mechanism of adverse events associated with terazosin: an analysis of the Veterans Affairs cooperative study.
Jones, K; Lepor, H; Williford, W, 2000
)
0.56
" Of these adverse events only postural hypotension was associated with orthostatic blood pressure changes."( The mechanism of adverse events associated with terazosin: an analysis of the Veterans Affairs cooperative study.
Jones, K; Lepor, H; Williford, W, 2000
)
0.56
"Dizziness and asthenia are not associated with changes in blood pressure, suggesting that these treatment related adverse events associated with alpha1-blockers are not related to vascular events."( The mechanism of adverse events associated with terazosin: an analysis of the Veterans Affairs cooperative study.
Jones, K; Lepor, H; Williford, W, 2000
)
0.56
" No unknown adverse reactions were observed in either groups, and the drugs were shown to be highly safe."( [The efficacy and safety of terazosin and tamsulosin in patients with urinary disturbance accompanying prostatic hypertrophy].
Fujioka, T; Goto, Y; Isurugi, K; Katoh, T; Numasato, S; Obara, W; Omori, S; Suzuki, Y, 2001
)
0.6
"Using claims data from a large Medigap plan, we examined the effect of initiating nonselective alpha1-antagonist therapy on the incidence of hypotension-related adverse events likely to be associated with vascular alpha-adrenoreceptor antagonism in patients with BPH."( Initiation of nonselective alpha1-antagonist therapy and occurrence of hypotension-related adverse events among men with benign prostatic hyperplasia: a retrospective cohort study.
Chao, J; Chrischilles, E; Gilden, D; Kreder, KJ; Rubenstein, L; Shah, H, 2001
)
0.31
" We examined the rate of possible hypotension-related adverse events (diagnosis codes for hypotension, syncope, dizziness, fractures, and other injuries) per 10,000 person-days for men who began therapy with alpha1 antagonists and for a random sample of nonusers, stratified by prior use of other antihypertensive agents."( Initiation of nonselective alpha1-antagonist therapy and occurrence of hypotension-related adverse events among men with benign prostatic hyperplasia: a retrospective cohort study.
Chao, J; Chrischilles, E; Gilden, D; Kreder, KJ; Rubenstein, L; Shah, H, 2001
)
0.31
" Thus, terazosine (setegis) is effective and safe in BPH patients with cardiovascular disease."( [Clinical efficacy and safety of terazosine (setegis) in patients with benign prostatic hyperplasia with concomitant cardiovascular diseases].
Bychkova, NV; Gurevich, MA; Pozdniakov, KV; Tazina, SIa; Trapeznikova, MF,
)
0.87
"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 primary objectives of the treatment for the lower urinary tract symptoms (LUTS) associated with benign prostatic hyperplasia (BPH) are to produce rapid, sustained, and safe improvements in the symptoms that affect the quality of life in the majority of men over 50."( Efficacy and safety of combined therapy with terazosin and tolteradine for patients with lower urinary tract symptoms associated with benign prostatic hyperplasia: a prospective study.
Li, HZ; Wang, W; Xiao, H; Yang, Y; Zhang, X; Zhang, Y; Zhao, XF, 2007
)
0.6
" The incidence of adverse effects in the combination group was higher than that in the terazosin group."( Efficacy and safety of combined therapy with terazosin and tolteradine for patients with lower urinary tract symptoms associated with benign prostatic hyperplasia: a prospective study.
Li, HZ; Wang, W; Xiao, H; Yang, Y; Zhang, X; Zhang, Y; Zhao, XF, 2007
)
0.82
" This study, although short term and limited numbers of patients, provides evidence that the combined therapy with terazosin plus tolterodine is a good approach for meeting the objectives of rapid, sustained, and safe improvements in the LUTS associated with BPH."( Efficacy and safety of combined therapy with terazosin and tolteradine for patients with lower urinary tract symptoms associated with benign prostatic hyperplasia: a prospective study.
Li, HZ; Wang, W; Xiao, H; Yang, Y; Zhang, X; Zhang, Y; Zhao, XF, 2007
)
0.81
" Prazosin prevented hepatotoxicity when administered 1 h before a toxic paracetamol insult and importantly, when administered up to 1 h post paracetamol injection."( alpha(1)-Adrenoceptor antagonists prevent paracetamol-induced hepatotoxicity in mice.
Kitteringham, NR; Macdonald, I; Park, BK; Randle, LE; Sathish, JG; Williams, DP, 2008
)
0.35

Pharmacokinetics

Prazosin and terazosin are two alpha 1-adrenoceptor blocking agents. Their principal difference is the longer half-life of terazOSin. The relatively long half- life of terzosin enables it to be administered in a once-a-day regimen.

ExcerptReferenceRelevance
" The relatively long half-life of terazosin (12 hours) enables it to be administered in a once-a-day regimen."( Terazosin: pharmacokinetics and the effect of age and dose on the incidence of adverse events.
Achari, R; Laddu, AR; Somberg, JC, 1991
)
2
"Prazosin and terazosin are two alpha 1-adrenoceptor blocking agents, their principal difference being the longer half-life of terazosin."( Effect of age on pharmacokinetics of and blood pressure responses to prazosin and terazosin.
Conway, EL; Drummer, OH; Louis, WJ; McNeil, JJ; Workman, BS, 1987
)
0.87
" However, recent studies have shown that it has substantial antihypertensive efficacy with minimal side effects at low doses, and that half-life is long enough to allow twice daily administration."( Comparison of pharmacokinetics and pharmacodynamics of adrenoceptor agonists and antagonists as antihypertensive agents.
Anavekar, SN; Conway, EL; Drummer, OH; Howes, LG; Jarrott, B; Louis, WJ; McNeil, JJ; Workman, B, 1987
)
0.27
" The mean beta-phase half-life is approximately 12 hours."( Pharmacokinetics of terazosin.
Sonders, RC, 1986
)
0.59
" The plasma half-life of terazosin in patients with normal renal function was 10."( Influence of renal insufficiency on the pharmacokinetics and pharmacodynamics of terazosin.
Chauveau, P; Ganeval, D; Jungers, P; Pertuiset, N, 1986
)
0.8
"Terazosin is a post-synaptic alpha 1-adrenoceptor antagonist with a similar pharmacodynamic profile to prazosin."( Terazosin. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in essential hypertension.
Monk, JP; Titmarsh, S, 1987
)
3.16
" For both routes of administration, the only pharmacokinetic variables significantly correlated with age were terminal elimination rate constant and the area under the plasma concentration-time curve (AUC)."( Effect of age on the pharmacokinetics of orally and intravenously administered terazosin.
Glassman, HN; Jordan, DC; Luther, RR; Sennello, LT; Sonders, RC; Tolman, KG, 1988
)
0.5
"alpha-Blockers and calcium antagonists are commonly used in the treatment of hypertension, but few data are available concerning first dose or steady state (SS) hemodynamic and pharmacokinetic effects of these drugs when they are used in combination therapy."( Combined terazosin and verapamil therapy in essential hypertension. Hemodynamic and pharmacokinetic interactions.
Johnston, W; Laddu, AR; Lenz, ML; Pool, JL; Taylor, AA; Varghese, A, 1995
)
0.71
" Multiple-dose coadministration of terazosin and finasteride did not alter the central values of steady-state pharmacokinetic parameters of either drug in a statistically significant manner."( Assessment of the pharmacokinetic-pharmacodynamic interaction between terazosin and finasteride.
Cavanaugh, J; Eason, C; Granneman, GR; Hosmane, B; Locke, C; Samara, EE, 1996
)
0.8
"A radioreceptor assay has been developed for alpha1-adrenoceptor subtypes and applied to a pharmacokinetic analysis of tamsulosin and terazosin."( Radioreceptor assay analysis of tamsulosin and terazosin pharmacokinetics.
Michel, MC; Schäfers, RF; Taguchi, K, 1998
)
0.76
" The aim of this study was to assess the potential pharmacokinetic interaction of doxazosin or terazosin when coadministered with finasteride."( Pharmacokinetic interaction between finasteride and terazosin, but not finasteride and doxazosin.
Chung, M; Hilbert, J; Lawrence, V; Phillips, K; Vashi, V, 1998
)
0.77
" The present HPLC method was successful for the pharmacokinetic study of terazosin in healthy volunteers."( High-performance liquid chromatographic analysis and pharmacokinetics of terazosin in healthy volunteers.
Kang, BC; Rhee, JE; Shin, WG; Suh, OK; Yang, CQ, 2001
)
0.77
" Therefore, this study was performed with DA-8159 (a long acting PDE 5 inhibitor) and terazosin in rats to find whether or not pharmacokinetic and pharmacodynamic interactions between the two drugs were observed."( Pharmacokinetic and pharmacodynamic consequences of inhibition of terazosin metabolism via CYP3A1 and/or 3A2 by DA-8159, an erectogenic, in rats.
Bae, SK; Kwon, JW; Lee, DC; Lee, MG; Oh, EY; You, M, 2007
)
0.8
"A rational drug discovery process was initiated to design a potent and prostate-selective alpha1(L)-adrenoceptor antagonist with pharmacokinetic properties suitable for once a day administration after oral dosing, for the treatment of benign prostatic hyperplasia."( Impact of physicochemical and structural properties on the pharmacokinetics of a series of alpha1L-adrenoceptor antagonists.
Atkinson, F; Beaumont, K; Betts, A; Fox, D; Gardner, I; Morgan, P; Webster, R, 2007
)
0.34
" Pharmacokinetic and pharmacodynamic modeling were performed subject by subject."( Pharmacokinetic and pharmacodynamic modelling of arterial haemodynamic effects of terazosin in healthy volunteers.
Azanza, JR; Campanero, MA; Muñoz-Juarez, MJ; Quetglas, EG; Sádaba, B, 2008
)
0.57
" 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

Compound-Compound Interactions

This open, multicenter phase III study was designed to assess the efficacy and long-term safety of terazosin (1 to 40 mg/day), alone or in combination with other antihypertensive drugs.

ExcerptReferenceRelevance
"This open, multicenter phase III study was designed to assess the efficacy and long-term safety of terazosin (1 to 40 mg/day), alone or in combination with other antihypertensive drugs, in 364 patients with mild to moderate essential hypertension."( Long-term efficacy and safety of terazosin alone and in combination with other antihypertensive agents.
Cohen, JD, 1991
)
0.78
"The short-term antihypertensive efficacy and safety of terazosin when administered with a diuretic were assessed in three randomized, double-blind, placebo-controlled studies."( Cumulative experience with terazosin administered in combination with diuretics.
Rudd, P, 1986
)
0.82
"In a randomized, double-blind, placebo-controlled, multicenter trial, the efficacy and safety of terazosin in combination with other antihypertensive agents were assessed using patients with inadequately controlled essential hypertension (supine diastolic blood pressure 95 mm Hg or greater)."( Experience with terazosin administered in combination with other antihypertensive agents.
Chrysant, SG, 1986
)
0.83
"To investigate the effects of amlodipine, a dihydropyridine calcium-channel blocker, alone or combined with terazosin, on urodynamics in rats with benign prostatic hyperplasia (BPH) and in female rats with detrusor instability (DI)."( Amlodipine alone or combined with terazosin improves lower urinary tract disorder in rat models of benign prostatic hyperplasia or detrusor instability: focus on detrusor overactivity.
Chen, GL; Liu, HP; Liu, P; Xu, XP, 2009
)
0.84
" The rats were intragastrically administered with assigned drugs (amlodipine, terazosin or both combined) for 14 days in three experiments."( Amlodipine alone or combined with terazosin improves lower urinary tract disorder in rat models of benign prostatic hyperplasia or detrusor instability: focus on detrusor overactivity.
Chen, GL; Liu, HP; Liu, P; Xu, XP, 2009
)
0.86
"Amlodipine alone or combined with terazosin might have the potential to alleviate lower urinary tract symptoms (LUTS)."( Amlodipine alone or combined with terazosin improves lower urinary tract disorder in rat models of benign prostatic hyperplasia or detrusor instability: focus on detrusor overactivity.
Chen, GL; Liu, HP; Liu, P; Xu, XP, 2009
)
0.91
"Amlodipine alone or combined with terazosin can improve the PVR of the LUTS patient effectively, but had no significant difference compared with terazosin."( [Amlodipine combined with terazosin reduces postvoid residual and the risk of acute urinary retention].
Fang, J; Li, YL; Liu, HP; Qin, XH; Xu, XP; Yang, C; Zhang, X, 2009
)
0.93
"This study aimed to explore the effect of terazosin hydrochloride combined with interventional embolisation on prostate volume and quality of life (QOL) of elderly patients with prostatic hyperplasia (PH)."( Effect of Terazosin Hydrochloride Combined with Interventional Embolisation on Prostate Volume and Quality of Life of Elderly Patients with Prostatic Hyperplasia.
Liu, N; Su, C; Xue, J, 2023
)
1.58
" Based on different treatment regimens, 89 patients who received interventional embolisation alone were included in the control group (CG), and 86 patients undergoing interventional embolisation combined with terazosin hydrochloride were included in the study group (SG)."( Effect of Terazosin Hydrochloride Combined with Interventional Embolisation on Prostate Volume and Quality of Life of Elderly Patients with Prostatic Hyperplasia.
Liu, N; Su, C; Xue, J, 2023
)
1.5
"Terazosin hydrochloride combined with interventional embolisation overtly reduces the prostate volume and improves the clinical symptoms of patients with fewer side effects, which has a certain clinical application value."( Effect of Terazosin Hydrochloride Combined with Interventional Embolisation on Prostate Volume and Quality of Life of Elderly Patients with Prostatic Hyperplasia.
Liu, N; Su, C; Xue, J, 2023
)
2.76

Bioavailability

ExcerptReferenceRelevance
" Pharmacokinetic interactions, including an increase in the bioavailability of T when V was added, did not correlate with the degree of orthostasis."( Combined terazosin and verapamil therapy in essential hypertension. Hemodynamic and pharmacokinetic interactions.
Johnston, W; Laddu, AR; Lenz, ML; Pool, JL; Taylor, AA; Varghese, A, 1995
)
0.71
"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
" While many of the compounds tested displayed poor pharmacokinetics, compound 48 was found to have adequate bioavailability (>20%) and half-life (>6 h) in both rats and dogs."( In vitro and in vivo evaluation of dihydropyrimidinone C-5 amides as potent and selective alpha(1A) receptor antagonists for the treatment of benign prostatic hyperplasia.
Barrish, A; Barrow, JC; Broten, TP; Chang, RS; Ellis, JD; Forray, C; Freidinger, RM; Gilbert, KF; Glass, KL; Homnick, CF; Kassahun, K; Kling, P; Leppert, P; Nagarathnam, D; Nantermet, PG; O'Malley, SS; Olah, TV; Ransom, RW; Reiss, D; Rittle, KE; Schorn, TW; Selnick, HG; Steele, TG, 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
"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

Dosage Studied

Terazosin is generally well tolerated, but caution is recommended at treatment initiation and when dosage adjustments are made due to an increased risk of postural hypotension.

ExcerptRelevanceReference
" The daily dosage of terazosin was titrated to 5 mg over a 2-week interval."( The relative efficacy of terazosin versus terazosin and flutamide for the treatment of symptomatic BPH.
Lepor, H; Machi, G, 1992
)
0.91
" In this article the pharmacokinetics of terazosin are reviewed, and the incidence of adverse events in a dose-response study and a meta-analysis of 20 placebo-controlled trials involving a total of 1814 patients is presented."( Terazosin: pharmacokinetics and the effect of age and dose on the incidence of adverse events.
Achari, R; Laddu, AR; Somberg, JC, 1991
)
1.99
" The aim of this multicenter study, performed in 256 patients with mild to moderate essential hypertension, was to define the dosing characteristics of terazosin (in the range of 1 to 80 mg) administered once daily."( Antihypertensive dose-response relationships: studies with the selective alpha 1-blocking agent terazosin.
Cheung, DG; Laddu, AR; Luther, RR; Weber, MA, 1991
)
0.7
" Unlike prazosin, the terminal-phase plasma half-life is long, at approximately 12 h, and effective blood pressure control is usually achieved with a once-daily dosing regimen."( Terazosin: a new antihypertensive agent with favorable effects on lipids.
Luther, RR, 1989
)
1.72
" The dose of terazosin was titrated over 2 weeks to a maintenance dosage of 10 mg once daily for 4 weeks."( Antihypertensive therapy with once-daily administration of terazosin, a new alpha 1-adrenergic-receptor blocker.
Abraham, PA; Halstenson, CE; Keane, WF; Matzke, GR; Napier, JL,
)
0.74
" Although equally efficacious in spontaneously hypertensive rats as its congener prazosin, terazosin exhibited a more gradual onset of action than prazosin, a more uniform and linear dose-response curve, and a less variable duration of action."( Pharmacology of terazosin.
Kyncl, JJ, 1986
)
0.84
" In the fixed-dose studies, titration continued until a predetermined dosage level of terazosin or corresponding placebo was reached."( Terazosin: an effective once-daily monotherapy for the treatment of hypertension.
Dauer, AD, 1986
)
1.94
" Doses of study medications were administered twice daily and were increased at weekly intervals until the average supine diastolic blood pressure was 90 mm Hg or less, with a decrease from baseline of at least 10 mm Hg, or until the maximum specified dosage of a given study drug was reached."( Comparative trials of terazosin with other antihypertensive agents.
Ruoff, G, 1986
)
0.59
" In this study, the dosage of medication was titrated until a satisfactory decrease in supine diastolic blood pressure was obtained, or until the maximum daily dosage (20 mg) was reached."( Effect of terazosin on serum lipids.
Deger, G, 1986
)
0.67
" The results of this study indicate that terazosin may be safely administered to patients with renal insufficiency without altering the usual dosing regimen."( Influence of renal insufficiency on the pharmacokinetics and pharmacodynamics of terazosin.
Chauveau, P; Ganeval, D; Jungers, P; Pertuiset, N, 1986
)
0.76
" Doses of 2, 5, and 10 mg were examined in sequence over 3 days to define dose-response characteristics."( The hemodynamic and clinical responses to terazosin, a new alpha blocking agent, in congestive heart failure.
Huss, P; Leier, CV; Parrish, D; Patterson, SE; Unverferth, DV, 1986
)
0.54
" This allows once daily dosing of terazosin and a potential advantage in ensuring patient compliance to treatment."( Terazosin: a new long-acting alpha 1-adrenergic antagonist for hypertension.
Eisen, G; Frishman, WH; Lapsker, J, 1988
)
2
" From these data, we conclude that the dosage of terazosin does not need to be adjusted on the basis of age alone; the dose of terazosin is titrated in all patients to the lowest effective dose that is well tolerated."( Effect of age on the pharmacokinetics of orally and intravenously administered terazosin.
Glassman, HN; Jordan, DC; Luther, RR; Sennello, LT; Sonders, RC; Tolman, KG, 1988
)
0.76
" When administered daily for 1 month at dosages of 0, 10, 40 or 150 mg/kg/day, the no-toxic-effect dosage was 40 mg/kg/day."( Terazosin: intravenous safety evaluation in rats.
Cusick, PK; Fort, FL; Heyman, IA; Kesterson, JW; Majors, K; Tekeli, S, 1984
)
1.71
"Terazosin or placebo once daily, with terazosin dosage titrated to the patient's response."( Terazosin in the treatment of benign prostatic hyperplasia. Terazosin Benign Prostatic Hyperplasia Study Group.
Adams, G; Brawer, MK; Epstein, H, 1993
)
3.17
" Dosage was started at 1 mg/d and increased as tolerated to 2, 5, and 10 mg/d over the test period."( Effect of terazosin on urine storage and voiding in the aging male with prostatism.
Bottaccini, MR; Gleason, DM, 1994
)
0.69
" Terazosin is generally well tolerated, but caution is recommended at treatment initiation and when dosage adjustments are made due to an increased risk of postural hypotension and related adverse effects at these times; such a risk has also been observed with several other alpha 1-adrenoceptor antagonists."( Terazosin. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in benign prostatic hyperplasia.
Fitton, A; Sorkin, EM; Wilde, MI,
)
2.48
"In this pilot study, the effect of dosing schedule on the efficacy and safety of the long-acting alpha 1-adrenergic blockers, terazosin (TER) and doxazosin (DOX), was evaluated in 43 consecutive normotensive men (mean age 59."( Terazosin and doxazosin in normotensive men with symptomatic prostatism: a pilot study to determine the effect of dosing regimen on efficacy and safety.
Kaplan, SA; Olsson, CA; Soldo, KA, 1995
)
1.94
" The dosage was gradually increased to 1-2 mg twice daily, depending upon patient tolerance and a minimum acceptable systolic blood pressure of 90 mm Hg."( Efficacy and safety of terazosin to improve voiding in spinal cord injury patients.
Perkash, I, 1995
)
0.6
" Terazosin, an alpha 1-adrenergic blocking agent, was given initially at the dosage of 1 mg daily."( Terazosin: ex vivo and in vitro platelet aggregation effects in patients with arterial hypertension.
Angeli-Greaves, M; Armas Padilla, MC; Armas-Hernández, MJ; Carvajal, AR; Guerrero Pajuelo, J; Hernández Hernández, R, 1996
)
2.65
" The parallelism of the dose-response curves indicates activation of a common receptor subtype."( alpha-Adrenoceptor and opioid receptor modulation of clonidine-induced antinociception.
Miranda, HF; Naquira, D; Pinardi, G; Sierralta, F, 1996
)
0.29
"The purpose of this study was to determine the potency and selectivity of the alpha-1 adrenergic receptor antagonist terazosin based on relationships between plasma concentrations and blockade of intraurethral pressure (IUP) and mean arterial pressure (MAP) responses after single dosing and to determine cumulative effects after repeated dosing."( Relationships between pharmacokinetics and blockade of agonist-induced prostatic intraurethral pressure and mean arterial pressure in the conscious dog after single and repeated daily oral administration of terazosin.
Brune, ME; Hancock, AA; Katwala, SP; Kerwin, JF; Milicic, I; Witte, DG, 1997
)
0.69
" This retrospective analysis evaluated dosing regimens and drug acquisition costs for 101 patients identified from medical records in a large metropolitan hospital as having hypertension and/or benign prostatic hyperplasia and receiving alpha-blocker therapy with either doxazosin or terazosin."( Trends in alpha-blocker treatment of patients with benign prostatic hyperplasia and hypertension: dosing regimens and cost comparisons.
Raymond, JL; Smith, CS,
)
0.31
" Twenty-eight men (78%) were on other anti-hypertensive medication; the type and dosage were not changed during the study."( The treatment of benign prostatic hyperplasia with alpha blockers in men over the age of 80 years.
Ikeguchi, E; Kaplan, SA; Santarosa, RP; Te, AE, 1997
)
0.3
"Once-daily dosing of TAM after breakfast at a fixed dose level (0."( A double-blind comparison of terazosin and tamsulosin on their differential effects on ambulatory blood pressure and nocturnal orthostatic stress testing.
de Mey, C; McEwen, J; Michel, MC; Moreland, T, 1998
)
0.59
" After a one-week titration phase, terazosin was administered for 4 weeks at the dosage of 5 mg per day as a single dose in the evening at bedtime."( [Patterns of use of terazosine in current medical practice in ambulatory patients with obstructive and irritative obstructive disorders of urination].
Boumendil, O; Reitz, C; Rossi, D; Serment, G, 2000
)
0.91
"A double-blind, randomized, placebo-controlled, multicenter study was conducted to describe the dose-response curve for terazosin on blood pressure."( The relationship between terazosin dose and blood pressure response in hypertensive patients.
Achari, R; Bonacci, E; Hosmane, B; O'Dea, R, 2000
)
0.82
"Specific agents, such as alpha-adrenoblockers, in low dosage may be effective in women with urinary tract disorders in case of careful and comprehensive evaluation of functional BOO."( [Use of alpha1-adrenergic blockaders in voiding disorders in women].
Egorov, AA; Romikh, VV; Sivkov, AV,
)
0.13
" The improvement of lipid metabolism was related to the dosage of terazosin but not to antihypertensive effects of terazosin."( Effect of terazosin on blood pressure and serum lipids.
Cheng, L; Gong, P; Lu, Z; Tang, J; Zeng, F; Zhang, J, 1999
)
0.94
" Three decision trees for solid oral dosage forms or liquid suspensions are provided for evaluating when and how polymorphs of drug substances should be monitored and controlled in ANDA submissions."( Regulatory considerations of pharmaceutical solid polymorphism in Abbreviated New Drug Applications (ANDAs).
Adams, RC; Furness, MS; Gill, DS; Holcombe, FO; Raw, AS; Yu, LX, 2004
)
0.32
" Higher rates of twice-daily (or 2 units per day) dosing are associated with higher incremental cost-effectiveness ratios."( Cost-effectiveness of tamsulosin, doxazosin, and terazosin in the treatment of benign prostatic hyperplasia.
Chrischilles, EA; Klein, RW; Kreder, KJ; Ohsfeldt, RL,
)
0.39
"Initially a dose-response curve of phenylephrine was constructed at dose strengths of 1-16 microg/kg in a cumulative manner."( Effects of alpha-1 adrenergic receptor antagonist, terazosin, on cardiovascular functions in anaesthetised dogs.
Ahuja, VM; Fahim, M; Sharma, R, 2004
)
0.58
" The first 7-year old boy however developed some dizziness when the dose of terazosine was increased to 2 mg (after 4 weeks of administrating 1 mg), and this disappeared immediately when the dosage was reduced back to 1 mg daily."( The use and rationale of selective alpha blockade in children with non-neurogenic neurogenic bladder dysfunction.
Beckers, G; Bogaert, G; Lombaerts, R,
)
0.36
" Meanwhile the number of pain episodes, analgesic dosage and the number of days for spontaneous passage of the calculi through the ureter were also recorded."( The comparison and efficacy of 3 different alpha1-adrenergic blockers for distal ureteral stones.
Basar, H; Basar, MM; Batislam, E; Ferhat, M; Tuglu, D; Yilmaz, E, 2005
)
0.33
" In conclusion, the prediction of alpha(1)-adrenoceptor occupancy in the human prostate by alpha(1)-adrenoceptor antagonists may provide the rationale for the optimum dosage regimen of these drugs in the therapy of BPH."( Prediction of alpha1-adrenoceptor occupancy in the human prostate from plasma concentrations of silodosin, tamsulosin and terazosin to treat urinary obstruction in benign prostatic hyperplasia.
Kagawa, Y; Kato, Y; Kawabe, K; Okura, T; Yamada, S, 2007
)
0.55
" All treatments were given by mouth once daily (bedtime) at an initial dosage of 2 mg/d for the first 2 weeks."( Effects of branded versus generic terazosin hydrochloride in adults with benign prostatic hyperplasia: a randomized, open-label, crossover study in Taiwan.
Lan, SK; Ou, JH; Tsai, YS; Tzai, TS, 2007
)
0.62
" Mean analgesic dosage per patient in groups 1, 2, and 3 were 231, 256, and 347 mg, respectively."( Efficacy of an alpha1 blocker in expulsive therapy of lower ureteral stones.
Chang, CH; Huang, SW; Wang, CJ, 2008
)
0.35
" The doses used in this study are in lower and nontoxic anticancer dosage range, suggesting this combination has potential for therapeutic use."( Combined effects of terazosin and genistein on a metastatic, hormone-independent human prostate cancer cell line.
Chang, KL; Cheng, HL; Chih, TT; Hsieh, BS; Hu, YC; Huang, LW; Shyu, HW; Su, SJ, 2009
)
0.68
" The number of colic episodes, lower urinary tract symptoms, analgesic dosage and days for spontaneous passage of the stones through the ureter were recorded by diary."( Adjunctive medical therapy with an alpha-1A-specific blocker after shock wave lithotripsy of lower ureteral stones.
Chang, CH; Huang, SW; Wang, CJ, 2009
)
0.35
"Administration of an alpha-1A-specific blocker reduced analgesic dosage and colic episodes after SWL of lower ureteral stones."( Adjunctive medical therapy with an alpha-1A-specific blocker after shock wave lithotripsy of lower ureteral stones.
Chang, CH; Huang, SW; Wang, CJ, 2009
)
0.35
" The number of pain episodes, analgesic dosage and the number of days of spontaneous passage of the calculi through the ureter were also recorded."( Efficacy of three different alpha 1-adrenergic blockers and hyoscine N-butylbromide for distal ureteral stones.
Canat, L; Caskurlu, T; Gurbuz, MC; Kilic, M; Polat, H,
)
0.13
"A highly sensitive, cheap, simple and accurate spectrofluorimetric method has been developed and validated for the determination of alfuzosin hydrochloride and terazosin hydrochloride in their pharmaceutical dosage forms and in human plasma."( Utility of Hantzsch reaction for development of highly sensitive spectrofluorimetric method for determination of alfuzosin and terazosin in bulk, dosage forms and human plasma.
Hammad, MA; Omar, MA; Salman, BI, 2017
)
0.86
"A new, selective and sensitive spectrofluorimetric method was designed for the quantitation of doxazosin (DOX), terazosin (TER) and alfuzosin (ALF) in their dosage forms and human plasma."( An efficient spectrofluorimetric method adopts doxazosin, terazosin and alfuzosin coupling with orthophthalaldehyde: Application in human plasma.
Derayea, SM; Hammad, MA; Mohamed, AA; Mohamed, AI; Omar, MA, 2018
)
0.94
" Additional dose-response analyses were carried out."( Association of Glycolysis-Enhancing α-1 Blockers With Risk of Developing Parkinson Disease.
Liu, L; Narayanan, NS; Pottegård, A; Simmering, JE; Welsh, MJ, 2021
)
0.62
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (3)

RoleDescription
antineoplastic agentA substance that inhibits or prevents the proliferation of neoplasms.
antihypertensive agentAny drug used in the treatment of acute or chronic vascular hypertension regardless of pharmacological mechanism.
alpha-adrenergic antagonistAn agent that binds to but does not activate alpha-adrenergic receptors thereby blocking the actions of endogenous or exogenous alpha-adrenergic agonists. alpha-Adrenergic antagonists are used in the treatment of hypertension, vasospasm, peripheral vascular disease, shock, and pheochromocytoma.
[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 (4)

ClassDescription
quinazolinesAny organic heterobicyclic compound based on a quinazoline skeleton and its substituted derivatives.
piperazines
furansCompounds containing at least one furan ring.
primary amino compoundA compound formally derived from ammonia by replacing one hydrogen atom by an organyl group.
[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 (55)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Beta-lactamaseEscherichia coli K-12Potency35.48130.044717.8581100.0000AID485294
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency0.63100.177814.390939.8107AID2147
LuciferasePhotinus pyralis (common eastern firefly)Potency37.93300.007215.758889.3584AID588342
acid sphingomyelinaseHomo sapiens (human)Potency25.118914.125424.061339.8107AID504937
thioredoxin reductaseRattus norvegicus (Norway rat)Potency40.86850.100020.879379.4328AID488772; AID588453; AID588456
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency28.18380.011212.4002100.0000AID1030
EWS/FLI fusion proteinHomo sapiens (human)Potency33.17340.001310.157742.8575AID1259253
glucocerebrosidaseHomo sapiens (human)Potency3.98110.01268.156944.6684AID2101
arylsulfatase AHomo sapiens (human)Potency0.84921.069113.955137.9330AID720538
alpha-galactosidaseHomo sapiens (human)Potency33.55214.466818.391635.4813AID1467; AID2107
IDH1Homo sapiens (human)Potency29.09290.005210.865235.4813AID686970
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency37.68580.035520.977089.1251AID504332
lysosomal alpha-glucosidase preproproteinHomo sapiens (human)Potency25.11890.036619.637650.1187AID1466; AID2242
D(1A) dopamine receptorHomo sapiens (human)Potency15.84890.02245.944922.3872AID488983
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency28.18380.001815.663839.8107AID894
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency18.35640.00419.984825.9290AID504444
huntingtin isoform 2Homo sapiens (human)Potency4.46680.000618.41981,122.0200AID2669
urokinase-type plasminogen activator precursorMus musculus (house mouse)Potency3.54810.15855.287912.5893AID540303
plasminogen precursorMus musculus (house mouse)Potency3.54810.15855.287912.5893AID540303
urokinase plasminogen activator surface receptor precursorMus musculus (house mouse)Potency3.54810.15855.287912.5893AID540303
survival motor neuron protein isoform dHomo sapiens (human)Potency3.98110.125912.234435.4813AID1458
lamin isoform A-delta10Homo sapiens (human)Potency0.11220.891312.067628.1838AID1487
Neuronal acetylcholine receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency25.11893.548118.039535.4813AID1466
Neuronal acetylcholine receptor subunit beta-2Rattus norvegicus (Norway rat)Potency25.11893.548118.039535.4813AID1466
Chain A, Beta-lactamaseEscherichia coli K-12Potency44.66840.044717.8581100.0000AID485294
Chain A, Putative fructose-1,6-bisphosphate aldolaseGiardia intestinalisPotency5.01190.140911.194039.8107AID2451
Chain A, HADH2 proteinHomo sapiens (human)Potency14.21910.025120.237639.8107AID886; AID893
Chain B, HADH2 proteinHomo sapiens (human)Potency14.21910.025120.237639.8107AID886; AID893
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency12.58930.177814.390939.8107AID2147
LuciferasePhotinus pyralis (common eastern firefly)Potency33.80780.007215.758889.3584AID588342
acid sphingomyelinaseHomo sapiens (human)Potency25.118914.125424.061339.8107AID504937
thioredoxin reductaseRattus norvegicus (Norway rat)Potency76.11040.100020.879379.4328AID588453; AID588456
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency10.00000.011212.4002100.0000AID1030
glucocerebrosidaseHomo sapiens (human)Potency28.18380.01268.156944.6684AID2101
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency12.58930.001815.663839.8107AID894
transcriptional regulator ERG isoform 3Homo sapiens (human)Potency39.81070.794321.275750.1187AID624246
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency35.48130.00798.23321,122.0200AID2551
gemininHomo sapiens (human)Potency0.70790.004611.374133.4983AID624297
[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)
Alpha-1A adrenergic receptorOryctolagus cuniculus (rabbit)Ki0.03980.00000.02040.2512AID36753
Solute carrier family 22 member 1 Homo sapiens (human)IC50 (µMol)23.70000.21005.553710.0000AID386625
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50 (µMol)133.00000.63154.45319.3000AID1473740
Multidrug resistance-associated protein 4Homo sapiens (human)IC50 (µMol)36.80000.20005.677410.0000AID1473741
Bile salt export pumpHomo sapiens (human)IC50 (µMol)133.00000.11007.190310.0000AID1473738
Alpha-2A adrenergic receptorHomo sapiens (human)IC50 (µMol)13.83200.00001.44217.3470AID625201
Alpha-2A adrenergic receptorHomo sapiens (human)Ki2.29770.00010.807410.0000AID35931; AID35936; AID35952; AID36077; AID625201
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)Ki0.10740.00010.949010.0000AID36409; AID37510
Alpha-2B adrenergic receptorHomo sapiens (human)IC50 (µMol)0.42800.00001.23808.1590AID625202
Alpha-2B adrenergic receptorHomo sapiens (human)Ki0.16750.00020.725710.0000AID36218; AID36231; AID36242; AID625202
Alpha-1A adrenergic receptorBos taurus (cattle)Ki2.47280.00000.50723.7020AID35952; AID36460; AID36466
Alpha-2C adrenergic receptorHomo sapiens (human)IC50 (µMol)6.04200.00001.47257.8980AID625203
Alpha-2C adrenergic receptorHomo sapiens (human)Ki0.31260.00030.483410.0000AID36393; AID36397; AID36409; AID36538; AID625203
Alpha-1B adrenergic receptorMesocricetus auratus (golden hamster)Ki0.00070.00002.01679.6000AID32974
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)Ki0.00630.00000.929610.0000AID35328; AID36252; AID36757
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)Ki0.00580.00000.970810.0000AID35328; AID36757
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)Ki0.00580.00000.937510.0000AID35328; AID36757
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)Ki0.03680.00000.575110.0000AID32975; AID35601; AID35603; AID36409
Alpha-1D adrenergic receptorHomo sapiens (human)IC50 (µMol)0.01100.00020.75688.8970AID1915717; AID625200
Alpha-1D adrenergic receptorHomo sapiens (human)Ki0.04920.00000.360910.0000AID35299; AID35303; AID35319; AID35328; AID35468; AID35472; AID35891; AID36252; AID36393; AID36409; AID625200
Alpha-2B adrenergic receptorMus musculus (house mouse)Ki0.00690.00020.10912.1500AID36474
Alpha-1A adrenergic receptorHomo sapiens (human)IC50 (µMol)0.00500.00020.56145.4000AID1915717
Alpha-1A adrenergic receptorHomo sapiens (human)Ki0.06330.00000.272610.0000AID35750; AID36252; AID36393; AID36409; AID36466; AID36474; AID36478; AID36605; AID36608; AID36618; AID36753; AID36757
Alpha-1B adrenergic receptorHomo sapiens (human)IC50 (µMol)0.00500.00020.65268.3300AID1915717
Alpha-1B adrenergic receptorHomo sapiens (human)Ki0.05040.00000.471310.0000AID35768; AID36252; AID36393; AID36409; AID37183; AID37196; AID37200; AID37218; AID37335; AID37478; AID37485
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Ki0.07260.00000.965010.0000AID32968; AID36409; AID36898
5-hydroxytryptamine receptor 7Cavia porcellus (domestic guinea pig)IC50 (µMol)23.70002.03005.53139.9000AID386625
Alpha-2C adrenergic receptorMus musculus (house mouse)Ki0.00690.00020.10912.1500AID36474
Alpha-2A adrenergic receptorMus musculus (house mouse)Ki0.00690.00020.10912.1500AID36474
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC50 (µMol)17.78280.00091.901410.0000AID576612
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)133.00002.41006.343310.0000AID1473739
[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)
Alpha-1A adrenergic receptorOryctolagus cuniculus (rabbit)Kd0.02000.00020.01430.0501AID37056
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)Kd0.00250.00020.52667.5858AID1374280; AID1374290
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)Kd0.02000.00020.62779.3325AID37056
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)Kd0.02000.00020.62779.3325AID37056
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)Kd0.02000.00020.62779.3325AID37056
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)Kd0.00190.00020.89627.5858AID1374281; AID1374288
Alpha-1D adrenergic receptorHomo sapiens (human)Kd0.02510.00000.19451.2882AID36126
Alpha-1A adrenergic receptorHomo sapiens (human)EC50 (µMol)0.05140.00010.50987.1000AID1194510; AID1323687
Alpha-1A adrenergic receptorHomo sapiens (human)Kd0.02510.00000.20481.2882AID36126
Alpha-1B adrenergic receptorHomo sapiens (human)EC50 (µMol)0.00110.00011.30105.6000AID1194511; AID1323689
Alpha-1B adrenergic receptorHomo sapiens (human)Kd0.02170.00000.11991.2882AID36126; AID37056
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Kd0.01090.00020.51397.5858AID1374279; AID1374289
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (167)

Processvia Protein(s)Taxonomy
xenobiotic metabolic processSolute carrier family 22 member 1 Homo sapiens (human)
neurotransmitter transportSolute carrier family 22 member 1 Homo sapiens (human)
serotonin transportSolute carrier family 22 member 1 Homo sapiens (human)
establishment or maintenance of transmembrane electrochemical gradientSolute carrier family 22 member 1 Homo sapiens (human)
organic cation transportSolute carrier family 22 member 1 Homo sapiens (human)
quaternary ammonium group transportSolute carrier family 22 member 1 Homo sapiens (human)
prostaglandin transportSolute carrier family 22 member 1 Homo sapiens (human)
monoamine transportSolute carrier family 22 member 1 Homo sapiens (human)
putrescine transportSolute carrier family 22 member 1 Homo sapiens (human)
spermidine transportSolute carrier family 22 member 1 Homo sapiens (human)
acetylcholine transportSolute carrier family 22 member 1 Homo sapiens (human)
dopamine transportSolute carrier family 22 member 1 Homo sapiens (human)
norepinephrine transportSolute carrier family 22 member 1 Homo sapiens (human)
thiamine transportSolute carrier family 22 member 1 Homo sapiens (human)
xenobiotic transportSolute carrier family 22 member 1 Homo sapiens (human)
epinephrine transportSolute carrier family 22 member 1 Homo sapiens (human)
serotonin uptakeSolute carrier family 22 member 1 Homo sapiens (human)
norepinephrine uptakeSolute carrier family 22 member 1 Homo sapiens (human)
thiamine transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
metanephric proximal tubule developmentSolute carrier family 22 member 1 Homo sapiens (human)
purine-containing compound transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
dopamine uptakeSolute carrier family 22 member 1 Homo sapiens (human)
monoatomic cation transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
transport across blood-brain barrierSolute carrier family 22 member 1 Homo sapiens (human)
(R)-carnitine transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
acyl carnitine transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
spermidine transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
cellular detoxificationSolute carrier family 22 member 1 Homo sapiens (human)
xenobiotic transport across blood-brain barrierSolute carrier family 22 member 1 Homo sapiens (human)
xenobiotic metabolic processATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
bile acid and bile salt transportATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transportATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
leukotriene transportATP-binding cassette sub-family C member 3Homo sapiens (human)
monoatomic anion transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transport across blood-brain barrierATP-binding cassette sub-family C member 3Homo sapiens (human)
prostaglandin secretionMultidrug resistance-associated protein 4Homo sapiens (human)
cilium assemblyMultidrug resistance-associated protein 4Homo sapiens (human)
platelet degranulationMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
bile acid and bile salt transportMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transportMultidrug resistance-associated protein 4Homo sapiens (human)
urate transportMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
cAMP transportMultidrug resistance-associated protein 4Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 4Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 4Homo sapiens (human)
guanine nucleotide transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
positive regulation of cytokine productionAlpha-2A adrenergic receptorHomo sapiens (human)
DNA replicationAlpha-2A adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
Ras protein signal transductionAlpha-2A adrenergic receptorHomo sapiens (human)
Rho protein signal transductionAlpha-2A adrenergic receptorHomo sapiens (human)
female pregnancyAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of cell population proliferationAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of norepinephrine secretionAlpha-2A adrenergic receptorHomo sapiens (human)
regulation of vasoconstrictionAlpha-2A adrenergic receptorHomo sapiens (human)
actin cytoskeleton organizationAlpha-2A adrenergic receptorHomo sapiens (human)
platelet activationAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of cell migrationAlpha-2A adrenergic receptorHomo sapiens (human)
activation of protein kinase activityAlpha-2A adrenergic receptorHomo sapiens (human)
activation of protein kinase B activityAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of epinephrine secretionAlpha-2A adrenergic receptorHomo sapiens (human)
cellular response to hormone stimulusAlpha-2A adrenergic receptorHomo sapiens (human)
receptor transactivationAlpha-2A adrenergic receptorHomo sapiens (human)
vasodilationAlpha-2A adrenergic receptorHomo sapiens (human)
glucose homeostasisAlpha-2A adrenergic receptorHomo sapiens (human)
fear responseAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of potassium ion transportAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of MAP kinase activityAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of epidermal growth factor receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of calcium ion-dependent exocytosisAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of insulin secretionAlpha-2A adrenergic receptorHomo sapiens (human)
intestinal absorptionAlpha-2A adrenergic receptorHomo sapiens (human)
thermoceptionAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of lipid catabolic processAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of membrane protein ectodomain proteolysisAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of calcium ion transportAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of insulin secretion involved in cellular response to glucose stimulusAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of uterine smooth muscle contractionAlpha-2A adrenergic receptorHomo sapiens (human)
adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-inhibiting adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
phospholipase C-activating adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of wound healingAlpha-2A adrenergic receptorHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of calcium ion transmembrane transporter activityAlpha-2A adrenergic receptorHomo sapiens (human)
MAPK cascadeAlpha-2B adrenergic receptorHomo sapiens (human)
angiogenesisAlpha-2B adrenergic receptorHomo sapiens (human)
regulation of vascular associated smooth muscle contractionAlpha-2B adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-2B adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-2B adrenergic receptorHomo sapiens (human)
female pregnancyAlpha-2B adrenergic receptorHomo sapiens (human)
negative regulation of norepinephrine secretionAlpha-2B adrenergic receptorHomo sapiens (human)
platelet activationAlpha-2B adrenergic receptorHomo sapiens (human)
activation of protein kinase B activityAlpha-2B adrenergic receptorHomo sapiens (human)
negative regulation of epinephrine secretionAlpha-2B adrenergic receptorHomo sapiens (human)
receptor transactivationAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of neuron differentiationAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of blood pressureAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of uterine smooth muscle contractionAlpha-2B adrenergic receptorHomo sapiens (human)
adrenergic receptor signaling pathwayAlpha-2B adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-2B adrenergic receptorHomo sapiens (human)
regulation of vasoconstrictionAlpha-1A adrenergic receptorBos taurus (cattle)
positive regulation of MAPK cascadeAlpha-1A adrenergic receptorBos taurus (cattle)
regulation of cardiac muscle contractionAlpha-1A adrenergic receptorBos taurus (cattle)
regulation of smooth muscle contractionAlpha-2C adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-2C adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-2C adrenergic receptorHomo sapiens (human)
negative regulation of norepinephrine secretionAlpha-2C adrenergic receptorHomo sapiens (human)
regulation of vasoconstrictionAlpha-2C adrenergic receptorHomo sapiens (human)
platelet activationAlpha-2C adrenergic receptorHomo sapiens (human)
activation of protein kinase B activityAlpha-2C adrenergic receptorHomo sapiens (human)
negative regulation of epinephrine secretionAlpha-2C adrenergic receptorHomo sapiens (human)
receptor transactivationAlpha-2C adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-2C adrenergic receptorHomo sapiens (human)
positive regulation of neuron differentiationAlpha-2C adrenergic receptorHomo sapiens (human)
adrenergic receptor signaling pathwayAlpha-2C adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-2C adrenergic receptorHomo sapiens (human)
negative regulation of insulin secretionAlpha-2C adrenergic receptorHomo sapiens (human)
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)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by hormonePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion homeostasisPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cardiac muscle contractionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cellular response to xenobiotic stimulusPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane depolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion import across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
xenobiotic metabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
negative regulation of gene expressionCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bile acid and bile salt transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
heme catabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic export from cellCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transepithelial transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
leukotriene transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
monoatomic anion transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (61)

Processvia Protein(s)Taxonomy
acetylcholine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
neurotransmitter transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
dopamine:sodium symporter activitySolute carrier family 22 member 1 Homo sapiens (human)
norepinephrine:sodium symporter activitySolute carrier family 22 member 1 Homo sapiens (human)
protein bindingSolute carrier family 22 member 1 Homo sapiens (human)
monoamine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
secondary active organic cation transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
organic anion transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
organic cation transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
prostaglandin transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
pyrimidine nucleoside transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
thiamine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
putrescine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
spermidine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
quaternary ammonium group transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
toxin transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
identical protein bindingSolute carrier family 22 member 1 Homo sapiens (human)
xenobiotic transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
(R)-carnitine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
ATP bindingATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type bile acid transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
icosanoid transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
guanine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ATP bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
urate transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
purine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type bile acid transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
alpha2-adrenergic receptor activityAlpha-2A adrenergic receptorHomo sapiens (human)
protein bindingAlpha-2A adrenergic receptorHomo sapiens (human)
protein kinase bindingAlpha-2A adrenergic receptorHomo sapiens (human)
alpha-1B adrenergic receptor bindingAlpha-2A adrenergic receptorHomo sapiens (human)
alpha-2C adrenergic receptor bindingAlpha-2A adrenergic receptorHomo sapiens (human)
thioesterase bindingAlpha-2A adrenergic receptorHomo sapiens (human)
heterotrimeric G-protein bindingAlpha-2A adrenergic receptorHomo sapiens (human)
protein homodimerization activityAlpha-2A adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-2A adrenergic receptorHomo sapiens (human)
epinephrine bindingAlpha-2A adrenergic receptorHomo sapiens (human)
norepinephrine bindingAlpha-2A adrenergic receptorHomo sapiens (human)
guanyl-nucleotide exchange factor activityAlpha-2A adrenergic receptorHomo sapiens (human)
alpha2-adrenergic receptor activityAlpha-2B adrenergic receptorHomo sapiens (human)
protein bindingAlpha-2B adrenergic receptorHomo sapiens (human)
epinephrine bindingAlpha-2B adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-1A adrenergic receptorBos taurus (cattle)
alpha2-adrenergic receptor activityAlpha-2C adrenergic receptorHomo sapiens (human)
protein bindingAlpha-2C adrenergic receptorHomo sapiens (human)
alpha-2A adrenergic receptor bindingAlpha-2C adrenergic receptorHomo sapiens (human)
protein homodimerization activityAlpha-2C adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-2C adrenergic receptorHomo sapiens (human)
epinephrine bindingAlpha-2C adrenergic receptorHomo sapiens (human)
guanyl-nucleotide exchange factor activityAlpha-2C adrenergic receptorHomo sapiens (human)
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)
transcription cis-regulatory region bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ubiquitin protein ligase bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
identical protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein homodimerization activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
C3HC4-type RING finger domain bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
scaffold protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
organic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type xenobiotic transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP hydrolysis activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (37)

Processvia Protein(s)Taxonomy
plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
basal plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
membraneSolute carrier family 22 member 1 Homo sapiens (human)
basolateral plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
apical plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
lateral plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
presynapseSolute carrier family 22 member 1 Homo sapiens (human)
plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basal plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basolateral plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
nucleolusMultidrug resistance-associated protein 4Homo sapiens (human)
Golgi apparatusMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
platelet dense granule membraneMultidrug resistance-associated protein 4Homo sapiens (human)
external side of apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
cytoplasmAlpha-2A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2A adrenergic receptorHomo sapiens (human)
basolateral plasma membraneAlpha-2A adrenergic receptorHomo sapiens (human)
neuronal cell bodyAlpha-2A adrenergic receptorHomo sapiens (human)
axon terminusAlpha-2A adrenergic receptorHomo sapiens (human)
presynaptic active zone membraneAlpha-2A adrenergic receptorHomo sapiens (human)
dopaminergic synapseAlpha-2A adrenergic receptorHomo sapiens (human)
postsynaptic density membraneAlpha-2A adrenergic receptorHomo sapiens (human)
glutamatergic synapseAlpha-2A adrenergic receptorHomo sapiens (human)
GABA-ergic synapseAlpha-2A adrenergic receptorHomo sapiens (human)
receptor complexAlpha-2A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2A adrenergic receptorHomo sapiens (human)
cytosolAlpha-2B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2B adrenergic receptorHomo sapiens (human)
cell surfaceAlpha-2B adrenergic receptorHomo sapiens (human)
intracellular membrane-bounded organelleAlpha-2B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2B adrenergic receptorHomo sapiens (human)
nucleusAlpha-1A adrenergic receptorBos taurus (cattle)
cytoplasmAlpha-1A adrenergic receptorBos taurus (cattle)
plasma membraneAlpha-1A adrenergic receptorBos taurus (cattle)
caveolaAlpha-1A adrenergic receptorBos taurus (cattle)
nuclear membraneAlpha-1A adrenergic receptorBos taurus (cattle)
cytoplasmAlpha-2C adrenergic receptorHomo sapiens (human)
endosomeAlpha-2C adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2C adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2C adrenergic receptorHomo sapiens (human)
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)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cell surfacePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
perinuclear region of cytoplasmPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cell surfaceCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
intercellular canaliculusCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (310)

Assay IDTitleYearJournalArticle
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
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.
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.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
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.
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.
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.
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.
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.
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.
AID588378qHTS for Inhibitors of ATXN expression: Validation
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID35768Ability to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylaminomethyl tetralone from human cloned Alpha-1b adrenergic receptor stably expressed in LM cells1998Bioorganic & medicinal chemistry letters, Sep-22, Volume: 8, Issue:18
Design and synthesis of N-alkylated saccharins as selective alpha-1a adrenergic receptor antagonists.
AID58506In vivo for selective antagonistic activity against intra-urethral pressure in dog, using phenylephrine as agonist2000Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15
De novo design of a novel oxazolidinone analogue as a potent and selective alpha1A adrenergic receptor antagonist with high oral bioavailability.
AID58512Potency inhibiting phenylephrine induced diastolic blood pressure in dog.1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 2. Approaches to eliminate opioid agonist metabolites via modification of linker and 4-methoxycarbonyl-4-phenylpiperidine moiety.
AID220559Evaluated for the inhibition of phenylephrine-induced contraction (SEM<10%) in dog.2000Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14
In vitro and in vivo evaluation of dihydropyrimidinone C-5 amides as potent and selective alpha(1A) receptor antagonists for the treatment of benign prostatic hyperplasia.
AID678713Inhibition of human CYP2C9 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-methoxy-4-trifluoromethylcoumarin-3-acetic acid as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID1202261Antagonist activity at Sprague-Dawley rat prostatic vas deferens adrenergic alpha-1A receptor after 20 mins2015European journal of medicinal chemistry, , Volume: 96Novel naftopidil-related derivatives and their biological effects as alpha1-adrenoceptors antagonists and antiproliferative agents.
AID36469In vitro antagonistic activity against alpha-1A receptor in dog prostate.2001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
Structure-activity studies for a novel series of bicyclic substituted hexahydrobenz[e]isoindole alpha1A adrenoceptor antagonists as potential agents for the symptomatic treatment of benign prostatic hyperplasia.
AID195210Antagonism against norepinephrine induced contractions in rat aorta.1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 2. Approaches to eliminate opioid agonist metabolites via modification of linker and 4-methoxycarbonyl-4-phenylpiperidine moiety.
AID226253Fold selectivity against alpha 1A adrenergic receptor over alpha 2A, 2B and 2C adrenergic receptors1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 3. Approaches to eliminate opioid agonist metabolites by using substituted phenylpiperazine side chains.
AID35472Binding affinity determined by displacement of [3H]prazosin from alpha-1D adrenergic receptor1998Journal of medicinal chemistry, Jul-02, Volume: 41, Issue:14
Identification of a dihydropyridine as a potent alpha1a adrenoceptor-selective antagonist that inhibits phenylephrine-induced contraction of the human prostate.
AID36915In vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in rat vas deferens1997Journal of medicinal chemistry, Sep-26, Volume: 40, Issue:20
Synthesis and pharmacological characterization of 3-[2-((3aR,9bR)-cis-6-methoxy-2,3,3a,4,5,9b-hexahydro-1H-benz[e] isoindol-2-yl)ethyl]pyrido-[3',4':4,5]thieno[3,2-d]pyrimidine-2,4 (1H,3H)-dione (A-131701): a uroselective alpha 1A adrenoceptor antagonist
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.
AID36393Ability to displace [3H]rauwolscine from cloned human Alpha-2C adrenergic receptor1995Journal of medicinal chemistry, May-12, Volume: 38, Issue:10
Discovery of alpha 1a-adrenergic receptor antagonists based on the L-type Ca2+ channel antagonist niguldipine.
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.
AID35747Compound was evaluated for its affinity for Alpha-1a adrenergic receptor in dog aorta preparations1998Bioorganic & medicinal chemistry letters, Sep-22, Volume: 8, Issue:18
Design and synthesis of N-alkylated saccharins as selective alpha-1a adrenergic receptor antagonists.
AID1194511Antagonist activity at alpha-1B adrenergic receptor (unknown origin) incubated for 30 mins prior to agonist addition measured after 5 hrs by CCF4-AM staining-based cellular assay2015Bioorganic & medicinal chemistry, May-01, Volume: 23, Issue:9
α-Adrenoceptor antagonistic and hypotensive properties of novel arylpiperazine derivatives of pyrrolidin-2-one.
AID1374281Antagonist activity at alpha1D-adrenoreceptor in Sprague-Dawley rat thoracic aorta assessed as relaxation of (-)-noradrenaline-induced contractile response
AID29359Ionization constant (pKa)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
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.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID58520Potency to inhibit phenylephrine stimulated intraurethral pressure in dog.1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 1. Structure-activity relationship in dihydropyrimidinones.
AID58514Potency to inhibi phenylephrine stimulated diastolic blood pressure in dog.1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 1. Structure-activity relationship in dihydropyrimidinones.
AID35303Binding affinity against human adrenergic receptor subtype Alpha-1D adrenergic receptor using [3H]prazosin as radioligand1997Journal of medicinal chemistry, Sep-26, Volume: 40, Issue:20
Synthesis and pharmacological characterization of 3-[2-((3aR,9bR)-cis-6-methoxy-2,3,3a,4,5,9b-hexahydro-1H-benz[e] isoindol-2-yl)ethyl]pyrido-[3',4':4,5]thieno[3,2-d]pyrimidine-2,4 (1H,3H)-dione (A-131701): a uroselective alpha 1A adrenoceptor antagonist
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).
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.
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.
AID29126Antagonist dissociation constant in rat spleen, number of determinations => 3.2000Journal of medicinal chemistry, Apr-20, Volume: 43, Issue:8
Structure-activity studies for a novel series of tricyclic substituted hexahydrobenz[e]isoindole alpha(1A) adrenoceptor antagonists as potential agents for the symptomatic treatment of benign prostatic hyperplasia (BPH).
AID26304Partition coefficient (logD6.5)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID35748Compound was evaluated for its affinity for Alpha-1a adrenergic receptor in dog prostate tissue preparations1998Bioorganic & medicinal chemistry letters, Sep-22, Volume: 8, Issue:18
Design and synthesis of N-alkylated saccharins as selective alpha-1a adrenergic receptor antagonists.
AID678722Covalent binding affinity to human liver microsomes assessed per mg of protein at 10 uM after 60 mins presence of NADPH2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID36898Compound was evaluated for its ability to displace [125I]HEAT binding from rat Alpha-1A adrenergic receptor1998Journal of medicinal chemistry, Apr-09, Volume: 41, Issue:8
4-Amino-2-[4-[1-(benzyloxycarbonyl)-2(S)- [[(1,1-dimethylethyl)amino]carbonyl]-piperazinyl]-6, 7-dimethoxyquinazoline (L-765,314): a potent and selective alpha1b adrenergic receptor antagonist.
AID190260Pseudo ED50 in Spontaneously Hypertensive Rat (SHR) model. Number determinations => 3.2000Journal of medicinal chemistry, Apr-20, Volume: 43, Issue:8
Structure-activity studies for a novel series of tricyclic substituted hexahydrobenz[e]isoindole alpha(1A) adrenoceptor antagonists as potential agents for the symptomatic treatment of benign prostatic hyperplasia (BPH).
AID1374284Selectivity index, ratio of pA2 for alpha1A-adrenoreceptor in Sprague-Dawley rat vas deferens to pA2 for antagonist activity at alpha1B-adrenoreceptor in Sprague-Dawley rat spleen
AID36605Compound was tested for its binding affinity utilizing cloned receptor binding assays by using [125 I]HEAT as radioligand to the human Alpha-1A adrenergic receptor1998Journal of medicinal chemistry, Apr-09, Volume: 41, Issue:8
4-Amino-2-[4-[1-(benzyloxycarbonyl)-2(S)- [[(1,1-dimethylethyl)amino]carbonyl]-piperazinyl]-6, 7-dimethoxyquinazoline (L-765,314): a potent and selective alpha1b adrenergic receptor antagonist.
AID678721Metabolic stability in human liver microsomes assessed as GSH adduct formation at 100 uM after 90 mins by HPLC-MS analysis2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID36466In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor1997Journal of medicinal chemistry, Aug-15, Volume: 40, Issue:17
N-arylpiperazinyl-N'-propylamino derivatives of heteroaryl amides as functional uroselective alpha 1-adrenoceptor antagonists.
AID32968In vitro binding affinity using [3H]prazosin as radioligand against adrenoceptor alpha 1A2000Journal of medicinal chemistry, Apr-20, Volume: 43, Issue:8
Structure-activity studies for a novel series of tricyclic substituted hexahydrobenz[e]isoindole alpha(1A) adrenoceptor antagonists as potential agents for the symptomatic treatment of benign prostatic hyperplasia (BPH).
AID91481Binding constant against human serum albumin (HSA)2001Journal of medicinal chemistry, Dec-06, Volume: 44, Issue:25
Cheminformatic models to predict binding affinities to human serum albumin.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID678716Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using diethoxyfluorescein as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
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).
AID35319Compound was tested for its binding affinity utilizing cloned receptor binding assays by using [125 I]HEAT as radioligand to the human Alpha-1D adrenergic receptor1998Journal of medicinal chemistry, Apr-09, Volume: 41, Issue:8
4-Amino-2-[4-[1-(benzyloxycarbonyl)-2(S)- [[(1,1-dimethylethyl)amino]carbonyl]-piperazinyl]-6, 7-dimethoxyquinazoline (L-765,314): a potent and selective alpha1b adrenergic receptor antagonist.
AID1323691Selectivity ratio of EC50 for human alpha1B adrenergic receptor expressed in CHOK1 cells co-expressing aequorin assessed as inhibition of agonist induced calcium mobilization to EC50 for alpha1A adrenergic receptor (unknown origin) assessed as inhibition 2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Arylsulfonamide derivatives of (aryloxy)ethyl pyrrolidines and piperidines as α
AID36124pA2 for Alpha-1 adrenergic receptor from human prostate.1997Journal of medicinal chemistry, Apr-25, Volume: 40, Issue:9
Pharmacological options in the treatment of benign prostatic hyperplasia.
AID36409The compound was tested for binding affinity against alpha-2C-adrenoceptor, from human clones.1995Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification.
AID229687Selectivity ratio( alpha-1b,1d/alpha1a)1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 1. Structure-activity relationship in dihydropyrimidinones.
AID365574Activation of [3H]prazosin uptake at transport-P transporter protein in mouse GT1-1 cells at 100 uM relative to control2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Molecular features of the prazosin molecule required for activation of Transport-P.
AID35601Compound was evaluated for its ability to displace [125I]HEAT binding from rat Alpha-1D adrenergic receptor1998Journal of medicinal chemistry, Apr-09, Volume: 41, Issue:8
4-Amino-2-[4-[1-(benzyloxycarbonyl)-2(S)- [[(1,1-dimethylethyl)amino]carbonyl]-piperazinyl]-6, 7-dimethoxyquinazoline (L-765,314): a potent and selective alpha1b adrenergic receptor antagonist.
AID678712Inhibition of human CYP1A2 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using ethoxyresorufin as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID196237In vitro inhibition of A-61603 induced contractions in rat prostate tissue2000Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15
De novo design of a novel oxazolidinone analogue as a potent and selective alpha1A adrenergic receptor antagonist with high oral bioavailability.
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).
AID36611In vitro binding affinity against alpha-1A adrenergic receptor of human liver microsomes1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 2. Approaches to eliminate opioid agonist metabolites via modification of linker and 4-methoxycarbonyl-4-phenylpiperidine moiety.
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.
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.
AID35931Ability to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptor1995Journal of medicinal chemistry, May-12, Volume: 38, Issue:10
Discovery of alpha 1a-adrenergic receptor antagonists based on the L-type Ca2+ channel antagonist niguldipine.
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.
AID24568Duration of action in rat1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 2. Approaches to eliminate opioid agonist metabolites via modification of linker and 4-methoxycarbonyl-4-phenylpiperidine moiety.
AID35328Binding affinity against Alpha-1D adrenergic receptor, from human clones.1995Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
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.
AID229690Selectivity ratio( alpha-2a,2b,2c/alpha1a)1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 2. Approaches to eliminate opioid agonist metabolites via modification of linker and 4-methoxycarbonyl-4-phenylpiperidine moiety.
AID35324In vitro binding affinity against Alpha-1D adrenergic receptor of human liver microsomes.1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 3. Approaches to eliminate opioid agonist metabolites by using substituted phenylpiperazine side chains.
AID36218Ability to displace [3H]rauwolscine from cloned human Alpha-2B adrenergic receptor1995Journal of medicinal chemistry, May-12, Volume: 38, Issue:10
Discovery of alpha 1a-adrenergic receptor antagonists based on the L-type Ca2+ channel antagonist niguldipine.
AID37335Binding affinity against Alpha-1B adrenergic receptor from human clone1995Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID678717Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-benzyloxyquinoline as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID35613In vitro antagonism against Alpha-1D adrenergic receptor using phenylephrine (PE) challenge in rat aorta1997Journal of medicinal chemistry, Sep-26, Volume: 40, Issue:20
Synthesis and pharmacological characterization of 3-[2-((3aR,9bR)-cis-6-methoxy-2,3,3a,4,5,9b-hexahydro-1H-benz[e] isoindol-2-yl)ethyl]pyrido-[3',4':4,5]thieno[3,2-d]pyrimidine-2,4 (1H,3H)-dione (A-131701): a uroselective alpha 1A adrenoceptor antagonist
AID1473739Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
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).
AID5936450% reduction in intraurethral pressure (IUP) in response to hypogastric nerve stimulation or agonist (phenylephrine or norepinephrine) administration in anesthetized dog1997Journal of medicinal chemistry, Apr-25, Volume: 40, Issue:9
Pharmacological options in the treatment of benign prostatic hyperplasia.
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.
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.
AID23622Plasma half life in rat1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 2. Approaches to eliminate opioid agonist metabolites via modification of linker and 4-methoxycarbonyl-4-phenylpiperidine moiety.
AID36077Binding affinity determined by displacement of [3H]rauwolscine from alpha-2A adrenergic receptor1998Journal of medicinal chemistry, Jul-02, Volume: 41, Issue:14
Identification of a dihydropyridine as a potent alpha1a adrenoceptor-selective antagonist that inhibits phenylephrine-induced contraction of the human prostate.
AID186991Antagonistic activity against norepinephrine induced contractions in rat aorta.1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 1. Structure-activity relationship in dihydropyrimidinones.
AID197368Compound was tested for selectivity in a challenge spontaneously hypertensive rat (SHR) model using an ascending in vitro dose paradigm1997Journal of medicinal chemistry, Sep-26, Volume: 40, Issue:20
Synthesis and pharmacological characterization of 3-[2-((3aR,9bR)-cis-6-methoxy-2,3,3a,4,5,9b-hexahydro-1H-benz[e] isoindol-2-yl)ethyl]pyrido-[3',4':4,5]thieno[3,2-d]pyrimidine-2,4 (1H,3H)-dione (A-131701): a uroselective alpha 1A adrenoceptor antagonist
AID1374279Antagonist activity at alpha1A-adrenoreceptor in Sprague-Dawley rat vas deferens assessed as relaxation of (-)-noradrenaline-induced contractile response
AID196114Antagonism against phenylephrine induced contractions in rat prostate.1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 2. Approaches to eliminate opioid agonist metabolites via modification of linker and 4-methoxycarbonyl-4-phenylpiperidine moiety.
AID35603Binding affinity against Alpha-1D adrenergic receptor, from rat clones.1995Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification.
AID35468Binding affinity was tested on human Alpha-1D adrenergic receptor1997Journal of medicinal chemistry, Apr-25, Volume: 40, Issue:9
Pharmacological options in the treatment of benign prostatic hyperplasia.
AID1374280Antagonist activity at alpha1B-adrenoreceptor in Sprague-Dawley rat spleen assessed as relaxation of (-)-noradrenaline-induced contractile response
AID169745Dose required to produce 50% inhibition of phenylephrine induced diastolic blood pressure in rat.1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 1. Structure-activity relationship in dihydropyrimidinones.
AID36474Ability to displace [3H]prazosin from cloned human Alpha-1A adrenergic receptor1995Journal of medicinal chemistry, May-12, Volume: 38, Issue:10
Discovery of alpha 1a-adrenergic receptor antagonists based on the L-type Ca2+ channel antagonist niguldipine.
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.
AID1374282Selectivity index, ratio of pA2 for antagonist activity at alpha1D-adrenoreceptor in Sprague-Dawley rat thoracic aorta to pA2 for antagonist activity at alpha1A-adrenoreceptor in Sprague-Dawley rat vas deferens
AID197367Antagonistic activity in spontaneously hypertensive rat model.2001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
Structure-activity studies for a novel series of bicyclic substituted hexahydrobenz[e]isoindole alpha1A adrenoceptor antagonists as potential agents for the symptomatic treatment of benign prostatic hyperplasia.
AID37183Binding affinity against Alpha-1B adrenergic receptor from hamster clones.1995Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification.
AID169744Dose required to produce 50% inhibition of phenylephrine induced contractile response in situ rat prostate.1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 1. Structure-activity relationship in dihydropyrimidinones.
AID1374290Antagonist activity at alpha1B-adrenoreceptor in Sprague-Dawley rat spleen assessed as relaxation of phenylephrine-induced contractile response
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.
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.
AID93445In vitro inhibition of A-61603 induced contractions in human prostate tissue2000Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15
De novo design of a novel oxazolidinone analogue as a potent and selective alpha1A adrenergic receptor antagonist with high oral bioavailability.
AID35299Ability to displace [3H]prazosin from cloned human Alpha-1D adrenergic receptor1995Journal of medicinal chemistry, May-12, Volume: 38, Issue:10
Discovery of alpha 1a-adrenergic receptor antagonists based on the L-type Ca2+ channel antagonist niguldipine.
AID32975In vitro binding affinity using [3H]prazosin as radioligand against adrenoceptor alpha 1d expressed in LTK cell2000Journal of medicinal chemistry, Apr-20, Volume: 43, Issue:8
Structure-activity studies for a novel series of tricyclic substituted hexahydrobenz[e]isoindole alpha(1A) adrenoceptor antagonists as potential agents for the symptomatic treatment of benign prostatic hyperplasia (BPH).
AID37033In vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferens2001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
Structure-activity studies for a novel series of bicyclic substituted hexahydrobenz[e]isoindole alpha1A adrenoceptor antagonists as potential agents for the symptomatic treatment of benign prostatic hyperplasia.
AID23625Plasma half life in rat.1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 1. Structure-activity relationship in dihydropyrimidinones.
AID32974In vitro binding affinity using [3H]prazosin as radioligand against adrenoceptor alpha 1b expressed in LTK cell2000Journal of medicinal chemistry, Apr-20, Volume: 43, Issue:8
Structure-activity studies for a novel series of tricyclic substituted hexahydrobenz[e]isoindole alpha(1A) adrenoceptor antagonists as potential agents for the symptomatic treatment of benign prostatic hyperplasia (BPH).
AID36397Binding affinity against human Alpha-2C adrenergic receptor using [3H]rauwolscine as radioligand1997Journal of medicinal chemistry, Sep-26, Volume: 40, Issue:20
Synthesis and pharmacological characterization of 3-[2-((3aR,9bR)-cis-6-methoxy-2,3,3a,4,5,9b-hexahydro-1H-benz[e] isoindol-2-yl)ethyl]pyrido-[3',4':4,5]thieno[3,2-d]pyrimidine-2,4 (1H,3H)-dione (A-131701): a uroselective alpha 1A adrenoceptor antagonist
AID36612In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 3. Approaches to eliminate opioid agonist metabolites by using substituted phenylpiperazine side chains.
AID18653Oral bioavailability in rat1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 1. Structure-activity relationship in dihydropyrimidinones.
AID404304Effect on human MRP2-mediated estradiol-17-beta-glucuronide transport in Sf9 cells inverted membrane vesicles relative to control2008Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11
Prediction and identification of drug interactions with the human ATP-binding cassette transporter multidrug-resistance associated protein 2 (MRP2; ABCC2).
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).
AID1374288Antagonist activity at alpha1D-adrenoreceptor in Sprague-Dawley rat thoracic aorta assessed as relaxation of phenylephrine-induced contractile response
AID36252Binding affinity against rat Alpha-2B adrenergic receptor using [3H]rauwolscine as radioligand1997Journal of medicinal chemistry, Sep-26, Volume: 40, Issue:20
Synthesis and pharmacological characterization of 3-[2-((3aR,9bR)-cis-6-methoxy-2,3,3a,4,5,9b-hexahydro-1H-benz[e] isoindol-2-yl)ethyl]pyrido-[3',4':4,5]thieno[3,2-d]pyrimidine-2,4 (1H,3H)-dione (A-131701): a uroselective alpha 1A adrenoceptor antagonist
AID175126Duration of action in rat1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 1. Structure-activity relationship in dihydropyrimidinones.
AID37200Binding affinity against human adrenergic receptor subtype Alpha-1B adrenergic receptor using [3H]prazosin as radioligand1997Journal of medicinal chemistry, Sep-26, Volume: 40, Issue:20
Synthesis and pharmacological characterization of 3-[2-((3aR,9bR)-cis-6-methoxy-2,3,3a,4,5,9b-hexahydro-1H-benz[e] isoindol-2-yl)ethyl]pyrido-[3',4':4,5]thieno[3,2-d]pyrimidine-2,4 (1H,3H)-dione (A-131701): a uroselective alpha 1A adrenoceptor antagonist
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID37485Binding affinity determined by displacement of [3H]prazosin from alpha-1B adrenergic receptor1998Journal of medicinal chemistry, Jul-02, Volume: 41, Issue:14
Identification of a dihydropyridine as a potent alpha1a adrenoceptor-selective antagonist that inhibits phenylephrine-induced contraction of the human prostate.
AID365573Activation of [3H]prazosin uptake at transport-P transporter protein in mouse GT1-1 cells at 10 uM relative to control2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Molecular features of the prazosin molecule required for activation of Transport-P.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID18408Oral bioavailability in rat2000Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15
De novo design of a novel oxazolidinone analogue as a potent and selective alpha1A adrenergic receptor antagonist with high oral bioavailability.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID93446In vitro binding affinity against human prostate using A-61603 as agonist.1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 2. Approaches to eliminate opioid agonist metabolites via modification of linker and 4-methoxycarbonyl-4-phenylpiperidine moiety.
AID29811Oral bioavailability in human2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
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.
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.
AID37329In vitro binding affinity against Alpha-1B adrenergic receptor of human liver microsomes.1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 3. Approaches to eliminate opioid agonist metabolites by using substituted phenylpiperazine side chains.
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).
AID229372Ratio of intraurethral pressure to that of pressor response in dog.1997Journal of medicinal chemistry, Apr-25, Volume: 40, Issue:9
Pharmacological options in the treatment of benign prostatic hyperplasia.
AID755121Antihypertensive activity in Wistar rat assessed as inhibition of phenylephrine-induced pressor response at 0.24 micromol pretreated with losartan prior to compound administration2013Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13
Design and synthesis of 6,7-dimethoxyquinazoline analogs as multi-targeted ligands for α1- and AII-receptors antagonism.
AID36618Binding affinity against Alpha-1A adrenergic receptor from human clone1995Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification.
AID37478Binding affinity was tested on human Alpha-1B adrenergic receptor1997Journal of medicinal chemistry, Apr-25, Volume: 40, Issue:9
Pharmacological options in the treatment of benign prostatic hyperplasia.
AID229688Selectivity ratio( alpha-1b,1d/alpha1a)1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 2. Approaches to eliminate opioid agonist metabolites via modification of linker and 4-methoxycarbonyl-4-phenylpiperidine moiety.
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.
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.
AID425652Total body clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID37327In vitro binding affinity against Alpha-1B adrenergic receptor of human liver microsomes.1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 1. Structure-activity relationship in dihydropyrimidinones.
AID60978In vitro inhibition of phenylephrine induced contractions in dog prostate tissue2000Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15
De novo design of a novel oxazolidinone analogue as a potent and selective alpha1A adrenergic receptor antagonist with high oral bioavailability.
AID1202263Antagonist activity at Sprague-Dawley rat thoracic aorta adrenergic alpha-1D receptor after 20 mins2015European journal of medicinal chemistry, , Volume: 96Novel naftopidil-related derivatives and their biological effects as alpha1-adrenoceptors antagonists and antiproliferative agents.
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).
AID365572Activation of [3H]prazosin uptake at transport-P transporter protein in mouse GT1-1 cells at 1 uM relative to control2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Molecular features of the prazosin molecule required for activation of Transport-P.
AID36468In vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in dog prostate1997Journal of medicinal chemistry, Sep-26, Volume: 40, Issue:20
Synthesis and pharmacological characterization of 3-[2-((3aR,9bR)-cis-6-methoxy-2,3,3a,4,5,9b-hexahydro-1H-benz[e] isoindol-2-yl)ethyl]pyrido-[3',4':4,5]thieno[3,2-d]pyrimidine-2,4 (1H,3H)-dione (A-131701): a uroselective alpha 1A adrenoceptor antagonist
AID1194510Antagonist activity at alpha-1A adrenergic receptor (unknown origin) incubated for 30 mins prior to agonist addition measured after 5 hrs by CCF4-AM staining-based cellular assay2015Bioorganic & medicinal chemistry, May-01, Volume: 23, Issue:9
α-Adrenoceptor antagonistic and hypotensive properties of novel arylpiperazine derivatives of pyrrolidin-2-one.
AID36126Activity against Alpha-1 adrenergic receptor subtypes of human prostate tissue1997Journal of medicinal chemistry, Aug-15, Volume: 40, Issue:17
N-arylpiperazinyl-N'-propylamino derivatives of heteroaryl amides as functional uroselective alpha 1-adrenoceptor antagonists.
AID29124Antagonist dissociation constant in dog prostate, number of determinations => 3.2000Journal of medicinal chemistry, Apr-20, Volume: 43, Issue:8
Structure-activity studies for a novel series of tricyclic substituted hexahydrobenz[e]isoindole alpha(1A) adrenoceptor antagonists as potential agents for the symptomatic treatment of benign prostatic hyperplasia (BPH).
AID318739Antagonist activity at alpha-1L-adrenoceptor in human prostate assessed as inhibition of noradrenaline-mediated contraction2007Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 35, Issue:8
Impact of physicochemical and structural properties on the pharmacokinetics of a series of alpha1L-adrenoceptor antagonists.
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.
AID365571Inhibition of prazosin uptake at transport-P transporter protein in mouse GT1-1 cells at 100 uM relative to desipramine2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Molecular features of the prazosin molecule required for activation of Transport-P.
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID36757Binding affinity determined by displacement of [3H]prazosin from alpha-1A adrenergic receptor1998Journal of medicinal chemistry, Jul-02, Volume: 41, Issue:14
Identification of a dihydropyridine as a potent alpha1a adrenoceptor-selective antagonist that inhibits phenylephrine-induced contraction of the human prostate.
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).
AID196111Dose required to inhibit 50% of contractile responses induced by phenylephrine in rat prostate.1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 2. Approaches to eliminate opioid agonist metabolites via modification of linker and 4-methoxycarbonyl-4-phenylpiperidine moiety.
AID60481In vivo for selective antagonistic activity against diastolic blood pressure in dog, using phenylephrine as agonist2000Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15
De novo design of a novel oxazolidinone analogue as a potent and selective alpha1A adrenergic receptor antagonist with high oral bioavailability.
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.
AID1202266Selectivity ratio for Sprague-Dawley rat thoracic aorta adrenergic alpha-1D receptor to Sprague-Dawley rat spleen adrenergic alpha-1A receptor2015European journal of medicinal chemistry, , Volume: 96Novel naftopidil-related derivatives and their biological effects as alpha1-adrenoceptors antagonists and antiproliferative agents.
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.
AID678714Inhibition of human CYP2C19 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 3-butyryl-7-methoxycoumarin as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID35155In vitro antagonistic activity against alpha-1B receptor in rat spleen.2001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
Structure-activity studies for a novel series of bicyclic substituted hexahydrobenz[e]isoindole alpha1A adrenoceptor antagonists as potential agents for the symptomatic treatment of benign prostatic hyperplasia.
AID24855Antagonist dissociation constant in rat vas deferens, number of determinations => 3.2000Journal of medicinal chemistry, Apr-20, Volume: 43, Issue:8
Structure-activity studies for a novel series of tricyclic substituted hexahydrobenz[e]isoindole alpha(1A) adrenoceptor antagonists as potential agents for the symptomatic treatment of benign prostatic hyperplasia (BPH).
AID1323687Intrinsic activity at alpha1A adrenergic receptor (unknown origin) assessed as inhibition of agonist induced effect preincubated for 30 mins followed by agonist addition measured after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gen2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Arylsulfonamide derivatives of (aryloxy)ethyl pyrrolidines and piperidines as α
AID62842Compound was tested for efficacy in a challenge intraurethral pressure (IUP) model using aged anesthetized dogs1997Journal of medicinal chemistry, Sep-26, Volume: 40, Issue:20
Synthesis and pharmacological characterization of 3-[2-((3aR,9bR)-cis-6-methoxy-2,3,3a,4,5,9b-hexahydro-1H-benz[e] isoindol-2-yl)ethyl]pyrido-[3',4':4,5]thieno[3,2-d]pyrimidine-2,4 (1H,3H)-dione (A-131701): a uroselective alpha 1A adrenoceptor antagonist
AID35762In vitro affinity for Alpha-1a adrenergic receptor in isolated rat aorta preparations was determined by functional assay1998Bioorganic & medicinal chemistry letters, Sep-22, Volume: 8, Issue:18
Design and synthesis of N-alkylated saccharins as selective alpha-1a adrenergic receptor antagonists.
AID36231Binding affinity against Alpha-2B adrenergic receptor from human clones.1995Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification.
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID1202264Selectivity ratio for Sprague-Dawley rat thoracic aorta adrenergic alpha-1D receptor to Sprague-Dawley rat spleen adrenergic alpha-1B receptor2015European journal of medicinal chemistry, , Volume: 96Novel naftopidil-related derivatives and their biological effects as alpha1-adrenoceptors antagonists and antiproliferative agents.
AID37510Compound was evaluated for its ability to displace [125I]HEAT binding from rat Alpha-1B adrenergic receptor1998Journal of medicinal chemistry, Apr-09, Volume: 41, Issue:8
4-Amino-2-[4-[1-(benzyloxycarbonyl)-2(S)- [[(1,1-dimethylethyl)amino]carbonyl]-piperazinyl]-6, 7-dimethoxyquinazoline (L-765,314): a potent and selective alpha1b adrenergic receptor antagonist.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
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.
AID386623Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells at 100 uM by confocal microscopy2008Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
Structural requirements for drug inhibition of the liver specific human organic cation transport protein 1.
AID1374289Antagonist activity at alpha1A-adrenoreceptor in Sprague-Dawley rat vas deferens assessed as relaxation of phenylephrine-induced contractile response
AID36478Binding affinity against human adrenergic receptor subtype Alpha-1A adrenergic receptor using [3H]prazosin as radioligand1997Journal of medicinal chemistry, Sep-26, Volume: 40, Issue:20
Synthesis and pharmacological characterization of 3-[2-((3aR,9bR)-cis-6-methoxy-2,3,3a,4,5,9b-hexahydro-1H-benz[e] isoindol-2-yl)ethyl]pyrido-[3',4':4,5]thieno[3,2-d]pyrimidine-2,4 (1H,3H)-dione (A-131701): a uroselective alpha 1A adrenoceptor antagonist
AID35936Binding affinity against human adrenergic receptor subtype Alpha-2A adrenergic receptor using [3H]rauwolscine as radioligand1997Journal of medicinal chemistry, Sep-26, Volume: 40, Issue:20
Synthesis and pharmacological characterization of 3-[2-((3aR,9bR)-cis-6-methoxy-2,3,3a,4,5,9b-hexahydro-1H-benz[e] isoindol-2-yl)ethyl]pyrido-[3',4':4,5]thieno[3,2-d]pyrimidine-2,4 (1H,3H)-dione (A-131701): a uroselective alpha 1A adrenoceptor antagonist
AID93443Antagonistic activity against Alpha-1 adrenergic receptor in human prostate tissue using phenylephrine as agonist1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 1. Structure-activity relationship in dihydropyrimidinones.
AID36610In vitro binding affinity against Alpha-1A adrenergic receptor of human liver microsomes.1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 1. Structure-activity relationship in dihydropyrimidinones.
AID1473741Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID36608In vitro binding affinity radioligand1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 1. Structure-activity relationship in dihydropyrimidinones.
AID37056Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay1997Journal of medicinal chemistry, Aug-15, Volume: 40, Issue:17
N-arylpiperazinyl-N'-propylamino derivatives of heteroaryl amides as functional uroselective alpha 1-adrenoceptor antagonists.
AID35154In vitro antagonism against Alpha-1B adrenergic receptor using phenylephrine (PE) challenge in rat spleen1997Journal of medicinal chemistry, Sep-26, Volume: 40, Issue:20
Synthesis and pharmacological characterization of 3-[2-((3aR,9bR)-cis-6-methoxy-2,3,3a,4,5,9b-hexahydro-1H-benz[e] isoindol-2-yl)ethyl]pyrido-[3',4':4,5]thieno[3,2-d]pyrimidine-2,4 (1H,3H)-dione (A-131701): a uroselective alpha 1A adrenoceptor antagonist
AID62832In vivo antagonist dissociation constant in intaraurethral pressure model in dogs.2001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
Structure-activity studies for a novel series of bicyclic substituted hexahydrobenz[e]isoindole alpha1A adrenoceptor antagonists as potential agents for the symptomatic treatment of benign prostatic hyperplasia.
AID36538Binding affinity assayed by displacement of [3H]rauwolscine from human alpha-2C adrenergic receptor1998Journal of medicinal chemistry, Jul-02, Volume: 41, Issue:14
Identification of a dihydropyridine as a potent alpha1a adrenoceptor-selective antagonist that inhibits phenylephrine-induced contraction of the human prostate.
AID755128Antagonist activity at alpha1-adrenergic receptor in Wistar rat endothelium denuded thoracic aorta assessed as inhibition of phenylephrine-induced contraction preincubated for 30 mins prior to phenylephrine-challenge2013Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13
Design and synthesis of 6,7-dimethoxyquinazoline analogs as multi-targeted ligands for α1- and AII-receptors antagonism.
AID1323689Intrinsic activity at human alpha1B adrenergic receptor expressed in CHOK1 cells co-expressing aequorin assessed as inhibition of agonist induced calcium mobilization preincubated for 15 mins followed by agonist addition measured for 20 secs in presence o2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Arylsulfonamide derivatives of (aryloxy)ethyl pyrrolidines and piperidines as α
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).
AID58508In vivo inhibitory activity against phenylepinephrine-induced increase in urethral pressure (IUP) in dog1998Bioorganic & medicinal chemistry letters, Sep-22, Volume: 8, Issue:18
Design and synthesis of N-alkylated saccharins as selective alpha-1a adrenergic receptor antagonists.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID755127Antagonist activity at angiotensin-2 receptor in Wistar rat endothelium denuded thoracic aorta assessed as inhibition of angiotensin 2-induced contraction preincubated for 30 mins prior to angiotensin 2-challenge2013Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13
Design and synthesis of 6,7-dimethoxyquinazoline analogs as multi-targeted ligands for α1- and AII-receptors antagonism.
AID1202262Antagonist activity at Sprague-Dawley rat spleen adrenergic alpha-1B receptor after 20 mins2015European journal of medicinal chemistry, , Volume: 96Novel naftopidil-related derivatives and their biological effects as alpha1-adrenoceptors antagonists and antiproliferative agents.
AID678715Inhibition of human CYP2D6 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 4-methylaminoethyl-7-methoxycoumarin as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID232245Selectivity ratio (antolog[pA2 of IUP-pED50 of SHR]) of the compound2001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
Structure-activity studies for a novel series of bicyclic substituted hexahydrobenz[e]isoindole alpha1A adrenoceptor antagonists as potential agents for the symptomatic treatment of benign prostatic hyperplasia.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID576612Inhibition of human ERG2011European journal of medicinal chemistry, Feb, Volume: 46, Issue:2
Predicting hERG activities of compounds from their 3D structures: development and evaluation of a global descriptors based QSAR model.
AID224638Evaluated for the inhibition of A61603-induced contraction; n=4 and data for each concentration was averaged (SEM<10%) in rat. 2000Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14
In vitro and in vivo evaluation of dihydropyrimidinone C-5 amides as potent and selective alpha(1A) receptor antagonists for the treatment of benign prostatic hyperplasia.
AID220545Dose effecting a 20 mmHg change in diastolic blood pressure (SEM<10%) in dog.2000Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14
In vitro and in vivo evaluation of dihydropyrimidinone C-5 amides as potent and selective alpha(1A) receptor antagonists for the treatment of benign prostatic hyperplasia.
AID318740Antagonist activity at alpha-1-adrenoceptor in rat aorta assessed as inhibition of noradrenaline-mediated contraction2007Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 35, Issue:8
Impact of physicochemical and structural properties on the pharmacokinetics of a series of alpha1L-adrenoceptor antagonists.
AID35758Compound was evaluated for its affinity for Alpha-1a adrenergic receptor in human prostate tissue preparations1998Bioorganic & medicinal chemistry letters, Sep-22, Volume: 8, Issue:18
Design and synthesis of N-alkylated saccharins as selective alpha-1a adrenergic receptor antagonists.
AID1473738Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
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).
AID229689Selectivity ratio( alpha-2a,2b,2c/alpha1a)1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 1. Structure-activity relationship in dihydropyrimidinones.
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).
AID232246Selectivity ratio (antolog[pA2rat vas deferens/pA2 rat spleen]) of the compound2001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
Structure-activity studies for a novel series of bicyclic substituted hexahydrobenz[e]isoindole alpha1A adrenoceptor antagonists as potential agents for the symptomatic treatment of benign prostatic hyperplasia.
AID22293Delta logD (logD6.5 - logD7.4)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
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.
AID1202265Selectivity ratio for Sprague-Dawley rat thoracic aorta adrenergic alpha-1A receptor to Sprague-Dawley rat spleen adrenergic alpha-1B receptor2015European journal of medicinal chemistry, , Volume: 96Novel naftopidil-related derivatives and their biological effects as alpha1-adrenoceptors antagonists and antiproliferative agents.
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).
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID95594Displacement of [3H]nitrendipine from rat brain L-type [Ca2+] channel1995Journal of medicinal chemistry, May-12, Volume: 38, Issue:10
Discovery of alpha 1a-adrenergic receptor antagonists based on the L-type Ca2+ channel antagonist niguldipine.
AID1374283Selectivity index, ratio of pA2 for antagonist activity at alpha1D-adrenoreceptor in Sprague-Dawley rat thoracic aorta to pA2 for antagonist activity at alpha1B-adrenoreceptor in Sprague-Dawley rat spleen
AID58507In vivo inhibitory activity against phenylepinephrine-induced increase in diastolic blood pressure (DBP) in dog1998Bioorganic & medicinal chemistry letters, Sep-22, Volume: 8, Issue:18
Design and synthesis of N-alkylated saccharins as selective alpha-1a adrenergic receptor antagonists.
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).
AID294856Dissociation constant, pKa of the compound2007Bioorganic & medicinal chemistry, Apr-15, Volume: 15, Issue:8
Computational approach to the basicity of a series of alpha1-adrenoceptor ligands in aqueous solution.
AID59533Intraurethral pressure (IUP) in Beagle dogs values are expressed as pseudo pA2 values.2000Journal of medicinal chemistry, Apr-20, Volume: 43, Issue:8
Structure-activity studies for a novel series of tricyclic substituted hexahydrobenz[e]isoindole alpha(1A) adrenoceptor antagonists as potential agents for the symptomatic treatment of benign prostatic hyperplasia (BPH).
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.
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).
AID425653Renal clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID36753Binding affinity was tested on human Alpha-1A adrenergic receptor1997Journal of medicinal chemistry, Apr-25, Volume: 40, Issue:9
Pharmacological options in the treatment of benign prostatic hyperplasia.
AID1915717Antagonist activity at Adrenergic alpha-1 receptor in human Prostate cell in presence of (125I)-Heat by Competitive binding assay2021European journal of medicinal chemistry, Feb-05, Volume: 211Therapeutic progression of quinazolines as targeted chemotherapeutic agents.
AID35750Ability to displace beta ([125I]-iodo-4-hydroxyphenyl)-ethylaminomethyl tetralone from human Alpha-1a adrenergic receptor stably expressed in Chinese Hamster Ovary (CHO) cells1998Bioorganic & medicinal chemistry letters, Sep-22, Volume: 8, Issue:18
Design and synthesis of N-alkylated saccharins as selective alpha-1a adrenergic receptor antagonists.
AID37218Compound was tested for its binding affinity utilizing cloned receptor binding assays by using [125 I]HEAT as radioligand to the human Alpha-1B adrenergic receptor1998Journal of medicinal chemistry, Apr-09, Volume: 41, Issue:8
4-Amino-2-[4-[1-(benzyloxycarbonyl)-2(S)- [[(1,1-dimethylethyl)amino]carbonyl]-piperazinyl]-6, 7-dimethoxyquinazoline (L-765,314): a potent and selective alpha1b adrenergic receptor antagonist.
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.
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID1473740Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID35891Ability to displace beta ([125I]-iodo-4-hydroxyphenyl) ethylamino methyl tetralone from human cloned Alpha-1d adrenergic receptor stably expressed in HEK cells.1998Bioorganic & medicinal chemistry letters, Sep-22, Volume: 8, Issue:18
Design and synthesis of N-alkylated saccharins as selective alpha-1a adrenergic receptor antagonists.
AID35763In vitro affinity for Alpha-1a adrenergic receptor in isolated rat prostate tissue preparations was determined by functional assay1998Bioorganic & medicinal chemistry letters, Sep-22, Volume: 8, Issue:18
Design and synthesis of N-alkylated saccharins as selective alpha-1a adrenergic receptor antagonists.
AID5936350% reduction in agonist induced pressor response in anesthetized dog1997Journal of medicinal chemistry, Apr-25, Volume: 40, Issue:9
Pharmacological options in the treatment of benign prostatic hyperplasia.
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.
AID36242Binding affinity determined by displacement of [3H]rauwolscine from alpha-2B adrenergic receptor1998Journal of medicinal chemistry, Jul-02, Volume: 41, Issue:14
Identification of a dihydropyridine as a potent alpha1a adrenoceptor-selective antagonist that inhibits phenylephrine-induced contraction of the human prostate.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID62357Compound was evaluated for in vivo selectivity for intraurethal pressure over diastolic blood pressure in dog; 1x1998Bioorganic & medicinal chemistry letters, Sep-22, Volume: 8, Issue:18
Design and synthesis of N-alkylated saccharins as selective alpha-1a adrenergic receptor antagonists.
AID169742Compound was tested in situ for the inhibition of phenylephrine-induced contractions in anesthetized rat2000Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15
De novo design of a novel oxazolidinone analogue as a potent and selective alpha1A adrenergic receptor antagonist with high oral bioavailability.
AID386625Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy2008Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
Structural requirements for drug inhibition of the liver specific human organic cation transport protein 1.
AID35322In vitro binding affinity against Alpha-1D adrenergic receptor of human liver microsomes.1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 1. Structure-activity relationship in dihydropyrimidinones.
AID35952Binding affinity against Alpha-2A adrenergic receptor, from human clones.1995Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification.
AID58513Potency inhibiting phenylephrine induced intraurethral pressure in dog.1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 2. Approaches to eliminate opioid agonist metabolites via modification of linker and 4-methoxycarbonyl-4-phenylpiperidine moiety.
AID37196Ability to displace [3H]prazosin from cloned human Alpha-1B adrenergic receptor1995Journal of medicinal chemistry, May-12, Volume: 38, Issue:10
Discovery of alpha 1a-adrenergic receptor antagonists based on the L-type Ca2+ channel antagonist niguldipine.
AID195213In vitro inhibition of norepinephrine induced contractions in isolated rat aorta2000Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15
De novo design of a novel oxazolidinone analogue as a potent and selective alpha1A adrenergic receptor antagonist with high oral bioavailability.
AID18633Bioavailability in rat1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 2. Approaches to eliminate opioid agonist metabolites via modification of linker and 4-methoxycarbonyl-4-phenylpiperidine moiety.
AID27441Half-life in rat2000Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15
De novo design of a novel oxazolidinone analogue as a potent and selective alpha1A adrenergic receptor antagonist with high oral bioavailability.
AID36460Binding affinity against Alpha-1A adrenergic receptor from bovine clone1995Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification.
AID35757Compound was evaluated for its affinity for Alpha-1a adrenergic receptor in human aorta preparations1998Bioorganic & medicinal chemistry letters, Sep-22, Volume: 8, Issue:18
Design and synthesis of N-alkylated saccharins as selective alpha-1a adrenergic receptor antagonists.
AID37161Antagonistic activity against Alpha-1 adrenergic receptor in rat prostate tissue using A61603 as agonist1999Journal of medicinal chemistry, Nov-18, Volume: 42, Issue:23
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 1. Structure-activity relationship in dihydropyrimidinones.
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.
AID1346000Human alpha1B-adrenoceptor (Adrenoceptors)1997Journal of medicinal chemistry, Sep-26, Volume: 40, Issue:20
Synthesis and pharmacological characterization of 3-[2-((3aR,9bR)-cis-6-methoxy-2,3,3a,4,5,9b-hexahydro-1H-benz[e] isoindol-2-yl)ethyl]pyrido-[3',4':4,5]thieno[3,2-d]pyrimidine-2,4 (1H,3H)-dione (A-131701): a uroselective alpha 1A adrenoceptor antagonist
AID1345908Human alpha1A-adrenoceptor (Adrenoceptors)1997Journal of medicinal chemistry, Sep-26, Volume: 40, Issue:20
Synthesis and pharmacological characterization of 3-[2-((3aR,9bR)-cis-6-methoxy-2,3,3a,4,5,9b-hexahydro-1H-benz[e] isoindol-2-yl)ethyl]pyrido-[3',4':4,5]thieno[3,2-d]pyrimidine-2,4 (1H,3H)-dione (A-131701): a uroselective alpha 1A adrenoceptor antagonist
AID1345971Human alpha1D-adrenoceptor (Adrenoceptors)1997Journal of medicinal chemistry, Sep-26, Volume: 40, Issue:20
Synthesis and pharmacological characterization of 3-[2-((3aR,9bR)-cis-6-methoxy-2,3,3a,4,5,9b-hexahydro-1H-benz[e] isoindol-2-yl)ethyl]pyrido-[3',4':4,5]thieno[3,2-d]pyrimidine-2,4 (1H,3H)-dione (A-131701): a uroselective alpha 1A adrenoceptor antagonist
AID1224864HCS microscopy assay (F508del-CFTR)2016PloS one, , Volume: 11, Issue:10
Increasing the Endoplasmic Reticulum Pool of the F508del Allele of the Cystic Fibrosis Transmembrane Conductance Regulator Leads to Greater Folding Correction by Small Molecule Therapeutics.
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.
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.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
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.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (615)

TimeframeStudies, This Drug (%)All Drugs %
pre-199070 (11.38)18.7374
1990's219 (35.61)18.2507
2000's206 (33.50)29.6817
2010's93 (15.12)24.3611
2020's27 (4.39)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 94.53

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 Index94.53 (24.57)
Research Supply Index6.72 (2.92)
Research Growth Index4.78 (4.65)
Search Engine Demand Index171.99 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (94.53)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials173 (26.29%)5.53%
Trials0 (0.00%)5.53%
Reviews79 (12.01%)6.00%
Reviews0 (0.00%)6.00%
Case Studies22 (3.34%)4.05%
Case Studies0 (0.00%)4.05%
Observational2 (0.30%)0.25%
Observational0 (0.00%)0.25%
Other382 (58.05%)84.16%
Other6 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (20)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Assessing Target Engagement of Terazosin in Healthy Adults [NCT04551040]Phase 118 participants (Anticipated)Interventional2021-03-26Active, not recruiting
a Randomized, Double Blind, Placebo Controlled Clinical Trial Exploring the Target Engagement and Tolerability of Terazosin Hydrochloride in Patients With Dementia With Lewy Bodies [NCT04760860]Phase 1/Phase 240 participants (Anticipated)Interventional2024-10-31Not yet recruiting
Alpha-blocker Plus Diuretic Combination Therapy as Second-line Treatment for Nocturia in Men With LUTS: a Pilot Study [NCT00700583]72 participants (Actual)Interventional2008-05-31Completed
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
-Clinical Efficacy of Pharmacological Treatments Targeting Energy Metabolism, Evaluated by Gait Analysis, on Motor Function in Parkinson's Disease Patients [NCT05855577]Phase 450 participants (Anticipated)Interventional2023-12-31Not yet recruiting
The Effect of alpha1- Adrenergic Receptor Antagonist Therapy on Cardiac and Striatal Transporter Uptake in Pre-Motor and Symptomatic Parkinson's Disease: A Follow up Study [NCT05109364]Phase 215 participants (Anticipated)Interventional2022-09-23Recruiting
The Effect of a1- Adrenergic Receptor Antagonist Therapy on Cardiac and Striatal Transporter Uptake in Pre-Motor and Symptomatic Parkinson's Disease [NCT04386317]Phase 215 participants (Anticipated)Interventional2020-11-01Recruiting
A Pilot Study of the Efficacy and Tolerability of Terazosin for the Treatment of Antidepressant-Induced Excessive Sweating [NCT00237510]15 participants (Anticipated)Interventional2005-05-31Completed
[NCT00693199]360 participants (Actual)Interventional2006-07-31Completed
The Clinical Efficacy of Non-steroidal Anti-inflammation Drugs in Patients With Benign Prostatic Hyperplasia: A Prospective Randomized Multicenter Trial [NCT00687388]Phase 40 participants (Actual)Interventional2008-05-31Withdrawn(stopped due to in order to prepare a new clinical trial to evaluate with pathological change)
Effect of Renin-angiotensin-system Blockade on Urinary Free Light Chains in Patients With Type 2 Diabetes Mellitus [NCT02046395]Phase 428 participants (Actual)Interventional2012-01-31Completed
Antidepressant Induced Excessive Sweating: Measurement and Treatment With Terazosin [NCT00449683]Phase 423 participants (Actual)Interventional2007-03-31Completed
Randomized Trial Comparing Terazosin 5 mg Daily and Doxazosin GITS 4 mg Daily in the Successful Rate of Trial Without Catheter in Acute Urinary Retention With Long Term Follow up [NCT00563485]120 participants (Anticipated)Interventional2005-10-31Terminated
Atrial Substrate Modification With Aggressive Blood Pressure Lowering to Prevent AF [NCT00438113]Phase 4184 participants (Actual)Interventional2009-12-31Completed
Phase One of Study on Urinary Stent Complications and Treatment [NCT01530243]Phase 2/Phase 3104 participants (Actual)Interventional2012-01-31Completed
Action to Control Cardiovascular Risk in Diabetes (ACCORD) [NCT00000620]Phase 310,251 participants (Actual)Interventional1999-09-30Completed
Effect of Diesel Exhaust Exposures on Vascular Function in Humans: The Role of Sympathetic Activation [NCT01508637]24 participants (Anticipated)Interventional2012-01-31Recruiting
Clinical Progression and Costs in Benign Prostatic Hyperplasia Patients Treated With Early Versus Delayed Combination Therapy [NCT01435954]13,551 participants (Actual)Observational2010-08-31Completed
A Pilot Study Assessing the Safety and Efficacy of Low Dosage of Terazosin in Subjects Undergoing Carotid Artery Stenting [NCT03195673]Phase 2160 participants (Anticipated)Interventional2018-03-02Recruiting
A Pilot Study of Terazosin for Parkinson's Disease [NCT03905811]Phase 1/Phase 213 participants (Actual)Interventional2019-09-24Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00000620 (6) [back to overview]Death From Any Cause in the Glycemia Trial.
NCT00000620 (6) [back to overview]First Occurrence of a Major Cardiovascular Event (MCE); Specifically Nonfatal Heart Attack, Nonfatal Stroke, or Cardiovascular Death (Measured Throughout the Study) in the Glycemia Trial.
NCT00000620 (6) [back to overview]First Occurrence of Major Cardiovascular Event (MCE) in the Blood Pressure Trial.
NCT00000620 (6) [back to overview]First Occurrence of Major Cardiovascular Event (MCE) in the Lipid Trial.
NCT00000620 (6) [back to overview]First Occurrence of MCE or Revascularization or Hospitalization for Congestive Heart Failure (CHF) in Lipid Trial.
NCT00000620 (6) [back to overview]Stroke in the Blood Pressure Trial.
NCT01530243 (3) [back to overview]Lower Urinary Tract Symptoms (LUTS)
NCT01530243 (3) [back to overview]Pain
NCT01530243 (3) [back to overview]Quality of Life
NCT02046395 (2) [back to overview]Change in the Level of Urinary Free Light Chains
NCT02046395 (2) [back to overview]Change in Urine Microalbumin Creatinine Ratio
NCT03905811 (6) [back to overview]Frequency of Drop-out From Study/Discontinuation of Study Intervention for Any Reason
NCT03905811 (6) [back to overview]Incidence of Falls Between Treatment Arms
NCT03905811 (6) [back to overview]Incidence of Intervention-related Adverse Events Between Treatment Arms
NCT03905811 (6) [back to overview]Number of Participants With Intolerable Side Effects
NCT03905811 (6) [back to overview]Participants Demonstrating Non-Compliance
NCT03905811 (6) [back to overview]To Assess the Mean Change in Blood Pressure

Death From Any Cause in the Glycemia Trial.

"Time to death from any cause. Secondary measure for Glycemia Trial.~A finding of higher mortality in the intensive-therapy group led to an early discontinuation of therapy after a mean of 3.5 years of follow-up. Intensive arm participants were transitioned to standard arm strategy over a period of 0.2 year and followed for an additional 1.2 years to the planned end of the Glycemia Trial while participating in one of the other sub-trials (BP or Lipid)." (NCT00000620)
Timeframe: 4.9 years

Interventionparticipants (Number)
Glycemia Trial: Intensive Control391
Glycemia Trial: Standard Control327

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First Occurrence of a Major Cardiovascular Event (MCE); Specifically Nonfatal Heart Attack, Nonfatal Stroke, or Cardiovascular Death (Measured Throughout the Study) in the Glycemia Trial.

"Time to first occurrence of nonfatal myocardial infarction, nonfatal stroke, or cardiovascular death. This was the primary outcome measure in all three trials: Glycemia (all participants), Blood Pressure (subgroup of participants not in Lipid Trial), and Lipid (subgroup of participants not in Blood Pressure Trial).~In the Glycemia Trial, a finding of higher mortality in the intensive arm group led to an early discontinuation of therapy after a mean of 3.5 years of follow-up. Intensive arm participants were transitioned to standard arm strategy over a period of 0.2 year and followed for an additional 1.2 years to the planned end of the Glycemia Trial while participating in one of the other sub-trials (BP or Lipid) to their planned completion." (NCT00000620)
Timeframe: 4.9 years

Interventionparticipants (Number)
Glycemia Trial: Intensive Control503
Glycemia Trial: Standard Control543

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First Occurrence of Major Cardiovascular Event (MCE) in the Blood Pressure Trial.

Time to first occurrence of nonfatal myocardial infarction, nonfatal stroke, or cardiovascular death. Primary outcome for Blood Pressure Trial. (NCT00000620)
Timeframe: 4.7 years

Interventionparticipants (Number)
BP Trial: Intensive Control208
BP Trial: Standard Control237

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First Occurrence of Major Cardiovascular Event (MCE) in the Lipid Trial.

Time to first occurrence of nonfatal myocardial infarction, nonfatal stroke, or cardiovascular death in Lipid Trial participants. (NCT00000620)
Timeframe: 4.7 years

Interventionparticipants (Number)
Lipid Trial: Fenofibrate291
Lipid Trial: Placebo310

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First Occurrence of MCE or Revascularization or Hospitalization for Congestive Heart Failure (CHF) in Lipid Trial.

Time to first occurrence of nonfatal myocardial infarction, nonfatal stroke, cardiovascular death, revascularization procedure or hospitalization for CHF in Lipid Trial participants. (NCT00000620)
Timeframe: 4.7 years

Interventionparticipants (Number)
Lipid Trial: Fenofibrate641
Lipid Trial: Placebo667

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Stroke in the Blood Pressure Trial.

Time to first occurrence of nonfatal or fatal stroke among participants in the BP Trial. (NCT00000620)
Timeframe: 4.7 years

Interventionparticipants (Number)
BP Trial: Intensive Control36
BP Trial: Standard Control62

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Lower Urinary Tract Symptoms (LUTS)

LUTS was evaluated using the International Prostate Symptom Score (IPSS) questionnaire perioperatively. The IPSS constitutes of seven questions assigned score from 0 to 5 to evaluate the severity of LUTS in patients. Total scoring of IPSS ranges from 0 to 35, asymptomatic to very symptomatic. The more the score on scale is, the worse the outcome is.Therefore, the higher values represent worse outcomes. (NCT01530243)
Timeframe: Expected average of 2 weeks

Interventionunits on a scale (Mean)
Placebo11.12
Terazosin4.39
Tolterodine7.21
Tolterodine + Terazosin5.58

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Pain

The visual analogue scale (VAS) was used to evaluate the pain at the time of voiding. This VAS scoring ranges from 0 to 10. The higher values represent worse outcomes, having more pain. (NCT01530243)
Timeframe: Expected 2 weeks later

Interventionunits on a scale (Mean)
Placebo4.16
Terazosin3.21
Tolterodine1.34
Tolterodine + Terazosin1.37

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Quality of Life

The Quality of life of patients was evaluated using single question in IPSS questionnaire in which each of patients received scoring from 0 to 6. The higher values represent the worse quality of life. (NCT01530243)
Timeframe: Expected 2 weeks later

Interventionunits on a scale (Mean)
Placebo3.37
Terazosin2
Tolterodine2.30
Tolterodine + Terazosin0.95

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Change in the Level of Urinary Free Light Chains

In relation to kidney function and washout/reintroduction of ACE/ARB medication the level of urinary free light chains will be assessed. (NCT02046395)
Timeframe: Visit 1 (Baseline), Visit 3 (Day 60)

Interventionmg/g (Mean)
Alternate Antihypertensive Arm1.14

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Change in Urine Microalbumin Creatinine Ratio

Kidney function will be assessed throughout the study to assess changes in function prior to the washout of ACE/ARB medication and reintroduction of the ACE/ARB medication. (NCT02046395)
Timeframe: Visit 1 (Baseline), Visit 3 (Day 60)

Interventionmg/g (Mean)
Alternate Antihypertensive Arm15

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Frequency of Drop-out From Study/Discontinuation of Study Intervention for Any Reason

The number of participants in each group who drop out of the study for any reason will be compared. (NCT03905811)
Timeframe: 12 weeks

InterventionParticipants (Count of Participants)
Active3
Placebo0

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Incidence of Falls Between Treatment Arms

The number of participants in each group who report a fall, as determined by the site investigator, will be reported. (NCT03905811)
Timeframe: 12 weeks

InterventionEvent (Number)
Active0
Placebo0

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Number of Participants With Intolerable Side Effects

How many participants discontinued study as a result of intolerable adverse events that were deemed to be medication-related. (NCT03905811)
Timeframe: 12 weeks

InterventionParticipants (Count of Participants)
Active3
Placebo0

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Participants Demonstrating Non-Compliance

All participants will be asked to bring their study intervention bottles to their 6 week visit and their 12 week visit so the Investigational Drug Pharmacy can count remaining pills and assess compliance based on dispensing history. A participant will be considered non-compliant if they had more than 5 missed doses during the course of the study. (NCT03905811)
Timeframe: At 2 weeks, 6 weeks and 12 weeks

,
InterventionParticipants (Count of Participants)
Non-compliance at 2 weeksNon-compliance at 6 weeksNon-compliance at 12 weeks
Active000
Placebo000

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To Assess the Mean Change in Blood Pressure

Mean change in sitting systolic blood pressure and diastolic blood pressure from baseline reading at 2 weeks, 6 weeks, and 12 weeks. A negative number indicates a decrease in blood pressure while a positive number indicates an increase in blood pressure. (NCT03905811)
Timeframe: At Baseline, 2 weeks, 6 weeks, and 12 weeks

,
InterventionmmHg (Mean)
Systolic at 2 weeksSystolic at 6 weeksSystolic at 12 weeksDiastolic at 2 weeksDiastolic at 6 weeksDiastolic at 12 weeks
Active-5.29-15.05-11.0-2.00-5.29-9.40
Placebo-2.202.20-3.20-2.204.20-2.00

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