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phenoxybenzamine

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Description

Phenoxybenzamine is a non-selective, irreversible alpha-adrenergic receptor antagonist. It is a synthetic compound that was first synthesized in the 1950s. Phenoxybenzamine blocks the effects of norepinephrine and epinephrine, which are neurotransmitters that stimulate alpha-adrenergic receptors. These receptors are found in the smooth muscles of the blood vessels, the heart, the gastrointestinal tract, and the urinary tract. Phenoxybenzamine has been used to treat a variety of conditions, including hypertension, pheochromocytoma, and Raynaud's phenomenon. It is also used in the treatment of benign prostatic hyperplasia (BPH). Phenoxybenzamine is a potent drug with a long duration of action. It can cause a variety of side effects, including hypotension, tachycardia, and dizziness. It is important to note that phenoxybenzamine is not a first-line treatment for any of the conditions mentioned above. There are other drugs that are generally considered to be safer and more effective. Phenoxybenzamine is typically reserved for patients who have not responded to other treatments. Phenoxybenzamine is still studied today to understand its potential therapeutic applications in various medical conditions and to develop new and improved drugs that target the alpha-adrenergic receptors.'

Phenoxybenzamine: An alpha-adrenergic antagonist with long duration of action. It has been used to treat hypertension and as a peripheral vasodilator. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID4768
CHEMBL ID753
CHEBI ID8077
SCHEMBL ID5722
MeSH IDM0016529

Synonyms (139)

Synonym
AC-13214
AB00053702-12
benzylamine, n-(2-chloroethyl)-n-(1-methyl-2-phenoxyethyl)-
benzenemethanamine, n-(2-chloroethyl)-n-(1-methyl-2-phenoxyethyl)-
DIVK1C_000800
KBIO1_000800
n-(2-chloroethyl)-n-(phenylmethyl)-1-(phenyloxy)propan-2-amine
dibenzyline
bensylyt
688a
hsdb 4005
n-(2-chloroethyl)-n-(1-methyl-2-phenoxyethyl)benzenemethanamine
dibenyline
2-(n-benzyl-2-chloroethylamino)-1-phenoxypropane
einecs 200-446-8
fenossibenzamina [dcit]
phenoxybenzaminum [inn-latin]
brn 2129697
n-phenoxyisopropyl-n-benzyl-beta-chloroethylamine
phenoxybenzamine [inn:ban]
benzylyt
dibenylene
benzyl(2-chloroethyl)-(1-methyl-2-phenoxyethyl)amine
n-(2-chloroethyl)-n-(1-methyl-2-phenoxyethyl)benzylamine
fenoxibenzamina [inn-spanish]
a 688
nsc 37448
ccris 505
dibenylin
SPECTRUM_000378
IDI1_002234
BSPBIO_002356
PRESTWICK2_000944
BIO2_000959
BIO2_000479
BSPBIO_001278
BSPBIO_000908
IDI1_000800
PRESTWICK3_000944
LOPAC0_000235
AB00053702
C07435
phenoxybenzamine
59-96-1
DB00925
fenossibenzamina
SPECTRUM5_001370
NCGC00089748-05
NCGC00089748-04
KBIO3_001095
KBIO2_005754
KBIOGR_001158
KBIO2_005994
KBIO2_003426
KBIO2_000618
KBIO2_000858
KBIO3_001096
KBIOSS_000858
KBIO2_003186
KBIOSS_000618
KBIOGR_000618
SPBIO_001829
SPECTRUM2_001815
SPECTRUM4_000769
PRESTWICK0_000944
SPBIO_003067
NINDS_000800
PRESTWICK1_000944
BPBIO1_001000
NCGC00089748-07
NCGC00089748-03
HMS1990P19
HMS2089J09
NCGC00015121-11
chebi:8077 ,
CHEMBL753 ,
L001197
phenoxybenzamine (inn)
D08358
HMS1792P19
HMS1362P19
n-benzyl-n-(2-chloroethyl)-1-phenoxypropan-2-amine
bdbm50017679
benzyl-(2-chloro-ethyl)-(1-methyl-2-phenoxy-ethyl)-amine
NCGC00015121-08
4-12-00-02204 (beilstein handbook reference)
phenoxybenzaminum
0ttz664r7z ,
fenoxibenzamina
unii-0ttz664r7z
cas-59-96-1
dtxsid0023458 ,
tox21_110087
dtxcid803458
CCG-204330
AKOS015961144
NCGC00015121-09
NCGC00015121-14
NCGC00015121-12
NCGC00015121-04
NCGC00015121-06
NCGC00015121-03
NCGC00015121-13
NCGC00015121-05
NCGC00015121-07
bensylyte
NCGC00015121-16
benzyl(2-chloroethyl)(1-phenoxypropan-2-yl)amine
gtpl7268
n-phenoxyisopropyl-n-benzyl-.beta.-chloroethylamine
(+/-)-phenoxybenzamine
phenoxybenzamine [who-dd]
102737-84-8
phenoxybenzamine [hsdb]
phenoxybenzamine [vandf]
phenoxybenzamine [inn]
phenoxybenzamine [mi]
SCHEMBL5722
NCGC00015121-17
tox21_110087_1
Q-201556
n-benzyl-n-(2-chloroethyl)-1-phenoxy-2-propanamine #
HMS3403P19
AB00053702_14
AB00053702_13
EN300-57590
MRF-0000619
SBI-0050223.P003
Q419824
59-96-1 (free)
SDCCGSBI-0050223.P004
FT-0778642
SB82886
CS-0255342
HY-B0431
fenoxibenzamina (inn-spanish)
phenoxybenzaminum (inn-latin)
c04ax02
n-(2-chloroethyl)-n-(1-methyl-2-phenoxyethyl)-benzenemethanamine

Research Excerpts

Overview

Phenoxybenzamine (PBZ) is an FDA approved α-1 adrenergic receptor antagonist. It is currently used to treat symptoms of pheochromocytoma.

ExcerptReferenceRelevance
"Phenoxybenzamine (PXB) is a commonly used α-blockade to prevent it."( Influence of duration of preoperative treatment with phenoxybenzamine and secretory phenotypes on perioperative hemodynamics and postoperative outcomes in pheochromocytoma and paraganglioma.
Fan, J; Guo, Y; Lin, T; Wang, L; Yao, Y; Zhang, S, 2023
)
1.88
"Phenoxybenzamine (PBZ) is an FDA approved α-1 adrenergic receptor antagonist that is currently used to treat symptoms of pheochromocytoma. "( Phenoxybenzamine is neuroprotective in a rat model of severe traumatic brain injury.
Kothiwal, A; Poulsen, DJ; Rau, TF; Rhoderick, JF; Rova, A, 2014
)
3.29
"Phenoxybenzamine (PBZ) is a nonselective, irreversible alpha-adrenergic receptor antagonist that is approved for the treatment of diaphoresis and hypertension associated with pheochromocytoma. "( A modern rationale for the use of phenoxybenzamine in urinary tract disorders and other conditions.
Te, AE, 2002
)
2.04
"Phenoxybenzamine is an effective agent with a prolonged duration of action, specifically preventing catecholamine mediated vasospasm of radial artery conduits."( Comparative efficacies and durations of action of phenoxybenzamine, verapamil/nitroglycerin solution, and papaverine as topical antispasmodics for radial artery coronary bypass grafting.
Black, E; Channon, KM; Dipp, MA; Guzik, TJ; Mussa, S; Taggart, DP, 2003
)
1.29
"Phenoxybenzamine is an irreversible, selective alpha 1-adrenoceptor antagonist that results in long-lasting attenuation of the effects of alpha-adrenoceptor agonists in vivo and in vitro. "( Recovery in vivo and in vitro of alpha-adrenoceptor responses and radioligand binding after phenoxybenzamine.
Dalrymple, H; Hamilton, C; Reid, J, 1982
)
1.93
"Phenoxybenzamine is a valuable drug in the treatment of patients with severe vasospastic disease."( Finger systolic pressures and skin temperatures in severe Raynaud's syndrome: the relationship to healing of skin lesions and the use of oral phenoxybenzamine.
Carter, SA, 1981
)
1.19
"Phenoxybenzamine is a safe and effective vasodilator which usually causes an increase in arterial blood pressure, an increase in cardiac index, an increase in urine output and a decrease in pulmonary artery pressure and central venous pressure in states of severe shock if hypovolemia has been corrected. "( Treatment of severe shock with phenoxybenzamine.
Hardaway, RM, 1980
)
1.99
"Phenoxybenzamine is a welcomed adjunct in the pharmacologic management of patients with neurogenic bladder dysfunction resulting from spinal cord trauma. "( Phenoxybenzamine in neurogenic bladder dysfunction after spinal cord injury. I. Voiding dysfunction.
Morrow, JW; Scott, MB, 1978
)
3.14
"Phenoxybenzamine is a potent irreversible H1 receptor antagonist in a variety of tissues. "( Resistance of the histamine H2 receptor in guinea-pig heart to blockade by phenoxybenzamine.
Cook, DA; Krueger, CA, 1978
)
1.93
"Phenoxybenzamine is a beta-haloalkylamine which alkylates chemically active radicals such as hydroxy, sulfhydryl, and amino groups."( Phenoxybenzamine selectively and irreversibly inactivates dopaminergic D2 receptors on primary cultured rat lactotrophs.
Heisler, RL; McAssey, K; Shin, SH; Szabo, MS, 1992
)
2.45
"Phenoxybenzamine is a beta-haloalkylamine which alkylates and irreversibly inactivates adrenergic alpha-receptors in smooth muscle."( High concentrations of dopamine and epinephrine protect dopaminergic D2 receptors from inactivation by phenoxybenzamine on primary cultured rat lactotrophs.
Heisler, RL; Shin, SH, 1992
)
1.22
"Phenoxybenzamine was confirmed to be a potent inhibitor of both the Uptake(2) and Uptake(1) mechanisms, with IC50 values for these two systems of 2.8 muM and 0.9 muM respectively.4."( Inhibition of catecholamine uptake in the isolated rat heart by haloalkylamines related to phenoxybenzamine.
Iversen, LL; Salt, PJ; Wilson, HA, 1972
)
1.19

Effects

Phenoxybenzamine has been the standard agent for blockade before adrenalectomy for pheochromocytoma. It has been shown to have a depressant action on K+-depolarization contracture in cat ventricular muscle.

ExcerptReferenceRelevance
"Phenoxybenzamine has an extended action in arterial grafts in vivo."( Duration of action of antispasmodic agents: novel use of a mouse model as an in vivo pharmacological assay.
Alp, N; Channon, KM; Mussa, S; Prior, T; Taggart, DP; Wood, K, 2004
)
1.04
"Phenoxybenzamine has been the standard agent for blockade before adrenalectomy for pheochromocytoma. "( Phenoxybenzamine is no longer the standard agent used for alpha blockade before adrenalectomy for pheochromocytoma: A national study of 552 patients.
Chen, L; Kuo, EJ; Kuo, JH; Lee, JA; McManus, CM; Wright, JD, 2023
)
3.8
"Phenoxybenzamine has an extended action in arterial grafts in vivo."( Duration of action of antispasmodic agents: novel use of a mouse model as an in vivo pharmacological assay.
Alp, N; Channon, KM; Mussa, S; Prior, T; Taggart, DP; Wood, K, 2004
)
1.04
"Phenoxybenzamine (Dibenzyline) has been extremely effective in treating patients with detrusor dyssynergia. "( Effect of phenoxybenzamine (dibenzyline) on sexual function in man.
Kedia, KR; Persky, L, 1981
)
2.11
"Phenoxybenzamine has been shown to have a depressant action on K+-depolarization contracture in cat ventricular muscle. "( Depressant effects of phenoxygenzamine on potassium contracture in cat ventricular muscle.
Bassett, AL; Gelband, H; Wiggins, JR, 1979
)
1.7
"Phenoxybenzamine has been extremely effective in treating patients with vesical dysfunctions, its minimal side effects include anejaculation and delay and difficulty in ejaculation. "( Effect of an alpha-blocking agent (phenoxybenzamine) in the management of premature ejaculation.
Beretta, G; Chelo, E; Fanciullacci, F; Zanollo, A,
)
1.85

Actions

Phenoxybenzamine does not inhibit reduction in blood pressure and plasma catecholamines induced by clonidine in patients with essential hypertension. Phenoxybenchzamine was shown to increase bladder neck opening by an average of 30% and give symptomatic relief.

ExcerptReferenceRelevance
"Phenoxybenzamine may blunt intraoperative hypertension better than doxazosin, but this difference did not translate to fewer cardiovascular complications and is offset by a considerably increased cost."( Comparison of Preoperative Alpha-blockade for Resection of Paraganglioma and Pheochromocytoma.
Hong, JC; Hu, MY; Isorena, J; Kamdar, NV; Kuo, EJ; Lee, JS; Livhits, MJ; Tseng, CH; Yeh, MW; Yu, R; Zhu, CY, 2022
)
2.16
"Phenoxybenzamine does not inhibit reduction in blood pressure and plasma catecholamines induced by clonidine in patients with essential hypertension or interfere with the clonidine suppression test in patients with pheochromocytomas."( Effect of phenoxybenzamine on cardiovascular and plasma catecholamine responses to clonidine.
Gross, M; Sisson, J; Zweifler, A, 1983
)
1.39
"Phenoxybenzamine was shown to increase bladder neck opening by an average of 30% and give symptomatic relief."( Effects of phenoxybenzamine on bladder neck opening.
Waterfall, NB; Williams, G, 1980
)
1.37
"Phenoxybenzamine does not produce detrimental effects if given in appropriate instances."( Treatment of severe shock with phenoxybenzamine.
Hardaway, RM, 1980
)
1.27
"Phenoxybenzamine did not cause any effects additional to those attributable to the solvent alone."( Effects of some alpha-adrenoceptor antagonists on central cardio-decelerator mechanisms in the rabbit.
Evans, MH, 1985
)
0.99
"1) Phenoxybenzamine was found to cause irreversible antagonism of the effects of 5-hydroxytryptamine (5-HT)."( Interconversion into a low active state protects vascular 5-HT2-receptors against irreversible antagonism by phenoxybenzamine.
Frenken, M; Kaumann, AJ, 1987
)
1

Treatment

Phenoxybenzamine treatment caused nonparallel rightward shifts of the concentration-response curves to the lower concentrations of noradrenaline and adrenaline. It also reduced maximal specific binding of the alpha 1-selective antagonist [3H]prazosin to liver cell membranes.

ExcerptReferenceRelevance
"Phenoxybenzamine pretreatment had no effect on peri-operative mortality."( Risk factors influencing death prior to discharge in 302 dogs undergoing unilateral adrenalectomy for treatment of primary adrenal gland tumours.
Abrams, BE; Amsellem, P; Cray, MT; Dornbusch, JA; Lapsley, JM; Liptak, JM; Murphy, C; Piegols, HJ; Selmic, LE; Skinner, OT; Souza, CH; Stephens, JA; Traverson, M; Williams, E; Wustefeld-Janssens, BG, 2023
)
1.63
"Phenoxybenzamine treatment showed a dose-dependent effect on cell viability over several clinically employed concentrations."( Phenoxybenzamine treatment can lead to loss of endothelial cell viability.
Browning, PG; Conant, AR; Dihmis, WC; Pai, KR, 2008
)
2.51
"Phenoxybenzamine-treated radial artery failed to respond to noradrenaline but did respond to vasopressin, angiotensin II, endothelin-1, and KCl. "( Phenoxybenzamine treatment is insufficient to prevent spasm in the radial artery: the effect of other vasodilators.
Chester, MR; Conant, AR; Dihmis, WC; Oo, AY; Shackcloth, MJ; Simpson, AW, 2003
)
3.2
"In phenoxybenzamine-treated sections of radial artery, circulating vasoconstrictor agonists may still contribute to the induction of spasm. "( Phenoxybenzamine treatment is insufficient to prevent spasm in the radial artery: the effect of other vasodilators.
Chester, MR; Conant, AR; Dihmis, WC; Oo, AY; Shackcloth, MJ; Simpson, AW, 2003
)
2.38
"Phenoxybenzamine treatment enabled his indwelling catheter to be discarded in favour of a penile sheath, but it caused unacceptable dizziness and was stopped after 7 years."( Chronic lymphocytic leukaemia, synchronous small cell carcinoma and squamous neoplasia of the urinary bladder in a paraplegic man following long-term phenoxybenzamine therapy.
Hughes, PL; Mansour, P; Singh, G; Soni, BM; Vaidyanathan, S, 2006
)
1.25
"In phenoxybenzamine-treated cats, the maximum output of noradrenaline of 4 ng/stimulus was obtained at 5 or 10/sec."( Release of noradrenaline by splenic nerve stimulation and its dependence on calcium.
Kirpekar, SM; Misu, Y, 1967
)
0.76
"Phenoxybenzamine treatment did not inhibit enzymes involved in PG synthesis, inasmuch as bradykinin was capable of markedly stimulating PG release from IBC treated with phenoxybenzamine."( Alpha-adrenergic stimulation of prostaglandin release from rabbit iris-ciliary body in vitro.
Dunham, EW; Engstrom, P, 1982
)
0.99
"In phenoxybenzamine-treated dogs, bulbocapnine, a dopamine antagonist, blocked the increases in RBF stimulated by intrarenal injections of 0.1 to 24 micrograms/kg dopamine but had no effect on the responses to 0.5 to 100 ng/kg of PGE2."( Renal vasodilation by a prostaglandin analog during dopaminergic and alpha-adrenergic blockade.
Blaine, EH; Seymour, AA, 1983
)
0.78
"In phenoxybenzamine-pretreated preparations, Sgd 101/75 (400 microM) did not antagonise NA (maximal effect and EC50 values not changed significantly), so it was concluded that Sgd 101/75 and NA interact with different alpha 1-adrenoceptor subtypes in this tissue."( Sgd 101/75: a sympathomimetic that can be used to identify a new subtype of alpha-adrenoceptor, the alpha 1s-adrenoceptor.
Chadwick, MA; Coates, J; Ismail, S; Jahn, U; Lawson, K; Thiele, K; Turner, N; Weetman, DF, 1983
)
0.78
"Phenoxybenzamine treatment also caused a dose-dependent reduction in specific [3H]prazosin and [3H]clonidine binding."( Acute effects of phenoxybenzamine on alpha-adrenoceptor responses in vivo and in vitro: relation of in vivo pressor responses to the number of specific adrenoceptor binding sites.
Hamilton, CA; Reid, JL; Sumner, DJ,
)
1.19
"Phenoxybenzamine treatment reduced maximal specific binding of the alpha 1-selective antagonist [3H]prazosin to liver cell membranes."( Simultaneous loss and reappearance of alpha 1-adrenergic responses and [3H]prazosin binding sites in rat liver after irreversible blockade by phenoxybenzamine.
Deth, RC; Lynch, CJ; Steer, ML, 1983
)
1.19
"3. Phenoxybenzamine treatment caused nonparallel rightward shifts of the concentration-response curves to the lower concentrations of noradrenaline and adrenaline."( Characterization of the contractile responses to noradrenaline and adrenaline of aorta from normotensive and hypertensive rats.
Doggrell, SA, 1994
)
0.8
"Phenoxybenzamine pretreatment produced a significant rightward shift and depression of the upper asymptote of the noradrenaline concentration-effect (E/[A]) curve."( Analysis of receptor inactivation experiments with the operational model of agonism yields correlated estimates of agonist affinity and efficacy.
Stam, WB; Van der Graaf, PH,
)
0.85
"phenoxybenzamine pretreatment might be of importance in warm ischaemia as it seems to delay the consequences."( Ultrastructure of the liver after 24-hour preservation with various solutions.
Faller, J; Ungváry, G, 1977
)
0.98
"Phenoxybenzamine pretreatment reduced the maximal response to NK-1 agonists and produced a rightward shift of the curve to NK-2 agonists, without depression of the maximum."( Tachykinin receptors in the guinea-pig isolated bronchi.
Maggi, CA; Patacchini, R; Quartara, L; Rovero, P; Santicioli, P, 1991
)
1
"Oral phenoxybenzamine treatment in 2 subjects did not significantly affect either the number of EMG bursts of the BC or the subjective pleasure of the orgasm but did significantly reduce the volume of semen expelled."( Erection and ejaculation in man. Assessment of the electromyographic activity of the bulbocavernosus and ischiocavernosus muscles.
Gerstenberg, TC; Levin, RJ; Wagner, G, 1990
)
0.73
"Phenoxybenzamine treatment did not change the resting cardiac output or systemic vascular resistance."( Hemodynamic observations during paroxysmal hypertension in a pregnancy with pheochromocytoma.
Benedetti, TJ; Combs, CA; Easterling, TR; Schmucker, BC, 1989
)
1
"Phenoxybenzamine-pretreatment completely prevented the pressor response without altering the tachycardiac response, whereas propranolol intervention completely inhibited the tachycardiac response and also attenuated the pressor response."( The involvement of the sympathetic nervous system in the centrogenic pressor and tachycardiac effects of prostaglandins E2 and F2 alpha in anaesthetised cats.
Manchanda, SC; Nayar, U; Rao, TS; Seth, SD, 1987
)
0.99
"Phenoxybenzamine pretreatment also blunted endotoxin-induced mortality (LD80), hypoglycemia, hemoconcentration, and decreased plasma beta-glucuronidase (BG)."( The effects of alpha adrenergic blockade on arachidonic acid metabolism and shock sequelae in endotoxemia.
Armstrong, J; Cook, JA; Halushka, PV; Tempel, GE; Wise, WC, 1986
)
0.99
"In phenoxybenzamine treated cats, reduction of sodium in the perfusing solution also increased the noradrenaline output by nearly twofold following either the low or the high dose of KCl.5."( Release of noradrenaline from the cat spleen by potassium.
Kirpekar, SM; Wakade, AR, 1968
)
0.76
"Treatment with phenoxybenzamine and dichloroisoprenaline prevented the rise of blood pressure, contraction of the nictitating membrane and increase in cardiac contractile force produced by intravenous injections of bretylium and guanethidine in anaesthetized or spinal cats. "( Mechanism of the initial adrenergic effects of bretylium and guanethidine.
GOKHALE, SD; GULATI, OD; KELKAR, VV, 1963
)
0.59
"Pretreatment with phenoxybenzamine, an alpha adrenoceptor blocking agent, resulted in a small but statistically significant attenuation in the response of SCBF to brushing."( Responses of dorsal spinal cord blood flow to innocuous cutaneous stimulation in anesthetized rats.
Budgell, B; Kurosawa, M; Maruyama, H; Watanabe, O, 2006
)
0.66
"Treatment with phenoxybenzamine resulted in a dose-dependent reduction in the maximum pressor response to both phenylephrine and guanabenz, although phenoxybenzamine was a more potent antagonist at postsynaptic alpha 1- than at postsynaptic alpha 2-adrenoceptors."( Acute effects of phenoxybenzamine on alpha-adrenoceptor responses in vivo and in vitro: relation of in vivo pressor responses to the number of specific adrenoceptor binding sites.
Hamilton, CA; Reid, JL; Sumner, DJ,
)
0.81
"Pretreatment with phenoxybenzamine or diethyldithiocarbamate suppressed the LH increase induced by naloxone, whereas pretreatment with propranolol had no significant effects on the naloxone-induced LH release."( Evidence for noradrenergic involvement in naloxone-induced stimulation of luteinizing hormone release in prepubertal female rats.
Imura, H; Kinoshita, F; Koh, T; Nakai, Y; Tsujii, S; Tsukada, T, 1983
)
0.59
"Treatment with phenoxybenzamine caused an irreversible, dose-dependent decrease in the density of both alpha 1- and alpha 2-adrenergic receptors."( Phenoxybenzamine is more potent in inactivating alpha 1- than alpha 2-adrenergic receptor binding sites.
Minneman, KP, 1983
)
2.05
"Pretreatment with phenoxybenzamine (100 microgram/kg, iv) completely blocked the effects of norepinephrine on blood pressure and heart rate but only partially (about 50%) inhibited the norepinephrine effect on ADH release."( The role of central adrenoreceptors in the control of vasopressin release and blood pressure.
Crofton, JT; Kimura, T; Share, L; Wang, BC, 1981
)
0.59
"Treatment with phenoxybenzamine (1 microM) plus atenolol also reduced adenosine release (7.4 +/- 0.8 nmol/g/20 min)."( Adenosine formation during hypoxia in isolated hearts: effect of adrenergic blockade.
Gorman, MW; He, MX; Sparks, HV, 1994
)
0.63
"Pretreatment with phenoxybenzamine accentuated the inhibitory actions of captopril and a combination of phenoxybenzamine and captopril significantly increased the ED50 without altering the maximum response."( Pressor responses to the alpha 1-adrenoceptor agonist cirazoline: effects of captopril, phenoxybenzamine and nifedipine.
Tabrizchi, R; Triggle, CR, 1994
)
0.83
"Pretreatment with phenoxybenzamine decreased maximal responses to norepinephrine (NE) with only small decreases in apparent potency, suggesting similar small receptor reserves for all three subtypes."( Selectivity of agonists for cloned alpha 1-adrenergic receptor subtypes.
Esbenshade, TA; Han, C; Hollinger, S; Minneman, KP; Theroux, TL, 1994
)
0.61
"Pretreatment with phenoxybenzamine, guanethidine, or reserpine attenuated vasopressor activities of these peptides."( Vasopressor activities of N-terminal fragments of adrenomedullin in anesthetized rat.
Inui, T; Itahara, Y; Nakajima, K; Sakakibara, S; Watanabe, TX; Yoshizawa-Kumagaye, K, 1996
)
0.62
"Pretreatment with phenoxybenzamine (5 mg/kg) attenuated the pressor response, consistent with sympathetically mediated vasoconstriction."( Nociceptin/orphanin FQ increases blood pressure and heart rate via sympathetic activation in sheep.
Arndt, ML; Soong, Y; Szeto, HH; Wu, D, 1999
)
0.63
"Pretreatment with phenoxybenzamine (3 microM) abolished responses to UK-14304, but left those elicited by oxymetazoline largely unaffected."( Evidence for a non-adrenoceptor, imidazoline-mediated contractile response to oxymetazoline in the porcine isolated rectal artery.
Blaylock, NA; Chan, SL; Dunn, WR; Minyan, W; Wilson, VG, 2001
)
0.63
"Pretreatment with phenoxybenzamine (10(-5)M) increases the size of the neurogenic response and displaces the NE dose-relaxation curve to the left."( Facial vein in the rabbit. Neurogenic vasodilation mediated by beta-adrenergic receptors.
Bevan, JA; Bevan, RD; Pegram, BL, 1976
)
0.58
"Treatment with phenoxybenzamine was found valuable in patients with multiple sclerosis and poor bladder emptying as well as in patients with lower motor neuron bladder paresis."( Alpha-blockers and urethral pressure in neurological patients.
Nordling, J, 1978
)
0.6
"A pretreatment by phenoxybenzamine of the animals did not affect epinephrine influence whereas a pretreatment by propranolol completely abolished the inhibitory effect of epinephrine on gastric motility."( The role of adrenergic receptors in the regulation of gastric motility in the rat.
Gáti, T; Gelencsér, F; Hideg, J, 1975
)
0.58
"Pretreatment with phenoxybenzamine and perfusion by an albumin-containing solution reduced the lesion of the liver, while prednisolone and oxygenation of the perfusion solution improved preserving effect only moderately."( Enzyme histochemical studies of the preserved rat liver.
Faller, J; Kokas, P; Kupcsulik, P, 1976
)
0.58
"Pretreatment with phenoxybenzamine completely prevented the fusion of components I and II, although the mean arterial blood pressure was substantially lower than in dogs not pretreated with phenoxybenzamine."( Intrarenal blood flow distribution during endotoxemia in dogs.
Neiberger, RE; Passmore, JC, 1978
)
0.58
"Pretreatment with phenoxybenzamine, an alpha-adrenoceptor antagonist, also abolished the inhibitory effect of tyramine on renin release, indicating that alpha-adrenoceptors mediated the observed inhibition of renin release."( Inhibitory effect of tyramine-induced release of catecholamines on renin secretion.
Herrmann, M; Meyer, DK, 1978
)
0.58
"Pretreatment with phenoxybenzamine (3.0 mg/l aquarium water), an alpha-adrenergic antagonist, abolished the cold-shock leucocytic phases, except 27 min."( Catecholamines and the abundance of blood cells in a fresh water tropical teleost (Colisa fasciatus) in relation to cold-shock.
Agrawal, U; Srivastava, AK, 1976
)
0.58
"Pretreatment with phenoxybenzamine reduced the pressor effect of all three compounds."( Pressor effects of tryptamine analogues.
Bosin, TR; Hixson, EJ; Maickel, RP, 1976
)
0.58
"Pretreatment with phenoxybenzamine decreased norepinephrine-stimulated 3H-InsP formation in a dose-dependent manner in both neurons and glia by decreasing the maximal response without altering potency."( Comparison of alpha 1-adrenergic receptor-stimulated inositol phosphate formation in primary neuronal and glial cultures.
Gilchrist, S; Minneman, KP; Wilson, KM, 1990
)
0.6
"Pretreatment with phenoxybenzamine enhanced the renal vasodilatory effect of TA-870."( A novel orally active dopamine prodrug TA-870. II. Evidence that TA-870 is a dopamine prodrug.
Akimoto, Y; Nakajima, H; Nishiyama, S; Yamaguchi, I; Yoshikawa, M, 1989
)
0.6
"Pretreatment with phenoxybenzamine (500 micrograms/100 g b.wt.i.v.), an alpha-antagonist, blunted the decrease of MBH DA levels induced by clonidine."( Effects of clonidine and naloxone on the dopamine levels in the rat mediobasal hypothalamus measured by in vivo voltammetry.
Imura, H; Kato, Y; Koshiyama, H; Shimatsu, A, 1989
)
0.6
"Pretreatment with phenoxybenzamine (0.5 mg/kg) prevented these changes in 8 of 10 dogs; however, this drug was ineffective if given after the cyanide."( Studies of cyanide poisoning.
Froehlich, HL; Vick, JA, 1985
)
0.59
"Treatment with phenoxybenzamine, alpha-adrenergic blocker, normalized the peripheral pulse responses, reduced the complaint of insomnia, and reduced the sleep related leg movements but resulted in only mild sleep improvements."( Peripheral vasoconstriction in patients with sleep related periodic leg movements.
Blumoff, R; Pittard, JT; Ware, JC, 1988
)
0.61
"Pretreatment with phenoxybenzamine (5 microM) reduced the maximum inhibition of release by about 50%."( The determination of presynaptic KA values of methacholine and pilocarpine and of a presynaptic receptor reserve in the rat perfused heart.
Fuchs, P; Fuder, H, 1985
)
0.59
"Treatment with phenoxybenzamine caused a decrease in the number of alpha but not beta adrenoceptor ligand binding sites on platelets from male rabbits and thus a decrease in the ratio of alpha/beta adrenoceptor number. "( Changes in rabbit platelet alpha and beta adrenoceptor number and platelet aggregation.
Deighton, NM; Hamilton, CA; Jones, CR; Reid, JL, 1986
)
0.62
"Pretreatment with phenoxybenzamine (5.0 mg/kg) resulted in a significant leftward shift of the control curve for stereotypy."( Influence of phenoxybenzamine on the stereotyped behaviour induced by fencamfamine in rats: evidence for a qualitative alteration.
Aizenstein, ML; Bernardi, MM; DeLucia, R; Scavone, C, 1985
)
0.96
"Pretreatment with phenoxybenzamine, piperoxane or cocaine further increased catecholamine excretion, but desipramine caused only a small increase in catecholamine excretion which did not correlate with its effect on dye extravasation.5 It is suggested that phenoxybenzamine, phentolamine, piperoxane and cocaine reduce vascular permeability in the mouse peritoneum by releasing and/or potentiating the effects of endogenous catecholamines on beta-adrenoceptors."( Role of endogenous catecholamines in the anti-inflammatory activity of alpha-adrenoceptor blocking agents.
Green, KL, 1974
)
0.58
"Treatment with phenoxybenzamine for 2 days, 20mg/kg/day, for 8 days, 10mg/kg/day, were did not prevent the rise causing a reduction in blood flow through the ovary rather than acting as a neurogenic stimulus in the hypothalamus."( Effect of phenoxybenzamine on luteinizing hormone release in the female rat.
Ratner, A; Solomon, S, 1971
)
0.99
"Pretreatment with phenoxybenzamine, phentolamine, propranolol, or atropine did not alter the redistribution of cortical flow during hemorrhage."( Mechanism of the redistribution of renal cortical blood flow during hemorrhagic hypotension in the dog.
Boonjarern, S; Ferris, TF; Mauk, RC; Stein, JH, 1973
)
0.58

Toxicity

ExcerptReferenceRelevance
" These data suggest that monoamines are involved in mediating the motor activity of cocaine but not implicated in the toxic effect of the drug."( [Attempt at modification of the pharmacological and toxic effects of cocaine].
Lallemant, AM, 1979
)
0.26
" One such possibility is that N2O causes adverse reproductive toxicity secondary to its sympathomimetic effects."( Preventive effects of phenoxybenzamine on nitrous oxide-induced reproductive toxicity in Sprague-Dawley rats.
Baden, JM; Fujinaga, M; Mazze, RI; Myatt, JK; Suto, A, 1991
)
0.6
"Treatment of RA grafts with phenoxybenzamine was associated with a reduction in perioperative myocardial injury and adverse cardiac events in this study population."( Radial artery graft treatment with phenoxybenzamine is clinically safe and may reduce perioperative myocardial injury.
Bourke, ME; Gunning, D; Kulik, A; Mesana, TG; Rubens, FD; Ruel, M, 2007
)
0.91
"Many adverse drug reactions are caused by the cytochrome P450 (CYP)-dependent activation of drugs into reactive metabolites."( Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
Jones, LH; Nadanaciva, S; Rana, P; Will, Y, 2016
)
0.43

Pharmacokinetics

ExcerptReferenceRelevance
" It was noted that the direction and the amplitude of changes concerning the half-life of Na131I do not depend on the blood pressure."( [Muscular clearance after administration of phenoxybenzamine in shock].
Cardan, E; Imre, S; Micluţia, M,
)
0.39
"Our preliminary pharmacodynamic studies on the lower urinary tract of adult female dogs indicate that cholinergic and adrenergic (alpha and beta) neuroreceptors in the urethra appear to coordinate the detrusor and urethral function during micturition."( Cholinergic and adrenergic neuroreceptors in urinary tract of female dogs. Evaluation of function with pharmacodynamics.
Gonick, P; Heber, D; Khanna, OP, 1975
)
0.25

Compound-Compound Interactions

ExcerptReferenceRelevance
"Inhibition of renal vasoconstriction during hyperacute rejection by phenoxybenzamine or methylprednisolone combined with either the antiplatelet agent pyridinolcarbamate or heparin was evaluted in primates."( Successful short-term modification of hyperacute renal allograft rejection in the primate. Intrarenal effects of phenoxybenzamine and methylprednisolone combined with heparin.
Busch, GJ; Colman, RW; Hollenberg, NK; Martins, AC; Moretz, RC; Wilson, RE, 1976
)
0.7
") was administered to pentobarbital-anesthetized dogs alone and combined with dopamine (DA) and dobutamine."( Cardiovascular and renal hemodynamic effects of intravenous infusions of the selective DA1 agonist, fenoldopam, used alone or in combination with dopamine and dobutamine.
Glock, D; Goldberg, LI; Lass, NA, 1988
)
0.27
"Forty-three children with overt neurological disease and neuropathic vesicourethral dysfunction were entered into a trial comparing clean intermittent catheterisation (CIC) with manual expression combined with drug treatment (non-CIC)."( Neuropathic vesicourethral dysfunction in children. A trial comparing clean intermittent catheterisation with manual expression combined with drug treatment.
Borzyskowski, M; Chantler, C; Haycock, GB; Joyce, MR; Kinder, CH; Mundy, AR; Neville, BG; Park, L, 1982
)
0.26
" Data were analysed using the 2R-1T model to characterize the observed exposure-response relationships and drug-drug interaction."( Quantitative systems pharmacology analysis of drug combination and scaling to humans: the interaction between noradrenaline and vasopressin in vasoconstriction.
Stam, WB; van der Graaf, PH; van Hasselt, JGC; Yamada, A; Yin, A, 2018
)
0.48
"The 2R-1T model can be of relevance to quantitatively characterize the interaction between two drugs that interact via different receptors and a common transducer pathway."( Quantitative systems pharmacology analysis of drug combination and scaling to humans: the interaction between noradrenaline and vasopressin in vasoconstriction.
Stam, WB; van der Graaf, PH; van Hasselt, JGC; Yamada, A; Yin, A, 2018
)
0.48

Bioavailability

ExcerptReferenceRelevance
" It is concluded that the addition of phenoxybenzamine to subcutaneously injected insulin increases the bioavailability of insulin for at least 3 h, which leads to a greater fall in plasma glucose concentrations."( Insulin absorption accelerated by alpha-adrenergic blockade at injection site.
Dandona, P; Gaylarde, PM; Grace, AA; Hyden, AM; Menon, RK,
)
0.4
"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

The authors compared the effects of an angiotensin antagonist (saralasin) and an alpha-adrenergic blocking agent (phenoxybenzamine) in supramaximal dosage. They found that the asystole of electroshock (ES) was significnatly prolonged by high spinal anesthesia in rabbits. In the presence of low concentrations of phenoxyBenzamine, the dose-response curve for histamine undergoes a parallel shift of about 0.5%.

ExcerptRelevanceReference
"7 log units in the dose-response curve to histamine."( Blockade of histamine-induced contractions of guinea pig ielum by beta-haloalkylamines.
Cook, DA; Kenakin, TP, 1976
)
0.26
" From dose-response curves for adrenaline and 5-hydroxytryptamine (5-HT) obtained in strips of rat aorta before and after incubation with each of the three blocking agents, the fractions of receptors remaining active for adrenaline and 5-HT, respectively, were estimated."( Selective alpha-adrenoceptor blocking actions of a new derivative of 2-halogenotheylamine: 6-(2-bromoethyl)-10,11-methylenedioxy-5,6,7,8-tetrahydrodibenz[c,e]azocine.
Ishida, Y; Kihar, M; Kobayashi, S; Watanabe, K, 1976
)
0.26
" Fentanyl also shifted the dose-response curve of the contractile response of aorta to norepinephrine to the right."( Alpha-adrenergic blocking action of fentanyl on the isolated aorta of the rabbit.
Hatano, Y; Toda, N, 1977
)
0.26
" Resistance to alpha adrenergic blocking agents developed when the patient's daily propranolol dosage was lowered from 10 to 1 mg/kg."( Childhood pheochromocytoma: treatment with alpha methyl tyrosine for resistant hypertension.
DeQuattro, V; Grushkin, CM; Lieberman, E; Robinson, RG, 1977
)
0.26
" It can be administered only subcutaneously or orally, and adequate dosage is necessary for a successful response."( Uropharmacology: v. choline esters and other parasympathomimetic drugs.
Bissada, NK; Finkbeiner, AE; Welch, LT, 1977
)
0.26
" Presynaptic alpha-adrenoceptor antagonist activity was assessed by studying the effects of increasing concentrations of the antagonists on cumulative clonidine dose-response curves on the stimulated vas deferens."( Selectivity of blocking agents for pre-and postsynaptic alpha-adrenoceptors.
Doxey, JC; Smith, CF; Walker, JM, 1977
)
0.26
" Dose-response curves were established for the blockade of ICSS by the antipsychotic drugs chlorpromazine, thioridazine, clozapine, and pimozide and the alpha-antagonist phenoxybenzamine."( Blockade of intracranial self-stimulation by antipsychotic drugs: failure to correlate with central alpha-noradrenergic blockade.
Setler, P; Weidley, E; Zarevics, P, 1977
)
0.45
" Propranolol, a beta-adrenergic antagonist, when administered at a dosage of 20 mg/kg of body weight, enhanced both passive hemagglutinating and IgE (passive cutaneous anaphylaxis) antibody formation."( Enhancement of IgE antibody formation in the rabbit by adrenergic antagonists.
Cain, WA; Homer, JT, 1979
)
0.26
" Values of KA and A50 were calculated from dose-response curves obtained for three alpha-adrenergic agonists (phenylephrine, methoxamine and norepinephrine) in the presence and absence of partial irreversible blockade by phenoxybenzamine."( Determination of the stimulus-response relation for three alpha-adrenergic agonists on rabbit aorta.
Gero, A; Raffa, RB; Tallarida, RJ, 1979
)
0.44
" The increase was blocked by phenoxybenzamine at a dosage level of 20 mg/kg which did not, of itself, reduce flexor reflex amplitude."( A system for measuring the noradrenaline receptor contribution to the flexor reflex.
Austin, JH; Fuxe, K; Nygren, LG, 1976
)
0.55
"In rabbits the topical administration of sodium azide (NaNs) or sodium nitroprusside (SNP) increased intraocular pressure in a dose-response manner."( Increased intraocular pressure following topical azide or nitroprusside.
Becker, B; Fritz, C; Holmberg, N; Krupin, T; Weiss, A, 1977
)
0.26
" We have compared the effects of an angiotensin antagonist (saralasin) and an alpha-adrenergic blocking agent (phenoxybenzamine) in supramaximal dosage on cardiac output, total peripheral resistance, and venous tone in rabbits rendered hypovolemic by restriction of sodium intake, supplemented by a furosemide-induced diuresis 48 h prior to study."( Cardiovascular responses to blockade of angiotensin and alpha-adrenergic receptors.
Borucki, LJ; Hollenberg, NK; Levenson, D, 1978
)
0.47
"In human adipose tissue in vitro, dose-response curves of lipolytic agents in releasing free fatty acids and glycerol into an albumine-containing medium were followed."( Adrenergic lipolysis in human adipose tissue in vitro.
Kuhn, E; Wenke, M; Wenkeová, J, 1975
)
0.25
" Log dose-response curves to isoprenaline from spontaneously contracting muscle strips from rabbit uterus have been obtained."( Action of beta-adrenoceptor antagonists on the response to isoprenaline in the oestrogen dominated rabbit uterus.
Nesheim, BI, 1975
)
0.25
"From a study on the interrelationship between electroshock-induced convulsions, autonomic function, catecholamines, and cardiovascular homeostasis in dogs, the authors found that: (1) the asystole of electroshock (ES) was significnatly prolonged by high spinal anesthesia but not by relative alpha- or beta-adrenergic blockade; (2) increased levels of circulating catecholamines were solely responsible for the marked hypertensive response to ES, since the pressor effect could be blocked by preventing the release of catecholamines with high spinal anesthesia or by inhibiting alpha-adrenergic receptors with phenoxybenzamine; (3) the adrenal medulla appeared to be the source of most of the ES-induced increase in circulating catecholamines; (4) the asystole and arrhythmias of ES were a cholinergic effect, since they were blocked by atropine; (5) there was a dose-response relationship between the coulombs of electricity administered and the catecholamine and cardiovascular responses; and (6) that the adverse cardiovascular effects of ES therapy could be ameliorated pharmacologically."( Autonomic blockade and the cardiovascular and catecholamine response to electroshock.
Anton, AH; Redderson, CL; Uy, DS,
)
0.29
" The dose-response curves for PGE1, SH-869 and VK-774 were approximately parallel, whereas that for dipyridamole was considerably less steep."( The effect of intravenous adenosine diphosphate on the number of circulating platelets in experimental animals: inhibition by prostaglandin E1, dipyridamole, SH-869 and VK-774.
Freuler, F; Holmes, IB; Smith, GM, 1977
)
0.26
" The dose-response curves for isoprenaline were shifted to the right on treatment with practolol."( Distribution and characterization of the adrenoceptors in dog coronary arteries.
Morishita, H, 1979
)
0.26
" The order of potency for the agonists, together with blocking experiments (including a parallel shift in the log dose-response curve induced by bulbocapnine), indicated that the vasodilatation is mediated by specific dopamine receptors."( Effects of dopaminergic agonists and antagonists on isolated cerebral blood vessels.
Edvinsson, L; Hardebo, JE; McCulloch, J; Owman, C, 1978
)
0.26
", or the same dosage of phenoxybenzamine plus plasma infusion (16 ml."( Hemodynamic effects of phenoxybenzamine and volume replacement in segmental ischemia of the rat small intestine.
Norlén, K; Rentzhog, L; Wikström, S, 1978
)
0.88
" In the presence of PBZ or phentolamine blockade, the dose-response curves of oxytocin and VP were shifted to the left, resulting in an apparent doubling of the pressor potency of the neurohypophysial peptides."( The site and the mechanism of phenoxy-benzamine potentiation of the pressor response to oxytocin and vasopressin: in vivo and isolated aortic strips studies.
Chan, WY; Erker, EF, 1977
)
0.26
" By titrating the dosage of both drugs against pulse rate and blood pressure response, propranolol was given between 80 and 160 mg."( An approach to the treatment of essential hypertension.
Mendlowitz, M; Vlachakis, ND, 1976
)
0.26
" Intravenous use, however, was ineffective in the dosage with which total systemic alpha adrenergic blockade was obtained."( Effect of phenoxybenzamine on experimental cerebral arterial spasm in cats.
Handa, H; Handa, J; Koyama, T; Matsuda, M; Yoneda, S, 1975
)
0.66
"The intrarenal distribution of blood flow in the baboon was measured using the 133xenon clearance technique, and dose-response curves for the various components of renal blood flow were determined during intra-arterial infusions of noradrenaline; the alpha-adrenergic blocking agent, phenoxybenzamine; the beta-adrenergic blocking agent, propranolol; and tyramine which causes the release of endogenous NA."( The effect of noradrenaline, adrenergic blocking agents, and tyramine on the intrarenal distribution of blood flow in the baboon.
Bomzon, L; Farr, J; Rosendorff, C; Scriven, DR, 1975
)
0.43
" Dose-response curves of isoproterenol were shifted significantly to the left by 2 x 10(-5) M aminophylline."( Comparison of the relaxing effect of dopamine with that of adenosine, isoproterenol and acetylcholine in isolated canine coronary arteries.
Hojo, M; Sakae, K; Toda, N; Usui, H, 1975
)
0.25
" Phenoxybenzamine also blocked the response to NA but a dose-response relationship was not apparent."( Effect of intraventricular administration of noradrenaline on water diuresis in goats.
Peeters, G; Vandeputte-Van Messon, G, 1975
)
1.16
" A concentration of 1 X 10(-8) g/ml PBZ produced a parallel shift of the dose-response effects while higher concentrations reduced both the slope and maximal response."( 5-hydroxytryptamine receptors in uterine smooth muscle.
Ammar, EM; Osman, FH, 1975
)
0.25
" Intravenous administration of PBZ in the dosage with which the pressor response to phenylephrine was completely blocked, or three times that dosage, failed to show any preventive effect on the vasospasm."( [Effect of phenoxybenzamine on the experimental cerebral vasospasm in cats (author's transl)].
Handa, H; Handa, J; Koyama, T; Matsuda, M; Yoneda, S, 1975
)
0.64
" Intraventricular injection of phenylephrine produced a dose-dependent hypothermia, whereas no dose-response relationship was obtained by isoproterenol."( [Role of brain biogenic amines in the central thermoregulatory mechanism of the rat (author's transl)].
Fukushima, N, 1975
)
0.25
" The acute or chronic administration of phenoxybenzamine alone displaced the dose-response curve to cirazoline to the right in a dose-dependent manner, while reducing the slope function and maximum response to the agonist."( A comparison of the effects of acute versus chronic administration of phenoxybenzamine on pressor responses elicited by the selective alpha 1-adrenoceptor agonist cirazoline in the pithed rat preparation.
Tabrizchi, R; Triggle, CR, 1992
)
0.78
"Akin to receptor inactivation with phenoxybenzamine (PBZ) (1 microM, 1 hr), treatment of anterior pituitary cells with 17 beta-estradiol (10 nM, 3 days) right-shifted the dose-response curve for inhibition of prolactin (PRL) secretion by the full agonist R-(-)-N-n-propylnorapomorphine (NPA) and reduced the maximal effect [EC50 (pM) and percent maximal effect: control, 25."( Comparative effects of receptor inactivation, 17 beta-estradiol and pertussis toxin on dopaminergic inhibition of prolactin secretion in vitro.
Bohmaker, K; Diamond, J; Lieu, HD; Meller, E; Puza, T, 1992
)
0.56
" A dose-response relationship was examined between concentrations of phenoxybenzamine pretreatment and prolactin release using a monolayer cell culture system."( Phenoxybenzamine selectively and irreversibly inactivates dopaminergic D2 receptors on primary cultured rat lactotrophs.
Heisler, RL; McAssey, K; Shin, SH; Szabo, MS, 1992
)
1.96
"This prospective clinical study evaluates the possible beneficial effects of increased phenoxybenzamine dosage in the preoperative treatment of patients with pheochromocytoma."( [The importance of high-dose alpha-receptor blockade for blood volume and hemodynamics in pheochromocytoma].
Dralle, H; Grosse, H; Hausen, B; Schober, O; Schröder, D, 1990
)
0.5
" In experiment 2, a dose-response curve for pimozide (0."( A role for catecholaminergic neurons in the suppression of pulsatile luteinizing hormone secretion in the prepubertal ewe lamb.
Brango, CW; Goodman, RL; Whisnant, CS, 1990
)
0.28
" In separate groups of rats, the log dose-response curve for bolus intravenous injection of AII was shifted to the right by SQ-29,548 while that for PE was unaffected."( Thromboxane mediation of the pressor response to infused angiotensin II.
Welch, WJ; Wilcox, CS, 1990
)
0.28
" Chloroethylclonidine (1-5 X 10(-5) M) shifted noradrenaline dose-response curve to the right approximately 5000-fold without depressing the maximum."( Chloroethylclonidine unmasks a non-alpha-adrenoceptor noradrenaline binding site in the rat aorta.
Bevan, JA; Oriowo, MA, 1990
)
0.28
" However, the dose-response curves of salbutamol on the venous and arterial systems overlapped, indicating that the increase in venous return represents a combination of properties common to both beta 1 and beta 2 adrenoceptors."( Dopamine and norepinephrine increase venous return by stimulating alpha and beta adrenoceptors in the dog.
Banning, JW; Morgan, JP; Roebel, LE; Van Maanen, EF, 1988
)
0.27
" Yohimbine caused about a 30 fold shift to the right in the dose-response curve whereas idazoxan almost completely abolished the mydriatic response to (+)-Amp."( Mechanism of dexamphetamine-induced mydriasis in the anaesthetized rat.
Hey, JA; Ito, T; Koss, MC, 1989
)
0.28
"5 hr washout, shifted to the right in a dose-dependent manner the dose-response curves for phenylephrine and norepinephrine."( Interaction of a chemically reactive prazosin analog with alpha-1 adrenoceptors of rat tissues.
Kusiak, JW; Piascik, MT; Pitha, J, 1989
)
0.28
" IBI at 10(-6) M shifted the dose-response curve of phenylephrine to the right with reduction in maxima."( Paradoxical effects of isothiocyanate analog of tolazoline on rat aorta and human platelets.
Feller, DR; Hamada, A; Miller, DD; Patil, PN; Shams, G; Venkataraman, BV, 1989
)
0.28
" The inactivation of a small receptor fraction shifted the dose-response curves for isoprenaline and clonidine to the right but did not alter the maximum effect of the agonists (responsiveness)."( Adrenoceptor occupancy in isolated human fat cells and its relationship with lipolysis rate.
Arner, P; Engfeldt, P; Hellmér, J; Ostman, J; Wennlund, A, 1988
)
0.27
" The inhibition, which was dose and time dependent, was characterized by progressive shift to the right in the norepinephrine dose-response curve."( Alkylation of alpha-1 receptors with a chemically reactive analog of prazosin reveals low affinity sites for norepinephrine in rabbit aorta.
Babich, M; Butler, BT; Kusiak, JW; Le, HT; Piascik, MT; Pitha, J, 1988
)
0.27
"The dose-response curves of the central and peripheral airways to intravenously injected nicotine were studied in 55 anesthetized dogs."( Dose-response curves of central and peripheral airways to nicotine injections in dogs.
Haga, T; Miyano, M; Nakamura, M; Sasaki, H; Takishima, T, 1986
)
0.27
" The dose-response curve to intra-arterial noradrenaline (after beta-adrenoceptor blockade) was shifted rightwards about ten fold by benextramine (10 mg kg-1) and by phenoxybenzamine (5 mg kg-1)."( Lack of involvement of alpha-adrenoceptors in sympathetic neural vasoconstriction in the hindquarters of the rabbit.
Hirst, GD; Lew, MJ, 1987
)
0.47
" Reserpinization shifted the (-)-norephedrine dose-response curve slightly to the right, indicating that only a minor portion of its activity is due to the release of stored endogenous catecholamines."( Adrenergic receptor subtype activation by (+)-, (-)- and (+/-)-norephedrine in the pithed rat.
Maher, TJ; Moya-Huff, FA, 1987
)
0.27
" In isolated guinea pig ileum these irreversible antagonists produce a parallel shift in the dose-response curve to histamine with retention of the maximum response if they are used at concentrations less than about 10(-6)M."( The action of agonists and antagonists at the histamine H1 receptor and receptor protection studies in guinea pig ileum.
Cook, DA; Ramji, K; Vollrath, B; Yong, MS, 1988
)
0.27
"1 mg/kg) and of yohimbine (1 mg/kg) on the dose-response curves for cirazoline in the pithed rat, and for phenylephrine in the anaesthetized dog were compared, after various doses of phenoxybenzamine."( Loss of selectivity of so-called selective alpha 1-adrenoceptor agonists after phenoxybenzamine.
Gonçalves, J; Guimarães, S; Nunes, JP; Paiva, MQ, 1988
)
0.69
" Further studies demonstrated a rightward shift in the dose-response curves for the inhibition by norepinephrine of cyclic AMP accumulation following pretreatment with increasing phenoxybenzamine concentration."( Alpha 2-adrenergic receptor-mediated regulation of adenylate cyclase in the intact human platelet. Evidence for a receptor reserve.
Ehrlich, YH; Ellis, J; Lenox, RH; Van Riper, D, 1985
)
0.46
" Dose-response curves to NE were biphasic in the basilar artery."( Alpha adrenoceptor number limits response of some rabbit arteries to norepinephrine.
Bevan, JA; Laher, I, 1985
)
0.27
" 5-HT agonists stimulated [3H]inositol phosphate accumulation in a dose-related but biphasic manner and only the high-affinity component of the dose-response curve was sensitive to antagonists."( 5-Hydroxytryptamine-stimulated inositol phospholipid hydrolysis in rat cerebral cortex slices: pharmacological characterization and effects of antidepressants.
Kendall, DA; Nahorski, SR, 1985
)
0.27
"3 mg/kg) in presence of prazosin shifted the norepinephrine pressor dose-response curves to the right whereas it was ineffective in yohimbine-pretreated animals."( Calcium entry blockade by nitrendipine and alpha adrenergic responsiveness in vivo: comparison with noncalcium entry blocker vasodilators in absence and presence of phenoxybenzamine pretreatment.
Pedrinelli, R; Tarazi, RC, 1985
)
0.46
" 6-hydroxydopamine (2 X 250 micrograms) there was a small increase in alpha 1-adrenoceptor binding sites but a parallel shift to the left in the noradrenaline [3H]inositol phosphate accumulation dose-response curve."( Alpha 1-adrenoceptor-mediated inositol phospholipid hydrolysis in rat cerebral cortex: relationship between receptor occupancy and response and effects of denervation.
Brown, E; Kendall, DA; Nahorski, SR, 1985
)
0.27
" Prazosin caused a parallel shift to the right of the dose-response curve to phenylephrine."( Pre- and postjunctional alpha-adrenoceptors at sympathetic neuroeffector junction in bovine mesenteric lymphatics.
Azuma, T; Ohhashi, T, 1986
)
0.27
" Dose-response curves (DRCs) to NE were made in the absence and presence of PBZ pretreatment which minimized the contribution of alpha adrenoceptors."( Norepinephrine-sensitive, phenoxybenzamine-resistant receptor sites associated with contraction in rabbit arterial but not venous smooth muscle: possible role in adrenergic neurotransmission.
Bevan, JA; Khayal, MA; Laher, I, 1986
)
0.57
"2 (SD) days of preoperative phenoxybenzamine therapy in a dosage of 148 +/- 45."( QRS amplitudes, QTc intervals and ECG abnormalities in pheochromocytoma patients before, during and after treatment.
Stenström, G; Swedberg, K, 1988
)
0.57
"8 micrograms of dopamine during one minute, and 2) by dose-response curves."( Effects of dopamine on intestinal vessels in anesthetized dogs.
Charbon, GA; van Alphen, MM; van Kesteren, RG, 1988
)
0.27
" Treatment with PBZ resulted in biphasic dose-response curves to NE."( Prazosin selectively antagonizes norepinephrine contractions at low-affinity, non-alpha adrenoceptor sites (extraceptors) in arterial muscle.
Bevan, JA; Laher, I; Nishimura, S, 1986
)
0.27
" Propranolol also shifted the dose-response curves to the right, but was apparently more potent in preparations with basal tone than in tissues where high tone was induced by carbachol or K+."( Noradrenergic and non-noradrenergic relaxation at basal and high tone levels in the guinea-pig tracheal smooth muscle.
Abe, M; Furukawa, T, 1986
)
0.27
"3 Other comparable mast cell degranulating agents (48/80 and melittin) showed little evidence of anti-inflammatory activity when tested at comparable dosage on turpentine arthritis and carrageenin oedema."( Anti-inflammatory property of 401 (MCD-peptide), a peptide from the venom of the bee Apis mellifera (L.).
Hanson, JM; Morley, J; Soria-Herrera, C, 1974
)
0.25
" The dose-response relationship for hyperactivity in grouped mice following the injection of morphine sulphate has been established."( Monoamine mediation of the morphine-induced activation of mice.
Carroll, BJ; Sharp, PT, 1972
)
0.25
" Grading of dosage and the use of dibenzyline revealed that these species exhibit alpha and beta adrenergic vascular responses in a manner qualitatively similar but quantitatively dissimilar to that for mammals."( Adrenergic blood pressure responses in the shark.
Borzelleca, JF; Schwartz, SL, 1969
)
0.25
" Dose-response curves for the alpha1-adrenoceptor-mediated vasoconstrictor effects of cirazoline were shifted in a rightward direction with no depression of the maximum response by lower does of phenoxybenzamine (0."( Existence of spare alpha 1-adrenoreceptors, but not alpha 2-adrenoreceptors, for respective vasopressor effects of cirazoline and B-HT 933 in the pithed rat.
Ruffolo, RR; Yaden, EL,
)
0.32
" Propranolol, in a dosage insufficient to change MABP, decreased both CO and CBF."( Relationship of cerebral blood flow to cardiac output, mean arterial pressure, blood volume, and alpha and beta blockade in cats.
Davis, DH; Sundt, TM, 1980
)
0.26
" In the isolated rabbit aorta, E-643 blocked noradrenaline-induced contraction of the aorta with a parallel shift of the dose-response curve to the right."( alpha-Adrenoceptor blocking properties of a new antihypertensive agent, 2-[4-(n-butyryl)-homopiperazine-1-yl]-4-amino-6,7-dimethoxyquinazoline (E-643).
Daiku, Y; Igarashi, T; Shoji, T, 1980
)
0.26
" The reduction in alpha 1-adrenergic receptor density following phenoxybenzamine treatment was determined by Scatchard analysis of specific 125IBE binding sites and compared with the expected reduction (q values) calculated from the agonist dose-response curves before and after phenoxybenzamine treatment."( "Spare" alpha 1-adrenergic receptors and the potency of agonists in rat vas deferens.
Abel, PW; Minneman, KP, 1984
)
0.51
" Disopyramide at high concentrations potentiated the contractile response of mesenteric arteries to norepinephrine and tyramine, while, in contrast, procainamide and quinidine shifted the dose-response curve for norepinephrine to the right."( Influence of disopyramide, compared with procainamide and quinidine, on isolated dog arteries in response to transmural stimulation and norepinephrine.
Konishi, M; Miyazaki, M; Okunishi, H; Toda, N,
)
0.13
" Phenoxybenzamine did not affect the dose-response curves to SP, eledoisin-related peptide (ERP), kassinin, eledoisin or physalaemin, nor did it affect the responses to individual doses of DPDPDT or DT79."( A study of [D-Pro2, D-Phe7, D-Trp9]-substance P and [D-Trp7,9]-substance P as tachykinin partial agonists in the rat colon.
Bailey, SJ; Jordan, CC, 1984
)
1.18
" A dose-response relationship (5-100 mg/kg) for the hypothermic effect of delta 9-THC was seen."( The mechanism of action of delta 9-tetrahydrocannabinol on body temperature in mice.
Davies, JA; Graham, JD, 1980
)
0.26
" Cumulative dose-response curves with epinephrine and norepinephrine showed graded contraction."( Adrenergic receptors and sympathetic agents in isolated human pulmonary arteries.
Boe, J; Simonsson, BG, 1980
)
0.26
" As indicated by dose-response curves, receptor occupancy of each occurs to an almost equal extent at suboptimal epinephrine concentrations."( Cyclic AMP-dependent and cyclic AMP-independent antagonism of insulin activation of cardiac glycogen synthase.
Angelos, KL; Ramachandran, C; Walsh, DA, 1982
)
0.26
" A careful analysis of the dose-response curve showed, however, that the net effect recorded involved the sum of responses from at least two functional systems or receptor sites."( Separate noradrenergic receptors could mediate clonidine-induced antinociception.
Paalzow, GH; Paalzow, LK, 1982
)
0.26
" Norepinephrine ED50 values and dissociation constants (KA) were determined by analysis of dose-response data with and without partial inactivation of alpha receptors by phenoxybenzamine."( Qualitative and quantitative differences between the postsynaptic alpha adrenoceptors of rabbit ear artery and thoracic aorta.
Ashbrook, DW; Purdy, RE; Stupecky, GL; Watanabe, MY, 1983
)
0.46
" ED50 values and dissociation constants for norepinephrine (NE), epinephrine (EPI), isoproterenol (ISO), methoxamine (MET) and clonidine (CLO) were determined by analysis of dose-response data with and without partial inactivation of alpha receptors by phenoxybenzamine."( Characterization of the alpha adrenergic receptor properties of rabbit ear artery and thoracic aorta.
Purdy, RE; Stupecky, GL, 1984
)
0.45
"5 X 10(-6)M), added to the bath fluid 5 minutes before the administration of acetylcholine (10(-7) - 10(-6)M), caused an almost parallel shift (to the right) in the log dose-response curve of acetylcholine on isolated driven left atria of guinea-pigs."( Reversible antagonism between acetylcholine and phenoxybenzamine in isolated atria of guinea-pigs.
Ojewole, JA, 1984
)
0.52
" The conventional low dosage nitrite/thiosulfate (6."( Cyanide intoxication in sheep; therapeutics.
Burrows, GE, 1981
)
0.26
" Comparing dose-response relations, arteries from both groups were equally sensitive to NE and KCl."( Increased sensitivity to angiotensin in uterine arteries from pregnant rabbits.
Moisey, DM; Tulenko, T, 1983
)
0.27
" A higher (5 mg/kg) dosage of the drug proved to be detrimental."( Recovery of renal function after warm ischemia. I. The effect of chlorpromazine and phenoxybenzamine.
Birrell, C; Howden, B; Jablonski, P; Leslie, E; Marshall, VC; Rae, D; Tange, J, 1983
)
0.49
" Pretreatment of rats with 5 and 10 mg/kg of phenoxybenzamine or phentolamine displaced the dose-response curves for apomorphine-induced stereotypy to the left in a dose dependent manner."( Effects of alpha-adrenergic blocking agents on stereotyped behavior induced by apomorphine in rats.
De-Souza, H; Palermo-Neto, J, 1982
)
0.52
" When isolated longitudinal muscle strips from this preparation were tested with E-2-P before and after blockade with 2-haloalkylamines, it was found that these agents produced an irreversible shift to the right in the dose-response curve without significant depression of the maximum response even at very high antagonist concentrations."( Irreversible blockade of responses to a partial agonist acting at the histamine H1-receptor.
Cook, D; Iwanow, D; Kenakin, T; Krueger, C, 1982
)
0.26
" The dose-response relationship for norepinephrine-induced [Ca2+]i response showed an increase in maximum effect with no change in agonist potency, and the increase in maximum effect was disproportionate to the difference in receptor density."( Effect of receptor density on the receptor-effector coupling: use of cloned and stably expressed alpha 1B-adrenoceptors in CHO cells.
Horie, K; Tsujimoto, G, 1995
)
0.29
" Pretreatment with captopril reduced the pressor responses to cirazoline and displaced the dose-response curve for this agonist to the right, significantly increasing the ED50 without altering the maximum response."( Pressor responses to the alpha 1-adrenoceptor agonist cirazoline: effects of captopril, phenoxybenzamine and nifedipine.
Tabrizchi, R; Triggle, CR, 1994
)
0.51
"055 nmol from the dose-response curve."( Central regulation of urine production by a selective mu-opioid agonist, [D-Ala2, N-Me-Phe4, Gly5-ol]-enkephalin, in rats.
Matsuda, T; Mori, M; Tsushima, H, 1997
)
0.3
" Whereas at low dosage (/=50 microgram/kg)."( Mechanisms of ventilatory inhibition by exogenous dopamine in cats.
Haouzi, P; Loos, N; Marchal, F, 1998
)
0.3
" Apparent rate constants for methoxamine binding and unbinding gave Kd values in agreement with EC50 values measured from dose-response relations."( Non-specific action of methoxamine on Ito, and the cloned channels hKv 1.5 and Kv 4.2.
Fedida, D; Li, Q; Parker, C, 1999
)
0.3
"The establishment of a dose-response relationship and its quantification is the usual procedure for analysing drug action on an isolated organ."( Time course of isolated rat fundus response to muscarinic agonists: a measure of intrinsic efficacy.
Jankovic, SM; Kouvelas, D; Mirtsou-Fidani, V, 1998
)
0.3
" Cocaine shifted the dose-response curve of noradrenaline to the left and enhanced its maximal effects."( Post-junctional mechanisms involved in the potentiation of cardiac adrenergic responses by cocaine.
Bechara, G; El-Bizri, NM; Khoury, HA; Sabra, R; Sharaf, LH, 2000
)
0.31
" Further study of selective alpha-1 antagonists in dogs is needed to determine appropriate oral dosing protocols that will produce maximal urethral effects with minimal hemodynamic effects, and to demonstrate clinical efficacy in dogs with functional urethral obstruction."( Urethral pressure profile and hemodynamic effects of phenoxybenzamine and prazosin in non-sedated male beagle dogs.
Cribb, AE; Fischer, JR; Lane, IF, 2003
)
0.57
" Sigmoid dose-response curves for pupillary dilation were produced in pentobarbital anesthetized rats by intravenous administration of increasing doses of agonists (guanabenz for alpha(2)-adrenoceptors, clonidine for both alpha(2)-adrenoceptors and imidazoline I(1) receptors, and rilmenidine for imidazoline I(1) receptors)."( Rat clonidine mydriasis model: imidazoline receptors are not involved.
Koss, MC; Yu, Y, 2005
)
0.33
" We show that the parameters of the widely used operational model of pharmacological agonism are difficult to estimate from single dose-response curves."( Estimating the parameters of the operational model of pharmacological agonism.
Frigyesi, A; Hössjer, O, 2006
)
0.33
" Vascular reactivity was measured by comparing 5HT dose-response characteristics in untreated near-term lamb common carotid arteries and arteries treated with 15 microg/kg/min of dopamine."( Effect of dopamine on vascular reactivity in near-term lamb carotids: role of the endothelium.
Angeles, DM; Pearce, WJ, 2006
)
0.33
" We proposed a systematic classification scheme using FDA-approved drug labeling to assess the DILI potential of drugs, which yielded a benchmark dataset with 287 drugs representing a wide range of therapeutic categories and daily dosage amounts."( FDA-approved drug labeling for the study of drug-induced liver injury.
Chen, M; Fang, H; Liu, Z; Shi, Q; Tong, W; Vijay, V, 2011
)
0.37
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
aromatic amineAn amino compound in which the amino group is linked directly to an aromatic system.
[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 (43)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
RAR-related orphan receptor gammaMus musculus (house mouse)Potency29.84930.006038.004119,952.5996AID1159523
USP1 protein, partialHomo sapiens (human)Potency50.11870.031637.5844354.8130AID504865
TDP1 proteinHomo sapiens (human)Potency30.70890.000811.382244.6684AID686978; AID686979
AR proteinHomo sapiens (human)Potency25.62050.000221.22318,912.5098AID1259243; AID1259247
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency28.18380.011212.4002100.0000AID1030
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency8.01480.001022.650876.6163AID1224838; AID1224839; AID1224893
progesterone receptorHomo sapiens (human)Potency26.60320.000417.946075.1148AID1346795
EWS/FLI fusion proteinHomo sapiens (human)Potency0.03320.001310.157742.8575AID1259253
GVesicular stomatitis virusPotency11.98770.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency0.33790.00108.379861.1304AID1645840
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency0.00750.001024.504861.6448AID743215
arylsulfatase AHomo sapiens (human)Potency0.60121.069113.955137.9330AID720538
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency26.67950.035520.977089.1251AID504332
heat shock 70kDa protein 5 (glucose-regulated protein, 78kDa)Homo sapiens (human)Potency41.39990.016525.307841.3999AID602332
aryl hydrocarbon receptorHomo sapiens (human)Potency29.84930.000723.06741,258.9301AID743085
thyroid stimulating hormone receptorHomo sapiens (human)Potency28.74660.001628.015177.1139AID1224843; AID1224895
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency26.83250.057821.109761.2679AID1159528
Histone H2A.xCricetulus griseus (Chinese hamster)Potency55.19650.039147.5451146.8240AID1224845
chromobox protein homolog 1Homo sapiens (human)Potency0.00950.006026.168889.1251AID488953
heat shock protein beta-1Homo sapiens (human)Potency16.78420.042027.378961.6448AID743210
flap endonuclease 1Homo sapiens (human)Potency0.26680.133725.412989.1251AID588795
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency30.22000.000627.21521,122.0200AID651741; AID743219
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency0.11420.005612.367736.1254AID624032
survival motor neuron protein isoform dHomo sapiens (human)Potency11.90470.125912.234435.4813AID1458
Interferon betaHomo sapiens (human)Potency11.98770.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency11.98770.01238.964839.8107AID1645842
Cellular tumor antigen p53Homo sapiens (human)Potency14.96010.002319.595674.0614AID651631
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency11.98770.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency11.98770.01238.964839.8107AID1645842
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency30.13130.060110.745337.9330AID485368
[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)
Solute carrier family 22 member 2Homo sapiens (human)IC50 (µMol)4.90000.40003.10009.7000AID681561
Solute carrier family 22 member 1 Homo sapiens (human)IC50 (µMol)8.91000.21005.553710.0000AID386625; AID681560
Solute carrier family 22 member 3Homo sapiens (human)IC50 (µMol)6.13000.09003.72779.5000AID682144
Bile salt export pumpHomo sapiens (human)IC50 (µMol)100.00000.11007.190310.0000AID1443986
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)Ki0.00180.00010.949010.0000AID35412
DRattus norvegicus (Norway rat)Ki0.12000.00010.610010.0000AID63016
D(3) dopamine receptorRattus norvegicus (Norway rat)Ki0.12000.00010.25675.8000AID63016
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)Ki0.00180.00000.575110.0000AID35412
D(1B) dopamine receptorRattus norvegicus (Norway rat)Ki0.12000.00020.24622.0000AID63016
D(4) dopamine receptorRattus norvegicus (Norway rat)Ki0.12000.00020.18872.0000AID63016
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Ki0.00180.00000.965010.0000AID35412
5-hydroxytryptamine receptor 7Cavia porcellus (domestic guinea pig)IC50 (µMol)15.10002.03005.53139.9000AID386625
D(2) dopamine receptorRattus norvegicus (Norway rat)Ki0.12000.00000.437510.0000AID63016
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (236)

Processvia Protein(s)Taxonomy
activation of cysteine-type endopeptidase activity involved in apoptotic processSolute carrier family 22 member 2Homo sapiens (human)
positive regulation of gene expressionSolute carrier family 22 member 2Homo sapiens (human)
organic cation transportSolute carrier family 22 member 2Homo sapiens (human)
monoatomic cation transportSolute carrier family 22 member 2Homo sapiens (human)
neurotransmitter transportSolute carrier family 22 member 2Homo sapiens (human)
serotonin transportSolute carrier family 22 member 2Homo sapiens (human)
body fluid secretionSolute carrier family 22 member 2Homo sapiens (human)
organic cation transportSolute carrier family 22 member 2Homo sapiens (human)
quaternary ammonium group transportSolute carrier family 22 member 2Homo sapiens (human)
prostaglandin transportSolute carrier family 22 member 2Homo sapiens (human)
amine transportSolute carrier family 22 member 2Homo sapiens (human)
putrescine transportSolute carrier family 22 member 2Homo sapiens (human)
spermidine transportSolute carrier family 22 member 2Homo sapiens (human)
acetylcholine transportSolute carrier family 22 member 2Homo sapiens (human)
choline transportSolute carrier family 22 member 2Homo sapiens (human)
dopamine transportSolute carrier family 22 member 2Homo sapiens (human)
norepinephrine transportSolute carrier family 22 member 2Homo sapiens (human)
xenobiotic transportSolute carrier family 22 member 2Homo sapiens (human)
epinephrine transportSolute carrier family 22 member 2Homo sapiens (human)
histamine transportSolute carrier family 22 member 2Homo sapiens (human)
serotonin uptakeSolute carrier family 22 member 2Homo sapiens (human)
histamine uptakeSolute carrier family 22 member 2Homo sapiens (human)
norepinephrine uptakeSolute carrier family 22 member 2Homo sapiens (human)
thiamine transmembrane transportSolute carrier family 22 member 2Homo sapiens (human)
purine-containing compound transmembrane transportSolute carrier family 22 member 2Homo sapiens (human)
amino acid import across plasma membraneSolute carrier family 22 member 2Homo sapiens (human)
dopamine uptakeSolute carrier family 22 member 2Homo sapiens (human)
L-arginine import across plasma membraneSolute carrier family 22 member 2Homo sapiens (human)
export across plasma membraneSolute carrier family 22 member 2Homo sapiens (human)
transport across blood-brain barrierSolute carrier family 22 member 2Homo sapiens (human)
L-alpha-amino acid transmembrane transportSolute carrier family 22 member 2Homo sapiens (human)
spermidine transmembrane transportSolute carrier family 22 member 2Homo sapiens (human)
L-arginine transmembrane transportSolute carrier family 22 member 2Homo sapiens (human)
cellular detoxificationSolute carrier family 22 member 2Homo sapiens (human)
xenobiotic transport across blood-brain barrierSolute carrier family 22 member 2Homo sapiens (human)
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)
histamine metabolic processSolute carrier family 22 member 3Homo sapiens (human)
organic cation transportSolute carrier family 22 member 3Homo sapiens (human)
quaternary ammonium group transportSolute carrier family 22 member 3Homo sapiens (human)
monoatomic ion transportSolute carrier family 22 member 3Homo sapiens (human)
neurotransmitter transportSolute carrier family 22 member 3Homo sapiens (human)
serotonin transportSolute carrier family 22 member 3Homo sapiens (human)
organic cation transportSolute carrier family 22 member 3Homo sapiens (human)
quaternary ammonium group transportSolute carrier family 22 member 3Homo sapiens (human)
organic anion transportSolute carrier family 22 member 3Homo sapiens (human)
monocarboxylic acid transportSolute carrier family 22 member 3Homo sapiens (human)
monoamine transportSolute carrier family 22 member 3Homo sapiens (human)
spermidine transportSolute carrier family 22 member 3Homo sapiens (human)
dopamine transportSolute carrier family 22 member 3Homo sapiens (human)
norepinephrine transportSolute carrier family 22 member 3Homo sapiens (human)
regulation of appetiteSolute carrier family 22 member 3Homo sapiens (human)
xenobiotic transportSolute carrier family 22 member 3Homo sapiens (human)
epinephrine transportSolute carrier family 22 member 3Homo sapiens (human)
histamine transportSolute carrier family 22 member 3Homo sapiens (human)
serotonin uptakeSolute carrier family 22 member 3Homo sapiens (human)
histamine uptakeSolute carrier family 22 member 3Homo sapiens (human)
norepinephrine uptakeSolute carrier family 22 member 3Homo sapiens (human)
epinephrine uptakeSolute carrier family 22 member 3Homo sapiens (human)
purine-containing compound transmembrane transportSolute carrier family 22 member 3Homo sapiens (human)
dopamine uptakeSolute carrier family 22 member 3Homo sapiens (human)
transport across blood-brain barrierSolute carrier family 22 member 3Homo sapiens (human)
spermidine transmembrane transportSolute carrier family 22 member 3Homo sapiens (human)
cellular detoxificationSolute carrier family 22 member 3Homo 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)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycle G2/M phase transitionCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
ER overload responseCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
mitophagyCellular tumor antigen p53Homo sapiens (human)
in utero embryonic developmentCellular tumor antigen p53Homo sapiens (human)
somitogenesisCellular tumor antigen p53Homo sapiens (human)
release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
hematopoietic progenitor cell differentiationCellular tumor antigen p53Homo sapiens (human)
T cell proliferation involved in immune responseCellular tumor antigen p53Homo sapiens (human)
B cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
T cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
response to ischemiaCellular tumor antigen p53Homo sapiens (human)
nucleotide-excision repairCellular tumor antigen p53Homo sapiens (human)
double-strand break repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
protein import into nucleusCellular tumor antigen p53Homo sapiens (human)
autophagyCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in cell cycle arrestCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in transcription of p21 class mediatorCellular tumor antigen p53Homo sapiens (human)
transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
Ras protein signal transductionCellular tumor antigen p53Homo sapiens (human)
gastrulationCellular tumor antigen p53Homo sapiens (human)
neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
protein localizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA replicationCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
determination of adult lifespanCellular tumor antigen p53Homo sapiens (human)
mRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
rRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
response to salt stressCellular tumor antigen p53Homo sapiens (human)
response to inorganic substanceCellular tumor antigen p53Homo sapiens (human)
response to X-rayCellular tumor antigen p53Homo sapiens (human)
response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
positive regulation of gene expressionCellular tumor antigen p53Homo sapiens (human)
cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
viral processCellular tumor antigen p53Homo sapiens (human)
glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
cerebellum developmentCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell growthCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
mitotic G1 DNA damage checkpoint signalingCellular tumor antigen p53Homo sapiens (human)
negative regulation of telomere maintenance via telomeraseCellular tumor antigen p53Homo sapiens (human)
T cell differentiation in thymusCellular tumor antigen p53Homo sapiens (human)
tumor necrosis factor-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
regulation of tissue remodelingCellular tumor antigen p53Homo sapiens (human)
cellular response to UVCellular tumor antigen p53Homo sapiens (human)
multicellular organism growthCellular tumor antigen p53Homo sapiens (human)
positive regulation of mitochondrial membrane permeabilityCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
entrainment of circadian clock by photoperiodCellular tumor antigen p53Homo sapiens (human)
mitochondrial DNA repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
transcription initiation-coupled chromatin remodelingCellular tumor antigen p53Homo sapiens (human)
negative regulation of proteolysisCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of RNA polymerase II transcription preinitiation complex assemblyCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
response to antibioticCellular tumor antigen p53Homo sapiens (human)
fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
circadian behaviorCellular tumor antigen p53Homo sapiens (human)
bone marrow developmentCellular tumor antigen p53Homo sapiens (human)
embryonic organ developmentCellular tumor antigen p53Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationCellular tumor antigen p53Homo sapiens (human)
protein stabilizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of helicase activityCellular tumor antigen p53Homo sapiens (human)
protein tetramerizationCellular tumor antigen p53Homo sapiens (human)
chromosome organizationCellular tumor antigen p53Homo sapiens (human)
neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
hematopoietic stem cell differentiationCellular tumor antigen p53Homo sapiens (human)
negative regulation of glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
type II interferon-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
cardiac septum morphogenesisCellular tumor antigen p53Homo sapiens (human)
positive regulation of programmed necrotic cell deathCellular tumor antigen p53Homo sapiens (human)
protein-containing complex assemblyCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to endoplasmic reticulum stressCellular tumor antigen p53Homo sapiens (human)
thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
necroptotic processCellular tumor antigen p53Homo sapiens (human)
cellular response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
cellular response to xenobiotic stimulusCellular tumor antigen p53Homo sapiens (human)
cellular response to ionizing radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to UV-CCellular tumor antigen p53Homo sapiens (human)
stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
cellular response to actinomycin DCellular tumor antigen p53Homo sapiens (human)
positive regulation of release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
cellular senescenceCellular tumor antigen p53Homo sapiens (human)
replicative senescenceCellular tumor antigen p53Homo sapiens (human)
oxidative stress-induced premature senescenceCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
oligodendrocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of execution phase of apoptosisCellular tumor antigen p53Homo sapiens (human)
negative regulation of mitophagyCellular tumor antigen p53Homo sapiens (human)
regulation of mitochondrial membrane permeability involved in apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of G1 to G0 transitionCellular tumor antigen p53Homo sapiens (human)
negative regulation of miRNA processingCellular tumor antigen p53Homo sapiens (human)
negative regulation of glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
negative regulation of pentose-phosphate shuntCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
regulation of fibroblast apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
positive regulation of cellular senescenceCellular tumor antigen p53Homo sapiens (human)
positive regulation of intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (78)

Processvia Protein(s)Taxonomy
amine transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
acetylcholine transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
neurotransmitter transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
monoamine transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
organic anion transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
organic cation transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
prostaglandin transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
L-amino acid transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
pyrimidine nucleoside transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
choline transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
thiamine transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
putrescine transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
efflux transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
spermidine transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
quaternary ammonium group transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
toxin transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
xenobiotic transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
L-arginine transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
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)
neurotransmitter transmembrane transporter activitySolute carrier family 22 member 3Homo sapiens (human)
protein bindingSolute carrier family 22 member 3Homo sapiens (human)
monoamine transmembrane transporter activitySolute carrier family 22 member 3Homo sapiens (human)
organic anion transmembrane transporter activitySolute carrier family 22 member 3Homo sapiens (human)
organic cation transmembrane transporter activitySolute carrier family 22 member 3Homo sapiens (human)
spermidine transmembrane transporter activitySolute carrier family 22 member 3Homo sapiens (human)
quaternary ammonium group transmembrane transporter activitySolute carrier family 22 member 3Homo sapiens (human)
toxin transmembrane transporter activitySolute carrier family 22 member 3Homo 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)
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
transcription cis-regulatory region bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
core promoter sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
TFIID-class transcription factor complex bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
protease bindingCellular tumor antigen p53Homo sapiens (human)
p53 bindingCellular tumor antigen p53Homo sapiens (human)
DNA bindingCellular tumor antigen p53Homo sapiens (human)
chromatin bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activityCellular tumor antigen p53Homo sapiens (human)
mRNA 3'-UTR bindingCellular tumor antigen p53Homo sapiens (human)
copper ion bindingCellular tumor antigen p53Homo sapiens (human)
protein bindingCellular tumor antigen p53Homo sapiens (human)
zinc ion bindingCellular tumor antigen p53Homo sapiens (human)
enzyme bindingCellular tumor antigen p53Homo sapiens (human)
receptor tyrosine kinase bindingCellular tumor antigen p53Homo sapiens (human)
ubiquitin protein ligase bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase regulator activityCellular tumor antigen p53Homo sapiens (human)
ATP-dependent DNA/DNA annealing activityCellular tumor antigen p53Homo sapiens (human)
identical protein bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase bindingCellular tumor antigen p53Homo sapiens (human)
protein heterodimerization activityCellular tumor antigen p53Homo sapiens (human)
protein-folding chaperone bindingCellular tumor antigen p53Homo sapiens (human)
protein phosphatase 2A bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingCellular tumor antigen p53Homo sapiens (human)
14-3-3 protein bindingCellular tumor antigen p53Homo sapiens (human)
MDM2/MDM4 family protein bindingCellular tumor antigen p53Homo sapiens (human)
disordered domain specific bindingCellular tumor antigen p53Homo sapiens (human)
general transcription initiation factor bindingCellular tumor antigen p53Homo sapiens (human)
molecular function activator activityCellular tumor antigen p53Homo sapiens (human)
promoter-specific chromatin bindingCellular tumor antigen p53Homo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (49)

Processvia Protein(s)Taxonomy
plasma membraneSolute carrier family 22 member 2Homo sapiens (human)
basal plasma membraneSolute carrier family 22 member 2Homo sapiens (human)
membraneSolute carrier family 22 member 2Homo sapiens (human)
basolateral plasma membraneSolute carrier family 22 member 2Homo sapiens (human)
apical plasma membraneSolute carrier family 22 member 2Homo sapiens (human)
extracellular exosomeSolute carrier family 22 member 2Homo sapiens (human)
presynapseSolute carrier family 22 member 2Homo sapiens (human)
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)
nuclear outer membraneSolute carrier family 22 member 3Homo sapiens (human)
plasma membraneSolute carrier family 22 member 3Homo sapiens (human)
endomembrane systemSolute carrier family 22 member 3Homo sapiens (human)
membraneSolute carrier family 22 member 3Homo sapiens (human)
basolateral plasma membraneSolute carrier family 22 member 3Homo sapiens (human)
apical plasma membraneSolute carrier family 22 member 3Homo sapiens (human)
mitochondrial membraneSolute carrier family 22 member 3Homo sapiens (human)
neuronal cell bodySolute carrier family 22 member 3Homo sapiens (human)
presynapseSolute carrier family 22 member 3Homo 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)
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
nuclear bodyCellular tumor antigen p53Homo sapiens (human)
nucleusCellular tumor antigen p53Homo sapiens (human)
nucleoplasmCellular tumor antigen p53Homo sapiens (human)
replication forkCellular tumor antigen p53Homo sapiens (human)
nucleolusCellular tumor antigen p53Homo sapiens (human)
cytoplasmCellular tumor antigen p53Homo sapiens (human)
mitochondrionCellular tumor antigen p53Homo sapiens (human)
mitochondrial matrixCellular tumor antigen p53Homo sapiens (human)
endoplasmic reticulumCellular tumor antigen p53Homo sapiens (human)
centrosomeCellular tumor antigen p53Homo sapiens (human)
cytosolCellular tumor antigen p53Homo sapiens (human)
nuclear matrixCellular tumor antigen p53Homo sapiens (human)
PML bodyCellular tumor antigen p53Homo sapiens (human)
transcription repressor complexCellular tumor antigen p53Homo sapiens (human)
site of double-strand breakCellular tumor antigen p53Homo sapiens (human)
germ cell nucleusCellular tumor antigen p53Homo sapiens (human)
chromatinCellular tumor antigen p53Homo sapiens (human)
transcription regulator complexCellular tumor antigen p53Homo sapiens (human)
protein-containing complexCellular tumor antigen p53Homo sapiens (human)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (118)

Assay IDTitleYearJournalArticle
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).
AID1146561Antagonist activity at alpha adrenergic receptor in guinea pig atrium assessed as reduction in tyramine-mediated ionotropic/chronotropic potency1978Journal of medicinal chemistry, Nov, Volume: 21, Issue:11
Molecular properties of the adrenergic alpha receptor. 2. Optimum covalent inhibition by two different prototypes of polyamine disulfides.
AID205267Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex1985Journal of medicinal chemistry, Mar, Volume: 28, Issue:3
[3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs.
AID1636465Drug activation in human Hep3B cells assessed as human CYP2D6-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 8.6 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of NA2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
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.
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).
AID1443995Hepatotoxicity in human assessed as drug-induced liver injury2014Hepatology (Baltimore, Md.), Sep, Volume: 60, Issue:3
Human drug-induced liver injury severity is highly associated with dual inhibition of liver mitochondrial function and bile salt export pump.
AID1146566Antagonist activity at alpha adrenergic receptor in guinea pig atrium assessed as inhibition of 30 uM NE-induced contractions treated at 0.147 uM1978Journal of medicinal chemistry, Nov, Volume: 21, Issue:11
Molecular properties of the adrenergic alpha receptor. 2. Optimum covalent inhibition by two different prototypes of polyamine disulfides.
AID682144TP_TRANSPORTER: inhibition of MPP+ uptake (MPP+: 0.25 uM) in OCT3-expressing HEK293 cells2002British journal of pharmacology, Jul, Volume: 136, Issue:6
Expression and pharmacological profile of the human organic cation transporters hOCT1, hOCT2 and hOCT3.
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.
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.
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1636397Drug activation in human Hep3B cells assessed as human CYP3A4-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 9.6 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of NA2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
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).
AID678718Metabolic stability in human liver microsomes assessed as high signal/noise ratio (S/N of >100) by measuring 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.
AID1146568Antagonist activity at muscarinic receptor in guinea pig atrium assessed as reduction in butyrylcholine-induced response1978Journal of medicinal chemistry, Nov, Volume: 21, Issue:11
Molecular properties of the adrenergic alpha receptor. 2. Optimum covalent inhibition by two different prototypes of polyamine disulfides.
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).
AID35412In vitro binding affinity was measured as the inhibition of [3H]WB-4101 binding to alpha-1 adrenergic receptor of rat cortical membranes1986Journal of medicinal chemistry, Aug, Volume: 29, Issue:8
4-Amino-6-chloro-2-piperazinopyrimidines with selective affinity for alpha 2-adrenoceptors.
AID1146567Antagonist activity at alpha adrenergic receptor in guinea pig atrium assessed as inhibition of 300 uM NE-induced contractions treated at 0.147 uM1978Journal of medicinal chemistry, Nov, Volume: 21, Issue:11
Molecular properties of the adrenergic alpha receptor. 2. Optimum covalent inhibition by two different prototypes of polyamine disulfides.
AID625278FDA Liver Toxicity Knowledge Base Benchmark Dataset (LTKB-BD) drugs of no concern for DILI2011Drug discovery today, Aug, Volume: 16, Issue:15-16
FDA-approved drug labeling for the study of drug-induced liver injury.
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).
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.
AID681560TP_TRANSPORTER: inhibition of MPP+ uptake (MPP+: 0.25 uM) in OCT1-expressing HEK293 cells2002British journal of pharmacology, Jul, Volume: 136, Issue:6
Expression and pharmacological profile of the human organic cation transporters hOCT1, hOCT2 and hOCT3.
AID1443986Inhibition of recombinant human BSEP expressed in baculovirus infected sf9 cell membrane vesicles assessed as reduction in ATP or AMP-dependent [3H]-taurocholic acid uptake in to vesicles preincubated for 5 mins followed by ATP/AMP addition measured after2014Hepatology (Baltimore, Md.), Sep, Volume: 60, Issue:3
Human drug-induced liver injury severity is highly associated with dual inhibition of liver mitochondrial function and bile salt export pump.
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).
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.
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.
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).
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).
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.
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).
AID681561TP_TRANSPORTER: inhibition of MPP+ uptake (MPP+: 0.25 uM) in OCT2-expressing HEK293 cells2002British journal of pharmacology, Jul, Volume: 136, Issue:6
Expression and pharmacological profile of the human organic cation transporters hOCT1, hOCT2 and hOCT3.
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).
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1061889Displacement of [3H]BTX-B from neuronal voltage-gated sodium channel in rat cerebral cortex synaptoneurosomes after 60 mins by scintillation counting2014Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
A highly predictive 3D-QSAR model for binding to the voltage-gated sodium channel: design of potent new ligands.
AID63016In vitro binding affinity to Dopamine receptors of rat striatal membranes by [3H]spiroperidol displacement.1986Journal of medicinal chemistry, Aug, Volume: 29, Issue:8
4-Amino-6-chloro-2-piperazinopyrimidines with selective affinity for alpha 2-adrenoceptors.
AID337596Inhibition of acetylcholine-induced contraction in guinea pig ileum at 0.5 ug/ml1994Journal of natural products, Sep, Volume: 57, Issue:9
(+/-)-Gelliusines A and B, two diastereomeric brominated tris-indole alkaloids from a deep water new caledonian marine sponge (Gellius or Orina sp.).
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).
AID1443992Total Cmax in human administered as single dose2014Hepatology (Baltimore, Md.), Sep, Volume: 60, Issue:3
Human drug-induced liver injury severity is highly associated with dual inhibition of liver mitochondrial function and bile salt export pump.
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).
AID205268Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex at 10 uM1985Journal of medicinal chemistry, Mar, Volume: 28, Issue:3
[3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs.
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.
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.
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.
AID1443991Induction of mitochondrial dysfunction in Sprague-Dawley rat liver mitochondria assessed as inhibition of mitochondrial respiration per mg mitochondrial protein measured for 20 mins by A65N-1 oxygen probe based fluorescence assay2014Hepatology (Baltimore, Md.), Sep, Volume: 60, Issue:3
Human drug-induced liver injury severity is highly associated with dual inhibition of liver mitochondrial function and bile salt export pump.
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).
AID1636516Drug activation in human Hep3B cells assessed as human CYP2C9-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 14 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of NAD2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
AID1146563Potentiation of NE-mediated alpha adrenergic receptor activity in guinea pig atrium1978Journal of medicinal chemistry, Nov, Volume: 21, Issue:11
Molecular properties of the adrenergic alpha receptor. 2. Optimum covalent inhibition by two different prototypes of polyamine disulfides.
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).
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
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.
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.
AID1347109qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
AID1347121qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
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.
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.
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.
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.
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.
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.
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.
AID1347115qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
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.
AID1347128qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
AID1347126qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
AID1347119qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
AID1347123qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347117qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
AID1347110qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347113qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
AID1347116qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
AID1347129qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
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.
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.
AID1347124qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
AID1347125qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
AID1347114qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
AID1347127qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
AID1347111qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
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.
AID1347122qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
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.
AID1347112qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
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.
AID1347118qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
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.
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.
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.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
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.
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.
AID588378qHTS for Inhibitors of ATXN expression: Validation
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.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID1346058Human alpha2B-adrenoceptor (Adrenoceptors)1991The Journal of biological chemistry, Nov-25, Volume: 266, Issue:33
Molecular cloning and characterization of a high affinity dopamine receptor (D1 beta) and its pseudogene.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (4,781)

TimeframeStudies, This Drug (%)All Drugs %
pre-19904193 (87.70)18.7374
1990's336 (7.03)18.2507
2000's143 (2.99)29.6817
2010's83 (1.74)24.3611
2020's26 (0.54)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 62.60

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 Index62.60 (24.57)
Research Supply Index8.53 (2.92)
Research Growth Index4.15 (4.65)
Search Engine Demand Index112.56 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (62.60)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials70 (1.40%)5.53%
Reviews134 (2.68%)6.00%
Case Studies164 (3.28%)4.05%
Observational0 (0.00%)0.25%
Other4,638 (92.65%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (6)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Pheochromocytoma Randomised Study Comparing Adrenoreceptor Inhibiting Agents for Preoperative Treatment [NCT01379898]Phase 4134 participants (Actual)Interventional2011-12-31Completed
Randomized Controlled Trial of Preoperative Alpha Blockade for Pheochromocytoma [NCT03176693]Phase 339 participants (Actual)Interventional2017-05-05Completed
Parenteral Phenoxybenzamine During Congenital Heart Disease Surgery [NCT00770705]Phase 20 participants (Actual)Interventional2008-10-31Withdrawn(stopped due to poor enrollment)
Intravenous Phenoxybenzamine Use in Pediatric Patients Undergoing Open-Heart Surgery [NCT00569855]Phase 2785 participants (Actual)Interventional2001-02-28Completed
Use of Phenoxybenzamine [PBZ] IV to Assist High Flow Low Pressure Perfusion [HFLPP] on Cardio-pulmonary Bypass in Infants and Children With Congenital Heart Disease and to Assist Steady State Alfa-blockade in the Intensive Care Phase [NCT00620945]87 participants (Actual)Interventional2006-06-30Terminated(stopped due to New protocol now being used for cardiopulmonary bypass)
A Pilot Study for Randomized Controlled Trial on the Effect and Safety of Omitting Preoperative Alpha-adrenergic Blockade for Normotensive Pheochromocytoma [NCT05702944]Phase 424 participants (Anticipated)Interventional2023-01-18Recruiting
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00569855 (1) [back to overview]Number of Participants Who Had Significant Hypotension as Defined in the Protocol as Need for Norepinephrine Dose >0.1mcq/kg/Min in the First 72 Hours Postoperatively
NCT00620945 (2) [back to overview]Mortality
NCT00620945 (2) [back to overview]Number of Participants Achieving High Flow Low Pressure on Cardiopulmonary Bypass
NCT03176693 (5) [back to overview]Daily Cost of Drug
NCT03176693 (5) [back to overview]Hemodynamic Instability
NCT03176693 (5) [back to overview]Morbidity as Assessed by Occurrence of Adverse Events
NCT03176693 (5) [back to overview]Mortality
NCT03176693 (5) [back to overview]Participants Admitted to Post-operative Intensive Care Unit (ICU)

Number of Participants Who Had Significant Hypotension as Defined in the Protocol as Need for Norepinephrine Dose >0.1mcq/kg/Min in the First 72 Hours Postoperatively

Number of subjects who required Norepinephrine >0.1mcq/kg/min (NCT00569855)
Timeframe: 72 hours postoperatively

Interventionparticipants (Number)
Subjects Who Received Study Drug25

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Mortality

Percentage of patients who died within 30 days of the procedure (NCT00620945)
Timeframe: 30 days

InterventionParticipants (Count of Participants)
Phenoxybenzamine Treatment5

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Number of Participants Achieving High Flow Low Pressure on Cardiopulmonary Bypass

Percentage of patients who achieved high flow, low pressure on cardiopulmonary bypass (NCT00620945)
Timeframe: From time of cardiopulmonary bypass initiation until the time that high flow, low pressure on cardiopulmonary bypass was achieved, assessed up to 1 hour

InterventionParticipants (Count of Participants)
Phenoxybenzamine Treatment87

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Daily Cost of Drug

(NCT03176693)
Timeframe: Preoperative (2-3 weeks prior to surgery)

InterventionDollars (Median)
Phenoxybenzamine442.20
Doxazosin5.06

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Hemodynamic Instability

"Proportion of operative time outside target thresholds: SBP >180 or <80; DBP > 90; MAP>150 or <50; HR>90.~Arterial line blood pressure measurements were extracted from the electronic medical record every 60 seconds." (NCT03176693)
Timeframe: Intraoperative, approximately 90 minutes

Interventionpercentage of total operative time (Median)
Phenoxybenzamine14
Doxazosin13

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Morbidity as Assessed by Occurrence of Adverse Events

Morbidity will be graded by Clavien Classification of adverse events (NCT03176693)
Timeframe: Postoperatively during inpatient stay and during readmissions up to 30 days postoperatively

Interventionevents (Number)
Phenoxybenzamine0
Doxazosin0

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Mortality

Death within 30 days of surgery (NCT03176693)
Timeframe: 30 days postoperatively

InterventionParticipants (Count of Participants)
Phenoxybenzamine0
Doxazosin0

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Participants Admitted to Post-operative Intensive Care Unit (ICU)

(NCT03176693)
Timeframe: up to 30 days post-surgery

InterventionParticipants (Count of Participants)
Phenoxybenzamine2
Doxazosin1

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