Page last updated: 2024-12-05

phentolamine

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Description

Phentolamine: A nonselective alpha-adrenergic antagonist. It is used in the treatment of hypertension and hypertensive emergencies, pheochromocytoma, vasospasm of RAYNAUD DISEASE and frostbite, clonidine withdrawal syndrome, impotence, and peripheral vascular disease. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

phentolamine : A substituted aniline that is 3-aminophenol in which the hydrogens of the amino group are replaced by 4-methylphenyl and 4,5-dihydro-1H-imidazol-2-ylmethyl groups respectively. An alpha-adrenergic antagonist, it is used for the treatment of hypertension. [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]

Cross-References

ID SourceID
PubMed CID5775
CHEMBL ID597
CHEBI ID8081
SCHEMBL ID5653
MeSH IDM0016538
PubMed CID5702144
CHEMBL ID1204146
SCHEMBL ID293522
MeSH IDM0016538

Synonyms (215)

Synonym
AB00053768-28
BRD-K90333595-003-04-0
BRD-K90333595-001-02-8
gtpl502
BSPBIO_002496
SMP1_000236
phentolamine
DIVK1C_000807
KBIO1_000807
regitin
50-60-2
3-[(4,5-dihydro-1h-imidazol-2-ylmethyl)(4-methylphenyl)amino]phenol
SPECTRUM_000077
BSPBIO_000279
BCBCMAP01_000014
2-(n'-p-tolyl-n'-m-hydroxyphenylaminomethyl)-2-imidazoline
2-imidazoline, 2-((n-(m-hydroxyphenyl)-p-toluidino)methyl)-
2-(m-hydroxy-n-p-tolylanilinomethyl)-2-imidazoline
einecs 200-053-1
phenol, 3-(((4,5-dihydro-1h-imidazol-2-yl)methyl)(4-methylphenyl)amino)-
fentolamin
phentolamine [inn:ban]
phentolaminum [inn-latin]
hsdb 3382
dibasin
regitine
brn 0272944
2-((n-(m-hydroxyphenyl)-p-toluidino)methyl)-2-imidazoline
phenol, m-(n-(2-imidazolin-2-ylmethyl)-p-toluidino)-
c 7337 ciba
fentolamina [inn-spanish]
c 7337
NCGC00016311-01
cas-73-05-2
SPECTRUM5_001704
rogitine
PRESTWICK2_000230
BSPBIO_001435
PRESTWICK3_000230
IDI1_000807
BPBIO1_000307
LOPAC0_000982
2-(n-(m-hydroxyphenyl)-p-toluidinomethyl)imidazoline
DB00692
NCGC00021804-07
NCGC00021804-09
NCGC00021804-08
MLS000040874 ,
smr000058051
KBIO2_000477
KBIO2_005613
KBIO3_001716
KBIOGR_001338
KBIO2_003045
KBIOSS_000477
SPECTRUM4_000899
NINDS_000807
PRESTWICK1_000230
SPBIO_002200
PRESTWICK0_000230
SPECTRUM3_000788
NCGC00021804-06
NCGC00016311-02
NCGC00016311-03
MLS001201741
NCGC00021804-10
HMS1989H17
HMS2089E03
NCGC00016311-15
L001116
chebi:8081 ,
phentolamin
CHEMBL597
D08362
phentolamine (inn)
HMS1791H17
STK802099
NCGC00016311-10
AKOS004119917
phenol, 3-[[(4,5-dihydro-1h-imidazol-2-yl)methyl](4-methylphenyl)amino]-
EN300-51916
3-{[(4,5-dihydro-1h-imidazol-2-yl)methyl](4-methylphenyl)amino}phenol
3-[n-(4,5-dihydro-1h-imidazol-2-ylmethyl)-4-methyl-anilino]phenol; methanesulfonic acid
A828197
BBL010978
dtxcid703462
cas-50-60-2
dtxsid4023462 ,
tox21_110364
CCG-205062
HMS2235D17
regitina
NCGC00016311-06
NCGC00016311-07
NCGC00016311-17
NCGC00016311-05
NCGC00016311-12
NCGC00016311-16
NCGC00016311-14
NCGC00016311-13
NCGC00016311-09
NCGC00016311-04
NCGC00016311-11
NCGC00016311-08
phenotolamine
regitipe
phentalamine
z468598hbv ,
phentolaminum
unii-z468598hbv
fentolamina
5-25-09-00365 (beilstein handbook reference)
FT-0603219
phentolamine [vandf]
3-((4,5-dihydro-1h-imidazol-2-ylmethyl)(4-methylphenyl)amino)phenol
phentolamine [inn]
phentolamine [who-dd]
phentolamine [mi]
phentolamine [hsdb]
HMS3372H21
SCHEMBL5653
tox21_110364_1
NCGC00016311-19
W-105944
2-[n-(3-hydroxyphenyl)-p-toluidinomethyl]-2-imidazolidine
cid_5775
3-[n-(4,5-dihydro-1h-imidazol-2-ylmethyl)-4-methylanilino]phenol;methanesulfonic acid
cid_91430
3-[n-(2-imidazolin-2-ylmethyl)-4-methyl-anilino]phenol;mesylic acid
3-[n-(2-imidazolin-2-ylmethyl)-4-methyl-anilino]phenol;hydrochloride
3-[4,5-dihydro-1h-imidazol-2-ylmethyl-(4-methylphenyl)amino]phenol;methanesulfonic acid
bdbm31046
3-(((4,5-dihydro-1h-imidazol-2-yl)methyl)(p-tolyl)amino)phenol
rogitine (salt/mix)
3-[(4,5-dihydro-1h-imidazol-2-ylmethyl)-4-methylanilino]phenol #
fentolamine
m-[n-(2-imidazolin-2-ylmethyl)-p-toluidino]phenol
HMS3402H17
OPERA_ID_116
AB00053768_30
AB00053768_29
phentolamine mesylas
HY-12717
3-[[(4,5-dihydro-1h-imidazol-2-yl)methyl](4-methylphenyl)amino]phenol
SBI-0050955.P004
Q420360
Z732246520
SDCCGSBI-0050955.P005
NCGC00016311-33
phentol amine
CS-0012293
2-((n-(m-hydroxyphenyl)-p-toluidino)methyl)-
v03ab36
c04ab01
phentolaminum (inn-latin)
fentolamina (inn-spanish)
2-(n-p'-tolyl-n-(m'-hydroxyphenyl)aminomethyl)imidazoline
MLS001077339
nsc-757431
phentolamine hcl
CHEMBL1204146
3-[4,5-dihydro-1h-imidazol-2-ylmethyl-(4-methylphenyl)amino]phenol
MLS000028589 ,
phentolamine hydrochloride [usp]
phenol, m-(n-(2-imidazolin-2-ylmethyl)-p-toluidino)-, monohydrochloride
phenol, 3-(((4,5-dihydro-1h-imidazol-2-yl)methyl)(4-methylphenyl)amino), monohydrochloride
phentolamine chloride
m-(n-(2-imidazolin-2-ylmethyl)-p-toluidino)phenol monohydrochloride
einecs 200-793-5
3-(((4,5-dihydro-1h-imidazol-2-yl)methyl)(4-methylphenyl)amino)phenol hydrochloride
regitine hydrochloride
c-7337
73-05-2
phentolamine hydrochloride
PRESTWICK_386
phentolamine hydrochloride, >=98% (tlc), powder
NCGC00094835-02
NCGC00094835-01
smr000058252
SPECTRUM1500691
NCGC00094835-04
NCGC00094835-03
HMS1921E06
HMS1568N21
unii-86drw83r1h
86drw83r1h ,
nsc 757431
pharmakon1600-01500691
nsc757431
FT-0673687
3-[[(4,5-dihydro-1h-imidazol-2-yl)methyl](4-methylphenyl)amino]-phenol hydrochloride
3-(((4,5-dihydro-1h-imidazol-2-yl)methyl)(p-tolyl)amino)phenol hydrochloride
2-[n-(m-hydroxyphenyl)-p-toluidinomethyl]imidazoline hydrochloride
CCG-212878
SCHEMBL293522
phentolamine hydrochloride [mi]
phenol, 3-(((4,5-dihydro-1h-imidazol-2-yl)methyl)(4-methylphenyl)amino)-, hydrochloride (1:1)
phentolamine hydrochloride [who-dd]
DTXSID40223271
AKOS024282662
phentolaminehydrochloride
OPERA_ID_1231
mfcd00079268
3-[(4,5-dihydro-1h-imidazol-2-ylmethyl)(4-methylphenyl)amino]phenol (hcl)
sr-01000000055
phentolamine hydrochloride, united states pharmacopeia (usp) reference standard
SR-01000000055-11
AS-16924
phentolamine (hydrochloride)
E78589
Q27269732
3-[n-(4,5-dihydro-1h-imidazol-2-ylmethyl)-4-methylanilino]phenol;hydrochloride
3-[n-(4,5-dihydro-1h-imidazol-2-ylmethyl)-4-methylanilino]phenol;hydron;chloride
HY-12717A
3-[[(4,5-dihydro-1h-imidazol-2-yl)methyl](4-methylphenyl)amino]phenol hydrochloride (1:1)

Research Excerpts

Overview

Phentolamine mesylate (PM) is a pharmacological agent capable of reducing the duration of soft tissue anesthesia following dental treatments. PM is a reversible competitive alpha-adrenergic antagonist with similar affinities for alphal and alpha2 receptors.

ExcerptReferenceRelevance
"Phentolamine Mesylate (PM) is a pharmacological agent capable of reducing the duration of soft tissue anesthesia following dental treatments."( Reversing the effects of 2% Lidocaine: A randomized controlled clinical trial.
Brillant, MS; Flood, B; Michaud, PL, 2018
)
1.2
"Phentolamine mesylate is an important step in the progress of developing patient care as well as an aid to the dental clinician."( Phentolamine mesylate: It's role as a reversal agent for unwarranted prolonged local analgesia.
Grover, HS; Gupta, A; Saini, N; Saksena, N,
)
2.3
"Phentolamine is a reversible competitive alpha-adrenergic antagonist with similar affinities for alphal and alpha2 receptors. "( Development of hibernomas in rats dosed with phentolamine mesylate during the 24-month carcinogenicity study.
Auletta, C; Berardi, MR; Bolte, H; Halliwell, W; Hartman, B; Poulet, FM,
)
1.83
"Phentolamine is a readily available treatment, which is easily and safely given in the emergency setting."( Adrenaline-induced digital ischaemia reversed with phentolamine.
Molony, D, 2006
)
1.31
"Phentolamine proved to be an efficient inhibitor of the hypertensive reaction."( The effect of autonomic receptor blockers on the ocular response to topical chemical irritation.
Uusitalo, H, 1984
)
0.99
"Phentolamine is a specific blocking agent of alpha-noradrenergic receptors and depresses dorsal ICSS more than that of the ventral region."( Effect of clonidine and phentolamine on self-stimulation behavior in the dorsal and ventral regions of the lateral hypothalamus in mice.
Cazala, P, 1980
)
1.29
"Phentolamine mesylate is an alpha-1 and alpha-2 selective adrenergic receptor antagonist which has undergone clinical trials for erectile dysfunction treatment. "( Oral phentolamine: an alpha-1, alpha-2 adrenergic antagonist for the treatment of erectile dysfunction.
Goldstein, I, 2000
)
2.26
"Phentolamine appears to be a safe, simple and specific diagnostic agent, and more potent than amyl nitrite in eliciting dynamic obstruction in IHSS; phentolamine and amyl nitrite do not affect the obstructive index in patients with beta blockade."( Evaluation of phentolamine as a provocative test for idiopathic hypertrophic subaortic stenosis.
Blonder, R; Edelstein, J; Kerin, NZ; Mori, I; Rubenfire, M, 1979
)
1.34
"Phentolamine, that is an adrenergic blocking agent, relieved the early spam remarkably, but it was less effective on the late spam."( [Experimental Subarachnoid hemmorrhage in dogs--effect of various drugs and sympathectomy on cerebral arterial spasm (author's transl)].
Noda, S, 1975
)
0.98

Effects

Phentolamine 5 x 10(-6)M has a small effect in reducing the inhibitory effect of sympathetic nerve stimulation or of NA. Phentolamines have a toxic effect upon the cochlea independent from the synaptic process.

Phentolamine mesylate has been reported to be an effective local anesthetic reversal agent for soft tissue but has not been studied regarding reversal of pulpal anesthesia. Phentolamines has a toxic effect upon the cochlea independent from the synaptic process.

ExcerptReferenceRelevance
"Phentolamine has a simple chemical structure and is not a P-gp substrate."( Repurposing of phentolamine as a potential anticancer agent against human castration-resistant prostate cancer: A central role on microtubule stabilization and mitochondrial apoptosis pathway.
Chang, WL; Chao, CC; Guh, JH; Ho, CH; Hsu, JL; Hsu, LC; Liu, SP, 2015
)
1.49
"Phentolamine,, however, has a toxic effect upon the cochlea independent from the synaptic process."( Evidence that catecholamines are not the afferent transmitter in the cochlea.
Evans, EF; Klinke, R, 1977
)
0.98
"Phentolamine 5 x 10(-6)M has a small effect in reducing the inhibitory effect of sympathetic nerve stimulation or of NA."( The site and receptors responsible for the inhibition by sympathetic nerves of intestinal smooth muscle and its parasympathetic motor nerves.
Gillespie, JS; Khoyi, MA, 1977
)
0.98
"Phentolamine has been shown to safely reverse the effects of adrenaline should the feared complication of digital ischemia occur."( WALANT: Perceptions, approaches, and contraindications in a tertiary hand surgery unit.
Caine, P; Kokkinos, C; McCaughran, PW; Mosahebi, A; Nikkhah, D; Southall, C; Zargaran, D, 2022
)
1.44
"Phentolamine mesylate has been reported to be an effective local anesthetic reversal agent for soft tissue but has not been studied regarding reversal of pulpal anesthesia. "( Reversal of pulpal and soft tissue anesthesia by using phentolamine: a prospective randomized, single-blind study.
Beck, M; Drum, M; Elmore, S; Fowler, S; Nusstein, J; Reader, A, 2013
)
2.08
"Phentolamine has a simple chemical structure and is not a P-gp substrate."( Repurposing of phentolamine as a potential anticancer agent against human castration-resistant prostate cancer: A central role on microtubule stabilization and mitochondrial apoptosis pathway.
Chang, WL; Chao, CC; Guh, JH; Ho, CH; Hsu, JL; Hsu, LC; Liu, SP, 2015
)
1.49
"Phentolamine has been reported to be an effective local anesthetic reversal agent for soft tissue but has not been studied in endodontics. "( Reversal of soft-tissue anesthesia in asymptomatic endodontic patients: a preliminary, prospective, randomized, single-blind study.
Beck, M; Drum, M; Fowler, S; Nusstein, J; Reader, A, 2011
)
1.81
"phentolamine has the same efficacy and equal prolonged erection rate as 1 ml."( Comparative study of papaverine plus phentolamine versus prostaglandin E1 in erectile dysfunction.
Bechara, A; Casabé, A; Chéliz, G; Fredotovich, N; Rey, H; Romano, S, 1997
)
1.29
"Phentolamine,, however, has a toxic effect upon the cochlea independent from the synaptic process."( Evidence that catecholamines are not the afferent transmitter in the cochlea.
Evans, EF; Klinke, R, 1977
)
0.98
"Phentolamine has no clinically useful anti-hypertensive effect in conjunction with beta-blockers in patients with essential hypertension."( The transient anti-hypertensive effect of phentolamine in patients receiving beta-blocker treatment.
Dawson, A; Johnson, BF; Smith, I, 1977
)
1.24
"Phentolamine 5 x 10(-6)M has a small effect in reducing the inhibitory effect of sympathetic nerve stimulation or of NA."( The site and receptors responsible for the inhibition by sympathetic nerves of intestinal smooth muscle and its parasympathetic motor nerves.
Gillespie, JS; Khoyi, MA, 1977
)
0.98
"Phentolamine has been advocated for several years as a beneficial agent for the treatment of shock."( Phentolamine.
Gould, L; Reddy, CV, 1976
)
2.42
"Phentolamine has been used to prevent necrosis from norepinephrine."( Treatment of peripheral ischemia secondary to lidocaine containing epinephrine.
Aycock, BG; Hawtof, DB; Moody, SB, 1989
)
1
"Phentolamine has been shown to improve peripheral hemodynamics and have a favorable central hemodynamic effect, reflected in clinical improvement, in children with bradycardia (11 patients with second- or third-degree atrioventricular block) and signs of circulatory insufficiency."( [Effect of phentolamine on the clinical manifestations of the disease and hemodynamics in children with 2d- and 3d-degree atrioventricular block].
Dvoriakovskaia, GM; Iukhansoo, TP; Ternova, TI, 1988
)
2.11

Actions

Phentolamine abolished the increase in salivary flow and had no effect on theSalivary protein concentration. The lower dose of propranolol (5 mg/kg) reduced the 5HT-induced hyperglycemia; whereas the higher dose (10 mg/ kg) prevented the hyper glycemia. Phentolamines did not suppress the generation of the inhibitory junction potential produced by a single stimulant.

ExcerptReferenceRelevance
"Phentolamine abolished the increase in salivary flow and had no effect on the salivary protein concentration, whereas propranolol only reduced the salivary protein concentration."( Effects of amphetamine on salivary secretion.
Giglio, D; Götrick, B; Tobin, G, 2009
)
1.07
"Phentolamine was able to suppress translocation of PKC."( DNA synthesis of rat bone marrow mesenchymal stem cells through alpha1-adrenergic receptors.
Ai, G; Cheng, T; Deng, J; Han, J; Li, R; Ran, X; Shi, C; Su, Y; Wang, J; Zhu, C; Zou, Z, 2009
)
1.07
"Phentolamine did not produce any such protective effects."( [Effect of preliminary blockade of alpha- and beta-adrenoreceptors on stress-induced disorders of myocardial relaxation and contractile functions].
Pshennikova, MG; Vorontsova, EIa, 1983
)
0.99
"Phentolamine did not cause any change in insulin of glucagon secretion."( The effect of hypoxia on insulin and glucagon secretion in the perfused pancreas of the rat.
Abe, M; Ikeda, YU; Matsuba, I; Narimiya, M; Tanese, T; Yamada, H, 1982
)
0.99
"Phentolamine leads to an increase in FBM by preferentially antagonizing presynaptic alpha 2-adrenoreceptors over postsynaptic alpha 1-adrenoreceptors."( Alpha 1- and alpha 2-adrenoreceptor actions of phentolamine and prazosin on breathing movements in fetal sheep in utero.
Bennet, L; Giussani, DA; Hanson, MA; Moore, PJ; Spencer, JA, 1995
)
1.27
"Phentolamine prevented the increase in the Bmax of alpha 1-adrenoceptors and increased the equilibrium dissociation constant of these receptors (KD 0.17 to 0.53 nmol/l)."( Phentolamine and hypoxia: modulation of contractility and alpha 1-adrenoceptors in isolated rat atria.
Borea, PA; Caparrotta, L; Chinellato, A; Fassina, G; Froldi, G; Guerra, L; Pandolfo, L; Ragazzi, E, 1994
)
2.45
"Phentolamine caused an increase in the NE outflow."( Effects of hepatic nerve stimulation on blood glucose and glycogenolysis in rat liver: studies with in vivo microdialysis.
Ikarashi, Y; Ishimaru, H; Kishi, E; Maruyama, Y; Takahashi, A, 1996
)
1.02
"Phentolamine and the lower dose of propranolol (5 mg/kg) reduced the 5HT-induced hyperglycemia; whereas the higher dose (10 mg/kg) prevented the hyperglycemia."( The acute pharmacologic effects of serotonin on the release of insulin and glucagon in the intact rat.
Bryce, GF; Jacoby, JH, 1978
)
0.98
"Phentolamine did not suppress the generation of the inhibitory junction potential produced by a single stimulation but did slightly suppress the hyperpolarization produced by repetitive stimulation."( Responses to field stimulation of the smooth muscle cell membrane of the guinea pig stomach.
Ito, Y; Kuriyama, H, 1975
)
0.98
"Phentolamine produced an increase in heart rate relative to control only early in exercise but not during later, more strenuous, exercise."( Pulmonary artery and aortic pressure changes during high intensity treadmill exercise in the horse: effect of frusemide and phentolamine.
Coffman, JR; Erickson, BK; Erickson, HH, 1992
)
1.21
"Phentolamine did not inhibit the vasoconstrictor effect of NPY (n = 4)."( Vasoconstrictor effect of neuropeptide Y (NPY) on canine coronary artery.
Aizawa, Y; Funazaki, T; Hayashi, M; Ito, S; Murata, M; Shibata, A, 1985
)
0.99

Treatment

Phentolamine mesylate was associated with increases in Erectile Function Domain score of the IIEF, successful vaginal penetrations, and in overall satisfaction. Pretreatment with phentolamines or propranolol also significantly attenuated the depression of colonic motility induced by morphine.

ExcerptReferenceRelevance
"In phentolamine-pretreated venules, EFS suppressed SVCs with a venular dilatation in a manner attenuated by propranolol (1μM) or l-nitro arginine (LNA, 10μM)."( Neurohumoral regulation of spontaneous constrictions in suburothelial venules of the rat urinary bladder.
Hashitani, H; Mitsui, R; Mochizuki, S; Shimizu, Y, 2014
)
0.92
"Phentolamine or FK506 treatment during reperfusion improves alveolar liquid clearance and decreases the severity of lung injury."( Pharmacologic modulation of alveolar liquid clearance in transplanted lungs by phentolamine and FK506.
Berthiaume, Y; Dagenais, A; Ferraro, P; Sugita, M; VanSpall, M, 2009
)
2.02
"Phentolamine treatment augmented the basal IRI, IRG and SLI concentrations."( The nervous control of rat somatostatin, glucagon and insulin secretions.
Assan, R; Bobbioni, E; Kronheim, S; Marre, M; Miller, J; Sheppard, M, 1982
)
0.99
"In phentolamine-treated dogs, arterial pressure and heart rate were kept constant to prevent exacerbation of ischemia."( Effect of alpha-adrenergic blockade on arrhythmias induced by acute myocardial ischemia and reperfusion in the dog.
Bolli, R; Fisher, DJ; Miller, RR; Taylor, AA; Young, JB, 1984
)
0.78
"In phentolamine-treated cats, reductions in arterial pressure and total peripheral resistance produced by infusions of dobutamine were little affected by the beta 2-adrenoceptor-selective antagonist butoxamine, but were antagonized by atenolol."( Beta-adrenoceptor selectivity of dobutamine: in vivo and in vitro studies.
Maccarrone, C; Malta, E; Raper, C,
)
0.65
"Phentolamine pretreatment completely blocked all vascular actions of norepinephrine, and largely inhibited the cutaneous vasoconstriction produced by the infusion of the low dose of serotonin."( Evidence that serotonin receptors mediate the cutaneous vasoconstriction produced by 5-hydroxytryptamine in canine forelimbs.
Adamski, SW; Dobbins, DE; Grega, GJ; Lokhandwala, MF, 1983
)
0.99
"Phentolamine pretreatment, which in itself caused a 55% decrease in dorsal aortic pressure, did not prevent the recovery of blood pressure after hemorrhage."( Vascular recovery following hemorrhage in the dogfish shark Squalus acanthias.
Carroll, RG; Keller, NE; Opdyke, DF, 1984
)
0.99
"Phentolamine pretreatment totally abolished ANG II pressor action in the hagfish and chicken and diminished the ANG II pressor response in other classes of vertebrates."( Evolution of angiotensin II-induced catecholamine release.
Carroll, RG; Opdyke, DF, 1982
)
0.99
"Phentolamine pretreatment at 15 mg/kg reduced locomotion, wall climbing and attenuated the reduction in core temperature."( Behavioral and temperature changes induced by clonidine in the developing rat.
Isaacson, RL; Reinstein, DK, 1981
)
0.98
"In phentolamine-treated patients, ST-segment changes and cardiac pain severity during the second inflation were similar to those observed during the first inflation (13+/-9 versus 12+/-8 mm, P=NS, and 51+/-34 versus 54+/-32 mm, P=NS, respectively), whereas in placebo-treated patients, they were significantly less (6+/-4 versus 13+/-7 mm, P<.01, and 26+/-20 versus 49+/-22 mm, P<.05, respectively)."( Phentolamine prevents adaptation to ischemia during coronary angioplasty: role of alpha-adrenergic receptors in ischemic preconditioning.
Chiariello, L; Crea, F; De Paulis, R; Gaspardone, A; Ghini, AS; Gioffrè, PA; Tomai, F; Versaci, F, 1997
)
2.25
"Phentolamine pretreatment (10 mg/kg) also significantly inhibited the effect of morphine."( Studies on the mechanism of the action of morphine on the peristalsis of guinea pig ileum in situ.
Aldunate, J; Mardones, J; Yojay, L, 1975
)
0.98
"In phentolamine-pretreated rats levodopa produced a further marked increase in the plasma IRI concentration."( The effects of levodopa on plasma glucose in two strains of rat.
Furman, BL; Wilson, GA, 1979
)
0.77
"In phentolamine-treated animals, bleeding produced a drop in AP and CO similar to that observed in the nontreated animals; however, the decrease in CBF was less marked."( Cerebral blood flow during hemorrhagic hypotension in the unanesthetized goat.
Alborch, E; Dieguez, G; Gómez, B; Lluch, S; Vallejo, AR, 1977
)
0.77
"Phentolamine treatment did not alter the T4 uptake and T3 production in perfused liver of fasting rats."( Possible role of adrenergic mechanism in starvation-induced reduction in circulating thyroxine and triiodothyronine in rats.
Hoshino, T; Ikeda, T; Mashiba, H; Ohtani, I; Takeuchi, T; Tanaka, Y, 1991
)
1
"Phentolamine pretreatment (0.1 mg/kg iv) blunted the hypoxemia-related decrease of mean Qtr n (-8%; P = NS)."( Independent control of mucosal and total airway blood flow during hypoxemia.
Baier, HJ; Chediak, AD; Elsasser, S; Long, WM; Wanner, A, 1991
)
1
"Phentolamine pretreatment (5 mumol.litre-1) markedly reduced the production of TXA2, but not of PGI2, in diabetic vessels."( Increased vasoconstrictor response to noradrenaline in femoral vascular bed of diabetic dogs. Is thromboxane A2 involved?
Ballagi-Pordány, G; Hadházy, P; Koltai, MZ; Pogátsa, G; Rösen, P, 1990
)
1
"3. Phentolamine treatment partially inhibited the pressor effects to A II."( Effects of angiotensin II on isolated toad (Bufo arenarum) aortic rings.
Coviello, A; Lebenshon de Chialvo, P; Peral de Bruno, M, 1988
)
0.79
"In phentolamine-treated cats dobutamine did not demonstrate inotropic selectivity and showed a relationship between increased inotropy and tachycardia which was not significantly different from that obtained with isoprenaline."( The importance of the alpha-adrenoceptor agonist activity of dobutamine to inotropic selectivity in the anaesthetized cat.
Johnson, SF; Kenakin, TP, 1985
)
0.78
"Phentolamine (10(-6) M) pretreatment had no effect on the ouabain-induced contraction but partially suppressed it in both SHR and WKY aortas when diltiazem (10(-5) M) was also added."( Ouabain-induced contraction of vascular smooth muscle in spontaneously hypertensive rats and the effect of hydralazine.
Iwasaki, T; Kawai, Y; Miyata, S; Morita, S; Nagai, K, 1988
)
1
"Phentolamine pretreatment significantly increased the arrhythmogenic and lethal doses of digoxin."( Increases in CSF norepinephrine associated with the onset of digoxin-induced arrhythmias.
Plunkett, LM; Tackett, RL, 1987
)
0.99
"Phentolamine pretreatment (3 mg/Kg, i.v.) did significantly antagonize the pressor effect in urethane anesthetized animals."( Cardiovascular effects of cocaine in anesthetized and conscious rats.
Marwah, J; Pitts, DK; Udom, CE, 1987
)
0.99
"Phentolamine pretreatment significantly decreased feeding elicited by norepinephrine without affecting feeding elicited by NPY."( Neuropeptide Y injected in the paraventricular hypothalamus: a powerful stimulant of feeding behavior.
Leibowitz, SF; Stanley, BG, 1985
)
0.99
"Pretreatment with phentolamine dramatically ameliorated LPS-inhibited cell proliferation."( Chronic stress enhances progression of periodontitis via α1-adrenergic signaling: a potential target for periodontal disease therapy.
Gu, J; Lin, S; Liu, S; Lu, H; Wang, F; Xu, M, 2014
)
0.73
"Treatment with phentolamine reduced the frequency and amplitude of the pacemaker currents and increased the resting outward currents."( Phentolamine inhibits the pacemaker activity of mouse interstitial cells of Cajal by activating ATP-sensitive K+ channels.
Ahn, SW; Choi, S; Jun, JY; Kim, JH; Kim, SH; So, I; Sun, JM; Wie, HW; Yeum, CH, 2010
)
2.14
"Pretreatment with phentolamine attenuated these effects except at 100 mcg/kg epinephrine."( Epinephrine induces rapid deterioration in pulmonary oxygen exchange in intact, anesthetized rats: a flow and pulmonary capillary pressure-dependent phenomenon.
Feinstein, DL; Hensel, P; Hiller, DB; Krishnamoorthy, V; Lin, B; Minshall, R; Oswald, S; Ripper, R; Rothschild, L; Rubinstein, I; Vogel, SM; Weinberg, GL, 2012
)
0.7
"Treatment with phentolamine mesylate was associated with increases in Erectile Function Domain score of the IIEF, successful vaginal penetrations, and in overall satisfaction."( Long-term safety and efficacy of oral phentolamine mesylate (Vasomax) in men with mild to moderate erectile dysfunction.
Auerbach, S; Coogan, C; Goldstein, I; Klimberg, I; Lammers, P; Padma-Nathan, H, 2002
)
0.93
"Pretreatment with phentolamine or propranolol also significantly attenuated the depression of colonic motility induced by morphine."( The sympathetic nervous system is involved in the inhibitory effect of morphine on the colon motility in rats.
Guo, SY; Hisamitsu, T; Jiao, YY; Okada, M; Umezawa, T, 2002
)
0.64
"Pretreatment with phentolamine (>1.0 mg kg(-1), i.v.) had no effect on the output of protein that occurred during combined stimulation of the parasympathetic and sympathetic innervations but increased the flow of saliva and the output of electrolytes."( Autonomic control of protein production by the parotid gland of the sheep.
Edwards, AV; Titchen, DA, 2003
)
0.64
"Pretreatment with phentolamine (30 microgram/5 microliter, icv, n=8), prazosin (10 microgram/5 microliter, icv, n=12) or alpha-helical CRF(9-41) (10 microgram/5 microliter, icv, n=9) prevented the decrease in cardiac output elicited by acute cold water stress in vascular responders without affecting mixed responders."( Central alpha-adrenergic receptors and corticotropin releasing factor mediate hemodynamic responses to acute cold stress.
Gan, Q; Knuepfer, MM; Tan, Y, 2003
)
0.64
"Pretreatment with phentolamine or propranolol at a dose of 100 microg kg(-1) had no effect on the increases in either MBF or LBF evoked by LN stimulation."( Evidence for parasympathetic vasodilator fibres in the rat masseter muscle.
Ishii, H; Izumi, H; Niioka, T; Sudo, E, 2005
)
0.65
"Pretreatment by phentolamine or by guanethidine did not influence the effect of indomethacin on renal haemodynamics or renal function."( Effects of alfa-receptor and adrenergic neuron blockade on indomethacin-induced changes of renal haemodynamics.
Fejes-Tóth, G; Zahajszky, T, 1980
)
0.59
"Pretreatment with phentolamine, 1 mg/kg i.v."( Inhibition of renin secretion by clonidine after alpha-adrenoceptor blockade in anesthetized dogs.
Nolan, PL; Reid, IA, 1981
)
0.59
"Pretreatment with phentolamine inhibited the contraction evoked by lower frequencies of perivascular nerve stimulation (below 0.5 Hz)."( Effects of 3,4-dihydro-8-(2-hydroxy-3-isopropylaminopropoxy)-3-nitroxy-2H-1-benzopyran (K-351) on smooth muscle cells and neuromuscular transmission in the canine mesenteric artery.
Kou, K; Kuriyama, H; Suzuki, H, 1982
)
0.59
"Pretreatment with phentolamine significantly increased basal plasma insulin concentration but the response pattern to splanchnic nerve stimulation was not altered."( Effects of adrenergic blockade on the release of insulin, glucagon and somatostatin from the pancreas in response to splanchnic nerve stimulation in cats.
Andersson, PO; Holst, J; Järhult, J, 1982
)
0.59
"Pre-treatment with phentolamine almost completely suppressed the growth hormone response to insulin-induced hypoglycaemia, but had no effect upon the amplitude or duration of the elevation of plasma ACTH or cortisol levels following insulin administration."( The effect of alpha-adrenergic blockade on the release of ACTH and cortisol in vivo.
Lister, D; Spencer, GS, 1983
)
0.58
"Pretreatment with phentolamine, an alpha-adrenergic blocker, increases the systemic arterial hypotension and shortens the survival time."( [Cardiovascular collapse after tracheal ligature in the rat].
Lagneaux, D; Lecomte, J; Remacle, R, 1980
)
0.58
"Pretreatment with phentolamine prevented the increase in CVR and the elevation in ST segment."( Coronary spasm produced by picrotoxin in cats.
Gillis, RA; Pearle, DL; Segal, SA, 1981
)
0.59
"Pre-treatment with phentolamine significantly reduced, but failed to eliminate, the release of both pancreatic glucagon and pancreatic polypeptide."( Characteristics of the neuroendocrine responses to stimulation of the splanchnic nerves in bursts in the conscious calf.
Bloom, SR; Edwards, AV, 1984
)
0.59
"Pretreatment with phentolamine (0.5 mg X kg-1), pizotifen (0.5 mg X kg-1) or their combination did not effectively modify the responses to ergotamine."( Ergotamine-induced constriction of cranial arteriovenous anastomoses in dogs pretreated with phentolamine and pizotifen.
Heiligers, J; Hof, RP; Koedam, NA; Saxena, PR, 1983
)
0.81
"Pretreatment with phentolamine or penfluridol did not modify the effect of CM 57493 on food intake."( Two novel agents affecting eating through an action on monoaminergic systems.
Miranda, GF; Roncucci, R; Verry, M, 1984
)
0.59
"Pretreatment with phentolamine, an alpha-adrenoceptor blocking agent (0.5 mg/kg i.v."( Long-lasting hypothermic effects of vincristine in rats.
Ammendola, D; De Gori, N; Gratteri, S; Naccari, F; Nisticò, G; Rotiroti, D, 1984
)
0.59
"A pretreatment with phentolamine, an antagonist at alpha-adrenoceptors prevented the hypothermic phase following the endotoxin administration."( Behavioural and body temperature effects of meningococcal lipopolysaccharide after intraventricular injection in adult fowls Gallus domesticus.
Focà, A; Fumarola, D; Mastroeni, P; Nisticò, G; Rotiroti, D, 1981
)
0.58
"Pretreatment with phentolamine or production of a functional sympathectomy by bilateral adrenal demedullation and chronic guanethidine treatment augmented the hyperinsulinaemic effect of isoprenaline."( Some factors modifying the insulinotropic and cardiovascular effects of isoprenaline in the rat.
Furman, BL; Twaij, HA, 1981
)
0.59
"pretreatment with phentolamine and 6-hydroxydopamine, respectively."( [Central hypotensive effects of guanfacine in anaesthetised rabbits (author's transl)].
Oguma, M; Ohkubo, K; Otorii, T; Suzuki, K, 1982
)
0.59
"Pretreatment with phentolamine significantly attenuated the constriction and augmentation of vasomotion."( Microvascular response to blockade of prostaglandin synthesis in rat skeletal muscle.
Faber, JE; Harris, PD; Joshua, IG, 1982
)
0.59
"Pretreatment with phentolamine (0.2 or 0.5 mg x kg-1 i.c.) prevented the bradycardia and produced dose-related attenuation of the pressor response."( Mechanisms of acute hypertension and bradycardia following intracisternal 6-hydroxydopamine in conscious rabbits.
Head, GA; Korner, PI, 1980
)
0.58
"Pretreatment with phentolamine reversed this BP response and this depressor effect was blocked by propranolol (2 mg/kg i.v.) suggesting that the pressor effect of cocaine was mediated by EPI."( Role of the sympathoadrenal axis in the cardiovascular response to cocaine in conscious unrestrained rats.
Chen, BX; Myles, J; Wilkerson, RD, 1995
)
0.61
"Treatment with phentolamine, yohimbine or idazoxan suppressed the IPSPs before and after potentiation by forskolin, suggesting that the IPSPs were mediated by release of norepinephrine acting at alpha 2-adrenoceptors."( Elevation of cAMP facilitates noradrenergic transmission in submucous neurons of guinea pig ileum.
Cooke, HJ; Wood, JD; Zafirov, DH, 1993
)
0.63
"Pretreatment with phentolamine (10(-5) M) (alpha-antagonist) converted the contraction induced by NE to relaxation in coronary rings precontracted with ONO11113 (thromboxane A2 derivative)."( Participation of alpha 1- and beta 1-adrenoceptors in norepinephrine-induced contraction and relaxation of isolated equine coronary artery in vitro.
Kabeyama, A; Nishio, A; Obi, T, 1994
)
0.61
"Pretreatment with phentolamine reduced fast-induced food intake by 39% (P < 0.05), with no evidence of an additive effect when phentolamine was given together with NPYAb."( A role for neuropeptide-Y, dynorphin, and noradrenaline in the central control of food intake after food deprivation.
al-Dokhayel, AA; Bloom, SR; Bohuon, C; Comoy, E; Gilbey, SG; Lambert, PD; Wilding, JP, 1993
)
0.61
"Pretreatment with phentolamine markedly inhibited the contractile responses to field stimulation of both diabetic and control caudal arteries, while 6-hydroxydopamine essentially abolished responses to electrical field stimulation and tyramine in both tissues."( Contractile responses of caudal arteries from diabetic rats to adrenergic nerve stimulation.
MacLeod, KM; Weber, LP,
)
0.45
"Pretreatment with phentolamine, an alpha-adrenergic receptor antagonist, and alprenolol, a beta-adrenergic receptor antagonist, or phentolamine alone significantly suppressed the hypertriglyceridemia induced by LTA."( Lipoteichoic acid stimulates lipolysis and hepatic triglyceride secretion in rats in vivo.
Feingold, KR; Grunfeld, C; Moser, AH; Nonogaki, K; Pan, XM; Staprans, I, 1995
)
0.61
"Pretreatment with phentolamine (1.0 mg/kg i.v.) completely blocked the immediate (1-4 min) pressor effect of U50,488H, but not the subsequent increase in blood pressure after 5 min."( U50,488H-induced pressor effect in the ovine foetus is mediated by sympathetic activation and vasopressin.
Fukuda, S; Soong, Y; Szeto, HH; Taylor, CT; Wu, D; Yee, JS, 1996
)
0.62
"Pretreatment with phentolamine attenuated the pancuronium-induced increase in PAP."( Pancuronium increases pulmonary arterial pressure in lung injury.
Du, H; Hanaoka, K; Hayashida, M; Hayashita, M; Kin, N; Orii, R; Suwa, K; Yamada, Y, 1996
)
0.62
"pretreatment with phentolamine had no effect on the tachycardia elicited by DAMGO (1 nmol); however, the pressor response was reversed to a state of hypotension, the renal and superior mesenteric vasoconstrictions were attenuated and the hindquarter vasodilation was potentiated."( Mechanisms of the regional hemodynamic effects of a mu-opioid receptor agonist microinjected into the hypothalamic paraventricular nuclei of conscious unrestrained rats.
Bachelard, H; Lessard, A; Pître, M, 1997
)
0.62
"Pretreatment with phentolamine, an alpha-adrenoceptor antagonist, inhibited the increase in the pulmonary vascular resistance index and restored the decrease in the systemic vascular resistance index during exercise in the bilateral group."( Simultaneous evaluation of left- and right-sided heart pumping function during dynamic leg exercise in patients with mild chronic congestive heart failure, with special reference to afterload and plasma noradrenaline.
Asano, K; Fujiwara, H; Ito, H; Kakami, M; Koshiji, M; Minatoguchi, S; Uno, Y; Yokoyama, H, 1997
)
0.62
"pretreatment with phentolamine and cyproheptadine caused a reduction of Fos-like immunoreactive neurons of only 4% on the intact side, namely, the differences in the number of Fos-like immunoreactive neurons on two sides of the lumbar spinal cord owing to the unilateral dorsolateral funiculus lesion were nearly abolished by i.t."( Effects of intrathecal monoamine antagonists on the nociceptive c-Fos expression in a lesioned rat spinal cord.
Dafny, N; Liu, RJ; Nie, H; Qiao, JT; Wang, R; Zhang, RX, 1997
)
0.62
"Pretreatment with phentolamine significantly increased the microvascular response in young rats at high (87 percent) and low (36 percent) frequency ES."( Age-related changes in sympathetic modulation of sensory nerve activity in rat skin.
Helme, RD; Khalil, Z; Merhi, M, 1998
)
0.62
"Treatment with phentolamine completely blocked the stimulatory effect of NA on serum levels of LH in NA treated geese."( Effects of third ventricle injection of norepinephrine analogue on LH secretion of the non-laying SIJI goose.
Cheng, Z; Taya, K; Watanabe, G; Yang, P, 2000
)
0.65
"Pretreatment with phentolamine (250 microg/animal, i.c.v.), an alpha-adrenoceptor antagonist, attenuated the elevation of plasma corticosterone evoked by SIN-1, but sotalol (300 microg/animal, i.c.v.), a beta-adrenoceptor antagonist, was without effects."( Centrally applied nitric oxide donor elevates plasma corticosterone by activation of the hypothalamic noradrenergic neurons in rats.
Murakami, Y; Okada, S; Yokotani, K, 2002
)
0.64
"Pretreatment with phentolamine and nitroglycerine increased transplanted cell entry in liver sinusoids, whereas labetalol, nifedipine, CGRP, and glucagon were ineffective."( Hepatic sinusoidal vasodilators improve transplanted cell engraftment and ameliorate microcirculatory perturbations in the liver.
Bhargava, KK; Gupta, S; Ito, Y; McCuskey, RS; Palestro, CJ; Rajvanshi, P; Slehria, S; Sokhi, RP, 2002
)
0.64
"Treatment by phentolamine was carried out in 30 patients presenting with an acute myocardial infarction complicated by left ventricular failure, 8 of which had cardiogenic shock. "( [Vasodilator treatment of the acute phase of myocardial infarct with phentolamine. Analysis of hemodynamic results and therapeutic indications].
Benhaiem, N; Castaigne, A; Estampes, B; Francoual, M; Lellouche, D; Vernant, P, 1978
)
0.86
"Pretreatment with phentolamine reduced the increases in aortic blood pressure and total peripheral vascular resistance produced by beta-phenylethylamine, whereas, the effects of beta-phenylethylamine on left ventricular dP/dt and (dP/dt)/P were abolished by propranolol."( Cardiovascular actions of beta-phenylethylamine.
Liang, CS; Sprecher, D, 1979
)
0.58
"Pretreatment with phentolamine abolished the alpha stimulant-induced inhibition of bihormonal output."( Effect of alpha adrenoreceptor stimulants infused intrapancreatically on glucagon and insulin secretion.
Kajinuma, H; Kaneto, A; Kosaka, K, 1977
)
0.58
"Pretreatment with phentolamine prevented the effect of dihydro-ouabain on perfusion pressure."( Effect of dihydro-ouabain on vascular tone on the perfused cannine hindlimb.
Bhat, HB; Gillis, RA; Quest, JA; Rowles, GS, 1976
)
0.58
"Treated with phentolamine (3.7-15 mg/kg) these rats increased the rate of lever pressing dose dependently, i.e."( [A method for determination of thermally motivated behavior (author's transl)].
Bürgel, P; Schulze, G, 1976
)
0.61
"Pretreatment with phentolamine evoked an enhancement in both basal output of insulin and its response to splanchnic stimulation, but did not exert any marked effect on glucagon output."( Effect of splanchnic nerve stimulation on glucagon and insulin output in the dog.
Kajinuma, H; Kaneto, A; Kosaka, K, 1975
)
0.58
"Pretreatment with phentolamine suppressed excitation of the afferent fibers, development of systolic bulge and elevation of the ST segment."( Sustained decreased in coronary blood flow and excitation of cardiac sensory fibers following sympathetic stimulation.
Murao, S; Uchida, Y, 1975
)
0.58
"Pretreatment with phentolamine injected into the 3rd ventricle produced a dose-dependent inhibition of the NA-induced antidiuretic effects."( Effect of intraventricular administration of noradrenaline on water diuresis in goats.
Peeters, G; Vandeputte-Van Messon, G, 1975
)
0.58
"Pretreatment with phentolamine (1 mg kg-1) significantly increased and pretreatment with clonidine (60 micrograms kg-1 h-1) significantly decreased somatostatin release caused by vagal stimulation, whereas gastrin levels remained largely unchanged."( Alpha 2-receptor-mediated inhibition of intraluminal release of gastric somatostatin in anaesthetized rats.
Aliño, SF; Garcia, D; Uvnäs-Moberg, K, 1992
)
0.61
"Treatment with phentolamine (6.6 mumol/L), an alpha-adrenoceptor antagonist, had similar effects, though the CPK release profile was shifted to the right and downwards."( Protective effects of berberine and phentolamine on myocardial reoxygenation damage.
Chen, S; Du, X; Han, Y; Huang, W; Huang, Z; Xu, S; Zhang, G, 1992
)
0.9
"Pretreatment with phentolamine, an alpha adrenergic antagonist, blocked the release of PA by epinephrine while pretreatment with the beta blocker propranolol had no effect."( Adrenergic stimulation of regional plasminogen activator release in rabbits.
Chandler, WL; Loo, SC; Mornin, D, 1992
)
0.61
"Pretreatment with phentolamine reversed the blood flow and PVO2 responses to PYY because SPBF, PVO2 and PBF were significantly increased above the control level."( Effects of peptide YY on pancreatic blood flow and oxygen consumption.
Czarnobilski, K; Gustaw, P; Hottenstein, OD; Konturek, SJ; Pawlik, WW; Sendur, R,
)
0.45
"Treatment with phentolamine did not sufficiently reduce the PAP and AP to test our hypothesis that a reduction in PAP and AP would eliminate EIPH."( Pulmonary artery and aortic pressure changes during high intensity treadmill exercise in the horse: effect of frusemide and phentolamine.
Coffman, JR; Erickson, BK; Erickson, HH, 1992
)
0.83
"Treatment with phentolamine converted the vein contraction to a relaxation, which was not influenced by propranolol but was abolished by droperidol."( Responses to dopamine of isolated human and monkey veins compared with those of the arteries.
Okamura, T; Toda, N; Yamazaki, M, 1991
)
0.62
"Pretreatment with phentolamine (2 mg kg-1 i.v.) eliminated the effect of opioid blockade indicating an interaction between the opioid and the adrenergic mechanisms."( Interaction between antisecretory opioid and sympathetic mechanisms in the rat small intestine.
Sjöqvist, A, 1991
)
0.6
"pretreatment with phentolamine; the coadministration of phentolamine with methysergide produced no greater antagonism of effects."( Intrathecal coadministration of clonidine with serotonin receptor agonists produces supra-additive visceral antinociception in the rat.
Danzebrink, RM; Gebhart, GF, 1991
)
0.6
"Pretreatment with phentolamine (2.5 mg/kg i.v.) had no effect on the inhibitory response produced by cromakalim but glibenclamide (25 mg/kg iv.), an inhibitor of ATP-sensitive potassium channels, blocked its effect."( A potassium channel activator modulates both excitatory noncholinergic and cholinergic neurotransmission in guinea pig airways.
Barnes, PJ; Ichinose, M, 1990
)
0.6
"Pretreatment with phentolamine blocked the vasoconstriction caused by injection of epinephrine, and produced a mild reduction in responses to neuropeptide Y."( Neuropeptide Y mimics a non-adrenergic component of sympathetic vasoconstriction in the bullfrog.
Fatherazi, S; Horn, JP; Stofer, WD, 1990
)
0.6
"Pretreatment with phentolamine accentuated the peak pressor response and the reduction in heart rate induced by NPY administration but had little effect on the local haemodynamic changes in each vascular bed."( Effects of neuropeptide Y on the renal, mesenteric and hindlimb vascular beds of the conscious rabbit.
Chalmers, J; McRitchie, R; Minson, R, 1989
)
0.6
"Pretreatment with phentolamine did not prevent the decrease in blood flow observed after electrically induced ventricular fibrillation."( Effect of alpha-adrenergic receptor blockers on the vulnerability of cat heart to ventricular fibrillation.
Dikshit, M; Kar, K; Srimal, RC,
)
0.45
"Treatment with phentolamine or saralasin failed to prevent the waning of the vasodilation during the prolonged infusion of BK into forelimbs perfused at constant flow."( Contribution of kininase II to the waning of vascular actions of bradykinin.
Adamski, SW; Grega, GJ, 1988
)
0.61
"Pretreatment with phentolamine had no effect on the prevalence of ascites."( Neurogenic hyperacute ascites in mice.
Bensch, KG; Morin, ME; Murphy, BJ; Nelson, DP; Robin, ED; Theodore, J; Wong, RJ, 1986
)
0.59
"Pretreatment with phentolamine and propranolol enhanced the dilator response of the pre- and postglomerular vessels (except the afferent arterioles near glomeruli and efferent arterioles near welling points) to dopamine (3 X 10(-5) and 1 X 10(-4) M), and abolished the reductions in diameter produced by the high dopamine levels."( Responses of in vivo renal microvessels to dopamine.
Dussel, R; Fleming, J; Parekh, N; Steinhausen, M; Weis, S, 1986
)
0.59
"Pretreatment with phentolamine antagonised the phasic response to stimulation and the contraction to noradrenaline."( Antagonism of the ATP component of sympathetic co-transmission in the rat vas deferens by AMP.
Satchell, D, 1986
)
0.59
"Pretreatment with phentolamine and haloperidol did not antagonize that effect, while pretreatment with propranolol or BW392C60 abolished or reversed the action of dopamine."( The effect of dopamine on blood flow in skeletal muscles.
Beutler, A; Chodera, A; Kozłowska, T; Krawczak, J; Wasik-Olejnik, A,
)
0.45
"Pretreatment with phentolamine (10 microM) abolished the resistance response and enhanced stimulated NE release, which roughly tripled at 10 Hz."( Perfused rat intestine for study of norepinephrine release.
Keeton, TK; Riedel, GL; Shepherd, AP, 1988
)
0.6
"Pretreatment with phentolamine (5 mg/kg i.p.) but not propranolol (15 mg/kg i.p.) inhibited the HA-induced hyperglycemia by about 50% and the combination of same doses of phentolamine and propranolol blocked the response completely."( Mechanism of the central hyperglycemic action of histamine in mice.
Itoh, Y; Nishibori, M; Oishi, R; Saeki, K, 1987
)
0.6
"Pretreatment with phentolamine and ketanserin, an alpha-adrenoceptor antagonist and a 5-hydroxytryptamine2 inhibitor, did not alter vasoconstriction to thiopental."( Mechanism of vascular responsiveness to barbiturates in isolated and perfused canine basilar arteries.
Chiba, S; Tsuji, T, 1987
)
0.6
"Pretreatment with phentolamine and nadolol did not eliminate the increases in left ventricular pressure and intracellular calcium activity caused by the infusion of the monovalent carboxylic ionophores monensin and salinomycin."( Alterations in intracellular calcium activity and contractility of isolated perfused rabbit hearts by ionophores and adrenergic agents.
Lattanzio, FA; Pressman, BC, 1986
)
0.59
"Treatment with phentolamine was accompanied by a marked increase in heart rate with a concomitant increase in cardiac index and the rate-pressure product."( Comparison of phentolamine and urapidil in controlling acute intra-operative hypertension in patients subjected to coronary artery bypass surgery.
Hess, W; Schulte-Sasse, U; Tarnow, J; Veit, S, 1985
)
0.97
"Pretreatment with phentolamine (17.7 nmol) in the nucleus tractus solitarius also reduced the sensitivity of the bradycardia component of the reflex and attenuated (3 and 6 nmol) the induced inhibition of the bradycardia induced by stimulation of the anterior hypothalamus."( Interaction between the baroreflex and anterior hypothalamic stimulation. Demonstration of a noradrenergic involvement.
Basuray, BN; Copeland, R; Simon, OR; West, WL, 1985
)
0.59
"Treatment with phentolamine and propranolol (both 1 muM) had no effect on the adenine nucleotide release elicited by nicotine and electrical field stimulation, whereas such treatment reduced the inhibitory action of both stimuli.5."( (3H)-adenosine nucleotide and (3H)-noradrenaline uptake by cold stored guinea-pig taenia caecum; mechanical effects and release of (3H)-adenosine nucleotide by noradrenaline, papaverine, and nitroglycerine.
Kuchii, M; Miyahara, JT; Shibata, S, 1973
)
0.59

Toxicity

The most common adverse events included rhinitis, headache, tachycardia, and nausea. The occurrence of adverse events (mild and moderate) was greater in phentolamine mesylate group compared to the control group.

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
" The toxic effect of epinephrine was eliminated by the addition of propranolol or selective beta 2 blockade, but not by alpha or beta 1 blockade."( Toxic effects of catecholamines on skin.
Burk, RW; Klitzman, B; Serafin, D, 1990
)
0.28
" However, for the safe implementation of this method, close and intensive cooperation between the physician and his patient is a condition that has to be guaranteed."( How safe is the treatment of impotence with intracavernous autoinjection?
Ludwig, G; Zentgraf, M; Ziegler, M, 1989
)
0.28
" This effect does not appear to result from an inhibition of the toxic metabolite(s) of cocaine, as a 10-fold molar excess of yohimbine failed to antagonize lipid peroxidation caused by in vitro incubation of cocaine with hepatic microsomes."( Antagonism of cocaine-induced hepatotoxicity by the alpha adrenergic antagonists phentolamine and yohimbine.
Harbison, RD; James, RC; Roberts, SM; Schiefer, MA, 1987
)
0.5
" One potential mechanism by which phentolamine may diminish the bromobenzene-induced hepatotoxicity is by a direct or indirect interference with the metabolism of bromobenzene to toxic metabolites."( Antagonism of bromobenzene-induced hepatotoxicity by phentolamine: evidence for a metabolism-independent intervention.
Gandy, J; Harbison, RD; Hinson, JA; James, RC; Kerger, BD; Roberts, SM, 1988
)
0.8
" The oral LD50 values for these species were similar."( Acute, subacute and chronic toxicity/Carcinogenicity of lofexidine.
Beitman, RE; Fontaine, R; Friehe, H; Gibson, JP; Larson, EJ; Tsai, TH, 1982
)
0.26
") reduced the "average total body clearance" (as measured by dose/AUC) and the LD50 of various compounds that are eliminated almost entirely by the kidneys."( Effects of isoproterenol on the toxicity in rats of compounds eliminated by the kidneys.
Gillette, JR; Maling, HM; Saul, W; Yasaka, WJ, 1980
)
0.26
" We conclude that self-injection with a combination of papaverine and phentolamine is an efficient and safe long-term treatment for erectile dysfunction."( [Effectiveness and safety of cavernous body auto-injection therapy with papaverine/phentolamine. Study group].
Hartmann, U; Thon, WF, 1993
)
0.74
" phentolamine administration is safe in patients with neuropathic pain."( The safety of intravenous phentolamine administration in patients with neuropathic pain.
Bourke, DL; Cameron, LB; Raja, SN; Shir, Y, 1993
)
1.5
"The adverse effects of vacuum therapy and intracavernous self-injection in patients on warfarin do not exceed the rate in the general urological population."( Minimally invasive therapies in the treatment of erectile dysfunction in anticoagulated cases: a study of satisfaction and safety.
Donatucci, CF; Henderson, D; Limoge, JP; Olins, E, 1996
)
0.29
" Thus, there is no evidence for direct toxic effects of norepinephrine in micromolar concentration on isolated cardiomyocytes of guinea-pigs."( Studies of the toxic effects of norepinephrine on isolated cardiomyocytes of guinea-pigs.
Biederbick, W; Klaus, W; Koch, AE; Rump, AF; Schierholz, J, 2001
)
0.31
" The combination of papaverine with either PGE(1) or phentolamine had a cumulative toxic effect, and maximal toxicity (70%) was observed with the triple combination."( Vasoactive agents induce cytotoxicity in cultured human penile smooth muscle cells.
Monga, M; Pagnon, V; Rajasekaran, M, 2002
)
0.56
" Studies have shown that sildenafil may not be effective in all patients, and has been associated with a variety of adverse effects and an adverse interaction with nitrates and inhibitors of cytochrome P450 enzymes."( Combination therapy for erectile dysfunction: a randomized, double blind, unblinded active-controlled, cross-over study of the pharmacodynamics and safety of combined oral formulations of apomorphine hydrochloride, phentolamine mesylate and papaverine hyd
Castaneda, J; Castell, R; Hurley, D; Lammers, PI; Lipezker, M; Loehr, LA; Lowrey, F; Ponce de Leon, R; Rubio-Aurioles, E, 2002
)
0.5
" Most adverse events were mild or moderate in severity and consistent with the known pharmacodynamic properties of phentolamine."( Long-term safety and efficacy of oral phentolamine mesylate (Vasomax) in men with mild to moderate erectile dysfunction.
Auerbach, S; Coogan, C; Goldstein, I; Klimberg, I; Lammers, P; Padma-Nathan, H, 2002
)
0.8
" The most common adverse events included rhinitis, headache, tachycardia, and nausea, with a higher frequency reported in patients receiving phentolamine than sildenafil (41% vs 33%), with the exception of headache, which was reported more frequently in sildenafil users."( Comparison of the efficacy and safety of sildenafil citrate (Viagra) and oral phentolamine for the treatment of erectile dysfunction.
Hurtado-Coll, A; Ugarte, F, 2002
)
0.74
" Endoluminal norepinephrine is safe in pigs and may be useful under endoscopy of the pyeloureter."( Endoluminal norepinephrine inhibits smooth muscle activity of the pig pyeloureter by stimulation of beta-adrenoceptors without side effects.
Andreasen, F; Holst, U; Jakobsen, JS; Mortensen, J, 2008
)
0.35
"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
"Though uncommon, medical emergencies in the dental office are harrowing occurrences that can be the result of adverse drug reactions."( Pharmacological Reversal Agents in Dental Practice: Keys to Patient Safety.
Donaldson, M; Goodchild, JH,
)
0.13
" They investigated time to recovery of normal sensation and function and the frequency of adverse events (AEs)."( Effectiveness and safety of phentolamine mesylate in routine dental care.
Daubländer, M; Kürzinger, ML; Liebaug, F; Niedeggen, G; Theobald, K, 2017
)
0.75
"There were no severe complications reported in any of the included studies, but the occurrence of adverse events (mild and moderate) was greater in the phentolamine mesylate group compared to the control group."( Safety profile of phentolamine mesylate as reversal agent of pulpal and soft tissue dental anesthesia: a systematic review and meta-analysis.
Kamatham, R; Vinnakota, DN, 2019
)
1.05
"Scoping review with the objective of describing the adverse effects related to the administration of norepinephrine through short peripheral venous access and the characteristics of drug administration in patients hospitalized in ICU, surgery, and emergency services."( Adverse effects related with norepinephrine through short peripheral venous access: Scoping review.
Arteaga-Noriega, A; Bedoya, OA; García-Uribe, J; Gutiérrez-Vargas, J; Lopera-Jaramillo, D,
)
0.13
"The main adverse effect was extravasation, no additional complications occurred, phentolamine and terbutaline seem to be useful, and its availability is a necessity."( Adverse effects related with norepinephrine through short peripheral venous access: Scoping review.
Arteaga-Noriega, A; Bedoya, OA; García-Uribe, J; Gutiérrez-Vargas, J; Lopera-Jaramillo, D,
)
0.36

Pharmacokinetics

Pharmacokinetic parameters estimated for phentolamine, lidocaine, and epinephrine included peak plasma concentration. This fully validated method was successfully applied to the pharmacokinetic study after oral administration of 60 mg phentlamine to 20 healthy male volunteers.

ExcerptReferenceRelevance
" Pharmacokinetic parameters estimated for phentolamine, lidocaine, and epinephrine included peak plasma concentration (Cmax), time to peak plasma concentration (Tmax), area under the plasma concentration-time curve from 0 to the last time point (AUClast) or from time 0 to infinity (AUCinf), elimination half-life (t1/2), clearance (CL), and volume of distribution (Vd)."( Pharmacokinetics of lidocaine with epinephrine following local anesthesia reversal with phentolamine mesylate.
Goodson, JM; Hersh, EV; Moore, PA; Navalta, L; Papas, AS; Rogy, S; Rutherford, B; Yagiela, JA, 2008
)
0.83
" This fully validated method was successfully applied to the pharmacokinetic study after oral administration of 60 mg phentolamine to 20 Chinese healthy male volunteers."( UPLC-MS/MS determination of phentolamine in human plasma and its application to a pharmacokinetic study.
Kan, X; Zheng, SL; Zhou, CY, 2014
)
0.91

Compound-Compound Interactions

Magnesium sulfate combined with phentolamine and nifedipine has a better therapeutic effect on gestational hypertension.

ExcerptReferenceRelevance
"We performed a double-blind, crossover study using objective measurements to compare maximum rigidity and duration of erections with papaverine hydrochloride in combination with phentolamine mesylate and/or prostaglandin E1."( Objective double-blind evaluation of erectile function with intracorporeal papaverine in combination with phentolamine and/or prostaglandin E1.
Allen, RP; Brendler, CB; Engel, RM; Smolev, JK, 1992
)
0.69
"This experimental study was aimed at the effect of phentolamine used separately or in combination with pituitrin on hepatic and systemic hemodynamics in cirrhotic portal hypertensive dogs."( [Effect of phentolamine in combination with pituitrin on the hepatic and systemic hemodynamics].
Dan, Z, 1990
)
0.92
" This vasoactive drug combination has been used in 116 patients for diagnostic testing and subsequent treatment."( An improved vasoactive drug combination for a pharmacological erection program.
Barada, JH; Bennett, AH; Carpenter, AJ, 1991
)
0.28
" prostaglandin E1 in combination with papaverine (although the difference is not statistically significant)."( Intracavernous injection of prostaglandin E1 in combination with papaverine: enhanced effectiveness in comparison with papaverine plus phentolamine and prostaglandin E1 alone.
Floth, A; Schramek, P, 1991
)
0.48
"5 mmol/liter per kg body weight intravenously) combined with stimulation of bilateral ansae subclaviae in anesthetized dogs were examined."( Prostaglandin modulation of early afterdepolarizations and ventricular tachyarrhythmias induced by cesium chloride combined with efferent cardiac sympathetic stimulation in dogs.
Miyazaki, T; Pride, HP; Zipes, DP, 1990
)
0.28
" While intracavernosal VIP alone produced disappointing penile responses, its combination with papaverine potentiated the response to this drug, probably by increasing venous outflow resistance."( Penile response to intracavernosal vasoactive intestinal polypeptide alone and in combination with other vasoactive agents.
Bloom, SR; Kiely, EA; Williams, G, 1989
)
0.28
" Anesthesia was maintained with thoracic epidural anesthesia combined with light general anesthesia using NLA technique."( [The effects of thoracic epidural anesthesia combined with phentolamine infusion in a patient with low left ventricular ejection fraction undergoing resection of aortic abdominal aneurysm].
Arai, M; Kato, S; Takenaka, T, 1997
)
0.54
" The purpose of the present study was to investigate whether the use of nicardipine (Nc) and phentolamine (Ph) in combination with NE could ameliorate the adverse vasoconstrictive action of NE."( Hemodynamic effects of nicardipine and phentolamine in combination with norepinephrine in a canine low-output-state model.
Hashiyada, H; Kugimiya, T; Miyagawa, N; Shibata, R; Takagi, M; Yamada, T; Yamauchi, H, 1997
)
0.79
" Patients were treated with sildenafil citrate alone or in combination with intracavernosal injection therapy."( Treatment of intracorporeal injection nonresponse with sildenafil alone or in combination with triple agent intracorporeal injection therapy.
Johnson, H; McMahon, CG; Samali, R, 1999
)
0.3
" Sildenafil in combination with intracavernosal injection is associated with a 33% incidence of adverse effects, including a 20% incidence of dizziness."( Treatment of intracorporeal injection nonresponse with sildenafil alone or in combination with triple agent intracorporeal injection therapy.
Johnson, H; McMahon, CG; Samali, R, 1999
)
0.3
"To evaluate which vasoactive agents have synergistic effects on the cavernosal smooth muscles of rabbits and rats when the agents are combined with sildenafil."( Synergistic effects of sildenafil on relaxation of rabbit and rat cavernosal smooth muscles when combined with various vasoactive agents.
Jun, IO; Kim, SC; Lee, MY; Oh, MM; Seo, KK, 2001
)
0.31
" There was significant synergism on rabbit cavernosal smooth muscle when the sildenafil was combined with forskolin, sodium nitroprusside, VIP or phentolamine."( Synergistic effects of sildenafil on relaxation of rabbit and rat cavernosal smooth muscles when combined with various vasoactive agents.
Jun, IO; Kim, SC; Lee, MY; Oh, MM; Seo, KK, 2001
)
0.51
"To study the effect of urapidil combined with phentolamine in the management of hypertension during extracorporeal circulation."( [Effect of urapidil combined with phentolamine on hypertension during extracorporeal circulation].
Chen, B; Liu, Y; Tu, F; Wang, F, 2014
)
0.94
"Urapidil combined with phentolamine can control hypertension during extracorporeal circulation without causing hypotension."( [Effect of urapidil combined with phentolamine on hypertension during extracorporeal circulation].
Chen, B; Liu, Y; Tu, F; Wang, F, 2014
)
0.99
"To investigate the effect of magnesium sulfate combined with phentolamine and nifedipine for the treatment of gestational hypertension and on the levels of serum LIF and Apelin."( Effect of Magnesium Sulfate Combined with Phentolamine and Nifedipine for Gestational Hypertension and Serum Levels of LIF and Apelin.
Li, X; Wen, J, 2019
)
1.02
"Magnesium sulfate combined with phentolamine and nifedipine has a better therapeutic effect on gestational hypertension, which can effectively regulate the levels of serum LIF and Apelin and improve pregnancy outcomes."( Effect of Magnesium Sulfate Combined with Phentolamine and Nifedipine for Gestational Hypertension and Serum Levels of LIF and Apelin.
Li, X; Wen, J, 2019
)
1.06
"To observe the effect and mechanism of alpha-adrenergic receptor inhibitor phentolamine (PTL) in a rabbit model of acute pulmonary embolism (APE) combined with shock."( Effects and related mechanism of alpha-adrenergic receptor inhibitor phentolamine in a rabbit model of acute pulmonary embolism combined with shock.
Gu, Y; Hu, L; Qiu, L; Wang, Y; Yu, D; Yu, Y, 2022
)
1.19
"Twenty-four New Zealand rabbits were randomly divided into sham operation group (S group, n = 8), model group (M group, n = 8) and PTL group (n = 8), the model of APE combined with shock was established."( Effects and related mechanism of alpha-adrenergic receptor inhibitor phentolamine in a rabbit model of acute pulmonary embolism combined with shock.
Gu, Y; Hu, L; Qiu, L; Wang, Y; Yu, D; Yu, Y, 2022
)
0.96

Bioavailability

ExcerptReferenceRelevance
" Net water absorption rate was largely unaffected by intestinal vasodilatation."( The effect of vasodilatation and sympathetic nerve activation on net water absorption in the cat's small intestine.
Brunsson, I; Eklund, S; Jodal, M; Lundgren, O; Sjövall, H, 1979
)
0.26
"The aim of the study was to test the hypothesis that the sympathetic nerves to the jejunum enhance net fluid absorption rate by inhibiting an electrogenic flux of anions into the lumen."( Electrogenic and electroneutral components of the sympathetic effect on fluid absorption in the rat jejunum.
Butcher, P; Hemlin, M; Sjövall, H, 1987
)
0.27
" In the present experiments, 33 ketamine-anesthetized Sprague-Dawley rats were exposed to 2450-MHz microwaves at an average power density of 60 mW/sq cm (whole-body average specific absorption rate of approximately 14 W/kg) until death occurred."( Microwave-induced lethal heat stress: effects of phentolamine, prazosin and metoprolol.
Berger, RE; Chang, KS; Frei, MR; Jauchem, JR, 1995
)
0.55
" These results suggest that regular aerobic exercise training enhances NO bioavailability in middle-aged and older adults and that basal limb blood flow does not change with exercise training because of the contrasting influences of sympathetic nervous system activity and endothelium-derived vasodilation on the vasculature."( Systemic alpha-adrenergic and nitric oxide inhibition on basal limb blood flow: effects of endurance training in middle-aged and older adults.
Hayashi, K; Komine, H; Maeda, S; Miyauchi, T; Otsuki, T; Shimojo, N; Sugawara, J; Tanaka, H; Yokoi, T; Yoshizawa, M, 2007
)
0.34
" Combining of xanthone with piperazine moiety resulted in obtaining of compounds with increased bioavailability after oral administration."( Synthesis and evaluation of pharmacological properties of some new xanthone derivatives with piperazine moiety.
Bojarski, AJ; Gunia, A; Marona, H; Pytka, K; Satała, G; Siwek, A; Szkaradek, N; Szneler, E; Waszkielewicz, AM, 2013
)
0.39
"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

Isolated rings (circular preparations) obtained from rat thoracic aortae responded to increasing concentrations of NE with dose-dependent tonic enhancement. In the presence of phentolamine (10(-6) M), the dose-response curve to 5-HT was shifted to the right, the pA2 value for this antagonism was 6.

ExcerptRelevanceReference
"4-fold shift to the right in the dose-response curve to norepinephrine."( Potassium release from the rat submaxillary gland in vitro. I. Induction by catecholamines.
Giles, M; Martinez, JR; Quissell, DO, 1976
)
0.26
" For this purpose dose-response relations of seven sympathomimetic amines were compared under the influence of alpha- and/or beta-adrenolytic drugs."( alpha-Adrenoceptors mediating positive inotropic effects on the ventricular myocardium: some aspects of structure-activity relationship of sympathomimetic amines.
Endoh, M; Hillen, B; Krappitz, N; Schümann, HJ, 1976
)
0.26
" Propranolol shifted the dose-response curves downward and to the right for all agonists; phentolamine, shifter the curves upward and to the left."( Effects of adrenergic amines on electrophysiological properties and automaticity of neonatal and adult canine Purkinje fibers: evidence for alpha- and beta-adrenergic actions.
Danilo, P; Hordof, AJ; Ilvento, JP; Rosen, MR, 1977
)
0.48
" 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
" 3 Log dose-response curves of noradrenaline induced increases in systolic and diastolic pressure 20 min after intravenous phentolamine were shifted to the right in a parallel manner compared with the curves before phentolamine administration."( Circulatory and alpha-adrenoceptor blocking effects of phentolamine.
Prichard, BN; Richards, DA; Woodings, EP, 1978
)
0.71
", total dose) did not modify the dose-response curve to 5-HT except for the lowest dose."( Analysis of the contractile effect of 5-hydroxytryptamine on the isolated posterior communicating artery of the cat.
Gómez, B; Lluch, S; Marco, EJ; Marín, J; Salaices, M, 1979
)
0.26
" Maximum dosage administered to the heart in situ led to a resistance decrease to about 60%, equivalent to an elevation of conductance to about 170%."( On the range of alpha-adrenergic regulation of coronary vascular resistance.
Ertl, G; Lochner, W; Steinke, E; Wichmann, J,
)
0.13
" In vitro dose-response curves to gastrin I, CCK, and the octapeptide of CCK (OP) demonstrated that both CCK and OP were partial agonists on the LES muscle."( Mechanism of cholecystokinin inhibition of lower esophageal sphincter pressure.
Cohen, S; DiMarino, AJ; Fisher, RS, 1975
)
0.25
"2 mg/kg) of apomorphine reduced locomotion in a dose-dependent manner, while the reduction after higher doses was less pronounced, indicating a biphasic dose-response relationship."( Catecholamine receptor agonists: effects on motor activity and rate of tyrosine hydroxylation in mouse brain.
Strömbom, U, 1976
)
0.26
" Furthermore the dose-response relationships for increases of cAMP and of developed tension elicited by phenylephrine were determined."( Relationship between the level of cAMP and the contractile force under stimulation of alpha- and beta-adrenoceptors by phenylephrine in the isolated rabbit papillary muscle.
Brodde, OE; Endoh, M; Schümann, HJ, 1976
)
0.26
" The dose-response curve for dopamine was not affected by the antagonists pimozide (10(-6) M), yohimbine (10(-5) M) pindolol (3 x 10(-8) M) and phentolamine (10(-6) M) when these agents were given separately."( No evidence for involvement of dopaminergic receptors in the positive inotropic action of dopamine on the isolated rabbit papillary muscle.
Brodde, OE; Motomura, S; Schümann, HJ, 1978
)
0.46
" A dose-response relationship between the changes in renin release and cyclic AMP content was not observed."( Effect of norepinephrine on renin release and the cyclic AMP content of rat kidney slices: modification by sodium deficiency and alpha-adrenergic blockade.
Ganong, WF; Lopez, GA; Reid, IA; Rose, JC, 1978
)
0.26
"3 Propranolol caused a parallel shift to the right of the noradrenaline dose-response curve which was not changed by phentolamine."( alpha And beta-adrenoceptors in the detrusor muscle and bladder base of the pig and beta-adrenoceptors in the detrusor muscle of man.
Larsen, JJ, 1979
)
0.47
" Dose-response lines for all the compounds except clonidine were parallel."( Comparison of pre-junctional alpha-adrenoceptors at the neuromuscular junction with vascular post-junctional alpha-receptors in cat skeletal muscle.
Malta, E; McPherson, GA; Raper, C, 1979
)
0.26
"0 Hz, the log dose-response curve for the positive inotropic effect of epinine was displaced to the left, whereas the maximum of the developed tension was not changed."( Studies on the mechanism of the positive inotropic action evoked by epinine on the rabbit isolated papillary muscle at different rates of beating.
Brodde, OE; Motomura, S; Schümann, HJ,
)
0.13
"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
"Cumulative dose-response curves to angiotensin II were performed on helical strips from canine lateral saphenous vein."( Unusual venoconstrictor effects of angiotensin II.
Goldberg, MR; Hyman, AL; Joiner, PD; Kadowitz, PJ, 1975
)
0.25
" All three agents diminished vascular resistance and lowered blood pressure, although they differed in the intensity of their effects (NP greater than PH = GTN) and in the steepness of their dose-response curves (NP greater than PH greater than GTN)."( Comparison of the cardiovascular effects of phentolamine, sodium nitroprusside and nitroglycerin in anaesthetized cats (comparison of vasodilators).
Hoffmann, A; Meier, M,
)
0.39
" This may have been mediated by vascular alpha-adrenoceptors because log dose-response curves of saralasin-induced increases in systolic pressure were shifted to the right in a parallel fashion after phentolamine."( The pressor actions of noradrenaline, angiotensin II and saralasin in chronic autonomic failure treated with fludrocortisone.
Bannester, R; Davies, B; Sever, P; Wilcox, C, 1979
)
0.45
" The specific therapy can then be effectively and safely delivered by a careful analysis of the dose-response relation as identified by hemodynamic monitoring."( Contributions of hemodynamic monitoring to the treatment of chronic congestive heart failure.
Armstrong, PW, 1979
)
0.26
"5 mg/kg, 24 h prior to the experiment) the dose-response curve was not significantly affected by haloperidol, a dopamine vascular receptor antagonist (10(-6)-3X10(-6) M)."( Studies on the positive inotropic effect of dopamine in the guinea-pig heart.
Ledda, F; Maccioni, T; Mantelli, L; Mugelli, A; Torrini, M, 1977
)
0.26
" Propranolol (10(-8) and 10(-7) M) produced a parallel shift to the right in the log dose-response curves of ethylephrine with no decrease in the maximal response, indicating that the antagonism was competitive."( Positive inotropic effect of ethylephrine on the isolated rat atria.
Aramendía, P; Márquez, MT; Puntoni de Mikulić, LE, 1977
)
0.26
" The alpha-adrenergic blocker, phentolamine, shifted the dose-response curve upward and to the left and enhanced the hyperpolarization of RAF."( Alpha and beta adrenergic effects on human atrial specialized conducting fibers.
Bowman, FO; Hordof, AJ; Malm, JR; Mary-Rabine, L; Rosen, MR, 1978
)
0.54
" Pretreatment of animals with reserpine or treatment of tissues with an alpha-adrenoceptor blocking agent failed to alter the dose-response relationship for ATP."( The postjunctional effects and neural release of purine compounds in the guinea-pig vas deferens.
Rowe, JN; Stitzel, RE; Westfall, DP, 1978
)
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
"In human adipose tissue in vitro, dose-response curves were followed for different adrenomimetics releasing free fatty acids and glycerol into an albumin-containing medium."( Some adrenomimetic drugs affecting lipolysis in human adipose tissue in vitro.
Kuhn, E; Wenke, M; Wenkeová, J, 1976
)
0.26
" While 3 to 100 mg/kg of TRH reduced pentobarbital sleeping time when administered prior to the barbiturate, a dose-response relationship to TRH could not be established."( Effects of thyrotropin-releasing hormone (TRH) on the actions of pentobarbital and other centrally acting drugs.
Breese, GR; Cooper, BR; Cott, JM; Lipton, MA; Plotnikoff, NP; Prange, AJ, 1975
)
0.25
"47-fold shift to the left in the dose-response curve to norepinephrine and carbachol, respectively, after pretreatment with reserpine."( Potassium release from the rat submaxillary gland in vitro. III. Effects of pretreatment with reserpine.
Martinez, JR, 1977
)
0.26
" 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
)
0.55
" The average fall in mean arterial pressure for each dosage of hydralazine was no different with or without propranolol, even though propranolol inhibited rises in plasma renin activity and pulse due to hydralazine."( Synergistic effects of hydralazine and alpha- or beta-adrenergic blockers: the role of plasma renin activity.
Chin, BK; Das, B; Gutkin, M; Mezey, K; Modlinger, RS,
)
0.13
"5 Hz, the dose-response curve for phenylephrine via alpha-adrenoceptors was shifted to the left (delta pD2-0."( Influence of temperature and frequency on the positive inotropic action of phenylephrine in the isolated rabbit papillary muscle.
Endoh, M; Hillen, B; Schümann, HJ, 1977
)
0.26
" Both drugs also shift to the left the dose-response curves for noradrenaline and adrenaline on isolated strips, cocaine being most potent."( Uptake and release of catecholamines in sympathetic nerve fibres in the spleen of the cod, Gadus morhua.
Holmgren, S; Nilsson, S, 1976
)
0.26
" The distribution of experimental points suggested a sigmoidal dose-response curve."( Effect of environmental temperature on glucose-induced insulin response in the newborn rat.
Assan, R; Gilbert, M; Girard, JR; Jost, A; Kervran, A, 1976
)
0.26
" Dose-response curves for noradrenaline, 5-HT and ergotamine were established without and after a 30 min incubation with phentolamine or pizotifen."( Evidence for stimulation of 5-HT receptors in canine saphenous arteries by ergotamine.
Müller-Schweinitzer, E, 1976
)
0.46
" Droperidol induced a dose-dependent shift of the noradrenaline dose-response curve to the right, but proved to be 20 times less potent than phentolamine."( Effects of droperidol on cardiovascular adrenoceptors.
Göthert, M; Thies, FK; Veth, N, 1976
)
0.46
"The development of a suitable formulation and a freeze-dry cycle for a pharmaceutical dosage form requires knowledge of some basic properties such as (1) eutectic temperature, if one exists, (2) temperature effect on solubility, (3) degree of supercooling, (4) heat transfer properties of the frozen product and (5) equipment design and equipment capability."( Research and development of phamaceutical dosage forms.
DeLuca, PP, 1976
)
0.26
" The dose-response curve for phenylephrine was markedly shifted to the right by raising the temperature (pD2=0."( Influence of temperature on the positive inotropic effects mediated by alpha-and-beta-adrenoceptors in the isolated rabbit papillary muscle.
Endoh, M; Schümann, HJ; Wagner, J, 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
)
0.25
" In dose-response studies on the aortic strip, trans-metanicotine was significantly less active than nicotine."( Nicotine-like actions of cis-metanicotine and trans-metanicotine.
Bowman, ER; Chang, RS; McKennis, H; Wilson, KL, 1976
)
0.26
"Regional blood volumes (Vb), unstressed volumes (V0), blood flow distribution, venous compliances (Cv), venous resistances (Rv), and time constants of drainage (tau v) were determined in dogs anesthetized with alpha-chloralose at carotid sinus pressures (Pcs) of 50 and 200 mmHg and dosed with alpha-adrenergic or ganglionic blockade at a Pcs of 50 mmHg."( Baroreflex control of regional capacitance and blood flow distribution with or without alpha-adrenergic blockade.
Deschamps, A; Magder, S, 1992
)
0.28
" Dose-response curves for phentolamine and propranolol established maximally effective doses (3."( Influence of sympatho-adrenal system on insulin sensitivity using the euglycemic clamp technique.
Funado, T; Iguchi, A; Iida, T; Kato, K; Kusunoki, M; Oshida, Y; Sakamoto, N; Sato, Y; Suga, T, 1992
)
0.58
" E1-PG dosage varied from 10 to 40 mcg based on diagnosis, and was readjusted in 6 of the 9 patients which in the initial tests had not obtained sufficient erection, therefore bringing about a final 91."( [Prospective study of the effectiveness and side effects of intracavernous prostaglandin E1 versus papaverine or papaverine phentolamine in the diagnosis and treatment of erection dysfunction. Review of the literature].
Alvarez González, E; Chandeck Montesa, K; Chen Jiménez, J; Rodríguez Antolín, A; Tamayo, JC, 1992
)
0.49
" Cells were held at 0 mV and BRL 38227 was added cumulatively to construct a dose-response relationship."( Effects of BRL 38227 on potassium currents in smooth muscle cells isolated from rabbit portal vein and human mesenteric artery.
Aaronson, PI; Russell, SN; Smirnov, SV, 1992
)
0.28
" In control aortic rings the dose-response curves for either clonidine or naphazoline were biphasic, consisting of high- and low-affinity components."( Interaction of imidazolines with alkylation-sensitive and -resistant alpha-1 adrenoceptor subtypes.
Piascik, MT; Pruitt, TA; Sparks, MS, 1991
)
0.28
" A portable home nocturnal tumescence monitor classification of severity of sexual dysfunction provided a guideline for the intracavernous pharmacological injection initial dosage and the probability of success or failure in patients who desire this form of therapy for male sexual dysfunction."( Classification of sexual dysfunction for management of intracavernous medication-induced erections.
Fein, RL, 1990
)
0.28
" The enhanced attenuation of responses to noxious colorectal distension produced by the coadministration of these drugs is evidenced by significant leftward shifts in the dose-response curves as compared to those of each drug alone and by isobolographic analysis."( Intrathecal coadministration of clonidine with serotonin receptor agonists produces supra-additive visceral antinociception in the rat.
Danzebrink, RM; Gebhart, GF, 1991
)
0.28
" Dose-response curves for IT morphine were obtained in the presence of fixed doses (0."( Interaction of intrathecal morphine and ST-91 on antinociception in the rat: dose-response analysis, antagonism and clearance.
Monasky, MS; Stevens, CW; Yaksh, TL; Zinsmeister, AR, 1990
)
0.28
" In I, four cumulative noradrenaline (NA) dose-response curves (10(-9) to 10(-3) M) were constructed."( Reversal of alpha-adrenoceptor blockade by propranolol in isolated rat pulmonary artery.
Abdelrahman, A; Nguyen, H; Pang, CC, 1990
)
0.28
" However, the dose-response curves to phentolamine and the alpha-2 adrenoceptor agonist UK 14,304 on stimulus-induced overflow from the kidney were not significantly different after NE treatment."( Effects of chronic norepinephrine administration on sympathetic neurotransmission in the isolated perfused rat kidney.
Eikenburg, DC, 1990
)
0.55
" In potassium loaded, ureter-ligated dogs, heparin increases transmembrane potassium transfer as effectively as does a dosage of atropine large enough to cross the blood-brain barrier and its influence on potassium transfer, like that of atropine, is suppressed by beta-adrenoreceptor blockade."( Heparin mediates transmembrane potassium transfer in hyperkalemic dogs.
Hiatt, JR; Hiatt, N, 1990
)
0.28
" After exact dosage adjustment the danger of drug-induced priapism is low."( [Priapism following intracavernous injection of vasoactive substances as a urologic emergency].
Papadopoulos, I; Wand, H; Weichert-Jacobsen, K, 1990
)
0.28
" The dosage of phentolamine mesylate-papaverin hydrochloride injection required was determined in each patient individually."( [Corpus cavernosum autoinjection therapy: initial experiences in erectile dysfunction].
Altwein, JE; Bähren, W; Gall, H; Gallwitz, A; Scherb, W; Stief, CG, 1986
)
0.62
" To minimize complications, careful selection of candidates, cautious dosage determination, and thorough instruction on injection technique are mandatory."( Vasoactive intracavernous pharmacotherapy.
Sidi, AA, 1988
)
0.27
" Furthermore, a chemical prosthesis is suitable mainly for the treatment of impotence due to diabetes, by adjusting the dosage and administration."( [Diagnosis and treatment of impotence with administration of chemical prosthesis using real-time mechanical sector duplex scanner--with special reference to diabetic patients].
Kaneda, S; Matsuoka, K; Nakajima, Y; Shibayama, T; Suzuki, Y; Yamamoto, H, 1989
)
0.28
" The high dosage regimen (10 mg/kg per dose) of phentolamine or idazoxan that had been found to be hepatoprotective in earlier studies potentiated this hypothermia and more than doubled the net decrease in core body temperature experienced by the animals."( Antagonism of bromobenzene-induced hepatotoxicity by the alpha-adrenoreceptor blocking agents phentolamine and idazoxan: role of hypothermia.
Harbison, RD; James, RC; Kerger, BD; Roberts, SM, 1989
)
0.75
" Clonidine also produced biphasic effects on blood pressure in conscious rats, with the dose-response function shifted upward and to the left of that observed in anesthetized rats."( Pharmacological characterization of alpha adrenoceptors involved in the antinociceptive and cardiovascular effects of intrathecally administered clonidine.
Brody, MJ; Gebhart, GF; Solomon, RE, 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
" In contrast to agonist affinity, phentolamine affinity, determined from Schild-plot analysis, was not different from controls, even for the highest daily dosage of verapamil."( Effects of chronic treatment with verapamil on adrenoceptor-mediated contraction of rabbit aorta.
Aceto, JF; Tallarida, RJ,
)
0.41
" The doses for each drug were selected based on the results of dose-response curves."( Adrenergic effects on internal cardiac defibrillation threshold.
Jones, DL; Klein, GJ; Rattes, MF; Sharma, AD; Szabo, T, 1987
)
0.27
" Denervation caused a shift to the left of the 86Rb efflux dose-response curve to carbachol and phenylephrine (3."( Effect of parasympathetic denervation on K+ release by rat parotid slices.
Adham, N; Templeton, D, 1987
)
0.27
"0 mg/kg intravenously) was administered after the highest phenylephrine infusion dosage to assure complete beta-blockade."( In vivo demonstration of maturational changes of the chronotropic response to alpha-adrenergic stimulation.
Gelband, H; McCormack, J; Pickoff, AS; Stolfi, A; Villafañe, J; Xu, H, 1988
)
0.27
" Phentolamine effected a partial dose-related inhibition of flow reductions; however, prazosin and yohimbine, given separately or in combination, failed to produce any significant effect despite an alpha-blocking action equivalent to or greater than that of phentolamine (alpha-agonist dose-response studies)."( Influence of alpha-adrenergic blockade on platelet-mediated thrombosis in stenosed canine coronary arteries.
Bolli, R; Brandon, TA; Mace, ML; Weibaecher, DG, 1985
)
1.18
" The thrombin dose-response relationship was complex and did not have a classic sigmoidal shape, whether the endothelium was functional or not."( Alpha adrenoceptor antagonists selectively reduce thrombin-stimulated contraction in rabbit arteries.
Bevan, JA; Garland, CJ, 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
)
0.27
" Its dose-response curve was shifted to the right at 23 degrees C/0."( B-HT 920 and B-HT 958: presynaptic effects on electrically evoked 3H-dopamine release from slices of rat nucleus accumbens.
Cichini, G; Placheta, P; Singer, EA, 1987
)
0.27
"5 ml/kg dosage of bromobenzene."( Antagonism of bromobenzene-induced hepatotoxicity by the alpha-adrenergic blocking agents, phentolamine and idazoxan.
Bucci, TJ; Gandy, J; Harbison, RD; James, RC; Kerger, BD; Roberts, SM, 1988
)
0.5
" In the first series of experiments cumulative dose-response curves for propranolol, atenolol and ICI 118,551, nonselective beta-, beta 1- and beta 2-selective antagonists, respectively, were constructed in rats subjected to a continuous intravenous infusion of phentolamine."( Pressor response to beta 1- and beta 2-blockers in conscious rats treated with phentolamine.
King, KA; Pang, CC; Tabrizchi, R, 1988
)
0.68
" Tityustoxin caused a slight leftward shift of the dose-response curves to adrenaline and norepinephrine and a large potentiation of the frequency-response curves to electrical stimulation."( Effects of tityustoxin on the rat isolated tail artery.
Catanzaro, OL; Savino, EA, 1985
)
0.27
" Dose-response curves were determined for either isoproterenol or dobutamine 30 min after treatment with hexamethonium (20mg/kg)."( Role of alpha-adrenergic receptors in the intrinsic inotropic selectivity of dobutamine in anesthetized dogs.
Gorczynski, RJ; Shaffer, JE, 1985
)
0.27
" HA-1004 shifted the dose-response curve for CaCl2 to the right in a competitive manner in depolarized rabbit renal arterial strips."( Relaxation of vascular smooth muscle by HA-1004, an inhibitor of cyclic nucleotide-dependent protein kinase.
Hidaka, H; Inagaki, M; Ishikawa, T; Watanabe, M, 1985
)
0.27
" After chronic withdrawal of TSH from the growth medium, the magnitude of the response to NE is considerably reduced; however, there is no substantial shift in the dose-response curve."( Norepinephrine and thyroid-stimulating hormone induce inositol phosphate accumulation in FRTL-5 cells.
Alling, DW; Bone, EA; Grollman, EF, 1986
)
0.27
"1% respectively; the dose-response curve for NE inhibitory action is described."( Quantitative evaluation of alpha- and beta-adrenoceptor modulation of [3H]choline release in guinea pig superior cervical ganglia.
Belluzzi, O; Bonifazzi, C; Perri, V; Travagli, RA, 1987
)
0.27
" At this dosage prostaglandin E1 was most effective in inducing artificial penile erection (11 of 12 patients)."( Efficiency and side effects of prostaglandin E1 in the treatment of erectile dysfunction.
Schramek, P; Waldhauser, M, 1988
)
0.27
" The dose-response curves for norepinephrine and prazosin on glycogen synthase were well correlated with those on diacylglycerol."( Regulation of hepatic glycogen phosphorylase and glycogen synthase by calcium and diacylglycerol.
Bouscarel, B; Exton, JH, 1986
)
0.27
" Isolated rings (circular preparations) obtained from rat thoracic aortae responded to increasing concentrations of NE with dose-dependent tonic enhancement, not significantly affected by the presence of indomethacin (10(-6)M); whereas, preincubation with phentolamine (10(-6)M), yohimbine (10(-7)M) or prazosin (10(-8)M), shifted significantly to the right points of the positive inotropic dose-response curve for NE."( Possible prostacyclin involvement on disparate tonic responses to "in vitro" norepinephrine in circular and in longitudinal preparations from rat thoracic aorta.
Chaud, M; Franchi, AM; Gimeno, AL; Gimeno, MA, 1987
)
0.45
" Two patients who failed to achieve erections had the lowest penile brachial index values and 1 in whom priapism developed had the highest value, indicating that this may be a useful technique to determine the initial dosage of the injection."( Pharmacological treatment of erectile dysfunction after radical prostatectomy.
Dennis, RL; McDougal, WS, 1988
)
0.27
" For each agent tested in this study, dose-response curves were established."( Micturition in the unanesthetized rat: spinal vs. peripheral pharmacology of the adrenergic system.
Durant, PA; Lucas, PC; Yaksh, TL, 1988
)
0.27
" Intravenously administered PGE2 at a five times higher dosage failed to significantly alter net water and electrolyte fluxes."( Central nervous system influence of prostaglandin E2 on jejunal water and electrolyte transport in conscious dogs.
Bueno, L; Primi, MP, 1986
)
0.27
" The dose-response curve to vasopressin and its maximal effect measured on stimulation of glucose production were unchanged in thyroidectomized rats."( Hormonal control of glucose production and pyruvate kinase activity in isolated rat liver cells: influence of hypothyroidism.
Beylot, M; Comte, B; Khalfallah, Y; Laville, M; Riou, JP; Vidal, H, 1987
)
0.27
" Dose-response curves to serotonin were not altered in the high potassium medium whereas those to adrenaline displayed slight changes."( Responses of potassium-depolarized rat tail arteries to adrenaline and serotonin.
Polidoro, JH; Savino, EA, 1987
)
0.27
" The dose-response curve for morphine (i."( Central and systemic morphine-induced antinociception in mice: contribution of descending serotonergic and noradrenergic pathways.
Wigdor, S; Wilcox, GL, 1987
)
0.27
" When the doses of NPY was changed, a dose-response relation was found (n = 4)."( Vasoconstrictor effect of neuropeptide Y (NPY) on canine coronary artery.
Aizawa, Y; Funazaki, T; Hayashi, M; Ito, S; Murata, M; Shibata, A, 1985
)
0.27
" No long-lasting effect of the alpha-adrenergic blocker was apparent since the response to norepinephrine was not altered following a 1-hour washout of phentolamine after the isoproterenol dose-response curve."( Phentolamine and rat aortic smooth muscle responsiveness to potassium chloride, isoproterenol and norepinephrine.
Katovich, MJ; Soltis, EE, 1985
)
1.91
"75 to 750 pM) of alpha-thrombin prior to contracting in response to higher concentrations during cumulative dose-response experiments."( Thrombin-elicited contractile responses of aortic smooth muscle.
Aiken, M; Anderson, GF; Ciaglowski, RE; Fenton, JW; Walz, DA, 1985
)
0.27
" 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
"3 A second cannabis extract (II) with a different ratio of cannabinoids (also administered in dosage equivalent to 10 mg Delta(9)-THC/kg) failed to affect pentobarbitone anaesthesia in mice."( Interaction of cannabis and general anaesthetic agents in mice.
Chesher, GB; Jackson, DM; Starmer, GA, 1974
)
0.25
" A study of dose-response relationships suggests a competitive interaction between MJ 1999 and DMAB."( Beta-adrenoceptor stimulating properties of para-dimethylaminobenzaldehyde.
Ghouri, MS; Shibata, S, 1970
)
0.25
" 6) In the presence of cocaine, the dose-response curves plotted from the mechanical activity induced by excess [K]o or by noradrenaline shifted to the left and the maximum responses evoked by either treatment were enhanced."( Effects of cocaine on a hypogastric nerve-vas deferens preparation of the guinea pig.
Hashiguchi, T; Ito, Y; Kuriyama, H, 1974
)
0.25
"The dopamine alpha- and beta-adrenoceptor dose-response curves are investigated in four patients who are exempt from cardiovascular disease."( The use of low doses of dopamine in intensive care medicine.
D'Orio, V; el Allaf, D; Juchmès, J; Marcelle, R, 1984
)
0.27
" The dose-response curve for propranolol inhibition of 125I-hydroxybenzylpindolol binding duplicated that reported for its physiologic action."( Beta receptor occupancy. Assessment in the intact animal.
Homcy, CJ; Kopiwoda, S; Strauss, HW, 1980
)
0.26
" Prazosin (PRZ), a selective alpha 1-receptor blocker, inhibited preferentially the positive phase of the inotropic response and displaced the dose-response curve of PE to the right in nanomolar concentrations, indicating a competitive mechanism of inhibition."( Competitive blockade of alpha-adrenergic receptors in rat heart by prazosin.
Osnes, JB; Oye, I; Skomedal, T, 1980
)
0.26
" Furthermore, at the end of the 52-day chronic dosing period tiodazosin caused appreciably less alpha-adrenergic receptor antagonist activity than prazosin as assessed by the norepinephrine dose-pressor response profiles."( Effects of tiodazosin, praxosin, trimazosin and phentolamine on blood pressure, heart rate and on pre- and postsynaptic alpha-adrenergic receptors in the rat.
Buyniski, JP; Campbell, JA; Pircio, AW; Schurig, JE, 1980
)
0.52
" Continuous intra-aortic infusion of phentolamine produced a dose-response decrease in uterine activity and blood flow."( Effect of adrenergic blockade on dynamics of the pregnant primate uterus (Macaca mulatta).
Harbert, GM; Spisso, KR, 1981
)
0.54
" Presynaptic alpha-adrenoceptor antagonist activity was assessed by studying the effect of increasing concentrations of the antagonists on cumulative clonidine dose-response curves on the stimulated vas deferens."( [Comparative study of the pre and post-synaptic alpha blocking activity of thymoxamine and its metabolites in the rat vas deferens (author's transl)].
Canellas, J; Demichel, P; Malek, A; Roquebert, J,
)
0.13
" 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
" Atropine blocked the pressor responses to norepinephrine and shifted the dose-response curve for norepinephrine to the right to a similar extent in spontaneously hypertensive and Wistar-Kyoto rats."( Studies on the hypotensive response to atropine in hypertensive rats.
Abraham, S; Cantor, EH; Spector, S, 1981
)
0.26
" GB converted the negative chronotropic effect to positive chronotropic action but had no effect on the inotropic dose-response relation."( Cardiovascular pharmacology of ASL-7022. II. Mechanisms of inotropic selectivity.
Gorczynski, RJ; Wroble, RW, 1982
)
0.26
" The dose-response curve to guanfacine for increase in blood pressure was shifted in a parallel fashion to the right by 1 mg/kg of yohimbine, an alpha 2-antagonist and by 1 mg/kg of phentolamine, a nonselective alpha 1- and alpha 2-antagonist."( [Effects of guanfacine on pre- and postsynaptic alpha-adrenoceptors studied in comparison with those of clonidine].
Chin, W; Imai, S; Nakagawa, Y, 1982
)
0.46
" Pre-treatment of the rats with syrosingopine shifted the dose-response curve to the left (enhancement) while combined propranolol (800 micrograms/kg) and phentolamine (800 micrograms/kg) shifted the dose-response curve to the right (depression)."( Rat endometrial bioelectric activity in vivo and in vitro: effects of adrenaline.
Levin, RJ; Phillips, JC, 1983
)
0.46
" Shifts in the (-)-noradrenaline dose-response curve produced by BE2254 and prazosin were parallel and there was no significant effect on the observed maximal response."( Competitive antagonism of alpha 1-adrenoceptor mediated pressor responses in the rat mesenteric artery.
Coupar, IM; McPherson, GA; Taylor, DA, 1984
)
0.27
" However, POB shifted the dose-response curve for NAT induction by norepinephrine (NE) to the left."( Modulation of rat pineal acetyl-Co A:arylamine N-acetyltransferase induction by alpha adrenergic drugs.
Alphs, L; Lovenberg, W, 1984
)
0.27
" The dose-response curve for alpha-methylnorepinephrine in the presence of prazosin, using Hofstee's plots, revealed alpha 1- and alpha 2-adrenoceptors, respective proportions being 80."( Postjunctional alpha-adrenoceptors. Alpha 1 and alpha 2 subtypes in rat vasculature in vitro and in vivo.
Decker, N; Ehrhardt, JD; Leclerc, G; Schwartz, J, 1984
)
0.27
" SCH 19927 produced a competitive alpha 1- and beta 1-blockade in vitro as indicated by the parallel shift to the right of the dose-response curves for norepinephrine and isoprenaline, respectively."( Effects of the R, R-isomer of labetalol, SCH 19927, in isolated tissues and in spontaneously hypertensive rats during a repeated treatment.
Bamonte, F; Forlani, A; Monopoli, A; Ongini, E; Parravicini, L, 1984
)
0.27
" Alpha-blockade was confirmed by alpha-agonist dose-response studies."( Effect of alpha-adrenergic blockade on arrhythmias induced by acute myocardial ischemia and reperfusion in the dog.
Bolli, R; Fisher, DJ; Miller, RR; Taylor, AA; Young, JB, 1984
)
0.27
" In both preparations only the combined application of phentolamine (10(-6) M) and pindolol (3 X 10(-8) M) shifted the entire dose-response curves for the positive inotropic effect of dopamine to the right, while either antagonist used separately had no effect."( The mode of direct action of dopamine on the rabbit heart.
Brodde, OE; Inui, J; Motomura, S; Schümann, HJ,
)
0.38
" An equihypotensive dosage of the alpha 1-adrenoceptor blocking agent prazosin (1."( Alpha-adrenoceptor blockade by phentolamine causes beta-adrenergic vasodilation by increased catecholamine release due to presynaptic alpha-blockade.
Bassenge, E; Holtz, J; Saeed, M; Sommer, O,
)
0.42
"5 In rats with a sustained tachycardia (100 beats/min produced by electrical stimulation of the spinal cord) both mianserin and phentolamine, in contrast to desipramine, shifted the clonidine heart rate dose-response curve to the right."( Comparison of mianserin with desipramine, maprotiline and phentolamine on cardiac presynaptic and vascular postsynaptic alpha-adrenoceptors and noradrenaline reuptake in pithed normotensive rats.
Cavero, I; Gomeni, R; Lefèvre-Borg, F; Roach, AG, 1980
)
0.71
" To measure affinity, dose-response curves were first obtained for agonist alone and then for agonist in the presence of various concentrations of phentolamine, a reversible alpha-adrenergic antagonist."( The effect of preload on the dissociation constant of phentolamine in isolated rabbit thoracic aorta.
Raffa, RB; Tallarida, RJ, 1981
)
0.71
" There was a shift to the left in pressor dose-response curves to the alpha 1-adrenoreceptor agonist phenylephrine and the mixed alpha 1/alpha 2-adrenoreceptor agonist noradrenaline in 6-hydroxydopamine-pretreated animals."( The effects of intravenous 6-hydroxydopamine on peripheral alpha-adrenoreceptors.
Hamilton, CA; Reid, JL, 1982
)
0.26
" For this purpose, dose-response curves for isoproterenol before and after addition of propranolol (5 X 10(-9) to 10(-6) M) or phentolamine (10(-6) M) to the bath were determined."( [Analysis of the contraction induced by isoproterenol in isolated cerebral and femoral arteries of cat].
Marín, J; Salaices, M, 1982
)
0.47
" 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
)
0.27
" But the dose-response curve for Ca2+ in the presence of A23187 (3 X 10(-5) M), a Ca ionophore, was not affected at all by verapamil (10(-6) M)."( Contractile response of the rabbit aorta to maitotoxin, the most potent marine toxin.
Ohizumi, Y; Yasumoto, T, 1983
)
0.27
" The dose-response curve for ATP-induced contraction was shifted to the right by theophylline."( Effect of apamin and theophylline on adenosine-5'-triphosphate-induced response of the guinea pig gallbladder.
Ishikawa, Y; Takahashi, T; Yamamura, T, 1983
)
0.27
" Prazosin (a preferential alpha 1-antagonist) inhibited the dose-response curves to noradrenaline and phenylephrine 100 and 1000-times respectively more effectively than either phentolamine or rauwolscine (a preferential alpha 2-antagonist)."( Pharmacological characterization of alpha-adrenoreceptor subtypes in rat isolated thoracic aorta.
Charlton, KG; Clarke, DE; Hamed, AT; Johnson, TD, 1983
)
0.46
" Conventional measurements of maximum isometric force and dose-response relations for l-phenylephrine in strips of ascending aorta in vitro were followed by radioligand studies on homogenates made from the same strips."( Relation between alpha adrenergic receptor occupation and contractile response: radioligand and physiologic studies in canine aorta.
Griendling, KK; Milnor, WR; Rusher, MM; Sastre, A, 1984
)
0.27
" Agonist-antagonist interactions were studied by pretreating the vessels with methysergide, ketanserin and phentolamine and then establishing the dose-response curves to 5-HT or noradrenaline (NA)."( Tryptaminergic receptors in the bovine pulmonary vasculature: effects of ketanserin.
Eyre, P; Ogunbiyi, PO, 1984
)
0.48
" Full PH dose-response curves for standard antihypertensive drugs were explored and were compared to their hypotensive dose-response curves."( Antihypertensive drugs: their postural hypotensive effect and their blood pressure lowering activity in conscious normotensive rats.
Carver, LA; Lee, CH; Strosberg, AM, 1983
)
0.27
" Following control measurements of Pm and arteriolar and venular dimensions, dose-response curves of arteriolar and venular dimensions to topical norepinephrine (10(-10) M to 10(-3) M) was obtained."( Microvascular responses to E. coli endotoxin with altered adrenergic activity.
Baker, CH; Wilmoth, FR, 1984
)
0.27
" Acid and pepsin secretion were inhibited in dose-response manner by dopamine in innervated mucosa, but all other effects of the compounds were different in parietal cells and chief cells and in vagally innervated and denervated mucosa."( Dopaminergic and adrenergic influence on gastric acid and pepsin secretion stimulated by food. The role of vagal innervation.
Berstad, A; Guldvog, I; Linnestad, P; Schrumpf, E, 1984
)
0.27
" The beta 1,2 antagonist employed in the test decreased the contrast dosage by 13 per cent, causing the LD50."( Diazepam, alpha and beta neurotransmission modifying drugs and contrast media mortality in mice.
Johansson, G; Luostarinen, M; Virkkunen, P, 1984
)
0.27
" In cases in which methysergide induced vasoconstriction, the dose-response curves were bell-shaped and the constriction became smaller with large doses."( Responses of isolated canine intermediate auricular arteries to 5-hydroxytryptamine and methysergide.
Chiba, S; Ito, T, 1984
)
0.27
" Moreover, in vitro cumulative dose-response curves for the contractile effect of these three PGs, on identical oviductal segments, were constructed."( Role of endogenous and exogenous prostaglandins on the contractile functioning of isolated sow (Sus scrofa) oviducts.
Chaud, M; Franchi, AM; Gimeno, AL; Gimeno, MF; Gonzalez, ET; Viggiano, M, 1984
)
0.27
" In cerebral arteries, the dose-response curve for serotonin was shifted to the right and downward by treatment with cinanserin, whereas in femoral and mesenteric arteries, the curves were shifted to the right."( Analysis of the contractile response to serotonin and tryptamine of isolated dog cerebral, femoral and mesenteric arteries.
Fu, LH; Toda, N, 1983
)
0.27
" The adrenaline-stimulated water flux exhibited a linear dose-response curve up to an adrenaline dosage of 750 micrograms kg-1; wt."( Cholinergic and adrenergic effects on diffusional water flux in the toadfish, Opsanus beta.
Evans, DH; Oduleye, SO, 1983
)
0.27
" Dose-response curves obtained by infusing Ca2+ (2-8 mg X min-1 X kg-1) were identical in N and Db."( Enhanced sensitivity of diabetic hearts to alpha-adrenoceptor stimulation.
Downing, SE; Fripp, RR; Lee, JC, 1983
)
0.27
" The dose-response curve for Phe was markedly shifted to the left by papaverine in 6W rats, but slightly in 7M rats."( Age-dependent differences in the positive inotropic effect of phenylephrine on rat isolated atria.
Hashimoto, H; Nakashima, M; Sugino, N, 1983
)
0.27
" The dose-response curve for the stimulating effect of neostigmine on saliva production was shifted to the right in borderline hypertensive as compared with normotensive subjects."( Studies of salivary flow in borderline hypertension: effects of drugs acting on structures innervated by the autonomic nervous system.
Rahn, KH; Schols, M; van Baak, MA; van Hooff, M, 1984
)
0.27
" The constant perfusate flow also allows cumulative dose-response curves to be constructed, even for powerful vasoconstrictor agents."( Application of the isolated perfused rat liver preparation to pharmacological studies of the intrahepatic portal vascular bed.
Bhathal, PS; Grossman, HJ, 1984
)
0.27
" Phentolamine produced parallel shift of the dose-response curves both for arteries and veins."( Analysis of vasospasm in hand arteries by in vitro pharmacology, hand angiography and finger plethysmography.
Arneklo-Nobin, B; Edvinsson, L; Eklöf, B; Haffajee, D; Owman, C; Thylén, U, 1983
)
1.18
" AM was not able to cause contraction of strips obtained from dogs pretreated with reserpine; phentolamine shifted the dose-response curve of AM to the right."( On the mechanism of action of amezinium methylsulphate on the dog saphenous vein.
Araújo, D; Caramona, MM; Osswald, W, 1983
)
0.48
" 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
)
0.5
" Trifluoperazine significantly inhibited glycogenolytic effect of phenylephrine and angiotensin II by lowering maximal response, and that of vasopressin by shifting the dose-response curve to the right, while alpha-antagonist phentolamine was inhibitory only to phenylephrine."( Inhibition by trifluoperazine of glycogenolytic effects of phenylephrine, vasopressin, and angiotensin II.
Kimura, S; Koide, Y; Kugai, N; Tada, R; Yamashita, K, 1982
)
0.45
" In aortic strip preparations, Wu-Chu-Yu caused the increase of contractile force, and the dose-response curve was parallel shift to the right in the presence of phentolamine."( In vivo and in vitro studies on the mechanism of cardiovascular effects of Wu-Chu-Yu (Evodiae fructus).
Chen, CF; Chen, SM; Chow, SY; Lin, MT, 1981
)
0.46
" The chronotropic dose-response curves were made in both spontaneously beating atria while inotropic effects were derived from left atria driven at 1 Hz, 5 msec and voltage about 20 percent above threshold."( Interactions between sympathomimetic agonists and blocking agents: cardiac effects of phenylephrine and isoproterenol.
Aramendía, P; Márquez, MT; Mikulić, LE,
)
0.13
" The dose-response curve showed a tendency to plateau at concentrations above 5 x 10(-5) M, with a maximal constriction of 28."( The response of feline spinal pial arterioles to norepinephrine.
Crawford, RA; Gregory, PC; Griffiths, IR, 1980
)
0.26
" Lidoncaine, 5 x 10(-4) M, and MEGX, 2 x 10(-3) M, shifted the dose-response curve of NE to the right, whereas GX, 5 x 10(-4) M, shifted the curve to the left."( Modifications by lidocaine and its N-dealkylated metabolites of the response of the isolated rabbit aorta to transmural electrical stimulation.
Fukuda, S; Takeshita, H; Toda, N, 1980
)
0.26
" Dose-response curves obtained for carbachol and isoproterenol indicated that the maximum response to carbachol is greater than that to isoproterenol but that the threshold for response to isoproterenol is much lower than that to carbachol."( Autonomic control of lacrimal protein secretion.
Bromberg, BB, 1981
)
0.26
" Dose-response curves were plotted for all measured variables, and males and females were compared to identify potential gender differences."( Role of alpha-adrenoceptors in the maintenance of core temperature in humans.
Afifi, O; el-Gamal, N; Frank, SM; Raja, SN; Wu, PK, 1995
)
0.29
" The peptides produced dose-related increases in perfusion pressure, and dose-response curves to all six peptides were parallel."( Analysis of responses to angiotensin peptides in the hindquarters vascular bed of the cat.
Garrison, EA; Kadowitz, PJ; Osei, SY; Santiago, JA, 1995
)
0.29
") was used in all experiments except the dose-response relationship study."( Role of the sympathoadrenal axis in the cardiovascular response to cocaine in conscious unrestrained rats.
Chen, BX; Myles, J; Wilkerson, RD, 1995
)
0.29
" Techniques of injection, dosing and followup are discussed."( Experience with intracavernosal tri-mixture for the management of neurogenic erectile dysfunction.
Chao, R; Clowers, DE, 1994
)
0.29
" NA increased mucociliary activity at a dosage of 10(-5) mol/kg, the maximal increase being 16."( The effect of noradrenaline on mucociliary activity in the rabbit maxillary sinus.
Cervin, A; Lindberg, S; Mercke, U, 1993
)
0.29
" We describe the procedure to establish the dosage for home use and discuss the implications of the low dosages relative to previous reports."( Intracavernous pharmacotherapy for impotence: selection of appropriate agent and dose.
Donatucci, CF; Kaula, N; Lue, TF; von Heyden, B, 1993
)
0.29
" At the lowest dose studied (20 microgram/kg iv), the inhibitory effects of candesartan were competitive, whereas at the highest dose (100 microgram/kg iv) the dose-response curve for angiotensin II was shifted to the right in a nonparallel manner with inhibitory effects that could not be surmounted."( Role of AT(1) receptors and autonomic nervous system in mediating acute pressor responses to ANG II in anesthetized mice.
Bivalacqua, TJ; Champion, HC; Dalal, A; Kadowitz, PJ, 1999
)
0.3
" This progressive method of treatment enabled us to select the optimal dosage and combinations of compounds in 441/452 patients (97."( [Evaluation of 452 patients with erectile dysfunction treated by combinations of vasoactive agents by penile injection].
Baniel, J; Israilov, S; Livne, P; Segenreich, E; Shmueli, J; Simon, D, 1998
)
0.3
" In separate groups of animals, dose-response curves for increases in diastolic pressure produced by phenylephrine were generated after the administration of saline (control), ouabain (18 microg/kg), L-omega-N-nitro arginine methyl ester (L-NAME, 3 micromol/kg) and angiotensin II (15 ng/kg per min)."( Acute pressor actions of ouabain do not enhance the actions of phenylephrine or norepinephrine in anesthetized rats.
Barker, LA; Rossoni, LV; Vassallo, DV, 2001
)
0.31
" There is a strong dose-response relationship in maximum plasma concentration (Cmax) and area under the curve (AUC), and there are no clear age-related differences in absorption or elimination rates."( Vasomax for the treatment of male erectile dysfunction.
Carson, C; Goldstein, I; Islam, A; Rosen, R, 2001
)
0.31
" Previously others have suggested that repeat dosing with vasoactive medication may improve the diagnostic accuracy of vascular testing."( Improving the accuracy of vascular testing in impotent men: correcting hemodynamic alterations using a vasoactive medication re-dosing schedule.
Abdel-Moneim, A; Abobakr, R; Goldstein, I; Mulhall, JP, 2001
)
0.31
" However, it is also known to accumulate in various tissues up to several times higher after standard oral dosing and we now have evidence from both in vivo and in vitro experiments with spontaneously hypertensive rats (SHR) that millimolar levels stimulate release of norepinephrine (NE) from vascular sympathetic nerve endings (SNEs)."( A possible indirect sympathomimetic action of metformin in the arterial vessel wall of spontanously hypertensive rats.
Lee, JM; Peuler, JD, 2001
)
0.31
" These results indicate that factors that can influence alpha-adrenergic receptors may be critical in assessing dose-response data used in the risk assessment process."( Activation of alpha(1)-adrenergic receptors potentiates the nephrotoxicity of ethylene dibromide.
Banasik, M; Harbison, RD; Mosquera, DI; Muro-Cacho, C; Stedeford, T, 2003
)
0.32
" The dosage of sildenafil and phentolamine was respectively 50-100 mg and 40 mg."( [Assessment of curative effect on erectile dysfunction of two drugs].
Jiao, Y; Ma, XN; Yang, DZ; Yu, ZJ, 2003
)
0.61
" A decline in mean arterial pressure was observed in both groups with increasing dosage of phentolamine."( Preserved alpha-adrenergic tone in the leg vascular bed of spinal cord-injured individuals.
Hopman, MT; Kooijman, M; Rongen, GA; Smits, P, 2003
)
0.54
"Patients received four cumulative dosage steps of phentolamine (0."( Obstructive apneic events induce alpha-receptor mediated digital vasoconstriction.
Eder, DN; Grote, L; Hedner, J; Peker, Y; Zou, D, 2004
)
0.58
" Systemic exposure as measured by plasma drug concentration increased with dose and duration of dosing and slight drug accumulation occurred, particularly in high-dose males."( Development of hibernomas in rats dosed with phentolamine mesylate during the 24-month carcinogenicity study.
Auletta, C; Berardi, MR; Bolte, H; Halliwell, W; Hartman, B; Poulet, FM,
)
0.39
" We set out to evaluate the impact of varying the ingredient dosage on response and short-term safety of Tx compared with PgE1."( A prospective randomized study to optimize the dosage of trimix ingredients and compare its efficacy and safety with prostaglandin E1.
Akhras, AA; Mohamed, K; Rashwan, H; Seyam, R,
)
0.13
" The stimulation parameters in all but dose-response sessions included a frequency of 20 ppm, pulse width of 200 ms, and amplitude of 3 mA."( Anal electrical stimulation with long pulses increases anal sphincter pressure in conscious dogs.
Chen, JD; Nie, Y; Pasricha, JP, 2006
)
0.33
" However, the dose-response curve of noradrenaline was shifted to the left when the strip preparation was treated with aldosterone (1 x 10(-5)M) for 20 min before administering noradrenaline."( Effect of aldosterone on isolated human penile corpus cavernosum tissue.
Anzai, H; Kagawa, J; Kanayama, HO; Kawanishi, Y; Kishimoto, T; Kojima, K; Muguruma, H; Numata, A; Sugiyama, H; Tanimoto, S; Yamanaka, M, 2008
)
0.35
" Because PM had not been approved previously for submucosal administration, 2 Good Laboratory Practices (GLP) studies in dogs designed to investigate systemic toxicity and the local effects of single and repeated dosing of OraVerse on the inferior alveolar nerve and branches of the superior alveolar nerve and adjacent soft tissues after local administration were conducted."( Local and systemic toxicity of intraoral submucosal injections of phentolamine mesylate (OraVerse).
Rutherford, B; Thake, D; Zeller, JR, 2009
)
0.59
" Due to inappropriate dosage adjustment, however, outpatient phenoxybenzamine therapy did not achieve adequate α-adrenergic-receptor blockade; during the laparoscopic resection procedure, the woman developed severe hypertension, leading to cardiac arrest and discontinuation of the operation."( Phentolamine continuous infusion in a patient with pheochromocytoma.
Charash, WE; Christian, RC; McMillian, WD; Trombley, BJ, 2011
)
1.81
" 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
" In the PGE1-only group, the maintenance dosage was significantly correlated with preoperative sexual function and nerve sparing (NS) (P<0."( Experience with intracavernous injection in the treatment of erectile dysfunction after radical prostatectomy: dose considerations.
Cha, TL; Chuang, FP; Lakin, M; Montague, DK; Sun, GH; Wu, ST,
)
0.13
" Here we use these as case studies to emphasize the importance of informed drug target selection, the early evaluation of dose-response relationships in human studies, and the value of the deep phenotyping of patients in clinical studies to better understand inter-individual variation in patient response."( Why drugs fail in clinical trials in pulmonary arterial hypertension, and strategies to succeed in the future.
Attard, M; Ghataorhe, P; Lythgoe, MP; Rhodes, CJ; Wharton, J; Wilkins, MR, 2016
)
0.43
" There is relatively poor clinician knowledge surrounding adrenaline reversal and a lack of easily accessible information available about dosing and drug location within the hospital."( Adrenaline auto-injector injuries: Practical considerations in emergency management in a tertiary hand surgery unit.
Ellis, K; McCaughran, PW; Mosahebi, A; Nikkhah, D; Southall, C; Zargaran, D, 2023
)
0.91
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
alpha-adrenergic antagonistAn agent that binds to but does not activate alpha-adrenergic receptors thereby blocking the actions of endogenous or exogenous alpha-adrenergic agonists. alpha-Adrenergic antagonists are used in the treatment of hypertension, vasospasm, peripheral vascular disease, shock, and pheochromocytoma.
vasodilator agentA drug used to cause dilation of the blood vessels.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (4)

ClassDescription
imidazolesA five-membered organic heterocycle containing two nitrogen atoms at positions 1 and 3, or any of its derivatives; compounds containing an imidazole skeleton.
phenolsOrganic aromatic compounds having one or more hydroxy groups attached to a benzene or other arene ring.
tertiary amino compoundA compound formally derived from ammonia by replacing three hydrogen atoms by organyl groups.
substituted aniline
[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 (67)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency31.62280.003245.467312,589.2998AID2517
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency89.12510.631035.7641100.0000AID504339
ClpPBacillus subtilisPotency22.38721.995322.673039.8107AID651965
phosphopantetheinyl transferaseBacillus subtilisPotency64.77570.141337.9142100.0000AID1490
ATAD5 protein, partialHomo sapiens (human)Potency29.08100.004110.890331.5287AID493107
GLS proteinHomo sapiens (human)Potency11.90470.35487.935539.8107AID624146; AID624170
TDP1 proteinHomo sapiens (human)Potency31.91780.000811.382244.6684AID686978; AID686979
GLI family zinc finger 3Homo sapiens (human)Potency13.33320.000714.592883.7951AID1259369; AID1259392
regulator of G-protein signaling 4Homo sapiens (human)Potency0.75190.531815.435837.6858AID504845
EWS/FLI fusion proteinHomo sapiens (human)Potency15.72210.001310.157742.8575AID1259253; AID1259256
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency6.74000.000214.376460.0339AID720691
cytochrome P450 2D6Homo sapiens (human)Potency0.30900.00108.379861.1304AID1645840
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency79.43280.707936.904389.1251AID504333
arylsulfatase AHomo sapiens (human)Potency10.69101.069113.955137.9330AID720538
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency24.36160.035520.977089.1251AID504332
activating transcription factor 6Homo sapiens (human)Potency10.68220.143427.612159.8106AID1159516
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency0.79430.00207.533739.8107AID891
D(1A) dopamine receptorHomo sapiens (human)Potency8.60000.02245.944922.3872AID488982; AID488983
chromobox protein homolog 1Homo sapiens (human)Potency50.11870.006026.168889.1251AID488953
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency0.70790.01789.637444.6684AID588834
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency30.04740.000323.4451159.6830AID743065; AID743067
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency13.33220.000627.21521,122.0200AID743202
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency50.11870.050127.073689.1251AID588590
urokinase-type plasminogen activator precursorMus musculus (house mouse)Potency12.58930.15855.287912.5893AID540303
plasminogen precursorMus musculus (house mouse)Potency12.58930.15855.287912.5893AID540303
urokinase plasminogen activator surface receptor precursorMus musculus (house mouse)Potency12.58930.15855.287912.5893AID540303
lamin isoform A-delta10Homo sapiens (human)Potency5.01190.891312.067628.1838AID1487
Cellular tumor antigen p53Homo sapiens (human)Potency26.21780.002319.595674.0614AID651631; AID720552
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency10.00000.009610.525035.4813AID1479145
Ataxin-2Homo sapiens (human)Potency39.81070.011912.222168.7989AID588378
Chain A, Beta-lactamaseEscherichia coli K-12Potency17.78280.044717.8581100.0000AID485294
Chain A, Putative fructose-1,6-bisphosphate aldolaseGiardia intestinalisPotency17.74070.140911.194039.8107AID2451
glp-1 receptor, partialHomo sapiens (human)Potency31.62280.01846.806014.1254AID624417
phosphopantetheinyl transferaseBacillus subtilisPotency4.46680.141337.9142100.0000AID1490
ATAD5 protein, partialHomo sapiens (human)Potency29.09290.004110.890331.5287AID504467
GLS proteinHomo sapiens (human)Potency35.48130.35487.935539.8107AID624170
TDP1 proteinHomo sapiens (human)Potency9.12180.000811.382244.6684AID686978; AID686979
Microtubule-associated protein tauHomo sapiens (human)Potency19.95260.180013.557439.8107AID1460
chromobox protein homolog 1Homo sapiens (human)Potency89.12510.006026.168889.1251AID540317
[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)
estrogen receptor beta isoform 1Homo sapiens (human)IC50 (µMol)50.00001.91098.316518.7976AID733
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)IC50 (µMol)0.39600.00011.00768.7800AID625218
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)Ki0.20700.00000.887110.0000AID625218
Bile salt export pumpHomo sapiens (human)IC50 (µMol)1,000.00000.11007.190310.0000AID1443987; AID1449628
Alpha-2A adrenergic receptorHomo sapiens (human)IC50 (µMol)0.00600.00001.44217.3470AID625201
Alpha-2A adrenergic receptorHomo sapiens (human)Ki0.01350.00010.807410.0000AID254396; AID337883; AID35951; AID36190; AID625201
Cytochrome P450 2D6Homo sapiens (human)IC50 (µMol)10.00000.00002.015110.0000AID625249
Angiotensin-converting enzymeOryctolagus cuniculus (rabbit)IC50 (µMol)20.07630.00001.612910.0000AID625171
Angiotensin-converting enzymeOryctolagus cuniculus (rabbit)Ki16.44800.00042.03378.6606AID625171
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)0.03160.00021.874210.0000AID167198; AID33132; AID36170; AID36731; AID36851; AID36866
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)Ki0.01540.00010.949010.0000AID1353523; AID36637; AID37313; AID37454
Alpha-2B adrenergic receptorHomo sapiens (human)IC50 (µMol)0.01800.00001.23808.1590AID625202
Alpha-2B adrenergic receptorHomo sapiens (human)Ki0.01720.00020.725710.0000AID254397; AID36190; AID36231; AID625202
Alpha-1A adrenergic receptorBos taurus (cattle)Ki0.00380.00000.50723.7020AID36455; AID36466
Alpha-2C adrenergic receptorHomo sapiens (human)IC50 (µMol)0.11000.00001.47257.8980AID625203
Alpha-2C adrenergic receptorHomo sapiens (human)Ki0.02740.00030.483410.0000AID254398; AID36190; AID36408; AID625203
Alpha-1B adrenergic receptorMesocricetus auratus (golden hamster)Ki0.22000.00002.01679.6000AID37067
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)0.04920.00031.09147.7625AID219808; AID33132; AID36922
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)Ki0.02200.00000.929610.0000AID35187
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)0.04920.00031.09147.7625AID219808; AID33132; AID36922
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)Ki0.02200.00000.970810.0000AID35187
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)0.04920.00031.06917.7625AID219808; AID33132; AID36922
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)Ki0.01330.00000.937510.0000AID35187; AID36553
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)0.03160.00021.270410.0000AID167198; AID33132; AID36170; AID36731; AID36851; AID36866
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)Ki0.02140.00000.575110.0000AID1353523; AID35591; AID36637; AID37313; AID37454
Alpha-1D adrenergic receptorHomo sapiens (human)IC50 (µMol)0.01730.00020.75688.8970AID1229077; AID625200
Alpha-1D adrenergic receptorHomo sapiens (human)Ki0.01270.00000.360910.0000AID1229077; AID254395; AID625200
5-hydroxytryptamine receptor 2AHomo sapiens (human)IC50 (µMol)0.35900.00010.88018.8500AID625192
5-hydroxytryptamine receptor 2AHomo sapiens (human)Ki0.10300.00000.385510.0000AID625192
5-hydroxytryptamine receptor 2CHomo sapiens (human)IC50 (µMol)0.39600.00011.03029.0000AID625218
5-hydroxytryptamine receptor 2CHomo sapiens (human)Ki0.20700.00010.954910.0000AID625218
Alpha-1A adrenergic receptorHomo sapiens (human)IC50 (µMol)0.00110.00020.56145.4000AID1229075
Alpha-1A adrenergic receptorHomo sapiens (human)Ki0.00440.00000.272610.0000AID1229075; AID1380705; AID254386; AID36466
Histamine H1 receptorHomo sapiens (human)IC50 (µMol)316.22800.00000.44365.1768AID697786
Alpha-1B adrenergic receptorHomo sapiens (human)IC50 (µMol)0.01080.00020.65268.3300AID1229076
Alpha-1B adrenergic receptorHomo sapiens (human)Ki0.02610.00000.471310.0000AID1229076; AID254394
5-hydroxytryptamine receptor 2BHomo sapiens (human)IC50 (µMol)3.80700.00011.18738.9125AID625217
5-hydroxytryptamine receptor 2BHomo sapiens (human)Ki2.42200.00030.769310.0000AID625217
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)0.03160.00001.819410.0000AID167198; AID33132; AID36170; AID36731; AID36851; AID36866
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Ki0.01540.00000.965010.0000AID1353523; AID36637; AID37313; AID37454
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC50 (µMol)20.07630.00091.901410.0000AID625171
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)Ki16.44800.00211.840710.0000AID625171
Nuclear receptor subfamily 3 group C member 3 Bos taurus (cattle)IC50 (µMol)20.07630.10482.83988.3173AID625171
Nuclear receptor subfamily 3 group C member 3 Bos taurus (cattle)Ki16.44800.08582.95428.6606AID625171
Sigma non-opioid intracellular receptor 1Homo sapiens (human)IC50 (µMol)0.54950.00030.70285.3660AID203852
NischarinHomo sapiens (human)Ki0.01140.00420.21923.8019AID342861
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Hsf1 proteinMus musculus (house mouse)EC50 (µMol)195.00000.160024.4900236.5000AID2382
Alpha-1A adrenergic receptorOryctolagus cuniculus (rabbit)Kd0.00630.00020.01430.0501AID37056
Alpha-2A adrenergic receptorHomo sapiens (human)Kd0.00370.00370.16750.5754AID33124
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)EC50 (µMol)1.00000.00132.612925.7000AID36580
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)Kd0.02670.00020.52667.5858AID196984; AID33142; AID33143; AID35866; AID36640
Alpha-2B adrenergic receptorHomo sapiens (human)Kd0.00370.00370.16750.5754AID33124
Alpha-2C adrenergic receptorHomo sapiens (human)Kd0.00370.00370.16750.5754AID33124
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)EC50 (µMol)1.00000.02700.87933.0000AID36656
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)Kd0.05390.00020.62779.3325AID196987; AID33142; AID33143; AID35363; AID37056
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)EC50 (µMol)1.00000.02700.97093.0000AID36656
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)Kd0.05390.00020.62779.3325AID196987; AID33142; AID33143; AID35363; AID37056
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)EC50 (µMol)1.00000.02700.97093.0000AID36656
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)Kd0.05390.00020.62779.3325AID196987; AID33142; AID33143; AID35363; AID37056
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)EC50 (µMol)1.00000.00133.394625.7000AID36580
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)Kd0.02670.00020.89627.5858AID196984; AID33142; AID33143; AID35866; AID36640
Alpha-1D adrenergic receptorHomo sapiens (human)Kd0.00370.00000.19451.2882AID33124
Adenosine receptor A2aRattus norvegicus (Norway rat)Kd0.00600.00020.04910.3802AID33143
Alpha-1A adrenergic receptorHomo sapiens (human)Kd0.00370.00000.20481.2882AID33124
Alpha-1B adrenergic receptorHomo sapiens (human)Kd0.00540.00000.11991.2882AID33124; AID37056
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)EC50 (µMol)1.00000.00133.394625.7000AID36580
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Kd0.02670.00020.51397.5858AID196984; AID33142; AID33143; AID35866; AID36640
Beta-2 adrenergic receptorHomo sapiens (human)Kd10.00000.00000.62888.9130AID41321
Beta-1 adrenergic receptorHomo sapiens (human)Kd10.00000.00010.803910.0000AID41321
Beta-3 adrenergic receptorHomo sapiens (human)Kd10.00000.00010.76318.9130AID41321
Alpha-1D adrenergic receptorHomo sapiens (human)Kd0.01660.00000.19451.2882AID33122
Alpha-1A adrenergic receptorHomo sapiens (human)Kd0.01660.00000.20481.2882AID33122
Alpha-1B adrenergic receptorHomo sapiens (human)Kd0.01660.00000.11991.2882AID33122
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Alpha-2A adrenergic receptorHomo sapiens (human)Kb0.00700.00700.00700.0070AID36052
Alpha-2B adrenergic receptorHomo sapiens (human)Kb0.00700.00700.00700.0070AID36052
Alpha-2C adrenergic receptorHomo sapiens (human)Kb0.00700.00180.00440.0070AID36052
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)Kb0.01180.01180.30660.8800AID255429
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (367)

Processvia Protein(s)Taxonomy
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
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)
positive regulation of cytokine productionAlpha-2A adrenergic receptorHomo sapiens (human)
DNA replicationAlpha-2A adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
Ras protein signal transductionAlpha-2A adrenergic receptorHomo sapiens (human)
Rho protein signal transductionAlpha-2A adrenergic receptorHomo sapiens (human)
female pregnancyAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of cell population proliferationAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of norepinephrine secretionAlpha-2A adrenergic receptorHomo sapiens (human)
regulation of vasoconstrictionAlpha-2A adrenergic receptorHomo sapiens (human)
actin cytoskeleton organizationAlpha-2A adrenergic receptorHomo sapiens (human)
platelet activationAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of cell migrationAlpha-2A adrenergic receptorHomo sapiens (human)
activation of protein kinase activityAlpha-2A adrenergic receptorHomo sapiens (human)
activation of protein kinase B activityAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of epinephrine secretionAlpha-2A adrenergic receptorHomo sapiens (human)
cellular response to hormone stimulusAlpha-2A adrenergic receptorHomo sapiens (human)
receptor transactivationAlpha-2A adrenergic receptorHomo sapiens (human)
vasodilationAlpha-2A adrenergic receptorHomo sapiens (human)
glucose homeostasisAlpha-2A adrenergic receptorHomo sapiens (human)
fear responseAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of potassium ion transportAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of MAP kinase activityAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of epidermal growth factor receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of calcium ion-dependent exocytosisAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of insulin secretionAlpha-2A adrenergic receptorHomo sapiens (human)
intestinal absorptionAlpha-2A adrenergic receptorHomo sapiens (human)
thermoceptionAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of lipid catabolic processAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of membrane protein ectodomain proteolysisAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of calcium ion transportAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of insulin secretion involved in cellular response to glucose stimulusAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of uterine smooth muscle contractionAlpha-2A adrenergic receptorHomo sapiens (human)
adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-inhibiting adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
phospholipase C-activating adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of wound healingAlpha-2A adrenergic receptorHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of calcium ion transmembrane transporter activityAlpha-2A adrenergic receptorHomo sapiens (human)
xenobiotic metabolic processCytochrome P450 2D6Homo sapiens (human)
steroid metabolic processCytochrome P450 2D6Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2D6Homo sapiens (human)
estrogen metabolic processCytochrome P450 2D6Homo sapiens (human)
coumarin metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid catabolic processCytochrome P450 2D6Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2D6Homo sapiens (human)
isoquinoline alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2D6Homo sapiens (human)
retinol metabolic processCytochrome P450 2D6Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2D6Homo sapiens (human)
negative regulation of bindingCytochrome P450 2D6Homo sapiens (human)
oxidative demethylationCytochrome P450 2D6Homo sapiens (human)
negative regulation of cellular organofluorine metabolic processCytochrome P450 2D6Homo sapiens (human)
arachidonic acid metabolic processCytochrome P450 2D6Homo sapiens (human)
MAPK cascadeAlpha-2B adrenergic receptorHomo sapiens (human)
angiogenesisAlpha-2B adrenergic receptorHomo sapiens (human)
regulation of vascular associated smooth muscle contractionAlpha-2B adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-2B adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-2B adrenergic receptorHomo sapiens (human)
female pregnancyAlpha-2B adrenergic receptorHomo sapiens (human)
negative regulation of norepinephrine secretionAlpha-2B adrenergic receptorHomo sapiens (human)
platelet activationAlpha-2B adrenergic receptorHomo sapiens (human)
activation of protein kinase B activityAlpha-2B adrenergic receptorHomo sapiens (human)
negative regulation of epinephrine secretionAlpha-2B adrenergic receptorHomo sapiens (human)
receptor transactivationAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of neuron differentiationAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of blood pressureAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of uterine smooth muscle contractionAlpha-2B adrenergic receptorHomo sapiens (human)
adrenergic receptor signaling pathwayAlpha-2B adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-2B adrenergic receptorHomo sapiens (human)
regulation of vasoconstrictionAlpha-1A adrenergic receptorBos taurus (cattle)
positive regulation of MAPK cascadeAlpha-1A adrenergic receptorBos taurus (cattle)
regulation of cardiac muscle contractionAlpha-1A adrenergic receptorBos taurus (cattle)
regulation of smooth muscle contractionAlpha-2C adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-2C adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-2C adrenergic receptorHomo sapiens (human)
negative regulation of norepinephrine secretionAlpha-2C adrenergic receptorHomo sapiens (human)
regulation of vasoconstrictionAlpha-2C adrenergic receptorHomo sapiens (human)
platelet activationAlpha-2C adrenergic receptorHomo sapiens (human)
activation of protein kinase B activityAlpha-2C adrenergic receptorHomo sapiens (human)
negative regulation of epinephrine secretionAlpha-2C adrenergic receptorHomo sapiens (human)
receptor transactivationAlpha-2C adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-2C adrenergic receptorHomo sapiens (human)
positive regulation of neuron differentiationAlpha-2C adrenergic receptorHomo sapiens (human)
adrenergic receptor signaling pathwayAlpha-2C adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-2C adrenergic receptorHomo sapiens (human)
negative regulation of insulin secretionAlpha-2C adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of cell population proliferationAlpha-1D adrenergic receptorHomo sapiens (human)
neuron-glial cell signalingAlpha-1D adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-1D adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of vasoconstrictionAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-1D adrenergic receptorHomo sapiens (human)
temperature homeostasis5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cytokine production involved in immune response5-hydroxytryptamine receptor 2AHomo sapiens (human)
glycolytic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2AHomo sapiens (human)
activation of phospholipase C activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cytosolic calcium ion concentration5-hydroxytryptamine receptor 2AHomo sapiens (human)
memory5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cell population proliferation5-hydroxytryptamine receptor 2AHomo sapiens (human)
response to xenobiotic stimulus5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
regulation of dopamine secretion5-hydroxytryptamine receptor 2AHomo sapiens (human)
artery smooth muscle contraction5-hydroxytryptamine receptor 2AHomo sapiens (human)
urinary bladder smooth muscle contraction5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of heat generation5-hydroxytryptamine receptor 2AHomo sapiens (human)
negative regulation of potassium ion transport5-hydroxytryptamine receptor 2AHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transduction5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of neuron apoptotic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein localization to cytoskeleton5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of fat cell differentiation5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of glycolytic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of vasoconstriction5-hydroxytryptamine receptor 2AHomo sapiens (human)
symbiont entry into host cell5-hydroxytryptamine receptor 2AHomo sapiens (human)
sensitization5-hydroxytryptamine receptor 2AHomo sapiens (human)
behavioral response to cocaine5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of inflammatory response5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylation5-hydroxytryptamine receptor 2AHomo sapiens (human)
detection of temperature stimulus involved in sensory perception of pain5-hydroxytryptamine receptor 2AHomo sapiens (human)
detection of mechanical stimulus involved in sensory perception of pain5-hydroxytryptamine receptor 2AHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2AHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergic5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
presynaptic modulation of chemical synaptic transmission5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of execution phase of apoptosis5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of platelet aggregation5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of DNA biosynthetic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2AHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2AHomo sapiens (human)
behavioral fear response5-hydroxytryptamine receptor 2CHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2CHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
locomotory behavior5-hydroxytryptamine receptor 2CHomo sapiens (human)
feeding behavior5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2CHomo sapiens (human)
cGMP-mediated signaling5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of nervous system process5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of appetite5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of corticotropin-releasing hormone secretion5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of fat cell differentiation5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of calcium-mediated signaling5-hydroxytryptamine receptor 2CHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2CHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2CHomo sapiens (human)
MAPK cascadeAlpha-1A adrenergic receptorHomo sapiens (human)
negative regulation of heart rate involved in baroreceptor response to increased systemic arterial blood pressureAlpha-1A adrenergic receptorHomo sapiens (human)
norepinephrine-epinephrine vasoconstriction involved in regulation of systemic arterial blood pressureAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of heart rate by epinephrine-norepinephrineAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of the force of heart contraction by epinephrine-norepinephrineAlpha-1A adrenergic receptorHomo sapiens (human)
apoptotic processAlpha-1A adrenergic receptorHomo sapiens (human)
smooth muscle contractionAlpha-1A adrenergic receptorHomo sapiens (human)
signal transductionAlpha-1A adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-1A adrenergic receptorHomo sapiens (human)
activation of phospholipase C activityAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationAlpha-1A adrenergic receptorHomo sapiens (human)
adult heart developmentAlpha-1A adrenergic receptorHomo sapiens (human)
negative regulation of cell population proliferationAlpha-1A adrenergic receptorHomo sapiens (human)
response to xenobiotic stimulusAlpha-1A adrenergic receptorHomo sapiens (human)
response to hormoneAlpha-1A adrenergic receptorHomo sapiens (human)
negative regulation of autophagyAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of cardiac muscle hypertrophyAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of synaptic transmission, GABAergicAlpha-1A adrenergic receptorHomo sapiens (human)
intracellular signal transductionAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of action potentialAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of vasoconstrictionAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of smooth muscle contractionAlpha-1A adrenergic receptorHomo sapiens (human)
calcium ion transport into cytosolAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of cardiac muscle contractionAlpha-1A adrenergic receptorHomo sapiens (human)
cell growth involved in cardiac muscle cell developmentAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of protein kinase C signalingAlpha-1A adrenergic receptorHomo sapiens (human)
pilomotor reflexAlpha-1A adrenergic receptorHomo sapiens (human)
neuron-glial cell signalingAlpha-1A adrenergic receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayAlpha-1A adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-1A adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-1A adrenergic receptorHomo sapiens (human)
inflammatory responseHistamine H1 receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayHistamine H1 receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayHistamine H1 receptorHomo sapiens (human)
memoryHistamine H1 receptorHomo sapiens (human)
visual learningHistamine H1 receptorHomo sapiens (human)
regulation of vascular permeabilityHistamine H1 receptorHomo sapiens (human)
positive regulation of vasoconstrictionHistamine H1 receptorHomo sapiens (human)
regulation of synaptic plasticityHistamine H1 receptorHomo sapiens (human)
cellular response to histamineHistamine H1 receptorHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayHistamine H1 receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerHistamine H1 receptorHomo sapiens (human)
chemical synaptic transmissionHistamine H1 receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
regulation of vasoconstrictionAlpha-1B adrenergic receptorHomo sapiens (human)
intracellular signal transductionAlpha-1B adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-1B adrenergic receptorHomo sapiens (human)
regulation of cardiac muscle contractionAlpha-1B adrenergic receptorHomo sapiens (human)
neuron-glial cell signalingAlpha-1B adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-1B adrenergic receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationAlpha-1B adrenergic receptorHomo sapiens (human)
neural crest cell migration5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of cytokine production5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of endothelial cell proliferation5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled receptor internalization5-hydroxytryptamine receptor 2BHomo sapiens (human)
heart morphogenesis5-hydroxytryptamine receptor 2BHomo sapiens (human)
cardiac muscle hypertrophy5-hydroxytryptamine receptor 2BHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
activation of phospholipase C activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of cell population proliferation5-hydroxytryptamine receptor 2BHomo sapiens (human)
response to xenobiotic stimulus5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2BHomo sapiens (human)
neural crest cell differentiation5-hydroxytryptamine receptor 2BHomo sapiens (human)
intestine smooth muscle contraction5-hydroxytryptamine receptor 2BHomo sapiens (human)
phosphorylation5-hydroxytryptamine receptor 2BHomo sapiens (human)
calcium-mediated signaling5-hydroxytryptamine receptor 2BHomo sapiens (human)
cGMP-mediated signaling5-hydroxytryptamine receptor 2BHomo sapiens (human)
vasoconstriction5-hydroxytryptamine receptor 2BHomo sapiens (human)
negative regulation of apoptotic process5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of canonical NF-kappaB signal transduction5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of MAP kinase activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transduction5-hydroxytryptamine receptor 2BHomo sapiens (human)
embryonic morphogenesis5-hydroxytryptamine receptor 2BHomo sapiens (human)
regulation of behavior5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of nitric-oxide synthase activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of cell division5-hydroxytryptamine receptor 2BHomo sapiens (human)
ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2BHomo sapiens (human)
protein kinase C signaling5-hydroxytryptamine receptor 2BHomo sapiens (human)
cellular response to temperature stimulus5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2BHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2BHomo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by hormonePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion homeostasisPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cardiac muscle contractionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cellular response to xenobiotic stimulusPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane depolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion import across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of receptor internalizationAtaxin-2Homo sapiens (human)
regulation of translationAtaxin-2Homo sapiens (human)
RNA metabolic processAtaxin-2Homo sapiens (human)
P-body assemblyAtaxin-2Homo sapiens (human)
stress granule assemblyAtaxin-2Homo sapiens (human)
RNA transportAtaxin-2Homo sapiens (human)
lipid transportSigma non-opioid intracellular receptor 1Homo sapiens (human)
nervous system developmentSigma non-opioid intracellular receptor 1Homo sapiens (human)
G protein-coupled opioid receptor signaling pathwaySigma non-opioid intracellular receptor 1Homo sapiens (human)
regulation of neuron apoptotic processSigma non-opioid intracellular receptor 1Homo sapiens (human)
protein homotrimerizationSigma non-opioid intracellular receptor 1Homo sapiens (human)
apoptotic processNischarinHomo sapiens (human)
Rac protein signal transductionNischarinHomo sapiens (human)
actin cytoskeleton organizationNischarinHomo sapiens (human)
negative regulation of cell migrationNischarinHomo sapiens (human)
outer dynein arm assemblyNischarinHomo sapiens (human)
diet induced thermogenesisBeta-2 adrenergic receptorHomo sapiens (human)
regulation of sodium ion transportBeta-2 adrenergic receptorHomo sapiens (human)
transcription by RNA polymerase IIBeta-2 adrenergic receptorHomo sapiens (human)
receptor-mediated endocytosisBeta-2 adrenergic receptorHomo sapiens (human)
smooth muscle contractionBeta-2 adrenergic receptorHomo sapiens (human)
cell surface receptor signaling pathwayBeta-2 adrenergic receptorHomo sapiens (human)
activation of transmembrane receptor protein tyrosine kinase activityBeta-2 adrenergic receptorHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayBeta-2 adrenergic receptorHomo sapiens (human)
endosome to lysosome transportBeta-2 adrenergic receptorHomo sapiens (human)
response to coldBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of protein kinase A signalingBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of bone mineralizationBeta-2 adrenergic receptorHomo sapiens (human)
heat generationBeta-2 adrenergic receptorHomo sapiens (human)
negative regulation of multicellular organism growthBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeBeta-2 adrenergic receptorHomo sapiens (human)
bone resorptionBeta-2 adrenergic receptorHomo sapiens (human)
negative regulation of G protein-coupled receptor signaling pathwayBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIBeta-2 adrenergic receptorHomo sapiens (human)
negative regulation of smooth muscle contractionBeta-2 adrenergic receptorHomo sapiens (human)
brown fat cell differentiationBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of mini excitatory postsynaptic potentialBeta-2 adrenergic receptorHomo sapiens (human)
adrenergic receptor signaling pathwayBeta-2 adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of protein serine/threonine kinase activityBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of cold-induced thermogenesisBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of autophagosome maturationBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of lipophagyBeta-2 adrenergic receptorHomo sapiens (human)
cellular response to amyloid-betaBeta-2 adrenergic receptorHomo sapiens (human)
response to psychosocial stressBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of cAMP-dependent protein kinase activityBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of AMPA receptor activityBeta-2 adrenergic receptorHomo sapiens (human)
norepinephrine-epinephrine-mediated vasodilation involved in regulation of systemic arterial blood pressureBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of heart rate by epinephrine-norepinephrineBeta-1 adrenergic receptorHomo sapiens (human)
positive regulation of the force of heart contraction by epinephrine-norepinephrineBeta-1 adrenergic receptorHomo sapiens (human)
diet induced thermogenesisBeta-1 adrenergic receptorHomo sapiens (human)
response to coldBeta-1 adrenergic receptorHomo sapiens (human)
heat generationBeta-1 adrenergic receptorHomo sapiens (human)
negative regulation of multicellular organism growthBeta-1 adrenergic receptorHomo sapiens (human)
fear responseBeta-1 adrenergic receptorHomo sapiens (human)
regulation of circadian sleep/wake cycle, sleepBeta-1 adrenergic receptorHomo sapiens (human)
brown fat cell differentiationBeta-1 adrenergic receptorHomo sapiens (human)
regulation of postsynaptic membrane potentialBeta-1 adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayBeta-1 adrenergic receptorHomo sapiens (human)
positive regulation of cold-induced thermogenesisBeta-1 adrenergic receptorHomo sapiens (human)
norepinephrine-epinephrine-mediated vasodilation involved in regulation of systemic arterial blood pressureBeta-1 adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeBeta-1 adrenergic receptorHomo sapiens (human)
receptor-mediated endocytosisBeta-3 adrenergic receptorHomo sapiens (human)
negative regulation of G protein-coupled receptor signaling pathwayBeta-3 adrenergic receptorHomo sapiens (human)
diet induced thermogenesisBeta-3 adrenergic receptorHomo sapiens (human)
carbohydrate metabolic processBeta-3 adrenergic receptorHomo sapiens (human)
generation of precursor metabolites and energyBeta-3 adrenergic receptorHomo sapiens (human)
energy reserve metabolic processBeta-3 adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerBeta-3 adrenergic receptorHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayBeta-3 adrenergic receptorHomo sapiens (human)
response to coldBeta-3 adrenergic receptorHomo sapiens (human)
heat generationBeta-3 adrenergic receptorHomo sapiens (human)
negative regulation of multicellular organism growthBeta-3 adrenergic receptorHomo sapiens (human)
eating behaviorBeta-3 adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeBeta-3 adrenergic receptorHomo sapiens (human)
brown fat cell differentiationBeta-3 adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayBeta-3 adrenergic receptorHomo sapiens (human)
positive regulation of cold-induced thermogenesisBeta-3 adrenergic receptorHomo sapiens (human)
norepinephrine-epinephrine-mediated vasodilation involved in regulation of systemic arterial blood pressureBeta-3 adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of cell population proliferationAlpha-1D adrenergic receptorHomo sapiens (human)
neuron-glial cell signalingAlpha-1D adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-1D adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of vasoconstrictionAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-1D adrenergic receptorHomo sapiens (human)
MAPK cascadeAlpha-1A adrenergic receptorHomo sapiens (human)
negative regulation of heart rate involved in baroreceptor response to increased systemic arterial blood pressureAlpha-1A adrenergic receptorHomo sapiens (human)
norepinephrine-epinephrine vasoconstriction involved in regulation of systemic arterial blood pressureAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of heart rate by epinephrine-norepinephrineAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of the force of heart contraction by epinephrine-norepinephrineAlpha-1A adrenergic receptorHomo sapiens (human)
apoptotic processAlpha-1A adrenergic receptorHomo sapiens (human)
smooth muscle contractionAlpha-1A adrenergic receptorHomo sapiens (human)
signal transductionAlpha-1A adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-1A adrenergic receptorHomo sapiens (human)
activation of phospholipase C activityAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationAlpha-1A adrenergic receptorHomo sapiens (human)
adult heart developmentAlpha-1A adrenergic receptorHomo sapiens (human)
negative regulation of cell population proliferationAlpha-1A adrenergic receptorHomo sapiens (human)
response to xenobiotic stimulusAlpha-1A adrenergic receptorHomo sapiens (human)
response to hormoneAlpha-1A adrenergic receptorHomo sapiens (human)
negative regulation of autophagyAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of cardiac muscle hypertrophyAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of synaptic transmission, GABAergicAlpha-1A adrenergic receptorHomo sapiens (human)
intracellular signal transductionAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of action potentialAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of vasoconstrictionAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of smooth muscle contractionAlpha-1A adrenergic receptorHomo sapiens (human)
calcium ion transport into cytosolAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of cardiac muscle contractionAlpha-1A adrenergic receptorHomo sapiens (human)
cell growth involved in cardiac muscle cell developmentAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of protein kinase C signalingAlpha-1A adrenergic receptorHomo sapiens (human)
pilomotor reflexAlpha-1A adrenergic receptorHomo sapiens (human)
neuron-glial cell signalingAlpha-1A adrenergic receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayAlpha-1A adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-1A adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-1A adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
regulation of vasoconstrictionAlpha-1B adrenergic receptorHomo sapiens (human)
intracellular signal transductionAlpha-1B adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-1B adrenergic receptorHomo sapiens (human)
regulation of cardiac muscle contractionAlpha-1B adrenergic receptorHomo sapiens (human)
neuron-glial cell signalingAlpha-1B adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-1B adrenergic receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationAlpha-1B adrenergic receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (98)

Processvia Protein(s)Taxonomy
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
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)
alpha2-adrenergic receptor activityAlpha-2A adrenergic receptorHomo sapiens (human)
protein bindingAlpha-2A adrenergic receptorHomo sapiens (human)
protein kinase bindingAlpha-2A adrenergic receptorHomo sapiens (human)
alpha-1B adrenergic receptor bindingAlpha-2A adrenergic receptorHomo sapiens (human)
alpha-2C adrenergic receptor bindingAlpha-2A adrenergic receptorHomo sapiens (human)
thioesterase bindingAlpha-2A adrenergic receptorHomo sapiens (human)
heterotrimeric G-protein bindingAlpha-2A adrenergic receptorHomo sapiens (human)
protein homodimerization activityAlpha-2A adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-2A adrenergic receptorHomo sapiens (human)
epinephrine bindingAlpha-2A adrenergic receptorHomo sapiens (human)
norepinephrine bindingAlpha-2A adrenergic receptorHomo sapiens (human)
guanyl-nucleotide exchange factor activityAlpha-2A adrenergic receptorHomo sapiens (human)
monooxygenase activityCytochrome P450 2D6Homo sapiens (human)
iron ion bindingCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activityCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2D6Homo sapiens (human)
heme bindingCytochrome P450 2D6Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
alpha2-adrenergic receptor activityAlpha-2B adrenergic receptorHomo sapiens (human)
protein bindingAlpha-2B adrenergic receptorHomo sapiens (human)
epinephrine bindingAlpha-2B adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-1A adrenergic receptorBos taurus (cattle)
alpha2-adrenergic receptor activityAlpha-2C adrenergic receptorHomo sapiens (human)
protein bindingAlpha-2C adrenergic receptorHomo sapiens (human)
alpha-2A adrenergic receptor bindingAlpha-2C adrenergic receptorHomo sapiens (human)
protein homodimerization activityAlpha-2C adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-2C adrenergic receptorHomo sapiens (human)
epinephrine bindingAlpha-2C adrenergic receptorHomo sapiens (human)
guanyl-nucleotide exchange factor activityAlpha-2C adrenergic receptorHomo sapiens (human)
protein bindingAlpha-1D adrenergic receptorHomo sapiens (human)
identical protein bindingAlpha-1D adrenergic receptorHomo sapiens (human)
alpha1-adrenergic receptor activityAlpha-1D adrenergic receptorHomo sapiens (human)
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
virus receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein tyrosine kinase activator activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
identical protein binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein-containing complex binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
identical protein binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled adenosine receptor activityAdenosine receptor A2aRattus norvegicus (Norway rat)
alpha1-adrenergic receptor activityAlpha-1A adrenergic receptorHomo sapiens (human)
protein bindingAlpha-1A adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-1A adrenergic receptorHomo sapiens (human)
histamine receptor activityHistamine H1 receptorHomo sapiens (human)
G protein-coupled serotonin receptor activityHistamine H1 receptorHomo sapiens (human)
neurotransmitter receptor activityHistamine H1 receptorHomo sapiens (human)
protein bindingAlpha-1B adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-1B adrenergic receptorHomo sapiens (human)
alpha1-adrenergic receptor activityAlpha-1B adrenergic receptorHomo sapiens (human)
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
G-protein alpha-subunit binding5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
GTPase activator activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2BHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2BHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
transcription cis-regulatory region bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ubiquitin protein ligase bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
identical protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein homodimerization activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
C3HC4-type RING finger domain bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
scaffold protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
RNA bindingAtaxin-2Homo sapiens (human)
epidermal growth factor receptor bindingAtaxin-2Homo sapiens (human)
protein bindingAtaxin-2Homo sapiens (human)
mRNA bindingAtaxin-2Homo sapiens (human)
G protein-coupled opioid receptor activitySigma non-opioid intracellular receptor 1Homo sapiens (human)
protein bindingSigma non-opioid intracellular receptor 1Homo sapiens (human)
integrin bindingNischarinHomo sapiens (human)
protein bindingNischarinHomo sapiens (human)
phosphatidylinositol bindingNischarinHomo sapiens (human)
identical protein bindingNischarinHomo sapiens (human)
dynein heavy chain bindingNischarinHomo sapiens (human)
alpha-tubulin bindingNischarinHomo sapiens (human)
amyloid-beta bindingBeta-2 adrenergic receptorHomo sapiens (human)
beta2-adrenergic receptor activityBeta-2 adrenergic receptorHomo sapiens (human)
protein bindingBeta-2 adrenergic receptorHomo sapiens (human)
adenylate cyclase bindingBeta-2 adrenergic receptorHomo sapiens (human)
potassium channel regulator activityBeta-2 adrenergic receptorHomo sapiens (human)
identical protein bindingBeta-2 adrenergic receptorHomo sapiens (human)
protein homodimerization activityBeta-2 adrenergic receptorHomo sapiens (human)
protein-containing complex bindingBeta-2 adrenergic receptorHomo sapiens (human)
norepinephrine bindingBeta-2 adrenergic receptorHomo sapiens (human)
beta-adrenergic receptor activityBeta-1 adrenergic receptorHomo sapiens (human)
beta1-adrenergic receptor activityBeta-1 adrenergic receptorHomo sapiens (human)
protein bindingBeta-1 adrenergic receptorHomo sapiens (human)
PDZ domain bindingBeta-1 adrenergic receptorHomo sapiens (human)
alpha-2A adrenergic receptor bindingBeta-1 adrenergic receptorHomo sapiens (human)
protein heterodimerization activityBeta-1 adrenergic receptorHomo sapiens (human)
G protein-coupled neurotransmitter receptor activity involved in regulation of postsynaptic membrane potentialBeta-1 adrenergic receptorHomo sapiens (human)
norepinephrine bindingBeta-3 adrenergic receptorHomo sapiens (human)
beta-adrenergic receptor activityBeta-3 adrenergic receptorHomo sapiens (human)
protein bindingBeta-3 adrenergic receptorHomo sapiens (human)
beta3-adrenergic receptor activityBeta-3 adrenergic receptorHomo sapiens (human)
beta-3 adrenergic receptor bindingBeta-3 adrenergic receptorHomo sapiens (human)
protein homodimerization activityBeta-3 adrenergic receptorHomo sapiens (human)
epinephrine bindingBeta-3 adrenergic receptorHomo sapiens (human)
protein bindingAlpha-1D adrenergic receptorHomo sapiens (human)
identical protein bindingAlpha-1D adrenergic receptorHomo sapiens (human)
alpha1-adrenergic receptor activityAlpha-1D adrenergic receptorHomo sapiens (human)
alpha1-adrenergic receptor activityAlpha-1A adrenergic receptorHomo sapiens (human)
protein bindingAlpha-1A adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-1A adrenergic receptorHomo sapiens (human)
protein bindingAlpha-1B adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-1B adrenergic receptorHomo sapiens (human)
alpha1-adrenergic receptor activityAlpha-1B adrenergic receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (76)

Processvia Protein(s)Taxonomy
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
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)
cytoplasmAlpha-2A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2A adrenergic receptorHomo sapiens (human)
basolateral plasma membraneAlpha-2A adrenergic receptorHomo sapiens (human)
neuronal cell bodyAlpha-2A adrenergic receptorHomo sapiens (human)
axon terminusAlpha-2A adrenergic receptorHomo sapiens (human)
presynaptic active zone membraneAlpha-2A adrenergic receptorHomo sapiens (human)
dopaminergic synapseAlpha-2A adrenergic receptorHomo sapiens (human)
postsynaptic density membraneAlpha-2A adrenergic receptorHomo sapiens (human)
glutamatergic synapseAlpha-2A adrenergic receptorHomo sapiens (human)
GABA-ergic synapseAlpha-2A adrenergic receptorHomo sapiens (human)
receptor complexAlpha-2A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2A adrenergic receptorHomo sapiens (human)
mitochondrionCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulumCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2D6Homo sapiens (human)
cytoplasmCytochrome P450 2D6Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2D6Homo sapiens (human)
cytosolAlpha-2B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2B adrenergic receptorHomo sapiens (human)
cell surfaceAlpha-2B adrenergic receptorHomo sapiens (human)
intracellular membrane-bounded organelleAlpha-2B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2B adrenergic receptorHomo sapiens (human)
nucleusAlpha-1A adrenergic receptorBos taurus (cattle)
cytoplasmAlpha-1A adrenergic receptorBos taurus (cattle)
plasma membraneAlpha-1A adrenergic receptorBos taurus (cattle)
caveolaAlpha-1A adrenergic receptorBos taurus (cattle)
nuclear membraneAlpha-1A adrenergic receptorBos taurus (cattle)
cytoplasmAlpha-2C adrenergic receptorHomo sapiens (human)
endosomeAlpha-2C adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2C adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2C adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1D adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1D adrenergic receptorHomo sapiens (human)
neurofilament5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
caveola5-hydroxytryptamine receptor 2AHomo sapiens (human)
axon5-hydroxytryptamine receptor 2AHomo sapiens (human)
cytoplasmic vesicle5-hydroxytryptamine receptor 2AHomo sapiens (human)
presynaptic membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
neuronal cell body5-hydroxytryptamine receptor 2AHomo sapiens (human)
dendritic shaft5-hydroxytryptamine receptor 2AHomo sapiens (human)
postsynaptic membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
cell body fiber5-hydroxytryptamine receptor 2AHomo sapiens (human)
glutamatergic synapse5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2CHomo sapiens (human)
synapse5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2CHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2CHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2CHomo sapiens (human)
Golgi membraneAdenosine receptor A2aRattus norvegicus (Norway rat)
nucleusAlpha-1A adrenergic receptorHomo sapiens (human)
nucleoplasmAlpha-1A adrenergic receptorHomo sapiens (human)
cytoplasmAlpha-1A adrenergic receptorHomo sapiens (human)
cytosolAlpha-1A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1A adrenergic receptorHomo sapiens (human)
caveolaAlpha-1A adrenergic receptorHomo sapiens (human)
nuclear membraneAlpha-1A adrenergic receptorHomo sapiens (human)
intracellular membrane-bounded organelleAlpha-1A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1A adrenergic receptorHomo sapiens (human)
cytosolHistamine H1 receptorHomo sapiens (human)
plasma membraneHistamine H1 receptorHomo sapiens (human)
synapseHistamine H1 receptorHomo sapiens (human)
dendriteHistamine H1 receptorHomo sapiens (human)
plasma membraneHistamine H1 receptorHomo sapiens (human)
nucleusAlpha-1B adrenergic receptorHomo sapiens (human)
cytoplasmAlpha-1B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1B adrenergic receptorHomo sapiens (human)
caveolaAlpha-1B adrenergic receptorHomo sapiens (human)
nuclear membraneAlpha-1B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1B adrenergic receptorHomo sapiens (human)
nucleoplasm5-hydroxytryptamine receptor 2BHomo sapiens (human)
cytoplasm5-hydroxytryptamine receptor 2BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2BHomo sapiens (human)
synapse5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2BHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2BHomo sapiens (human)
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cell surfacePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
perinuclear region of cytoplasmPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cytoplasmAtaxin-2Homo sapiens (human)
Golgi apparatusAtaxin-2Homo sapiens (human)
trans-Golgi networkAtaxin-2Homo sapiens (human)
cytosolAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
membraneAtaxin-2Homo sapiens (human)
perinuclear region of cytoplasmAtaxin-2Homo sapiens (human)
ribonucleoprotein complexAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
nuclear envelopeSigma non-opioid intracellular receptor 1Homo sapiens (human)
nuclear inner membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
nuclear outer membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
endoplasmic reticulumSigma non-opioid intracellular receptor 1Homo sapiens (human)
endoplasmic reticulum membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
lipid dropletSigma non-opioid intracellular receptor 1Homo sapiens (human)
cytosolSigma non-opioid intracellular receptor 1Homo sapiens (human)
postsynaptic densitySigma non-opioid intracellular receptor 1Homo sapiens (human)
membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
growth coneSigma non-opioid intracellular receptor 1Homo sapiens (human)
cytoplasmic vesicleSigma non-opioid intracellular receptor 1Homo sapiens (human)
anchoring junctionSigma non-opioid intracellular receptor 1Homo sapiens (human)
postsynaptic density membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
endoplasmic reticulumSigma non-opioid intracellular receptor 1Homo sapiens (human)
nucleoplasmNischarinHomo sapiens (human)
early endosomeNischarinHomo sapiens (human)
cytosolNischarinHomo sapiens (human)
plasma membraneNischarinHomo sapiens (human)
microtubule cytoskeletonNischarinHomo sapiens (human)
membraneNischarinHomo sapiens (human)
intracellular membrane-bounded organelleNischarinHomo sapiens (human)
intercellular bridgeNischarinHomo sapiens (human)
recycling endosomeNischarinHomo sapiens (human)
cytoplasmNischarinHomo sapiens (human)
nucleusBeta-2 adrenergic receptorHomo sapiens (human)
lysosomeBeta-2 adrenergic receptorHomo sapiens (human)
endosomeBeta-2 adrenergic receptorHomo sapiens (human)
early endosomeBeta-2 adrenergic receptorHomo sapiens (human)
Golgi apparatusBeta-2 adrenergic receptorHomo sapiens (human)
plasma membraneBeta-2 adrenergic receptorHomo sapiens (human)
endosome membraneBeta-2 adrenergic receptorHomo sapiens (human)
membraneBeta-2 adrenergic receptorHomo sapiens (human)
apical plasma membraneBeta-2 adrenergic receptorHomo sapiens (human)
clathrin-coated endocytic vesicle membraneBeta-2 adrenergic receptorHomo sapiens (human)
neuronal dense core vesicleBeta-2 adrenergic receptorHomo sapiens (human)
receptor complexBeta-2 adrenergic receptorHomo sapiens (human)
plasma membraneBeta-2 adrenergic receptorHomo sapiens (human)
early endosomeBeta-1 adrenergic receptorHomo sapiens (human)
plasma membraneBeta-1 adrenergic receptorHomo sapiens (human)
Schaffer collateral - CA1 synapseBeta-1 adrenergic receptorHomo sapiens (human)
neuronal dense core vesicleBeta-1 adrenergic receptorHomo sapiens (human)
plasma membraneBeta-1 adrenergic receptorHomo sapiens (human)
plasma membraneBeta-3 adrenergic receptorHomo sapiens (human)
receptor complexBeta-3 adrenergic receptorHomo sapiens (human)
plasma membraneBeta-3 adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1D adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1D adrenergic receptorHomo sapiens (human)
nucleusAlpha-1A adrenergic receptorHomo sapiens (human)
nucleoplasmAlpha-1A adrenergic receptorHomo sapiens (human)
cytoplasmAlpha-1A adrenergic receptorHomo sapiens (human)
cytosolAlpha-1A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1A adrenergic receptorHomo sapiens (human)
caveolaAlpha-1A adrenergic receptorHomo sapiens (human)
nuclear membraneAlpha-1A adrenergic receptorHomo sapiens (human)
intracellular membrane-bounded organelleAlpha-1A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1A adrenergic receptorHomo sapiens (human)
nucleusAlpha-1B adrenergic receptorHomo sapiens (human)
cytoplasmAlpha-1B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1B adrenergic receptorHomo sapiens (human)
caveolaAlpha-1B adrenergic receptorHomo sapiens (human)
nuclear membraneAlpha-1B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1B adrenergic receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (315)

Assay IDTitleYearJournalArticle
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
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.
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1345857Rat alpha1A-adrenoceptor (Adrenoceptors)2001The Journal of biological chemistry, Jul-06, Volume: 276, Issue:27
Phe-308 and Phe-312 in transmembrane domain 7 are major sites of alpha 1-adrenergic receptor antagonist binding. Imidazoline agonists bind like antagonists.
AID1346049Human alpha2A-adrenoceptor (Adrenoceptors)1994European journal of pharmacology, Jan-24, Volume: 252, Issue:1
Further characterization of human alpha 2-adrenoceptor subtypes: [3H]RX821002 binding and definition of additional selective drugs.
AID1346049Human alpha2A-adrenoceptor (Adrenoceptors)1992Molecular pharmacology, Jul, Volume: 42, Issue:1
Pharmacological characteristics of alpha 2-adrenergic receptors: comparison of pharmacologically defined subtypes with subtypes identified by molecular cloning.
AID1346159Human alpha2C-adrenoceptor (Adrenoceptors)1992Molecular pharmacology, Jul, Volume: 42, Issue:1
Pharmacological characteristics of alpha 2-adrenergic receptors: comparison of pharmacologically defined subtypes with subtypes identified by molecular cloning.
AID1346159Human alpha2C-adrenoceptor (Adrenoceptors)1994European journal of pharmacology, Jan-24, Volume: 252, Issue:1
Further characterization of human alpha 2-adrenoceptor subtypes: [3H]RX821002 binding and definition of additional selective drugs.
AID1345908Human alpha1A-adrenoceptor (Adrenoceptors)1995Molecular pharmacology, Aug, Volume: 48, Issue:2
KMD-3213, a novel, potent, alpha 1a-adrenoceptor-selective antagonist: characterization using recombinant human alpha 1-adrenoceptors and native tissues.
AID1346000Human alpha1B-adrenoceptor (Adrenoceptors)1995Molecular pharmacology, Aug, Volume: 48, Issue:2
KMD-3213, a novel, potent, alpha 1a-adrenoceptor-selective antagonist: characterization using recombinant human alpha 1-adrenoceptors and native tissues.
AID1346058Human alpha2B-adrenoceptor (Adrenoceptors)1992Molecular pharmacology, Jul, Volume: 42, Issue:1
Pharmacological characteristics of alpha 2-adrenergic receptors: comparison of pharmacologically defined subtypes with subtypes identified by molecular cloning.
AID1346058Human alpha2B-adrenoceptor (Adrenoceptors)1994European journal of pharmacology, Jan-24, Volume: 252, Issue:1
Further characterization of human alpha 2-adrenoceptor subtypes: [3H]RX821002 binding and definition of additional selective drugs.
AID1345971Human alpha1D-adrenoceptor (Adrenoceptors)1995Molecular pharmacology, Aug, Volume: 48, Issue:2
KMD-3213, a novel, potent, alpha 1a-adrenoceptor-selective antagonist: characterization using recombinant human alpha 1-adrenoceptors and native tissues.
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.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
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.
AID36922Inhibition of specific [3H]clonidine binding (0.4 nM) to rat brain membranes Alpha-2 adrenergic receptor1984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists.
AID58333Percent inhibition of the pressor responses to 0.75 ug/kg iv norepinephrine in pentobarbital-anesthetized dogs for a dose of 1 mg/kg1981Journal of medicinal chemistry, Nov, Volume: 24, Issue:11
Synthesis and antihypertensive activity of a series of 8-substituted 1-oxa-3,8-diazaspiro[4.5]decan-2-ones.
AID400121Antihypertensive activity in anesthetized SHR rat assessed as increase in heart rate at 3 mg/kg, iv1998Journal of natural products, Mar, Volume: 61, Issue:3
Cardiovascular effects of aspidofractinine-type alkaloids from Kopsia.
AID37099Binding affinity towards Alpha-2 adrenergic receptor, using [3H]- atipamezole as radioligand from rat frontal cortex membranes1991Journal of medicinal chemistry, May, Volume: 34, Issue:5
Synthesis and in vitro evaluation of 2,3-dimethoxy-5-(fluoroalkyl)-substituted benzamides: high-affinity ligands for CNS dopamine D2 receptors.
AID1136070Blockade of alpha-adrenergic receptor in rabbit aortic strips assessed as reduction of epinephrine-induced response1979Journal of medicinal chemistry, Dec, Volume: 22, Issue:12
Derivatives of 1,3-disubstituted 2,4(1H,3H)-quinazolinediones as possible peripheral vasodilators or antihypertensive agents.
AID233915selectivity ratio is the ratio between pA2 values of alfa2 and alfa1 adrenoceptors1982Journal of medicinal chemistry, Jun, Volume: 25, Issue:6
Structure-activity relationships for 2-substituted imidazoles as alpha 2-adrenoceptor antagonists.
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID58334Percent inhibition of the pressor responses to 0.75 ug/kg iv norepinephrine in pentobarbital-anesthetized dogs for a dose of 10 mg/kg1981Journal of medicinal chemistry, Nov, Volume: 24, Issue:11
Synthesis and antihypertensive activity of a series of 8-substituted 1-oxa-3,8-diazaspiro[4.5]decan-2-ones.
AID35591Displacement of [3H]prazosin (0.3 nM) from rat Alpha-1D adrenergic receptor expressed in CHO cells2003Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2
Synthesis and structure-affinity relationship investigations of 5-heteroaryl-substituted analogues of the antipsychotic sertindole. A new class of highly selective alpha(1) adrenoceptor antagonists.
AID338167Displacement of [3H]RX781094 from alpha2 adrenergic receptor assessed as specific binding relative to total binding1993Journal of natural products, Apr, Volume: 56, Issue:4
The role of receptor binding in drug discovery.
AID254398Binding affinity towards human alpha-2C adrenergic receptor expressed in Chinese Hamster ovary (CHO) cells2005Bioorganic & medicinal chemistry letters, Nov-01, Volume: 15, Issue:21
Bioisosteric phentolamine analogs as potent alpha-adrenergic antagonists.
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).
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.
AID170692Percent change of heart rate in conscious DOCA Hypertensive rat at 2 hour after administration of dose of 10 mL (mg/kg po)1982Journal of medicinal chemistry, Jul, Volume: 25, Issue:7
Synthesis of some potential antihypertensive phthalazinyl- and quinoxalinylguanidines.
AID35866Antagonistic potency of compound for Alpha-1 adrenergic receptor1981Journal of medicinal chemistry, Nov, Volume: 24, Issue:11
Synthesis and antihypertensive activity of a series of 8-substituted 1-oxa-3,8-diazaspiro[4.5]decan-2-ones.
AID58336Percent inhibition of the pressor responses to 0.75 ug/kg iv norepinephrine in pentobarbital-anesthetized dogs for a dose of 5.0 mg/kg1981Journal of medicinal chemistry, Nov, Volume: 24, Issue:11
Synthesis and antihypertensive activity of a series of 8-substituted 1-oxa-3,8-diazaspiro[4.5]decan-2-ones.
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.
AID503661Antagonist activity at adrenergic alpha2A receptor expressed in HEK293 cells coexpressing yellow fluorescent and cyan fluorescent protein assessed as reversal of norepinephrine-induced resonance signal at 100 uM by FRET assay2005Nature chemical biology, Jun, Volume: 1, Issue:1
Molecular basis of inverse agonism in a G protein-coupled receptor.
AID342863Selectivity ratio of pKi for human imidazoline receptor 1 to pKi for human alpha2 adrenoceptors2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
QSAR study of imidazoline antihypertensive drugs.
AID59018Change in mean arterial pressure in anesthetized dogs for a dose of 0.1 mg/kg1981Journal of medicinal chemistry, Nov, Volume: 24, Issue:11
Synthesis and antihypertensive activity of a series of 8-substituted 1-oxa-3,8-diazaspiro[4.5]decan-2-ones.
AID697786Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of histamine-induced Ca2+ release by using fura-2AM-based fluorescence assay2012Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
Shape-based reprofiling of FDA-approved drugs for the H₁ histamine receptor.
AID58341Percent inhibition of the pressor responses to 7.5 ug/kg iv phenylephrine in pentobarbital-anesthetized dogs for a dose of 1 mg/kg1981Journal of medicinal chemistry, Nov, Volume: 24, Issue:11
Synthesis and antihypertensive activity of a series of 8-substituted 1-oxa-3,8-diazaspiro[4.5]decan-2-ones.
AID1278102Inhibition of 5-HT-induced contraction in Sprague-Dawley rat ileum at 1 uM incubated for 10 mins2016European journal of medicinal chemistry, Mar-03, Volume: 110Synthesis, in vitro and in vivo pharmacological evaluation of serotoninergic ligands containing an isonicotinic nucleus.
AID234827slope value of the compound1982Journal of medicinal chemistry, Jun, Volume: 25, Issue:6
Arylethanolamines derived from salicylamide with alpha- and beta-adrenoceptor blocking activities. Preparation of labetalol, its enantiomers, and related salicylamides.
AID35871Methoxamine antagonistic activity against alpha-1 adrenergic receptor in isolated, field -simulated vas deferens from rats1983Journal of medicinal chemistry, Dec, Volume: 26, Issue:12
alpha-Adrenergic activities of some substituted 2-(aminomethyl)imidazolines.
AID181464Antihypertensive activity as percentage fall in systolic blood pressure in spontaneously hypertensive rats after a period of 1 hr for a dose of 50 mg/kg1981Journal of medicinal chemistry, Nov, Volume: 24, Issue:11
Synthesis and antihypertensive activity of a series of 8-substituted 1-oxa-3,8-diazaspiro[4.5]decan-2-ones.
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).
AID337882Displacement of [3H]prazosin from alpha1 adrenergic receptor1993Journal of natural products, Apr, Volume: 56, Issue:4
The role of receptor binding in drug discovery.
AID36052Dissociation constant (KB) was evaluated for alpha-2 adrenergic receptor1983Journal of medicinal chemistry, Sep, Volume: 26, Issue:9
6-Chloro-2,3,4,5-tetrahydro-3-methyl-1H-3-benzazepine: a potent and selective antagonist of alpha 2-adrenoceptors.
AID35187Displacement of [3H]clonidine from Alpha-2 adrenergic receptor of rat brain membranes1982Journal of medicinal chemistry, Dec, Volume: 25, Issue:12
alpha 2 adrenoceptors: classification, localization, mechanisms, and targets for drugs.
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).
AID170699Percent change of mean arterial blood pressure in conscious DOCA Hypertensive rat at 1 hour, after administration of dose 10 mL (mg/kg po)1982Journal of medicinal chemistry, Jul, Volume: 25, Issue:7
Synthesis of some potential antihypertensive phthalazinyl- and quinoxalinylguanidines.
AID5588Ability to displace [3H]ketanserin (0.5 nM) from cerebral cortex of rat 5-hydroxytryptamine 2A receptor; NT=not tested2003Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2
Synthesis and structure-affinity relationship investigations of 5-heteroaryl-substituted analogues of the antipsychotic sertindole. A new class of highly selective alpha(1) adrenoceptor antagonists.
AID36580Agonist activity against alpha-1 adrenergic receptor from rat vas deferens1983Journal of medicinal chemistry, Dec, Volume: 26, Issue:12
alpha-Adrenergic activities of some substituted 2-(aminomethyl)imidazolines.
AID33260Tested for alpha adrenergic receptor agonistic activity on isolated rat vas deferens1983Journal of medicinal chemistry, Feb, Volume: 26, Issue:2
Conformational effects on the activity of drugs. 10. Synthesis, conformation, and pharmacological properties of 1-(2,5-dimethoxyphenyl)-2-aminoethanols and their morpholine analogues.
AID33124Evaluated for norepinephrine as agonist.1982Journal of medicinal chemistry, Jun, Volume: 25, Issue:6
Arylethanolamines derived from salicylamide with alpha- and beta-adrenoceptor blocking activities. Preparation of labetalol, its enantiomers, and related salicylamides.
AID181326Antihypertensive activity in DOCA/saline rat dosed at 50 mg/kg, po expressed as percent fall in blood pressure after 6 h; NS is not significant1983Journal of medicinal chemistry, Mar, Volume: 26, Issue:3
synthesis and antihypertensive activity of 2-sulfonamido- and 2-sulfamido-1,3,4,6,7,11b alpha-hexahydro-2H-benzo[a]quinolizines.
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).
AID254395Binding affinity towards human alpha-1D adrenergic receptor expressed in Chinese Hamster ovary (CHO) cells2005Bioorganic & medicinal chemistry letters, Nov-01, Volume: 15, Issue:21
Bioisosteric phentolamine analogs as potent alpha-adrenergic antagonists.
AID181474Percentage fall in systolic blood pressure in spontaneously hypertensive rats after 3 h following 50 mg/kg p.o.1981Journal of medicinal chemistry, Nov, Volume: 24, Issue:11
Synthesis and antihypertensive activity of a series of 8-substituted 1-oxa-3,8-diazaspiro[4.5]decan-2-ones.
AID37313Binding affinity towards Alpha-1 adrenergic receptor from rat cortical membranes2002Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
Structure-affinity relationship study on N-[4-(4-arylpiperazin-1-yl)butyl]arylcarboxamides as potent and selective dopamine D(3) receptor ligands.
AID41762In vitro inhibitory specificity for Beta adrenergic receptor was evaluated; ND=not determined1998Journal of medicinal chemistry, May-07, Volume: 41, Issue:10
Synthesis and adrenergic activity of a new series of N-aryl dicyclopropyl ketone oxime ethers: SAR and stereochemical aspects.
AID35361Antagonistic activity against presynaptic alpha-2 adrenergic receptor in isolated rat vas deferens using xylazine as agonist1987Journal of medicinal chemistry, Aug, Volume: 30, Issue:8
Berbanes: a new class of selective alpha 2-adrenoceptor antagonists.
AID400123Antihypertensive activity in anesthetized SHR rat assessed as decrease in heart rate at 3 mg/kg, iv after 10 mins1998Journal of natural products, Mar, Volume: 61, Issue:3
Cardiovascular effects of aspidofractinine-type alkaloids from Kopsia.
AID191918Antihypertensive activity in DOCA/saline rat dosed at 50 mg/kg, po expressed as percent rise in heart rate after 6 h; NS is not significant1983Journal of medicinal chemistry, Mar, Volume: 26, Issue:3
synthesis and antihypertensive activity of 2-sulfonamido- and 2-sulfamido-1,3,4,6,7,11b alpha-hexahydro-2H-benzo[a]quinolizines.
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).
AID400120Antihypertensive activity in anesthetized SHR rat assessed as decrease in basal mean arterial blood pressure at 3 mg/kg, iv1998Journal of natural products, Mar, Volume: 61, Issue:3
Cardiovascular effects of aspidofractinine-type alkaloids from Kopsia.
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.
AID337883Displacement of [3H]RX781094 from alpha2 adrenergic receptor1993Journal of natural products, Apr, Volume: 56, Issue:4
The role of receptor binding in drug discovery.
AID36707Alpha-1-adrenolytic activity was assessed in vitro from the ability to inhibit clonidine binding to rat aorta preparation1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
New 1,4-dihydropyridine derivatives combining calcium antagonism and alpha-adrenolytic properties.
AID80448The compound was tested for chronotropic effect studied in right atria isolated from guinea pig and is expressed in pA2; ND=not determined1998Journal of medicinal chemistry, May-07, Volume: 41, Issue:10
Synthesis and adrenergic activity of a new series of N-aryl dicyclopropyl ketone oxime ethers: SAR and stereochemical aspects.
AID1229077Displacement of [3H]-Prazosin from human alpha-1D adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis2015ACS medicinal chemistry letters, May-14, Volume: 6, Issue:5
Discovery of Quinazoline-Based Fluorescent Probes to α1-Adrenergic Receptors.
AID167198Inhibition of specific [3H]-prazosin binding (0.2 nM) to rat brain membranes alpha1 adrenoceptor.1984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists.
AID36731In vitro inhibitory activity against Alpha-1 adrenergic receptor by using [3H]prazosin radioligand binding assay1999Journal of medicinal chemistry, Feb-11, Volume: 42, Issue:3
1-aryl-4-[(5-methoxy-1,2,3, 4-tetrahydronaphthalen-1-yl)alkyl]piperazines and their analogues: influence of the stereochemistry of the tetrahydronaphthalen-1-yl nucleus on 5-HT1A receptor affinity and selectivity versus alpha1 and D2 receptors. 5.
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.
AID1365279Antagonist activity at 5-HT2A receptor in Sprague-Dawley rat ielum assessed as reduction in 5-HT-evoked contraction at 1 uM2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
New 5-HT
AID65297Ability to displace [3H]spiperone (0.3 nM) from CHO cells of human Dopamine receptor D3; NT=not tested2003Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2
Synthesis and structure-affinity relationship investigations of 5-heteroaryl-substituted analogues of the antipsychotic sertindole. A new class of highly selective alpha(1) adrenoceptor antagonists.
AID35905Binding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]prazosin as the radioligand1983Journal of medicinal chemistry, Dec, Volume: 26, Issue:12
alpha-Adrenergic activities of some substituted 2-(aminomethyl)imidazolines.
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).
AID254394Binding affinity towards human alpha-1B adrenergic receptor expressed in Chinese Hamster ovary (CHO) cells2005Bioorganic & medicinal chemistry letters, Nov-01, Volume: 15, Issue:21
Bioisosteric phentolamine analogs as potent alpha-adrenergic antagonists.
AID170691Percent change of heart rate in conscious DOCA Hypertensive rat at 1 hour after administration of dose of 10 mL (mg/kg po)1982Journal of medicinal chemistry, Jul, Volume: 25, Issue:7
Synthesis of some potential antihypertensive phthalazinyl- and quinoxalinylguanidines.
AID35860Antagonistic activity against Alpha-1 adrenergic receptor in the epidermal portion of the rat vas deferens1982Journal of medicinal chemistry, Jun, Volume: 25, Issue:6
Structure-activity relationships for 2-substituted imidazoles as alpha 2-adrenoceptor antagonists.
AID235866Index of alpha1/alpha2 adrenoceptor binding selectivity.1984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists.
AID254397Binding affinity towards human alpha-2B adrenergic receptor expressed in Chinese Hamster ovary (CHO) cells2005Bioorganic & medicinal chemistry letters, Nov-01, Volume: 15, Issue:21
Bioisosteric phentolamine analogs as potent alpha-adrenergic antagonists.
AID36408Binding affinity against Alpha-2C adrenergic receptor from human clones.1995Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification.
AID58339Percent inhibition of the pressor responses to 1 ug/kg iv Epinephrine in pentobarbital-anesthetized dogs for a dose of 10 mg/kg1981Journal of medicinal chemistry, Nov, Volume: 24, Issue:11
Synthesis and antihypertensive activity of a series of 8-substituted 1-oxa-3,8-diazaspiro[4.5]decan-2-ones.
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.
AID27922Calculated partition coefficient (clogP)2001Journal of medicinal chemistry, Dec-06, Volume: 44, Issue:25
trans-4-[4-(Methoxyphenyl)cyclohexyl]-1-arylpiperazines: a new class of potent and selective 5-HT(1A) receptor ligands as conformationally constrained analogues of 4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]-1-arylpiperazines.
AID256443Potency ratio against alpha-1D adrenergic receptor is determined KB of phenylephrine-induced contractions2005Bioorganic & medicinal chemistry letters, Nov-01, Volume: 15, Issue:21
Bioisosteric phentolamine analogs as potent alpha-adrenergic antagonists.
AID61662Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1; NT=not tested2003Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2
Synthesis and structure-affinity relationship investigations of 5-heteroaryl-substituted analogues of the antipsychotic sertindole. A new class of highly selective alpha(1) adrenoceptor antagonists.
AID254396Binding affinity towards human alpha-2A adrenergic receptor expressed in Chinese Hamster ovary (CHO) cells2005Bioorganic & medicinal chemistry letters, Nov-01, Volume: 15, Issue:21
Bioisosteric phentolamine analogs as potent alpha-adrenergic antagonists.
AID37067Displacement of [3H]prazosin (0.5 nM) from hamster Alpha-1B adrenergic receptor expressed in rat-1 cells2003Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2
Synthesis and structure-affinity relationship investigations of 5-heteroaryl-substituted analogues of the antipsychotic sertindole. A new class of highly selective alpha(1) adrenoceptor antagonists.
AID36190Binding affinity against alpha-2-adrenergic receptor using 10 nM [3H]yohimbine in human platelet membranes from three separate experiments using 10 inhibitor concentrations1984Journal of medicinal chemistry, Jul, Volume: 27, Issue:7
Development of an affinity ligand for purification of alpha 2-adrenoceptors from human platelet membranes.
AID59021Change in mean arterial pressure in anesthetized dogs for a dose of 10 mg/kg1981Journal of medicinal chemistry, Nov, Volume: 24, Issue:11
Synthesis and antihypertensive activity of a series of 8-substituted 1-oxa-3,8-diazaspiro[4.5]decan-2-ones.
AID342861Displacement of [125I]PIC from human imidazoline receptor 1 in human platelets analyzed under norepinephrine mask of alpha 2AR2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
QSAR study of imidazoline antihypertensive drugs.
AID400122Antihypertensive activity in anesthetized SHR rat assessed as decrease in basal mean arterial blood pressure at 3 mg/kg, iv after 10 mins1998Journal of natural products, Mar, Volume: 61, Issue:3
Cardiovascular effects of aspidofractinine-type alkaloids from Kopsia.
AID394756Inhibition of [3H]norepinephrine binding to Escherichia coli Qsec by liposome-based scintillation counting assay2008Science (New York, N.Y.), Aug-22, Volume: 321, Issue:5892
Targeting QseC signaling and virulence for antibiotic development.
AID196984Antagonist activity against phenylephrine-induced alpha1- adrenoceptor mediated vasoconstriction in pithed normotensive rats. 1984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists.
AID235334Selectivity ratio (Alpha-1: Alpha-2)1987Journal of medicinal chemistry, Aug, Volume: 30, Issue:8
Berbanes: a new class of selective alpha 2-adrenoceptor antagonists.
AID36656Agonistic activity against alpha alpha-2 adrenergic receptor in isolated, field -simulated vas deferens from rats1983Journal of medicinal chemistry, Dec, Volume: 26, Issue:12
alpha-Adrenergic activities of some substituted 2-(aminomethyl)imidazolines.
AID1194506Displacement of [3H]prazosin from rat cerebral cortex alpha-1 adrenergic receptor by liquid scintillation counting analysis2015Bioorganic & medicinal chemistry, May-01, Volume: 23, Issue:9
α-Adrenoceptor antagonistic and hypotensive properties of novel arylpiperazine derivatives of pyrrolidin-2-one.
AID36640Alpha-2 adrenergic receptor pA2 value against norepinephrine in vitro experiment in rat anococcygeus.1983Journal of medicinal chemistry, Jun, Volume: 26, Issue:6
alpha-adrenoreceptor reagents. 1. Synthesis of some 1,4-benzodioxans as selective presynaptic alpha 2-adrenoreceptor antagonists and potential antidepressants.
AID33132Inhibitory concentration required for displacement of Alpha adrenergic receptor specific ligand, 2-[ [ [(2,6-dimethoxyphenoxy) ethyl]amino]methyl]benzodioxan ([3H]WB-4101) from rat brain cerebral cortical membranes1982Journal of medicinal chemistry, Jun, Volume: 25, Issue:6
Syntheses and adrenergic agonist properties of ring-fluorinated isoproterenols.
AID181325Antihypertensive activity in DOCA/saline rat dosed at 50 mg/kg, po expressed as percent fall in blood pressure after 2 h1983Journal of medicinal chemistry, Mar, Volume: 26, Issue:3
synthesis and antihypertensive activity of 2-sulfonamido- and 2-sulfamido-1,3,4,6,7,11b alpha-hexahydro-2H-benzo[a]quinolizines.
AID219808Compound was tested for its ability to inhibit specific binding of [3H]-clonidine to alpha-2-adrenoceptor.1986Journal of medicinal chemistry, Jul, Volume: 29, Issue:7
Two stereoisomeric imidazoline derivatives: synthesis and optical and alpha 2-adrenoceptor activities.
AID5749Ability to displace [3H]mesulergine (0.5 nM) from SR-3T3 cells of rat 5-hydroxytryptamine 2C receptor; NT=not tested2003Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2
Synthesis and structure-affinity relationship investigations of 5-heteroaryl-substituted analogues of the antipsychotic sertindole. A new class of highly selective alpha(1) adrenoceptor antagonists.
AID239800Binding affinity for alpha 1b adrenoceptor2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Range and sensitivity as descriptors of molecular property spaces in dynamic QSAR analyses.
AID58342Percent inhibition of the pressor responses to 7.5 ug/kg iv phenylephrine in pentobarbital-anesthetized dogs for a dose of 10 mg/kg1981Journal of medicinal chemistry, Nov, Volume: 24, Issue:11
Synthesis and antihypertensive activity of a series of 8-substituted 1-oxa-3,8-diazaspiro[4.5]decan-2-ones.
AID36553The compound was tested for binding affinity against alpha-2D adrenergic receptor, from rat clones.1995Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification.
AID172994Antagonist effect to pressor response of 0.3 ug/kg of norepinephrine intravenously in rats at the dose 32 uM/kg1980Journal of medicinal chemistry, Nov, Volume: 23, Issue:11
Synthesis and adrenergic blocking effects of 2-(alkylamino)-3,4-dihydroquinazolines.
AID36422Inhibition of specific [3H]prazosin binding (0.2 nM) to rat brain membranes alpha-1 adrenergic receptor1984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists.
AID60485Relative adrenoceptor blocking activity (DR10) was recorded for the antagonism of Isoproterenol-induced responses in Positive chronotropy in beta1-Adrenoceptor blockade1982Journal of medicinal chemistry, Jun, Volume: 25, Issue:6
Arylethanolamines derived from salicylamide with alpha- and beta-adrenoceptor blocking activities. Preparation of labetalol, its enantiomers, and related salicylamides.
AID1229075Displacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis2015ACS medicinal chemistry letters, May-14, Volume: 6, Issue:5
Discovery of Quinazoline-Based Fluorescent Probes to α1-Adrenergic Receptors.
AID170702Percent change of mean arterial blood pressure in conscious DOCA Hypertensive rat at 3 hour, after administration of dose 10 mL (mg/kg po)1982Journal of medicinal chemistry, Jul, Volume: 25, Issue:7
Synthesis of some potential antihypertensive phthalazinyl- and quinoxalinylguanidines.
AID36868Inhibition of [3H]WB-4101 binding to alpha-1-adrenergic receptor from rat cerebral cortex membranes1983Journal of medicinal chemistry, Feb, Volume: 26, Issue:2
Buspirone analogues. 1. Structure-activity relationships in a series of N-aryl- and heteroarylpiperazine derivatives.
AID36058Antagonistic activity against longitudinal muscle strip of the guinea pig ileum using xylazine as agonist1987Journal of medicinal chemistry, Aug, Volume: 30, Issue:8
Berbanes: a new class of selective alpha 2-adrenoceptor antagonists.
AID231250Potency ratio in rat thoracic aorta1983Journal of medicinal chemistry, Mar, Volume: 26, Issue:3
Pyrimidine derivatives. 4. Synthesis and antihypertensive activity of 4-amino-2-(4-cinnamoylpiperazino)-6,7-dimethoxyquinazoline derivatives.
AID338166Displacement of [3H]prazosin from alpha1 adrenergic receptor assessed as specific binding relative to total binding1993Journal of natural products, Apr, Volume: 56, Issue:4
The role of receptor binding in drug discovery.
AID37454Binding affinity towards alpha-1 adrenergic receptor in rat cortical membranes2001Journal of medicinal chemistry, Dec-06, Volume: 44, Issue:25
trans-4-[4-(Methoxyphenyl)cyclohexyl]-1-arylpiperazines: a new class of potent and selective 5-HT(1A) receptor ligands as conformationally constrained analogues of 4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]-1-arylpiperazines.
AID35339Clonidine antagonistic activity against alpha-2 adrenergic receptor in isolated, field -simulated vas deferens from rats1983Journal of medicinal chemistry, Dec, Volume: 26, Issue:12
alpha-Adrenergic activities of some substituted 2-(aminomethyl)imidazolines.
AID35951The compound was tested for binding affinity against Alpha-2A adrenergic receptor from human clones.1995Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification.
AID170693Percent change of heart rate in conscious DOCA Hypertensive rat at 22 hour after administration of dose of 10 mL (mg/kg po)1982Journal of medicinal chemistry, Jul, Volume: 25, Issue:7
Synthesis of some potential antihypertensive phthalazinyl- and quinoxalinylguanidines.
AID37168Ability to displace [3H]prazosin (0.25 nM) from whole brain of rat alpha-1 adrenergic receptor2003Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2
Synthesis and structure-affinity relationship investigations of 5-heteroaryl-substituted analogues of the antipsychotic sertindole. A new class of highly selective alpha(1) adrenoceptor antagonists.
AID37363Compound was tested for the inhibition of [3H]clonidine binding Alpha-2 adrenergic receptor of crude rat brain membrane1982Journal of medicinal chemistry, Jan, Volume: 25, Issue:1
1-(alkylamino)isochromans: hypotensives with peripheral and central activities.
AID63493Evaluated for Adrenoceptor from guinea pig left atrium by using isoproterenol as agonist.1982Journal of medicinal chemistry, Jun, Volume: 25, Issue:6
Arylethanolamines derived from salicylamide with alpha- and beta-adrenoceptor blocking activities. Preparation of labetalol, its enantiomers, and related salicylamides.
AID4161Compound at 10E-5 M was tested in vitro for the inhibition of radioligand [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor in rat hippocampal membrane1997Journal of medicinal chemistry, Feb-14, Volume: 40, Issue:4
[[(Arylpiperazinyl)alkyl]thio]thieno[2,3-d]pyrimidinone derivatives as high-affinity, selective 5-HT1A receptor ligands.
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).
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.
AID36059In vitro for relative blocking action (pA2) of Presynaptic Alpha-2 adrenergic receptor from guinea pig ileum.1982Journal of medicinal chemistry, Jun, Volume: 25, Issue:6
Arylethanolamines derived from salicylamide with alpha- and beta-adrenoceptor blocking activities. Preparation of labetalol, its enantiomers, and related salicylamides.
AID36851Concentration of compound for 50% displacement of [3H]WB-4101 from Alpha-1 adrenergic receptor of rat brain1980Journal of medicinal chemistry, Aug, Volume: 23, Issue:8
Conformationally restricted tricyclic antidepressants. 1. Octahydrodibenzazepinonaphthyridines as rigid imipramine analogues.
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).
AID173770In vivo threshold intravenous dose required to cause reversal of clonidine on hypogastric nerves in pithed rat1982Journal of medicinal chemistry, Jul, Volume: 25, Issue:7
Synthesis of some potential antihypertensive phthalazinyl- and quinoxalinylguanidines.
AID33142Evaluated for norepinephrine as agonist.1982Journal of medicinal chemistry, Jun, Volume: 25, Issue:6
Arylethanolamines derived from salicylamide with alpha- and beta-adrenoceptor blocking activities. Preparation of labetalol, its enantiomers, and related salicylamides.
AID60615Relative adrenoceptor blocking activity (DR10) was recorded for the antagonism of Isoproterenol-induced responses in Vasodepression in beta2-Adrenoceptor blockade.1982Journal of medicinal chemistry, Jun, Volume: 25, Issue:6
Arylethanolamines derived from salicylamide with alpha- and beta-adrenoceptor blocking activities. Preparation of labetalol, its enantiomers, and related salicylamides.
AID63690Ability to displace [3H]YM-09151-2 (0.06 nM) from CHO cells of human Dopamine receptor D4; NT=not tested2003Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2
Synthesis and structure-affinity relationship investigations of 5-heteroaryl-substituted analogues of the antipsychotic sertindole. A new class of highly selective alpha(1) adrenoceptor antagonists.
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).
AID181469Percentage fall in systolic blood pressure in spontaneously hypertensive rats after 2 hr following 50 mg/kg p.o.1981Journal of medicinal chemistry, Nov, Volume: 24, Issue:11
Synthesis and antihypertensive activity of a series of 8-substituted 1-oxa-3,8-diazaspiro[4.5]decan-2-ones.
AID33144In vitro postsynaptic antagonist activity against Alpha adrenergic receptor in rat anococcygeus muscle1982Journal of medicinal chemistry, Jul, Volume: 25, Issue:7
Synthesis of some potential antihypertensive phthalazinyl- and quinoxalinylguanidines.
AID671058Displacement of [3H]prazosin from alpha1 adrenoceptor in rat cerebral cortex after 30 mins by beta scintillation counting2012Bioorganic & medicinal chemistry, Jul-15, Volume: 20, Issue:14
Synthesis and SAR-study for novel arylpiperazine derivatives of 5-arylidenehydantoin with α₁-adrenoceptor antagonistic properties.
AID36706Alpha-1-adrenolytic activity was assessed from the ability to inhibit [3H]prazosin binding to rat cerebral cortex preparation1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
New 1,4-dihydropyridine derivatives combining calcium antagonism and alpha-adrenolytic properties.
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).
AID36231Binding affinity against Alpha-2B adrenergic receptor from human clones.1995Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification.
AID181479Antihypertensive activity as percentage fall in systolic blood pressure in spontaneously hypertensive rats after a period of 4 hr for a dose of 50 mg/kg po1981Journal of medicinal chemistry, Nov, Volume: 24, Issue:11
Synthesis and antihypertensive activity of a series of 8-substituted 1-oxa-3,8-diazaspiro[4.5]decan-2-ones.
AID35904Binding affinity against alpha-2 adrenergic receptor from calf cerebral cortex, using [3H]clonidine as the radioligand1983Journal of medicinal chemistry, Dec, Volume: 26, Issue:12
alpha-Adrenergic activities of some substituted 2-(aminomethyl)imidazolines.
AID191917Antihypertensive activity in DOCA/saline rat dosed at 50 mg/kg, po expressed as percent rise in heart rate after 2 h1983Journal of medicinal chemistry, Mar, Volume: 26, Issue:3
synthesis and antihypertensive activity of 2-sulfonamido- and 2-sulfamido-1,3,4,6,7,11b alpha-hexahydro-2H-benzo[a]quinolizines.
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).
AID699069Displacement of [3H]prazoin from rat cerebral cortex adrenergic alpha1 receptor2012Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
Investigations on the 1-(2-biphenyl)piperazine motif: identification of new potent and selective ligands for the serotonin(7) (5-HT(7)) receptor with agonist or antagonist action in vitro or ex vivo.
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.
AID235865Index of alpha1/alpha2 adrenoceptor antagonist selectivity at pre and postsynaptic sites in vitro.1984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists.
AID170701Percent change of mean arterial blood pressure in conscious DOCA Hypertensive rat at 22 hour, after administration of dose 10 mL (mg/kg po)1982Journal of medicinal chemistry, Jul, Volume: 25, Issue:7
Synthesis of some potential antihypertensive phthalazinyl- and quinoxalinylguanidines.
AID36774Alpha-2 adrenergic receptor activity was assessed from the ability to inhibit [3H]yohimbine binding to rat cerebral cortex preparation1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
New 1,4-dihydropyridine derivatives combining calcium antagonism and alpha-adrenolytic properties.
AID697787Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting2012Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
Shape-based reprofiling of FDA-approved drugs for the H₁ histamine receptor.
AID36433In vitro relative blocking action (pA2) of the post-synaptic alpha-1-adrenoceptor from rat and rabbit aorta.1982Journal of medicinal chemistry, Jun, Volume: 25, Issue:6
Arylethanolamines derived from salicylamide with alpha- and beta-adrenoceptor blocking activities. Preparation of labetalol, its enantiomers, and related salicylamides.
AID41613The compound was tested for the concentration to inhibit 50% of Beta adrenergic receptor isolated from rat ventricle homogenates; ND=not determined1998Journal of medicinal chemistry, May-07, Volume: 41, Issue:10
Synthesis and adrenergic activity of a new series of N-aryl dicyclopropyl ketone oxime ethers: SAR and stereochemical aspects.
AID33143Evaluated for norepinephrine as agonist.1982Journal of medicinal chemistry, Jun, Volume: 25, Issue:6
Arylethanolamines derived from salicylamide with alpha- and beta-adrenoceptor blocking activities. Preparation of labetalol, its enantiomers, and related salicylamides.
AID170703Percent change of mean arterial blood pressure in conscious DOCA Hypertensive rat at 5 hour, after administration of dose 10 mL (mg/kg po)1982Journal of medicinal chemistry, Jul, Volume: 25, Issue:7
Synthesis of some potential antihypertensive phthalazinyl- and quinoxalinylguanidines.
AID196987Antagonist activity against B-HT 933-induced alpha-2-adrenoceptor-mediated vasoconstriction in pithed normotensive rats1984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists.
AID170695Percent change of heart rate in conscious DOCA Hypertensive rat at 5 hour after administration of dose of 10 mL (mg/kg po)1982Journal of medicinal chemistry, Jul, Volume: 25, Issue:7
Synthesis of some potential antihypertensive phthalazinyl- and quinoxalinylguanidines.
AID254386Binding affinity towards alpha-1A adrenergic receptor expressed in human embryonic kidney (HEK293) cells2005Bioorganic & medicinal chemistry letters, Nov-01, Volume: 15, Issue:21
Bioisosteric phentolamine analogs as potent alpha-adrenergic antagonists.
AID1449628Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
AID1636440Drug activation in human Hep3B cells assessed as human CYP2D6-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 300 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.
AID36866In vitro inhibitory concentration against radioligand [3H]prazosin binding to alpha-1 adrenergic receptor in rat cortical membrane.1997Journal of medicinal chemistry, Feb-14, Volume: 40, Issue:4
[[(Arylpiperazinyl)alkyl]thio]thieno[2,3-d]pyrimidinone derivatives as high-affinity, selective 5-HT1A receptor ligands.
AID1126943Displacement of [3H]prazosin from alpha1 adrenergic receptor in rat cerebral cortex after 30 mins by Microbeta scintillation counting analysis2014European journal of medicinal chemistry, May-06, Volume: 78SAR-studies on the importance of aromatic ring topologies in search for selective 5-HT(7) receptor ligands among phenylpiperazine hydantoin derivatives.
AID36170The compound was tested for the concentration to inhibit 50% of Alpha-1 adrenergic receptor isolated from rat ventricle homogenates.1998Journal of medicinal chemistry, May-07, Volume: 41, Issue:10
Synthesis and adrenergic activity of a new series of N-aryl dicyclopropyl ketone oxime ethers: SAR and stereochemical aspects.
AID173769In vivo threshold intravenous dose required to cause reversal of clonidine on blood pressure in pithed rat1982Journal of medicinal chemistry, Jul, Volume: 25, Issue:7
Synthesis of some potential antihypertensive phthalazinyl- and quinoxalinylguanidines.
AID36053Affinity (Kbeta) to alpha-2-adrenergic receptor was determined in guinea pig atrium1984Journal of medicinal chemistry, Jul, Volume: 27, Issue:7
Development of an affinity ligand for purification of alpha 2-adrenoceptors from human platelet membranes.
AID1322297Displacement of [3H]clonidine from alpha2 adrenergic receptor in rat brain cerebral cortex at 50 uM after 25 mins by microbeta scintillation counting method
AID170700Percent change of mean arterial blood pressure in conscious DOCA Hypertensive rat at 2 hour, after administration of dose 10 mL (mg/kg po)1982Journal of medicinal chemistry, Jul, Volume: 25, Issue:7
Synthesis of some potential antihypertensive phthalazinyl- and quinoxalinylguanidines.
AID4264Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor; NT=not tested2003Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2
Synthesis and structure-affinity relationship investigations of 5-heteroaryl-substituted analogues of the antipsychotic sertindole. A new class of highly selective alpha(1) adrenoceptor antagonists.
AID203852The compound was tested for affinity towards sigma-3 receptor1994Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24
Conformational analysis, pharmacophore identification, and comparative molecular field analysis of ligands for the neuromodulatory sigma 3 receptor.
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.
AID35864Antagonistic activity against postsynaptic Alpha-1 adrenergic receptor in isolated rat vas deferens using (-)-phenylephrine as agonist1987Journal of medicinal chemistry, Aug, Volume: 30, Issue:8
Berbanes: a new class of selective alpha 2-adrenoceptor antagonists.
AID58337Percent inhibition of the pressor responses to 1 ug/kg iv Epinephrine in pentobarbital-anesthetized dogs for a dose of 0.1 mg/kg1981Journal of medicinal chemistry, Nov, Volume: 24, Issue:11
Synthesis and antihypertensive activity of a series of 8-substituted 1-oxa-3,8-diazaspiro[4.5]decan-2-ones.
AID58340Percent inhibition of the pressor responses to 7.5 ug/kg iv phenylephrine in pentobarbital-anesthetized dogs for a dose of 0.1 mg/kg1981Journal of medicinal chemistry, Nov, Volume: 24, Issue:11
Synthesis and antihypertensive activity of a series of 8-substituted 1-oxa-3,8-diazaspiro[4.5]decan-2-ones.
AID41476The compound was tested for the concentration to inhibit 50% of Beta-2 adrenergic receptor isolated from rat lung homogenates; ND=not determined1998Journal of medicinal chemistry, May-07, Volume: 41, Issue:10
Synthesis and adrenergic activity of a new series of N-aryl dicyclopropyl ketone oxime ethers: SAR and stereochemical aspects.
AID239801Binding affinity for alpha 1d adrenoceptor2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Range and sensitivity as descriptors of molecular property spaces in dynamic QSAR analyses.
AID79688The compound was tested for inotropic effect in electrically driven left atrial preparation (Atria isolated from guinea pig) and is expressed in pA2; ND=not determined1998Journal of medicinal chemistry, May-07, Volume: 41, Issue:10
Synthesis and adrenergic activity of a new series of N-aryl dicyclopropyl ketone oxime ethers: SAR and stereochemical aspects.
AID36637Compound was tested for the inhibition of [3H]prazosin binding Alpha-1 adrenergic receptor of crude rat brain membrane.1982Journal of medicinal chemistry, Jan, Volume: 25, Issue:1
1-(alkylamino)isochromans: hypotensives with peripheral and central activities.
AID1636357Drug activation in human Hep3B cells assessed as human CYP3A4-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 300 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.
AID1380705Displacement of [3H]prazosin from recombinant human alpha1 adrenoceptor expressed in CHO cell membranes after 30 mins by liquid scintillation counting method
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).
AID36639Alpha-2 adrenergic receptor pA2 value against clonidine in vitro experiment in rat vas deferens1983Journal of medicinal chemistry, Jun, Volume: 26, Issue:6
alpha-adrenoreceptor reagents. 1. Synthesis of some 1,4-benzodioxans as selective presynaptic alpha 2-adrenoreceptor antagonists and potential antidepressants.
AID35574Ratio of alpha1, alpha2 adrenoceptor antagonistic activity was expressed as slelctivity ratio1981Journal of medicinal chemistry, Nov, Volume: 24, Issue:11
Synthesis and antihypertensive activity of a series of 8-substituted 1-oxa-3,8-diazaspiro[4.5]decan-2-ones.
AID3866Ability to displace [3H]5-CT (2.0 nM) from HeLa cells of human 5-hydroxytryptamine 1A receptor; NT=not tested2003Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2
Synthesis and structure-affinity relationship investigations of 5-heteroaryl-substituted analogues of the antipsychotic sertindole. A new class of highly selective alpha(1) adrenoceptor antagonists.
AID1136068Vasodilatory activity in dog assessed as increase of femoral blood flow by 100 mL/min administered as intraarterially1979Journal of medicinal chemistry, Dec, Volume: 22, Issue:12
Derivatives of 1,3-disubstituted 2,4(1H,3H)-quinazolinediones as possible peripheral vasodilators or antihypertensive agents.
AID33117Relative adrenoceptor blocking activity (DR10) was recorded for the antagonism of Phenylephrine-induced vasopressor responses in alpha-Adrenoceptor blockade in anesthetized dog1982Journal of medicinal chemistry, Jun, Volume: 25, Issue:6
Arylethanolamines derived from salicylamide with alpha- and beta-adrenoceptor blocking activities. Preparation of labetalol, its enantiomers, and related salicylamides.
AID59020Change in mean arterial pressure in anesthetized dogs for a dose of 1 mg/kg1981Journal of medicinal chemistry, Nov, Volume: 24, Issue:11
Synthesis and antihypertensive activity of a series of 8-substituted 1-oxa-3,8-diazaspiro[4.5]decan-2-ones.
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).
AID37056Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay1997Journal of medicinal chemistry, Aug-15, Volume: 40, Issue:17
N-arylpiperazinyl-N'-propylamino derivatives of heteroaryl amides as functional uroselective alpha 1-adrenoceptor antagonists.
AID170694Percent change of heart rate in conscious DOCA Hypertensive rat at 3 hour after administration of dose of 10 mL (mg/kg po)1982Journal of medicinal chemistry, Jul, Volume: 25, Issue:7
Synthesis of some potential antihypertensive phthalazinyl- and quinoxalinylguanidines.
AID33262Tested for alpha adrenergic receptor agonistic activity on isolated rat vas deferens1983Journal of medicinal chemistry, Feb, Volume: 26, Issue:2
Conformational effects on the activity of drugs. 10. Synthesis, conformation, and pharmacological properties of 1-(2,5-dimethoxyphenyl)-2-aminoethanols and their morpholine analogues.
AID36281Antagonistic activity against postsynaptic alpha-1 adrenergic receptor in rabbit pulmonary artery using l-norepinephrine as agonist1987Journal of medicinal chemistry, Aug, Volume: 30, Issue:8
Berbanes: a new class of selective alpha 2-adrenoceptor antagonists.
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.
AID36455Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells2003Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2
Synthesis and structure-affinity relationship investigations of 5-heteroaryl-substituted analogues of the antipsychotic sertindole. A new class of highly selective alpha(1) adrenoceptor antagonists.
AID1636356Drug activation in human Hep3B cells assessed as human CYP2C9-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 300 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.
AID36277Relative potency was determined with respect to Yohimbine against alpha-1 adrenergic receptor1987Journal of medicinal chemistry, Aug, Volume: 30, Issue:8
Berbanes: a new class of selective alpha 2-adrenoceptor antagonists.
AID1322298Displacement of [3H]CGP-12177 from beta1 adrenergic receptor in rat brain cerebral cortex at 50 uM after 60 mins by microbeta scintillation counting method
AID342860Displacement of [125I]PIC from human alpha2 adrenoceptors expressed in CHO cells2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
QSAR study of imidazoline antihypertensive drugs.
AID255429Potency against alpha-1D adrenergic receptor is determined by phenylephrine-induced contractions in rat2005Bioorganic & medicinal chemistry letters, Nov-01, Volume: 15, Issue:21
Bioisosteric phentolamine analogs as potent alpha-adrenergic antagonists.
AID588220Literature-mined public compounds from Kruhlak et al phospholipidosis modelling dataset2008Toxicology mechanisms and methods, , Volume: 18, Issue:2-3
Development of a phospholipidosis database and predictive quantitative structure-activity relationship (QSAR) models.
AID33145In vitro presynaptic antagonist activity against Alpha adrenergic receptor in rat vas deferens1982Journal of medicinal chemistry, Jul, Volume: 25, Issue:7
Synthesis of some potential antihypertensive phthalazinyl- and quinoxalinylguanidines.
AID1443987Inhibition of recombinant human BSEP expressed in baculovirus infected sf21 cell membrane vesicles assessed as reduction in ATP-dependent [3H]-taurocholate uptake in to vesicles after 5 mins by TopCount method2014Hepatology (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.
AID194147Distribution coefficient between 1-Octanol and phosphate buffer at pH7.41981Journal of medicinal chemistry, Nov, Volume: 24, Issue:11
Synthesis and antihypertensive activity of a series of 8-substituted 1-oxa-3,8-diazaspiro[4.5]decan-2-ones.
AID239799Binding affinity for alpha 1a adrenoceptor2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Range and sensitivity as descriptors of molecular property spaces in dynamic QSAR analyses.
AID227718Binding energy by using the equation deltaG obsd = -RT ln KD1984Journal of medicinal chemistry, Dec, Volume: 27, Issue:12
Functional group contributions to drug-receptor interactions.
AID36057Antagonistic activity against adrenergic alpha-2 receptor in longitudinal muscle strip of the guinea pig ileum using l-norepinephrine as agonist1987Journal of medicinal chemistry, Aug, Volume: 30, Issue:8
Berbanes: a new class of selective alpha 2-adrenoceptor antagonists.
AID36466In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor1997Journal of medicinal chemistry, Aug-15, Volume: 40, Issue:17
N-arylpiperazinyl-N'-propylamino derivatives of heteroaryl amides as functional uroselective alpha 1-adrenoceptor antagonists.
AID58338Percent inhibition of the pressor responses to 1 ug/kg iv Epinephrine in pentobarbital-anesthetized dogs for a dose of 1 mg/kg1981Journal of medicinal chemistry, Nov, Volume: 24, Issue:11
Synthesis and antihypertensive activity of a series of 8-substituted 1-oxa-3,8-diazaspiro[4.5]decan-2-ones.
AID188458Compound was tested for alpha-adrenoceptor blocking activity by its ability to antagonize norepinephrine contraction in the rat thoracic aorta1983Journal of medicinal chemistry, Mar, Volume: 26, Issue:3
Pyrimidine derivatives. 4. Synthesis and antihypertensive activity of 4-amino-2-(4-cinnamoylpiperazino)-6,7-dimethoxyquinazoline derivatives.
AID759363Displacement of [3H]prazosin from alpha1-adrenergic receptor in rat cerebral cortex after 30 mins by scintillation counting2013Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15
Synthesis and evaluation of pharmacological properties of some new xanthone derivatives with piperazine moiety.
AID35363Antagonistic potency of compound for Alpha-2 adrenergic receptor1981Journal of medicinal chemistry, Nov, Volume: 24, Issue:11
Synthesis and antihypertensive activity of a series of 8-substituted 1-oxa-3,8-diazaspiro[4.5]decan-2-ones.
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.
AID1353523Displacement of [3H]-prazosin from alpha1-adrenergic receptor in rat brain cortex after 30 mins by Microbeta scintillation counting method2018European journal of medicinal chemistry, Mar-10, Volume: 147Computer-aided insights into receptor-ligand interaction for novel 5-arylhydantoin derivatives as serotonin 5-HT
AID166854Antagonist activity against norepinephrine-induced alpha-2-adrenoceptor-mediated vasoconstriction of rabbit isolated pulmonary artery.1984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists.
AID35359Antagonistic activity against Alpha-2 adrenergic receptor in the prostatic portion of the rat vas deferens1982Journal of medicinal chemistry, Jun, Volume: 25, Issue:6
Structure-activity relationships for 2-substituted imidazoles as alpha 2-adrenoceptor antagonists.
AID218825Ratio of pA2 value against alpha-2 to alpha1 adrenoceptor1983Journal of medicinal chemistry, Jun, Volume: 26, Issue:6
alpha-adrenoreceptor reagents. 1. Synthesis of some 1,4-benzodioxans as selective presynaptic alpha 2-adrenoreceptor antagonists and potential antidepressants.
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.
AID63630Ability to displace [3H]spiperone (0.5 nM) from corpus striatum of rat Dopamine receptor D2; NT=not tested2003Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2
Synthesis and structure-affinity relationship investigations of 5-heteroaryl-substituted analogues of the antipsychotic sertindole. A new class of highly selective alpha(1) adrenoceptor antagonists.
AID1229076Displacement of [3H]-Prazosin from human alpha-1B adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis2015ACS medicinal chemistry letters, May-14, Volume: 6, Issue:5
Discovery of Quinazoline-Based Fluorescent Probes to α1-Adrenergic Receptors.
AID235864Index of alpha1/alpha2 adrenoceptor antagonist selectivity at post junctional vascular sites in vivo.1984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists.
AID1136069Antihypertensive activity in Wistar rat assessed as decrease of systolic blood pressure at 31 mg/kg, po up to 8 hrs1979Journal of medicinal chemistry, Dec, Volume: 22, Issue:12
Derivatives of 1,3-disubstituted 2,4(1H,3H)-quinazolinediones as possible peripheral vasodilators or antihypertensive agents.
AID1823833Displacement of [3H]-pyrilamine from human recombinant histamine H1 receptor expressed in human recombinant CHO-K1 cells at 1 uM incubated for 60 mins by solid scintillation counting method relative to control
AID1322293Displacement of [3H]prazosin from alpha1 adrenergic receptor in rat brain cerebral cortex after 30 mins by microbeta scintillation counting method
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.
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.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
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.
AID588378qHTS for Inhibitors of ATXN expression: Validation
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.
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.
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.
AID1508629Cell Viability qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1508627Counterscreen qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: GLuc-NoTag assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1508628Confirmatory 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.
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.
AID1224864HCS microscopy assay (F508del-CFTR)2016PloS one, , Volume: 11, Issue:10
Increasing the Endoplasmic Reticulum Pool of the F508del Allele of the Cystic Fibrosis Transmembrane Conductance Regulator Leads to Greater Folding Correction by Small Molecule Therapeutics.
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.
AID1159550Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening2015Nature cell biology, Nov, Volume: 17, Issue:11
6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
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.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
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.
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.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID172166Compound was tested for antihypertensive activity in spontaneously hypertensive rats(SHR)at 50 mg/kg (po) dose after 1 h1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Salicylamide derivatives related to medroxalol with alpha- and beta-adrenergic antagonist and antihypertension activity.
AID977599Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID79378spasmolytic activity in isolated guinea pig ileum preparation;- log KB; (Bacl2)1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Salicylamide derivatives related to medroxalol with alpha- and beta-adrenergic antagonist and antihypertension activity.
AID776867Displacement of [3H]-prazosin from alpha1 adrenoceptor in Wistar Hannover rat cerebral cortex membranes after 50 mins2013European journal of medicinal chemistry, Nov, Volume: 69Development of 3,4-dihydroisoquinolin-1(2H)-one derivatives for the Positron Emission Tomography (PET) imaging of σ₂ receptors.
AID172167Compound was tested for antihypertensive activity n spontaneously hypertensive rats(SHR),at 50 mg/kg (po) dose after 4 h1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Salicylamide derivatives related to medroxalol with alpha- and beta-adrenergic antagonist and antihypertension activity.
AID33122In vitro blocking activity against alpha adrenergic receptor, isolated from rabbit aortic strip1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Salicylamide derivatives related to medroxalol with alpha- and beta-adrenergic antagonist and antihypertension activity.
AID977602Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID41321In vitro blocking activity against beta adrenergic receptor, isolated from guinea pig atria1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Salicylamide derivatives related to medroxalol with alpha- and beta-adrenergic antagonist and antihypertension activity.
AID60484In vivo sympatholytic activity (phenylephrine-induced vasopressor response) at alpha-adrenergic receptor in anesthetized dog, iv1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Salicylamide derivatives related to medroxalol with alpha- and beta-adrenergic antagonist and antihypertension activity.
AID1224864HCS microscopy assay (F508del-CFTR)2016PloS one, , Volume: 11, Issue:10
Increasing the Endoplasmic Reticulum Pool of the F508del Allele of the Cystic Fibrosis Transmembrane Conductance Regulator Leads to Greater Folding Correction by Small Molecule Therapeutics.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (8,594)

TimeframeStudies, This Drug (%)All Drugs %
pre-19906356 (73.96)18.7374
1990's1351 (15.72)18.2507
2000's579 (6.74)29.6817
2010's253 (2.94)24.3611
2020's55 (0.64)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 69.60

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 Index69.60 (24.57)
Research Supply Index9.15 (2.92)
Research Growth Index4.11 (4.65)
Search Engine Demand Index127.80 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (69.60)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials270 (2.95%)5.53%
Trials0 (0.00%)5.53%
Reviews239 (2.61%)6.00%
Reviews1 (8.33%)6.00%
Case Studies147 (1.61%)4.05%
Case Studies0 (0.00%)4.05%
Observational1 (0.01%)0.25%
Observational0 (0.00%)0.25%
Other8,484 (92.81%)84.16%
Other11 (91.67%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (38)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Reversing the Effects of 2% Lidocaine: A Randomized Controlled Trial [NCT02861378]38 participants (Actual)Interventional2015-10-31Completed
Randomized, Placebo-Controlled, Double-Masked Study of the Safety and Efficacy of Nyxol (0.75% Phentolamine Ophthalmic Solution) in Subjects With Dim Light Vision Disturbances [NCT04638660]Phase 3144 participants (Actual)Interventional2020-12-30Completed
Sex Differences in Sympathetic Vascular Reactivity at High Altitude [NCT05525416]17 participants (Actual)Interventional2022-07-28Completed
A Study of the Pharmacokinetic and Pharmacodynamic Responses in Healthy and Altered Human Cardiovascular Systems [NCT03098680]Phase 118 participants (Actual)Interventional2017-04-24Terminated(stopped due to Unable to recruit in time before end of PhD studentship)
Randomized, Parallel Arm, Double-Masked, Placebo-Controlled Study of the Safety and Efficacy of Nyxol (0.75% Phentolamine Ophthalmic Solution) to Reverse Pharmacologically-Induced Mydriasis in Healthy Subjects [NCT05134974]Phase 3368 participants (Actual)Interventional2021-11-18Completed
Comparative Study of the Effect of Diode Laser and Oraverse on Reversing the Effect of Articaine 4% Soft Tissue Anasthesia in Children [NCT05473858]Phase 340 participants (Anticipated)Interventional2021-12-10Recruiting
Phentolamine Mesylate as a Reversal of Local Anesthesics [NCT03740386]90 participants (Actual)Interventional2016-01-01Completed
Randomized, Cross-Over, Double-Masked, Placebo-Controlled Study of the Safety and Efficacy of Phentolamine Mesylate Ophthalmic Solution to Reverse Pharmacologically Induced Mydriasis in Normal Healthy Subjects [NCT04024891]Phase 232 participants (Actual)Interventional2019-08-13Completed
New Perspective on Exploring the Post-apneic Blood Pressure Surge in Patients With Obstructive Sleep Apnea [NCT06172998]Early Phase 1350 participants (Anticipated)Interventional2022-04-01Recruiting
Safety and Efficacy of Nyxol (0.75% Phentolamine Ophthalmic Solution) With Pilocarpine Eye Drops in Subjects With Presbyopia [NCT04675151]Phase 2150 participants (Actual)Interventional2021-02-15Completed
Single Dose Study of Phentolamine Mesylate Eye Drops in Patients With Severe Night Vision Disturbances [NCT04004507]Phase 224 participants (Actual)Interventional2007-08-31Completed
Randomized, Parallel Arm, Double-Masked, Placebo-Controlled Study of the Safety and Efficacy of Nyxol (0.75% Phentolamine Ophthalmic Solution) to Reverse Pharmacologically-Induced Mydriasis in Healthy Subjects [NCT04620213]Phase 3185 participants (Actual)Interventional2020-11-18Completed
Randomized, Double-Masked, Placebo-Controlled, Multicenter, Phase 3 Study of the Safety and Efficacy of Nyxol (Phentolamine Ophthalmic Solution 0.75%) as a Single Agent and With Adjunctive Low-Dose Pilocarpine Hydrochloride Ophthalmic Solution 0.4% in Sub [NCT05646719]Phase 3333 participants (Actual)Interventional2022-12-22Completed
Comparative Effect of Hypotensive Anaesthesia Using Nitroglycerine vs Phentolamine on Event Related Potentials, Quantitative Electroencephalograghy and Cognitive Function in Patients Undergoing Septoplasty [NCT04110808]Early Phase 160 participants (Anticipated)Interventional2019-10-15Not yet recruiting
ZYESAMI (Aviptadil) for the Treatment of Critical COVID-19 With Respiratory Failure [NCT04311697]Phase 2/Phase 3203 participants (Actual)Interventional2020-05-15Completed
An International Randomised Controlled Trial to Establish the Effects of Low-dose rtPA and the Effects of Early Intensive Blood Pressure Lowering in Patients With Acute Ischaemic Stroke [NCT01422616]Phase 34,587 participants (Actual)Interventional2012-03-31Completed
Randomized, Parallel Arm, Double-Masked, Placebo-Controlled Study of the Safety and Efficacy of Nyxol (0.75% Phentolamine Ophthalmic Solution) to Reverse Pharmacologically Induced Mydriasis in Healthy Pediatric Subjects [NCT05223478]Phase 323 participants (Actual)Interventional2021-12-17Completed
A Phase 4, Multicenter, Randomized, Double-Blinded, Controlled Study of OraVerse® for Safety and Efficacy in Pediatric Dental Patients Undergoing Mandibular and Maxillary Procedures [NCT01474382]Phase 4150 participants (Actual)Interventional2012-02-29Completed
Vascular Function in Health & Disease: Rehabilitation for Hypertension; Exercise and Skeletal Muscle Afferent Feedback [NCT02966665]Phase 1420 participants (Anticipated)Interventional2008-09-30Recruiting
A Phase 2, Multicenter, Randomized, Blinded, Controlled Study of NV-101 for Safety and Efficacy in Pediatric Dental Patients Undergoing Mandibular and Maxillary Procedures [NCT00309322]Phase 2150 participants Interventional2006-03-31Completed
A Phase 3, Multicenter, Randomized, Blinded, Controlled Study of NV-101 for Efficacy, Pharmacodynamics and Safety in Dental Patients Undergoing Mandibular Procedures [NCT00309361]Phase 3240 participants Interventional2006-02-28Completed
A Double-Blind, Randomized, Placebo-Controlled Study of the Efficacy and Safety of NV-101 in Dental Patients [NCT00154167]Phase 2122 participants Interventional2003-02-28Completed
Sympathetic Neurovascular Transduction: Role of Adrenergic Receptors and Sex Differences [NCT05997732]Phase 430 participants (Anticipated)Interventional2023-10-31Recruiting
The Effect of a-Adrenergic Receptor Blockade on Insulin-Stimulated Forearm Glucose Uptake and Metabolism in Chronic Heart Failure [NCT00132106]0 participants Interventional2005-08-31Recruiting
A Randomized Phase II Trial Evaluating the Importance of Early Erectile Dysfunction Rehabilitation and Unilateral Autologous Sural Nerve Sparing Radical Prostatectomy Clinically Localized Prostate Cancer [NCT00080808]Phase 2111 participants (Actual)Interventional2001-08-31Completed
A Randomised Trial to Establish the Effects of Early Intensive Blood Pressure Lowering on Death and Disability in Patients With Stroke Due to Acute Intracerebral Haemorrhage [NCT00226096]404 participants (Actual)Interventional2005-11-30Completed
Reversing the Effects of 0.5% Bupivacaine: A Randomized Controlled Trial [NCT02995291]Phase 444 participants (Actual)Interventional2017-02-10Completed
A Phase 3, Multicenter, Randomized, Blinded, Controlled Study of NV-101 for Efficacy, Pharmacodynamics and Safety in Dental Patients Undergoing Maxillary Procedures [NCT00309335]Phase 3240 participants Interventional2006-02-28Completed
Vanderbilt University Medical Center [NCT03318094]Phase 136 participants (Anticipated)Interventional2017-10-24Recruiting
Sex Disparities in Hypoxic Vasodilation and Impact of Obesity [NCT05219799]Early Phase 172 participants (Anticipated)Interventional2023-03-14Recruiting
Double-Masked Parallel Evaluation of the Safety and Efficacy of Phentolamine Mesylate Ophthalmic Solution in Subjects With Severe Night Vision Disturbances [NCT01703559]Phase 260 participants (Actual)Interventional2011-09-09Completed
A Randomized Effectiveness of Phentolamine Mesylate as a Reversing Agent for Local Anesthesia in Decreasing Self- Inflicted Soft Tissue Trauma Following Local Anaesthesia Injection for Dental Procedure in Children: Randomized Clinical Trial [NCT05448807]Phase 380 participants (Anticipated)Interventional2022-10-31Not yet recruiting
Adrenergic Contribution to Glucose Counterregulation in Islet Transplantation [NCT03079921]Early Phase 111 participants (Actual)Interventional2017-01-20Active, not recruiting
Comparison Between the Use of Phentolamine Versus Glyceryl Trinitrate for Their Effect on Renal Function in Pre-eclampsia Patients in ICU [NCT05687669]Phase 4170 participants (Anticipated)Interventional2023-01-12Not yet recruiting
A Multicenter, Adaptive, Randomized, Blinded Controlled Trial of the Safety and Efficacy of Investigational Therapeutics for Hospitalized Patients With Acute Respiratory Distress Syndrome Associated With COVID-19 [NCT04843761]Phase 3473 participants (Actual)Interventional2021-04-20Completed
Sex Disparities in Hypoxic Sympatholysis and Impact of Obesity [NCT04436731]Early Phase 1104 participants (Anticipated)Interventional2020-12-09Recruiting
An International Randomised Controlled Trial to Establish the Effects of Early Intensive Blood Pressure Lowering in Patients With Intracerebral Haemorrhage. [NCT00716079]2,839 participants (Actual)Interventional2008-09-30Completed
Randomized, Placebo-Controlled, Double-Masked Study of the Safety and Efficacy of Phentolamine Mesylate Ophthalmic Solution in Subjects With Open Angle Glaucoma or Ocular Hypertension [NCT03960866]Phase 239 participants (Actual)Interventional2019-05-28Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00716079 (2) [back to overview]A Composite of Death or Dependency, With Dependency Being Defined by a Score of 3 to 5 on the Modified Rankin Scale (mRS)
NCT00716079 (2) [back to overview]Death at 90 Days
NCT03960866 (3) [back to overview]Pupil Diameter
NCT03960866 (3) [back to overview]Distance Visual Acuity
NCT03960866 (3) [back to overview]Intraocular Pressure
NCT04024891 (7) [back to overview]Best Corrected Distance Visual Acuity (BCDVA) Measured by Early Treatment Diabetic Retinopathy Study (ETDRS) Light Box Chart (Letters) at 4 Meters (Change From Baseline)
NCT04024891 (7) [back to overview]Pupil Diameter (Change From Max)
NCT04024891 (7) [back to overview]Conjunctival Hyperemia (Eye Redness) Assessed Visually With the Brien Holden Vision Institute (Formerly Corneal and Contact Lens Research Unit, or CCLRU) Bulbar Redness Scale (0-3)
NCT04024891 (7) [back to overview]Distance-Corrected Near Visual Acuity (DCNVA) Measured by Standard Reading Card (Original Series Sloan Letter ETDRS Card at 16 Inches, LogMAR Units) (Change From Baseline)
NCT04024891 (7) [back to overview]Pupil Diameter (Change From Max)
NCT04024891 (7) [back to overview]Pupil Diameter Return to Baseline
NCT04024891 (7) [back to overview]Accommodation Measured by the Near Point Rule (Diopters) (Change From Baseline), Percent With Unchanged Accommodation
NCT04311697 (5) [back to overview]Change in IL-6
NCT04311697 (5) [back to overview]Resolution of Respiratory Failure (Alive and Free of Respiratory Failure)
NCT04311697 (5) [back to overview]Oxygenation Index as Measured by PaO2:FiO2 Ratio
NCT04311697 (5) [back to overview]Number of Participants Achieving a Score of 6-8 on NIAID Ordinal Score Through Day 60
NCT04311697 (5) [back to overview]Number of Participants Alive at Day 60
NCT04620213 (4) [back to overview]Percent of Subjects With Unchanged Accommodation From Baseline
NCT04620213 (4) [back to overview]Pupil Diameter (Change From Max)
NCT04620213 (4) [back to overview]Percent of Subjects' Study Eyes With Pupil Diameter Returning to Baseline
NCT04620213 (4) [back to overview]Percent of Subjects' Study Eyes Pupil Diameter Returning to Baseline
NCT04638660 (5) [back to overview]Percent of Subjects With 3 Lines mLCVA Improvement in Study Eye
NCT04638660 (5) [back to overview]Change From Baseline in Study Eye Mesopic Pupil Diameter (PD)
NCT04638660 (5) [back to overview]Percent Change From Baseline in Study Eye Mesopic Pupil Diameter (PD)
NCT04638660 (5) [back to overview]Percent of Subjects With mLCVA Improvement in Study Eye
NCT04638660 (5) [back to overview]Percent of Subjects With Photopic Low Contrast Visual Acuity (pLCVA) and mHCVA Improvement in Study Eye
NCT04675151 (4) [back to overview]Percent of Subjects With ≥ 15 Letters of Improvement in Photopic Binocular DCNVA
NCT04675151 (4) [back to overview]Percentage of Subjects With Improvement of ≥ 5, ≥ 10, and ≥ 15 Letters in DCNVA (Photopic) From Baseline
NCT04675151 (4) [back to overview]Percentage of Subjects With Improvement in DCIVA (Photopic) From Baseline
NCT04675151 (4) [back to overview]Percentage of Subjects With Improvement of ≥ 15 Letters in DCNVA (Photopic) at 1 Hour and With < 5 Letters of Loss in Photopic Binocular BCDVA From Baseline
NCT05134974 (4) [back to overview]Percent of Subjects' Study Eyes With Pupil Diameter Returning to Baseline
NCT05134974 (4) [back to overview]Percent of Subjects With Unchanged Accommodation From Baseline
NCT05134974 (4) [back to overview]Pupil Diameter (Change From Max)
NCT05134974 (4) [back to overview]Change From Baseline in Best-Corrected Distance Visual Acuity (BCDVA) Under Normal Photopic Lighting Without Glare Conditions
NCT05223478 (8) [back to overview]Efficacy Measurement: Pupil Diameter
NCT05223478 (8) [back to overview]Change From Screening Blood Pressure (Diastolic)
NCT05223478 (8) [back to overview]Efficacy Measurement: Pupil Diameter
NCT05223478 (8) [back to overview]Safety Measurement
NCT05223478 (8) [back to overview]Safety Measurements
NCT05223478 (8) [back to overview]Vital Signs
NCT05223478 (8) [back to overview]Efficacy Measurement: Pupil Diameter
NCT05223478 (8) [back to overview]Vital Signs

A Composite of Death or Dependency, With Dependency Being Defined by a Score of 3 to 5 on the Modified Rankin Scale (mRS)

(NCT00716079)
Timeframe: 90 days

Interventionparticipants (Number)
Intensive Blood-Pressure Lowering719
Guideline-Recommended Blood-Pressure Lowering785

[back to top]

Death at 90 Days

(NCT00716079)
Timeframe: 90 days

Interventionparticipants (Number)
Intensive Blood-Pressure Lowering166
Guideline-Recommended Blood-Pressure Lowering170

[back to top]

Pupil Diameter

Change from Baseline Pupil Diameter (Photopic Conditions) (NCT03960866)
Timeframe: 15 days

,
Interventionmm (Mean)
Day 8 (8AM)Day 15 (8AM)
Nyxol Ophthalmic Solution 1%-0.77-0.77
Nyxol Ophthalmic Solution Vehicle-0.07-0.01

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Distance Visual Acuity

Percentage of Subjects Achieving ≥1 line improvement in Distance Visual Acuity from Baseline measured at 4 meters (photopic conditions) (NCT03960866)
Timeframe: 15 days

InterventionParticipants (Count of Participants)
Nyxol Ophthalmic Solution 1%12
Nyxol Ophthalmic Solution Vehicle4

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Intraocular Pressure

change from Baseline in mean diurnal IOP in the study eye (NCT03960866)
Timeframe: 15 days

InterventionmmHg (Mean)
Nyxol Ophthalmic Solution 1%-2.30
Nyxol Ophthalmic Solution Vehicle-2.18

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Best Corrected Distance Visual Acuity (BCDVA) Measured by Early Treatment Diabetic Retinopathy Study (ETDRS) Light Box Chart (Letters) at 4 Meters (Change From Baseline)

Change from baseline (-1 hour) in Best Corrected Distance Visual Acuity at each time point (0 min, 30 mins, 1 hour, 2 hours, 6 hours) in Study Eye (NCT04024891)
Timeframe: 0 mins, 30 mins, 1 hour, 2 hours, 4 hours, 6 hours

,
InterventionLetters Read (Mean)
0 mins30 mins1 hour2 hours4 hours6 hours
Phentolamine Mesylate Ophthalmic Solution 1%-0.45-0.550.290.651.060.45
Phentolamine Mesylate Ophthalmic Solution Vehicle-0.81-0.55-0.100.160.100.90

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Pupil Diameter (Change From Max)

Change in pharmacologically-induced mydriatic (maximum) pupil diameter at 2 hours post-treatment in the study eye. (NCT04024891)
Timeframe: 2 hours

Interventionmm (Least Squares Mean)
Phentolamine Mesylate Ophthalmic Solution 1%-1.69
Phentolamine Mesylate Ophthalmic Solution Vehicle-0.69

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Conjunctival Hyperemia (Eye Redness) Assessed Visually With the Brien Holden Vision Institute (Formerly Corneal and Contact Lens Research Unit, or CCLRU) Bulbar Redness Scale (0-3)

Conjunctival hyperemia at each timepoint (0 min, 30 min, 1 hour, 2 hours, 4 hours, 6 hours), for study eye; in all subjects. Scale 0-3 (None, Mild, Moderate, Severe) (NCT04024891)
Timeframe: 0 min, 30 min, 1 hour, 2 hours, 4 hours, 6 hours

,
Interventionscore on a scale (0-3) (Mean)
Baseline (-1 hr)0 min30 min1 hr2 hr4 hr6 hr
Phentolamine Mesylate Ophthalmic Solution 1%0.450.231.521.551.421.100.81
Phentolamine Mesylate Ophthalmic Solution Vehicle0.350.290.420.450.450.420.35

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Distance-Corrected Near Visual Acuity (DCNVA) Measured by Standard Reading Card (Original Series Sloan Letter ETDRS Card at 16 Inches, LogMAR Units) (Change From Baseline)

Change from baseline (-1 hour) in Distance Corrected Near Visual Acuity at each time point (0 min, 30 mins, 1 hour, 2 hours, 6 hours) in Study Eye (NCT04024891)
Timeframe: 0 mins, 30 mins, 1 hour, 2 hours, 4 hours, 6 hours

,
InterventionLogMar (Mean)
0 mins30 mins1 hour2 hours4 hours6 hours
Phentolamine Mesylate Ophthalmic Solution 1%0.140.090.050.030.00-0.02
Phentolamine Mesylate Ophthalmic Solution Vehicle0.130.090.070.000.010.00

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Pupil Diameter (Change From Max)

Change in pharmacologically-induced mydriatic (maximum) pupil diameter at remaining timepoints (30 min, 1 hours, 4 hours, 6 hours) (NCT04024891)
Timeframe: 30 min, 1 hours, 4 hours, 6 hours

,
Interventionmm (Least Squares Mean)
30 minutes1 hour4 hours6 hours
Phentolamine Mesylate Ophthalmic Solution 1%-0.06-0.77-2.83-3.24
Phentolamine Mesylate Ophthalmic Solution Vehicle-0.13-0.29-1.69-2.54

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Pupil Diameter Return to Baseline

Percent of Subjects Achieving Pupil Diameter No More Than 0.5 mm Above Baseline by Time Point with either phenylephrine or tropicamide (NCT04024891)
Timeframe: 0 min, 1 hour, 2 hours, 4 hours, 6 hours

,
InterventionParticipants (Count of Participants)
0 min1 hour2 hour4 hour6 hour
Phentolamine Mesylate Ophthalmic Solution 1%26112431
Phentolamine Mesylate Ophthalmic Solution Vehicle3361228

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Accommodation Measured by the Near Point Rule (Diopters) (Change From Baseline), Percent With Unchanged Accommodation

"Change from baseline (-1 hour) in accommodation at each time point (0 min, 2 hours, 4 hours) with Tropicamide and Phenylephrine~Worsening of accommodation is defined as an amplitude decrease of greater than 1 diopter compared to baseline" (NCT04024891)
Timeframe: 0 min, 2 hours, 4 hours

InterventionParticipants (Count of Participants)
Dilated with Tropicamide, 0 min72524499Dilated with Tropicamide, 0 min72524500Dilated with Tropicamide, 2 hr72524499Dilated with Tropicamide, 2 hr72524500Dilated with Tropicamide, 4 hr72524499Dilated with Tropicamide, 4 hr72524500Dilated with Phenylephrine, 0 min72524499Dilated with Phenylephrine, 0 min72524500Dilated with Phenylephrine, 2 hr72524499Dilated with Phenylephrine, 2 hr72524500Dilated with Phenylephrine, 4 hr72524499Dilated with Phenylephrine, 4 hr72524500
Unchanged AccommodationChanged Accommodation (≥1 D)
Phentolamine Mesylate Ophthalmic Solution 1%13
Phentolamine Mesylate Ophthalmic Solution Vehicle14
Phentolamine Mesylate Ophthalmic Solution 1%7
Phentolamine Mesylate Ophthalmic Solution Vehicle3
Phentolamine Mesylate Ophthalmic Solution 1%9
Phentolamine Mesylate Ophthalmic Solution 1%11
Phentolamine Mesylate Ophthalmic Solution Vehicle7
Phentolamine Mesylate Ophthalmic Solution 1%5
Phentolamine Mesylate Ophthalmic Solution Vehicle9
Phentolamine Mesylate Ophthalmic Solution 1%10
Phentolamine Mesylate Ophthalmic Solution Vehicle11
Phentolamine Mesylate Ophthalmic Solution Vehicle4
Phentolamine Mesylate Ophthalmic Solution Vehicle13
Phentolamine Mesylate Ophthalmic Solution 1%4
Phentolamine Mesylate Ophthalmic Solution Vehicle2
Phentolamine Mesylate Ophthalmic Solution 1%12
Phentolamine Mesylate Ophthalmic Solution 1%3

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Change in IL-6

Change in IL-6, an inflammatory marker (NCT04311697)
Timeframe: Day 28

InterventionIL-6 picogram/mL (Mean)
Aviptadil IV in Escalating Doses + Standard of Care19.8
Placebo + Standard of Care23.5

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Resolution of Respiratory Failure (Alive and Free of Respiratory Failure)

Participant is Alive and Free of Respiratory Failure (without subsequent relapse over 7 days) determined as no longer requiring acute care or more than low flow oxygen (NCT04311697)
Timeframe: Day 28

InterventionParticipants (Count of Participants)
Aviptadil IV in Escalating Doses + Standard of Care72
Placebo + Standard of Care33

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Oxygenation Index as Measured by PaO2:FiO2 Ratio

oxygenation index (also known as Respiratory Distress Ratio) as measured by PaO2:FiO2 ratio (Respiratory Distress while on mechanical ventilation). RDR: PaO2:FiO2 represents an intermediate clinical endpoint that is known to be predictive of survival. RDR can only be measured in patients on mechanical ventilation because of its reliance on arterial blood gas measurements that are not routinely collected in non-intubated patients. A higher score indicates a better clinical outcome. (NCT04311697)
Timeframe: Day 7

InterventionPaO2:FiO2 ratio (Mean)
Aviptadil IV in Escalating Doses + Standard of Care139.2
Placebo + Standard of Care116.2

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Number of Participants Achieving a Score of 6-8 on NIAID Ordinal Score Through Day 60

Achievement of score 6-8 on NIAID Ordinal Scale through day 60 The NIAID score is the patient's status on the following 8-point scale:1)Death2)Hospitalized, on invasive mechanical ventilation or extracorporeal membrane oxygenation (ECMO),3)Hospitalized, on non-invasive ventilation or high flow oxygen devices4)Hospitalized, requiring supplemental oxygen5)Hospitalized, not requiring supplemental oxygen - requiring ongoing medical care (COVID-19 related or otherwise)6)Hospitalized, not requiring supplemental oxygen - no longer requires ongoing medical care7)Not hospitalized, limitation on activities and/or requiring home oxygen8)Not hospitalized, no limitations on activities-- a lower NIAID score is a worse outcome. (NCT04311697)
Timeframe: Day 60

InterventionParticipants (Count of Participants)
Aviptadil IV in Escalating Doses + Standard of Care76
Placebo + Standard of Care35

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Number of Participants Alive at Day 60

Survival probability on logistic regression through day 60 (NCT04311697)
Timeframe: Day 60

InterventionParticipants (Count of Participants)
Aviptadil IV in Escalating Doses + Standard of Care85
Placebo + Standard of Care35

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Percent of Subjects With Unchanged Accommodation From Baseline

Percentage of subjects with unchanged accommodation from baseline (-1 hour) (NCT04620213)
Timeframe: up to 6 hours

InterventionParticipants (Count of Participants)
Phenylephrine, 0 minutes72307183Phenylephrine, 0 minutes72307184Phenylephrine, 60 minutes72307184Phenylephrine, 60 minutes72307183Phenylephrine, 90 minutes72307184Phenylephrine, 90 minutes72307183Phenylephrine, 2 hours72307183Phenylephrine, 2 hours72307184Phenylephrine, 3 hours72307183Phenylephrine, 3 hours72307184Phenylephrine, 4 hours72307183Phenylephrine, 4 hours72307184Phenylephrine, 6 hours72307184Phenylephrine, 6 hours72307183Tropicamide, 0 Minutes72307183Tropicamide, 0 Minutes72307184Tropicamide, 60 Minutes72307183Tropicamide, 60 Minutes72307184Tropicamide, 90 Minutes72307183Tropicamide, 90 Minutes72307184Tropicamide, 2 Hours72307183Tropicamide, 2 Hours72307184Tropicamide, 3 Hours72307184Tropicamide, 3 Hours72307183Tropicamide, 4 Hours72307184Tropicamide, 4 Hours72307183Tropicamide, 6 Hours72307183Tropicamide, 6 Hours72307184Paremyd, 0 Minutes72307183Paremyd, 0 Minutes72307184Paremyd, 60 Minutes72307183Paremyd, 60 Minutes72307184Paremyd, 90 Minutes72307183Paremyd, 90 Minutes72307184Paremyd, 2 Hours72307183Paremyd, 2 Hours72307184Paremyd, 3 Hours72307183Paremyd, 3 Hours72307184Paremyd, 4 Hours72307184Paremyd, 4 Hours72307183Paremyd, 6 Hours72307183Paremyd, 6 Hours72307184Tropicamide or Paremyd, 0 Minutes72307183Tropicamide or Paremyd, 0 Minutes72307184Tropicamide or Paremyd, 60 Minutes72307183Tropicamide or Paremyd, 60 Minutes72307184Tropicamide or Paremyd, 90 Minutes72307183Tropicamide or Paremyd, 90 Minutes72307184Tropicamide or Paremyd, 2 Hours72307183Tropicamide or Paremyd, 2 Hours72307184Tropicamide or Paremyd, 3 Hours72307183Tropicamide or Paremyd, 3 Hours72307184Tropicamide or Paremyd, 4 Hours72307183Tropicamide or Paremyd, 4 Hours72307184Tropicamide or Paremyd, 6 Hours72307184Tropicamide or Paremyd, 6 Hours72307183
Changed from BaselineUnchanged from Baseline
Phentolamine Ophthalmic Solution 0.75%30
Phentolamine Ophthalmic Solution Vehicle37
Phentolamine Ophthalmic Solution 0.75%26
Phentolamine Ophthalmic Solution 0.75%29
Phentolamine Ophthalmic Solution Vehicle39
Phentolamine Ophthalmic Solution 0.75%27
Phentolamine Ophthalmic Solution Vehicle40
Phentolamine Ophthalmic Solution 0.75%40
Phentolamine Ophthalmic Solution 0.75%16
Phentolamine Ophthalmic Solution 0.75%38
Phentolamine Ophthalmic Solution Vehicle45
Phentolamine Ophthalmic Solution 0.75%18
Phentolamine Ophthalmic Solution 0.75%39
Phentolamine Ophthalmic Solution Vehicle42
Phentolamine Ophthalmic Solution 0.75%17
Phentolamine Ophthalmic Solution 0.75%43
Phentolamine Ophthalmic Solution Vehicle48
Phentolamine Ophthalmic Solution 0.75%2
Phentolamine Ophthalmic Solution Vehicle2
Phentolamine Ophthalmic Solution Vehicle16
Phentolamine Ophthalmic Solution 0.75%13
Phentolamine Ophthalmic Solution Vehicle5
Phentolamine Ophthalmic Solution 0.75%9
Phentolamine Ophthalmic Solution Vehicle13
Phentolamine Ophthalmic Solution 0.75%6
Phentolamine Ophthalmic Solution 0.75%14
Phentolamine Ophthalmic Solution Vehicle10
Phentolamine Ophthalmic Solution 0.75%5
Phentolamine Ophthalmic Solution Vehicle8
Phentolamine Ophthalmic Solution Vehicle12
Phentolamine Ophthalmic Solution Vehicle6
Phentolamine Ophthalmic Solution Vehicle3
Phentolamine Ophthalmic Solution 0.75%7
Phentolamine Ophthalmic Solution 0.75%12
Phentolamine Ophthalmic Solution 0.75%11
Phentolamine Ophthalmic Solution 0.75%8
Phentolamine Ophthalmic Solution Vehicle7
Phentolamine Ophthalmic Solution 0.75%4
Phentolamine Ophthalmic Solution 0.75%34
Phentolamine Ophthalmic Solution Vehicle31
Phentolamine Ophthalmic Solution Vehicle11
Phentolamine Ophthalmic Solution Vehicle25
Phentolamine Ophthalmic Solution Vehicle24
Phentolamine Ophthalmic Solution 0.75%21
Phentolamine Ophthalmic Solution 0.75%24
Phentolamine Ophthalmic Solution Vehicle18
Phentolamine Ophthalmic Solution 0.75%28
Phentolamine Ophthalmic Solution Vehicle21
Phentolamine Ophthalmic Solution 0.75%10
Phentolamine Ophthalmic Solution Vehicle15
Phentolamine Ophthalmic Solution Vehicle23

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Pupil Diameter (Change From Max)

Change (mm) from maximum pharmacologically-induced mydriatic pupil diameter (0 minutes) (NCT04620213)
Timeframe: up to 24 hours

,
Interventionmillimeters (Mean)
Baseline (-1 Hour)0 minutes30 minutes60 minutes90 minutes2 hours3 hours4 hours6 hours24 Hours
Phentolamine Ophthalmic Solution 0.75%5.0857.2070.025-1.308-2.192-2.429-2.828-2.991-3.338-3.375
Phentolamine Ophthalmic Solution Vehicle5.1777.1970.075-0.122-0.329-0.518-0.806-1.159-1.634-2.173

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Percent of Subjects' Study Eyes With Pupil Diameter Returning to Baseline

Percentage of subjects' study eyes returning to less than or equal to 0.2 mm from baseline pupil diameter (NCT04620213)
Timeframe: 90 minutes

InterventionParticipants (Count of Participants)
Phentolamine Ophthalmic Solution 0.75%46
Phentolamine Ophthalmic Solution Vehicle6

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Percent of Subjects' Study Eyes Pupil Diameter Returning to Baseline

Percentage of subjects' study eyesreturning to less than or equal to 0.2 mm from baseline pupil diameter (NCT04620213)
Timeframe: up to 24 hours

,
InterventionParticipants (Count of Participants)
30 minutes60 minutes90 minutes2 hours3 hours4 hours6 Hours24 Hours
Phentolamine Ophthalmic Solution 0.75%126465575778586
Phentolamine Ophthalmic Solution Vehicle3261016274160

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Percent of Subjects With 3 Lines mLCVA Improvement in Study Eye

Percent of subjects with ≥ 15 Early Treatment Diabetic Retinopathy Study (ETDRS) letters (≥3 lines) of improvement in the study eye compared to baseline in monocular mLCVA at Day 8 (NCT04638660)
Timeframe: 8 days

InterventionParticipants (Count of Participants)
Phentolamine Ophthalmic Solution 0.75%9
Phentolamine Ophthalmic Solution Vehicle2

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Change From Baseline in Study Eye Mesopic Pupil Diameter (PD)

Change from baseline in study eye mesopic PD (NCT04638660)
Timeframe: up to 15 days

,
Interventionmillimeters (Mean)
8 Days, Change from Baseline15 Days, Change from Baseline
Phentolamine Ophthalmic Solution 0.75%-1.081-1.083
Phentolamine Ophthalmic Solution Vehicle-0.130-0.121

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Percent Change From Baseline in Study Eye Mesopic Pupil Diameter (PD)

Percent change from baseline in study eye mesopic PD (NCT04638660)
Timeframe: up to 15 days

,
Interventionpercentage of change (Mean)
8 Days, Percent Change from Baseline15 Days, Percent Change from Baseline
Phentolamine Ophthalmic Solution 0.75%-17.98-18.06
Phentolamine Ophthalmic Solution Vehicle-2.09-1.75

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Percent of Subjects With mLCVA Improvement in Study Eye

Percent of subjects with ≥ 5, ≥ 10, and ≥ 15 ETDRS letters (≥ 1, ≥ 2, and ≥ 3 lines, respectively) improvement compared to baseline in mLCVA at Day 8 (excluding the primary endpoint) (NCT04638660)
Timeframe: up to 15 days

InterventionParticipants (Count of Participants)
Day 872530875Day 872530877Day 1572530877Day 1572530875
10-14 letters>= 15 letters5-9 lettersLess than 5
Phentolamine Ophthalmic Solution 0.75%9
Phentolamine Ophthalmic Solution Vehicle2
Phentolamine Ophthalmic Solution 0.75%20
Phentolamine Ophthalmic Solution Vehicle14
Phentolamine Ophthalmic Solution 0.75%22
Phentolamine Ophthalmic Solution Vehicle29
Phentolamine Ophthalmic Solution 0.75%19
Phentolamine Ophthalmic Solution Vehicle28
Phentolamine Ophthalmic Solution 0.75%14
Phentolamine Ophthalmic Solution 0.75%16
Phentolamine Ophthalmic Solution Vehicle15
Phentolamine Ophthalmic Solution 0.75%28
Phentolamine Ophthalmic Solution Vehicle39
Phentolamine Ophthalmic Solution 0.75%10
Phentolamine Ophthalmic Solution Vehicle17

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Percent of Subjects With Photopic Low Contrast Visual Acuity (pLCVA) and mHCVA Improvement in Study Eye

Percent of subjects with ≥ 5, ≥ 10, and ≥ 15 ETDRS letters (≥ 1, ≥ 2, and ≥ 3 lines, respectively) improvement compared to baseline in pLCVA and mHCVA at Day 8 and Day 15 (NCT04638660)
Timeframe: up to 15 days

InterventionParticipants (Count of Participants)
pLVCA Day 872530875pLVCA Day 872530877pLVCA Day 1572530875pLVCA Day 1572530877mHCVA Day 872530875mHCVA Day 872530877mHCVA Day 1572530875mHCVA Day 1572530877
>= 15 letters10-14 letters5-9 lettersLess than 5 letters
Phentolamine Ophthalmic Solution Vehicle0
Phentolamine Ophthalmic Solution Vehicle9
Phentolamine Ophthalmic Solution 0.75%24
Phentolamine Ophthalmic Solution Vehicle11
Phentolamine Ophthalmic Solution 0.75%29
Phentolamine Ophthalmic Solution Vehicle53
Phentolamine Ophthalmic Solution 0.75%7
Phentolamine Ophthalmic Solution Vehicle1
Phentolamine Ophthalmic Solution 0.75%12
Phentolamine Ophthalmic Solution Vehicle4
Phentolamine Ophthalmic Solution 0.75%22
Phentolamine Ophthalmic Solution Vehicle20
Phentolamine Ophthalmic Solution 0.75%23
Phentolamine Ophthalmic Solution Vehicle46
Phentolamine Ophthalmic Solution 0.75%2
Phentolamine Ophthalmic Solution 0.75%5
Phentolamine Ophthalmic Solution Vehicle3
Phentolamine Ophthalmic Solution 0.75%16
Phentolamine Ophthalmic Solution 0.75%45
Phentolamine Ophthalmic Solution Vehicle56
Phentolamine Ophthalmic Solution 0.75%3
Phentolamine Ophthalmic Solution Vehicle5
Phentolamine Ophthalmic Solution 0.75%8
Phentolamine Ophthalmic Solution 0.75%19
Phentolamine Ophthalmic Solution Vehicle14
Phentolamine Ophthalmic Solution 0.75%34
Phentolamine Ophthalmic Solution Vehicle51

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Percent of Subjects With ≥ 15 Letters of Improvement in Photopic Binocular DCNVA

The primary efficacy endpoint was the percent of subjects with ≥ 15 letters of improvement in photopic binocular DCNVA on Visit 2 at 1 hour with POS + LDP compared to placebo alone. The improvement in binocular DCNVA for each subject was relative to the subject's own baseline value (Visit 1). (NCT04675151)
Timeframe: Visit 2 at 1 hour

Interventionpercentage of subjects with ≥ 15 letters (Number)
POS 0.75% First, Then LDP 0.4%60.5
POS 0.75% First, Then LDP Vehicle30.0
POS Vehicle First, Then LDP 0.4%45.2
POS Vehicle First, Then LDP Vehicle27.3

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Percentage of Subjects With Improvement of ≥ 5, ≥ 10, and ≥ 15 Letters in DCNVA (Photopic) From Baseline

The percentage of subjects with improvement of ≥ 5, ≥ 10, and ≥ 15 letters in DCNVA (photopic) from Baseline at 0.5 hours, at 2 hours, at 3 hours, at 4 hours, and at 6 hours (NCT04675151)
Timeframe: Visit 2 at 0.5 hours, at 2 hours, at 3 hours, at 4 hours, and at 6 hours

,,,
Interventionpercentage of subjects with improvement (Number)
% of subjects with improvement of ≥ 5 letters from baseline at 0.5 hours% of subjects with improvement of ≥ 10 letters from baseline at 0.5 hours% of subjects with improvement of ≥ 15 letters from baseline at 0.5 hours% of subjects with improvement of ≥ 5 letters from baseline at 2 hours% of subjects with improvement of ≥ 10 letters from baseline at 2 hours% of subjects with improvement of ≥ 15 letters from baseline at 2 hours% of subjects with improvement of ≥ 5 letters from baseline at 3 hours% of subjects with improvement of ≥ 10 letters from baseline at 3 hours% of subjects with improvement of ≥ 15 letters from baseline at 3 hours% of subjects with improvement of ≥ 5 letters from baseline at 4 hours% of subjects with improvement of ≥ 10 letters from baseline at 4 hours% of subjects with improvement of ≥ 15 letters from baseline at 4 hours% of subjects with improvement of ≥ 5 letters from baseline at 6 hours% of subjects with improvement of ≥ 10 letters from baseline at 6 hours% of subjects with improvement of ≥ 15 letters from baseline at 6 hours
POS 0.75% First, Then LDP 0.4%88.476.760.588.481.462.895.367.446.595.367.446.588.467.437.2
POS 0.75% First, Then LDP Vehicle86.750.033.393.360.026.783.360.026.783.360.030.086.760.036.7
POS Vehicle First, Then LDP 0.4%74.254.825.883.971.041.983.964.548.483.951.632.371.054.822.6
POS Vehicle First, Then LDP Vehicle70.552.315.970.545.518.272.743.220.575.050.020.572.750.018.2

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Percentage of Subjects With Improvement in DCIVA (Photopic) From Baseline

The percentage of subjects with improvement in DCIVA (photopic) from Baseline of ≥ 5, ≥ 10, and ≥ 15 letters (NCT04675151)
Timeframe: Visit 2 at 1 hour, at 3 hours, and at 6 hours

,,,
Interventionpercentage with improvement (Number)
% of subjects with improvement of ≥ 5 letters from baseline at 1 hour% of subjects with improvement of ≥ 10 letters from baseline at 1 hour% of subjects with improvement of ≥ 15 letters from baseline at 1 hour% of subjects with improvement of ≥ 5 letters from baseline at 3 hours% of subjects with improvement of ≥ 10 letters from baseline at 3 hours% of subjects with improvement of ≥ 15 letters from baseline at 3 hours% of subjects with improvement of ≥ 5 letters from baseline at 6 hours% of subjects with improvement of ≥ 10 letters from baseline at 6 hours% of subjects with improvement of ≥ 15 letters from baseline at 6 hours
POS 0.75% First, Then LDP 0.4%86.048.814.069.841.918.672.130.214.0
POS 0.75% First, Then LDP Vehicle46.723.310.043.330.010.056.716.710.0
POS Vehicle First, Then LDP 0.4%71.045.222.667.741.922.638.729.012.9
POS Vehicle First, Then LDP Vehicle56.825.04.550.025.04.547.718.24.5

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Percentage of Subjects With Improvement of ≥ 15 Letters in DCNVA (Photopic) at 1 Hour and With < 5 Letters of Loss in Photopic Binocular BCDVA From Baseline

The percentage of subjects with improvement of ≥ 15 letters in DCNVA (photopic) at 1 hour and with < 5 letters of loss in photopic binocular BCDVA from Baseline (NCT04675151)
Timeframe: Visit 2 at 1 hour

Intervention% of subjects with improvement (Number)
POS 0.75% First, Then LDP 0.4%60.5
POS 0.75% First, Then LDP Vehicle30.0
POS Vehicle First, Then LDP 0.4%41.9
POS Vehicle First, Then LDP Vehicle27.93

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Percent of Subjects' Study Eyes With Pupil Diameter Returning to Baseline

Percentage of subjects' study eyes returning to less than or equal to 0.2 mm from baseline pupil diameter (NCT05134974)
Timeframe: 30 minutes to 24 hours

InterventionParticipants (Count of Participants)
30 minutes7256622830 minutes7256622960 minutes7256622960 minutes7256622890 minutes7256622990 minutes725662282 Hours725662282 Hours725662293 Hours725662283 Hours725662294 Hours725662294 Hours725662286 Hours725662296 Hours7256622824 Hours7256622924 Hours72566228
Returning to <=0.2 mm of BaselineNot returning to <=0.2 mm of Baseline
Phentolamine Ophthalmic Solution 0.75%10
Phentolamine Ophthalmic Solution Vehicle5
Phentolamine Ophthalmic Solution 0.75%234
Phentolamine Ophthalmic Solution Vehicle119
Phentolamine Ophthalmic Solution 0.75%103
Phentolamine Ophthalmic Solution Vehicle3
Phentolamine Ophthalmic Solution 0.75%141
Phentolamine Ophthalmic Solution Vehicle121
Phentolamine Ophthalmic Solution 0.75%142
Phentolamine Ophthalmic Solution Vehicle7
Phentolamine Ophthalmic Solution 0.75%102
Phentolamine Ophthalmic Solution Vehicle117
Phentolamine Ophthalmic Solution 0.75%162
Phentolamine Ophthalmic Solution Vehicle9
Phentolamine Ophthalmic Solution 0.75%82
Phentolamine Ophthalmic Solution Vehicle115
Phentolamine Ophthalmic Solution 0.75%193
Phentolamine Ophthalmic Solution Vehicle17
Phentolamine Ophthalmic Solution 0.75%51
Phentolamine Ophthalmic Solution Vehicle107
Phentolamine Ophthalmic Solution 0.75%210
Phentolamine Ophthalmic Solution Vehicle21
Phentolamine Ophthalmic Solution 0.75%34
Phentolamine Ophthalmic Solution Vehicle103
Phentolamine Ophthalmic Solution 0.75%221
Phentolamine Ophthalmic Solution Vehicle44
Phentolamine Ophthalmic Solution 0.75%23
Phentolamine Ophthalmic Solution Vehicle80
Phentolamine Ophthalmic Solution 0.75%218
Phentolamine Ophthalmic Solution Vehicle89
Phentolamine Ophthalmic Solution 0.75%26
Phentolamine Ophthalmic Solution Vehicle35

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Percent of Subjects With Unchanged Accommodation From Baseline

Percentage of subjects with unchanged accommodation from baseline (-1 hour) (NCT05134974)
Timeframe: 90 minutes to 6 Hours

InterventionParticipants (Count of Participants)
90 Minutes7256622890 Minutes725662292 Hours725662282 Hours725662293 Hours725662283 Hours725662296 Hours725662286 Hours72566229
Unchanged from BaselineChanged from Baseline
Phentolamine Ophthalmic Solution 0.75%155
Phentolamine Ophthalmic Solution Vehicle65
Phentolamine Ophthalmic Solution 0.75%89
Phentolamine Ophthalmic Solution Vehicle59
Phentolamine Ophthalmic Solution 0.75%165
Phentolamine Ophthalmic Solution Vehicle66
Phentolamine Ophthalmic Solution 0.75%79
Phentolamine Ophthalmic Solution Vehicle58
Phentolamine Ophthalmic Solution 0.75%186
Phentolamine Ophthalmic Solution Vehicle81
Phentolamine Ophthalmic Solution 0.75%58
Phentolamine Ophthalmic Solution Vehicle43
Phentolamine Ophthalmic Solution 0.75%204
Phentolamine Ophthalmic Solution Vehicle86
Phentolamine Ophthalmic Solution 0.75%40
Phentolamine Ophthalmic Solution Vehicle38

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Pupil Diameter (Change From Max)

Change (mm) from maximum pharmacologically-induced mydriatic pupil diameter (0 minutes) (NCT05134974)
Timeframe: 30 minutes to 24 hours

,
Interventionmillimeters (Mean)
30 Minutes60 Minutes90 Minutes2 Hours3 Hours4 Hours6 Hours24 Hours
Phentolamine Ophthalmic Solution 0.75%-0.109-1.457-2.157-2.478-2.917-3.078-3.267-3.134
Phentolamine Ophthalmic Solution Vehicle0.092-0.059-0.284-0.488-0.987-1.261-1.755-2.313

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Change From Baseline in Best-Corrected Distance Visual Acuity (BCDVA) Under Normal Photopic Lighting Without Glare Conditions

Change from Baseline in best-corrected distance visual acuity (BCDVA) under normal photopic lighting without glare conditions (NCT05134974)
Timeframe: 6 hours

Interventionletters (Mean)
Phentolamine Ophthalmic Solution 0.75%0.3
Phentolamine Ophthalmic Solution Vehicle-0.2

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Efficacy Measurement: Pupil Diameter

Time (Hours) to Return to ≤ 0.2 mm from Baseline (-1 Hour) Pupil Diameter (Time-savings Analysis) (Study Eye) (NCT05223478)
Timeframe: Up to 24 Hours

Interventionhours (Mean)
Phentolamine Ophthalmic Solution 0.75%2.95
Phentolamine Ophthalmic Solution Vehicle5.54

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Change From Screening Blood Pressure (Diastolic)

(NCT05223478)
Timeframe: 3 Hours, 24 Hours

,
InterventionmmHg (Mean)
3 Hours24 Hours
Phentolamine Ophthalmic Solution 0.75%-2.4-1.1
Phentolamine Ophthalmic Solution Vehicle1.0-3.8

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Efficacy Measurement: Pupil Diameter

Percentage of Subjects Returning to ≤ 0.2 mm from Baseline (-1 hour) Pupil Diameter (Study Eye) (NCT05223478)
Timeframe: 90 Minutes, 3 Hours, and 24 Hours

,
InterventionParticipants (Count of Participants)
90 Minutes3 Hours24 Hours
Phentolamine Ophthalmic Solution 0.75%7910
Phentolamine Ophthalmic Solution Vehicle346

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Safety Measurement

Study Eye Change from Baseline (-1 Hour) in Best Corrected Distance Visual Acuity (NCT05223478)
Timeframe: 0 Minutes, 3 Hours, 24 Hours

,
Interventionletters (Mean)
0 Minutes3 Hours24 Hours
Phentolamine Ophthalmic Solution 0.75%-1.21.21.5
Phentolamine Ophthalmic Solution Vehicle-0.30.10.7

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Safety Measurements

Study Eye Change from Baseline (-1 Hour) Conjunctival Hyperemia Grading; Cornea and Contact Lens Research Unit (CCLRU scale) Grades range from 0 to 3, with 3 being considered the most severe. (NCT05223478)
Timeframe: 0 Minutes, 90 Minutes, 3 Hours, 24 Hours

,
Interventionscore on a scale (Mean)
0 Minutes90 Minutes3 Hours24 Hours
Phentolamine Ophthalmic Solution 0.75%0.31.61.10.1
Phentolamine Ophthalmic Solution Vehicle-0.20.0-0.1-0.2

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Vital Signs

Change from Screening Blood Pressure (Systolic) (NCT05223478)
Timeframe: 3 Hours, 24 Hours

,
InterventionmmHg (Mean)
3 Hours24 Hours
Phentolamine Ophthalmic Solution 0.75%-4.6-2.8
Phentolamine Ophthalmic Solution Vehicle-0.8-5.8

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Efficacy Measurement: Pupil Diameter

Change (in mm) in Pupil Diameter from Max Pupil Dilation (0 minutes) (Study Eye) (NCT05223478)
Timeframe: 90 Minutes, 3 Hours, and 24 Hours

,
Interventionmillimeters (Mean)
90 Minutes3 Hours24 Hours
Phentolamine Ophthalmic Solution 0.75%-1.475-2.031-2.005
Phentolamine Ophthalmic Solution Vehicle-0.378-0.723-1.44

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Vital Signs

Change from Screening Heart Rate (NCT05223478)
Timeframe: 3 Hours, 24 Hours

,
Interventionbeats per minute (Mean)
3 Hours24 Hours
Phentolamine Ophthalmic Solution 0.75%-1.1-2.5
Phentolamine Ophthalmic Solution Vehicle-2.0-3.5

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