Page last updated: 2024-11-04

quipazine

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Description

Quipazine is a non-selective serotonin receptor agonist, primarily targeting the 5-HT1A receptor subtype. It is structurally related to the antipsychotic drug chlorpromazine, but exhibits distinct pharmacological properties. Quipazine has been studied for its potential therapeutic applications in various conditions, including anxiety, depression, and addiction. Its effects include anxiolytic, antidepressant, and anti-addictive properties. Research suggests that quipazine acts as a partial agonist at 5-HT1A receptors, leading to an increase in serotonin levels in the brain. Quipazine is a valuable tool for investigating the role of serotonin in various physiological and pathological processes. '

Quipazine: A pharmacologic congener of serotonin that contracts smooth muscle and has actions similar to those of tricyclic antidepressants. It has been proposed as an oxytocic. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID5011
CHEMBL ID18772
CHEBI ID93368
SCHEMBL ID322181
MeSH IDM0018361

Synonyms (99)

Synonym
brn 0196945
1-(2-quinolinyl)piperazine
quipazinum [inn-latin]
quipazina [inn-spanish]
1-(2-quinolyl)piperazine
quinoline, 2-(1-piperazinyl)-
2-(1-piperazinyl)quinoline
quipazine [inn]
2-(1-piperazinyl)chinolin
quipazine
STL308727
BRD-K77925998-332-03-8
BRD-K77925998-050-02-8
BRD-K77925998-001-01-3
gtpl173
DIVK1C_000911
KBIO1_000911
SPECTRUM_001733
OPREA1_342540
4774-24-7
lopac-q-1004
NCGC00015872-02
cas-4774-24-7
tocris-0629
NCGC00015872-01
NCGC00024694-01
BPBIO1_001393
PRESTWICK3_000617
IDI1_000911
LOPAC0_001019
BPBIO1_000610
AB00053761
2-piperazin-1-yl-quinoline
BIOMOL-NT_000103
BSPBIO_000554
PRESTWICK2_000617
NCGC00024694-03
KBIOSS_002213
KBIOGR_001818
KBIO2_004781
KBIO2_002213
KBIO3_002971
KBIO2_007349
SPECTRUM2_001182
SPECTRUM4_001259
SPECTRUM3_001824
SPBIO_001223
PRESTWICK1_000617
SPBIO_002773
PRESTWICK0_000617
NINDS_000911
BSPBIO_003467
NCGC00024694-02
2-piperazin-1-ylquinoline
L000958
CHEMBL18772 ,
2-(piperazin-1-yl)quinoline
F3306-0004
2-piperazin-1-yl-quinoline (quipazine)
2-piperazin-1-yl-quinoline(quipazine)
bdbm50014407
AKOS000124312
A827323
CCG-205099
NCGC00015872-04
NCGC00015872-06
NCGC00015872-03
quipazinum
4wcy05c0sj ,
quipazina
unii-4wcy05c0sj
5-23-03-00069 (beilstein handbook reference)
FT-0635438
AB05466
AB00053761-06
SCHEMBL322181
piperazin-1-yl-quinoline
1-(quinolin-2-yl)piperazine
2-(piperazin-1-yl)-quinoline
XRXDAJYKGWNHTQ-UHFFFAOYSA-N
DTXSID3046952
mfcd00242605
Q-103520
AC-22858
AB00053761_11
AB00053761_12
2-(1-piperazino)quinoline
VU0005330-3
CHEBI:93368
SBI-0050992.P003
130895-61-3
AS-38262
Q7272557
EN300-39715
BCP23281
2-piperazin-1-yl-quinoline;2-(piperazin-1-yl)quinoline
CS-0072166
HY-W028142
SY238379

Research Excerpts

Overview

summarize : Quipazine is a 5-HT.

ExcerptReferenceRelevance
"Quipazine is a 5-HT"( Stimulation of 5-HT2A receptors recovers sensory responsiveness in acute spinal neonatal rats.
Allmond, JT; Brumley, MR; Kauer, SD; Swann, HE, 2017
)
1.9

Actions

ExcerptReferenceRelevance
"The quipazine-induced increase in serum corticosterone was antagonized by 17 different serotonin antagonists; of these, MDL 11939, pirenperone, setoperone, mianserin, LY 281067, ketanserin, ritanserin and clozapine have relatively selective affinity for the 5-HT2 subtype of receptor."( Serotonin receptor subtypes involved in the elevation of serum corticosterone concentration in rats by direct- and indirect-acting serotonin agonists.
Fuller, RW; Snoddy, HD, 1990
)
0.76

Treatment

Quipazine-treated, hyperglycemic animals did not show any increase in plasma insulin levels. Quipazine treatment during the subjective day (which phase-advances the circadian rhythm of neuronal firing in the SCN) decreased c-fos mRNA levels in the dorsomedial but not ventrolateral SCN.

ExcerptReferenceRelevance
"Quipazine-treated, hyperglycemic animals did not show any increase in plasma insulin levels."( Hyperglycemia induced by pharmacological activation of central serotonergic pathways depends on the functional integrity of brain CRH system and 5-HT3 receptors.
Barros, D; Carvalho, F; de Castro-E-Silva, E; Fregoneze, J; Rezende, E; Silva, J; Soares, M, 2005
)
1.05
"Quipazine, in mice pretreated with pargyline, induced head twitches which were inhibited by methysergide but not by D,L-propranolol."( Evidence for the role of noradrenaline in some effects of quipazine.
Francès, H; Lecrubier, Y; Puech, AJ; Simon, P, 1980
)
1.23
"Quipazine-treated animals required more elicitation attempts before displaying TI."( Tonic immobility in domestic fowl: anticataleptic effects of quipazine.
Wallnau, LB, 1980
)
1.22
"Quipazine treatment during the subjective day (which phase-advances the circadian rhythm of neuronal firing in the SCN) decreased c-fos mRNA levels in the dorsomedial but not ventrolateral SCN, but quipazine did not affect c-fos levels when administered at night."( c-fos mRNA in the suprachiasmatic nuclei in vitro shows a circadian rhythm and responds to a serotonergic agonist.
Heller, HC; Macdonald, ES; Prosser, RA, 1994
)
1.01
"CT 6 quipazine-treated animals also showed a sustained and significant shortening of rhythm period (tau) following treatment (-0.28 hr; p < 0.002)."( Serotonin and the mammalian circadian system: II. Phase-shifting rat behavioral rhythms with serotonergic agonists.
Dean, RR; Dement, WC; Edgar, DM; Miller, JD; Prosser, RA, 1993
)
0.74
"Pups treated with quipazine showed significantly more alternated fore- and hindlimb steps and plantar paw contact with the substrate, compared to pups treated with saline."( Sensory feedback modulates quipazine-induced stepping behavior in the newborn rat.
Brumley, MR; Roberto, ME; Strain, MM, 2012
)
1
"Pretreatment with quipazine alone in a group of animals trained to a shock level which normally results in high levels of suppression was not sufficient to produce memory impairment, suggesting that quipazine was probably antagonizing the facilitative effects of alaproclate and zimeldine directly, rather than overriding the facilitation through an indirect action on retrieval in general."( Role of serotonin in memory: facilitation by alaproclate and zimeldine.
Altman, HJ; Nordy, DA; Ogren, SO, 1984
)
0.59
"Pretreating with quipazine significantly decreased only the ratio of uptake in the medulla oblongata compared to the cerebellum."( N-methylquipazine: carbon-11 labelling of the 5-HT3 agonist and in vivo evaluation of its biodistribution using PET.
Eriksson, L; Ingvar, M; Stone-Elander, S; Thorell, JO, 1997
)
1.06
"Pretreatment with quipazine, a serotonin agonist, and clomipramine, a selective serotonin neuronal uptake blocker, was found to potentiate the cataleptic effect of haloperidol in a dose-dependent manner in rats. "( Effect of drugs influencing central serotonergic mechanisms on haloperidol-induced catalepsy.
Balsara, JJ; Chandorkar, AG; Jadhav, JH, 1979
)
0.59

Bioavailability

ExcerptReferenceRelevance
" This multifunctional drug candidate is orally bioavailable and exhibits good antipsychotic efficacy in vivo."( Discovery of a tetracyclic quinoxaline derivative as a potent and orally active multifunctional drug candidate for the treatment of neuropsychiatric and neurological disorders.
Beard, JD; Davis, RE; Hendrick, JP; Lee, T; Li, P; Mates, S; Peng, Y; Robichaud, AJ; Snyder, GL; Tomesch, J; Vanover, KE; Wennogle, LP; Yao, W; Zhang, Q; Zhu, H, 2014
)
0.4

Dosage Studied

Quipazine (nonselective 5-hydroxytryptamine [5-HT] agonist; 1.1 mg/kg) Dose-response relationships between quipazine and the area-under-the-MSR showed a significant shift to the right in the ACR 10 from control. Since the dose-response curves for quipazines during the day and night are virtually identical, we hypothesize that the nighttime 5-HT receptor is a 5- HT1-like receptor.

ExcerptRelevanceReference
" Dose-response studies were designed to determine the effects of these drugs on serum prolactin (PRL) concentrations."( Effects of metoclopramide and quipazine on serum prolactin concentrations in steers.
Lipham, LB; Stuedemann, JA; Thompson, FN, 1992
)
0.57
" Dose-response tests with LSD and LHM indicated that, as dose increased, the per cent of responding on the lever associated with the particular training drug also increased; little or no cross-transfer occurred between LSD and LHM."( Differentiation between the stimulus effects of (+)-lysergic acid diethylamide and lisuride using a three-choice, drug discrimination procedure.
Appel, JB; Callahan, PM, 1990
)
0.28
" Dose-response relationships between quipazine and the area-under-the-MSR showed a significant shift to the right in the ACR 10 from control and no significant change in the ACR 20 from control."( Acrylamide neurotoxicity: altered spinal monosynaptic responses to quipazine, a serotonin agonist, in cats.
Goldstein, BD, 1985
)
0.78
" In nodose ganglia three 4-5 point dose-response (DR) curves were established, using bolus injections of 5-HT (5-80 nmol)."( Further studies on the blockade of 5-HT depolarizations of rabbit vagal afferent and sympathetic ganglion cells by MDL 72222 and other antagonists.
Round, A; Wallis, DI, 1987
)
0.27
" The dose-response curves for the phenethylamine hallucinogens were shifted significantly to the right and to a greater degree than were those for the indolealkylamine hallucinogens."( The 5HT2 antagonist pirenperone reverses disruption of FR-40 by hallucinogenic drugs.
Mokler, DJ; Rech, RH; Stoudt, KW, 1985
)
0.27
" The DOM dose-response pattern for decrease in reinforcers was shifted to the greatest degree by metergoline, followed by pizotifen and cinanserin (ED50 values: 26."( Blockade of the behavioral effects of lysergic acid diethylamide, 2,5-dimethoxy-4-methylamphetamine, quipazine and lisuride by 5-hydroxytryptamine antagonists.
Commissaris, RL; Mokler, DJ; Rech, RH; Warner, MR, 1983
)
0.48
" A dose-response curve was generated for each antagonist and an ID50 value (dose that inhibits responding to 50% on the quipazine lever) was determined by log-logit analysis."( Discriminative stimulus properties of quipazine: mediation by serotonin2 binding sites.
Barrett, RJ; Friedman, RL; Sanders-Bush, E, 1984
)
0.75
" In the present study we determined the time-course and dose-response effects of 6-MeO-THbetaC for blockade of AGS."( Effects of 6-methoxy-1,2,3,4-tetrahydro-beta-carboline (6-MeO-THbetaC) on audiogenic seizures in DBA/2J mice.
Buckholtz, NS; Sparks, DL, 1980
)
0.26
" The dose-response curve for this discrimination was orderly with an ED50 of about one-half of the training dose (0."( A neuropharmacological analysis of the discriminative stimulus properties of fenfluramine.
Appel, JB; White, FJ, 1981
)
0.26
"1 mg/kg, metergoline (180 min prior to the session) the dose-response curves for the "pausing" produced by both DOM and quipazine were shifted significantly to the right."( Antagonism of the behavioral effects of 2,5-dimethoxy-4-methylamphetamine (DOM) and quipazine by metergoline.
Commissaris, RL; Rech, RH, 1981
)
0.7
" After acquisition, the quipazine and ketanserin dose-response curves were found to be orderly and reproducible."( Neurochemical and behavioral evidence that quipazine-ketanserin discrimination is mediated by serotonin2A receptor.
Barrett, RJ; Sanders-Bush, E; Smith, RL, 1995
)
0.86
"05) by the greatest dosage of LY 53,857 (LY: 5-HT1C and 5-HT2 antagonist) (1."( Serotonergic agonists and antagonists affect endurance performance in the rat.
Ahlborn, EN; Bailey, SP; Davis, JM, 1993
)
0.29
" However, since the dose-response curves for quipazine during the day and night are virtually identical, we hypothesize that the nighttime 5-HT receptor is a 5-HT1-like receptor."( Serotonin and the mammalian circadian system: I. In vitro phase shifts by serotonergic agonists and antagonists.
Dean, RR; Edgar, DM; Heller, HC; Miller, JD; Prosser, RA, 1993
)
0.55
" At the dosage used (0."( Spinal cord-transected mice learn to step in response to quipazine treatment and robotic training.
Burdick, JW; Cai, LL; Edgerton, VR; Fong, AJ; Otoshi, CK; Reinkensmeyer, DJ; Roy, RR, 2005
)
0.57
" The results indicate that quipazine and ES can have complementary effects on spinal circuits and that quipazine dosage is an important factor in differentially modulating these circuitries to improve the quality of the bipedal stepping on a treadmill belt."( Dose dependence of the 5-HT agonist quipazine in facilitating spinal stepping in the rat with epidural stimulation.
Edgerton, VR; Gerasimenko, Y; Ichiyama, RM; Jindrich, DL; Roy, RR; Zhong, H, 2008
)
0.92
"1 mg/kg/infusion) generated an inverted U-shaped dose-response function."( Effects of 1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane (DOM) and quipazine on heroin self-administration in rhesus monkeys.
France, CP; Koek, W; Li, JX; Maguire, DR, 2013
)
0.62
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (2)

ClassDescription
pyridinesAny organonitrogen heterocyclic compound based on a pyridine skeleton and its substituted derivatives.
piperazines
[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 (70)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency0.35480.004023.8416100.0000AID485290
Chain A, HADH2 proteinHomo sapiens (human)Potency39.81070.025120.237639.8107AID893
Chain B, HADH2 proteinHomo sapiens (human)Potency39.81070.025120.237639.8107AID893
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency25.66510.177814.390939.8107AID2147
glp-1 receptor, partialHomo sapiens (human)Potency35.48130.01846.806014.1254AID624172
phosphopantetheinyl transferaseBacillus subtilisPotency39.81070.141337.9142100.0000AID1490
GLS proteinHomo sapiens (human)Potency31.62280.35487.935539.8107AID624170
TDP1 proteinHomo sapiens (human)Potency14.96310.000811.382244.6684AID686978
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency37.64600.011212.4002100.0000AID1030
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency35.48130.01789.637444.6684AID588834
huntingtin isoform 2Homo sapiens (human)Potency35.48130.000618.41981,122.0200AID1688
mitogen-activated protein kinase 1Homo sapiens (human)Potency0.06310.039816.784239.8107AID995
ubiquitin carboxyl-terminal hydrolase 2 isoform aHomo sapiens (human)Potency5.01190.65619.452025.1189AID927
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency0.01440.005612.367736.1254AID624032
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency0.03980.031610.279239.8107AID884; AID885
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency15.37120.00106.000935.4813AID943; AID944
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency0.03981.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency0.03981.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency0.03981.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency0.03981.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency0.03981.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency0.03981.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency0.03981.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency0.03981.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency0.03981.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency0.03981.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency0.03981.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency0.03981.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency0.03981.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency0.03981.000012.224831.6228AID885
Disintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)Potency5.01191.584913.004325.1189AID927
GABA theta subunitRattus norvegicus (Norway rat)Potency0.03981.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency0.03981.000012.224831.6228AID885
[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)
5-hydroxytryptamine receptor 3EHomo sapiens (human)IC50 (µMol)0.00040.00042.08059.0000AID6355
5-hydroxytryptamine receptor 3EHomo sapiens (human)Ki0.00190.00100.88359.9000AID6335; AID6343
5-hydroxytryptamine receptor 3ACavia porcellus (domestic guinea pig)Ki6.66700.00100.03000.0851AID375324; AID441240
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)Ki10.00000.00000.887110.0000AID375324; AID441266; AID6200
5-hydroxytryptamine receptor 3BHomo sapiens (human)IC50 (µMol)0.00040.00041.95059.0000AID6355
5-hydroxytryptamine receptor 3BHomo sapiens (human)Ki0.00190.00100.87119.9000AID6335; AID6343
Beta-1 adrenergic receptorHomo sapiens (human)Ki6.30960.00011.33919.9840AID731817
5-hydroxytryptamine receptor 1AHomo sapiens (human)IC50 (µMol)1.44540.00010.666410.0000AID3458; AID3459
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)IC50 (µMol)0.47000.00040.629810.0000AID5707
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)Ki0.27140.00020.667710.0000AID5238; AID5267; AID5270; AID5273; AID5724; AID5757
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)IC50 (µMol)1.40000.00040.908610.0000AID5489
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)Ki0.60380.00010.601710.0000AID375323; AID441265; AID5238; AID5267; AID5270; AID5273; AID5342; AID5528; AID5581
DRattus norvegicus (Norway rat)Ki0.00100.00010.610010.0000AID6285
D(3) dopamine receptorRattus norvegicus (Norway rat)Ki0.00100.00010.25675.8000AID6285
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)IC50 (µMol)2.70000.00031.38338.4000AID3770
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Ki0.47520.00010.739610.0000AID205022; AID3695; AID4424
D(1A) dopamine receptorHomo sapiens (human)Ki0.00180.00010.836310.0000AID6335
5-hydroxytryptamine receptor 3AMus musculus (house mouse)Ki0.00870.00130.23781.4300AID6008
D(1B) dopamine receptorRattus norvegicus (Norway rat)Ki0.00100.00020.24622.0000AID6285
5-hydroxytryptamine receptor 2CHomo sapiens (human)IC50 (µMol)0.06170.00011.03029.0000AID5683; AID5685
5-hydroxytryptamine receptor 2CHomo sapiens (human)Ki0.20000.00010.954910.0000AID4747
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)IC50 (µMol)3.72970.00051.48357.8000AID4298; AID4299; AID4679
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)Ki0.17390.00031.29679.2440AID205022; AID3695; AID4699; AID4708; AID4722
5-hydroxytryptamine receptor 1DRattus norvegicus (Norway rat)Ki0.10530.00101.67479.2000AID205022; AID3695
D(4) dopamine receptorRattus norvegicus (Norway rat)Ki0.00100.00020.18872.0000AID6285
5-hydroxytryptamine receptor 1FRattus norvegicus (Norway rat)Ki0.10530.00101.67479.2000AID205022; AID3695
5-hydroxytryptamine receptor 5AMus musculus (house mouse)Ki10.00000.00203.98248.7000AID6492; AID6493
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)Ki0.28050.00020.590910.0000AID5238; AID5267; AID5270; AID5273
Sodium-dependent serotonin transporterHomo sapiens (human)Ki0.03000.00000.70488.1930AID644742
Sodium-dependent serotonin transporterRattus norvegicus (Norway rat)Ki0.03700.00000.705610.0000AID204521; AID205022
5-hydroxytryptamine receptor 7Homo sapiens (human)Ki3.03300.00030.380610.0000AID6678
5-hydroxytryptamine receptor 3ARattus norvegicus (Norway rat)IC50 (µMol)0.00350.00021.13514.6000AID6069; AID6080; AID6357
5-hydroxytryptamine receptor 3ARattus norvegicus (Norway rat)Ki0.00220.00020.484110.0000AID375321; AID441240; AID5893; AID5898; AID5911; AID6132; AID6284; AID6285; AID6295; AID6297; AID6298
5-hydroxytryptamine receptor 3AHomo sapiens (human)IC50 (µMol)0.00040.00011.07899.0000AID6355
5-hydroxytryptamine receptor 3AHomo sapiens (human)Ki0.00270.00000.74119.9000AID297966; AID6335; AID6343
5-hydroxytryptamine receptor 6Homo sapiens (human)Ki3.60000.00020.522910.0000AID6514
D(2) dopamine receptorRattus norvegicus (Norway rat)Ki0.00100.00000.437510.0000AID6285
5-hydroxytryptamine receptor 1DSus scrofa (pig)IC50 (µMol)3.71530.00030.64963.7153AID4851; AID4852
Adenylate cyclase type 5Rattus norvegicus (Norway rat)IC50 (µMol)1.44540.04680.88292.3000AID3459
5-hydroxytryptamine receptor 4 Rattus norvegicus (Norway rat)IC50 (µMol)10.00000.00501.35524.6000AID6232
5-hydroxytryptamine receptor 3DHomo sapiens (human)IC50 (µMol)0.00040.00042.08059.0000AID6355
5-hydroxytryptamine receptor 3DHomo sapiens (human)Ki0.00190.00100.88359.9000AID6335; AID6343
5-hydroxytryptamine receptor 2ABos taurus (cattle)IC50 (µMol)3.46740.00902.71404.3652AID5153; AID5154
5-hydroxytryptamine receptor 3CHomo sapiens (human)IC50 (µMol)0.00040.00042.08059.0000AID6355
5-hydroxytryptamine receptor 3CHomo sapiens (human)Ki0.00190.00100.88359.9000AID6335; AID6343
5-hydroxytryptamine receptor 3BMus musculus (house mouse)Ki0.00870.00130.26351.4300AID6008
5-hydroxytryptamine receptor 3BRattus norvegicus (Norway rat)IC50 (µMol)0.00350.00041.17424.6000AID6069; AID6080; AID6357
5-hydroxytryptamine receptor 3BRattus norvegicus (Norway rat)Ki0.00240.00020.502310.0000AID5893; AID5898; AID5911; AID6132; AID6284; AID6285; AID6295; AID6297; AID6298
[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)
5-hydroxytryptamine receptor 3EHomo sapiens (human)EC50 (µMol)0.00100.00100.00100.0010AID143671
5-hydroxytryptamine receptor 3BHomo sapiens (human)EC50 (µMol)0.00100.00101.10032.8000AID143671
Beta-1 adrenergic receptorHomo sapiens (human)Kd5.61170.00010.803910.0000AID731818
5-hydroxytryptamine receptor 1AHomo sapiens (human)Kd1.99530.00010.95285.0119AID438555
5-hydroxytryptamine receptor 3AHomo sapiens (human)EC50 (µMol)0.00100.00100.65503.8000AID143671
5-hydroxytryptamine receptor 3DHomo sapiens (human)EC50 (µMol)0.00100.00100.00100.0010AID143671
5-hydroxytryptamine receptor 3CHomo sapiens (human)EC50 (µMol)0.00100.00100.00100.0010AID143671
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (185)

Processvia Protein(s)Taxonomy
serotonin receptor signaling pathway5-hydroxytryptamine receptor 3EHomo sapiens (human)
monoatomic ion transmembrane transport5-hydroxytryptamine receptor 3EHomo sapiens (human)
excitatory postsynaptic potential5-hydroxytryptamine receptor 3EHomo sapiens (human)
inorganic cation transmembrane transport5-hydroxytryptamine receptor 3EHomo sapiens (human)
regulation of membrane potential5-hydroxytryptamine receptor 3EHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 3EHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 3BHomo sapiens (human)
monoatomic ion transmembrane transport5-hydroxytryptamine receptor 3BHomo sapiens (human)
excitatory postsynaptic potential5-hydroxytryptamine receptor 3BHomo sapiens (human)
inorganic cation transmembrane transport5-hydroxytryptamine receptor 3BHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 3BHomo sapiens (human)
regulation of membrane potential5-hydroxytryptamine receptor 3BHomo 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)
behavioral fear response5-hydroxytryptamine receptor 1AHomo sapiens (human)
G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
adenylate cyclase-inhibiting serotonin receptor signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
gamma-aminobutyric acid signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
positive regulation of cell population proliferation5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of serotonin secretion5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of vasoconstriction5-hydroxytryptamine receptor 1AHomo sapiens (human)
exploration behavior5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of dopamine metabolic process5-hydroxytryptamine receptor 1AHomo sapiens (human)
serotonin metabolic process5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of hormone secretion5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of behavior5-hydroxytryptamine receptor 1AHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 1AHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 1AHomo sapiens (human)
superoxide anion generationNeutrophil cytosol factor 1Homo sapiens (human)
protein targeting to membraneNeutrophil cytosol factor 1Homo sapiens (human)
superoxide metabolic processNeutrophil cytosol factor 1Homo sapiens (human)
cellular defense responseNeutrophil cytosol factor 1Homo sapiens (human)
cellular response to reactive oxygen speciesNeutrophil cytosol factor 1Homo sapiens (human)
superoxide anion generationNeutrophil cytosol factor 1Homo sapiens (human)
innate immune responseNeutrophil cytosol factor 1Homo sapiens (human)
respiratory burstNeutrophil cytosol factor 1Homo sapiens (human)
positive regulation of epidermal growth factor-activated receptor activityNeutrophil cytosol factor 1Homo sapiens (human)
positive regulation of DNA-templated transcriptionNeutrophil cytosol factor 1Homo sapiens (human)
positive regulation of JNK cascadeNeutrophil cytosol factor 1Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionNeutrophil cytosol factor 1Homo sapiens (human)
regulation of respiratory burst involved in inflammatory responseNeutrophil cytosol factor 1Homo sapiens (human)
cellular response to cadmium ionNeutrophil cytosol factor 1Homo sapiens (human)
cellular response to glucose stimulusNeutrophil cytosol factor 1Homo sapiens (human)
cellular response to testosterone stimulusNeutrophil cytosol factor 1Homo sapiens (human)
positive regulation of p38MAPK cascadeNeutrophil cytosol factor 1Homo sapiens (human)
reactive oxygen species biosynthetic processNeutrophil cytosol factor 1Homo sapiens (human)
temperature homeostasisD(1A) dopamine receptorHomo sapiens (human)
conditioned taste aversionD(1A) dopamine receptorHomo sapiens (human)
behavioral fear responseD(1A) dopamine receptorHomo sapiens (human)
regulation of protein phosphorylationD(1A) dopamine receptorHomo sapiens (human)
synaptic transmission, dopaminergicD(1A) dopamine receptorHomo sapiens (human)
response to amphetamineD(1A) dopamine receptorHomo sapiens (human)
protein import into nucleusD(1A) dopamine receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerD(1A) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayD(1A) dopamine receptorHomo sapiens (human)
activation of adenylate cyclase activityD(1A) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating dopamine receptor signaling pathwayD(1A) dopamine receptorHomo sapiens (human)
synapse assemblyD(1A) dopamine receptorHomo sapiens (human)
memoryD(1A) dopamine receptorHomo sapiens (human)
mating behaviorD(1A) dopamine receptorHomo sapiens (human)
grooming behaviorD(1A) dopamine receptorHomo sapiens (human)
adult walking behaviorD(1A) dopamine receptorHomo sapiens (human)
visual learningD(1A) dopamine receptorHomo sapiens (human)
response to xenobiotic stimulusD(1A) dopamine receptorHomo sapiens (human)
astrocyte developmentD(1A) dopamine receptorHomo sapiens (human)
dopamine transportD(1A) dopamine receptorHomo sapiens (human)
transmission of nerve impulseD(1A) dopamine receptorHomo sapiens (human)
neuronal action potentialD(1A) dopamine receptorHomo sapiens (human)
dentate gyrus developmentD(1A) dopamine receptorHomo sapiens (human)
striatum developmentD(1A) dopamine receptorHomo sapiens (human)
cerebral cortex GABAergic interneuron migrationD(1A) dopamine receptorHomo sapiens (human)
positive regulation of cell migrationD(1A) dopamine receptorHomo sapiens (human)
peristalsisD(1A) dopamine receptorHomo sapiens (human)
operant conditioningD(1A) dopamine receptorHomo sapiens (human)
synaptic transmission, glutamatergicD(1A) dopamine receptorHomo sapiens (human)
regulation of dopamine metabolic processD(1A) dopamine receptorHomo sapiens (human)
vasodilationD(1A) dopamine receptorHomo sapiens (human)
dopamine metabolic processD(1A) dopamine receptorHomo sapiens (human)
maternal behaviorD(1A) dopamine receptorHomo sapiens (human)
positive regulation of potassium ion transportD(1A) dopamine receptorHomo sapiens (human)
glucose importD(1A) dopamine receptorHomo sapiens (human)
habituationD(1A) dopamine receptorHomo sapiens (human)
sensitizationD(1A) dopamine receptorHomo sapiens (human)
behavioral response to cocaineD(1A) dopamine receptorHomo sapiens (human)
positive regulation of release of sequestered calcium ion into cytosolD(1A) dopamine receptorHomo sapiens (human)
regulation of dopamine uptake involved in synaptic transmissionD(1A) dopamine receptorHomo sapiens (human)
positive regulation of synaptic transmission, glutamatergicD(1A) dopamine receptorHomo sapiens (human)
prepulse inhibitionD(1A) dopamine receptorHomo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathwayD(1A) dopamine receptorHomo sapiens (human)
long-term synaptic potentiationD(1A) dopamine receptorHomo sapiens (human)
long-term synaptic depressionD(1A) dopamine receptorHomo sapiens (human)
cellular response to catecholamine stimulusD(1A) dopamine receptorHomo sapiens (human)
modification of postsynaptic structureD(1A) dopamine receptorHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionD(1A) dopamine receptorHomo sapiens (human)
positive regulation of neuron migrationD(1A) dopamine receptorHomo sapiens (human)
positive regulation of MAPK cascadeD(1A) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayD(1A) dopamine receptorHomo sapiens (human)
dopamine receptor signaling pathwayD(1A) dopamine receptorHomo 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)
monoamine transportSodium-dependent serotonin transporterHomo sapiens (human)
response to hypoxiaSodium-dependent serotonin transporterHomo sapiens (human)
neurotransmitter transportSodium-dependent serotonin transporterHomo sapiens (human)
response to nutrientSodium-dependent serotonin transporterHomo sapiens (human)
memorySodium-dependent serotonin transporterHomo sapiens (human)
circadian rhythmSodium-dependent serotonin transporterHomo sapiens (human)
response to xenobiotic stimulusSodium-dependent serotonin transporterHomo sapiens (human)
response to toxic substanceSodium-dependent serotonin transporterHomo sapiens (human)
positive regulation of gene expressionSodium-dependent serotonin transporterHomo sapiens (human)
positive regulation of serotonin secretionSodium-dependent serotonin transporterHomo sapiens (human)
negative regulation of cerebellar granule cell precursor proliferationSodium-dependent serotonin transporterHomo sapiens (human)
negative regulation of synaptic transmission, dopaminergicSodium-dependent serotonin transporterHomo sapiens (human)
response to estradiolSodium-dependent serotonin transporterHomo sapiens (human)
social behaviorSodium-dependent serotonin transporterHomo sapiens (human)
vasoconstrictionSodium-dependent serotonin transporterHomo sapiens (human)
sperm ejaculationSodium-dependent serotonin transporterHomo sapiens (human)
negative regulation of neuron differentiationSodium-dependent serotonin transporterHomo sapiens (human)
positive regulation of cell cycleSodium-dependent serotonin transporterHomo sapiens (human)
negative regulation of organ growthSodium-dependent serotonin transporterHomo sapiens (human)
behavioral response to cocaineSodium-dependent serotonin transporterHomo sapiens (human)
enteric nervous system developmentSodium-dependent serotonin transporterHomo sapiens (human)
brain morphogenesisSodium-dependent serotonin transporterHomo sapiens (human)
serotonin uptakeSodium-dependent serotonin transporterHomo sapiens (human)
membrane depolarizationSodium-dependent serotonin transporterHomo sapiens (human)
platelet aggregationSodium-dependent serotonin transporterHomo sapiens (human)
cellular response to retinoic acidSodium-dependent serotonin transporterHomo sapiens (human)
cellular response to cGMPSodium-dependent serotonin transporterHomo sapiens (human)
regulation of thalamus sizeSodium-dependent serotonin transporterHomo sapiens (human)
conditioned place preferenceSodium-dependent serotonin transporterHomo sapiens (human)
sodium ion transmembrane transportSodium-dependent serotonin transporterHomo sapiens (human)
amino acid transportSodium-dependent serotonin transporterHomo sapiens (human)
smooth muscle contraction5-hydroxytryptamine receptor 7Homo sapiens (human)
circadian rhythm5-hydroxytryptamine receptor 7Homo sapiens (human)
blood circulation5-hydroxytryptamine receptor 7Homo sapiens (human)
vasoconstriction5-hydroxytryptamine receptor 7Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 7Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 7Homo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 7Homo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 3AHomo sapiens (human)
monoatomic ion transmembrane transport5-hydroxytryptamine receptor 3AHomo sapiens (human)
excitatory postsynaptic potential5-hydroxytryptamine receptor 3AHomo sapiens (human)
inorganic cation transmembrane transport5-hydroxytryptamine receptor 3AHomo sapiens (human)
regulation of presynaptic membrane potential5-hydroxytryptamine receptor 3AHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 3AHomo sapiens (human)
regulation of membrane potential5-hydroxytryptamine receptor 3AHomo sapiens (human)
cerebral cortex cell migration5-hydroxytryptamine receptor 6Homo sapiens (human)
positive regulation of TOR signaling5-hydroxytryptamine receptor 6Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 6Homo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 6Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 6Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 6Homo sapiens (human)
positive regulation of epidermal growth factor receptor signaling pathwayDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
response to hypoxiaDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
neutrophil mediated immunityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
germinal center formationDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of leukocyte chemotaxisDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
proteolysisDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
membrane protein ectodomain proteolysisDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cell adhesionDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
Notch receptor processingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of cell population proliferationDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
response to xenobiotic stimulusDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of T cell chemotaxisDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
protein processingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
signal releaseDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
B cell differentiationDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of cell growthDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of cell migrationDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
response to lipopolysaccharideDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of chemokine productionDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of tumor necrosis factor productionDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
regulation of mast cell apoptotic processDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
T cell differentiation in thymusDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cell adhesion mediated by integrinDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
wound healing, spreading of epidermal cellsDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
amyloid precursor protein catabolic processDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of blood vessel endothelial cell migrationDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of cyclin-dependent protein serine/threonine kinase activityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of epidermal growth factor-activated receptor activityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of epidermal growth factor receptor signaling pathwayDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
spleen developmentDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cell motilityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
defense response to Gram-positive bacteriumDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cellular response to high density lipoprotein particle stimulusDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
commissural neuron axon guidanceDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
negative regulation of cold-induced thermogenesisDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of G1/S transition of mitotic cell cycleDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of tumor necrosis factor-mediated signaling pathwayDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of vascular endothelial cell proliferationDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
Notch signaling pathwayDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 3DHomo sapiens (human)
monoatomic ion transmembrane transport5-hydroxytryptamine receptor 3DHomo sapiens (human)
excitatory postsynaptic potential5-hydroxytryptamine receptor 3DHomo sapiens (human)
inorganic cation transmembrane transport5-hydroxytryptamine receptor 3DHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 3DHomo sapiens (human)
regulation of membrane potential5-hydroxytryptamine receptor 3DHomo sapiens (human)
glycolytic process5-hydroxytryptamine receptor 2ABos taurus (cattle)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2ABos taurus (cattle)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2ABos taurus (cattle)
phosphatidylinositol 3-kinase/protein kinase B signal transduction5-hydroxytryptamine receptor 2ABos taurus (cattle)
protein localization to cytoskeleton5-hydroxytryptamine receptor 2ABos taurus (cattle)
positive regulation of fat cell differentiation5-hydroxytryptamine receptor 2ABos taurus (cattle)
positive regulation of glycolytic process5-hydroxytryptamine receptor 2ABos taurus (cattle)
positive regulation of peptidyl-tyrosine phosphorylation5-hydroxytryptamine receptor 2ABos taurus (cattle)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2ABos taurus (cattle)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 3CHomo sapiens (human)
monoatomic ion transmembrane transport5-hydroxytryptamine receptor 3CHomo sapiens (human)
excitatory postsynaptic potential5-hydroxytryptamine receptor 3CHomo sapiens (human)
inorganic cation transmembrane transport5-hydroxytryptamine receptor 3CHomo sapiens (human)
regulation of membrane potential5-hydroxytryptamine receptor 3CHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 3CHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (54)

Processvia Protein(s)Taxonomy
serotonin-gated monoatomic cation channel activity5-hydroxytryptamine receptor 3EHomo sapiens (human)
excitatory extracellular ligand-gated monoatomic ion channel activity5-hydroxytryptamine receptor 3EHomo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potential5-hydroxytryptamine receptor 3EHomo sapiens (human)
serotonin-gated monoatomic cation channel activity5-hydroxytryptamine receptor 3BHomo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potential5-hydroxytryptamine receptor 3BHomo sapiens (human)
excitatory extracellular ligand-gated monoatomic ion channel activity5-hydroxytryptamine receptor 3BHomo 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)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 1AHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 1AHomo sapiens (human)
receptor-receptor interaction5-hydroxytryptamine receptor 1AHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 1AHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 1AHomo sapiens (human)
protein bindingNeutrophil cytosol factor 1Homo sapiens (human)
electron transfer activityNeutrophil cytosol factor 1Homo sapiens (human)
superoxide-generating NAD(P)H oxidase activityNeutrophil cytosol factor 1Homo sapiens (human)
SH3 domain bindingNeutrophil cytosol factor 1Homo sapiens (human)
phosphatidylinositol bindingNeutrophil cytosol factor 1Homo sapiens (human)
phosphatidylinositol-3,4-bisphosphate bindingNeutrophil cytosol factor 1Homo sapiens (human)
superoxide-generating NADPH oxidase activator activityNeutrophil cytosol factor 1Homo sapiens (human)
dopamine neurotransmitter receptor activity, coupled via GsD(1A) dopamine receptorHomo sapiens (human)
G-protein alpha-subunit bindingD(1A) dopamine receptorHomo sapiens (human)
dopamine neurotransmitter receptor activityD(1A) dopamine receptorHomo sapiens (human)
protein bindingD(1A) dopamine receptorHomo sapiens (human)
heterotrimeric G-protein bindingD(1A) dopamine receptorHomo sapiens (human)
dopamine bindingD(1A) dopamine receptorHomo sapiens (human)
arrestin family protein bindingD(1A) dopamine receptorHomo sapiens (human)
G protein-coupled receptor activityD(1A) dopamine receptorHomo 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)
integrin bindingSodium-dependent serotonin transporterHomo sapiens (human)
monoatomic cation channel activitySodium-dependent serotonin transporterHomo sapiens (human)
neurotransmitter transmembrane transporter activitySodium-dependent serotonin transporterHomo sapiens (human)
serotonin:sodium:chloride symporter activitySodium-dependent serotonin transporterHomo sapiens (human)
protein bindingSodium-dependent serotonin transporterHomo sapiens (human)
monoamine transmembrane transporter activitySodium-dependent serotonin transporterHomo sapiens (human)
antiporter activitySodium-dependent serotonin transporterHomo sapiens (human)
syntaxin-1 bindingSodium-dependent serotonin transporterHomo sapiens (human)
cocaine bindingSodium-dependent serotonin transporterHomo sapiens (human)
sodium ion bindingSodium-dependent serotonin transporterHomo sapiens (human)
identical protein bindingSodium-dependent serotonin transporterHomo sapiens (human)
nitric-oxide synthase bindingSodium-dependent serotonin transporterHomo sapiens (human)
actin filament bindingSodium-dependent serotonin transporterHomo sapiens (human)
serotonin bindingSodium-dependent serotonin transporterHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 7Homo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 7Homo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 7Homo sapiens (human)
protein binding5-hydroxytryptamine receptor 3AHomo sapiens (human)
serotonin-gated monoatomic cation channel activity5-hydroxytryptamine receptor 3AHomo sapiens (human)
identical protein binding5-hydroxytryptamine receptor 3AHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 3AHomo sapiens (human)
ligand-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potential5-hydroxytryptamine receptor 3AHomo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potential5-hydroxytryptamine receptor 3AHomo sapiens (human)
excitatory extracellular ligand-gated monoatomic ion channel activity5-hydroxytryptamine receptor 3AHomo sapiens (human)
histamine receptor activity5-hydroxytryptamine receptor 6Homo sapiens (human)
protein binding5-hydroxytryptamine receptor 6Homo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 6Homo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 6Homo sapiens (human)
endopeptidase activityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
metalloendopeptidase activityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
Notch bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
interleukin-6 receptor bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
integrin bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
protein bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
peptidase activityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
metallopeptidase activityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
SH3 domain bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cytokine bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
PDZ domain bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
tumor necrosis factor bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
metal ion bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
metalloendopeptidase activity involved in amyloid precursor protein catabolic processDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
protein binding5-hydroxytryptamine receptor 3DHomo sapiens (human)
serotonin-gated monoatomic cation channel activity5-hydroxytryptamine receptor 3DHomo sapiens (human)
excitatory extracellular ligand-gated monoatomic ion channel activity5-hydroxytryptamine receptor 3DHomo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potential5-hydroxytryptamine receptor 3DHomo sapiens (human)
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2ABos taurus (cattle)
protein tyrosine kinase activator activity5-hydroxytryptamine receptor 2ABos taurus (cattle)
identical protein binding5-hydroxytryptamine receptor 2ABos taurus (cattle)
serotonin binding5-hydroxytryptamine receptor 2ABos taurus (cattle)
1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding5-hydroxytryptamine receptor 2ABos taurus (cattle)
protein binding5-hydroxytryptamine receptor 3CHomo sapiens (human)
serotonin-gated monoatomic cation channel activity5-hydroxytryptamine receptor 3CHomo sapiens (human)
excitatory extracellular ligand-gated monoatomic ion channel activity5-hydroxytryptamine receptor 3CHomo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potential5-hydroxytryptamine receptor 3CHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (46)

Processvia Protein(s)Taxonomy
plasma membrane5-hydroxytryptamine receptor 3EHomo sapiens (human)
postsynaptic membrane5-hydroxytryptamine receptor 3EHomo sapiens (human)
serotonin-activated cation-selective channel complex5-hydroxytryptamine receptor 3EHomo sapiens (human)
neuron projection5-hydroxytryptamine receptor 3EHomo sapiens (human)
transmembrane transporter complex5-hydroxytryptamine receptor 3EHomo sapiens (human)
synapse5-hydroxytryptamine receptor 3EHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 3EHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 3BHomo sapiens (human)
postsynaptic membrane5-hydroxytryptamine receptor 3BHomo sapiens (human)
serotonin-activated cation-selective channel complex5-hydroxytryptamine receptor 3BHomo sapiens (human)
cell surface5-hydroxytryptamine receptor 3BHomo sapiens (human)
transmembrane transporter complex5-hydroxytryptamine receptor 3BHomo sapiens (human)
synapse5-hydroxytryptamine receptor 3BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 3BHomo sapiens (human)
neuron projection5-hydroxytryptamine receptor 3BHomo 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 membrane5-hydroxytryptamine receptor 1AHomo sapiens (human)
synapse5-hydroxytryptamine receptor 1AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 1AHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 1AHomo sapiens (human)
cytosolNeutrophil cytosol factor 1Homo sapiens (human)
plasma membraneNeutrophil cytosol factor 1Homo sapiens (human)
cytoplasmic side of plasma membraneNeutrophil cytosol factor 1Homo sapiens (human)
membraneNeutrophil cytosol factor 1Homo sapiens (human)
dendriteNeutrophil cytosol factor 1Homo sapiens (human)
phagolysosomeNeutrophil cytosol factor 1Homo sapiens (human)
NADPH oxidase complexNeutrophil cytosol factor 1Homo sapiens (human)
neuronal cell bodyNeutrophil cytosol factor 1Homo sapiens (human)
cytoplasmNeutrophil cytosol factor 1Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
nucleusD(1A) dopamine receptorHomo sapiens (human)
endoplasmic reticulum membraneD(1A) dopamine receptorHomo sapiens (human)
plasma membraneD(1A) dopamine receptorHomo sapiens (human)
ciliumD(1A) dopamine receptorHomo sapiens (human)
presynaptic membraneD(1A) dopamine receptorHomo sapiens (human)
dendritic spineD(1A) dopamine receptorHomo sapiens (human)
postsynaptic membraneD(1A) dopamine receptorHomo sapiens (human)
ciliary membraneD(1A) dopamine receptorHomo sapiens (human)
non-motile ciliumD(1A) dopamine receptorHomo sapiens (human)
glutamatergic synapseD(1A) dopamine receptorHomo sapiens (human)
GABA-ergic synapseD(1A) dopamine receptorHomo sapiens (human)
G protein-coupled receptor complexD(1A) dopamine receptorHomo sapiens (human)
plasma membraneD(1A) dopamine receptorHomo 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)
plasma membraneSodium-dependent serotonin transporterHomo sapiens (human)
focal adhesionSodium-dependent serotonin transporterHomo sapiens (human)
endosome membraneSodium-dependent serotonin transporterHomo sapiens (human)
endomembrane systemSodium-dependent serotonin transporterHomo sapiens (human)
presynaptic membraneSodium-dependent serotonin transporterHomo sapiens (human)
membrane raftSodium-dependent serotonin transporterHomo sapiens (human)
synapseSodium-dependent serotonin transporterHomo sapiens (human)
postsynaptic membraneSodium-dependent serotonin transporterHomo sapiens (human)
serotonergic synapseSodium-dependent serotonin transporterHomo sapiens (human)
synapseSodium-dependent serotonin transporterHomo sapiens (human)
plasma membraneSodium-dependent serotonin transporterHomo sapiens (human)
neuron projectionSodium-dependent serotonin transporterHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 7Homo sapiens (human)
trans-Golgi network membrane5-hydroxytryptamine receptor 7Homo sapiens (human)
synapse5-hydroxytryptamine receptor 7Homo sapiens (human)
dendrite5-hydroxytryptamine receptor 7Homo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 7Homo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 3AHomo sapiens (human)
cleavage furrow5-hydroxytryptamine receptor 3AHomo sapiens (human)
postsynaptic membrane5-hydroxytryptamine receptor 3AHomo sapiens (human)
serotonin-activated cation-selective channel complex5-hydroxytryptamine receptor 3AHomo sapiens (human)
synapse5-hydroxytryptamine receptor 3AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 3AHomo sapiens (human)
transmembrane transporter complex5-hydroxytryptamine receptor 3AHomo sapiens (human)
neuron projection5-hydroxytryptamine receptor 3AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 6Homo sapiens (human)
cilium5-hydroxytryptamine receptor 6Homo sapiens (human)
synapse5-hydroxytryptamine receptor 6Homo sapiens (human)
dendrite5-hydroxytryptamine receptor 6Homo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 6Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
cell-cell junctionDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
focal adhesionDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
ruffle membraneDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
Golgi membraneDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cytoplasmDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
endoplasmic reticulum lumenDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cytosolDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
plasma membraneDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cell surfaceDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
actin cytoskeletonDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
membraneDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
apical plasma membraneDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
membrane raftDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
plasma membraneDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 3DHomo sapiens (human)
postsynaptic membrane5-hydroxytryptamine receptor 3DHomo sapiens (human)
serotonin-activated cation-selective channel complex5-hydroxytryptamine receptor 3DHomo sapiens (human)
synapse5-hydroxytryptamine receptor 3DHomo sapiens (human)
transmembrane transporter complex5-hydroxytryptamine receptor 3DHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 3DHomo sapiens (human)
neuron projection5-hydroxytryptamine receptor 3DHomo sapiens (human)
caveola5-hydroxytryptamine receptor 2ABos taurus (cattle)
axon5-hydroxytryptamine receptor 2ABos taurus (cattle)
cytoplasmic vesicle5-hydroxytryptamine receptor 2ABos taurus (cattle)
presynapse5-hydroxytryptamine receptor 2ABos taurus (cattle)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2ABos taurus (cattle)
plasma membrane5-hydroxytryptamine receptor 3CHomo sapiens (human)
postsynaptic membrane5-hydroxytryptamine receptor 3CHomo sapiens (human)
serotonin-activated cation-selective channel complex5-hydroxytryptamine receptor 3CHomo sapiens (human)
synapse5-hydroxytryptamine receptor 3CHomo sapiens (human)
transmembrane transporter complex5-hydroxytryptamine receptor 3CHomo sapiens (human)
neuron projection5-hydroxytryptamine receptor 3CHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 3CHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (132)

Assay IDTitleYearJournalArticle
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.
AID4424The compound was tested for the binding affinity against 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT as radioligand.1999Journal of medicinal chemistry, Oct-21, Volume: 42, Issue:21
Pyrroloquinoxaline derivatives as high-affinity and selective 5-HT(3) receptor agonists: synthesis, further structure-activity relationships, and biological studies.
AID5154Binding affinity towards 5-hydroxytryptamine 2A receptor1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.
AID5757The compound was tested for the binding affinity against 5-hydroxytryptamine 2C receptor using [3H]Mesulergine as radioligand.1999Journal of medicinal chemistry, Oct-21, Volume: 42, Issue:21
Pyrroloquinoxaline derivatives as high-affinity and selective 5-HT(3) receptor agonists: synthesis, further structure-activity relationships, and biological studies.
AID6328Intrinsic activity towards 5-hydroxytryptamine 3 receptor was determined by Benzold-Jarisch reflex (peripheral assay); PA: Partial agonist2002Bioorganic & medicinal chemistry letters, Oct-07, Volume: 12, Issue:19
Electrostatic potential surfaces of 5-HT(3)R agonists suggest accessory cation-pi site adjacent to agonist binding domain.
AID5273Binding affinity to 5-hydroxytryptamine 2 receptor in rat frontal cortical membranes by [3H]- KET displacement.1987Journal of medicinal chemistry, Jan, Volume: 30, Issue:1
Central serotonin receptors as targets for drug research.
AID4693Binding affinity against 5-hydroxytryptamine 1B receptor of rat striatum.1999Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
Novel potent and selective central 5-HT3 receptor ligands provided with different intrinsic efficacy. 2. Molecular basis of the intrinsic efficacy of arylpiperazine derivatives at the central 5-HT3 receptors.
AID6355Binding affinity against 5-hydroxytryptamine 3 receptor was measured using [3H]granisetron as radioligand1997Journal of medicinal chemistry, Jun-06, Volume: 40, Issue:12
Novel and selective partial agonists of 5-HT3 receptors. 2. Synthesis and biological evaluation of piperazinopyridopyrrolopyrazines, piperazinopyrroloquinoxalines, and piperazinopyridopyrroloquinoxalines.
AID6232Inhibition of radiolabeled [3H]GR-113808 ligand binding to 5-hydroxytryptamine 4 receptor1997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
Novel and highly potent 5-HT3 receptor agonists based on a pyrroloquinoxaline structure.
AID4708The compound was tested for their binding affinity towards 5-hydroxytryptamine 1B receptor from rat striatum using [3H]5-HT as radioligand1995Journal of medicinal chemistry, Jul-07, Volume: 38, Issue:14
Novel, potent, and selective 5-HT3 receptor antagonists based on the arylpiperazine skeleton: synthesis, structure, biological activity, and comparative molecular field analysis studies.
AID3770Inhibition of radiolabeled [3H]-8-OH-DPAT ligand binding to 5-hydroxytryptamine 1A receptor1997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
Novel and highly potent 5-HT3 receptor agonists based on a pyrroloquinoxaline structure.
AID6128Intrinsic efficacy against 5-hydroxytryptamine 3 receptor; A means pure agonist1999Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
Novel potent and selective central 5-HT3 receptor ligands provided with different intrinsic efficacy. 2. Molecular basis of the intrinsic efficacy of arylpiperazine derivatives at the central 5-HT3 receptors.
AID204521Ability to displace [3H]paroxetine bound to Serotonin transporter receptor in rat forebrain1998Journal of medicinal chemistry, Feb-26, Volume: 41, Issue:5
Novel potent and selective central 5-HT3 receptor ligands provided with different intrinsic efficacy. 1. Mapping the central 5-HT3 receptor binding site by arylpiperazine derivatives.
AID6492Binding affinity towards mouse 5-hydroxytryptamine 5A receptor was evaluated using [3H]LSD as radioligand2003Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14
Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7).
AID5342The compound was tested for the binding affinity against 5-hydroxytryptamine 2A receptor using [3H]ketanserin as radioligand.1999Journal of medicinal chemistry, Oct-21, Volume: 42, Issue:21
Pyrroloquinoxaline derivatives as high-affinity and selective 5-HT(3) receptor agonists: synthesis, further structure-activity relationships, and biological studies.
AID297964Displacement of [3H]methyllycaconitine from human alpha-7 in tsA201 cells coexpressed with 5HT3A receptor2007Journal of medicinal chemistry, Sep-20, Volume: 50, Issue:19
Pharmacological characteristics and binding modes of caracurine V analogues and related compounds at the neuronal alpha7 nicotinic acetylcholine receptor.
AID4686Ability to displace [3H]5-HT bound to 5-hydroxytryptamine 1B receptor in rat striatum1998Journal of medicinal chemistry, Feb-26, Volume: 41, Issue:5
Novel potent and selective central 5-HT3 receptor ligands provided with different intrinsic efficacy. 1. Mapping the central 5-HT3 receptor binding site by arylpiperazine derivatives.
AID441240Displacement of [3H]LY278584 from 5HT3 receptor in rat cortical homogenate2009Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21
Novel, potent, and selective quinoxaline-based 5-HT(3) receptor ligands. 1. Further structure-activity relationships and pharmacological characterization.
AID233645Ratio of the binding constants for 5-HT3 receptor and 5-HT1A receptor1995Journal of medicinal chemistry, Jul-07, Volume: 38, Issue:14
Novel, potent, and selective 5-HT3 receptor antagonists based on the arylpiperazine skeleton: synthesis, structure, biological activity, and comparative molecular field analysis studies.
AID5581Binding affinity to 5-hydroxytryptamine 2A receptor from rat cortex assayed using [3H]ketanserin as radioligand.1995Journal of medicinal chemistry, Jul-07, Volume: 38, Issue:14
Novel, potent, and selective 5-HT3 receptor antagonists based on the arylpiperazine skeleton: synthesis, structure, biological activity, and comparative molecular field analysis studies.
AID5724Binding affinity against 5-hydroxytryptamine 2C receptor of rat cortex.1999Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
Novel potent and selective central 5-HT3 receptor ligands provided with different intrinsic efficacy. 2. Molecular basis of the intrinsic efficacy of arylpiperazine derivatives at the central 5-HT3 receptors.
AID731817Displacement of [3H]dihydroalprenolol from human wild type beta1 adrenergic receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis2013Journal of medicinal chemistry, May-09, Volume: 56, Issue:9
Biophysical fragment screening of the β1-adrenergic receptor: identification of high affinity arylpiperazine leads using structure-based drug design.
AID731818Binding affinity to His-tagged human beta1 adrenergic receptor expressed in HEK293 cell membranes by surface plasmon resonance analysis2013Journal of medicinal chemistry, May-09, Volume: 56, Issue:9
Biophysical fragment screening of the β1-adrenergic receptor: identification of high affinity arylpiperazine leads using structure-based drug design.
AID180155Inhibitory activity for 5-HT uptake was determined using [3H]- Citalopram1997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
Novel and highly potent 5-HT3 receptor agonists based on a pyrroloquinoxaline structure.
AID4364The compound was tested for their binding affinity towards 5-hydroxytryptamine 1A receptor from rat hippocampus using [3H]-8-OH-DPAT as radioligand1995Journal of medicinal chemistry, Jul-07, Volume: 38, Issue:14
Novel, potent, and selective 5-HT3 receptor antagonists based on the arylpiperazine skeleton: synthesis, structure, biological activity, and comparative molecular field analysis studies.
AID4851Binding affinity against 5-hydroxytryptamine 1D receptor was measured using [3H]5-HT as radioligand1997Journal of medicinal chemistry, Jun-06, Volume: 40, Issue:12
Novel and selective partial agonists of 5-HT3 receptors. 2. Synthesis and biological evaluation of piperazinopyridopyrrolopyrazines, piperazinopyrroloquinoxalines, and piperazinopyridopyrroloquinoxalines.
AID235505Selectivity the ratio of binding affinity against 5-HT transporter to that of 5-HT3 receptor1998Journal of medicinal chemistry, Feb-26, Volume: 41, Issue:5
Novel potent and selective central 5-HT3 receptor ligands provided with different intrinsic efficacy. 1. Mapping the central 5-HT3 receptor binding site by arylpiperazine derivatives.
AID235509Selectivity the ratio of binding affinity against 5-HT2C receptor to that of 5-HT3 receptor1998Journal of medicinal chemistry, Feb-26, Volume: 41, Issue:5
Novel potent and selective central 5-HT3 receptor ligands provided with different intrinsic efficacy. 1. Mapping the central 5-HT3 receptor binding site by arylpiperazine derivatives.
AID441266Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum2009Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21
Novel, potent, and selective quinoxaline-based 5-HT(3) receptor ligands. 1. Further structure-activity relationships and pharmacological characterization.
AID5898Inhibitory activity against 5-hydroxytryptamine 3 receptor in rat cortical membranes using [3H]- 1-Methyl-1H-indazole-3-carboxylic acid (8-methyl-8-aza-bicyclo[3.2.1]oct-3-yl)-amide as a radioligand1990Journal of medicinal chemistry, Dec, Volume: 33, Issue:12
Synthesis and biochemical evaluation of tritium-labeled 1-methyl-N-(8-methyl-8-azabicyclo[3.2.1]oct-3-yl)-1H-indazole-3-carboxa mide, a useful radioligand for 5HT3 receptors.
AID6008The binding affinity was measured for 5-hydroxytryptamine 3 receptor on NG 108-15 cell line of mouse neuroblastoma-glioma cells in presence of [3H]5 radioligand (in vitro)1990Journal of medicinal chemistry, Nov, Volume: 33, Issue:11
Synthesis, in vitro binding profile, and central nervous system penetrability of the highly potent 5-HT3 receptor antagonist [3H]-4-(2-methoxyphenyl)-2-[4(5)-methyl-5(4)-imidazolylmethyl]thiazole.
AID204703Inhibition of [3H]citalopram binding to Serotonin transporter of rat cerebral cortex2000Bioorganic & medicinal chemistry letters, Jul-17, Volume: 10, Issue:14
Syntheses and binding affinities of 6-nitroquipazine analogues for serotonin transporter. Part 1.
AID5498Ability to displace [3H]- ketanserin bound to 5-hydroxytryptamine 2A receptor in rat pre-frontal cortex1998Journal of medicinal chemistry, Feb-26, Volume: 41, Issue:5
Novel potent and selective central 5-HT3 receptor ligands provided with different intrinsic efficacy. 1. Mapping the central 5-HT3 receptor binding site by arylpiperazine derivatives.
AID1132774Central serotoninmimetic activity in CF mouse assessed as induction of head twitches at 6 mg/kg, ip after 60 mins1978Journal of medicinal chemistry, Jun, Volume: 21, Issue:6
Piperazinylpyrazines with central serotoninmimetic activity.
AID1507220Agonist activity at 5-HT2A receptor in human MCF7 cells assessed as increase in calcium flux at 5 uM measured at 5 secs time interval for 2 mins by Fluo-4AM dye based fluorescence microscopic analysis2017European journal of medicinal chemistry, Aug-18, Volume: 1364-Phenyl quinoline derivatives as potential serotonin receptor ligands with antiproliferative activity.
AID5710Ability to displace [3H]mesulergine bound to 5-hydroxytryptamine 2C receptor in rat cortex1998Journal of medicinal chemistry, Feb-26, Volume: 41, Issue:5
Novel potent and selective central 5-HT3 receptor ligands provided with different intrinsic efficacy. 1. Mapping the central 5-HT3 receptor binding site by arylpiperazine derivatives.
AID235507Selectivity the ratio of binding affinity against 5-HT1B receptor to that of 5-HT3 receptor1998Journal of medicinal chemistry, Feb-26, Volume: 41, Issue:5
Novel potent and selective central 5-HT3 receptor ligands provided with different intrinsic efficacy. 1. Mapping the central 5-HT3 receptor binding site by arylpiperazine derivatives.
AID644742Displacement of [3H]-5HT from human SERT2012European journal of medicinal chemistry, Mar, Volume: 49Synthesis, in vitro binding studies and docking of long-chain arylpiperazine nitroquipazine analogues, as potential serotonin transporter inhibitors.
AID375321Displacement of [3H]LY278584 from 5HT3 receptor in rat cortical homogenate2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Specific targeting of peripheral serotonin 5-HT(3) receptors. Synthesis, biological investigation, and structure-activity relationships.
AID1132775Central serotoninmimetic activity in CF mouse assessed as induction of head twitches at 30 mg/kg, ip after 60 mins1978Journal of medicinal chemistry, Jun, Volume: 21, Issue:6
Piperazinylpyrazines with central serotoninmimetic activity.
AID6357Binding affinity towards 5-hydroxytryptamine 3 receptor1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.
AID5238Binding affinity to rat cortical membranes at 5-hydroxytryptamine 2 receptor binding site by using [3H]- DOB as a radioligand1987Journal of medicinal chemistry, Jan, Volume: 30, Issue:1
Central serotonin receptors as targets for drug research.
AID297961Displacement of [3H]epibatidine from rat recombinant alpha-4-beta-2 nAChR in HEK293 cell line2007Journal of medicinal chemistry, Sep-20, Volume: 50, Issue:19
Pharmacological characteristics and binding modes of caracurine V analogues and related compounds at the neuronal alpha7 nicotinic acetylcholine receptor.
AID4096Evaluated for the binding affinity to hippocampus striatal membranes at 5-hydroxytryptamine 1A receptor binding site by using [3H]-8-OH- DPAT as a radioligand.1987Journal of medicinal chemistry, Jan, Volume: 30, Issue:1
Central serotonin receptors as targets for drug research.
AID1582676Binding affinity to immobilized recombinant human His-tagged p47phox SH3A-B domain (151 to 285 residues) expressed in Escherichia coli BL21 (DE3) cells assessed as dissociation constant by SPR assay2020Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3
Developing Inhibitors of the p47phox-p22phox Protein-Protein Interaction by Fragment-Based Drug Discovery.
AID297966Displacement of [3H]GR65630 from human 5HT3A receptor in HEK293 cells2007Journal of medicinal chemistry, Sep-20, Volume: 50, Issue:19
Pharmacological characteristics and binding modes of caracurine V analogues and related compounds at the neuronal alpha7 nicotinic acetylcholine receptor.
AID5489Inhibition of radiolabeled [3H]-Ketanserin ligand binding to 5-hydroxytryptamine 2A receptor1997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
Novel and highly potent 5-HT3 receptor agonists based on a pyrroloquinoxaline structure.
AID6329Intrinsic activity towards CNS 5-hydroxytryptamine 3 receptor was determined; A: agonist2002Bioorganic & medicinal chemistry letters, Oct-07, Volume: 12, Issue:19
Electrostatic potential surfaces of 5-HT(3)R agonists suggest accessory cation-pi site adjacent to agonist binding domain.
AID6297The compound was tested for the binding affinity against 5-hydroxytryptamine 3 receptor using [3H]zacopride as radioligand.1999Journal of medicinal chemistry, Oct-21, Volume: 42, Issue:21
Pyrroloquinoxaline derivatives as high-affinity and selective 5-HT(3) receptor agonists: synthesis, further structure-activity relationships, and biological studies.
AID441264Displacement of [3H]8-OHDPAT from 5HT1A receptor in rat hippocampus2009Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21
Novel, potent, and selective quinoxaline-based 5-HT(3) receptor ligands. 1. Further structure-activity relationships and pharmacological characterization.
AID5267Displacement of [3H]ketanserin from 5-hydroxytryptamine 2 receptor of rat cortical membrane homogenates1986Journal of medicinal chemistry, Nov, Volume: 29, Issue:11
5-HT1 and 5-HT2 binding characteristics of some quipazine analogues.
AID4679Inhibition of radiolabeled [3H]-5-HT ligand binding to 5-hydroxytryptamine 1B receptor1997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
Novel and highly potent 5-HT3 receptor agonists based on a pyrroloquinoxaline structure.
AID375322Displacement of [3H]8-OHDPAT from 5HT1A receptor in rat hippocampus2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Specific targeting of peripheral serotonin 5-HT(3) receptors. Synthesis, biological investigation, and structure-activity relationships.
AID6284Binding affinity to 5-hydroxytryptamine 3 receptor using [3H]GR-65630 as radioligand in rat cortex1990Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
Conformation-activity relationship study of 5-HT3 receptor antagonists and a definition of a model for this receptor site.
AID5153Binding affinity against 5-hydroxytryptamine 2A receptor was measured using [3H]ketanserin as radioligand1997Journal of medicinal chemistry, Jun-06, Volume: 40, Issue:12
Novel and selective partial agonists of 5-HT3 receptors. 2. Synthesis and biological evaluation of piperazinopyridopyrrolopyrazines, piperazinopyrroloquinoxalines, and piperazinopyridopyrroloquinoxalines.
AID4004Binding affinity against 5-hydroxytryptamine 1A receptor of rat hippocampus tissue.1999Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
Novel potent and selective central 5-HT3 receptor ligands provided with different intrinsic efficacy. 2. Molecular basis of the intrinsic efficacy of arylpiperazine derivatives at the central 5-HT3 receptors.
AID5707Inhibition of radiolabeled [3H]mesulergine ligand binding to 5-hydroxytryptamine 2C receptor1997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
Novel and highly potent 5-HT3 receptor agonists based on a pyrroloquinoxaline structure.
AID5911Binding affinity for 5-hydroxytryptamine 3 receptor from rat cortex using [3H]BRL-43694 as radioligand1995Journal of medicinal chemistry, Jul-07, Volume: 38, Issue:14
Novel, potent, and selective 5-HT3 receptor antagonists based on the arylpiperazine skeleton: synthesis, structure, biological activity, and comparative molecular field analysis studies.
AID233647Ratio of the binding constants for 5-HT3 receptor and 5-HT2 receptor1995Journal of medicinal chemistry, Jul-07, Volume: 38, Issue:14
Novel, potent, and selective 5-HT3 receptor antagonists based on the arylpiperazine skeleton: synthesis, structure, biological activity, and comparative molecular field analysis studies.
AID297965Displacement of [3H]methyllycaconitine from alpha7 nAChR in tsA201 cells co-expressed with Ric32007Journal of medicinal chemistry, Sep-20, Volume: 50, Issue:19
Pharmacological characteristics and binding modes of caracurine V analogues and related compounds at the neuronal alpha7 nicotinic acetylcholine receptor.
AID644741Displacement of [3H]8-OH-DPAT from 5HT1A receptor in cerebral cortex homogenates after 15 mins2012European journal of medicinal chemistry, Mar, Volume: 49Synthesis, in vitro binding studies and docking of long-chain arylpiperazine nitroquipazine analogues, as potential serotonin transporter inhibitors.
AID233646Ratio of the binding constants for 5-HT3 receptor and 5-HT1B receptor1995Journal of medicinal chemistry, Jul-07, Volume: 38, Issue:14
Novel, potent, and selective 5-HT3 receptor antagonists based on the arylpiperazine skeleton: synthesis, structure, biological activity, and comparative molecular field analysis studies.
AID1582668Covalent inhibition of recombinant human His-tagged p47phox SH3A-B domain (151 to 285 residues) expressed in Escherichia coli BL21 (DE3) cells interaction with Cy5-p22phox149-162 incubated for 10 mins by fluorescence polarization competition assay2020Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3
Developing Inhibitors of the p47phox-p22phox Protein-Protein Interaction by Fragment-Based Drug Discovery.
AID117217Lethal dose was evaluated against reserpine induced hypothermia in mice by intraperitoneal administration1985Journal of medicinal chemistry, Oct, Volume: 28, Issue:10
Design, synthesis, and pharmacological activities of 2-substituted 4-phenylquinolines as potential antidepressant drugs.
AID375323Displacement of [3H]ketanserin from 5HT2A receptor in rat cortex2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Specific targeting of peripheral serotonin 5-HT(3) receptors. Synthesis, biological investigation, and structure-activity relationships.
AID6080Binding affinity against 5-hydroxytryptamine 3 (5-HT3) receptor from rat cortical homogenate using [3H]zacopride as radioligand1999Journal of medicinal chemistry, Oct-21, Volume: 42, Issue:21
Pyrroloquinoxaline derivatives as high-affinity and selective 5-HT(3) receptor agonists: synthesis, further structure-activity relationships, and biological studies.
AID6493Binding affinity towards murine 5-hydroxytryptamine 5A receptor2003Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14
Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7).
AID644740Displacement of [3H]-Citalopram from SERT in rat cerebral cortex homogenates after 1 hr by liquid scintillation counter2012European journal of medicinal chemistry, Mar, Volume: 49Synthesis, in vitro binding studies and docking of long-chain arylpiperazine nitroquipazine analogues, as potential serotonin transporter inhibitors.
AID6335Binding affinity towards 5-hydroxytryptamine 3 receptor2002Bioorganic & medicinal chemistry letters, Oct-07, Volume: 12, Issue:19
Electrostatic potential surfaces of 5-HT(3)R agonists suggest accessory cation-pi site adjacent to agonist binding domain.
AID235508Selectivity the ratio of binding affinity against 5-HT2A receptor to that of 5-HT3 receptor1998Journal of medicinal chemistry, Feb-26, Volume: 41, Issue:5
Novel potent and selective central 5-HT3 receptor ligands provided with different intrinsic efficacy. 1. Mapping the central 5-HT3 receptor binding site by arylpiperazine derivatives.
AID112173Effective dose was evaluated for its antagonism to reserpine induced hypothermia in mice by intraperitoneal administration1985Journal of medicinal chemistry, Oct, Volume: 28, Issue:10
Design, synthesis, and pharmacological activities of 2-substituted 4-phenylquinolines as potential antidepressant drugs.
AID4699Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.1987Journal of medicinal chemistry, Jan, Volume: 30, Issue:1
Central serotonin receptors as targets for drug research.
AID3459Binding affinity for 5-hydroxytryptamine 1A receptor1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.
AID375324Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Specific targeting of peripheral serotonin 5-HT(3) receptors. Synthesis, biological investigation, and structure-activity relationships.
AID143675The compound was tested for efficacy against 5-Hydroxytryptamine 3 receptor by measuring [14C]guanidinium uptake on NG108-15 cells; PA=Partial agonist1999Journal of medicinal chemistry, Oct-21, Volume: 42, Issue:21
Pyrroloquinoxaline derivatives as high-affinity and selective 5-HT(3) receptor agonists: synthesis, further structure-activity relationships, and biological studies.
AID5270Binding affinity to rat cortical membranes at 5-hydroxytryptamine 2 (5-HT2) receptor using [3H]KET as a radioligand1987Journal of medicinal chemistry, Jan, Volume: 30, Issue:1
Central serotonin receptors as targets for drug research.
AID4203Ability to displace [3H]- -OH-DPAT bound to 5-hydroxytryptamine 1A receptor in rat hippocampus1998Journal of medicinal chemistry, Feb-26, Volume: 41, Issue:5
Novel potent and selective central 5-HT3 receptor ligands provided with different intrinsic efficacy. 1. Mapping the central 5-HT3 receptor binding site by arylpiperazine derivatives.
AID6343Compound was tested for the inhibition of [3H]GR-65630 binding to 5-hydroxytryptamine 3 receptor expressed in NG 108-15 cells1996Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
Structure-activity relationships for the binding of arylpiperazines and arylbiguanides at 5-HT3 serotonin receptors.
AID6678Binding affinity of compound towards rodent 5-hydroxytryptamine 7 receptor2003Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14
Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7).
AID5893Ability to displace [3H]granisetron specifically bound to 5-hydroxytryptamine 3 receptor in rat cortical membrane1998Journal of medicinal chemistry, Feb-26, Volume: 41, Issue:5
Novel potent and selective central 5-HT3 receptor ligands provided with different intrinsic efficacy. 1. Mapping the central 5-HT3 receptor binding site by arylpiperazine derivatives.
AID188742Effect on the wet dog shake response(WDS) in rats after 9 determinations at a dose of 1 mg/kg, sc pretreated with 200 mg/kg ip of pCPA.1998Journal of medicinal chemistry, May-21, Volume: 41, Issue:11
(R)-(+)-2-[[[3-(Morpholinomethyl)-2H-chromen-8-yl]oxy]methyl] morpholine methanesulfonate: a new selective rat 5-hydroxytryptamine1B receptor antagonist.
AID3697Displacement of [3H]5-HT from 5-hydroxytryptamine 1 receptor of rat cortical membrane homogenates1986Journal of medicinal chemistry, Nov, Volume: 29, Issue:11
5-HT1 and 5-HT2 binding characteristics of some quipazine analogues.
AID143669Agonist/antagonist activity by observing the uptake of [14C]guanidinium, on the neuroblastoma-glioma hybrid NG108-15 cells; pure agonist1997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
Novel and highly potent 5-HT3 receptor agonists based on a pyrroloquinoxaline structure.
AID4747Evaluated for the binding affinity to porcine choroid plexus at 5-hydroxytryptamine 2C receptor binding site by using [3H]-MES as a radioligand.1987Journal of medicinal chemistry, Jan, Volume: 30, Issue:1
Central serotonin receptors as targets for drug research.
AID5891Compound was evaluated for its binding affinity for 5-hydroxytryptamine 3 receptor by measuring displacement [3H]GR-65630 in rat cerebral cortex1998Journal of medicinal chemistry, Jan-29, Volume: 41, Issue:3
5-HT3 antagonists derived from aminopyridazine-type muscarinic M1 agonists.
AID205022Effect of compound on Serotonin transporter uptake from rat cortex using [3H]citalopram as radioligand1995Journal of medicinal chemistry, Jul-07, Volume: 38, Issue:14
Novel, potent, and selective 5-HT3 receptor antagonists based on the arylpiperazine skeleton: synthesis, structure, biological activity, and comparative molecular field analysis studies.
AID4298Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand1997Journal of medicinal chemistry, Jun-06, Volume: 40, Issue:12
Novel and selective partial agonists of 5-HT3 receptors. 2. Synthesis and biological evaluation of piperazinopyridopyrrolopyrazines, piperazinopyrroloquinoxalines, and piperazinopyridopyrroloquinoxalines.
AID143663Quantitative effect on the [14C]guanidinium accumulation in NG 108-15 cells.1999Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
Novel potent and selective central 5-HT3 receptor ligands provided with different intrinsic efficacy. 2. Molecular basis of the intrinsic efficacy of arylpiperazine derivatives at the central 5-HT3 receptors.
AID235506Selectivity the ratio of binding affinity against 5-HT1A receptor to that of 5-HT3 receptor1998Journal of medicinal chemistry, Feb-26, Volume: 41, Issue:5
Novel potent and selective central 5-HT3 receptor ligands provided with different intrinsic efficacy. 1. Mapping the central 5-HT3 receptor binding site by arylpiperazine derivatives.
AID4852Binding affinity for 5-hydroxytryptamine 1D receptor1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.
AID438555Binding affinity to 5HT1A receptor2009Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19
Physical binding pocket induction for affinity prediction.
AID143666Effective concentration for uptake of [14C]guanidinium on NG108-15 cells1997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
Novel and highly potent 5-HT3 receptor agonists based on a pyrroloquinoxaline structure.
AID297963Displacement of [3H]epibatidine from recombinant rat alpha-4-beta-4 nAChr in HEK293 cell line2007Journal of medicinal chemistry, Sep-20, Volume: 50, Issue:19
Pharmacological characteristics and binding modes of caracurine V analogues and related compounds at the neuronal alpha7 nicotinic acetylcholine receptor.
AID5528Binding affinity against 5-hydroxytryptamine 2A receptor of rat pre-frontal cortex.1999Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
Novel potent and selective central 5-HT3 receptor ligands provided with different intrinsic efficacy. 2. Molecular basis of the intrinsic efficacy of arylpiperazine derivatives at the central 5-HT3 receptors.
AID6298pKi value for inhibition of [3H]LY-278584 binding to 5-hydroxytryptamine 3 receptor1990Journal of medicinal chemistry, Dec, Volume: 33, Issue:12
Synthesis and biochemical evaluation of tritium-labeled 1-methyl-N-(8-methyl-8-azabicyclo[3.2.1]oct-3-yl)-1H-indazole-3-carboxa mide, a useful radioligand for 5HT3 receptors.
AID3695Evaluated for binding affinity towards rat cortical membranes at 5-hydroxytryptamine 1 receptor binding site by using [3H]-5-HT as a radioligand.1987Journal of medicinal chemistry, Jan, Volume: 30, Issue:1
Central serotonin receptors as targets for drug research.
AID233644Ratio of the binding constants for 5-HT3 receptor and 5-HT receptor1995Journal of medicinal chemistry, Jul-07, Volume: 38, Issue:14
Novel, potent, and selective 5-HT3 receptor antagonists based on the arylpiperazine skeleton: synthesis, structure, biological activity, and comparative molecular field analysis studies.
AID6011Binding affinity towards 5-hydroxytryptamine 3 receptor was determined by using [3H]-ICS 205-930 as radioligand in mouse N1E 115 cells1990Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
Conformation-activity relationship study of 5-HT3 receptor antagonists and a definition of a model for this receptor site.
AID5685Binding affinity towards 5-hydroxytryptamine 2C receptor1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.
AID4299Binding affinity for 5-hydroxytryptamine 1B receptor1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Novel selective and partial agonists of 5-HT3 receptors. Part 1. Synthesis and biological evaluation of piperazinopyrrolothienopyrazines.
AID6514Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand2003Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14
Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7).
AID6132Inhibition of [3H]granisetron binding to 5-hydroxytryptamine 3 receptor of rat cortical membrane1999Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
Novel potent and selective central 5-HT3 receptor ligands provided with different intrinsic efficacy. 2. Molecular basis of the intrinsic efficacy of arylpiperazine derivatives at the central 5-HT3 receptors.
AID441265Displacement of [3H]ketanserin from 5HT2A receptor in rat cortex2009Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21
Novel, potent, and selective quinoxaline-based 5-HT(3) receptor ligands. 1. Further structure-activity relationships and pharmacological characterization.
AID297962Displacement of [3H]epibatidine from recombinant rat alpha-3-beta-4 nAChr in HEK293 cell line2007Journal of medicinal chemistry, Sep-20, Volume: 50, Issue:19
Pharmacological characteristics and binding modes of caracurine V analogues and related compounds at the neuronal alpha7 nicotinic acetylcholine receptor.
AID6069Inhibition of [3H]BRL-43694 binding to 5-hydroxytryptamine 3 receptor of rat cortical homogenate.1997Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
Novel and highly potent 5-HT3 receptor agonists based on a pyrroloquinoxaline structure.
AID4722The compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.1999Journal of medicinal chemistry, Oct-21, Volume: 42, Issue:21
Pyrroloquinoxaline derivatives as high-affinity and selective 5-HT(3) receptor agonists: synthesis, further structure-activity relationships, and biological studies.
AID6295Binding affinity at 5-hydroxytryptamine 3 receptor in rat cortical membrane by [3H]graniestron displacement.1998Journal of medicinal chemistry, Feb-26, Volume: 41, Issue:5
Novel potent and selective central 5-HT3 receptor ligands provided with different intrinsic efficacy. 1. Mapping the central 5-HT3 receptor binding site by arylpiperazine derivatives.
AID6200The compound was tested for the binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand.1999Journal of medicinal chemistry, Oct-21, Volume: 42, Issue:21
Pyrroloquinoxaline derivatives as high-affinity and selective 5-HT(3) receptor agonists: synthesis, further structure-activity relationships, and biological studies.
AID6285Binding affinity to 5-hydroxytryptamine 3 receptor using [3H]quipazine as radioligand in rat cortex1990Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
Conformation-activity relationship study of 5-HT3 receptor antagonists and a definition of a model for this receptor site.
AID143671Effective concentration against 5-Hydroxytryptamine 3 receptor by measuring [14C]guanidinium uptake on NG108-15 cells.1999Journal of medicinal chemistry, Oct-21, Volume: 42, Issue:21
Pyrroloquinoxaline derivatives as high-affinity and selective 5-HT(3) receptor agonists: synthesis, further structure-activity relationships, and biological studies.
AID6180The compound was tested for their binding affinity towards 5-HT4 receptor from guinea pig striatum using [3H]GR-113808 as radioligand; Nonactive at 10 uM1995Journal of medicinal chemistry, Jul-07, Volume: 38, Issue:14
Novel, potent, and selective 5-HT3 receptor antagonists based on the arylpiperazine skeleton: synthesis, structure, biological activity, and comparative molecular field analysis studies.
AID3458Binding affinity against 5-hydroxytryptamine 1A receptor was measured using [3H]8-OH-DPAT as radioligand1997Journal of medicinal chemistry, Jun-06, Volume: 40, Issue:12
Novel and selective partial agonists of 5-HT3 receptors. 2. Synthesis and biological evaluation of piperazinopyridopyrrolopyrazines, piperazinopyrroloquinoxalines, and piperazinopyridopyrroloquinoxalines.
AID235738Therapeutic index as the ratio of LD50 to that of ED50 values.1985Journal of medicinal chemistry, Oct, Volume: 28, Issue:10
Design, synthesis, and pharmacological activities of 2-substituted 4-phenylquinolines as potential antidepressant drugs.
AID188740Effect on the wet dog shake response(WDS) in rats after 10 determinations at a dose of 1 mg/kg, sc pretreated with saline1998Journal of medicinal chemistry, May-21, Volume: 41, Issue:11
(R)-(+)-2-[[[3-(Morpholinomethyl)-2H-chromen-8-yl]oxy]methyl] morpholine methanesulfonate: a new selective rat 5-hydroxytryptamine1B receptor antagonist.
AID5683Binding affinity against 5-Hydroxytryptamine 2C Receptor was measured using [3H]N-methyl-mesulergine as radioligand1997Journal of medicinal chemistry, Jun-06, Volume: 40, Issue:12
Novel and selective partial agonists of 5-HT3 receptors. 2. Synthesis and biological evaluation of piperazinopyridopyrrolopyrazines, piperazinopyrroloquinoxalines, and piperazinopyridopyrroloquinoxalines.
AID204548Binding affinity towards Serotonin transporter was determined in rat forebrain membrane1999Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
Novel potent and selective central 5-HT3 receptor ligands provided with different intrinsic efficacy. 2. Molecular basis of the intrinsic efficacy of arylpiperazine derivatives at the central 5-HT3 receptors.
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.
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.
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.
AID624216Agonists at Human 5-Hydroxytryptamine receptor 5-HT2C2000Synapse (New York, N.Y.), Feb, Volume: 35, Issue:2
Agonist high and low affinity state ratios predict drug intrinsic activity and a revised ternary complex mechanism at serotonin 5-HT(2A) and 5-HT(2C) receptors.
AID1346867Human 5-HT2B receptor (5-Hydroxytryptamine receptors)2004Naunyn-Schmiedeberg's archives of pharmacology, Aug, Volume: 370, Issue:2
Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors.
AID1346893Human 5-HT2C receptor (5-Hydroxytryptamine receptors)1999Journal of neurochemistry, May, Volume: 72, Issue:5
High-affinity agonist binding correlates with efficacy (intrinsic activity) at the human serotonin 5-HT2A and 5-HT2C receptors: evidence favoring the ternary complex and two-state models of agonist action.
AID1346893Human 5-HT2C receptor (5-Hydroxytryptamine receptors)2004Naunyn-Schmiedeberg's archives of pharmacology, Aug, Volume: 370, Issue:2
Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors.
AID624216Agonists at Human 5-Hydroxytryptamine receptor 5-HT2C1999Journal of neurochemistry, May, Volume: 72, Issue:5
High-affinity agonist binding correlates with efficacy (intrinsic activity) at the human serotonin 5-HT2A and 5-HT2C receptors: evidence favoring the ternary complex and two-state models of agonist action.
AID1259419Human 5-HT2A receptor (5-Hydroxytryptamine receptors)2004Naunyn-Schmiedeberg's archives of pharmacology, Aug, Volume: 370, Issue:2
Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors.
AID1346893Human 5-HT2C receptor (5-Hydroxytryptamine receptors)2000Synapse (New York, N.Y.), Feb, Volume: 35, Issue:2
Agonist high and low affinity state ratios predict drug intrinsic activity and a revised ternary complex mechanism at serotonin 5-HT(2A) and 5-HT(2C) receptors.
AID624216Agonists at Human 5-Hydroxytryptamine receptor 5-HT2C2004Naunyn-Schmiedeberg's archives of pharmacology, Aug, Volume: 370, Issue:2
Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors.
AID624240Agonists at Rat 5-Hydroxytryptamine receptor 5-HT2B1993Molecular pharmacology, Mar, Volume: 43, Issue:3
Pharmacological characteristics of the newly cloned rat 5-hydroxytryptamine2F receptor.
AID1346903Rat 5-HT2B receptor (5-Hydroxytryptamine receptors)1993Molecular pharmacology, Mar, Volume: 43, Issue:3
Pharmacological characteristics of the newly cloned rat 5-hydroxytryptamine2F receptor.
AID624235Agonists at Human 5-Hydroxytryptamine receptor 5-HT2A2004Naunyn-Schmiedeberg's archives of pharmacology, Aug, Volume: 370, Issue:2
Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors.
AID624219Agonists at Human 5-Hydroxytryptamine receptor 5-HT2B2004Naunyn-Schmiedeberg's archives of pharmacology, Aug, Volume: 370, Issue:2
Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (637)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990346 (54.32)18.7374
1990's171 (26.84)18.2507
2000's73 (11.46)29.6817
2010's40 (6.28)24.3611
2020's7 (1.10)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 29.87

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index29.87 (24.57)
Research Supply Index6.49 (2.92)
Research Growth Index4.19 (4.65)
Search Engine Demand Index40.78 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (29.87)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews10 (1.52%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other648 (98.48%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]