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5-hydroxytryptamine 2A receptor inverse agonist

An inverse agonist that binds to the same receptor as a 5-hydroxytryptamine 2A receptor agonist, but which induces a pharmacological response opposite to that agonist.

ChEBI ID: 133016

Members (1)

MemberDefinitionClass
pimavanserinA member of the class of ureas in which three of the four hydrogens are replaced by 4-fluorobenzyl, 1-methylpiperidin-4-yl, and 4-(isopropyloxy)benzyl groups. An atypical antipsychotic that is used (in the form of its tartrate salt) for treatment of hallucinations and delusions associated with Parkinson's disease.pimavanserin

Research

Studies (149)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's10 (6.71)29.6817
2010's79 (53.02)24.3611
2020's60 (40.27)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials23 (14.47%)5.53%
Reviews38 (23.90%)6.00%
Case Studies5 (3.14%)4.05%
Observational1 (0.63%)0.25%
Other92 (57.86%)84.16%

Protein Targets (17)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
cytochrome P450 2C9, partialHomo sapiens (human)Potency37.908311
cytochrome P450 2D6Homo sapiens (human)Potency5.354711
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency21.317411
GVesicular stomatitis virusPotency37.908311
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency37.908311
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency37.908312
Interferon betaHomo sapiens (human)Potency37.908311
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency39.810711

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
5-hydroxytryptamine receptor 2AHomo sapiens (human)IC500.033556
5-hydroxytryptamine receptor 2AHomo sapiens (human)Ki0.000923
5-hydroxytryptamine receptor 2BHomo sapiens (human)IC500.046412
5-hydroxytryptamine receptor 2CHomo sapiens (human)IC500.046412
5-hydroxytryptamine receptor 2CHomo sapiens (human)Ki0.001223
Cytochrome P450 1A2Homo sapiens (human)IC5052.000011
Cytochrome P450 2C19Homo sapiens (human)IC5049.800011
Cytochrome P450 2C9 Homo sapiens (human)IC50100.000011
Cytochrome P450 2D6Homo sapiens (human)IC50100.000011
Cytochrome P450 3A4Homo sapiens (human)IC50100.000011
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC500.410011

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
5-hydroxytryptamine receptor 2AHomo sapiens (human)Kb0.000611