Page last updated: 2024-11-10

ro 60-0175

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

Ro 60-0175: a 5HT 2C receptor agonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

1-(6-chloro-5-fluoroindol-1-yl)-propan-2-amine : A member of the class of indoles that is 6-chloro-5-fluoroindole in which the hydrogen attached to the nitrogen has been replaced by a 2-aminopropyl group. [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]

(2S)-1-(6-chloro-5-fluoroindol-1-yl)-propan-2-amine : A 1-(6-chloro-5-fluoroindol-1-yl)-propan-2-amine that has S configuration. A selective agonist for both the 5-hydroxytryptamine 2B (5-HT2B) and 5-hydroxytryptamine 2C (5-HT2C)serotonin receptor subtypes, commonly used as fumarate salt. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID5191289
CHEBI ID91736
SCHEMBL ID8959606
MeSH IDM0271426
PubMed CID3045227
CHEMBL ID76781
CHEBI ID142183
SCHEMBL ID255454
MeSH IDM0271426

Synonyms (40)

Synonym
1-(6-chloro-5-fluoroindol-1-yl)propan-2-amine
ro 60-0175
L000517
nsc_3045226
cas_3045226
bdbm85528
BRD-A49370193-051-01-7
SCHEMBL8959606
CHEBI:91736
1-(6-chloro-5-fluoroindol-1-yl)-propan-2-amine
1-(6-chloro-5-fluoro-1h-indol-1-yl)propan-2-amine
2-(6-chloro-5-fluoroindol-1-yl)-1-methylethylamine
1-(6-chloro-5-fluoro-1-indolyl)-2-propanamine
Q27163547
icx5608849
CHEMBL76781 ,
ro-600175
ro600175
gtpl166
(s)-1-(6-chloro-5-fluoro-1h-indol-1-yl)propan-2-amine
bdbm50144841
(2s)-1-(6-chloro-5-fluoroindol-1-yl)propan-2-amine
org 35030
(1s)-2-(6-chloro-5-fluoroindol-1-yl)-1-methylethylamine
(s)-2-(6-chloro-5-fluoroindol-1-yl)-1-methylethylamine
CHEBI:142183
(s)-2-(6-chloro-5-fluoro-indol-1-yl)-1-methyl-ethylamine
(2s)-1-(6-chloro-5-fluoro-1h-indol-1-yl)propan-2-amine
ro-60-0175
(s)-6-chloro-5-fluoro-alpha-methyl-1h-indole-1-ethanamine
(2s)-1-(6-chloro-5-fluoroindol-1-yl)-propan-2-amine
bdbm50428891
SCHEMBL255454
Q27088596
169675-08-5
MS-23283
HY-123838
EX-A6809
CS-0086511
AKOS040756990

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" The secondary aims were to evaluate the side effect profiles of lorcaserin and CP-809101 and to determine the plasma levels of lorcaserin at a dose (1 mg/kg) that reduces both food and nicotine reinforcement for comparison to plasma concentrations reported in human trials."( Evaluation of chemically diverse 5-HT₂c receptor agonists on behaviours motivated by food and nicotine and on side effect profiles.
Coen, K; de Lannoy, IA; Fletcher, PJ; Higgins, GA; Izhakova, J; Lau, W; Le, AD; Lee, DK; Silenieks, LB, 2013
)
0.39
" Finally, there may be differences in the side effect profiles between lorcaserin and CP-809101, raising the possibility for tolerability differences amongst 5-HT2C agonists."( Evaluation of chemically diverse 5-HT₂c receptor agonists on behaviours motivated by food and nicotine and on side effect profiles.
Coen, K; de Lannoy, IA; Fletcher, PJ; Higgins, GA; Izhakova, J; Lau, W; Le, AD; Lee, DK; Silenieks, LB, 2013
)
0.39

Dosage Studied

ExcerptRelevanceReference
" In the drug discrimination procedure, Ro-60-0175 was not generalised with nicotine but shifted the nicotine dose-response curve to the right in a dose-related manner."( The serotonin 2C receptor agonist Ro-60-0175 attenuates effects of nicotine in the five-choice serial reaction time task and in drug discrimination.
Naylor, CG; Quarta, D; Stolerman, IP, 2007
)
0.34
"25-1 mg/kg) did not alter the dose-response curve of nicotine, while DOI (0."( Effects of the serotonin 5-HT2A and 5-HT2C receptor ligands on the discriminative stimulus effects of nicotine in rats.
Filip, M; McCreary, AC; Przegaliński, E; Zaniewska, M, 2007
)
0.34
" The effects of the phenethylamine hallucinogen R(-)-2,5-dimethoxy-4-iodoamphetamine (DOI) on head-twitch behavior were studied over a range of doses in the mouse, generating a characteristic biphasic dose-response curve."( Interaction of 5-HT2A and 5-HT2C receptors in R(-)-2,5-dimethoxy-4-iodoamphetamine-elicited head twitch behavior in mice.
Cohen, MS; Fantegrossi, WE; Henson, CM; Rice, KC; Simoneau, J; Woods, JH; Zimmerman, SM, 2010
)
0.36
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
5-hydroxytryptamine 2B receptor agonistAn agonist at the 5-hydroxytryptamine 2B (5-HT2B) receptor.
5-hydroxytryptamine 2C receptor agonistAn agonist at the 5-hydroxytryptamine 2B (5-HT2C) receptor.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (5)

ClassDescription
indolesAny compound containing an indole skeleton.
organofluorine compoundAn organofluorine compound is a compound containing at least one carbon-fluorine bond.
organochlorine compoundAn organochlorine compound is a compound containing at least one carbon-chlorine bond.
primary amino compoundA compound formally derived from ammonia by replacing one hydrogen atom by an organyl group.
1-(6-chloro-5-fluoroindol-1-yl)-propan-2-amineA member of the class of indoles that is 6-chloro-5-fluoroindole in which the hydrogen attached to the nitrogen has been replaced by a 2-aminopropyl group.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (11)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
5-hydroxytryptamine receptor 2AHomo sapiens (human)Ki0.03670.00000.385510.0000AID259796; AID324621; AID5191; AID5416
5-hydroxytryptamine receptor 2CHomo sapiens (human)Ki0.00800.00010.954910.0000AID259798; AID324620; AID5645; AID5869
Glutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)Ki0.00230.00030.86666.6900AID259798
5-hydroxytryptamine receptor 2BHomo sapiens (human)Ki0.00510.00030.769310.0000AID259797; AID5764
D(2) dopamine receptorRattus norvegicus (Norway rat)Ki0.00510.00000.437510.0000AID259797
Glutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)Ki0.00230.00030.68056.6900AID259798
Glutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)Ki0.00230.00030.70716.6900AID259798
Glutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)Ki0.00230.00030.81966.6900AID259798
Glutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)Ki0.00230.00030.70726.6900AID259798
Glutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)Ki0.00230.00030.70726.6900AID259798
Glutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)Ki0.00230.00030.70726.6900AID259798
[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 2AHomo sapiens (human)EC50 (µMol)0.17800.00000.22763.4750AID259793; AID312492; AID324624; AID5162
5-hydroxytryptamine receptor 2CHomo sapiens (human)EC50 (µMol)0.02300.00010.10082.4500AID259795; AID312493; AID324623; AID5842
5-hydroxytryptamine receptor 2BHomo sapiens (human)EC50 (µMol)0.00310.00040.20611.0000AID259794; AID312494; AID324625; AID5383
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (72)

Processvia Protein(s)Taxonomy
temperature homeostasis5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cytokine production involved in immune response5-hydroxytryptamine receptor 2AHomo sapiens (human)
glycolytic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2AHomo sapiens (human)
activation of phospholipase C activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cytosolic calcium ion concentration5-hydroxytryptamine receptor 2AHomo sapiens (human)
memory5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cell population proliferation5-hydroxytryptamine receptor 2AHomo sapiens (human)
response to xenobiotic stimulus5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
regulation of dopamine secretion5-hydroxytryptamine receptor 2AHomo sapiens (human)
artery smooth muscle contraction5-hydroxytryptamine receptor 2AHomo sapiens (human)
urinary bladder smooth muscle contraction5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of heat generation5-hydroxytryptamine receptor 2AHomo sapiens (human)
negative regulation of potassium ion transport5-hydroxytryptamine receptor 2AHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transduction5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of neuron apoptotic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein localization to cytoskeleton5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of fat cell differentiation5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of glycolytic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of vasoconstriction5-hydroxytryptamine receptor 2AHomo sapiens (human)
symbiont entry into host cell5-hydroxytryptamine receptor 2AHomo sapiens (human)
sensitization5-hydroxytryptamine receptor 2AHomo sapiens (human)
behavioral response to cocaine5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of inflammatory response5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylation5-hydroxytryptamine receptor 2AHomo sapiens (human)
detection of temperature stimulus involved in sensory perception of pain5-hydroxytryptamine receptor 2AHomo sapiens (human)
detection of mechanical stimulus involved in sensory perception of pain5-hydroxytryptamine receptor 2AHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2AHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergic5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
presynaptic modulation of chemical synaptic transmission5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of execution phase of apoptosis5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of platelet aggregation5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of DNA biosynthetic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2AHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2AHomo sapiens (human)
behavioral fear response5-hydroxytryptamine receptor 2CHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2CHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
locomotory behavior5-hydroxytryptamine receptor 2CHomo sapiens (human)
feeding behavior5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2CHomo sapiens (human)
cGMP-mediated signaling5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of nervous system process5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of appetite5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of corticotropin-releasing hormone secretion5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of fat cell differentiation5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of calcium-mediated signaling5-hydroxytryptamine receptor 2CHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2CHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2CHomo sapiens (human)
neural crest cell migration5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of cytokine production5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of endothelial cell proliferation5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled receptor internalization5-hydroxytryptamine receptor 2BHomo sapiens (human)
heart morphogenesis5-hydroxytryptamine receptor 2BHomo sapiens (human)
cardiac muscle hypertrophy5-hydroxytryptamine receptor 2BHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
activation of phospholipase C activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of cell population proliferation5-hydroxytryptamine receptor 2BHomo sapiens (human)
response to xenobiotic stimulus5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2BHomo sapiens (human)
neural crest cell differentiation5-hydroxytryptamine receptor 2BHomo sapiens (human)
intestine smooth muscle contraction5-hydroxytryptamine receptor 2BHomo sapiens (human)
phosphorylation5-hydroxytryptamine receptor 2BHomo sapiens (human)
calcium-mediated signaling5-hydroxytryptamine receptor 2BHomo sapiens (human)
cGMP-mediated signaling5-hydroxytryptamine receptor 2BHomo sapiens (human)
vasoconstriction5-hydroxytryptamine receptor 2BHomo sapiens (human)
negative regulation of apoptotic process5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of canonical NF-kappaB signal transduction5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of MAP kinase activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transduction5-hydroxytryptamine receptor 2BHomo sapiens (human)
embryonic morphogenesis5-hydroxytryptamine receptor 2BHomo sapiens (human)
regulation of behavior5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of nitric-oxide synthase activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of cell division5-hydroxytryptamine receptor 2BHomo sapiens (human)
ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2BHomo sapiens (human)
protein kinase C signaling5-hydroxytryptamine receptor 2BHomo sapiens (human)
cellular response to temperature stimulus5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2BHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2BHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (12)

Processvia Protein(s)Taxonomy
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
virus receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein tyrosine kinase activator activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
identical protein binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein-containing complex binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
identical protein binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
G-protein alpha-subunit binding5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
GTPase activator activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2BHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2BHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (17)

Processvia Protein(s)Taxonomy
neurofilament5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
caveola5-hydroxytryptamine receptor 2AHomo sapiens (human)
axon5-hydroxytryptamine receptor 2AHomo sapiens (human)
cytoplasmic vesicle5-hydroxytryptamine receptor 2AHomo sapiens (human)
presynaptic membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
neuronal cell body5-hydroxytryptamine receptor 2AHomo sapiens (human)
dendritic shaft5-hydroxytryptamine receptor 2AHomo sapiens (human)
postsynaptic membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
cell body fiber5-hydroxytryptamine receptor 2AHomo sapiens (human)
glutamatergic synapse5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2CHomo sapiens (human)
synapse5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2CHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2CHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2CHomo sapiens (human)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)
nucleoplasm5-hydroxytryptamine receptor 2BHomo sapiens (human)
cytoplasm5-hydroxytryptamine receptor 2BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2BHomo sapiens (human)
synapse5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2BHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2BHomo sapiens (human)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (52)

Assay IDTitleYearJournalArticle
AID312510Selectivity ratio of pEC50 for human 5HT2A to pEC50 for human 5HT2C2008Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
Discovery and structure-activity relationship of (1R)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-benzazepine (Lorcaserin), a selective serotonin 5-HT2C receptor agonist for the treatment of obesity.
AID186084Compound was tested in schedule induced polydipsia in rats expressed as %maximum suppression at minimum effective dose of 10 mg/kg intraperitoneally1997Journal of medicinal chemistry, Aug-15, Volume: 40, Issue:17
Novel agonists of 5HT2C receptors. Synthesis and biological evaluation of substituted 2-(indol-1-yl)-1-methylethylamines and 2-(indeno[1,2-b]pyrrol-1-yl)-1-methylethylamines. Improved therapeutics for obsessive compulsive disorder.
AID324627Intrinsic activity at human cloned 5HT2A receptor expressed in CHO cells assessed as maximal stimulation of 10 uM 5HT-induced myo-[3H]inositol hydrolysis2008Bioorganic & medicinal chemistry, Feb-15, Volume: 16, Issue:4
Synthesis and structure-activity relationships of a series of substituted 2-(1H-furo[2,3-g]indazol-1-yl)ethylamine derivatives as 5-HT2C receptor agonists.
AID5416Binding affinity against human 5-hydroxytryptamine 2A receptor using displacement of [3H]5-HT1997Journal of medicinal chemistry, Aug-15, Volume: 40, Issue:17
Novel agonists of 5HT2C receptors. Synthesis and biological evaluation of substituted 2-(indol-1-yl)-1-methylethylamines and 2-(indeno[1,2-b]pyrrol-1-yl)-1-methylethylamines. Improved therapeutics for obsessive compulsive disorder.
AID259791Binding to human 5HT2B receptor expressed in CHO cells relative to 5HT2006Bioorganic & medicinal chemistry letters, Feb, Volume: 16, Issue:3
Pyrrolo(iso)quinoline derivatives as 5-HT(2C) receptor agonists.
AID5402Relative efficacy against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate reader relative to 10 uM 5-HT2004Bioorganic & medicinal chemistry letters, May-03, Volume: 14, Issue:9
Indoline derivatives as 5-HT(2C) receptor agonists.
AID259797Displacement of [3H]5-HT from human 5HT2B2006Bioorganic & medicinal chemistry letters, Feb, Volume: 16, Issue:3
Pyrrolo(iso)quinoline derivatives as 5-HT(2C) receptor agonists.
AID259794Binding to human 5HT2B receptor expressed in CHO cells2006Bioorganic & medicinal chemistry letters, Feb, Volume: 16, Issue:3
Pyrrolo(iso)quinoline derivatives as 5-HT(2C) receptor agonists.
AID324626Intrinsic activity at human cloned 5HT2C receptor expressed in CHO cells assessed as maximal stimulation of 10 uM 5HT-induced myo-[3H]inositol hydrolysis2008Bioorganic & medicinal chemistry, Feb-15, Volume: 16, Issue:4
Synthesis and structure-activity relationships of a series of substituted 2-(1H-furo[2,3-g]indazol-1-yl)ethylamine derivatives as 5-HT2C receptor agonists.
AID324620Displacement of [3H]5-HT from human 5HT2C receptor expressed in CHO cells2008Bioorganic & medicinal chemistry, Feb-15, Volume: 16, Issue:4
Synthesis and structure-activity relationships of a series of substituted 2-(1H-furo[2,3-g]indazol-1-yl)ethylamine derivatives as 5-HT2C receptor agonists.
AID180519Induction of penile erection in rats after subcutaneous administration, indicative of 5-HT 2c receptor activation1997Journal of medicinal chemistry, Aug-15, Volume: 40, Issue:17
Novel agonists of 5HT2C receptors. Synthesis and biological evaluation of substituted 2-(indol-1-yl)-1-methylethylamines and 2-(indeno[1,2-b]pyrrol-1-yl)-1-methylethylamines. Improved therapeutics for obsessive compulsive disorder.
AID5764Affinity for human 5-hydroxytryptamine 2B receptor expressed in mammalian cell line2004Bioorganic & medicinal chemistry letters, May-03, Volume: 14, Issue:9
Indoline derivatives as 5-HT(2C) receptor agonists.
AID5842Functional activity against human 5-hydroxytryptamine 2C receptor expressed in CHO cells using fluorometric imaging plate reader2004Bioorganic & medicinal chemistry letters, May-03, Volume: 14, Issue:9
Indoline derivatives as 5-HT(2C) receptor agonists.
AID324622Selectivity for human 5HT2A to human 5HT2C2008Bioorganic & medicinal chemistry, Feb-15, Volume: 16, Issue:4
Synthesis and structure-activity relationships of a series of substituted 2-(1H-furo[2,3-g]indazol-1-yl)ethylamine derivatives as 5-HT2C receptor agonists.
AID259793Binding to human 5HT2A receptor expressed in CHO cells2006Bioorganic & medicinal chemistry letters, Feb, Volume: 16, Issue:3
Pyrrolo(iso)quinoline derivatives as 5-HT(2C) receptor agonists.
AID179681Intrinsic 5-HT 2c receptor activity as induced IP3 turnover in vitro in rat choroid plexus1997Journal of medicinal chemistry, Aug-15, Volume: 40, Issue:17
Novel agonists of 5HT2C receptors. Synthesis and biological evaluation of substituted 2-(indol-1-yl)-1-methylethylamines and 2-(indeno[1,2-b]pyrrol-1-yl)-1-methylethylamines. Improved therapeutics for obsessive compulsive disorder.
AID5191Affinity for human 5-hydroxytryptamine 2A receptor expressed in mammalian cell line2004Bioorganic & medicinal chemistry letters, May-03, Volume: 14, Issue:9
Indoline derivatives as 5-HT(2C) receptor agonists.
AID324632Induction of penile erection in po dosed rat2008Bioorganic & medicinal chemistry, Feb-15, Volume: 16, Issue:4
Synthesis and structure-activity relationships of a series of substituted 2-(1H-furo[2,3-g]indazol-1-yl)ethylamine derivatives as 5-HT2C receptor agonists.
AID5634Relative efficacy against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader relative to 10 uM 5-HT2004Bioorganic & medicinal chemistry letters, May-03, Volume: 14, Issue:9
Indoline derivatives as 5-HT(2C) receptor agonists.
AID5869Affinity for human 5-hydroxytryptamine 2C receptor expressed in mammalian cell line2004Bioorganic & medicinal chemistry letters, May-03, Volume: 14, Issue:9
Indoline derivatives as 5-HT(2C) receptor agonists.
AID259792Binding to human 5HT2C receptor expressed in CHO cells relative to 5HT2006Bioorganic & medicinal chemistry letters, Feb, Volume: 16, Issue:3
Pyrrolo(iso)quinoline derivatives as 5-HT(2C) receptor agonists.
AID259798Displacement of [3H]5-HT from human 5HT2C2006Bioorganic & medicinal chemistry letters, Feb, Volume: 16, Issue:3
Pyrrolo(iso)quinoline derivatives as 5-HT(2C) receptor agonists.
AID233882Selectivity ratio was measured as pKi ratio of 5-HT2C to that of 5-HT2A receptor1997Journal of medicinal chemistry, Aug-15, Volume: 40, Issue:17
Novel agonists of 5HT2C receptors. Synthesis and biological evaluation of substituted 2-(indol-1-yl)-1-methylethylamines and 2-(indeno[1,2-b]pyrrol-1-yl)-1-methylethylamines. Improved therapeutics for obsessive compulsive disorder.
AID324623Agonist activity at human cloned 5HT2C receptor expressed in CHO cells assessed as myo-[3H]inositol hydrolysis2008Bioorganic & medicinal chemistry, Feb-15, Volume: 16, Issue:4
Synthesis and structure-activity relationships of a series of substituted 2-(1H-furo[2,3-g]indazol-1-yl)ethylamine derivatives as 5-HT2C receptor agonists.
AID5645Binding affinity against human 5-hydroxytryptamine 2C receptor using displacement of [3H]DOB1997Journal of medicinal chemistry, Aug-15, Volume: 40, Issue:17
Novel agonists of 5HT2C receptors. Synthesis and biological evaluation of substituted 2-(indol-1-yl)-1-methylethylamines and 2-(indeno[1,2-b]pyrrol-1-yl)-1-methylethylamines. Improved therapeutics for obsessive compulsive disorder.
AID324628Intrinsic activity at human cloned 5HT2B receptor expressed in HEK293-EBNA cells assessed as maximal stimulation of 10 uM 5HT-induced myo-[3H]inositol hydrolysis2008Bioorganic & medicinal chemistry, Feb-15, Volume: 16, Issue:4
Synthesis and structure-activity relationships of a series of substituted 2-(1H-furo[2,3-g]indazol-1-yl)ethylamine derivatives as 5-HT2C receptor agonists.
AID324621Displacement of [3H]5-HT from human 5HT2A receptor expressed in CHO cells2008Bioorganic & medicinal chemistry, Feb-15, Volume: 16, Issue:4
Synthesis and structure-activity relationships of a series of substituted 2-(1H-furo[2,3-g]indazol-1-yl)ethylamine derivatives as 5-HT2C receptor agonists.
AID312493Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation2008Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
Discovery and structure-activity relationship of (1R)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-benzazepine (Lorcaserin), a selective serotonin 5-HT2C receptor agonist for the treatment of obesity.
AID5162Functional activity against human 5-hydroxytryptamine 2A receptor expressed in CHO cells using fluorometric imaging plate reader2004Bioorganic & medicinal chemistry letters, May-03, Volume: 14, Issue:9
Indoline derivatives as 5-HT(2C) receptor agonists.
AID324630Selectivity ratio of EC50 for human cloned 5HT2B receptor over EC50 for human cloned 5HT2C receptor2008Bioorganic & medicinal chemistry, Feb-15, Volume: 16, Issue:4
Synthesis and structure-activity relationships of a series of substituted 2-(1H-furo[2,3-g]indazol-1-yl)ethylamine derivatives as 5-HT2C receptor agonists.
AID312492Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation2008Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
Discovery and structure-activity relationship of (1R)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-benzazepine (Lorcaserin), a selective serotonin 5-HT2C receptor agonist for the treatment of obesity.
AID312494Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation2008Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
Discovery and structure-activity relationship of (1R)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-benzazepine (Lorcaserin), a selective serotonin 5-HT2C receptor agonist for the treatment of obesity.
AID5383Functional activity against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader2004Bioorganic & medicinal chemistry letters, May-03, Volume: 14, Issue:9
Indoline derivatives as 5-HT(2C) receptor agonists.
AID259795Binding to human 5HT2C receptor expressed in CHO cells2006Bioorganic & medicinal chemistry letters, Feb, Volume: 16, Issue:3
Pyrrolo(iso)quinoline derivatives as 5-HT(2C) receptor agonists.
AID324624Agonist activity at human cloned 5HT2A receptor expressed in CHO cells assessed as myo-[3H]inositol hydrolysis2008Bioorganic & medicinal chemistry, Feb-15, Volume: 16, Issue:4
Synthesis and structure-activity relationships of a series of substituted 2-(1H-furo[2,3-g]indazol-1-yl)ethylamine derivatives as 5-HT2C receptor agonists.
AID324631Induction of penile erection in sc dosed rat2008Bioorganic & medicinal chemistry, Feb-15, Volume: 16, Issue:4
Synthesis and structure-activity relationships of a series of substituted 2-(1H-furo[2,3-g]indazol-1-yl)ethylamine derivatives as 5-HT2C receptor agonists.
AID180517Induction of penile erection in rats following p.o. administration, indicative of 5-HT 2c receptor activation1997Journal of medicinal chemistry, Aug-15, Volume: 40, Issue:17
Novel agonists of 5HT2C receptors. Synthesis and biological evaluation of substituted 2-(indol-1-yl)-1-methylethylamines and 2-(indeno[1,2-b]pyrrol-1-yl)-1-methylethylamines. Improved therapeutics for obsessive compulsive disorder.
AID324625Agonist activity at human cloned 5HT2B receptor expressed in HEK293-EBNA cells assessed as myo-[3H]inositol hydrolysis2008Bioorganic & medicinal chemistry, Feb-15, Volume: 16, Issue:4
Synthesis and structure-activity relationships of a series of substituted 2-(1H-furo[2,3-g]indazol-1-yl)ethylamine derivatives as 5-HT2C receptor agonists.
AID312511Selectivity ratio of pEC50 for human 5HT2B to pEC50 for human 5HT2C2008Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
Discovery and structure-activity relationship of (1R)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-benzazepine (Lorcaserin), a selective serotonin 5-HT2C receptor agonist for the treatment of obesity.
AID5773Relative efficacy against human 5-hydroxytryptamine 2B receptor expressed in CHO cells using fluorometric imaging plate reader relative to 10 uM 5-HT2004Bioorganic & medicinal chemistry letters, May-03, Volume: 14, Issue:9
Indoline derivatives as 5-HT(2C) receptor agonists.
AID259796Displacement of [125I]DOI from human 5HT2A2006Bioorganic & medicinal chemistry letters, Feb, Volume: 16, Issue:3
Pyrrolo(iso)quinoline derivatives as 5-HT(2C) receptor agonists.
AID197353Efficacy (pEC50) was evaluated for 5-HT2C receptor-mediated stimulation of IP3 formation in vitro in choroid plexus of the rat1997Journal of medicinal chemistry, Aug-15, Volume: 40, Issue:17
Novel agonists of 5HT2C receptors. Synthesis and biological evaluation of substituted 2-(indol-1-yl)-1-methylethylamines and 2-(indeno[1,2-b]pyrrol-1-yl)-1-methylethylamines. Improved therapeutics for obsessive compulsive disorder.
AID324629Selectivity ratio of EC50 for human cloned 5HT2C receptor over EC50 for human cloned 5HT2A receptor2008Bioorganic & medicinal chemistry, Feb-15, Volume: 16, Issue:4
Synthesis and structure-activity relationships of a series of substituted 2-(1H-furo[2,3-g]indazol-1-yl)ethylamine derivatives as 5-HT2C receptor agonists.
AID259790Binding to human 5HT2A receptor expressed in CHO cells relative to 5HT2006Bioorganic & medicinal chemistry letters, Feb, Volume: 16, Issue:3
Pyrrolo(iso)quinoline derivatives as 5-HT(2C) receptor agonists.
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.
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.
AID1346893Human 5-HT2C receptor (5-Hydroxytryptamine receptors)2004European journal of pharmacology, Jan-01, Volume: 483, Issue:1
Pharmacological profile of YM348, a novel, potent and orally active 5-HT2C receptor agonist.
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.
AID624216Agonists at Human 5-Hydroxytryptamine receptor 5-HT2C2004European journal of pharmacology, Jan-01, Volume: 483, Issue:1
Pharmacological profile of YM348, a novel, potent and orally active 5-HT2C receptor agonist.
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.
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.
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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (90)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's7 (7.78)18.2507
2000's50 (55.56)29.6817
2010's32 (35.56)24.3611
2020's1 (1.11)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 18.15

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 Index18.15 (24.57)
Research Supply Index2.08 (2.92)
Research Growth Index5.04 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (18.15)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Observational0 (0.00%)0.25%
Other84 (100.00%)84.16%
Other7 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]