Page last updated: 2024-12-07

cp 93129

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

Description

3-(1,2,5,6-tetrahydropyrid-4-yl)pyrrolo(3,2-b)pyrid-5-one: serotonin agonist; structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID124007
CHEMBL ID304008
CHEBI ID93436
SCHEMBL ID9696192
SCHEMBL ID781544
MeSH IDM0179017

Synonyms (34)

Synonym
BRD-K81876028-300-01-2
3-(1,2,3,6-tetrahydropyridin-4-yl)-1,4-dihydropyrrolo[2,3-e]pyridin-5-one
cp93129
gtpl11
tocris-1032
NCGC00024952-01
127792-75-0
PDSP2_000784
PDSP1_000796
cp 93129
5h-pyrrolo(3,2-b)pyridin-5-one, 1,4-dihydro-3-(1,2,3,6-tetrahydro-4-pyridinyl)-
3-(1,2,5,6-tetrahydropyrid-4-yl)pyrrolo(3,2-b)pyrid-5-one
cp-93,129
CHEMBL304008 ,
L000200
3-(1,2,3,6-tetrahydropyridin-4-yl)-1,4-dihydropyrrolo[3,2-b]pyridin-5-one
unii-y4bw369lgs
y4bw369lgs ,
cas_127792-75-0
bdbm84737
3-(1,2,3,6-tetrahydro-pyridin-4-yl)-1,4-dihydro-pyrrolo[3,2-b]pyridin-5-one
cp-93129
879089-64-2
3-(1,2,3,6-tetrahydropyridin-4-yl)-1,4-dihydro-5h-pyrrolo[3,2-b]pyridin-5-one
AB07658
SCHEMBL9696192
SCHEMBL781544
DTXSID50155670
CHEBI:93436
5-hydroxy-3(4-1,2,5,6-tetrahydropyridyl)-4-azaindole
Q5013583
5h-pyrrolo[3,2-b]pyridin-5-one, 1,4-dihydro-3-(1,2,3,6-tetrahydro-4-pyridinyl)-
3-(1,2,5,6-tetrahydropyridin-4-yl)-1,4-dihydropyrrolo[3,2-b]pyridin-5-one
1,4-dihydro-3-(1,2,3,6-tetrahydro-4-pyridinyl)-5h-pyrrolo[3,2-b]pyridin-5-one

Research Excerpts

Dosage Studied

ExcerptRelevanceReference
" This effect was intensity-dependent (the sigmoidal dose-response curve was characterized by an EI(50) of 662+/-69 microT and a maximal increase of 321+/-13% of the control K(d)), reversible, temperature-dependent and specific to the 5-HT(1B) receptors."( Magnetic field desensitizes 5-HT(1B) receptor in brain: pharmacological and functional studies.
Bailly, JM; Deschamps, F; Fillion, G; Grimaldi, B; Kochanek, M; Lambrozo, J; Massot, O, 2000
)
0.31
" In addition, the different dose-response to fluvoxamine suggests that 5-HT(1B) knockout mice have possible adaptations of 5-HT transporters in order to compensate for the loss of the terminal 5-HT(1B) autoreceptor."( The effects of selective serotonin reuptake inhibitors on extracellular 5-HT levels in the hippocampus of 5-HT(1B) receptor knockout mice.
De Groote, L; Olivier, B; Westenberg, HG, 2002
)
0.31
"5 mg/kg) did not modify dose-response curves of the psychostimulant, nor did it affect its ED50 value."( Serotonin1B receptor ligands in the nucleus accumbens shell do not affect the discriminative stimulus effects of amphetamine in rats.
Baran, L; Filip, M; Nowak, E; PrzegaliƄski, E,
)
0.13
"5 mg/kg) produced a leftward shift in the cocaine dose-response curve and a decrease in its ED(50) value."( Effects of serotonin (5-HT)(1B) receptor ligands, microinjected into accumbens subregions, on cocaine discrimination in rats.
Filip, M; Jungersmith, K; Nowak, E; Papla, I; PrzegaliƄski, E, 2002
)
0.31
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
pyrrolopyridine
[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 (19)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Putative fructose-1,6-bisphosphate aldolaseGiardia intestinalisPotency25.05940.140911.194039.8107AID2451
Chain A, HADH2 proteinHomo sapiens (human)Potency31.62280.025120.237639.8107AID886; AID893
Chain B, HADH2 proteinHomo sapiens (human)Potency31.62280.025120.237639.8107AID886; AID893
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency31.62280.177814.390939.8107AID2147
USP1 protein, partialHomo sapiens (human)Potency56.23410.031637.5844354.8130AID504865
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency28.18380.011212.4002100.0000AID1030
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency2.51190.00207.533739.8107AID891
cytochrome P450 2C19 precursorHomo sapiens (human)Potency0.12590.00255.840031.6228AID899
cytochrome P450 2C9 precursorHomo sapiens (human)Potency7.94330.00636.904339.8107AID883
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency35.48130.001815.663839.8107AID894
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency7.94330.00638.235039.8107AID883
[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 2CRattus norvegicus (Norway rat)IC50 (µMol)10.00000.00040.629810.0000AID4802
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)IC50 (µMol)10.00000.00040.908610.0000AID4802
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)IC50 (µMol)3.00000.00031.38338.4000AID3771
5-hydroxytryptamine receptor 1DHomo sapiens (human)IC50 (µMol)2.20000.00050.28702.4000AID4532
5-hydroxytryptamine receptor 2CHomo sapiens (human)IC50 (µMol)6.40000.00011.03029.0000AID4743
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)IC50 (µMol)0.01500.00051.48357.8000AID4674
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)IC50 (µMol)10.00000.00040.615610.0000AID4802
[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 1BRattus norvegicus (Norway rat)EC50 (µMol)0.05600.01260.03790.0631AID4667
5-hydroxytryptamine receptor 1DRattus norvegicus (Norway rat)EC50 (µMol)10.00000.00130.03880.0970AID4871
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (25)

Processvia Protein(s)Taxonomy
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 1DHomo sapiens (human)
intestine smooth muscle contraction5-hydroxytryptamine receptor 1DHomo sapiens (human)
regulation of locomotion5-hydroxytryptamine receptor 1DHomo sapiens (human)
vasoconstriction5-hydroxytryptamine receptor 1DHomo sapiens (human)
regulation of behavior5-hydroxytryptamine receptor 1DHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 1DHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 1DHomo sapiens (human)
adenylate cyclase-inhibiting serotonin receptor signaling pathway5-hydroxytryptamine receptor 1DHomo 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)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (7)

Processvia Protein(s)Taxonomy
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 1DHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 1DHomo 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)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (4)

Processvia Protein(s)Taxonomy
plasma membrane5-hydroxytryptamine receptor 1DHomo sapiens (human)
synapse5-hydroxytryptamine receptor 1DHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 1DHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 1DHomo 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)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (20)

Assay IDTitleYearJournalArticle
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.
AID1347161Confirmatory screen NINDS Rhodamine 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.
AID1347168HepG2 cells viability 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.
AID1347153Confirmatory 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.
AID1347149Furin counterscreen 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.
AID1347169Tertiary RLuc qRT-PCR qHTS assay 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.
AID1347152Confirmatory screen NINDS 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.
AID1347167Vero cells viability 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.
AID4743Compound was evaluated for its inhibitory activity against 5-hydroxytryptamine 1C receptor of pig choroid plexus using [3H]mesulergine as the radioligand1990Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
3-(1,2,5,6-Tetrahydropyrid-4-yl)pyrrolo[3,2-b]pyrid-5-one: a potent and selective serotonin (5-HT1B) agonist and rotationally restricted phenolic analogue of 5-methoxy-3-(1,2,5,6-tetrahydropyrid-4-yl)indole.
AID3771Displacement of [3H]8-OH-DPAT from rat cortex 5-hydroxytryptamine 1A receptor1990Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
3-(1,2,5,6-Tetrahydropyrid-4-yl)pyrrolo[3,2-b]pyrid-5-one: a potent and selective serotonin (5-HT1B) agonist and rotationally restricted phenolic analogue of 5-methoxy-3-(1,2,5,6-tetrahydropyrid-4-yl)indole.
AID4532Compound was evaluated for its inhibitory activity against 5-hydroxytryptamine 1D receptor of bovine caudate using [3H]5-HT as the radioligand1990Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
3-(1,2,5,6-Tetrahydropyrid-4-yl)pyrrolo[3,2-b]pyrid-5-one: a potent and selective serotonin (5-HT1B) agonist and rotationally restricted phenolic analogue of 5-methoxy-3-(1,2,5,6-tetrahydropyrid-4-yl)indole.
AID3503Inhibition of Forskolin-stimulated adenylate cyclase activity against 5-hydroxytryptamine 1A receptor of guinea pig hippocampus1990Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
3-(1,2,5,6-Tetrahydropyrid-4-yl)pyrrolo[3,2-b]pyrid-5-one: a potent and selective serotonin (5-HT1B) agonist and rotationally restricted phenolic analogue of 5-methoxy-3-(1,2,5,6-tetrahydropyrid-4-yl)indole.
AID193608Effect of direct injection into the PVN (paraventricular medial hypothalamus) of rats on feeding behavior and the inhibition of food intake1990Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
3-(1,2,5,6-Tetrahydropyrid-4-yl)pyrrolo[3,2-b]pyrid-5-one: a potent and selective serotonin (5-HT1B) agonist and rotationally restricted phenolic analogue of 5-methoxy-3-(1,2,5,6-tetrahydropyrid-4-yl)indole.
AID4674Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT1990Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
3-(1,2,5,6-Tetrahydropyrid-4-yl)pyrrolo[3,2-b]pyrid-5-one: a potent and selective serotonin (5-HT1B) agonist and rotationally restricted phenolic analogue of 5-methoxy-3-(1,2,5,6-tetrahydropyrid-4-yl)indole.
AID4802Compound was evaluated for its inhibitory activity against 5-hydroxytryptamine 2 receptor of rat anterior cortex using [3H]ketanserin as the radioligand1990Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
3-(1,2,5,6-Tetrahydropyrid-4-yl)pyrrolo[3,2-b]pyrid-5-one: a potent and selective serotonin (5-HT1B) agonist and rotationally restricted phenolic analogue of 5-methoxy-3-(1,2,5,6-tetrahydropyrid-4-yl)indole.
AID4667Inhibition of Forskolin-stimulated adenylate cyclase activity against 5-hydroxytryptamine 1B receptor of rat substantia nigra1990Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
3-(1,2,5,6-Tetrahydropyrid-4-yl)pyrrolo[3,2-b]pyrid-5-one: a potent and selective serotonin (5-HT1B) agonist and rotationally restricted phenolic analogue of 5-methoxy-3-(1,2,5,6-tetrahydropyrid-4-yl)indole.
AID4871Inhibition of Forskolin-stimulated adenylate cyclase activity against 5-hydroxytryptamine 1D receptor of rat substantia nigra1990Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
3-(1,2,5,6-Tetrahydropyrid-4-yl)pyrrolo[3,2-b]pyrid-5-one: a potent and selective serotonin (5-HT1B) agonist and rotationally restricted phenolic analogue of 5-methoxy-3-(1,2,5,6-tetrahydropyrid-4-yl)indole.
AID1345615Human 5-HT1A receptor (5-Hydroxytryptamine receptors)1997Naunyn-Schmiedeberg's archives of pharmacology, Jun, Volume: 355, Issue:6
Agonist activity of antimigraine drugs at recombinant human 5-HT1A receptors: potential implications for prophylactic and acute therapy.
AID624210Agonists at Human 5-Hydroxytryptamine receptor 5-HT1A1997Naunyn-Schmiedeberg's archives of pharmacology, Jun, Volume: 355, Issue:6
Agonist activity of antimigraine drugs at recombinant human 5-HT1A receptors: potential implications for prophylactic and acute therapy.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (105)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's37 (35.24)18.2507
2000's55 (52.38)29.6817
2010's11 (10.48)24.3611
2020's2 (1.90)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other109 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]