Page last updated: 2024-11-07

cp 122288

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

Description

CP 122288: activates the trigeminovascular receptor blocking neurogenic inflammation within dura mater; a 5-HT1 receptor agonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID132552
CHEMBL ID159332
SCHEMBL ID7103413
MeSH IDM0226348

Synonyms (26)

Synonym
cp122288
gtpl110
cp-122288
PDSP2_000545
PDSP1_000547
cp 122288
n-methyl-3-((1-methylpyrrolidin-2-yl)methyl)-1h-indole-5-methanesulfonamide
1h-indole-5-methanesulfonamide, n-methyl-3-((1-methyl-2-pyrrolidinyl)methyl)-, (r)-
cp-122,288
1h-indole-5-methanesulfonamide, n-methyl-3-[[(2r)-1-methyl-2-pyrrolidinyl]methyl]-
CHEMBL159332 ,
n-methyl-1-[3-[[(2r)-1-methylpyrrolidin-2-yl]methyl]-1h-indol-5-yl]methanesulfonamide
59e9wct6em ,
143321-74-8
unii-59e9wct6em
BWQZTHPHLITOOZ-CQSZACIVSA-N ,
(r)-5-(methylaminosulfonylmethyl)-3-(n-methylpyrrolidin-2-ylmethyl)-1h-indole
(r)-n-methyl-[3-(1-methyl-2-pyrrolidinylmethyl)-1h-indol-5-yl]methanesulfonamide
SCHEMBL7103413
bdbm50473521
DTXSID00931820
n-methyl-1-{3-[(1-methylpyrrolidin-2-yl)methyl]-1h-indol-5-yl}methanesulfonamide
Q20707282
1h-indole-5-methanesulfonamide, n-methyl-3-[(1-methyl-2-pyrrolidinyl)methyl]-, (r)-
n-methyl-1-(3-(((2r)-1-methylpyrrolidin-2-yl)methyl)-1h-indol-5-yl)methanesulfonamide
AKOS040748165

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
" A qualitative model for pharmacokinetic properties was then used to guide the synthesis toward molecules likely to have oral bioavailability in humans."( Discovery of 4-[3-(trans-3-dimethylaminocyclobutyl)-1H-indol-5-ylmethyl]-(4S)-oxazolidin-2-one (4991W93), a 5HT(1B/1D) receptor partial agonist and a potent inhibitor of electrically induced plasma extravasation.
Barrett, V; Brockwell, M; Cambridge, D; Farrant, DR; Foster, C; Giles, H; Glen, RC; Hill, AP; Hobbs, H; Honey, A; Jandu, KS; Martin, GR; Salmon, J; Selwood, DL; Smith, D; Woollard, P, 2001
)
0.31

Dosage Studied

ExcerptRelevanceReference
"2 mumol/kg), GR-127,935 right-shifted the dose-response curve of sumatriptan."( The 5-HT1D receptor antagonist GR-127,935 prevents inhibitory effects of sumatriptan but not CP-122,288 and 5-CT on neurogenic plasma extravasation within guinea pig dura mater.
Cutrer, FM; Moskowitz, MA; Waeber, C; Yu, XJ, 1997
)
0.3
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (2)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
5-hydroxytryptamine receptor 1DHomo sapiens (human)IC50 (µMol)0.00720.00050.28702.4000AID4642
5-hydroxytryptamine receptor 1BHomo sapiens (human)IC50 (µMol)0.01440.00050.39756.5000AID4270
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (27)

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)
G protein-coupled receptor internalization5-hydroxytryptamine receptor 1BHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 1BHomo sapiens (human)
adenylate cyclase-inhibiting serotonin receptor signaling pathway5-hydroxytryptamine receptor 1BHomo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 1BHomo sapiens (human)
negative regulation of gamma-aminobutyric acid secretion5-hydroxytryptamine receptor 1BHomo sapiens (human)
regulation of dopamine secretion5-hydroxytryptamine receptor 1BHomo sapiens (human)
negative regulation of serotonin secretion5-hydroxytryptamine receptor 1BHomo sapiens (human)
negative regulation of synaptic transmission, GABAergic5-hydroxytryptamine receptor 1BHomo sapiens (human)
response to cocaine5-hydroxytryptamine receptor 1BHomo sapiens (human)
vasoconstriction5-hydroxytryptamine receptor 1BHomo sapiens (human)
drinking behavior5-hydroxytryptamine receptor 1BHomo sapiens (human)
response to ethanol5-hydroxytryptamine receptor 1BHomo sapiens (human)
bone remodeling5-hydroxytryptamine receptor 1BHomo sapiens (human)
regulation of behavior5-hydroxytryptamine receptor 1BHomo sapiens (human)
response to mineralocorticoid5-hydroxytryptamine receptor 1BHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergic5-hydroxytryptamine receptor 1BHomo sapiens (human)
cellular response to alkaloid5-hydroxytryptamine receptor 1BHomo sapiens (human)
cellular response to xenobiotic stimulus5-hydroxytryptamine receptor 1BHomo sapiens (human)
cellular response to temperature stimulus5-hydroxytryptamine receptor 1BHomo sapiens (human)
presynaptic modulation of chemical synaptic transmission5-hydroxytryptamine receptor 1BHomo sapiens (human)
regulation of presynaptic cytosolic calcium ion concentration5-hydroxytryptamine receptor 1BHomo sapiens (human)
positive regulation of vascular associated smooth muscle cell proliferation5-hydroxytryptamine receptor 1BHomo sapiens (human)
regulation of synaptic vesicle exocytosis5-hydroxytryptamine receptor 1BHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 1BHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 1BHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (5)

Processvia Protein(s)Taxonomy
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 1DHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 1DHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 1BHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 1BHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 1BHomo sapiens (human)
voltage-gated calcium channel activity involved in regulation of presynaptic cytosolic calcium levels5-hydroxytryptamine receptor 1BHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 1BHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (8)

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)
endoplasmic reticulum5-hydroxytryptamine receptor 1BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 1BHomo sapiens (human)
presynaptic membrane5-hydroxytryptamine receptor 1BHomo sapiens (human)
calyx of Held5-hydroxytryptamine receptor 1BHomo sapiens (human)
serotonergic synapse5-hydroxytryptamine receptor 1BHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 1BHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 1BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 1BHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (6)

Assay IDTitleYearJournalArticle
AID4642Binding affinity in CHO-K1 cells transfected with human 5-hydroxytryptamine 1D receptor2001Journal of medicinal chemistry, Mar-01, Volume: 44, Issue:5
Discovery of 4-[3-(trans-3-dimethylaminocyclobutyl)-1H-indol-5-ylmethyl]-(4S)-oxazolidin-2-one (4991W93), a 5HT(1B/1D) receptor partial agonist and a potent inhibitor of electrically induced plasma extravasation.
AID166851Binding affinity towards rabbit saphenous vein value in parenthesis represents intrinsic activity for RbSv;(1 for 5-HT)2001Journal of medicinal chemistry, Mar-01, Volume: 44, Issue:5
Discovery of 4-[3-(trans-3-dimethylaminocyclobutyl)-1H-indol-5-ylmethyl]-(4S)-oxazolidin-2-one (4991W93), a 5HT(1B/1D) receptor partial agonist and a potent inhibitor of electrically induced plasma extravasation.
AID4270Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor2001Journal of medicinal chemistry, Mar-01, Volume: 44, Issue:5
Discovery of 4-[3-(trans-3-dimethylaminocyclobutyl)-1H-indol-5-ylmethyl]-(4S)-oxazolidin-2-one (4991W93), a 5HT(1B/1D) receptor partial agonist and a potent inhibitor of electrically induced plasma extravasation.
AID74182Ability to inhibit [125I]- albumin extravasation into dura following electrical stimulation of trigeminal ganglion of Guinea pig2001Journal of medicinal chemistry, Mar-01, Volume: 44, Issue:5
Discovery of 4-[3-(trans-3-dimethylaminocyclobutyl)-1H-indol-5-ylmethyl]-(4S)-oxazolidin-2-one (4991W93), a 5HT(1B/1D) receptor partial agonist and a potent inhibitor of electrically induced plasma extravasation.
AID1346528Human 5-HT1D receptor (5-Hydroxytryptamine receptors)1997Naunyn-Schmiedeberg's archives of pharmacology, Sep, Volume: 356, Issue:3
Characterization of human serotonin 1D and 1B receptors using [3H]-GR-125743, a novel radiolabelled serotonin 5HT1D/1B receptor antagonist.
AID1346264Human 5-HT1B receptor (5-Hydroxytryptamine receptors)1997Naunyn-Schmiedeberg's archives of pharmacology, Sep, Volume: 356, Issue:3
Characterization of human serotonin 1D and 1B receptors using [3H]-GR-125743, a novel radiolabelled serotonin 5HT1D/1B receptor antagonist.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (16)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's12 (75.00)18.2507
2000's4 (25.00)29.6817
2010's0 (0.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.25

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 weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index11.25 (24.57)
Research Supply Index2.94 (2.92)
Research Growth Index4.19 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.25)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (5.88%)5.53%
Reviews1 (5.88%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other15 (88.24%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]