GR 127935

Term ID

CHEBI:64114

Synonyms

• 2'-Methyl-4'-(5-methyl-(1,2,4)-oxadiazol-3-yl)biphenyl-4-carboxylic acid (4-methoxy-3-(4-methylpiperazin-1-yl)phenyl)amide
• GR-127935
• GR127935
• N-[4-methoxy-3-(4-methylpiperazin-1-yl)phenyl]-2'-methyl-4'-(5-methyl-1,2,4-oxadiazol-3-yl)biphenyl-4-carboxamide

Definition

A member of the class of benzamides obtained by formal condensation of the carboxy group of 2'-methyl-4'-(5-methyl-1,2,4-oxadiazol-3-yl)biphenyl-4-carboxylic acid and the anilino group of 4-methoxy-3-(4-methylpiperazin-1-yl)aniline. Potent and selective 5-HT1B/1D receptor antagonist (pKi values are 8.5 for both guinea pig 5-HT1D and rat 5-HT1B receptors). Displays > 100-fold selectivity over 5HT1A, 5-HT2A, 5-HT2C receptors and other receptor types. Centrally active following oral administration.

References

• CAS:148672-13-3
• LINCS:LSM-2243
• PMID:18952090
• PMID:19135047
• PMID:19356724
• PMID:19945477
• PMID:20152720
• PMID:20171242
• PMID:20385119
• PMID:20422941
• PMID:21262272
• PMID:21473863
• PMID:21653728
• PMID:21868165
• Patent:EP760665
• Patent:US5340810
• Reaxys:7061533

Ontology

ChEBI  ( EBI )