N-[4-Methoxy-3-(4-methylpiperazin-1-yl)-phenyl]-4-[2-methyl-4-(5-methyl-1,2,4-oxadiazol-3-yl)phenyl]benzamide

Uses

GR 127935 Hydrochloride Hydrate is a 5-HT1B/1D antagonist used in the treatment of depression and anxiety affecting serotonin levels.

Definition

ChEBI: GR 127935 is 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. It is a N-alkylpiperazine, a N-arylpiperazine, a 1,2,4-oxadiazole and a member of benzamides. It is a conjugate base of a GR 127935(1+).

Biological Activity

Potent and selective 5-HT 1B/1D receptor antagonist (pK i values are 8.5 for both guinea pig 5-HT 1D and rat 5-HT 1B receptors). Displays > 100-fold selectivity over 5HT 1A , 5-HT 2A , 5-HT 2C receptors and other receptor types. Centrally active following oral administration.

IC 50

5-HT_1D Receptor