Biochemical and behavioral studies of the 5‐HT_1B receptor agonist, CP‐94,253

Abstract

Abstract CP‐94,253, 3‐(1,2,5,6‐tetrahydro‐4‐pyridyl)‐5‐propoxypyrrolo[3,2‐ b ]pyridine, a new serotonergic ligand, was found to exhibit significantly greater binding affinity at 5‐HT 1B receptors than at 5‐HT 1A or 5‐HT 1C receptors. Saturation studies showed CP‐94,253 to be a competitive inhibitor of [ 125 l]iodocyanopindolol binding to 5‐HT 1B sites. Its competition curve with this radioligand was shifted to the right (decreased affinity) in the presence of Gpp(NH)p, indicating an agonist function for CP‐94,253. Oral administration of CP‐94,253 to rats caused inhibition of food intake, decrease in body weight gain, and hyperlocomotion, effects apparently elicited via activation of 5‐HT 1B receptors. © 1992 Wiley‐Liss, Inc.