Biochemical and behavioral studies of the 5-HT1B receptor agonist,CP-94,253

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 [¹²⁵l]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.