CP 94,253 (hydrochloride)

CP 94,253 is an agonist of the serotonin (5-HT) receptor subtype 5-HT_1B (K_i = 2 nM in a radioligand binding assay).¹ It is selective for 5-HT_1B over 5-HT_1A, 5-HT_1D, 5-HT_1C, and 5-HT₂ receptors (K_is = 89, 49, 860, and 1,600 nM, respectively). CP 94,253 (10 and 17 mg/kg) reduces aggressive behavior in a resident-intruder test in mice, as well as decreases alcohol-induced aggression in mice with an ED₅₀ value of 3.8 mg/kg.² It decreases the time mice spend immobile in the forced swim test by 43%, indicating antidepressant-like activity, when administered at a dose of 5 mg/kg.³ CP 94,253 (2.5 mg/kg) also increases drinking in the Vogel punished drinking task, indicating anxiolytic-like activity, in rats.⁴

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1. Koe, B.K., Nielsen, J.A., Macor, J.E., et al. Biochemical and behavioral studies of the 5-HT_1B receptor agonist, CP-94,253. Drug Dev. Res. 26(3), 241-250 (1992).

2. Fish, E.W., Faccidomo, S., and Miczek, K.A. Aggression heightened by alcohol or social instigation in mice: Reduction by the 5-HT_1B receptor agonist CP-94,253. Psychopharmacology (Berl.) 146(4), 391-399 (1999).

3. Tatarczyńska, E., Antkiewicz-Michaluk, L., Kłodzińska, A., et al. Antidepressant-like effect of the selective 5-HT_1B receptor agonist CP 94253: A possible mechanism of action. Eur. J. Pharmacol. 516(1), 46-50 (2005).

4. Chojnacka-Wójcik, E., Kłodzińska, A., and Tatarczyńska, E. The anxiolytic-like effect of 5-HT_1B receptor ligands in rats: A possible mechanism of action. J. Pharm. Pharmacol. 57(2), 253-257 (2005).