CP-94253 is a drug which acts as a potent and selectiveserotonin5-HT1Breceptoragonist, with approximately 25× and 40× selectivity over the closely related 5-HT1D and 5-HT1A receptors.[1] It has a range of behavioral effects, based on animal testing. The effects include the following: promoting wakefulness by increasing dopamine release in the brain;[2][3] reducing food intake and promoting satiety;[4][5][6] enhancing the reinforcing effects of cocaine;[7][8][9][10] and possible antidepressant effects.[11] A recent study[12] found that "Regardless of sex, CP94253 decreased cocaine intake after abstinence and during resumption of SA [self-administration] and decreased cue reactivity" suggesting that agonism of the inhibitory 5-HT2B receptors may diminish the cognitive reward of cocaine usage and increased use of the drug without a period of abstinence may be a product of test subjects trying to achieve a previously rewarding experience through larger dosages of cocaine.
^Koe KB, Nielsen JA, Macor JE, Heym J (1992). "Biochemical and behavioral studies of the 5-HT1B receptor agonist, CP-94,253".Drug Development Research.26 (3):241–250.doi:10.1002/ddr.430260305.S2CID85358992.
^Monti JM, Monti D, Jantos H, Ponzoni A (December 1995). "Effects of selective activation of the 5-HT1B receptor with CP-94,253 on sleep and wakefulness in the rat".Neuropharmacology.34 (12):1647–1651.doi:10.1016/0028-3908(95)00112-3.PMID8788962.S2CID11872727.
^Iyer RN, Bradberry CW (April 1996). "Serotonin-mediated increase in prefrontal cortex dopamine release: pharmacological characterization".The Journal of Pharmacology and Experimental Therapeutics.277 (1):40–47.PMID8613947.
^Halford JC, Blundell JE (September 1996). "The 5-HT1B receptor agonist CP-94,253 reduces food intake and preserves the behavioural satiety sequence".Physiology & Behavior.60 (3):933–939.doi:10.1016/0031-9384(96)00073-x.PMID8873272.S2CID24349948.
^Lee MD, Simansky KJ (June 1997). "CP-94, 253: a selective serotonin1B (5-HT1B) agonist that promotes satiety".Psychopharmacology.131 (3):264–270.doi:10.1007/s002130050292.PMID9203237.S2CID33969765.
^Lee MD, Kennett GA, Dourish CT, Clifton PG (October 2002). "5-HT1B receptors modulate components of satiety in the rat: behavioural and pharmacological analyses of the selective serotonin1B agonist CP-94,253".Psychopharmacology.164 (1):49–60.doi:10.1007/s00213-002-1162-7.PMID12373419.S2CID2926575.
^Przegalinski E, Filip M, Papla I, Siwanowicz J (April 2001). "Effect of serotonin (5-HT)1B receptor ligands on cocaine sensitization in rats".Behavioural Pharmacology.12 (2):109–116.doi:10.1097/00008877-200104000-00004.PMID11396515.
^Przegaliński E, Gołda A, Frankowska M, Zaniewska M, Filip M (March 2007). "Effects of serotonin 5-HT1B receptor ligands on the cocaine- and food-maintained self-administration in rats".European Journal of Pharmacology.559 (2–3):165–172.doi:10.1016/j.ejphar.2006.12.012.PMID17291490.
^Przegaliński E, Gołda A, Filip M (2008). "Effects of serotonin (5-HT)(1B) receptor ligands on cocaine-seeking behavior in rats".Pharmacological Reports.60 (6):798–810.PMID19211971.
^Tatarczyńska E, Antkiewicz-Michaluk L, Kłodzińska A, Stachowicz K, Chojnacka-Wójcik E (May 2005). "Antidepressant-like effect of the selective 5-HT1B receptor agonist CP 94253: a possible mechanism of action".European Journal of Pharmacology.516 (1):46–50.doi:10.1016/j.ejphar.2005.04.025.PMID15913599.
^Scott SN, Garcia R, Powell GL, Doyle SM, Ruscitti B, Le T, et al. (October 2021). "5-HT1B receptor agonist attenuates cocaine self-administration after protracted abstinence and relapse in rats".Journal of Psychopharmacology.35 (10):1216–1225.doi:10.1177/02698811211019279.PMID34049460.S2CID235243643.