CP-94253 explained

CP-94253 is a drug which acts as a potent and selective serotonin 5-HT1B receptor agonist, 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.

Notes and References

  1. 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 . 10.1002/ddr.430260305 . 85358992 .
  2. Monti JM, Monti D, Jantos H, Ponzoni A . 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 . December 1995 . 8788962 . 10.1016/0028-3908(95)00112-3 . 11872727 .
  3. Iyer RN, Bradberry CW . Serotonin-mediated increase in prefrontal cortex dopamine release: pharmacological characterization . The Journal of Pharmacology and Experimental Therapeutics . 277 . 1 . 40–47 . April 1996 . 8613947 .
  4. Halford JC, Blundell JE . The 5-HT1B receptor agonist CP-94,253 reduces food intake and preserves the behavioural satiety sequence . Physiology & Behavior . 60 . 3 . 933–939 . September 1996 . 8873272 . 10.1016/0031-9384(96)00073-x . 24349948 .
  5. Lee MD, Simansky KJ . CP-94, 253: a selective serotonin1B (5-HT1B) agonist that promotes satiety . Psychopharmacology . 131 . 3 . 264–270 . June 1997 . 9203237 . 10.1007/s002130050292 . 33969765 .
  6. Lee MD, Kennett GA, Dourish CT, Clifton PG . 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 . October 2002 . 12373419 . 10.1007/s00213-002-1162-7 . 2926575 .
  7. Parsons LH, Weiss F, Koob GF . Serotonin1B receptor stimulation enhances cocaine reinforcement . The Journal of Neuroscience . 18 . 23 . 10078–10089 . December 1998 . 9822762 . 6793270 . 10.1523/JNEUROSCI.18-23-10078.1998 .
  8. Przegalinski E, Filip M, Papla I, Siwanowicz J . Effect of serotonin (5-HT)1B receptor ligands on cocaine sensitization in rats . Behavioural Pharmacology . 12 . 2 . 109–116 . April 2001 . 11396515 . 10.1097/00008877-200104000-00004 .
  9. Przegaliński E, Gołda A, Frankowska M, Zaniewska M, Filip M . 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 . March 2007 . 17291490 . 10.1016/j.ejphar.2006.12.012 .
  10. Przegaliński E, Gołda A, Filip M . Effects of serotonin (5-HT)(1B) receptor ligands on cocaine-seeking behavior in rats . Pharmacological Reports . 60 . 6 . 798–810 . 2008 . 19211971 .
  11. Tatarczyńska E, Antkiewicz-Michaluk L, Kłodzińska A, Stachowicz K, Chojnacka-Wójcik E . 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 . May 2005 . 15913599 . 10.1016/j.ejphar.2005.04.025 .
  12. Scott SN, Garcia R, Powell GL, Doyle SM, Ruscitti B, Le T, Esquer A, Blattner KM, Blass BE, Neisewander JL . 6 . 5-HT1B receptor agonist attenuates cocaine self-administration after protracted abstinence and relapse in rats . Journal of Psychopharmacology . 35 . 10 . 1216–1225 . October 2021 . 34049460 . 10.1177/02698811211019279 . 235243643 .

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