Chemistry:CP-94253

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CP-94253 is a drug of the tetrahydropyridinylpyrrolopyridine family which acts as a potent and selective serotonin 5-HT1B receptor agonist, with approximately 25- and 40-fold selectivity over the closely related serotonin 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] In addition, CP-94253 reduces aggression without causing sedation in rodents.[12][13][14][15][16][17][18][19]

A 2021 study[20] 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.

See also

References

  1. ↑ "Biochemical and behavioral studies of the 5-HT1B receptor agonist, CP-94,253". Drug Development Research 26 (3): 241–250. 1992. doi:10.1002/ddr.430260305. 
  2. ↑ "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. doi:10.1016/0028-3908(95)00112-3. PMID 8788962. 
  3. ↑ "Serotonin-mediated increase in prefrontal cortex dopamine release: pharmacological characterization". The Journal of Pharmacology and Experimental Therapeutics 277 (1): 40–47. April 1996. doi:10.1016/S0022-3565(25)12836-X. PMID 8613947. 
  4. ↑ "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. doi:10.1016/0031-9384(96)00073-x. PMID 8873272. 
  5. ↑ "CP-94, 253: a selective serotonin1B (5-HT1B) agonist that promotes satiety". Psychopharmacology 131 (3): 264–270. June 1997. doi:10.1007/s002130050292. PMID 9203237. 
  6. ↑ "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. doi:10.1007/s00213-002-1162-7. PMID 12373419. 
  7. ↑ "Serotonin1B receptor stimulation enhances cocaine reinforcement". The Journal of Neuroscience 18 (23): 10078–10089. December 1998. doi:10.1523/JNEUROSCI.18-23-10078.1998. PMID 9822762. 
  8. ↑ "Effect of serotonin (5-HT)1B receptor ligands on cocaine sensitization in rats". Behavioural Pharmacology 12 (2): 109–116. April 2001. doi:10.1097/00008877-200104000-00004. PMID 11396515. 
  9. ↑ "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. doi:10.1016/j.ejphar.2006.12.012. PMID 17291490. 
  10. ↑ "Effects of serotonin (5-HT)(1B) receptor ligands on cocaine-seeking behavior in rats". Pharmacological Reports 60 (6): 798–810. 2008. PMID 19211971. 
  11. ↑ "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. doi:10.1016/j.ejphar.2005.04.025. PMID 15913599. 
  12. ↑ "Social and neural determinants of aggressive behavior: pharmacotherapeutic targets at serotonin, dopamine and gamma-aminobutyric acid systems". Psychopharmacology (Berl) 163 (3-4): 434–458. October 2002. doi:10.1007/s00213-002-1139-6. PMID 12373445. 
  13. ↑ "Differential effects of CGS 12066B and CP-94,253 on murine social and agonistic behaviour". Pharmacol Biochem Behav 52 (1): 7–16. September 1995. doi:10.1016/0091-3057(95)00077-a. PMID 7501681. 
  14. ↑ "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. October 1999. doi:10.1007/pl00005484. PMID 10550489. 
  15. ↑ "Acute and long-term effects of a single dose of MDMA on aggression in Dark Agouti rats". Int J Neuropsychopharmacol 9 (1): 63–76. February 2006. doi:10.1017/S146114570500581X. PMID 16060968. 
  16. ↑ "5-HT(1B) receptors, ventral orbitofrontal cortex, and aggressive behavior in mice". Psychopharmacology (Berl) 185 (4): 441–450. May 2006. doi:10.1007/s00213-006-0333-3. PMID 16550387. 
  17. ↑ "Anti-aggressive effects of agonists at 5-HT1B receptors in the dorsal raphe nucleus of mice". Psychopharmacology (Berl) 193 (2): 295–304. August 2007. doi:10.1007/s00213-007-0780-5. PMID 17440711. 
  18. ↑ "5-HT(1B) receptor inhibition of alcohol-heightened aggression in mice: comparison to drinking and running". Psychopharmacology (Berl) 197 (1): 145–156. March 2008. doi:10.1007/s00213-007-1017-3. PMID 18071678. 
  19. ↑ "TAAR1 and 5-HT1B receptor agonists attenuate autism-like irritability and aggression in rats prenatally exposed to valproic acid". Pharmacol Biochem Behav 245: 173862. December 2024. doi:10.1016/j.pbb.2024.173862. PMID 39197535. 
  20. ↑ "5-HT1B receptor agonist attenuates cocaine self-administration after protracted abstinence and relapse in rats". Journal of Psychopharmacology 35 (10): 1216–1225. October 2021. doi:10.1177/02698811211019279. PMID 34049460. 



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