Chemistry:Ipsapirone

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Ipsapirone (INN, USAN, BAN; developmental code names BAY Q 7821 and TVX Q 7821) is a selective 5-HT1A receptor partial agonist of the arylpiperazine and azapirone families which was under development for the treatment of major depressive disorder and anxiety disorders but was never marketed.[1][2] It is taken orally.[1]

The drug produces antidepressant-like, anxiolytic-like, and antiaggressive effects in rodents.[2][3] It has been found to increase oxytocin levels in rodents,[4][5][6][7] whereas findings in humans have been mixed.[8][9] Ipsapirone produces adverse effects including vertigo, dizziness, and dysphoria in humans.[10]

Ipsapirone produces 1-(2-pyrimidinyl)piperazine (1-PP), a potent α2-adrenergic receptor antagonist, as an active metabolite.[11] However, whereas 1-PP levels with buspirone are 8-fold higher than levels of buspirone itself, 1-PP is only a minor metabolite of ipsapirone constituting 2% of its exposure.[11]

Ipsapirone was first described in the scientific literature by 1984.[12][13] It was developed by Bayer.[1] The drug reached phase 3 clinical trials for treatment of major depressive disorder prior to the discontinuation of its development in 1997.[1] It was also studied for treatment of generalized anxiety disorder.[14]

See also

References

  1. ↑ 1.0 1.1 1.2 1.3 "Ipsapirone". 3 January 1997. https://adisinsight.springer.com/drugs/800000695. 
  2. ↑ 2.0 2.1 "Ipsapirone: a novel anxiolytic and selective 5-HT1A receptor ligand". Progress in Clinical and Biological Research 361: 461–467. 1990. PMID 1981264. 
  3. ↑ "5-HT1A and 5-HT1B receptor agonists and aggression: a pharmacological challenge of the serotonin deficiency hypothesis". Eur J Pharmacol 526 (1-3): 125–139. December 2005. doi:10.1016/j.ejphar.2005.09.065. PMID 16310183. 
  4. ↑ "Stimulation of 5-HT1A and 5-HT2/5-HT1C receptors induce oxytocin release in the male rat". Brain Res 611 (2): 330–332. May 1993. doi:10.1016/0006-8993(93)90521-n. PMID 8334526. 
  5. ↑ "Attenuation of hormone responses to the 5-HT1A agonist ipsapirone by long-term treatment with fluoxetine, but not desipramine, in male rats". Biol Psychiatry 36 (5): 300–308. September 1994. doi:10.1016/0006-3223(94)90627-0. PMID 7993956. 
  6. ↑ "Role of the hypothalamic paraventricular nucleus in 5-HT1A, 5-HT2A and 5-HT2C receptor-mediated oxytocin, prolactin and ACTH/corticosterone responses". Behav Brain Res 73 (1-2): 277–280. 1996. doi:10.1016/0166-4328(96)00112-x. PMID 8788518. 
  7. ↑ "Studies on the sites and mechanisms of 5-HT1A receptor-mediated in vivo actions". Acta Physiol Hung 84 (4): 399–401. 1996. PMID 9328612. 
  8. ↑ "Neuroendocrine and hypothermic effects of 5-HT1A receptor stimulation with ipsapirone in healthy men: a placebo-controlled study". Int Clin Psychopharmacol 13 (1): 23–32. January 1998. doi:10.1097/00004850-199801000-00004. PMID 9988364. 
  9. ↑ "Low doses of ipsapirone increase growth hormone but not oxytocin secretion in normal male and female subjects". Psychopharmacology (Berl) 145 (1): 99–104. July 1999. doi:10.1007/s002130051037. PMID 10445378. 
  10. ↑ Cite error: Invalid <ref> tag; no text was provided for refs named FuhrStaibHarder1994
  11. ↑ 11.0 11.1 Cite error: Invalid <ref> tag; no text was provided for refs named BerlinChalonPayan1995
  12. ↑ "Brain serotonin receptors as a target for the putative anxiolytic TVX Q 7821". Brain Res Bull 12 (6): 741–744. June 1984. doi:10.1016/0361-9230(84)90155-2. PMID 6541079. 
  13. ↑ "3H-TVX Q 7821: identification of 5-HT1 binding sites as target for a novel putative anxiolytic". Naunyn Schmiedebergs Arch Pharmacol 328 (4): 467–470. February 1985. doi:10.1007/BF00692918. PMID 2859533. 
  14. ↑ "Azapirones for generalized anxiety disorder". The Cochrane Database of Systematic Reviews 2006 (3). July 2006. doi:10.1002/14651858.CD006115. PMID 16856115. 



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