Chemistry:Flesinoxan

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Flesinoxan (developmental code name DU-29373) is a potent and selective 5-HT1A receptor partial or near-full agonist of the phenylpiperazine class.[1][2][3][4] Originally developed as a potential antihypertensive drug,[2][3][5] flesinoxan was later found to possess antidepressant and anxiolytic effects in animal tests.[6][7] As a result, it was investigated in several small human pilot studies for the treatment of major depressive disorder, and was found to have robust effectiveness and very good tolerability.[8][9] It was also developed for treatment of anxiety disorders.[1] The drug reached phase 3 clinical trials for anxiety disorders.[1] However, due to "management decisions", the development of flesinoxan was stopped and it was not pursued any further.[1][10] In humans, flesinoxan enhances REM sleep latency, decreases body temperature, and increases ACTH, cortisol, prolactin, and growth hormone secretion.[3][9] In addition, both flesinoxan and LY-178210 induce anxiety in humans.[11]

See also

References

  1. ↑ 1.0 1.1 1.2 1.3 "Flesinoxan". 23 November 1999. https://adisinsight.springer.com/drugs/800001126. 
  2. ↑ 2.0 2.1 "Centrally acting hypotensive agents with affinity for 5-HT1A binding sites inhibit forskolin-stimulated adenylate cyclase activity in calf hippocampus". British Journal of Pharmacology 95 (3): 975–85. November 1988. doi:10.1111/j.1476-5381.1988.tb11728.x. PMID 3207999. 
  3. ↑ 3.0 3.1 3.2 "Hormonal and temperature responses to flesinoxan in normal volunteers: an antagonist study". European Neuropsychopharmacology 14 (2): 151–5. March 2004. doi:10.1016/S0924-977X(03)00108-1. PMID 15013031. 
  4. ↑ "Characterization of 5-hydroxytryptamine1A properties of flesinoxan: in vivo electrophysiology and hypothermia study". Neuropharmacology 34 (10): 1311–26. October 1995. doi:10.1016/0028-3908(95)00098-Q. PMID 8570029. 
  5. ↑ "Flesinoxan lowers blood pressure and heart rate in cats via 5-HT1A receptors". European Journal of Pharmacology 149 (3): 213–23. May 1988. doi:10.1016/0014-2999(88)90651-6. PMID 2842163. 
  6. ↑ "Flesinoxan shows antidepressant activity in a DRL 72-s screen". Psychopharmacology 107 (4): 474–9. 1992. doi:10.1007/BF02245258. PMID 1351303. 
  7. ↑ "Antianxiety and behavioral suppressant actions of the novel 5-HT1A receptor agonist, flesinoxan". Pharmacology, Biochemistry, and Behavior 48 (4): 959–63. August 1994. doi:10.1016/0091-3057(94)90205-4. PMID 7972301. 
  8. ↑ "An open study of oral flesinoxan, a 5-HT1A receptor agonist, in treatment-resistant depression". International Clinical Psychopharmacology 8 (3): 167–72. 1993. doi:10.1097/00004850-199300830-00005. PMID 8263314. 
  9. ↑ 9.0 9.1 "Pilot study of flesinoxan, a 5-HT1A agonist, in major depression: Effects on sleep REM latency and body temperature.". Human Psychopharmacology: Clinical and Experimental 8 (4): 279–283. 2004. doi:10.1002/hup.470080407. https://orbi.uliege.be/bitstream/2268/87817/1/Pilot%20study%20of%20flesinoxan%20in%20major%20depression.%20Effect%20on%20REM%20latency%20and%20body%20temperature.pdf. 
  10. ↑ "Serotonin 5-HT1A receptors as targets for agents to treat psychiatric disorders: rationale and current status of research". CNS Drugs 27 (9): 703–16. September 2013. doi:10.1007/s40263-013-0071-0. PMID 23757185. 
  11. ↑ "The broad-spectrum antiemetic effects ETI-385 result from stimulation of 5-HT1A and 5-HT1D receptors". Exp Brain Res 232 (8): 2699–2707. August 2014. doi:10.1007/s00221-014-4004-z. PMID 24913143. "Another hindrance to the clinical evaluation of this mechanism is that both flesinoxan (van Vliet et al. 1996) and LY22879 (pers. com.) induced anxiety in humans.". 



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