Chemistry:Pirenperone

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Pirenperone (INN, USAN, BAN; developmental code names R-47456, R-50656) is a serotonin receptor antagonist closely related to ketanserin and risperidone which is described as an antipsychotic and tranquilizer and was never marketed.[1][2]

It is a relatively selective antagonist of the serotonin 5-HT2A receptor and has been used in scientific research to study the serotonin system.[3][2][4][5] Its affinities (Ki) for serotonin and other receptors have been reported to be 0.3 to 1.1 nM for the serotonin 5-HT2A receptor, 6.5 nM for the serotonin 5-HT7 receptor, 20 nM for the α1B-adrenergic receptor, 20 nM for the α2B-adrenergic receptor, 61 nM for the serotonin 5-HT2B receptor, 60 to 77 nM for the serotonin 5-HT2C receptor, 485 to 1,700 nM for the serotonin 5-HT1A receptor, and >1,000 or 6,600 nM for the serotonin 5-HT1B receptor, whereas other receptors were not reported.[3][5]

In the 1980s, the drug was found to block the effects of the lysergic acid diethylamide (LSD) in animals, and, along with ketanserin, led to the elucidation of the 5-HT2A receptor as the biological mediator of the effects of serotonergic psychedelics.[6]

See also

References

  1. ↑ The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies. Springer. 14 November 2014. pp. 994–. ISBN 978-1-4757-2085-3. https://books.google.com/books?id=0vXTBwAAQBAJ&pg=PA994. 
  2. ↑ 2.0 2.1 Concise Dictionary of Pharmacological Agents: Properties and Synonyms. Springer Science & Business Media. 31 October 1999. pp. 223–. ISBN 978-0-7514-0499-9. https://books.google.com/books?id=mqaOMOtk61IC&pg=PA223. 
  3. ↑ 3.0 3.1 ""Selective" serotonin 5-HT2A receptor antagonists". Biochem Pharmacol 200. June 2022. doi:10.1016/j.bcp.2022.115028. PMID 35381208. 
  4. ↑ Transduction Mechanisms of Drug Stimuli. Springer Science & Business Media. 6 December 2012. pp. 29–. ISBN 978-3-642-73223-2. https://books.google.com/books?id=9PfRBgAAQBAJ&pg=PT29. 
  5. ↑ 5.0 5.1 "Central serotonin receptors as targets for drug research". J Med Chem 30 (1): 1–12. January 1987. doi:10.1021/jm00384a001. PMID 3543362. "Table II. Affinities of Selected Phenalkylamines for 5-HT1 and 5-HT2 Binding Sites". 
  6. ↑ "Psychedelics". Pharmacological Reviews 68 (2): 264–355. April 2016. doi:10.1124/pr.115.011478. PMID 26841800. 



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