Pirenperone

 ( 5-ht2 Antagonists ) 

Pirenperone (, , ; developmental code names R-47456 and 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.

(1999). 9780751404999, Springer Science & Business Media. . ISBN 9780751404999

It is a relatively selective antagonist of the serotonin 5-HT_2A receptor and has been used in scientific research to study the serotonin system.

Its affinities (K_i) for serotonin and other receptors have been reported to be 0.3 to 1.1nM for the serotonin 5-HT_2A receptor, 6.5nM for the serotonin 5-HT₇ receptor, 20nM for the α_1B-adrenergic receptor, 20nM for the α_2B-adrenergic receptor, 61nM for the serotonin 5-HT_2B receptor, 60 to 77nM for the serotonin 5-HT_2C receptor, 485 to 1,700nM for the serotonin 5-HT_1A receptor, and >1,000 or 6,600nM for the serotonin 5-HT_1B receptor, whereas other receptors were not reported.

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-HT_2A receptor as the biological mediator of the effects of serotonergic psychedelics.

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See also

• Serotonin 5-HT_2A receptor antagonist
• Altanserin
• Ketanserin
• Setoperone
• Risperidone
• Ocaperidone

Categories: 5-ht2 Antagonists, Abandoned Drugs, Antipsychotics, Anxiolytics, 4-fluorophenyl Compounds, Hallucinogen Antidotes, Ketones, Piperidines, Pyridopyrimidines

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