Pirenperone
chemical compound
Pirenperone (INNTooltip International Nonproprietary Name, USANTooltip United States Adopted Name, BANTooltip British Approved Name; 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.
It is a relatively selective antagonist of the serotonin 5-HT2A receptor and has been used in scientific research to study the serotonin system. 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.
The elimination half-life of pirenperone has been said to be 4 to 6 hours.
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. Along similar lines, there has been interest in pirenperone for potential use as a trip killer against psychedelics in humans.
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This entry incorporates text from “Pirenperone” on English Wikipedia. Contributors are listed in the page history. Text is available under the Creative Commons Attribution-ShareAlike 4.0 License. Selected authority identifiers and statements are retrieved from Wikidata under CC0; their references and qualifiers remain part of the verification path.