4F-4PP, or 4F4PP, also known as 4-(4-fluorobenzoyl)-1-(4-phenylbutyl)piperidine, is a selective serotonin 5-HT2A receptor antagonist which is used in scientific research.
Pharmacology 4F-4PP shows high affinity for the serotonin 5-HT2A receptor (Ki = 5.3nM) and 120-fold lower affinity for the serotonin 5-HT2C receptor (Ki = 620nM). For comparison, ketanserin showed only 14-fold higher affinity for the serotonin 5-HT2A receptor over the serotonin 5-HT2C receptor in the same study. In a functional assay, 4F-4PP was 204-fold more potent as a serotonin 5-HT2A receptor antagonist than as a serotonin 5-HT2C receptor antagonist. The drug does not appear to block the serotonin 5-HT2B receptor. It showed limited and non-significant effects on the oxytocin and vasopressin secretion induced by the serotonin 5-HT2A and 5-HT2C receptor agonist and serotonergic psychedelic DOI in rodents.
Chemistry Analogues A radiolabeled isotopologue for use in positron emission tomography (PET) imaging has been described.
History 4F-4PP first described in the scientific literature by 1992. It is an analogue of and was derived via structural modification of ketanserin.
See also Serotonin 5-HT2A receptor antagonist Lenperone Glemanserin Lidanserin Volinanserin
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