5-HT2a/2c receptor blockade by amesergide fully attenuates prolactin response to d-fenfluramine challenge in physically healthy human subjects.

Prolactin responses to d-fenfluramine (d-FEN) challenge (0.5 mg/kg PO) were examined after pre-treatment with and without the 5-HT2a/2c receptor antagonist amesergide in eight physically healthy male volunteers. Compared to pretreatment with placebo, pre-treatment with amesergide completely blocked the prolactin (PRL) response to d-FEN challenge in all subjects. These data are consistent with data demonstrating a complete blockade of the PRL response to d-FEN with the 5-HT2a/2c receptor antagonist ritanserin, and suggest that the PRL response to d-FEN challenge in humans may largely be due to activation of the 5-HT2a/2c receptor.