Pharmacological profile of ritanserin: A very specific central serotonin S2‐antagonist
Drug Development Research January 1, 1988 F. Awouters, C. J. E. Niemegeers, Anton A. H. P. Megens et al. 139 citations
Ritanserin, a novel methylenepiperidine derivative, acts as a potent, long-lasting, and specific central serotonin S2 antagonist in rats. It inhibits tryptamine-induced cyanosis at 0.0070 mg/kg and bilateral clonic seizures at 0.037 mg/kg, and it blocks mescaline- and 5-HTP-induced head twitches at doses up to 0.11 mg/kg. The compound does not generalize with LSD but weakly antagonizes the LSD discriminative stimulus. It reverses mast cell serotonin cyanosis at 0.012 mg/kg and inhibits gastric lesions at 0.028 mg/kg. Ritanserin shows no central dopamine antagonism or interference with norepinephrine or acetylcholine at doses up to 40 mg/kg. Peripheral histamine antagonism requires 270 times the central S2-antagonism dose.