Pharmacological effects of MDL 11,939: A selective, centrally acting antagonist of 5-HT2 receptors

MDL 11,939 (α-phenyl-1-(2-phenylethyl)-4-piperidine methanol) has been shown, through in vitro studies utilizing radioligand binding and isolated tissues as well as through in vivo tests of central and peripheral serotonergic activity, to be a potent, selective antagonist at 5-hydroxytryptamine receptors of the 5-HT2 subtype. In particular, MDL 11,939 shows low affinity for the 5-HT1 and 5-HT3 subtypes of the serotonin receptor and displays low or negligible affinity for alpha adrenergic, dopaminergic, cholinergic, histamininergic, and opiate receptors. Because the 5-HT2 subtype of the serotonin receptor has been implicated in the control of both the central nervous and vascular systems of experimental animals, it is likely that a compound with the potency and specificity of MDL 11,939 has interesting therapeutic potential.