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‐HT 2 subtype. In particular, MDL 11,939 shows low affinity for the 5‐HT 1 and 5‐HT 3 subtypes of the serotonin receptor and displays low or negligible affinity for alpha adrenergic, dopaminergic, cholinergic, histamininergic, and opiate receptors. Because the 5‐HT 2 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.