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Pharmacological effects of MDL 11,939: A selective, centrally acting antagonist of 5‐HT 2 receptors
Author(s) -
Dudley Mark W.,
Wiech Norbert L.,
Miller Francis P.,
Carr Albert A.,
Cheng Hsien C.,
Roebel Lawrence E.,
Doherty Niall S.,
Yamamura Henry I.,
Ursillo Richard C.,
Palfreyman Michael G.
Publication year - 1988
Publication title -
drug development research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.582
H-Index - 60
eISSN - 1098-2299
pISSN - 0272-4391
DOI - 10.1002/ddr.430130104
Subject(s) - serotonergic , serotonin , receptor , 5 ht receptor , pharmacology , cholinergic , antagonist , chemistry , serotonin antagonists , receptor antagonist , radioligand , 5 ht2 receptor , medicine , endocrinology , biology , biochemistry
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.