MDL 11939

MDL 11939 is a potent, orally bioavailable, and selective antagonist of the serotonin (5-HT) receptor subtype 5-HT_2A (K_i = 6.06 nM for the human receptor).¹ It is selective for the human 5-HT_2A receptor over human 5-HT_2B and 5-HT_2C and rat 5-HT_2B receptors (K_is = 3,020, 1,020, and 4,700 nM, respectively), as well as 5-HT₁, 5-HT_1A, α₁- and α₂-adrenergic, dopamine D₂, muscarinic acetylcholine, histamine, and opiate receptors.^1,2 MDL 11939 administered to rats prior to or following learned helplessness-induced stress prevents increases in acoustic startle response.³ MDL 11939 (10 mg/kg, i.v.) also has anti-arrhythmic activity in anesthetized dogs following myocardial infarction.⁴

WARNING This product is not for human or veterinary use.

1. Dudley, M.W., Wiech, N.L., Miller, F.P., et al. Pharmacological effects of MDL 11,939: A selective, centrally acting antagonist of 5-HT₂ receptors. Drug Dev. Res. 13(1), 29-43 (1988).

2. Wainscott, D.B., Lucaites, V.L., Kursar, J.D., et al. Pharmacologic characterization of the human 5-hydroxytryptamine2B receptor: Evidence for species differences. J. Pharmacol. Exp. Ther. 276(2), 720-727 (1996).

3. Jiang, X., Zhang, Z.-j., Zhang, S., et al. 5-HT_2A receptor antagonism by MDL 11,939 during inescapable stress prevents subsequent exaggeration of acoustic startle response and reduced body weight in rats. J. Psychopharmacol. 25(2), 289-297 (2011).

4. Koerner, J.E., and Dage, R.C. Antiarrhythmic and electrophysiologic effects of MDL 11,939, a novel class III antiarrhythmic agent in anesthetized dogs. J. Cardiovasc. Pharmacol. 16(3), 383-393 (1990).