Molindone hydrochloride (EN-1733A)

A dopamine receptor antagonist

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10mg

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480.00

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Background

Molindone is a dopamine receptor antagonist.¹ It selectively inhibits radioligand binding to dopamine D₂ receptors in rat brain homogenates (IC₅₀s = 56 and >10,000 nM for D₂ and D₁ receptors, respectively), however, it inhibits radioligand binding to both D₂ and D₁ receptors in vivo (ED₅₀s = 4.9 and 51 mg/kg, respectively). Molindone (0.4-0.8 mg/kg) reverses depression of dopamine neurons induced by D-amphetamine and apomorphine and increases dopamine synthesis and dihydroxyphenylacetic acid levels in the striatum and olfactory tubercles in rats.² It suppresses spontaneous locomotion and blocks conditioned avoidance responses in male mice and female rats.³ It inhibits climbing behavior in mice induced by the D₂ receptor agonist bromocriptine .⁴ Molindone (0.3-5.6 mg/kg) increases error rates and reduces response rate in pigeons following learned acquisition.⁵ Formulations containing molindone have been used in the treatment of schizophrenia.

1.Andersen, P.H.Comparison of the pharmacological characteristics of [3H]raclopride and [3H]SCH 23390 binding to dopamine receptors in vivo in mouse brainEur. J. Pharmacol.146(1)113-120(1988) 2.Bunney, B.S., Roth, R.H., and Aghajanian, G.K.Effects of molindone on central dopaminergic neuronal activity and metabolism: Similarity to other neurolepticsPsychopharmacol. Commun.1(4)349-358(1975) 3.Rubin, A.A., Yen, H.C., and Pfeffer, M.Psychopharmacological profile of molindoneNature216(5115)578-579(1967) 4.Balsara, J.J., Nandal, N.V., Gada, V.P., et al.Antagonism of bromocriptine-induced cage climbing behaviour in mice by the selective D-2 dopamine receptor antagonists, metoclopramide and molindoneIndian J. Physiol. Pharmacol.30(1)85-90(1986) 5.Poling, A., Cleary, J., Berens, K., et al.Neuroleptics and learning: Effects of haloperidol, molindone, mesoridazine and thioridazine on the behavior of pigeons under a repeated acquisition procedureJ. Pharmacol. Exp. Ther.255(3)1240-1245(1990)