3,5-Dinitrocatechol

3,5-Dinitrocatechol is a potent catechol O-methyltransferase (COMT) inhibitor (IC₅₀ = 12 nM).¹ It is selective for COMT over tyrosine hydroxylase, dopamine β-hydroxylase, dopamine decarboxylase, monoamine oxidase A (MAO-A), and MAO-B (IC₅₀s = >14 μM for all). 3,5-Dintrocatechol (30 mg/kg), in combination with L-DOPA (Item No. 13248) and carbidopa (Item No. 23783), reduces 3-O-methyldopa (3-OMD) levels in rat serum, compared with control animals receiving only L-DOPA and carbidopa. Chronic administration of 3,5-dinitrocatechol (15 mg/kg per day for seven days) induces COMT-dependent thermal hyperalgesia and increases preference for dark in a light/dark preference test, indicating anxiety-like behavior, in rats, effects that can be prevented by the β-adrenergic receptor antagonist propranolol (Item No. 23349).²

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1. Nissinen, E., Lindén, I.-B., Schultz, E., et al. Inhibition of catechol-O-methyltransferase activity by two novel disubstituted catechols in the rat. Eur. J. Pharmacol. 153(2-3), 263-269 (1988).

2. Kline, R.H., IV, Exposto, F.G., O'Buckley, S.C., et al. Catechol-O-methyltransferase inhibition alters pain and anxiety-related volitional behaviors through activation of β-adrenergic receptors in the rat. Neuroscience 290, 561-569 (2015).