Nitecapone

Nitecapone is a reversible inhibitor of S-catechol-O-methyltransferase (S-COMT; IC₅₀ = 300 nM in rat liver).¹ It is selective for S-COMT over tyrosine hydroxylase, dopamine-β-hydroxylase, DOPA decarboxylase, monoamine oxidase A (MAO-A), and MAO-B (IC₅₀s = >1 µM for all). In vivo, nitecapone inhibits liver, duodenal, and brain S-COMT (ID₅₀s = 5, 5, and 25 mg/kg, respectively). Nitecapone (3–30 mg/kg) reduces 3-O-methyl-DOPA (3-OMD) formation and increases serum and brain L-DOPA, dopamine, and DOPAC levels when administered in combination with L-DOPA (Item No. 13248) and carbidopa (Item No. 23783). Nitecapone (30 mg/kg) reduces mechanical and cold allodynia in a rat model of spinal nerve ligation-induced neuropathy.²

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1. Männistö, P.T., and Kaakkola, S. Catechol-O-methyltransferase (COMT): Biochemistry, molecular biology, pharmacology, and clinical efficacy of the new selective COMT inhibitors. Pharmacol. Rev. 51(4), 593-628 (1999).

2. Kambur, O., Männistö, P.T., Pusa, A.M., et al. Nitecapone reduces development and symptoms of neuropathic pain after spinal nerve ligation in rats. Eur. J. Pain 15(7), 732-740 (2015).