Opicapone (BIA 9-1067) 是一种有效的第三代儿茶酚-O-甲基转移酶 (COMT)抑制剂，有潜力用于帕金森病和运动波动的研究。Opicapone 降低细胞 ATP 含量，IC₅₀ 为 98 μM。

Opicapone (BIA 9-1067) is a potent third-generation catechol-O-methyltransferase (COMT) inhibitor for the research of Parkinsons disease and motor fluctuations. Opicapone decreases the ATP content of the cells with an IC 50 of 98 μM.

Solid

COMT

Opicapone has a prolonged inhibitory effect on peripheral COMT, which extends the bioavailability of L-DOPA, without inducing toxicity. Opicapone decreases the ATP content of the cells with IC50 values of 98 μM. Incubation of human primary hepatocytes for 24 h with increasing concentrations of Ro 40-7592, OR-611 or Opicapone resulted in a concentration-dependent decrease in the mitochondrial membrane potential of the cells, evaluated by the ratio JC-1 aggregates over JC-1 monomer (ratio λex 544 λem 590 over λex 485 λem 538). Opicapone decreases the mitochondrial membrane potential of the cells with IC50 of 181 μM. has not independently confirmed the accuracy of these methods. They are for reference only.

Opicapone inhibits rat peripheral COMT with ED 50 values below 1.4 mg/kg up to 6 h post-administration. The effect is sustained over the first 8 h and by 24 h COMT had not returned to control values. A single administration of Opicapone resulted in increased and sustained plasma L-DOPA levels with a concomitant reduction in 3-OMD from 2 h up to 24 h post-administration, while Ro 40-7592 produces significant effects only at 2 h post-administration. The effects of Opicapone on brain catecholamines after L-DOPA administration are sustained up to 24 h post-administration. Opicapone is also the least potent compound in decreasing both the mitochondrial membrane potential and the ATP content in human primary hepatocytes after a 24 h incubation period. has not independently confirmed the accuracy of these methods. Th

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[1]. Bonifácio MJ, et al. Pharmacological profile of Opicapone, a third-generation nitrocatechol catechol-O-methyl transferase inhibitor, in the rat. Br J Pharmacol. 2015 Apr;172(7):1739-52.
[2]. Ferreira JJ, et al. Opicapone as an adjunct to L-DOPA in patients with Parkinsons disease and end-of-dose motor fluctuations: a randomised, double-blind, controlled trial. Lancet Neurol. 2016 Feb;15(2):154-165.

In Vitro: DMSO : 100 mg/mL (242.03 mM; Need ultrasonic)H₂O : < 0.1 mg/mL (insoluble)配制储备液