第二代高选择性、强效、无毒、口服的COMT抑制剂托卡朋和安托卡朋经临床前和临床药理试验证明能够安全有效地抑制左旋多巴的代谢,延长其半衰期,从而提高L-dopa的生物利用度,但却不增加它的剂峰浓度,因此并不加重剂峰毒性作用如运动障碍和幻视,成为一种具有重大应用潜力的帕金森病辅助治疗药物。 The second generation of highly selective, potent, nontoxic, oral COMT inhibitor tokapen and antacoban proved to be safe and effective in inhibiting levodopa metabolism and prolonging its half-life by preclinical and clinical pharmacological tests The bioavailability of L-dopa, however, does not increase its peak concentration and therefore does not exacerbate peak peak toxicities such as dyskinesia and hallucination, making it an adjunct to Parkinson’s disease of great potential.