单胺氧化酶B抑制剂在治疗帕金森病中的研究

Progression of MAO-B Inhibition in the Treatment of Parkinson’s Disease

理想的帕金森病治疗药物应是既能缓解症状,又能减缓疾病的进展。Safinamide是一种新型单胺氧化酶B(MAO-B)抑制剂,目前正在用于抗痉挛、抗帕金森病和神经保护方面的研究。Safinamide具有独特的分子结构、多重作用机制和很高的治疗指数。它既能高效、选择性和可逆的抑制MAO-B的活性,又能阻断钠、钙通道和抑制谷氨酸的释放。Safinamide还具有极好的的生物利用度、线型动力学、较长的半衰期和良好的安全性及耐受性。本文对主要的MAO-B抑制剂作一介绍。

The therapeutics in Parkinson＇s disease（PD） are to relieve symptoms and delay disease progression. Safinamide, as a novel monoamine oxidase B（MAO-B） inhibitor, currently is in clinical trials for the treatment of PD, anti-convulsion and neuroprotection. Safinamide is a unique molecule with multiple mecha- nisms of action and very high therapeutic index. It combines potent, selective, and reversible inhibition of MAO-B with blockade of voltage-dependent Na~ and Ca2~ channels and inhibition of glutamate release. Safinamide has excellent bioavailability, linear kinetics, fairly long half-time, good safety and tolerance. Therefore, safinamide may be a valuable therapeutic drug which can not only relieve symptoms but delay progression.