Lieberman A, Chin L, Baumann G
Department of Neurology, N.Y.U. School of Medicine, NY 10016.
Clin Neuropharmacol. 1988 Jun;11(3):191-200. doi: 10.1097/00002826-198806000-00001.
MK 458 is a potent and selective D2 receptor agonist. MK 458 consists of (+)-4-propyl-9-hydroxynaphthoxazine (PHNO) in a hydroxypropyl-methylcellulose-lactose matrix. MK 458, mean dose 8.1 mg (range 2.5 to 13.5 mg), was administered to 14 patients with advanced Parkinson's disease (PD) who were no longer satisfactorily responding to levodopa. The duration of the study was 4 weeks with a titration to maximum dose in 2 weeks. The addition of MK 458 resulted in a mean reduction in levodopa of 41% (range 0 to 81%). This degree of levodopa reduction was not seen in previous studies with other DA agonists. While the reduction in signs of PD was comparable to those on levodopa, MK 458 did not induce dyskinesias or dystonias. It is postulated that MK 458 may be able to replace levodopa as the primary treatment for PD.
MK 458是一种强效且具有选择性的D2受体激动剂。MK 458由（+）-4-丙基-9-羟基萘并恶嗪（PHNO）存在于羟丙基甲基纤维素-乳糖基质中构成。给14例晚期帕金森病（PD）患者服用MK 458，这些患者对左旋多巴的反应不再令人满意，平均剂量为8.1毫克（范围为2.5至13.5毫克）。研究持续时间为4周，在2周内滴定至最大剂量。添加MK 458导致左旋多巴平均减少41%（范围为0至81%）。在先前使用其他多巴胺激动剂的研究中未观察到这种程度的左旋多巴减少。虽然帕金森病体征的减轻与使用左旋多巴时相当，但MK 458未诱发异动症或肌张力障碍。据推测，MK 458或许能够取代左旋多巴作为帕金森病的主要治疗方法。
