Braun A, Fabbrini G, Mouradian M M, Serrati C, Barone P, Chase T N
J Neural Transm. 1987;68(1-2):41-50. doi: 10.1007/BF01244638.
Preclinical evidence suggests that the D-1 dopamine receptor contributes to the generation of behaviors used as models for human extrapyramidal disorders. To evaluate the potential of D-1 receptor stimulation in neurologic disease, SKF 38393, a selective D-1 dopamine receptor agonist, was administered to seven patients with idiopathic Parkinson's disease in a double-blind, placebo controlled study. SKF 38393 was found to be rapidly absorbed when administered orally, and to occur in micromolar concentrations in spinal fluid. No change in scores of parkinsonian severity were noted when SKF 38393 was administered alone, or when the drug was combined with intravenous levodopa. The results support the view that the pathophysiology of Parkinson's disease may relate exclusively to the D-2 subclass of dopamine receptors.
临床前证据表明，D-1多巴胺受体有助于产生用作人类锥体外系疾病模型的行为。为了评估D-1受体刺激在神经疾病中的潜力，在一项双盲、安慰剂对照研究中，对7例特发性帕金森病患者给予了选择性D-1多巴胺受体激动剂SKF 38393。发现口服SKF 38393后吸收迅速，且在脑脊液中以微摩尔浓度存在。单独给予SKF 38393时，或该药物与静脉注射左旋多巴合用时，帕金森病严重程度评分均无变化。这些结果支持了帕金森病的病理生理学可能仅与多巴胺受体的D-2亚类有关的观点。
