Domino E F
Department of Pharmacology, University of Michigan, Ann Arbor 48109-0632, USA.
Brain Res Bull. 1997;43(1):93-5. doi: 10.1016/s0361-9230(96)00346-2.
Both SKF-82958 and N-0923, selective full D1-like and D2-like agonists, respectively, given IM produced contraversive circling and reduced neurologic deficits in six MPTP-induced hemiparkinsonian monkeys. A small fixed dose of N-0923 (10 micrograms/kg) and increasing doses of SKF-82958 (23.4-234 micrograms/kg) in combination were synergistic or antagonistic in this animal model. A small dose (23.4 micrograms/kg) of SKF-82958, in combination with N-0923, caused potentiation, an intermediate dose (74.8 micrograms/kg) in combination produced additive effects, while a very large dose (234 micrograms/kg) in combination produced antagonism. All three doses of SKF-82958 prolonged the duration of action of a small dose (10 ng/kg) of N-0923. Selective D1-like and D2-like agonists should be studied as potential therapeutic agents alone and in combination in human idiopathic parkinsonism, especially using low and intermediate doses.
选择性的完全D1样激动剂SKF-82958和D2样激动剂N-0923,分别通过肌肉注射给予6只MPTP诱导的偏侧帕金森病猴,均产生了向对侧旋转,并减轻了神经功能缺损。在该动物模型中,小固定剂量的N-0923(10微克/千克)与递增剂量的SKF-82958(23.4 - 234微克/千克)联合使用时具有协同或拮抗作用。小剂量(23.4微克/千克)的SKF-82958与N-0923联合使用会产生增强作用,中等剂量(74.8微克/千克)联合使用产生相加作用,而大剂量(234微克/千克)联合使用则产生拮抗作用。所有三个剂量的SKF-82958均延长了小剂量(10纳克/千克)N-0923的作用持续时间。应单独或联合研究选择性D1样和D2样激动剂作为人类特发性帕金森病潜在治疗药物的可能性,尤其是使用低剂量和中等剂量时。