Kreiss D S, Bergstrom D A, Gonzalez A M, Huang K X, Sibley D R, Walters J R
Neurophysiological Pharmacology Section, National Institute of Neurological Disorders and Stroke, National Institutes of Health, Bethesda, MD 20892-1406, USA.
Eur J Pharmacol. 1995 Apr 24;277(2-3):209-14. doi: 10.1016/0014-2999(95)00069-w.
The potencies for in vivo inhibition of substantia nigra pars compacta dopamine single cell firing were determined for apomorphine, BHT 920, N-0923, (+/-)-7-hydroxy-dipropylaminotetralin (7-OH-DPAT), (+)-3-(3-hydroxyphenyl)-N-propylpiperidine (3-PPP), pramipexole, quinelorane, quinpirole, RU 24926, U-86170, and U-91356. Significant correlation was obtained between the potencies of these 11 highly efficacious dopamine receptor agonists and the in vitro binding affinities at dopamine D3 receptors, but not at dopamine D2L receptors. These results support a functional role for the dopamine D3 receptor subtype in the autoreceptor-mediated regulation of dopamine cell activity, while a role for dopamine D2 receptors awaits further analysis. In addition, the results demonstrate the limitations of using currently available dopamine receptor agonists to delineate relative in vivo roles for the dopamine D2 and D3 receptor subtypes.
测定了阿扑吗啡、BHT 920、N - 0923、（±）-7 - 羟基 - 二丙基氨基四氢萘（7 - OH - DPAT）、（+）-3 -（3 - 羟基苯基）-N - 丙基哌啶（3 - PPP）、普拉克索、喹洛雷、喹吡罗、RU 24926、U - 86170和U - 91356对黑质致密部多巴胺单细胞放电的体内抑制效力。这11种高效多巴胺受体激动剂的效力与多巴胺D3受体的体外结合亲和力之间存在显著相关性，但与多巴胺D2L受体的体外结合亲和力之间不存在显著相关性。这些结果支持多巴胺D3受体亚型在自受体介导的多巴胺细胞活性调节中发挥功能作用，而多巴胺D2受体的作用有待进一步分析。此外，结果表明使用目前可用的多巴胺受体激动剂来描述多巴胺D2和D3受体亚型在体内的相对作用存在局限性。
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