Flietstra R J, Levant B
Department of Pharmacology, Toxicology, and Therapeutics, University of Kansas Medical Center, Kansas City 66160-7417, USA.
Life Sci. 1998;62(20):1825-31. doi: 10.1016/s0024-3205(98)00148-9.
This study used quantitative autoradiography to simultaneously evaluate the relative affinities of dopaminergic compounds for dopamine D2 and D3 receptors in rat brain. PD 152255, PD 128907, and l-nafadotride exhibited significantly higher affinity for cerebellar dopamine D3 sites than [3H]quinpirole-labeled sites in caudate/putamen (6.3-, 6.0-, and 2.3-fold, respectively). In contrast, chlorpromazine, risperidone, and domperidone were more potent at striatal dopamine D2 receptors (3.8-, 31-, and 40-fold, respectively). Dopamine, quinelorane, (+)-UH 232, and RS-trans-7-OH-PIPAT exhibited relatively little D2/D3 selectivity.
本研究采用定量放射自显影术，同时评估多巴胺能化合物对大鼠脑内多巴胺D2和D3受体的相对亲和力。与尾状核/壳核中[3H]喹吡罗标记的位点相比，PD 152255、PD 128907和l-萘法朵曲对小脑多巴胺D3位点表现出显著更高的亲和力（分别为6.3倍、6.0倍和2.3倍）。相比之下，氯丙嗪、利培酮和多潘立酮对纹状体多巴胺D2受体的活性更高（分别为3.8倍、31倍和40倍）。多巴胺、喹氯雷、(+)-UH 232和RS-反式-7-羟基-PIPAT表现出相对较小的D2/D3选择性。
