Levant B, Grigoriadis D E, De Souza E B
DuPont Merck Pharmaceutical Company, Wilmington, DE 19880, USA.
Eur J Pharmacol. 1995 May 24;278(3):243-7. doi: 10.1016/0014-2999(95)00160-m.
Quantitative autoradiography was used to evaluate the pharmacological profile of dopamine D2-like receptors labeled by [125I]iodosulpiride. Caudate/putamen, a brain region associated primarily with dopamine D2 receptor mRNA, was used as a prototypical D2 tissue; cerebellar lobule X (D3 mRNA associated), as a D3 tissue. 7-OH-DPAT ((+/-)-2-dipropylamino-7-hydroxy-1,2,3,4- tetrahydronaphthalene) exhibited selectively for cerebellar receptors (24-fold), followed by quinpirole (6-fold). Haloperidol and domperidone were 4- and 18-fold more potent at striatal receptors, respectively. These data are in close agreement with that derived from dopamine D2 and D3 receptor-expressing cell lines.
采用定量放射自显影术评估[125I]碘舒必利标记的多巴胺D2样受体的药理学特征。尾状核/壳核是主要与多巴胺D2受体mRNA相关的脑区，用作典型的D2组织；小脑小叶X（与D3 mRNA相关）用作D3组织。7-OH-DPAT（(+/-)-2-二丙基氨基-7-羟基-1,2,3,4-四氢萘）对小脑受体具有选择性（24倍），其次是喹吡罗（6倍）。氟哌啶醇和多潘立酮对纹状体受体的效力分别高4倍和18倍。这些数据与源自表达多巴胺D2和D3受体的细胞系的数据密切一致。
