O'Boyle K M, Waddington J L
Department of Clinical Pharmacology, Royal College of Surgeons in Ireland, St. Stephen's Green, Dublin.
Neuropharmacology. 1987 Dec;26(12):1807-10. doi: 10.1016/0028-3908(87)90139-0.
3H-SCH 23390 and 3H-spiperone were used to label D-1 and D-2 dopamine receptors, respectively, in human post-mortem brain. SK&F 82958 and SK&F 77434, new substituted 1-phenyl-1H-3-benzazepines, showed selective affinity for the D-1 receptor. While S- and R- enantiomers of dihydroxynomifensine showed only weak stereoselective affinity for the D-1 receptor, the thieno [2,3-c]-and thieno [3,2-c]- analogues SK&F 89145 and SK&F 89641 showed selective D-1 affinity comparable to that of the benzazepines. These novel agents provide new information on structure-affinity relationships and D-1 receptor topography, and constitute new tools for functional studies.
3H-SCH 23390和3H-螺哌隆分别用于标记人死后大脑中的D-1和D-2多巴胺受体。新型取代的1-苯基-1H-3-苯并氮杂卓SK&F 82958和SK&F 77434对D-1受体表现出选择性亲和力。虽然二羟基米芬新的S-和R-对映体对D-1受体仅表现出较弱的立体选择性亲和力，但噻吩并[2,3-c]-和噻吩并[3,2-c]-类似物SK&F 89145和SK&F 89641表现出与苯并氮杂卓相当的选择性D-1亲和力。这些新型药物提供了有关结构-亲和力关系和D-1受体拓扑结构的新信息，并构成了功能研究的新工具。
