New substituted 1-phenyl-3-benzazepine analogues of SK&F 38393 and N-methyl-thienopyridine analogues of dihydroxynomifensine with selective affinity for the D-1 dopamine receptor in human post-mortem brain.
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.
D015647:2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine; D001552:Benzazepines / Q000378:metabolism*; D001667:Binding, Competitive; D001923:Brain Chemistry; D006801:Humans; D066298:In Vitro Techniques; D007700:Kinetics; D008024:Ligands; D009627:Nomifensine / Q000031:analogs & derivatives* / Q000378:metabolism; D011699:Putamen / Q000378:metabolism; D011725:Pyridines / Q000378:metabolism; D011954:Receptors, Dopamine / Q000378:metabolism*; D013134:Spiperone / Q000378:metabolism; D013876:Thiophenes / Q000378:metabolism
D001552:Benzazepines; D008024:Ligands; D011725:Pyridines; D011954:Receptors, Dopamine; D013876:Thiophenes; D009627:Nomifensine; D013134:Spiperone; D015647:2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine; C024878:3',4'-dihydroxynomifensine