Selective and stereospecific interactions of R-SK & F 38393 with [3H]piflutixol but not [3H]spiperone binding to striatal D1 and D2 dopamine receptors: comparisons with SCH 23390.
Four benzazepine derivatives, racemic SK&F 38393, its resolved R- and S-enantiomers, and SCH 23390 have been investigated for their interactions with striatal D1 and D2 dopamine receptors, as indexed by the binding of [3H] piflutixol and [3H]spiperone respectively. For the agonist SK&F 38393, its R-enantiomer was active in displacing [3H] piflutixol while its S- antipode was 100 fold less potent. In contrast, both enantiomers showed similar and negligible activity to displace [3H]spiperone. SCH 23390, an antagonist analogue with an R-configuration, potently displaced [3H] piflutixol but not [3H]spiperone. R-SK&F 38393 and SCH 23390 may help clarify the structural requirements for, and functional consequences of, selective actions at the D1 dopamine receptor.
D015647:2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine; D000818:Animals; D014150:Antipsychotic Agents / Q000378:metabolism*; D001067:Appetite Depressants / Q000378:metabolism*; D001552:Benzazepines / Q000378:metabolism*; D001667:Binding, Competitive; D002090:Butyrophenones / Q000378:metabolism*; D003342:Corpus Striatum / Q000378:metabolism*; D066298:In Vitro Techniques; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains; D011954:Receptors, Dopamine / Q000378:metabolism*; D013134:Spiperone / Q000378:metabolism*; D013237:Stereoisomerism; D013892:Thioxanthenes / Q000378:metabolism*
D014150:Antipsychotic Agents; D001067:Appetite Depressants; D001552:Benzazepines; D002090:Butyrophenones; D011954:Receptors, Dopamine; D013892:Thioxanthenes; D013134:Spiperone; D015647:2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine; C015448:piflutixol