Blockade of dopamine receptors in the renal vasculature by isomers of flupenthixol and sulpiride.
We studied the renal vascular effects of flupenthixol and sulpiride isomers in the isolated perfused rat kidney in the presence of phenoxybenzamine (10(-5) M) and sotalol (10(-5) M). The vascular bed was contracted with prostaglandin F2 alpha (10(-7) -3 X 10(-6) M) and dose-dependently relaxed with dopamine. Cis-flupenthixol (10(-9)-10(-7) M) antagonized competitively the response to dopamine (apparent pA2 = 8.34 +/- 0.09; mean +/- SD) without affecting papaverine-induced relaxation. Trans-flupenthixol was without effect at 10(-7) M. The dopamine receptor antagonist activities of the sulpiride isomers are low and d-sulpiride is twice as active as 1-sulpiride. Thus, the renal vascular dopamine receptor can be further characterized by the relative antagonist activities of cis-flupenthixol and sulpiride and by a rather low stereospecificity in favor of d-sulpiride.
D000818:Animals; D002069:Butaclamol / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D005475:Flupenthixol / Q000494:pharmacology*; D008297:Male; D010208:Papaverine / Q000494:pharmacology; D051381:Rats; D011919:Rats, Inbred Strains; D011954:Receptors, Dopamine / Q000187:drug effects*; D012079:Renal Circulation / Q000187:drug effects*; D013237:Stereoisomerism; D013469:Sulpiride / Q000494:pharmacology*; D013892:Thioxanthenes / Q000494:pharmacology*
D011954:Receptors, Dopamine; D013892:Thioxanthenes; D013469:Sulpiride; D002069:Butaclamol; D010208:Papaverine; D005475:Flupenthixol