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Vasodilator effects of dopaminomimetics in the perfused rat kidney.

Abstract：

:The renal vascular effects of dopaminomimetics were studied in the isolated perfused rat kidney after pretreatment with 10(-5) M phenoxybenzamine and 10(-5) M sotalol and after contraction of the vascular bed with prostaglandin F2 alpha (10(-7) to 3 x 10(-6) M). Under these conditions, our criterion for vascular dopaminomimetic activity was renal vasodilation, competitively inhibited by d-butaclamol (10(-8) M) but not by 1-butaclamol (3 x 10(-8) M). Dopamine is active at micromolar concentrations (ED50 = 2.53 +/- 0.34 x 10(-6) M). The N-alkylated analogues of dopamine preserve this activity if the alkyl group is a methyl group (epinine) or two n-propyl groups (di-n-propyl-dopamine). The catechol nucleus appears essential for renal vascular dopaminomimetic activity (SK&F 38393, active; p-tyramine, di-n-propyl-m-tyramine and RU 24926, inactive). Bromocriptine reproduces renal dopaminergic vasodilation with an ED50 of 1.3 +/- 0.14 x 10(-6) M. The study of structure-activity relationships of dopaminomimetics relates the vascular dopamine receptor, associated with renal vasodilation, to the dopamine receptor, associated with stimulation of dopamine-sensitive adenylate cyclase.

journal_name

Eur J Pharmacol

journal_title

European journal of pharmacology

authors

Schmidt M,Imbs JL,Giesen EM,Schwartz J

doi

10.1016/0014-2999(82)90157-1

subject

Has Abstract

pub_date

1982-10-15 00:00:00

pages

61-70

issue

1-2

eissn

0014-2999

issn

1879-0712

pii

0014-2999(82)90157-1

journal_volume

84

pub_type

杂志文章

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