The central effects of a novel dopamine agonist

A new peripheral dopamine agonist which causes dopaminergic renal vasodilation, was tested for central dopaminergic activity. SK & F 38393 stimulated the dopamine-sensitive adenylate cyclase in homogenates of rat caudate, as a partial agonist, and caused contralateral rotation in rats with unila...

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Bibliographic Details
Published inEuropean journal of pharmacology Vol. 50; no. 4; p. 419
Main Authors Setler, P E, Sarau, H M, Zirkle, C L, Saunders, H L
Format Journal Article
LanguageEnglish
Published Netherlands 15.08.1978
Subjects
Adenylyl Cyclases - metabolism
Animals
Benzazepines - pharmacology
Dogs
Dopamine - metabolism
Dopamine - physiology
Female
Humans
Male
Prolactin - blood
Rats
Stereotyped Behavior - drug effects
Substantia Nigra - physiology
Vomiting - chemically induced
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Summary:A new peripheral dopamine agonist which causes dopaminergic renal vasodilation, was tested for central dopaminergic activity. SK & F 38393 stimulated the dopamine-sensitive adenylate cyclase in homogenates of rat caudate, as a partial agonist, and caused contralateral rotation in rats with unilateral 6-OHDA lesions of substantia nigra. Rotation was shown to be due to a direct effect on supersensitive dopamine receptors. Stimulation of cAMP formation and rotation were blocked by dopamine antagonists. In contrast to other dopamine agonists, SK & F 38393 did not cause stereotypy, emesis or inhibition of prolactin release, nor did SK & F 38393 affect dopamine turnover. The results suggest that SK & F 38393 may selectively stimulate supersensitive central dopamine receptors in vivo or may activate only a certain subclass of dopamine receptors including the receptor in the renal vasculature and the adenylate cyclase coupled postsynaptic receptor in the caudate.
ISSN:0014-2999
1879-0712
DOI:10.1016/0014-2999(78)90148-6