Lergotrile and lisuride: in vivo dopaminergic agonists which do not stimulate the presynaptic dopamine autoreceptor. |
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| Authors: | J W Kebabian P R Kebabian |
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| Institution: | Biochemical Neuropharmacology Unit, Experimental Therapeutics Branch, National Institute of Neurological and Communicative Disorders and Stroke, National Institutes of Health, Bethesda, Maryland 20014, USA |
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| Abstract: | The presynaptic dopaminergic autoreceptor which regulates tyrosine hydroxylase is unaffected by the dopaminergic ergots and their specific antagonists. Apomorphine inhibits the conversion of tyrosine to catechols by striatal synaptosomes; neither lergotrile nor lisuride mimic this action of apomorphine. Furthermore metoclopramide, a potent dopaminergic antagonist in the anterior pituitary, does not block the inhibitory effect of apomorphine. The data demonstrate that the several categories pharmacologically distinct dopamine receptors exist. |
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