Journal article

SELECTIVITY OF SOME ERGOT DERIVATIVES FOR 5-HT1 AND 5-HT2 RECEPTORS OF RAT CEREBRAL-CORTEX

PM BEART, D MCDONALD, M CINCOTTA, DJ DEVRIES, AL GUNDLACH

GENERAL PHARMACOLOGY | PERGAMON-ELSEVIER SCIENCE LTD | Published : 1986

Abstract

The affinities of several ergot derivatives for 5-HT1 and 5-HT2 receptors were evaluated using [3H]5-HT and [3H]mianserin, and membranes prepared from rat frontal cortex. CQ 32-084, which had a Ki value against the 5-HT2 component of [3H]mianserin binding of 9 nM, had little effect on [3H]5-HT binding and was selective for the 5-HT2 receptor. Lisuride and LY-158A also displayed preferential affinity for the 5-HT2 receptor. Dihydroergocryptine, CM 29-712, lergotrile and LY-062 were more selective for the 5-HT1 receptor. Bromocriptine showed little selectivity for either subtype. Overall, the ergot derivatives displayed markedly different affinities and selectivities for central 5-HT receptors..

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