Dopaminergic Ergots

Abstract

In recent years the ability of ergot derivatives to interact with dopamine receptors has attracted considerable interest. Bromocriptine was the first ergot derivative recognised as a potent, centrally acting dopaminomimetic drug and is now widely used in the treatment of Parkinson’s disease and endocrine disorders. Ergot derivatives also proved to be valuable tools in research. For instance, the sub-classification of dopamine receptors into D-1 and D-2 types has its origin in the observation that dopaminergic ergots such as bromocriptine or lergotrile mimic the inhibitory effect of dopamine on prolactin secretion but fail to stimulate adenylate cyclase (Kebabian and Calne,1979). Recently, new types of ergot derivatives have been described which exhibit various properties of dopamine receptor antagonists and which may expand the use of these compounds into the treatment of schizophrenia. All ergot derivatives have the tetracyclic ergolene moiety as a common structural element which, in turn, bears a structural relationship to serotonin and catecholamines. It is therefore not surprising that dopaminergic ergots interact not only with dopamine but also to a certain extent, with serotonin and α-adrenoceptors. This short overview describes some novel dopaminergic ergot derivatives and their possible therapeutic uses.