title: Dopamine receptor stimulating effects of chanoclavine analogues, tricyclic ergot alkaloids, in the brain.
abstract: The abilities of tricyclic ergot alkaloids, chanoclavine-I and its analogues, and bromocriptine to stimulate dopamine receptors in the brain were investigated. Receptor binding of 3H-spiperone has shown that bromocriptine exhibits clear affinity for this compound. The order of displacement potencies was bromocriptine much greater than ergometrine, KSU-1415 greater than chanoclavine-I, KSU-1118, KSU-1791. In the striatum of mice treated with an amino acid decarboxylase inhibitor, gamma-butyrolactone-induced DOPA accumulation was markedly inhibited by bromocriptine and KSU-1415, but not inhibited by chanoclavine-I. In mice with unilateral striatal 6-hydroxydopamine lesions, bromocriptine and KSU-1415 produced a long-lasting contralateral rotation that was suppressed by prior treatment with (+/-)-sulpiride. These results suggest that a tricyclic ergot alkaloid of the chanoclavine type stimulates D-2 receptors in the brain.
mesh_terms: D015107:4-Butyrolactone / Q000378:metabolism; D000818:Animals; D001667:Binding, Competitive / Q000187:drug effects; D001921:Brain / Q000187:drug effects / Q000378:metabolism*; D002396:Catechols / Q000378:metabolism; D003342:Corpus Striatum / Q000187:drug effects / Q000378:metabolism; D004295:Dihydroxyphenylalanine / Q000378:metabolism; D004873:Ergolines / Q000493:pharmacokinetics / Q000494:pharmacology*; D004876:Ergot Alkaloids / Q000494:pharmacology; D066298:In Vitro Techniques; D008297:Male; D051379:Mice; D051381:Rats; D011919:Rats, Inbred Strains; D011954:Receptors, Dopamine / Q000187:drug effects*; D012399:Rotation; D013134:Spiperone / Q000378:metabolism; D013239:Stereotyped Behavior / Q000187:drug effects; D013997:Time Factors
chemical_list: D002396:Catechols; D004873:Ergolines; D004876:Ergot Alkaloids; D011954:Receptors, Dopamine; C006959:chanoclavine; D013134:Spiperone; D004295:Dihydroxyphenylalanine; D015107:4-Butyrolactone