Terguride, a mixed dopamine agonist-antagonist, in animal models of Parkinson's disease.
Terguride, an analogue of lisuride, decreased locomotor activity, produced cataplexy, and blocked apomorphine-induced stereotypic behavior. It did not induce stereotypies in rodents or emesis in dogs. However, in rats with unilateral 6-hydroxydopamine lesions of the substantia nigra, terguride produced contralateral rotation. Terguride bound to D-2 striatal dopamine receptors. Terguride has both agonist and antagonist actions at striatal dopamine receptors, but chronic administration did not produce behavioral supersensitivity. These pharmacologic properties differ from those of other antiparkinsonian agents; terguride may be effective for the chronic treatment of Parkinson's disease.
D000661:Amphetamine / Q000494:pharmacology; D000818:Animals; D001058:Apomorphine / Q000494:pharmacology; D001522:Behavior, Animal / Q000187:drug effects*; D001921:Brain / Q000378:metabolism; D004195:Disease Models, Animal; D004873:Ergolines / Q000494:pharmacology*; D007980:Levodopa / Q000494:pharmacology; D008090:Lisuride / Q000031:analogs & derivatives / Q000494:pharmacology* / Q000627:therapeutic use; D008297:Male; D009043:Motor Activity / Q000187:drug effects; D010300:Parkinson Disease / Q000188:drug therapy*; D051381:Rats; D011919:Rats, Inbred Strains; D011954:Receptors, Dopamine / Q000378:metabolism; D013239:Stereotyped Behavior / Q000187:drug effects
D004873:Ergolines; D011954:Receptors, Dopamine; C006208:dironyl; D007980:Levodopa; D000661:Amphetamine; D008090:Lisuride; D001058:Apomorphine