Inhibition of dopamine synthesis in striatal synaptosomes by lisuride: stereospecific reversal by (-)-sulpiride.
Lisuride, an ergot D2 dopamine receptor agonist inhibited dopamine synthesis in striatal synaptosomes concentration-dependently. Significant inhibition was detected at 10(-8) M, and the inhibition by 10(-4) M lisuride was 50%. The inhibitory effect of lisuride was reversed by more than 50% not only by the D1-D2 dopamine receptor blocker haloperidol but also by the D2 dopamine receptor blocker(-)-sulpiride. The effect of sulpiride was stereospecific. Under the same test conditions a similar inhibition of dopamine synthesis by apomorphine was reversed by the neuroleptics almost completely. The results suggest that there are dopamine autoreceptors controlling dopamine synthesis in synaptosomes and these receptors resemble D2 dopamine receptors according to the nomenclature of Kebabian and Calne (1979).
D000818:Animals; D003342:Corpus Striatum / Q000187:drug effects* / Q000378:metabolism; D004298:Dopamine / Q000096:biosynthesis*; D004873:Ergolines / Q000494:pharmacology*; D006220:Haloperidol / Q000494:pharmacology; D066298:In Vitro Techniques; D008090:Lisuride / Q000037:antagonists & inhibitors / Q000494:pharmacology*; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains; D013237:Stereoisomerism; D013469:Sulpiride / Q000494:pharmacology*; D013574:Synaptosomes / Q000187:drug effects*
D004873:Ergolines; D013469:Sulpiride; D008090:Lisuride; D006220:Haloperidol; D004298:Dopamine