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• W2146837512 endingPage "1189" @default.
• W2146837512 startingPage "1179" @default.
• W2146837512 abstract "D(2)-like dopamine receptors mediate functional changes via activation of inhibitory G proteins, including those that affect adenylate cyclase activity, and potassium and calcium channels. Although it is assumed that the binding of a drug to a single isoform of a D(2)-like receptor will cause similar changes in all receptor-mediated functions, it has been demonstrated in brain that the dopamine agonists dihydrexidine (DHX) and N-n-propyl-DHX are functionally selective. The current study explores the underlying mechanism using transfected MN9D cells and D(2)-producing anterior pituitary lactotrophs. Both dopamine and DHX inhibited adenylate cyclase activity in a concentration-dependent manner in both systems, effects blocked by D(2), but not D(1), antagonists. In the MN9D cells, quinpirole and R-(-)-N-propylnorapomorphine (NPA) also inhibited the K(+)-stimulated release of [(3)H]dopamine in a concentration-responsive, antagonist-reversible manner. Conversely, neither DHX, nor its analogs, inhibited K(+)-stimulated [(3)H]dopamine release, although they antagonized the effects of quinpirole. S-(+)-NPA actually had the reverse functional selectivity profile from DHX (i.e., it was a full agonist at D(2L) receptors coupled to inhibition of dopamine release, but a weak partial agonist at D(2L) receptor-mediated inhibition of adenylate cyclase). In lactotrophs, DHX had little intrinsic activity at D(2) receptors coupled to G protein-coupled inwardly rectifying potassium channels, and actually antagonized the effects of dopamine at these D(2) receptors. Together, these findings provide compelling evidence for agonist-induced functional selectivity with the D(2L) receptor. Although the underlying molecular mechanism is controversial (e.g., conformational induction versus drug-active state selection), such data are irreconcilable with the widely held view that drugs have intrinsic efficacy." @default.
• W2146837512 created "2016-06-24" @default.
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• W2146837512 date "2002-06-01" @default.
• W2146837512 modified "2023-09-27" @default.
• W2146837512 title "Functional Selectivity of Dopamine Receptor Agonists. II. Actions of Dihydrexidine in D_2LReceptor-Transfected MN9D Cells and Pituitary Lactotrophs" @default.
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• W2146837512 doi "https://doi.org/10.1124/jpet.301.3.1179" @default.
• W2146837512 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/12023553" @default.
• W2146837512 hasPublicationYear "2002" @default.
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