PMID: 12023553May 23, 2002Paper

Functional selectivity of dopamine receptor agonists. II. Actions of dihydrexidine in D2L receptor-transfected MN9D cells and pituitary lactotrophs

The Journal of Pharmacology and Experimental Therapeutics
Jason D KiltsR B Mailman

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 inhib...Continue Reading

References

Dec 29, 1976·Naunyn-Schmiedeberg's Archives of Pharmacology·J R Walters, R H Roth
Mar 14, 1977·Naunyn-Schmiedeberg's Archives of Pharmacology·G K Aghajanian, B S Bunney
Aug 1, 1991·British Journal of Pharmacology·D F SchoorsA G Dupont
May 10, 1991·Science·M I SimonN Gautam
Jul 1, 1989·Physiological Reviews·K StarkeH Kilbinger
Jul 4, 1989·European Journal of Pharmacology·T W LovenbergR B Mailman
Feb 1, 1989·Trends in Pharmacological Sciences·L Vallar, J Meldolesi
Dec 22, 1988·Nature·J R BunzowO Civelli
Dec 1, 1994·Trends in Neurosciences·B Hille
Jun 1, 1995·Trends in Pharmacological Sciences·T Kenakin
Jul 1, 1995·Trends in Pharmacological Sciences·T Kenakin
Mar 31, 1995·The Journal of Biological Chemistry·J GuiramandE Borrelli
Jan 1, 1996·Annual Review of Pharmacology and Toxicology·R K SunaharaA G Gilman
Jan 1, 1996·Neuropharmacology·M JaberM G Caron
Nov 14, 1997·Trends in Pharmacological Sciences·P LeffK McKechnie
Jan 16, 1998·Cellular Signalling·N Dascal
May 23, 1998·Annual Review of Pharmacology and Toxicology·R J Miller
Jan 16, 1999·Molecular and Cellular Neurosciences·E V KuzhikandathilG S Oxford
May 18, 1999·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·C P LawlerR B Mailman
May 23, 2002·The Journal of Pharmacology and Experimental Therapeutics·David M MottolaRichard B Mailman

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Citations

Feb 7, 2008·Naunyn-Schmiedeberg's Archives of Pharmacology·Frederick J Ehlert
May 2, 2012·Pharmaceutical Research·E V Kuzhikandathil, S Kortagere
Feb 6, 2004·Pharmacology & Therapeutics·David E Nichols
Jun 20, 2012·Journal of Medicinal Chemistry·Maria FindeisenAnnette G Beck-Sickinger
Dec 17, 2009·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·Richard B Mailman, Vishakantha Murthy
Feb 16, 2013·Nature Reviews. Drug Discovery·Terry Kenakin, Arthur Christopoulos
Mar 24, 2006·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·Jonathan D UrbanRichard B Mailman
Oct 26, 2011·Proceedings of the National Academy of Sciences of the United States of America·John A AllenJian Jin
Oct 28, 2008·Molecular Pharmacology·Li ZhangDavid R Manning
Mar 13, 2009·American Journal of Physiology. Regulatory, Integrative and Comparative Physiology·Peter M Lalley
Jul 31, 2014·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·Daniel R RosellLarry J Siever
Jul 26, 2011·Nature Chemical Biology·Eneko UrizarJonathan A Javitch
Jun 2, 2012·Expert Opinion on Drug Discovery·Wayne StallaertMichel Bouvier
Mar 8, 2016·Biological Psychiatry·Amy F T ArnstenRichard B Mailman
Dec 25, 2010·Trends in Molecular Medicine·Erin J WhalenRobert J Lefkowitz
Nov 6, 2004·Neuropharmacology·Sarah A Nickolls, Philip G Strange
May 15, 2015·Saudi Pharmaceutical Journal : SPJ : the Official Publication of the Saudi Pharmaceutical Society·Abdelaziz Ghanemi
Aug 30, 2011·Progress in Neuro-psychopharmacology & Biological Psychiatry·Beryl KoenerEmmanuel Hermans
Jul 17, 2007·Trends in Pharmacological Sciences·Richard B Mailman
Sep 24, 2008·Handbook of Clinical Neurology·Richard B Mailman, Xuemei Huang
Nov 15, 2017·Scientific Reports·Javier BurgueñoJesús Giraldo
May 10, 2005·The Journal of Biological Chemistry·Joseph N McLaughlinHeidi E Hamm
Jun 5, 2003·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·David A ShapiroRichard Mailman
Jan 20, 2018·Molecular Pharmacology·Terry Kenakin
Jul 4, 2015·Molecular Pharmacology·Terry Kenakin
Jun 29, 2006·The Journal of Pharmacology and Experimental Therapeutics·Jonathan D UrbanRichard B Mailman
May 23, 2002·The Journal of Pharmacology and Experimental Therapeutics·David M MottolaRichard B Mailman
Oct 20, 2004·CNS Drug Reviews·Peter SalmiBjörn Kull
Apr 27, 2019·Frontiers in Pharmacology·UNKNOWN Frontiers Production Office
Dec 14, 2018·Frontiers in Pharmacology·Caitlin R M OyagawaNatasha Lillia Grimsey
Dec 7, 2020·European Journal of Pharmacology·Richard B MailmanXuemei Huang

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