The histamine autoreceptor is a short isoform of the H₃ receptor.

British Journal of Pharmacology
Florence GbahouJ-M Arrang

Abstract

BACKGROUND AND PURPOSE The histamine H(3) receptor was identified as the autoreceptor of brain histaminergic neurons. After its cloning, functional H(3) receptor isoforms generated by a deletion in the third intracellular loop were found in the brain. Here, we determined if this autoreceptor was the long or the short isoform. EXPERIMENTAL APPROACH We hypothesized that the deletion would affect H(3) receptor stereoselectivity. The effects of the enantiomers of two chiral ligands, N(α)-methyl-α-chloromethylhistamine (N(α) Me-αClMeHA) and sopromidine, were investigated on cAMP formation at the H(3(445)) and H(3(413)) receptor isoforms, common to all species. They were further compared with their effects at autoreceptors. They were also compared on [(35)S]GTPγ[S] binding to membranes of rat cerebral cortex, striatum and hypothalamus, the richest area in autoreceptors. KEY RESULTS The stereoselectivity of N(α) Me-αClMeHA enantiomers as agonists was similar at the H(3(413)) receptor isoform and autoreceptors, but lower at the long isoform. While (S) sopromidine did not discriminate between the isoforms, (R) sopromidine was an antagonist at the H(3(413)) receptor isoform and autoreceptors, but a full agonist at the long isoform. In ra...Continue Reading

References

Oct 29, 1985·European Journal of Pharmacology·J M ArrangW Schunack
Apr 23, 1985·European Journal of Pharmacology·J M ArrangJ C Schwartz
May 14, 1987·Nature·J M ArrangJ C Schwartz
Mar 31, 1995·The Journal of Biological Chemistry·J GuiramandE Borrelli
Jan 1, 1994·Fundamental & Clinical Pharmacology·E SchlickerM Göthert
Jun 24, 1998·Proceedings of the National Academy of Sciences of the United States of America·Z U KhanP S Goldman-Rakic
Sep 8, 2000·Neuroreport·S Cassar
Nov 9, 2000·The European Journal of Neuroscience·O V AnichtchikP Panula
Feb 13, 2001·Biochemical and Biophysical Research Communications·S MorissetJ M Arrang
Feb 24, 2001·Neuroreport·J Tardivel-LacombeJ M Arrang
Oct 20, 2001·Behavioural Brain Research·D R StevensH L Haas
Oct 20, 2001·Behavioural Brain Research·C Kamei
Oct 24, 2002·European Journal of Pharmacology·Birgitte S WulffKarin Rimvall
Nov 15, 2002·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·Diego CentonzePaolo Calabresi
Mar 26, 2003·Proceedings of the National Academy of Sciences of the United States of America·Niklas LindgrenGilberto Fisone
Sep 10, 2003·Proceedings of the National Academy of Sciences of the United States of America·Florence GbahouJean-Michel Arrang
Oct 11, 2003·Life Sciences·Arthur A HancockBetty Bei Yao
Sep 3, 2004·Journal of Neurochemistry·Agnès RouleauJean-Michel Arrang
Oct 6, 2004·Expert Opinion on Investigational Drugs·Arthur A Hancock, Gerard B Fox
Nov 9, 2004·Trends in Pharmacological Sciences·Maria Beatrice PassaniPatrizio Blandina
Jan 25, 2005·Nature Reviews. Drug Discovery·Rob LeursIwan J P de Esch
Dec 27, 2005·Drug Discovery Today·Sylvain CelanireIwan J P de Esch
Jan 18, 2006·Neuropharmacology·Claudia JompheLouis-Eric Trudeau
Jan 25, 2006·British Journal of Pharmacology·Florence GbahouJean-Michel Arrang
Mar 28, 2006·Molecular Interventions·Timothy A EsbenshadeMarlon D Cowart
Jun 19, 2007·Trends in Pharmacological Sciences·Jean-Michel ArrangFlorence Gbahou
Sep 5, 2007·Journal of Neurochemistry·Irit Itzhaki Van-HamPaul R Albert

❮ Previous
Next ❯

Citations

May 31, 2015·Neuropharmacology·Armin ZlomuzicaEkrem Dere
Mar 17, 2015·Trends in Pharmacological Sciences·Salomon Z Langer
Mar 19, 2014·Trends in Neurosciences·Bart A Ellenbroek, Bibinaz Ghiabi
Oct 19, 2016·Molecular Pharmacology·Gustavo Nieto-AlamillaJosé-Antonio Arias-Montaño
Mar 21, 2018·Journal of Receptor and Signal Transduction Research·Gustavo Nieto-AlamillaJosé-Antonio Arias-Montaño
Oct 21, 2018·British Journal of Pharmacology·Ekaterini Tiligada, Madeleine Ennis
Nov 20, 2016·Molecular Pharmacology·Darren M RiddyChristopher J Langmead
Jul 5, 2019·CNS & Neurological Disorders Drug Targets·Néstor F DíazAnayansi Molina-Hernández
Mar 16, 2013·British Journal of Pharmacology·K KarlstedtP Panula
Oct 11, 2020·Scientific Reports·Leonardo David Herrera-ZúñigaRachid C Maroun

❮ Previous
Next ❯

Related Concepts

Related Feeds

Basal Ganglia

Basal Ganglia are a group of subcortical nuclei in the brain associated with control of voluntary motor movements, procedural and habit learning, emotion, and cognition. Here is the latest research.