Pharmacological characterisation of the histamine H3 receptor in the rat hippocampus

Brain Research
A Alves-RodriguesR Leurs

Abstract

The purpose of this report was to pharmacologically characterise the histamine H3 in the rat hippocampus using radioligand binding studies with the H3 receptor antagonist [125I]iodophenpropit and the H3 receptor mediated inhibition of [3H]noradrenaline release. A dissociation constant of 0.33 nM and a maximal number of binding sites of 125 fmol/mg protein were found for [125I]iodophenpropit. Competition studies showed stereoselectivity for the (R) and (S) enantiomers of alpha-methylhistamine and 10 microM of GTPgammaS shifted the curve of (R)-alpha-methylhistamine rightwards. Up to 1 microM, (R)-alpha-methylhistamine displaced only 30% whereas the tested H3-antagonists displaced 50-60% of the total [125I]iodophenpropit bound. This indicates the presence of an additional non-H3 receptor binding site(s) for [125I]iodophenpropit in the rat hippocampus. This secondary site shows low affinity for H3 agonists, but high affinity for the tested H3 antagonists. Electrically evoked [3H]acetylcholine release was shown in slices of rat hippocampus. No H3 receptor modulation of [3H]acetylcholine release from hippocampal slices was detectable. However, H3 receptor activation inhibited 42% of the electrically-evoked [3H]noradrenaline release ...Continue Reading

References

Jan 1, 1990·Neuroscience·P PanulaE Kotilainen
Jul 1, 1988·Journal of Neurochemistry·J M ArrangJ C Schwartz
Dec 1, 1989·Naunyn-Schmiedeberg's Archives of Pharmacology·E SchlickerM Göthert
Jun 19, 1987·European Journal of Pharmacology·J F Van der WerfH Timmerman
May 1, 1988·Naunyn-Schmiedeberg's Archives of Pharmacology·E SchlickerM Göthert
Jun 1, 1985·Neuroscience·J M ArrangJ C Schwartz
Sep 1, 1980·Analytical Biochemistry·P J Munson, D Rodbard
Apr 1, 1995·British Journal of Pharmacology·A A RodriguesG D Prell
Apr 1, 1995·British Journal of Pharmacology·J M ArrangJ C Schwartz
Jan 23, 1995·Behavioural Brain Research·H L HaasI N Sharonova
Jan 1, 1994·Fundamental & Clinical Pharmacology·E SchlickerM Göthert
Jan 1, 1993·Journal of Neural Transmission. General Section·E SchlickerM Göthert
Jan 25, 1996·European Journal of Pharmacology·E A Clark, S J Hill
Mar 1, 1997·Inflammation Research : Official Journal of the European Histamine Research Society ... [et Al.]·M GiorgettiP Blandina

❮ Previous
Next ❯

Citations

Jun 29, 2011·Cellular and Molecular Neurobiology·Aisa ChepkovaOlga A Sergeeva
Apr 13, 2004·Journal of Cardiovascular Pharmacology·Satoshi YamamotoYasuo Matsumura
Jun 23, 2004·European Journal of Biochemistry·Venkata R P RatnalaWillem J DeGrip
Nov 9, 2004·Trends in Pharmacological Sciences·Maria Beatrice PassaniPatrizio Blandina
Nov 30, 2006·Biochemical Pharmacology·P BonaventureT Lovenberg
Oct 6, 2004·Expert Opinion on Investigational Drugs·Arthur A Hancock, Gerard B Fox
Jan 13, 2015·Bioorganic & Medicinal Chemistry·Zhongli GaoPascal G George
Oct 19, 2016·Molecular Pharmacology·Gustavo Nieto-AlamillaJosé-Antonio Arias-Montaño
May 14, 2008·The Journal of Pharmacology and Experimental Therapeutics·E DavenasJ M Arrang
Apr 11, 2001·American Journal of Physiology. Regulatory, Integrative and Comparative Physiology·T YamasakiY Matsumura

❮ Previous
Next ❯

Related Concepts

Related Feeds

Basal Forebrain- Circuits

Basal forebrain is a region in the brain important for production of acetylcholine and is the major cholinergic output of the CNS. Discover the latest research on circuits in the basal forebrain here.

© 2022 Meta ULC. All rights reserved