ORBi: Brabant Christian - Effects of the H(3) receptor inverse agonist thioperamide on cocaine-induced locomotion in mice: role of the histaminergic system and potential pharmacokinetic interactions.

Reference : Effects of the H(3) receptor inverse agonist thioperamide on cocaine-induced locomotion ...


	Document type :	Scientific journals : Article
	Discipline(s) :	Human health sciences : Pharmacy, pharmacology & toxicology Human health sciences : Psychiatry Social & behavioral sciences, psychology : Neurosciences & behavior
	To cite this reference:	http://hdl.handle.net/2268/6676

Title :	Effects of the H(3) receptor inverse agonist thioperamide on cocaine-induced locomotion in mice: role of the histaminergic system and potential pharmacokinetic interactions.
Language :	English
Author, co-author :	Brabant, Christian [Université de Liège - ULg > Département des sciences biomédicales et précliniques > Biochimie et physiologie humaine et pathologique >]
	Alleva, Livia [Université de Liège - ULg > Département des sciences cognitives > Neuroscience comportementale et psychopharmacologie expér. >]
	Grisar, Thierry [Centre Hospitalier Universitaire de Liège - CHU > > Neurologie Sart Tilman >]
	Quertemont, Etienne [Université de Liège - ULg > Département des sciences cognitives > Psychologie quantitative >]
	Lakaye, Bernard [Université de Liège - ULg > Département des sciences biomédicales et précliniques > Biochimie et physiologie humaine et pathologique >]
	Ohtsu, Hiroshi [Tohoku University > Department of Quantum Science and Energy Engineering > > >]
	Lin, Jian-Sheng [Université Claude Bernard - Lyon 1 - UCLB > Département de Médecine Expérimentale > > >]
	Jatlow, Peter [Yale University > Department of Laboratory Medicine > > >]
	Picciotto, Marina R [Yale University > Department of Psychiatry > > >]
	Tirelli, Ezio [Université de Liège - ULg > Département des sciences cognitives > Neuroscience comportementale et psychopharmacologie expér. >]
Publication date :	2009
Journal title :	Psychopharmacology
Publisher :	Springer Verlag
Volume :	202
Issue/season :	4
Pages :	673-87
Audience :	International
ISSN :	0033-3158
City :	Berlin
Country :	Germany
Keywords :	[en] Cocaine ; Histamine ; Thioperamide
	[fr] Immepip ; A-331440 ; H3 receptor ; Locomotion ; Knockout mouse
Abstract :	[en] RATIONALE: Previous studies have shown that intraperitoneal injections of thioperamide, an imidazole-based H(3) receptor inverse agonist that enhances histamine release in the brain, potentiate cocaine-induced hyperlocomotion. The present study examined the involvement of the histaminergic system in these effects of thioperamide in mice. MATERIALS AND METHODS: We investigated whether immepip, a selective H(3) agonist, could reverse the potentiating effects of thioperamide. Moreover, the non-imidazole H(3) inverse agonist A-331440 was tested on the locomotor effects of cocaine. Using high-performance liquid chromatography with ultraviolet detection, cocaine plasma concentrations were measured to study potential drug-drug interactions between thioperamide and cocaine. Finally, thioperamide was tested on the locomotor effects of cocaine in histamine-deficient knockout mice in order to determine the contribution of histamine to the modulating effects of thioperamide. RESULTS: Thioperamide potentiated cocaine-induced hyperlocomotion in normal mice, and to a higher extent, in histamine-deficient knockout mice. A-331440 only slightly affected the locomotor effects of cocaine. Immepip did not alter cocaine-induced hyperactivity but significantly reduced the potentiating actions of thioperamide on cocaine's effects. Finally, plasma cocaine concentrations were more elevated in mice treated with thioperamide than in mice that received cocaine alone. CONCLUSIONS: The present results indicate that histamine released by thioperamide through the blockade of H(3) autoreceptors is not involved in the ability of this compound to potentiate cocaine induced-hyperactivity. Our data suggest that thioperamide, at least at 10 mg/kg, increases cocaine-induced locomotion through the combination of pharmacokinetic effects and the blockade of H(3) receptors located on non-histaminergic neurons.
Research units :	Centre de Neurosciences Cognitives et Comportementales
Funders :	Fonds de la Recherche Scientifique (Communauté française de Belgique) - F.R.S.-FNRS ; National Institutes of Health - NIH
Target :	Researchers ; Professionals
Permalink :	http://hdl.handle.net/2268/6676
DOI :	10.1007/s00213-008-1345-y

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