p-[18F]MPPF, 5-HT1A antagonist: comparison to [3H]8-OH-DPAT with autoradiography

Plenevaux, Alain; Weissmann, D.; Lemaire, Christian; Aerts, Joël; Comar, D.; Le Bars, D.; Pujol, J.-F.; Luxen, André

Reference : p-[18F]MPPF, 5-HT1A antagonist: comparison to [3H]8-OH-DPAT with autoradiography


	Document type :	Scientific congresses and symposiums : Paper published in a journal
	Discipline(s) :	Human health sciences : Radiology, nuclear medicine & imaging
	To cite this reference:	http://hdl.handle.net/2268/79993

Title :	p-[18F]MPPF, 5-HT1A antagonist: comparison to [3H]8-OH-DPAT with autoradiography
Language :	English
Author, co-author :	Plenevaux, Alain [Université de Liège - ULiège > > Centre de recherches du cyclotron >]
	Weissmann, D. [ > > ]
	Lemaire, Christian [Université de Liège - ULiège > > Centre de recherches du cyclotron >]
	Aerts, Joël [Université de Liège - ULiège > > Centre de recherches du cyclotron >]
	Comar, D. [ > > ]
	Le Bars, D. [ > > ]
	Pujol, J.-F. [ > > ]
	Luxen, André [Université de Liège - ULiège > Département de chimie (sciences) > Chimie organique de synthèse - Centre de recherches du cyclotron >]
Publication date :	1999
Journal title :	Society for Neuroscience / Abstracts
Special issue title :	Society for Neuroscience / Abstracts
Peer reviewed :	Yes
On invitation :	No
Audience :	International
Event name :	Society for Neuroscience, 29th annual meeting.
Event date :	23-28-10/1999
Event organizer :	Society for Neuroscience
Event place (city) :	Miami
Event country :	USA
Abstract :	[en] p-MPPF 4-(2’-methoxyphenyl)-1-[2’-[N-(2’’-pyridinyl)-p-fluorobenzamido] ethyl]piperazine is the para-fluorobenzoyl analog of the highly selective 5-HT1A antagonist WAY-100635. The one step procedure used to label p-MPPF with fluorine-18 (cyclotron produced positron emitter of 110 min half-life) leads to a radiopharmaceutical compound easily prepared on a large scale. The preliminary evaluations conducted in rats and cats are good reason to consider p-[18F]MPPF as an interesting reversible radioligand to study the 5-HT1A receptor family in humans with positron emission tomography (PET). In this paper we report a careful comparison between p-[18F]MPPF and [3H]8-OH-DPAT with autoradiography and quantitative densitometry in the same animal. All experiments were conducted in Sprague Dawley male rats. For p-[18F]MMPF, the results were obtained ex-vivo after an intravenous injection of high specific activity radioligand (0.8-1.5 Ci/µmol) in vigil (no anesthesia), free moving and unstressed animals. For the purpose, permanent cannulation of the posterior vena cava were realized at least four days in advance. The [3H]8-OH-DPAT results were obtained in vitro on adjacent coronal sections to the one used for the p-[18F]MPPF autoradiography. Quantitative densitometry was employed to compare the values obtained in relevant brain structures (frontal cortex, lateral septum, hippocampus, dorsal raphe, entorhinal cortex and cerebellum). The plot of the p-[18F]MPPF values obtained for each structure against the [3H]8-OH-DPAT results displayed a significant linear correlation. These results demonstrate that from a qualitative as well as quantitative point of view, the binding of p-[18F]MPPF is totally comparable to the one of [3H]8-OH-DPAT. Supported by grants from INSERM/CGRI and FNRS Belgium.
Research centres :	Centre de Recherches du Cyclotron - CRC
Funders :	Fonds de la Recherche Scientifique (Communauté française de Belgique) - F.R.S.-FNRS
Target :	Researchers ; Professionals ; Students
Permalink :	http://hdl.handle.net/2268/79993

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