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See detailA reduced extracellular serotonin level increases the 5-HT1A PET ligand F-18-MPPF binding in the rat hippocampus
Zimmer, L.; Rbah, L.; Giacomelli, Fabrice ULg et al

in Journal of Nuclear Medicine (2003), 44(9), 1495-1501

4,2'-(Methoxyphenyl)-1-[2'-(N-2"-pyridinyl)-p-fluorobenzamido]ethylpiperazine (F-18-MPPF) is a radiotracer used in clinical PET studies for the visualization of serotonin-1A (5-HT1A) receptors. In a ... [more ▼]

4,2'-(Methoxyphenyl)-1-[2'-(N-2"-pyridinyl)-p-fluorobenzamido]ethylpiperazine (F-18-MPPF) is a radiotracer used in clinical PET studies for the visualization of serotonin-1A (5-HT1A) receptors. In a previous study, we demonstrated that a rapid enhancement of extracellular serotonin concentrations influences F-18-MPPF-specific binding. Because endogenous serotonin is significantly decreased in some pathologies, the aim of this study was to determine whether F-18-MPPF is sensitive to depletion of this neurotransmitter. Methods: Using the beta-microprobe, an original beta(+)-sensitive intracerebral probe, and micro-dialysis, the effect of decreased serotonin on the specific binding of F-18-MPPF to 5-HT1A receptors was investigated in the hippocampus of the anesthetized rat. Extracellular serotonin was pharmacologically decreased in the hippocampus after a single injection of p-ethynylphenylalanine ([p-EPA] 5 mg/kg), a new tryptophan hydroxylase inhibitor. Results: Our results showed that the F-18-MPPF-specific binding was significantly enhanced after the decrease of extracellular serotonin. These results were confirmed by the F-18-MPPF distribution in cerebral tissues (hippocampus-to-cerebellum ratio) and by the decrease of the extracellular F-18-MPPF collected in hippocampal dialysates. Conclusion: This study further supports the view that 18F-MPPF binding potential is increased in the hippocampus if the endogenous serotonin is pharmacologically decreased after a p-EPA injection. This phenomenon will be an additional factor in the interpretation of the results from F-18-MPPF clinical PET studies. [less ▲]

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See detailModeling [F-18]MPPF positron emission tomography kinetics for the determination of 5-hydroxytryptamine(1A) receptor concentration with multiinjection
Costes, Nicolas; Merlet, I.; Zimmer, L. et al

in Journal of Cerebral Blood Flow & Metabolism (2002), 22

The selectivity of [F-18]MPPF (fluorine-18-labeled 4-(2'-methoxyphenyl)-1-[2'-(N-2"-pirydynyl)-p-fluorobenzamido]ethylpiperazine) for serotonergic 5-hydroxytryptamine(1A) (5-HT1A) receptors has been ... [more ▼]

The selectivity of [F-18]MPPF (fluorine-18-labeled 4-(2'-methoxyphenyl)-1-[2'-(N-2"-pirydynyl)-p-fluorobenzamido]ethylpiperazine) for serotonergic 5-hydroxytryptamine(1A) (5-HT1A) receptors has been established in animals and humans. The authors quantified the parameters of ligand-receptor exchanges using a double-injection protocol. After injection of a tracer and a coinjection dose of [F-18]MPPF, dynamic positron emission tomography (PET) data Were acquired during a 160-minute session in five healthy males. These PET and magnetic resonance imaging data were coregistered for anatomical identification. A three-compartment model was used to determine six parameters: F-v (vascular fraction). K-1, k(2) (plasma/free compartment exchange rate). k(off). k(on)/V-r (association and dissociation rate), B-max (receptor concentration), and to deduce K-d (apparent equilibrium dissociation rate). The model was fitted with regional PET kinetics and arterial input function corrected for metabolites. Analytical distribution volume and binding potential Were compared With indices generated by Logan-Patlak graphical analysis. The 5HT(1A) specificity for MPPF was evidenced. A B-max of 2.9 pmol/mL and a K-d of 2.8 nmol/L were found in hippocampal regions, K-d and distribution volume in the free compartment were regionally stable. and the Logan binding potential was linearly correlated to B-max. This study confirms the value of MPPF in the investigation of normal and pathologic systems involving the limbic network and 5-HT1A receptors. Standard values can be used for the simulation of simplified protocols. [less ▲]

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See detailModeling p-18FMPPF pet kinetics for the detremination of local 5-HT1A receptor concentration.
Costes, N.; Le Bars, D.; Merlet, I. et al

in Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine (2001), 42(S1), 209

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See detail5-HT1A Receptors visualization with p-[18F]MPPF in healthy volunteers.
Plenevaux, Alain ULg; Lemaire, Christian ULg; Salmon, Eric ULg et al

in Journal of Labelled Compounds & Radiopharmaceuticals (1999), 42

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See detailp-[18F]MPPF, a fluoro analog of WAY-100635 for visualisation of 5-HT1A receptors in cat.
Le Bars, D.; Ginovart, N.; Hassoun, W. et al

in Journal of Labelled Compounds & Radiopharmaceuticals (1999), 42

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See detail5-HT1A receptor distribution in the human brain: preliminary PET data with p-[18F]MPPF.
Fuchs, Sonia ULg; Plenevaux, Alain ULg; Degueldre, Christian ULg et al

in Society for Neuroscience / Abstracts (1999), 25

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See detailp-[18F]MPPF, 5-HT1A antagonist: comparison to [3H]8-OH-DPAT with autoradiography
Plenevaux, Alain ULg; Weissmann, D.; Lemaire, Christian ULg et al

in Society for Neuroscience / Abstracts (1999)

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 ... [more ▼]

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. [less ▲]

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See detailMicrowave improved synthesis of p-[18F]MPPF, 5-HT1A antagonist and PET sudies on cat brain.
Le Bars, D.; Ginovart, N.; Lemaire, Christian ULg et al

in Journal of Labelled Compounds & Radiopharmaceuticals (1997), 40

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See detailTissue distribution, autoradiography and metabolism in rats of p-[18F]MPPF: 5-HT1A antagonist.
Plenevaux, Alain ULg; Aerts, Joël ULg; Lemaire, Christian ULg et al

in Journal of Labelled Compounds & Radiopharmaceuticals (1997), 40

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See detailHigh yield radiosynthesis of p-[F-18]MPPF, 5-HT1A antagonist, and PET studies in cat brain.
Le Bars, D.; Lemaire, Christian ULg; Plenevaux, Alain ULg et al

in Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine (1997), 38

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See detailEvaluation of p-[F-18]MPPF, 5-HT1A antagonist, in rats: tissue distribution, autoradiography and metabolism.
Plenevaux, Alain ULg; Aerts, Joël ULg; Lemaire, Christian ULg et al

in Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine (1997), 38

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See detailSep Pak as alternative to rotary evaporators for radiopharmaceutical formulations.
Lemaire, Christian ULg; Plenevaux, Alain ULg; Del Fiore, G. et al

in Journal of Labelled Compounds & Radiopharmaceuticals (1995), 37

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