High-Yield Radiosynthesis and Preliminary In Vivo Evaluation of p-[18F]MPPF, a Fluoro Analog of WAY-100635

Bars, Didier Le; Lemaire, Christian; Ginovart, Nathalie; Plenevaux, Alain; Aerts, Joël; Brihaye, C.; Hassoun, Wadad; Leviel, Vincent; Mekhsian, P.; Weissmann, Dinah; Pujol, J.F.; Luxen, André; Comar, D.

doi:10.1016/s0969-8051(97)00229-1

Cited by 126 publications

(83 citation statements)

References 20 publications

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“…MPPF was obtained by nucleophilic fluoration of a nitro precursor (Le Bars et al, 1998), with a radiochemical yield of 20%-25% at the end of the synthesis and a mean specific activity of 4.41 Ϯ 1.86 Ci/mol. A bolus of [ 18 F]MPPF was injected (mean injected dose, 4.16 Ϯ 0.52 mCi).…”

Section: Pet Scanmentioning

confidence: 99%

Oxytocin and Serotonin Brain Mechanisms in the Nonhuman Primate

et al. 2017

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Oxytocin (OT) is increasingly studied for its therapeutic potential in psychiatric disorders, which are associated with the deregulation of several neurotransmission systems. Studies in rodents demonstrated that the interaction between OT and serotonin (5-HT) is critical for several aspects of social behavior. Using PET scan in humans, we have recently found that 5-HT 1A receptor (5-HT 1A R) function is modified after intranasal oxytocin intake. However, the underlying mechanism between OT and 5-HT remains unclear. To understand this interaction, we tested 3 male macaque monkeys using both

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Section: Pet Scanmentioning

confidence: 99%

Oxytocin and Serotonin Brain Mechanisms in the Nonhuman Primate

et al. 2017

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“…The 5-HT 1A -specific antagonists currently being used for PET investigation of the 5-HT 1A system include [ 11 C]WAY-100635 (Pike et al, 1996), [ 18 F]MPPF (Le Bars et al, 1998), [ 18 F]FCWAY (Carson et al, 2000), and [ 18 F]mefway (Saigal et al, 2006), all of which are structurally related to WAY-100635. In-vitro measurements of B max have been reported with [ 11 C]WAY-100635 and validated by comparison with its tritiated form (Hall et al, 1997), finding high levels of 5-HT 1A receptor expression throughout the frontal, temporal, parietal, and cingulate cortices with the highest receptor density in the hippocampus (including regions CA1, subiculum, and uncus).…”

Section: Introductionmentioning

confidence: 99%

Measurement of 5-HT_1A Receptor Density and in-vivo Binding Parameters of [¹⁸F]mefway in the Nonhuman Primate

Hillmer

Moirano

Ahlers

et al. 2012

J Cereb Blood Flow Metab

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The goal of this work was to characterize the in-vivo behavior of [ 18 F]mefway as a suitable positron emission tomography (PET) radiotracer for the assay of 5-hydroxytryptamine 1A (5-HT 1A ) receptor density (B max ). Six rhesus monkeys were studied using a multiple-injection (M-I) protocol consisting of three sequential bolus injections of [ 18 F]mefway. Injection times and amounts of unlabeled mefway were optimized for the precise measurement of B max and specific binding parameters k off and k on for estimation of apparent K D . The PET time series were acquired for 180 minutes with arterial sampling performed throughout. Compartmental analysis using the arterial input function was performed to obtain estimates for K 1 , k 2 , k off , B max , and K Dapp in the cerebral cortex and raphe nuclei (RN) using a model that accounted for nontracer doses of mefway. Averaged over subjects, highest binding was seen in the mesial temporal and dorsal anterior cingulate cortices with B max values of 42 ± 8 and 36 ± 8 pmol/mL, respectively, and lower values in the superior temporal cortex, RN, and parietal cortex of 24 ± 4, 19 ± 4, and 13 ± 2 pmol/mL, respectively. The K Dapp of mefway for the 5-HT 1A receptor sites was 4.3 ± 1.3 nmol/L. In conclusion, these results show that M-I [ 18 F]mefway PET experiments can be used for the in-vivo measurement of 5-HT 1A receptor density.

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“…However, Mass Spectrometry (MS) may solve this problem, being a more sensitive tool for qualitative analyses of radiopharmaceuticals [3][4][5]. [6,7], [ 18 F]FBWAY [8] and 18 F-mefway [9] have been reported in the literature. Production of p-[…”

Section: Introductionmentioning

confidence: 99%

“…18 F] MPPF from its inactive precursor and labelled side-products is challenging and complex radioHPLC methods are needed for the analysis/purification of the crude product [6,7,11].…”

Section: Introductionmentioning

confidence: 99%

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Assessment of labelled products with different radioanalytical methods: study on 18F-fluorination reaction of 4-[18F]fluoro-N-[2-[1-(2-methoxyphenyl)-1-piperazinyl]ethyl-N-2-pyridinyl-benzamide (p-[18F]MPPF)

Koivula

Laine

Lipponen

et al. 2010

J Radioanal Nucl Chem

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High-Yield Radiosynthesis and Preliminary In Vivo Evaluation of p-[18F]MPPF, a Fluoro Analog of WAY-100635

Cited by 126 publications

References 20 publications

Oxytocin and Serotonin Brain Mechanisms in the Nonhuman Primate

Oxytocin and Serotonin Brain Mechanisms in the Nonhuman Primate

Measurement of 5-HT_1A Receptor Density and in-vivo Binding Parameters of [¹⁸F]mefway in the Nonhuman Primate

Assessment of labelled products with different radioanalytical methods: study on 18F-fluorination reaction of 4-[18F]fluoro-N-[2-[1-(2-methoxyphenyl)-1-piperazinyl]ethyl-N-2-pyridinyl-benzamide (p-[18F]MPPF)

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High-Yield Radiosynthesis and Preliminary In Vivo Evaluation of p-[18F]MPPF, a Fluoro Analog of WAY-100635

Cited by 126 publications

References 20 publications

Oxytocin and Serotonin Brain Mechanisms in the Nonhuman Primate

Oxytocin and Serotonin Brain Mechanisms in the Nonhuman Primate

Measurement of 5-HT1A Receptor Density and in-vivo Binding Parameters of [18F]mefway in the Nonhuman Primate

Assessment of labelled products with different radioanalytical methods: study on 18F-fluorination reaction of 4-[18F]fluoro-N-[2-[1-(2-methoxyphenyl)-1-piperazinyl]ethyl-N-2-pyridinyl-benzamide (p-[18F]MPPF)

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Measurement of 5-HT_1A Receptor Density and in-vivo Binding Parameters of [¹⁸F]mefway in the Nonhuman Primate