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Chemical Compound Review:

AC1NS1RR 4-fluoro-N-[2-[4-(2- methoxyphenyl)piperazi...

Synonyms: [18F]FPWAY, [18F]FBWAY 1,3 N

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Psychiatry related information on p-[18F]MPPF

The human study showed a significant increase in [18F]MPPF binding in sleep compared to wakefulness in the whole brain and all regions of interest examined (temporal cortex, mesial temporal region and cingulate cortex) [1].
14 subjects with narcolepsy cataplexy underwent [18F]MPPF PET scans in wakefulness and in sleep [1].

High impact information on p-[18F]MPPF

Binding of the radioligand [18F]MPPF to 5HT1A receptors is sensitive to levels of endogenous serotonin [1].
Methylphenidate is thought to have little or no effect on serotonergic neurotransmission, and in order to confirm the absence of an effect on [18F]MPPF binding, a concurrent study was performed using a beta-microprobe technique to examine the effect of methylphenidate administration on [18F]MPPF binding in Sprague-Dawley rats [1].
Nine TLE patients and 53 control subjects were studied by PET using a 5-HT1A receptor antagonist ([18F]MPPF) [2].
Fenfluramine treatment resulted in a 30-fold increase in extracellular 5-HT levels in the ventral hippocampus and induced a significant reduction of [18F]MPPF binding in the frontal cortex, hypothalamus, amygdala, and hippocampus [3].
Influence of P-glycoprotein on brain uptake of [18F]MPPF in rats [4].

Anatomical context of p-[18F]MPPF

It was therefore concluded that the internalization of 5-HT1A autoreceptors accounted for the decreased binding in vivo of [18F]MPPF in the nucleus raphe dorsalis of rats treated with 8-OH-DPAT [5].
PET radioactivity curves with [18F]MPPF were very reproducible in anaesthetized cats, with the highest radioactivity uptakes recorded in the hippocampus, cingulate cortex, septum, infralimbic cortex and raphe nucleus, whereas the lowest were found in the cerebellum [6].
Following intravenous injection of p-[18F]MPPF, high accumulation of radioactivity was observed in the hippocampus and cerebral cortex [7].

Associations of p-[18F]MPPF with other chemical compounds

The binding potentials for [18F]MPPF were 4-6 times lower than those that have been reported for [carbonyl-1C]-(N-(2-(4-(2-methoxyphenyl)-1-piperazinyl)ethyl)-N-(2-pyrid yl) cyclohexane-carboxamide (WAY 100635), indicating that [18F]MPPF has a lower in vivo affinity for 5-HT1A receptors [8].
Both effects were blocked by pretreatment with the 5-HT1A receptor antagonist (N-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-N-(2-pyridinyl) cyclohexane-carboxamide) (1 mg/kg, i.p.). In brain sections of NRD and hippocampus, [18F]MPPF autoradiographic labeling did not differ between fluoxetine- and saline-treated rats [9].

Analytical, diagnostic and therapeutic context of p-[18F]MPPF

[18F]MPPF binding was assessed in conscious rats using ex vivo autoradiography [3].
METHODS: [15O]H2O perfusion scanning was performed before intravenous injection of [18F]MPPF to obtain anatomic information [8].
Plasma metabolites of [18F]MPPF were determined by high-performance liquid chromatography [8].
Animal experiments have shown that 4-(2'-methoxyphenyl)-1-[2'-(N-2'-pyridinyl)-p-[18F]fluorobenzamido ]ethylpiperazine ([18F]MPPF) may be suitable for 5-HT1A receptor imaging in humans [8].
The aim of this study was to determine if [18F]MPPF can be used for the quantitative analysis of 5-HT1A receptor densities in brain regions of healthy human volunteers [8].

References

Increased serotonin receptor availability in human sleep: evidence from an [18F]MPPF PET study in narcolepsy. Derry, C., Benjamin, C., Bladin, P., le Bars, D., Tochon-Danguy, H., Berkovic, S.F., Zimmer, L., Costes, N., Mulligan, R., Reutens, D. Neuroimage (2006) [Pubmed]
5-HT1A receptor binding and intracerebral activity in temporal lobe epilepsy: an [18F]MPPF-PET study. Merlet, I., Ostrowsky, K., Costes, N., Ryvlin, P., Isnard, J., Faillenot, I., Lavenne, F., Dufournel, D., Le Bars, D., Mauguière, F. Brain (2004) [Pubmed]
Effect of increased serotonin levels on [18F]MPPF binding in rat brain: fenfluramine vs the combination of citalopram and ketanserin. Udo de Haes, J.I., Cremers, T.I., Bosker, F.J., Postema, F., Tiemersma-Wegman, T.D., den Boer, J.A. Neuropsychopharmacology (2005) [Pubmed]
Influence of P-glycoprotein on brain uptake of [18F]MPPF in rats. Passchier, J., van Waarde, A., Doze, P., Elsinga, P.H., Vaalburg, W. Eur. J. Pharmacol. (2000) [Pubmed]
Toward brain imaging of serotonin 5-HT1A autoreceptor internalization. Zimmer, L., Riad, M., Rbah, L., Belkacem-Kahlouli, A., Le Bars, D., Renaud, B., Descarries, L. Neuroimage (2004) [Pubmed]
A comparison of in vivo and in vitro neuroimaging of 5-HT 1A receptor binding sites in the cat brain. Aznavour, N., Rbah, L., Léger, L., Buda, C., Sastre, J.P., Imhof, A., Charnay, Y., Zimmer, L. J. Chem. Neuroanat. (2006) [Pubmed]
High-yield radiosynthesis and preliminary in vivo evaluation of p-[18F]MPPF, a fluoro analog of WAY-100635. Le Bars, D., Lemaire, C., Ginovart, N., Plenevaux, A., Aerts, J., Brihaye, C., Hassoun, W., Leviel, V., Mekhsian, P., Weissmann, D., Pujol, J.F., Luxen, A., Comar, D. Nucl. Med. Biol. (1998) [Pubmed]
In vivo delineation of 5-HT1A receptors in human brain with [18F]MPPF. Passchier, J., van Waarde, A., Pieterman, R.M., Elsinga, P.H., Pruim, J., Hendrikse, H.N., Willemsen, A.T., Vaalburg, W. J. Nucl. Med. (2000) [Pubmed]
Acute treatment with the antidepressant fluoxetine internalizes 5-HT1A autoreceptors and reduces the in vivo binding of the PET radioligand [18F]MPPF in the nucleus raphe dorsalis of rat. Riad, M., Zimmer, L., Rbah, L., Watkins, K.C., Hamon, M., Descarries, L. J. Neurosci. (2004) [Pubmed]

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