[18F]MPPF as a tool for the in vivo imaging of 5-HT1A receptors in animal and human brain.
Serotonin (5-hydroxytryptamine, 5-HT) and its various receptors are involved in numerous CNS functions and psychiatric disorders. 5-HT(1A), the best-characterized subtype of currently known 5-HT receptors, is tightly implicated in the pathogenesis of depression, anxiety, epilepsy and eating disorders. It thus represents an important target for drug therapy. Specific radioligands and positron emission tomography (PET) allow for a quantitative imaging of brain 5-HT(1A) receptor distribution in living animals and humans. Recently, the selective 5-HT(1A) receptor antagonist, MPPF, has been successfully labeled with [(18)F]fluorine ([(18)F]MPPF), and an increasing number of academic and industry centres have used this radiotracer in preclinical and clinical studies. After a brief account of some of the structural, distributional and electrophysiological characteristics of brain 5-HT(1A) receptors, this review focuses on studies conducted with [(18)F]MPPF, with emphasis on preclinical results illustrating the actual and potential value of this PET radioligand for clinical research and drug development.
Aznavour
Nicolas
N
Laboratoire de Neuropharmacologie, Université Lyon 1, Lyon, France.
Zimmer
Luc
L
D000818:Animals; D001921:Brain / Q000000981:diagnostic imaging* / Q000378:metabolism*; D006801:Humans; D008958:Models, Molecular; D010879:Piperazines / Q000493:pharmacokinetics*; D049268:Positron-Emission Tomography; D011725:Pyridines / Q000493:pharmacokinetics*; D044263:Receptors, Serotonin, 5-HT1 / Q000378:metabolism*
D010879:Piperazines; D011725:Pyridines; D044263:Receptors, Serotonin, 5-HT1; C416325:4-(2'-methoxyphenyl)-1-(2'-(N-2'-pyridinyl)-p-(18F)fluorobenzamido )ethylpiperazine