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Leung K1.


Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004-2013.
2012 Jul 20 [updated 2012 Nov 01].

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National Center for Biotechnology Information, NLM, NIH


5-Hydroxytryptamine (5-HT), commonly known as serotonin, has diverse physiological roles as a neurotransmitter in the central nervous system (1). 5-HT is involved in regulation and modulation of sleep, affective and personality behaviors, and pain. It also is a regulator of smooth muscle function and platelet aggregation. The brain cortical 5-HT system has been implicated in several neuropsychiatric disorders, including major depression, anxiety, schizophrenia, and obsessive-compulsive disorder (2, 3). The effects of 5-HT are mediated by as many as seven classes of receptor populations (5-HT1 to 5-HT7), many of which include several subtypes (4). There are five receptor subtypes within the G-protein–coupled 5-HT1 receptor family: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, and 5-HT1F. 5-HT7 receptors are abundantly present in the hippocampus, thalamus, and hypothalamus; low densities are observed in the cortex and amygdala (5-7). 5-HT7 receptors are involved in the mediation of emotion and the function of the hypothalamus. 5-HT7 receptors are implicated in anxiety, depression, hallucinogenic behavior, circadian rhythms and sleep, memory, epilepsy, and pain. Thus, there is a need for selective ligands to investigate the pharmacological role of 5-HT7 receptors. 1-(2-{(2R)-1-[(2-[18F]Fluorophenyl)sulfonyl]pyrrolidin-2-yl}ethyl)-4-methylpiperidine ([18F]-2FP3) was evaluated as a positron emission tomography (PET) probe for 5-HT7 receptors because the unlabeled 2FP3 was found to be a selective 5-HT7 antagonist with nanomolar affinity for the 5-HT7 receptor.

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