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3- N-(2-[ 18 F]Fluoroethyl)spiperone

3- N-(2-[ 18 F]Fluoroethyl)spiperone

Kam Leung

PMID: 20641672

Abstract:

Dopamine, a neurotransmitter, plays an important role in the mediation of movement, cognition, and emotion (1, 2). Dopamine shortage plays a role in various neuropsychiatric disorders, such as Parkinson's disease (PD), schizophrenia, autism, attention deficit hyperactivity disorder, and drug abuse. Two subtypes of dopamine receptors, D1 and D2, were well-characterized pharmacologically and biochemically (3). D2 dopamine receptors have been implicated in the pathophysiology of PD, Alzheimer's disease, and schizophrenia (4).
Serotonin (5-hydroxytryptamine, 5-HT) has diverse physiological roles as a neurotransmitter in the central nervous system (5). 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, obsessive-compulsive disorder, and schizophrenia (6, 7).
Spiperone and its analog, 3-N-(2-fluoroethyl)spiperone (FESP) are high-affinity D2 dopamine and 5-HT2 serotonin receptor antagonists, showing a low affinity for α1-adrenergic receptors and marginal binding to other receptors (8). 3-N-(2-[18F]Fluoroethyl)spiperone ([18F]FESP) has been studied as a positron emission tomography (PET) tracer for imaging D2 and 5HT2 receptor densities. It has also used as a reporter probe for dopamine D2 receptor in imaging transgene expression in rodents (9-11).

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP749020	Spiperone		749-02-0	Price

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