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6-[ 18 F]Fluoro-3-[2(S)-2-azetidinylmethoxy]pyridine

6-[ 18 F]Fluoro-3-[2(S)-2-azetidinylmethoxy]pyridine

Kam Leung

PMID: 20641785

Abstract:

Neuronal nicotinic cholinergic receptors (nAChRs) are a heterogeneous family of ligand-gated ion channels expressed in the central nervous system, where their activation by acetylcholine and nicotine always causes a rapid increase in cellular permeability to ions, such as Na+ and Ca2+ (1-3). Nicotinic receptors exist as pentamers (homomeric or heteromeric) in various brain regions and ganglia. There are nine subtypes of ligand-binding α (α2-α10) and four subtypes of structural β (β2-β5). nAChRs have been demonstrated to be involved in cognitive processes such as learning and memory and control of movement in normal subjects. Dysfunction of nAChR has been implicated to a number of human diseases such as schizophrenia, Huntington's disease, Alzheimer's disease (AD) and Parkinson's disease. nAChRs also play a significant role in nicotine addiction and related health problems associated with tobacco smoking.
3-[2(S)-2-azetidinylmethoxy]pyridine (A-85380) is a highly potent and selective α4β2 nAChR agonist with subnanomolar affinity (4, 5). A-85380 has been labeled as 6-[18F]Fluoro-3-[2(S)-2-azetidinylmethoxy]pyridine (6-[18F]fluoro-A-85380) (6-8). 6-[18F]fluoro-A-85380 (6-[18F]FA) is being developed as a PET agent for the non-invasive study of nAChR in the brain.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP5746861-B	Nicotine Related Compound F		5746-86-1	Price

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