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Polyethylene glycol-based homologated ligands for nicotinic acetylcholine receptors.


ABSTRACT: A homologous series of polyethylene glycol (PEG) monomethyl ethers were conjugated with three ligand series for nicotinic acetylcholine receptors. Conjugates of acetylaminocholine, the cyclic analog 1-acetyl-4,4-dimethylpiperazinium, and pyridyl ether A-84543 were prepared. Each series was found to retain significant affinity at nicotinic receptors in rat cerebral cortex with tethers of up to six PEG units. Such compounds are hydrophilic ligands which may serve as models for fluorescent/affinity probes and multivalent ligands for nAChR.

SUBMITTER: Scates BA 

PROVIDER: S-EPMC2903455 | biostudies-literature | 2008 Dec

REPOSITORIES: biostudies-literature

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Polyethylene glycol-based homologated ligands for nicotinic acetylcholine receptors.

Scates Bradley A BA   Lashbrook Bethany L BL   Chastain Benjamin C BC   Tominaga Kaoru K   Elliott Brandon T BT   Theising Nicholas J NJ   Baker Thomas A TA   Fitch Richard W RW  

Bioorganic & medicinal chemistry 20081101 24


A homologous series of polyethylene glycol (PEG) monomethyl ethers were conjugated with three ligand series for nicotinic acetylcholine receptors. Conjugates of acetylaminocholine, the cyclic analog 1-acetyl-4,4-dimethylpiperazinium, and pyridyl ether A-84543 were prepared. Each series was found to retain significant affinity at nicotinic receptors in rat cerebral cortex with tethers of up to six PEG units. Such compounds are hydrophilic ligands which may serve as models for fluorescent/affinity  ...[more]

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