Polyethylene Glycol-based Homologated Ligands for Nicotinic Acetylcholine Receptors

Overview

Journal Bioorg Med Chem

Specialties Biochemistry
Chemistry

Date 2008 Nov 14

PMID 19006672

Authors

Bradley A Scates

Bethany L Lashbrook

Benjamin C Chastain

Kaoru Tominaga

Brandon T Elliott

Nicholas J Theising

Thomas A Baker

Richard W Fitch

Affiliations

Soon will be listed here.

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.

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