Polyethylene glycol-based homologated ligands for nicotinic acetylcholine receptors

…, K Tominaga, BT Elliott, NJ Theising, TA Baker…

Index: Scates, Bradley A.; Lashbrook, Bethany L.; Chastain, Benjamin C.; Tominaga, Kaoru; Elliott, Brandon T.; Theising, Nicholas J.; Baker, Thomas A.; Fitch, Richard W. Bioorganic and Medicinal Chemistry, 2008 , vol. 16, # 24 p. 10295 - 10300

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Citation Number: 9

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 ...