title: 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.
authors.affiliation: Department of Chemistry, Indiana State University, 600 Chestnut Street, Science S35E, Terre Haute, IN 47809, USA.
authors.forename: Bradley A
authors.initials: BA
authors.lastname: Scates
authors.forename: Bethany L
authors.initials: BL
authors.lastname: Lashbrook
authors.forename: Benjamin C
authors.initials: BC
authors.lastname: Chastain
authors.forename: Kaoru
authors.initials: K
authors.lastname: Tominaga
authors.forename: Brandon T
authors.initials: BT
authors.lastname: Elliott
authors.forename: Nicholas J
authors.initials: NJ
authors.lastname: Theising
authors.forename: Thomas A
authors.initials: TA
authors.lastname: Baker
authors.forename: Richard W
authors.initials: RW
authors.lastname: Fitch
mesh_terms: D000818:Animals; D002460:Cell Line; D002540:Cerebral Cortex / Q000378:metabolism; D008024:Ligands; D011092:Polyethylene Glycols / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011725:Pyridines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011869:Radioligand Assay; D051381:Rats; D011978:Receptors, Nicotinic / Q000187:drug effects* / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D008024:Ligands; D011725:Pyridines; D011978:Receptors, Nicotinic; D011092:Polyethylene Glycols