Polyethylene glycol-based homologated ligands for nicotinic acetylcholine receptors.
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.
Scates
Bradley A
BA
Department of Chemistry, Indiana State University, 600 Chestnut Street, Science S35E, Terre Haute, IN 47809, USA.
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
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
D008024:Ligands; D011725:Pyridines; D011978:Receptors, Nicotinic; D011092:Polyethylene Glycols