- Polyethylene glycol-based homologated ligands for nicotinic acetylcholine receptors
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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.,Lashbrook, Bethany L.,Chastain, Benjamin C.,Tominaga, Kaoru,Elliott, Brandon T.,Theising, Nicholas J.,Baker, Thomas A.,Fitch, Richard W.
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supporting information; experimental part
p. 10295 - 10300
(2009/04/12)
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- RAPID REDUCTIVE-CARBOXYLATION OF SECONDARY AMINES. ONE POT SYNTHESIS OF TERTIARY N-METHYLATED AMINES
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Various tertiary N-methylated amines were synthesized by using a new reductive-carboxylation approach.Secondary amines, on carboxylation with carbon dioxide under moderate reaction conditions, afforded their corresponding carbamate esters, which, on in situ lithium aluminum hydride reduction, gave desired tertiary N-methylated amines in high yield.
- Ram, Siya,Ehrenkaufer, Richard E.
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p. 5367 - 5370
(2007/10/02)
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