a-84543 and epibatidine

a-84543 has been researched along with epibatidine* in 1 studies

Other Studies

1 other study(ies) available for a-84543 and epibatidine

ArticleYear
Novel pyridyl ring C5 substituted analogues of epibatidine and 3-(1-methyl-2(S)-pyrrolidinylmethoxy)pyridine (A-84543) as highly selective agents for neuronal nicotinic acetylcholine receptors containing beta2 subunits.
    Journal of medicinal chemistry, 2005, Mar-24, Volume: 48, Issue:6

    Introduction of a hydrophobic or hydrogen-bonding alkynyl group into the C5 position of the pyridyl ring of epibatidine and A-84543 significantly increased the selectivity for neuronal nicotinic acetylcholine receptors (nAChRs) containing beta2 subunits over nAChRs containing beta4 subunits (K(i) ratio up to 92000-fold). Our data indicate that the extracellular domains of the nAChRs are sufficiently different to allow for the design of novel ligands with high affinity and selectivity for the nAChR subtypes.

    Topics: Animals; Binding Sites; Bridged Bicyclo Compounds, Heterocyclic; Ligands; Models, Molecular; Neurons; Protein Subunits; Pyridines; Pyrrolidines; Rats; Receptors, Nicotinic

2005