ChemInform Abstract: Novel 3‐Pyridyl Ethers with Subnanomolar Affinity for Central Neuronal Nicotinic Acetylcholine Receptors (nAChR′s).

Abstract

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The novel hybrid agonist HyNDA-1 targets the D3R-nAChR heteromeric complex in dopaminergic neurons

“…With these criteria in mind, we selected the nAChR and D3R agonist building blocks after an accurate analysis of the literature. The choice of A-84543 [33] was further supported by studies demonstrating the ability of the C5 position of the pyridyl moiety of this α4β2 nAChR agonist to tolerate sterically bulky substituents without losing binding affinity or even increasing selectivity for the α4β2 subtype [34]. In particular, a set of A-84543 analogues containing hydrogen-bonding alkynyl substituents at the C5 position showed an exceptionally high selectivity for nAChRs containing β2 subunits over receptors containing β4 subunits [35] (Fig.…”

“…Ropinirole, dihydro-β-erythroidine hydrobromide and quinpirole were purchased from Tocris. 3-(1-Methyl-2(S) pyrrolidinyl)methoxy)pyridine fumarate (A-84543) was prepared according to a published procedure [33]; all analytical data of the synthesized compound matched those reported in the literature.…”