Molecular Determinants for Competitive Inhibition of α4β2 Nicotinic Acetylcholine Receptors

Recent Developments in Novel Antidepressants Targeting α4β2-Nicotinic Acetylcholine Receptors

Nicotinic acetylcholine receptors (nAChRs) have been investigated for developing drugs that can potentially treat various central nervous system disorders. Considerable evidence supports the hypothesis that modulation of the cholinergic system through activation and/or desensitization/inactivation of nAChR holds promise for the development of new antidepressants. The introductory portion of thi...

A noncompetitive, sequential mechanism for inhibition of rat α4β2 neuronal nicotinic acetylcholine receptors by carbamate pesticides

Endogenous acetylcholine modulates impulsive action via α4β2 nicotinic acetylcholine receptors in rats

Title Endogenous acetylcholine modulates impulsive action via α4β2 nicotinic acetylcholine receptors in rats Author(s) Tsutsui-Kimura, Iku; Ohmura, Yu; Izumi, Takeshi; Yamaguchi, Taku; Yoshida, Takayuki; Yoshioka, Mitsuhiro Citation European Journal of Pharmacology, 641(2-3): 148-153 Issue Date 2010-09-01 DOI Doc URL http://hdl.handle.net/2115/43803 Right Type article (author version) Additiona...

Molecular Recognition of the Neurotransmitter Acetylcholine by an Acetylcholine Binding Protein Reveals Determinants of Binding to Nicotinic Acetylcholine Receptors

Despite extensive studies on nicotinic acetylcholine receptors (nAChRs) and homologues, details of acetylcholine binding are not completely resolved. Here, we report the crystal structure of acetylcholine bound to the receptor homologue acetylcholine binding protein from Lymnaea stagnalis. This is the first structure of acetylcholine in a binding pocket containing all five aromatic residues con...

Agonist and antagonist effects of tobacco-related nitrosamines on human α4β2 nicotinic acetylcholine receptors

Regulation of the "neuronal" nicotinic acetylcholine receptors (nAChRs) is implicated in both tobacco addiction and smoking-dependent tumor promotion. Some of these effects are caused by the tobacco-derived N-nitrosamines, which are carcinogenic compounds that avidly bind to nAChRs. However, the functional effects of these drugs on specific nAChR subtypes are largely unknown. By using patch-cla...