Noncompetitive Functional Inhibition at Diverse, Human Nicotinic Acetylcholine Receptor Subtypes by Bupropion, Phencyclidine, and Ibogaine

摘要: Nicotinic acetylcholine receptors (nAChR) are diverse members of the neurotransmitter-gated ion channel superfamily and play critical roles in chemical signaling throughout nervous system. The present study establishes acute functional effects bupropion, phencyclidine, ibogaine on two human nAChR subtypes. Function muscle-type (alpha1 beta gamma delta) TE671/RD cells or ganglionic (alpha3 beta4 alpha5+/-beta2) SH-SY5Y neuroblastoma was measured with 86Rb+ efflux assays. Functional blockade is produced by each drugs low to intermediate micromolar range. insurmountable increasing agonist concentrations for these drugs, suggesting noncompetitive inhibition function. Based findings, we hypothesize that targets substances abuse agents used antiaddiction/smoking cessation strategies. We also heretofore underappreciated depression as clinically useful antidepressants.