Varenicline, a new nicotinic ligand based on the structure of cytisine, has recently been approve... more Varenicline, a new nicotinic ligand based on the structure of cytisine, has recently been approved by the U.S. Food and Drug Administration for use as a smoking cessation aid. Varenicline has been shown to be a partial agonist of ␣42 receptors, and in equilibrium binding assays, it is highly selective for the ␣42 receptor. In this study, we have examined the functional activity of varenicline at a variety of rat neuronal nicotinic receptors expressed in Xenopus laevis oocytes and assayed under two-electrode voltage clamp. We also find that varenicline is a potent, partial agonist at ␣42 receptors, with an EC 50 of 2.3 Ϯ 0.3 M and an efficacy (relative to acetylcholine) of ABBREVIATIONS: nAChR, nicotinic acetylcholine receptor; ACh, acetylcholine.
Varenicline, a new nicotinic ligand based on the structure of cytisine, has recently been approve... more Varenicline, a new nicotinic ligand based on the structure of cytisine, has recently been approved by the U.S. Food and Drug Administration for use as a smoking cessation aid. Varenicline has been shown to be a partial agonist of ␣42 receptors, and in equilibrium binding assays, it is highly selective for the ␣42 receptor. In this study, we have examined the functional activity of varenicline at a variety of rat neuronal nicotinic receptors expressed in Xenopus laevis oocytes and assayed under two-electrode voltage clamp. We also find that varenicline is a potent, partial agonist at ␣42 receptors, with an EC 50 of 2.3 Ϯ 0.3 M and an efficacy (relative to acetylcholine) of ABBREVIATIONS: nAChR, nicotinic acetylcholine receptor; ACh, acetylcholine.
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Papers by Karla Avalos