Varenicline Is a Partial Agonist at α4β2 and a Full Agonist at α7 Neuronal Nicotinic Receptors

  title={Varenicline Is a Partial Agonist at $\alpha$4$\beta$2 and a Full Agonist at $\alpha$7 Neuronal Nicotinic Receptors},
  author={Karla B. Mihalak and F. Ivy Carroll and Charles W. Luetje},
  journal={Molecular Pharmacology},
  pages={801 - 805}
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 α4β2 receptors, and in equilibrium binding assays, it is highly selective for the α4β2 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… 

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