The high-affinity nAChR partial agonists varenicline and sazetidine-A exhibit reinforcing properties in rats.

@article{Paterson2010TheHN,
  title={The high-affinity nAChR partial agonists varenicline and sazetidine-A exhibit reinforcing properties in rats.},
  author={Neil E. Paterson and Wenzhong William Min and Adrian Hackett and David Lowe and Taleen Hanania and Barbara J. Caldarone and Afshin Ghavami},
  journal={Progress in neuro-psychopharmacology & biological psychiatry},
  year={2010},
  volume={34 8},
  pages={1455-64}
}
Varenicline (Chantix®, Champix®) is a nicotinic acetylcholine receptor (nAChR) partial agonist clinically approved for smoking cessation, yet its potential abuse liability properties have not been fully characterized. The nAChR ligand sazetidine-A has been reported as a selective full or partial agonist at α4β2* nAChR subtypes in in vitro studies. In the present studies, varenicline, sazetidine-A and nicotine exhibited inverted U-shaped dose-response functions under fixed-ratio (peak responding… CONTINUE READING
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