Nicotinic receptor partial agonist

Caggiula AR, Donny EC, Chaudhri N, Perkins KA, Evans-Martin EF, Sved AF (2002) Importance of nonpharmacological factors in nicotine self-administration. Physiol Behav 77 683-687 Cahill K, Stead LF, Lancaster T (2007) Nicotine receptor partial agonists for smoking cessation. 

Varenicline is a selective nicotine receptor partial agonist that is used in smoking cessation. It is started 1-2 weeks before target stop date. It may cause gastrointestinal disturbances, dry mouth, taste disturbance and, less commonly, aphthous stomatitis. 

Varenicline is the first approved nicotinic receptor partial agonist. In this respect, it differs from other smoking cessation aids, such as the nicotinic antagonist, bupropion and nicotine replacement therapies. In May 2006, it was approved for sale in the United States. Varenicline increased the odds of successful long-term smoking cessation approximately threefold compared with pharmacologically unassisted quit attempts. In trials reported so far, more participants quit successfully with varenicline than with bupropion (see Cahill et al., 2007). 

Cahill K, Stead LF, Lancaster T. Nicotine receptor partial agonists for smoking cessation. Cochrane Database Syst Rev 2007. 

Although not an antidepressant also varenicline can be mentioned here. It is the first nicotinic receptor partial agonist approved to treat smoking addiction. As a partial agonist, it both reduces cravings for and decreases the pleasurable effects of cigarettes and other tobacco products. 

Varenicline (Chantix) An oc4p2 Nicotinic Receptor Partial Agonist... 

A series of pyridyl ethers, typified by (81) and (82), exhibited high binding affinity at cytisine rat forebrain sites (cytisine is a nicotinic receptor partial agonist), but only moderate affinity at H-epibatidine sites (109, 130). 

Coe, J.W. Brooks, P.R. Vetelino, M.G., et al. Varenicline a novel, potent, and a4 32 selective nicotinic receptor partial agonist for smoking cessation. J. Med. Chem. 2005, 48, 3A1A-3A11. 

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