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The contribution of agonist and antagonist activities of α4β2* nAChR ligands to smoking cessation efficacy: a quantitative analysis of literature data.

08:00 EDT 7th July 2018 | BioPortfolio

Summary of "The contribution of agonist and antagonist activities of α4β2* nAChR ligands to smoking cessation efficacy: a quantitative analysis of literature data."

Two mechanisms underlie smoking cessation efficacies of α4β2* nicotinic acetylcholine receptor (nAChR) agonists: a "nicotine-like" agonist activity reduces craving by substituting for nicotine during a quit attempt, and a "nicotine-blocking" antagonist activity attenuates reinforcement by competing with inhaled nicotine during a relapse. To evaluate the contribution of each mechanism to clinical efficacy, we estimated the degree of agonist and antagonist activities of nicotine replacement therapy (NRT), varenicline, cytisine, and the discontinued nAChR agonists dianicline, ABT-418, ABT-089, CP-601927, and CP-601932, relative to the functional effects of nicotine from smoking.

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This article was published in the following journal.

Name: Psychopharmacology
ISSN: 1432-2072
Pages:

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A benzazepine derivative that functions as an ALPHA4/BETA2 NICOTINIC RECEPTOR partial agonist. It is used for SMOKING CESSATION.

Discontinuation of the habit of smoking, the inhaling and exhaling of tobacco smoke.

Cessation of the habit of using tobacco products for smoking or chewing, including the use of snuff.

The first mixed agonist-antagonist analgesic to be marketed. It is an agonist at the kappa and sigma opioid receptors and has a weak antagonist action at the mu receptor. (From AMA Drug Evaluations Annual, 1991, p97)

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