Varenicline: an alpha4beta2 nicotinic receptor partial agonist for smoking cessation¶
Coe, J. W. (2005). Varenicline: an alpha4beta2 nicotinic receptor partial agonist for smoking cessation: an alpha4beta2 nicotinic receptor partial agonist for smoking cessation. Journal of Medicinal Chemistry.
Cited by¶
1 citation across 1 artifact.
Each citation links to the sentence it supports in the citing article.
Domain-specific¶
- Partial Agonist
- Receptor pharmacology — the foundational ligand classification (agonist / partial agonist / antagonist / inverse agonist), applied across G-protein-coupled receptors, ion channels, and nuclear receptors. Addiction medicine — partial agonism as the structural mechanism behind much of modern substitution therapy: buprenorphine at mu-opioid (analgesia and withdrawal relief with a ceiling on respiratory depression), varenicline at the α4β2 nicotinic receptor (craving relief while blocking nicotine's reinforcement)
This sourceThe alpha4beta2 partial-agonist design rationale for varenicline, blunting smoking-driven dopaminergic activation while relieving craving and withdrawal.
Supported in partVerified against the publisher's abstract
“We have pursued alpha4beta2 nicotinic receptor partial agonists to inhibit dopaminergic activation produced by smoking while simultaneously providing relief from the craving and withdrawal syndrome that accompanies cessation attempts.”
- Receptor pharmacology — the foundational ligand classification (agonist / partial agonist / antagonist / inverse agonist), applied across G-protein-coupled receptors, ion channels, and nuclear receptors. Addiction medicine — partial agonism as the structural mechanism behind much of modern substitution therapy: buprenorphine at mu-opioid (analgesia and withdrawal relief with a ceiling on respiratory depression), varenicline at the α4β2 nicotinic receptor (craving relief while blocking nicotine's reinforcement)
Verification¶
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