Varenicline Tartrate Tablets Reference Listed Drug

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Name	Varenicline Tartrate Tablets
Trade name	Champix
Specifications	0.5mg (calculated as C13H13N3)；1.0mg (calculated as C13H13N3)
Dosage form	tablet
Licensee	Pfizer Limited
Remarks	Original research import

Varenicline is a selective partial agonist of the nicotinic acetylcholine receptor α4β2 subtype, and has a high affinity for this receptor in nerves. Varenicline binds to α4β2 receptor to produce an agonistic effect, while blocking the binding of nicotine to this receptor. This is the mechanism by which varenicline exerts a smoking cessation effect. Electrophysiological studies in vitro and neurochemical studies in vivo have shown that varenicline binds to neural α4β2 nicotinic acetylcholine receptors and stimulates receptor-mediated activities, but this effect is significantly weaker than nicotine. Varenicline can block nicotine's activation of α4β2 receptors, thereby activating the mesolimbic dopamine system, which is the underlying neural mechanism of smoking enhancement-reward effect. Varenicline is highly selective for α4β2 receptor, and its binding force to this receptor subtype is stronger than that of other common nicotinic receptors (α3β4>500 times, α7>3500 times, α1βγδ>20,000 times), The binding power of non-nicotinic receptors and transporters (>2000 times). In addition, varenicline has a moderate affinity for 5-HT3 receptors (Ki=350nM).

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