varenicline

Varenicline (CP 526555) 是一种有效的α4β2 nAChR 烟碱乙酰胆碱受体的部分激动剂，EC50值为2.3 μM。Varenicline 是 α3β4 nAChR 和 α7 nAChR 乙酰胆碱受体的完全激动剂，EC50值分别为 55 μM 和 18 μM。Varenicline 是一种基于胞嘧啶结构的烟碱配体，具有戒烟治疗的潜力。

Varenicline Tartrate (CP 526555-18) 是α4β2 烟碱乙酰胆碱受体的部分激动剂，EC50为 2.3 μM。它是 α3β4 和 α7 乙酰胆碱受体完全激动剂，EC50值分别为 55 和 18 μM，用于戒烟方面的研究。

Hydroxy varenicline, a metabolite of the nicotinic acetylcholine receptor (nAChR) agonist varenicline, functions within the biochemical pathway by interacting with nAChR sites.

Varenicline Hydrochloride is a partial agonist of α4β2 nicotinic receptor.

Varenicline dihydrochloride是一种选择性 α4β2 烟碱乙酰胆碱受体部分激动剂。

Ultrapotent PSEM (uPSEM) agonist for PSAM4-GlyR and PSAM4-5HT3 (Ki = 0.7 nM for PSAM4-GlyR and <10 nM for PSAM4-5HT3). Exhibits >10,000-fold agonist selectivity for PSAM4-GlyR over α7-GlyR, α7-5HT3, and 5HT3-R, and 230-fold selectivity over α4β2 nAChR. Also weak partial agonist (~10 %) at α4β2 nAChR. Retains the potency of varenicline (Cat.No. 3754) for PSAM4-GlyR with enhanced chemogenetic selectivity. Does not act as a substrate for P-glycoprotein pumps. Silences neurons in vivo. Brain-penetrant. Magnus et al (2019) Ultrapotent chemogenetics for research and potential clinical applications. Science doi: 10.1126/science PMID:30872534