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CAS No. : 249296-44-4
MCE 国际站:Varenicline
产品活性:Varenicline (CP 526555) 是 α4β2 烟碱乙酰胆碱受体 (α4β2 nAChR) 的部分激动剂 其EC50 值为 2.3 μM)。Varenicline 是 α3β4 nAChR 和 α7 nAChR 的完全激动剂,其 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,可用于戒烟方面的研究。
研究领域:Membrane Transporter/Ion Channel | Neuronal Signaling
作用靶点:nAChR
In Vitro: Varenicline (1 μM, 24 h ) inhibits LPS-Induced cytokine secretions (IL-1β, IL-6, and TNF α) and cell proliferation rate in RAW 264.7 macrophages.Varenicline (250 nM) evokes action potentials (Aps) in the absence of ACh stimulation in Human adrenal chromaffin cells isolated from male and female organ donors.Varenicline (100 μM, 4 h) promotes migration of HUVECs by lowering the protein expression of VE-cadherin.
In Vivo: Varenicline (Subcutaneous injection, 0.01-1 mg/kg, 3 days) given 10 min prior to nicotine (0.5 mg/kg, s.c.) inhibits nicotine conditioned place preference (CPP).Varenicline (Subcutaneous injection, 2.5 mg/kg, 3 days) results in a place aversion which is dependent on α5 nAChRs but not β2 nAChRs.Varenicline (Subcutaneous injection, 0.1 and 0.5 mg/kg, 3 days) reverses nicotine withdrawal signs such as hyperalgesia and somatic signs and withdrawal-induced aversion in a dose-related manner.
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