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Varenicline dihydrochloride

CAS No. : 866823-63-4

MCE 站：Varenicline dihydrochloride

产品活性：Varenicline (CP 526555) dihydrochloride 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 dihydrochloride 是 α3β4 nAChR 和 α7 nAChR 的完全激动剂，其EC₅₀ 值分别为 55 μM 和 18 μM。Varenicline dihydrochloride 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 dihydrochloride (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 dihydrochloride (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 dihydrochloride (100 μM, 4 h) promotes migration of HUVECs by lowering the protein expression of VE-cadherin.

In Vivo: Varenicline dihydrochloride (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 dihydrochloride (Subcutaneous injection, 2.5 mg/kg, 3 days) results in a place aversion which is dependent on α5 nAChRs but not β2 nAChRs.
Varenicline dihydrochloride (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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