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Varenicline Hydrochloride (CP 526555) 是一种口服活性的α4β2 烟碱型乙酰胆碱受体(α4β2 nAChR, IC50 = 250 nM)部分激动剂,该受体被认为是尼古丁依赖的主要介质,其药理作用在调控与尼古丁暴露相关的成瘾行为中具有关键意义。Varenicline Hydrochloride (CP 526555) 阻断尼古丁对烟碱型乙酰胆碱受体的直接激动作用,同时以更温和和可控的方式刺激这些受体,使其成为广泛用于戒烟研究的重要化合物。

Varenicline Hydrochloride (CP 526555) 是一种口服活性的α4β2 烟碱型乙酰胆碱受体(α4β2 nAChR, IC50 = 250 nM)部分激动剂,该受体被认为是尼古丁依赖的主要介质,其药理作用在调控与尼古丁暴露相关的成瘾行为中具有关键意义。Varenicline Hydrochloride (CP 526555) 阻断尼古丁对烟碱型乙酰胆碱受体的直接激动作用,同时以更温和和可控的方式刺激这些受体,使其成为广泛用于戒烟研究的重要化合物。
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 1 mg | ¥ 266 | In stock | |
| 5 mg | ¥ 619 | In stock | |
| 10 mg | ¥ 828 | In stock | |
| 25 mg | ¥ 1,490 | In stock | |
| 50 mg | ¥ 2,250 | In stock | |
| 100 mg | ¥ 3,350 | In stock | |
| 200 mg | ¥ 4,870 | In stock | |
| 1 mL x 10 mM (in DMSO) | ¥ 683 | In stock |
Varenicline Hydrochloride 相关产品
| 产品描述 | Varenicline Hydrochloride (CP 526555) is an orally active partial agonist of the α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50 = 250 nM), which is recognized as the principal mediator of nicotine dependence, and its pharmacological effect is critical in modulating addictive behaviors associated with nicotine exposure. Varenicline Hydrochloride (CP 526555) blocks the direct agonist effects of nicotine on nicotinic acetylcholine receptors while simultaneously stimulating these receptors in a more moderate and controlled manner, making it a widely used research compound in smoking cessation. |
| 靶点活性 | α4β2 nAChR:250 nM |
| 体外活性 | Varenicline Hydrochloride (200 μM) 处理 HUVEC 24小时,对细胞活力无显著影响[3]。 |
| 体内活性 | 在大鼠中,皮下注射 Varenicline Hydrochloride(0.5, 1mg/kg)可剂量依赖地逆转芬太尼诱发的呼吸抑制,并轻度减弱芬太尼的镇静效应[4]。对已有尼古丁和可卡因使用史的成年恒河猴,连续 7–10 d、每日 23 小时 静脉滴注 Varenicline Hydrochloride (0.004–0.04 mg/kg/h),可剂量依赖地降低其单独或联合注射尼古丁与可卡因的自我给药量,而不影响以食物为奖励的操作反应[5]。在 C57BL/6J 和 CD-1 小鼠的强迫游泳实验中,口服Varenicline Hydrochloride (0.178-5.6 mg/kg) 表现出抗抑郁样作用[6]。 |
| 别名 | 盐酸伐尼克兰, CP526555 hydrochloride, CP 526555 hydrochloride |
| 分子量 | 247.72 |
| 分子式 | C13H14ClN3 |
| CAS No. | 230615-23-3 |
| Smiles | Cl.N1=CC=NC2=CC3=C(C=C12)C4CNCC3C4 |
| 密度 | 1.31g/cm3 |
| 颜色 | Yellow |
| 物理性状 | Solid |
| 存储 | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| 溶解度信息 | DMSO: ≥ 2 mg/mL, Sonication is recommended. H2O: 40 mg/mL (161.47 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
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H2O
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