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Product Category详细介绍
| 品牌 | absin | CAS | 375815-87-5 |
|---|---|---|---|
| 分子式 | C13H13N3·C4H6O6 | 纯度 | ＞98% |
| 分子量 | 361.35 | 货号 | abs47027806 |
| 规格 | 5mg | 供货周期 | 现货 |
| 主要用途 | used to treat nicotine addiction. | 应用领域 | 化工,生物产业,农林牧渔,制药/生物制药,综合 |
Varenicline Tartrate 375815-87-5
| 产品描述 | |
| 描述 | Varenicline Tartrate is a nicotinic AChR partial agonist, used to treat nicotine addiction. |
| 纯度 | ＞98% |
| 储存/保存方法 | Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 别名 | 酒石酸伐仑克林；CP 526555-18；Champix tartrate；Chantix tartrate |
| 外观 | white to beige powder |
| 可溶性/溶解性 | DMSO ：1 mg/mL Water ：72 mg/mL |
| 生物活性 | |
| 靶点 | AChR |
| In vitro(体外研究) | Varenicline is a partial agonist with 45% of nicotine's maximal efficacy atalpha4beta2 nAChRs in HEK cells expressing nAChRs. Varenicline is a potent, partial agonist at alpha4beta2 receptors, with an EC50 of 2.3 mM and an efficacy (relative to acetylcholine) of 13.4%. Varenicline has lower potency and higher efficacy at alpha3beta4 receptors, with an EC50 of 55 mM and an efficacy of 75%. |
| In vivo(体内研究) | Varenicline has significantly lower (40-60%) efficacy than nicotine in stimulating -dopamine release from rat brain slices in vitro and in increasing dopamine release from rat nucleus accumbens in vivo, while it is more potent than Nicotine. Varenicline effectively attenuates the nicotine-induced dopamine release to the level of the effect of Varenicline alone, consistent with partial agonism. Varenicline reduces nicotine self-administration in rats and supports lower self-administration break points than nicotine. Varenicline dose-dependently reduces nicotine self-administration and attenuates both nicotine prime and combined nicotine prime plus nicotine-paired cue-induced reinstatement. Varenicline, a partial agonist at thealpha4beta2 nAChRs, reduces nicotine intake and was recently approved as a smoking cessation aid. Varenicline selectively reduces ethanol but not sucrose seeking using an operant self-administration drinking paradigm and also decreases voluntary ethanol but not water consumption in animals chronically exposed to ethanol for 2 months before Varenicline treatment. |
| 参考文献 | |
| 参考文献 |
| 研究领域 | |
| 研究领域 | Neuroscience Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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