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Submit ReviewVarenicline tartrate
说明： Selective α4β2 nAChR partial agonist; orally active
化学名： 7,8,9,10-Tetrahydro-6,10-methano-6H-pyrazino[2,3-h][3]benzazepine tartrate
纯度： ≥99% (HPLC)
生物活性 for Varenicline tartrate
Varenicline tartrate is an orally active, subtype-selective partial agonist at α4β2 nicotinic receptors (Ki values are 0.06, 240, 322 and 3540 nM for α4β2, α3β4, α7, α1βγδ receptors respectively). Reduces nicotine-evoked dopamine release in vitro and decreases nicotine self-administration in vivo. Also potently activates PSAM4-5-HT3 and PSAM4-GlyR chimeric ion channels (EC50 values are 4 and 1.6 nM, respectively)
许可信息
Sold for research purposes under agreement from Pfizer Inc.
化合物库 for Varenicline tartrate
Varenicline tartrate is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen FDA-Approved Drugs. 了解 Tocris 化合物库的更多信息。
技术数据 for Varenicline tartrate
| 分子量 | 361.37 |
| 公式 | C13H13N3.C4H6O6 |
| 储存 | Desiccate at RT |
| 纯度 | ≥99% (HPLC) |
| CAS Number | 375815-87-5 |
| PubChem ID | 5310966 |
| InChI Key | JQSHBVHOMNKWFT-DTORHVGOSA-N |
| Smiles | OC(C(O)C(O)=O)C(O)=O.C1(C=C([C@H]4CNC[C@@H]3C4)C3=C2)=C2N=CC=N1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for Varenicline tartrate
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| water | 36.14 | 100 | |
| DMSO | 18.07 | 50 |
制备储备液 for Varenicline tartrate
以下数据基于产品分子量 361.37。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.77 mL | 13.84 mL | 27.67 mL |
| 5 mM | 0.55 mL | 2.77 mL | 5.53 mL |
| 10 mM | 0.28 mL | 1.38 mL | 2.77 mL |
| 50 mM | 0.06 mL | 0.28 mL | 0.55 mL |
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产品说明书 for Varenicline tartrate
参考文献 for Varenicline tartrate
参考文献是支持产品生物活性的出版物。
Coe et al (2005) Varenicline: an α4β2 nicotinic receptor partial agonist for smoking cessation. J.Med.Chem. 48 3474 PMID: 15887955
Rollema et al (2007) Pharmacological profile of the α4β2 nicotinic acetylcholine receptor partial agonist varenicline, an effective smoking cessation aid. Neuropharmacology 52 985 PMID: 17157884
Rollema et al (2009) Preclinical pharmacology of the α4β2 nAChR partial agonist vareni. related to effects on reward, mood and cognition. Biochem.Pharmacol. 78 813 PMID: 19501054
If you know of a relevant reference for Varenicline tartrate, please let us know.
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关键词: Varenicline tartrate, Varenicline tartrate supplier, nicotinic, receptors, subtype, selective, alpha4beta2, a4b2, α4β2, orally, active, nAChRs, acetylcholine, cholinergics, neuronal, nicotine, Pfizer, chemogenetics, Nicotinic, (a4b2), Receptors, PSEMs, 3754, Tocris Bioscience
10 篇 Varenicline tartrate 的引用文献
引用文献是使用了 Tocris 产品的出版物。 Varenicline tartrate 的部分引用包括：
Andrew et al (2023) Identification of nicotine-seeking and avoiding larval zebrafish using a new three-choice behavioral assay. Front Mol Neurosci 16 1112927 PMID: 37063370
David M et al (2023) Gestational ethanol exposure impairs motor skills in female mice through dysregulated striatal dopamine and acetylcholine function. Neuropsychopharmacology PMID: 37188849
Xin et al (2020) Validation of a nicotine vapor self-administration model in rats with relevance to electronic cigarette use. Neuropsychopharmacology 45 1909-1919 PMID: 32544927
Lacroix et al (2017) VRC Reduces Context-Induced Relapse to Alcohol-Seeking through Actions in the Nucleus Accumbens. Neuropsychopharmacology 42 1037 PMID: 27834390
Price et al (2015) Varenicline Interactions at the 5-HT3 Receptor Ligand Binding Site are Revealed by 5-HTBP. PLoS One 6 1151 PMID: 25648658
Cippitelli et al (2015) AT-1001: a high-affinity α3β4 nAChR ligand with novel nicotine-suppressive pharmacology. Br J Pharmacol 172 1834 PMID: 25440006
Magnus et al (2019) Ultrapotent chemogenetics for research and potential clinical applications Science 364 PMID: 30872534
Durham et al (2019) Direct Effects of Nicotine Exposure on Murine Calvaria and Calvarial Cells. Sci Rep 9 3805 PMID: 30846819
Kutlu et al (2018) Differential effects of α4β2 nicotinic receptor antagonists and partial-agonists on contextual fear extinction in male C57BL/6 mice. Psychopharmacology (Berl) 235 1211 PMID: 29383396
Kuryatov et al (2013) Chemical chaperones exceed the chaperone effects of RIC-3 in promoting assembly of functional α7 AChRs. Sci Rep 8 e62246 PMID: 23638015
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
Nicotinic ACh Receptors Scientific Review
Updated in 2014, this review by Sue Wonnacott summarizes the diverse structure and function of nicotinic acetylcholine receptors and gives an in-depth review of the ligands available for nAChR research. Compounds available from Tocris are listed.
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