866823-63-4
Chemical Structure
Varenicline dihydrochloride
Synonym(s): CP 526555 dihydrochloride
- CAS No.: 866823-63-4
- Formula:C13H15Cl2N3
- Molecular Weight:284.18
IUPAC Name: 7,8,9,10-tetrahydro-6H-6,10-methanoazepino[4,5-g]quinoxaline dihydrochloride
InChIKey: NZVVYNGXLGJKCW-UHFFFAOYSA-N
SMILES: [H]Cl.[H]Cl.C1(C2)CNCC2C3=CC4=NC=CN=C4C=C13
Biological Activity: Varenicline (CP 526555-18) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50 = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α7β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation[1][2][3][4][5].
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Varenicline dihydrochloride | 98.85% | Varenicline (CP 526555-18) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50 = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α7β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation. | ||||||||||||||||||||
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Varenicline dihydrochloride (Standard) | ≥98% | Varenicline (dihydrochloride) (Standard) is the analytical standard of Varenicline (dihydrochloride). This product is intended for research and analytical applications. Varenicline (CP 526555-18) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50 = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α7β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation. | ||||||||||||||||||||
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Varenicline-d4 dihydrochloride | Varenicline-d4 (dihydrochloride) is the deuterium labeled Varenicline dihydrochloride. | |||||||||||||||||||||
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Varenicline-d4 hydrochloride | Varenicline-d4 hydrochloride is a deuterium labeled Varenicline (dihydrochloride) (HY-10019A). Varenicline (CP 526555) dihydrochloride is a potent partial agonist for α4β2 nicotinic acetylcholine receptor (nAChR) with an EC50 value of 2.3 μM. Varenicline dihydrochloride is a full agonist for α3β4 and α7 nAChRs with EC50 values of 55 μM and 18 μM, respectively. Varenicline dihydrochloride is a nicotinic ligand based on the structure of cytosine, and has the potential for smoking cessation treatment. | |||||||||||||||||||||
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References
- [1]. Koegelenberg CF, et al. Efficacy of varenicline combined with nicotine replacement therapy vs varenicline alone for smoking cessation: a randomized clinical trial. JAMA. 2014 Jul;312(2):155-61. [Content Brief]
- [2]. Magnus CJ, et al. Ultrapotent chemogenetics for research and potential clinical applications. Science. 2019;364(6436):eaav5282. [Content Brief]
- [3]. Koga M, et al. Varenicline promotes endothelial cell migration by lowering vascular endothelial-cadherin levels via the activated α7 nicotinic acetylcholine receptor-mitogen activated protein kinase axis. Toxicology. 2017;390:1-9. [Content Brief]
- [4]. Ren J, et al. Countering Opioid-induced Respiratory Depression in Male Rats with Nicotinic Acetylcholine Receptor Partial Agonists Varenicline and ABT 594. Anesthesiology. 2020 May;132(5):1197-1211. [Content Brief]
- [5]. Mello NK, et al. Effects of chronic varenicline treatment on nicotine, cocaine, and concurrent nicotine+cocaine self-administration. Neuropsychopharmacology. 2014 Apr;39(5):1222-31. [Content Brief]
