| Identification | Back Directory | [Name]
Varenicline-d4 | [CAS]
2183239-01-0 | [Synonyms]
Varenicline-d4
7,8,9,10-tetrahydro-6H-6,10-methanoazepino[4,5-g]quinoxaline-7,7,9,9-d4 | [Molecular Formula]
C13H13N3 | [MOL File]
2183239-01-0.mol | [Molecular Weight]
211.27 |
| Hazard Information | Back Directory | [Description]
Varenicline-d4 is intended for use as an internal standard for the quantification of varenicline by GC- or LC-MS. Varenicline is a full agonist of α7 subunit-containing neuronal nicotinic acetylcholine receptors (nAChRs; EC50 = 18 μM) and a partial agonist of α4β2 subunit-containing nAChRs (EC50 = 2.3 μM). Formulations containing varenicline have been used as aids in smoking cessation. | [Uses]
Varenicline-d4 is deuterium labeled Varenicline. Varenicline (CP 526555) is a potent partial agonist for α4β2 nicotinic acetylcholine receptor (nAChR) with an EC50 value of 2.3 μM. Varenicline is a full agonist for α3β4 and α7 nAChRs with EC50 values of 55 μM and 18 μM, respectively[1]. Varenicline is a nicotinic ligand based on the structure of cytisine, has the potential for smoking cessation treatment[2]. | [storage]
Store at -20°C | [References]
[1] Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. DOI:10.1177/1060028018797110
[2] Mihalak KB, et al. Varenicline is a partial agonist at alpha4beta2 and a full agonist at alpha7 neuronal nicotinic receptors.Mol Pharmacol.?2006 Sep;70(3):801-5. Epub 2006 Jun 9. DOI:10.1124/mol.106.025130
[3] Bagdas D, et al. New insights on the effects of?varenicline?on nicotine reward, withdrawal and hyperalgesia in mice.Neuropharmacology.?2018 Aug;138:72-79. DOI:10.1016/j.neuropharm.2018.05.025 |
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