Varenicline

• CAT Number: I002845
• CAS Number: 249296-44-4
• Molecular Formula: C13H13N3
• Molecular Weight: 211.26
• Purity: ≥95%
• Synonyms: CP 526555;Champix
• Target: Nicotinic Receptor
• Solubility: DMSO: ＞ 2.1 mg/mL
• Storage: Store at -20C
• IUPAC Name: 5,8,14-triazatetracyclo[10.3.1.02,11.04,9]hexadeca-2,4,6,8,10-pentaene
• InChI: InChI=1S/C13H13N3/c1-2-16-13-5-11-9-3-8(6-14-7-9)10(11)4-12(13)15-1/h1-2,4-5,8-9,14H,3,6-7H2
• InChIKey: JQSHBVHOMNKWFT-UHFFFAOYSA-N
• SMILES: C1C2CNCC1C3=CC4=NC=CN=C4C=C23

Varenicline(CAT: I002845) is a selective α4β2 nicotinic receptor partial agonist; it stimulates nicotine receptors more weakly than nicotine itself does. Varenicline is a prescription medication used to treat smoking addiction. As a partial agonist, it both reduces cravings for and decreases the pleasurable effects of cigarettes and other tobacco products. Through these mechanisms, Varenicline can assist some patients to quit smoking.

Overview of Clinical Research

Varenicline is an alpha4 beta2 nicotinic receptor agonist. University of Zagreb planned a phase III trial for Smoking withdrawal (PO) in September 2019 (NCT04015414).

Reference

[1]. Kikkawa, H.; Maruyama, N.; Fujimoto, Y.; Hasunuma, T. Single- and multiple-dose pharmacokinetics of the selective nicotinic receptor partial agonist, varenicline, in healthy Japanese adult smokers. Journal of Clinical Pharmacology (2011), 51(4), 527-537.

[2]. Bordia T, Hrachova M, Chin M et al. Varenicline Is a Potent Partial Agonist at α6β2* Nicotinic Acetylcholine Receptors in Rat and Monkey Striatum. J Pharmacol Exp Ther. 2012 Aug;342(2):327-34.

[3]. Pachas GN, Cather C, Pratt SA et al. Varenicline for Smoking Cessation in Schizophrenia: Safety and Effectiveness in a 12-Week, Open-Label Trial. J Dual Diagn. 2012;8(2):117-125.

[4]. Krebs P, Sherman SE. Review: Varenicline for tobacco cessation does not increase CV serious adverse events. Ann Intern Med. 2012 Aug 21;157(4):JC2-2.