Varenicline

Names

[ Name ]:
Varenicline

[Synonym ]:
Vareniclene
Chantix
10-tetrahydro
10-Methano-6H-pyrazino[2
5,8,14-triazatetracycIo[10.3.1.0(2,11).0(4,9)]hexadeca-2(11),3,5,7,9-pentaene
5,8,14-triazatetracyclo[10.3.1.0(2,11),0(4,9)]hexadeca-2(l11),3,5,7,9-pentaene
3-h][3]benzazepine
5,8,14-triazatetracyclo[10.3.1.0(2,11).0(4,9)]hexadeca-2(11),3,5,7,9-pentaene
Varenicline
7,8,9,10-tetrahydro-6,10-methano-6H-pyrazino[2,3-h][3]benzazepine
Unii-W6hs99o8zo

Biological Activity

[Description]:

Varenicline(CP 526555;Champix) is a selective α4β2 nicotinic receptor partial agonist; it stimulates nicotine receptors more weakly than nicotine itself does.IC50 value:Target: nAChRVarenicline(CP 526555; Champix; Chantix) 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(CP 526555; Champix; Chantix) can assist some patients to quit smoking.

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> nAChR

Signaling Pathways >> Neuronal Signaling >> nAChR

Research Areas >> Neurological Disease

[References]

[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.

[Related Small Molecules]

Chemical & Physical Properties

[ Density]:
1.247g/cm3

[ Boiling Point ]:
400.6ºC at 760mmHg

[ Molecular Formula ]:
C₁₃H₁₃N₃

[ Molecular Weight ]:
211.26

[ Flash Point ]:
196.1ºC

[ PSA ]:
152.87000

[ LogP ]:
0.01010

[ Vapour Pressure ]:
1.25E-06mmHg at 25°C

[ Index of Refraction ]:
1.667

[ Storage condition ]:
2-8℃

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Related Compounds

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