Varenicline

Modify Date: 2025-08-20 18:40:01

Varenicline Structure
Varenicline structure
Common Name Varenicline
CAS Number 249296-44-4 Molecular Weight 211.26
Density 1.247g/cm3 Boiling Point 400.6ºC at 760mmHg
Molecular Formula C13H13N3 Melting Point N/A
MSDS N/A Flash Point 196.1ºC

 Use of Varenicline


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.

 Names

Name varenicline
Synonym More Synonyms

 Varenicline 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
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.

 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

~83%

Varenicline Structure

Varenicline

CAS#:249296-44-4

Literature: Teva Pharmaceutical Industries Ltd. Patent: US2010/324055 A1, 2010 ; Location in patent: Page/Page column 4-5 ;

~68%

Varenicline Structure

Varenicline

CAS#:249296-44-4

Literature: Teva Pharmaceutical Industries Ltd. Patent: US2010/324055 A1, 2010 ; Location in patent: Page/Page column 5 ;

~61%

Varenicline Structure

Varenicline

CAS#:249296-44-4

Literature: Teva Pharmaceutical Industries Ltd. Patent: US2010/324055 A1, 2010 ; Location in patent: Page/Page column 5 ;

~96%

Varenicline Structure

Varenicline

CAS#:249296-44-4

Literature: TEVA PHARMACEUTICAL INDUSTRIES LTD.; TEVA PHARMACEUTICALS USA, INC. Patent: WO2009/143347 A2, 2009 ; Location in patent: Page/Page column 25 ;

~65%

Varenicline Structure

Varenicline

CAS#:249296-44-4

Literature: Pasikanti, Srinivas; Srinivasa Reddy; Venkatesham; Dubey; Iqbal, Javed; Das, Parthasarathi Tetrahedron Letters, 2010 , vol. 51, # 1 p. 151 - 152

 Precursor & DownStream

Precursor  1

DownStream  1

 Synonyms

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
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