Varenicline Tartrate

Names

[ Name ]:
Varenicline Tartrate

[Synonym ]:
7,8,9,10-Tetrahydro-6,10-methano-6H-pyrazino[2,3-h][3]benzazepine tartrate Champix
(2R,3R)-3-carboxy-2,3-dihydroxypropanoate de (1R,12S)-5,8-diaza-14-azoniatétracyclo[10.3.1.0.0]hexadéca-2(11),3,5,7,9-pentaène
Chantix
(1R,12S)-5,8-Diaza-14-azoniatetracyclo[10.3.1.0.0]hexadeca-2(11),3,5,7,9-pentaene (2R,3R)-3-carboxy-2,3-dihydroxypropanoate
(1R,12S)-5,8-Diaza-14-azoniatetracyclo[10.3.1.0.0]hexadeca-2(11),3,5,7,9-pentaen-(2R,3R)-3-carboxy-2,3-dihydroxypropanoat
Butanedioic acid, 2,3-dihydroxy-, (2R,3R)-, compd. with (6R,10S)-7,8,9,10-tetrahydro-6,10-methano-6H-azepino[4,5-g]quinoxaline (1:1)
Champix
Varenicline tartrate

Biological Activity

[Description]:

Varenicline Tartrate(CP 526555;Champix) is a nicotinic receptor partial agonist; it stimulates nicotine receptors more weakly than nicotine itself does.IC50 value:Target: α4β2 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

Natural Products >> Others

[References]

[1]. 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.

[2]. 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.

[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]. 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.

[5]. Varenicline

[Related Small Molecules]

Chemical & Physical Properties

[ Boiling Point ]:
400.6ºC at 760 mmHg

[ Melting Point ]:
206-208ºC

[ Molecular Formula ]:
C₁₇H₁₉N₃O₆

[ Molecular Weight ]:
361.35

[ PSA ]:
23.79000

[ LogP ]:
4.49528

[ Storage condition ]:
Desiccate at RT

[ Water Solubility ]:
DMSO: >5mg/mL

MSDS

Click to get detail MSDS

Safety Information

[ Symbol ]:

GHS02, GHS06, GHS08

[ Signal Word ]:
Danger

[ Hazard Statements ]:
H225-H301 + H311 + H331-H370

[ Precautionary Statements ]:
P210-P260-P280-P301 + P310-P311

[ Hazard Codes ]:
Xn,N,T,F

[ Risk Phrases ]:
22-50-39/23/24/25-23/24/25-11

[ Safety Phrases ]:
22-57-45-36/37-16-7

[ RIDADR ]:
UN 3077 9 / PGIII

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Articles

Concurrent access to nicotine and sucrose in rats.

Psychopharmacol. Ser. 232(8) , 1451-60, (2015)

Animal models that allow concurrent access to drug and nondrug reinforcers provide unique insight into the etiology, maintenance, and treatment of drug use.We sought to develop and utilize a concurren...

Chronic treatment with varenicline changes expression of four nAChR binding sites in mice.

Neuropharmacology 99 , 142-55, (2015)

Chronic treatment with nicotine is known to increase the α4β2-nAChR sites in brain, to decrease α6β2-nAChR sites and to have minimal effect on α3β4-and α7-nAChR populations. Varenicline is now used as...

Effects of varenicline on ethanol-induced conditioned place preference, locomotor stimulation, and sensitization.

Alcohol. Clin. Exp. Res. 38(12) , 3033-42, (2015)

Varenicline, a partial nicotinic acetylcholine receptor (nAChR) agonist, is a promising new drug for the treatment of alcohol (ethanol [EtOH]) dependence. Varenicline has been approved by the Food and...