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Merck
CN

PZ0004

Sigma-Aldrich

Varenicline tartrate

≥98% (HPLC), α4β2 nAChR partial agonist, powder

Synonym(s):

7,8,9,10-Tetrahydro-6,10-methano-6H-pyrazino[2,3-h][3]benzazepine tartrate, Champix

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About This Item

Empirical Formula (Hill Notation):
C13H13N3 · C4H6O6
CAS Number:
375815-87-5
Molecular Weight:
361.35
MDL number:
MFCD08460603
UNSPSC Code:
12352200
PubChem Substance ID:
329823673
NACRES:
NA.77

Key Documents

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Product Name

Varenicline tartrate, ≥98% (HPLC)

Assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: >5 mg/mL

storage temp.

room temp

SMILES string

O[C@H]([C@@H](O)C(O)=O)C(O)=O.C1NC[C@H]2C[C@@H]1c3cc4nccnc4cc23

InChI

1S/C13H13N3.C4H6O6/c1-2-16-13-5-11-9-3-8(6-14-7-9)10(11)4-12(13)15-1;5-1(3(7)8)2(6)4(9)10/h1-2,4-5,8-9,14H,3,6-7H2;1-2,5-6H,(H,7,8)(H,9,10)/t8-,9+;1-,2-/m.1/s1

InChI key

TWYFGYXQSYOKLK-CYUSMAIQSA-N

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Application

Varenicline tartrate has been used to investigate its effect on sensorimotor gating in rats under prepulse inhibition (PPI). It is suitable for use as a reference standard in capillary isotachophoresis (ITP) coupled on-line with capillary zone electrophoresis (CZE) for the quantification of varenicline metabolite in urine samples. It is also suitable for use for testing its effect on locomotor and nonlocomotor behavioral deficits in rats.

Biochem/physiol Actions

Varenicline tartrate is a partial α4β2 nicotinic receptor agonist and α7 full agonist.
Varenicline tartrate is a partial α4β2 nicotinic receptor agonist and α7 full agonist. Varenicline competitively binds to α4β2 receptors and partially stimulates without creating a full nicotine effect, while simultaneoudly blocking the ability of nicotine to bind to the receptors. Varenicline thus blocks the ability of nicotine to activate α4β2 receptors and stimulate the central nervous mesolimbic dopamine system, believed to be the neuronal mechanism underlying reinforcement and reward experienced upon smoking.

Features and Benefits

This compound is a featured product for ADME Tox research. Click here to discover more featured ADME Tox products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.
This compound is featured on the Acetylcholine Receptors (Nicotinic) page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

Pictograms

Exclamation markEnvironment
GHS07,GHS09

Signal Word

Warning

Hazard Statements

H302,H400

Hazard Classifications

Acute Tox. 4 Oral - Aquatic Acute 1

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

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Certificates of Analysis (COA)

Lot/Batch Number
0000341594
0000341594
0000147465
0000147464
0000147465

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Nathan M Holmes et al.
Addiction biology, 24(5), 849-859 (2018-06-20)
Restricting when and where smoking can occur is a major focus of public health policies in Western countries. In conjunction with increased taxation, these approaches have contributed to a reduction in smoking uptake among adolescents, yet the consequences for established
Hiroyuki Mizoguchi et al.
Behavioural brain research, 359, 935-941 (2018-06-24)
Patients suffering from neuropsychiatric disorders such as substance use and addiction disorders show impaired decision-making, which may be associated with their psychiatric disorders. Previously, using a gambling test for rodents, we demonstrated that methamphetamine-dependent rats showed alterations in their decision-making
Elizabeth G Guy et al.
Behavioural pharmacology, 25(8), 775-783 (2014-09-18)
Smoking tobacco remains one of the leading causes of preventable deaths in North America. Nicotine reinforces smoking behavior, in part, by enhancing the reinforcing properties of reward-related stimuli, or conditioned stimuli (CSs), associated with tobacco intake. To investigate how pharmaceutical
Helen M Kamens et al.
Brain research bulletin, 138, 20-25 (2017-08-06)
Adolescence is a critical period in brain development that coincides with the initiation of alcohol use. Nicotinic acetylcholine receptors (nAChR) have been shown to modulate ethanol behaviors in adult humans and in animal models; however, the role of these receptors
Effect of varenicline on behavioral deficits in a rat model of Parkinson?s disease induced by unilateral 6-hydroxydopamine lesion of substantia nigra
Tan R, et al.
Behavioural Pharmacology, 29(4), 327-335 (2018)
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