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Merck
CN

PZ0004

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
UNSPSC Code:
12352200
PubChem Substance ID:
329823673
NACRES:
NA.77
MDL number:
MFCD08460603

Key Documents

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Product Name

Varenicline tartrate, ≥98% (HPLC)

SMILES string

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

InChI key

TWYFGYXQSYOKLK-CYUSMAIQSA-N

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

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: >5 mg/mL

storage temp.

room temp

Quality Level

100

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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

signalword

Warning

hcodes

H302,H400

Hazard Classifications

Acute Tox. 4 Oral - Aquatic Acute 1

Storage Class

11 - Combustible Solids

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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Anne Jackson et al.
Addiction biology, 22(5), 1316-1328 (2016-07-22)
There is recognition that cognitive problems can contribute to renewed drug taking in former addicts. Our previous work has indicated that current smokers show reduced performance on a probabilistic reversal learning (PRL) task, relative to former smokers. To further explore
On-line column coupled isotachophoresis-capillary zone electrophoresis hyphenated with tandem mass spectrometry in drug analysis: Varenicline and its metabolite in human urine
Pievstansky J, et al.
Analytica Chimica Acta, 826, 84-93 (2014)
Toshiki Kurosawa et al.
Journal of pharmaceutical sciences, 106(9), 2576-2582 (2017-04-30)
Varenicline is a selective partial α
Yi-Hsuan Chuang et al.
Cancers, 12(5) (2020-05-28)
Although many studies have shown the association between smoking and the increased incidence and adverse prognosis of head and neck squamous cell carcinoma (HNSCC), the mechanisms and pharmaceutical targets involved remain unclear. Here, we integrated gene expression signatures, genetic alterations
Andrea de Bejczy et al.
Alcoholism, clinical and experimental research, 39(11), 2189-2199 (2015-09-29)
Alcohol dependence is a devastating illness affecting a large population, and new pharmacological treatments with good efficacy are greatly needed. One potential candidate is varenicline, a smoking cessation agent with partial agonist action at α4 β2 nicotinic acetylcholine receptors. A
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