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PZ0004

Varenicline tartrate

Name: Varenicline tartrate
Brand: SIGMA

≥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

Assay:

≥98% (HPLC)

Form:

powder

Quality level:

100

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Properties

Product Name

Varenicline tartrate, ≥98% (HPLC)

Quality Level

100

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

Description

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.

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pictograms

GHS07,GHS09

signalword

Warning

hcodes

H302,H400

pcodes

P264 - P270 - P273 - P301 + P312 - P391 - P501

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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Articles

Acetylcholine Receptors (Nicotinic)

Sigma-Aldrich offers many products related to nicotinic acetylcholine receptors for your research needs.

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Involvement of Proton-Coupled Organic Cation Antiporter in Varenicline Transport at Blood-Brain Barrier of Rats and in Human Brain Capillary Endothelial Cells.

Toshiki Kurosawa et al.

Journal of pharmaceutical sciences, 106(9), 2576-2582 (2017-04-30)

Varenicline is a selective partial α

Varenicline, the clinically effective smoking cessation agent, restores probabilistic response reversal performance during withdrawal from nicotine.

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)

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Global Trade Item Number

SKU	GTIN
PZ0004-25MG	04061836687236
PZ0004-5MG	04061833220177