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
• 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

Properties

• 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

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.

Safety Information

• 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