Product overview

Name Varenicline tartrate
Description Selective α4β2 nAChR partial agonist; orally active
Purity >99%
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Biological Data

Biological description

Subtype-selective α4β2 nicotinic receptor partial agonist (Ki values are 0.06, 240, 322 and 3540 nM for α4β2, α3β4, α7, α1βγδ receptors respectively).

Also activates PSAM4-5HT3 and PSAM4-GlyR (EC50 values are 4 nM and 1.6 nM respectively) chimeric ion channels to silence neurons.

Stimulates dopamine release. Orally active. Shows excellent brain penetrance.

Solubility & Handling

Storage instructions Room temperature
Solubility overview Soluble in water (100 mM), and in DMSO (50 mM)
Important This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use

Calculators

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Dilution

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Chemical Data

Chemical name 7,8,9,10-Tetrahydro-6,10-methano-6H-pyrazino [2,3-h][3] benzazepine tartrate
Molecular Weight 361.37
Chemical structure  Chemical Structure
Molecular Formula C13H13N3.C4H6O6
CAS Number 375815-87-5
PubChem identifier 9906942
SMILES C1C2CNCC1C3=CC4=NC=CN=C4C=C23.[C@@H]([C@H](C(=O)O)O)(C(=O)O)O
InChi 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)/t;1-,2-/m.1/s1
InChiKey JQSHBVHOMNKWFT-DTORHVGOSA-N
MDL number MFCD08460603
Appearance White solid

References for Varenicline tartrate

References are publications that support the biological activity of the product
  • Ultrapotent chemogenetics for research and potential clinical applications

    Magnus CJ et al (2019) Science 364 : (6436)
  • Pharmacological profile of the alpha4beta2 nicotinic acetylcholine receptor partial agonist varenicline, an effective smoking cessation aid

    Rollema H et al (2007) Neuropharmacology 52(3) : 985-94
  • Varenicline is a partial agonist at alpha4beta2 and a full agonist at alpha7 neuronal nicotinic receptors.

    Mihalak et al (2006) Mol Pharmacol. 70(3) : 801-5