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Biological Data
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Biological description
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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.
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Solubility & Handling
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Storage instructions
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Room temperature |
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Solubility overview
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Soluble in water (100 mM), and in DMSO (50 mM) |
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Important
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This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use |
Chemical Data
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Chemical name
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7,8,9,10-Tetrahydro-6,10-methano-6H-pyrazino [2,3-h][3] benzazepine tartrate |
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Chemical structure
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Molecular Formula
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C13H13N3.C4H6O6 |
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PubChem identifier
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9906942 |
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SMILES
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C1C2CNCC1C3=CC4=NC=CN=C4C=C23.[C@@H]([C@H](C(=O)O)O)(C(=O)O)O |
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InChi
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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 |
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InChiKey
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JQSHBVHOMNKWFT-DTORHVGOSA-N |
References for Varenicline tartrate
References are publications that support the biological activity of the product
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Ultrapotent chemogenetics for research and potential clinical applications
Magnus CJ et al (2019)
Science 364 : (6436)
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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
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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
Selective α4β2 nAChR partial agonist; orally active
Understanding purity and quality - a guide for life scientists 
