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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 Solubility overview Soluble in water (100 mM), and in DMSO (50 mM)
Storage instructions Room temperature
Storage of solutions Prepare and use solutions on the same day if possible. Store solutions at -20°C for up to one month if storage is required. Equilibrate to RT and ensure the solution is precipitate free before use.
Shipping Conditions Stable for ambient temperature shipping. Follow storage instructions on receipt.
Important This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use
Chemical Data Chemical name 7,8,9,10-Tetrahydro-6,10-methano-6H-pyrazino [2,3-h][3] benzazepine tartrate
Chemical structure
Molecular Formula C13 H13 N3 .C4 H6 O6
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
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
Selective α4β2 nAChR partial agonist; orally active
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