Cat. No. 3754
Chemical Name: 7,8,9,10-Tetrahydro-6,10-methano-6H
Biological ActivityOrally active, subtype-selective partial agonist at α4β2 nicotinic receptors (Ki values are 0.06, 240, 322 and 3540 nM for α4β2, α3β4, α7, α1βγδ receptors respectively). Reduces nicotine-evoked dopamine release in vitro and decreases nicotine self-administration in vivo.
Licensing InformationSold for research purposes under agreement from Pfizer Inc.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Data Sheet
Rollema et al (2009) Preclinical pharmacology of the α4β2 nAChR partial agonist varenicline related to effects on reward, mood and cognition. Biochem.Pharmacol. 78 813. PMID: 19501054.
Rollema et al (2007) Pharmacological profile of the α4β2 nicotinic acetylcholine receptor partial agonist varenicline, an effective smoking cessation aid. Neuropharmacology 52 985. PMID: 17157884.
Coe et al (2005) Varenicline: an α4β2 nicotinic receptor partial agonist for smoking cessation. J.Med.Chem. 48 3474. PMID: 15887955.
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Citations are publications that use Tocris products. Selected citations for Varenicline tartrate include:
Price et al (2015) Varenicline Interactions at the 5-HT3 Receptor Ligand Binding Site are Revealed by 5-HTBP. PLoS One 6 1151. PMID: 25648658.
Kuryatov et al (2013) Chemical chaperones exceed the chaperone effects of RIC-3 in promoting assembly of functional α7 AChRs. Sci Rep 8 e62246. PMID: 23638015.
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Keywords: Varenicline tartrate, supplier, nicotinic, receptors, subtype, selective, alpha4beta2, a4b2, α4β2, orally, active, nAChRs, acetylcholine, cholinergics, neuronal, nicotine, Pfizer, Tocris Bioscience, Nicotinic (α4β2) Receptor Agonist products
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