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Product Description
– Varenicline-d4 is deuterium labeled Varenicline. Varenicline (CP 526555) is a potent partial agonist for α4β2 nicotinic acetylcholine receptor (nAChR) with an EC50 value of 2.3 μM. Varenicline is a full agonist for α3β4 and α7 nAChRs with EC50 values of 55 μM and 18 μM, respectively[1]. Varenicline is a nicotinic ligand based on the structure of cytisine, has the potential for smoking cessation treatment[2].
Web ID
– HY-10019S
Shipping
– Room temperature
Applications
– Neuroscience-Neuromodulation
Molecular Formula
– C13H9D4N3
References
– [1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. |[2]Bagdas D, et al. New insights on the effects of varenicline on nicotine reward, withdrawal and hyperalgesia in mice.Neuropharmacology. 2018 Aug;138:72-79.|[3]Mihalak KB, et al. Varenicline is a partial agonist at alpha4beta2 and a full agonist at alpha7 neuronal nicotinic receptors.Mol Pharmacol. 2006 Sep;70(3):801-5. Epub 2006 Jun 9.
CAS Number
– 2183239-01-0
Molecular Weight
– 215.29
SMILES
– [2H]C1([2H])NC([2H])([2H])C2CC1C3=CC4=NC=CN=C4C=C32
Clinical Information
– No Development Reported
Research Area
– Neurological Disease
Solubility
– 10 mM in DMSO
Target
– Isotope-Labeled Compounds;nAChR
Pathway
– Membrane Transporter/Ion Channel;Neuronal Signaling;Others
Product type
– Isotope-Labeled Compounds
Disclaimer: All products are for Research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation. Agdia Products are available for delivery only in Canada.
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