Varenicline Tartrate

Licensed by Pfizer Catalog No.S1440 Synonyms: CP 526555-18

Varenicline Tartrate Chemical Structure

Molecular Weight(MW): 361.35

Varenicline Tartrate is a nicotinic AChR partial agonist, used to treat nicotine addiction.

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Biological Activity

Description Varenicline Tartrate is a nicotinic AChR partial agonist, used to treat nicotine addiction.
Targets
AChR [1]
In vitro

Varenicline is a partial agonist with 45% of nicotine's maximal efficacy atalpha4beta2 nAChRs in HEK cells expressing nAChRs. [1] Varenicline is a potent, partial agonist at alpha4beta2 receptors, with an EC50 of 2.3 mM and an efficacy (relative to acetylcholine) of 13.4%. Varenicline has lower potency and higher efficacy at alpha3beta4 receptors, with an EC50 of 55 mM and an efficacy of 75%. [2]

In vivo Varenicline has significantly lower (40-60%) efficacy than nicotine in stimulating [(3)H]-dopamine release from rat brain slices in vitro and in increasing dopamine release from rat nucleus accumbens in vivo, while it is more potent than Nicotine. Varenicline effectively attenuates the nicotine-induced dopamine release to the level of the effect of Varenicline alone, consistent with partial agonism. Varenicline reduces nicotine self-administration in rats and supports lower self-administration break points than nicotine. [1] Varenicline dose-dependently reduces nicotine self-administration and attenuates both nicotine prime and combined nicotine prime plus nicotine-paired cue-induced reinstatement. [3] Varenicline, a partial agonist at thealpha4beta2 nAChRs, reduces nicotine intake and was recently approved as a smoking cessation aid. Varenicline selectively reduces ethanol but not sucrose seeking using an operant self-administration drinking paradigm and also decreases voluntary ethanol but not water consumption in animals chronically exposed to ethanol for 2 months before Varenicline treatment. [4]

Protocol

Solubility (25°C)

In vitro Water 72 mg/mL (199.25 mM)
DMSO 1 mg/mL (2.76 mM)
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 361.35
Formula

C13H13N3·C4H6O6

CAS No. 375815-87-5
Storage powder
in solvent
Synonyms CP 526555-18

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AChR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID