Home Neuronal Signaling AChR agonist Varenicline Tartrate (CP 526555-18) For research use only.

Varenicline Tartrate (CP 526555-18)

Synonyms: Chantix, Champix,CP 526555-18

Varenicline Tartrate (CP 526555-18, Chantix, Champix) is a nicotinic AChR partial agonist, used to treat nicotine addiction.

Varenicline Tartrate (CP 526555-18) Chemical Structure

Varenicline Tartrate (CP 526555-18) Chemical Structure

CAS No. 375815-87-5

Purity & Quality Control

Varenicline Tartrate (CP 526555-18) Related Products

Signaling Pathway

AChR Signaling Pathways

AChR Signaling Pathway

Biological Activity

Description Varenicline Tartrate (CP 526555-18, Chantix, Champix) is a nicotinic AChR partial agonist, used to treat nicotine addiction.
Targets
AChR [1]
In vitro
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
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01680887 Completed
Cocaine Dependence
University of Pennsylvania
 August 2012 Phase 2

Chemical Information & Solubility

Molecular Weight 361.35 Formula

C13H13N3·C4H6O6
CAS No. 375815-87-5 SDF Download Varenicline Tartrate (CP 526555-18) SDF
Smiles C1C2CNCC1C3=CC4=NC=CN=C4C=C23.C(C(C(=O)O)O)(C(=O)O)O
Storage (From the date of receipt)

In vitro
Batch:

Water : 72 mg/mL

DMSO : 16 mg/mL ( (44.27 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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