Varenicline Tartrate

SKU: orb1307855

Description

Varenicline Tartrate (CP 526555-18) is a partial agonist of the α4β2 nicotinic acetylcholine receptor, derived from benzazepine. It is a well-established pharmacological aid for smoking cessation. This compound is widely used in neuroscience and addiction research, supporting both in vitro binding studies and in vivo behavioral models of nicotine dependence.

Research Area

Neuroscience, Signal Transduction

Images & Validation

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Key Properties

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CAS Number	375815-87-5
MW	361.35
Purity	99.90%
Formula	C₁₃H₁₃N₃·C₄H₆O₆
SMILES	O[C@@H]([C@H](O)C(O)=O)C(O)=O.C1C2CNCC1c1cc3nccnc3cc21
Target	AChR,ERK,p38 MAPK
Solubility	DMSO:3.62 mg/mL (10.02 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.77 mM)

Bioactivity

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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. Varenicline dose-dependently reduces nicotine self-administration and attenuates both nicotine prime and combined nicotine prime plus nicotine-paired cue-induced reinstatement. 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.

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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nAChR, Nicotinic acetylcholine receptors, mAChR, inhibit, Inhibitor, CP 526555-18, Chantix Tartrate, Chantix tartrate, Champix tartrate, Champix Tartrate, Varenicline, Varenicline Tartrate

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Compound Identifiers

PubChem CID

170362 ↗

Key Properties

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No computed properties available.

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