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

Key Properties

• CAS Number: 375815-87-5
• MW: 361.4
• Purity: >98%
• Formula: C₁₃H₁₃N₃·C₄H₆O₆
• SMILES: O[C@@H]([C@H](O)C(O)=O)C(O)=O.C1C2CNCC1c1cc3nccnc3cc21
• Target: Acetylcholinesterase/Butyrylcholinesterase
• Solubility: Soluble in DMSO (up to 18 mg/ml) or in Water (up to 35 mg/ml).

Bioactivity

• 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.
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• In Vitro:
  Varenicline is a partial agonist with 45% of nicotine's maximal efficacy atalpha4beta2 nAChRs in HEK cells expressing nAChRs. 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%.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Chantix; CP-526,555-18

Compound Identifiers

PubChem CID

170362