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Varenicline

Catalog No. T4246L   CAS 249296-44-4

Varenicline (CP 526555), a cytisine-based nicotinic ligand, is a potent partial agonist for the α4β2 nicotinic acetylcholine receptor (nAChR) with an EC50 value of 2.3 μM and acts as a full agonist for α7 and α3β4 nAChRs, with respective EC50 values of 18 μM and 55 μM [1]. Notably, its effectiveness and potential in smoking cessation treatments are underscored by its pharmacological profile [2].

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Varenicline Chemical Structure
Varenicline, CAS 249296-44-4
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Biological Description
Chemical Properties
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Description Varenicline (CP 526555), a cytisine-based nicotinic ligand, is a potent partial agonist for the α4β2 nicotinic acetylcholine receptor (nAChR) with an EC50 value of 2.3 μM and acts as a full agonist for α7 and α3β4 nAChRs, with respective EC50 values of 18 μM and 55 μM [1]. Notably, its effectiveness and potential in smoking cessation treatments are underscored by its pharmacological profile [2].
In vivo Varenicline (CP 526555) (subcutaneous injection; 0.01, 0.05, 0.1 and 1 mg/kg; 3 days) iven 10 min prior to nicotine, dose-dependently inhibits nicotine CPP. At the doses of 0.1 and 1 mg/kg totally blocks the effect of nicotine in CPP test without inducing significant changes in preferences on their own [2].Varenicline (2.5 mg/kg) results in a place aversion that was dependent on α5 nAChRs but not β2 nAChRs [2].Varenicline (0.1 and 0.5 mg/kg) reverses nicotine withdrawal signs such as hyperalgesia and somatic signs and withdrawal-induced aversion in a dose-related manner [2]. Animal Model: ICR male mice (8 weeks) [1] Dosage: 0.01, 0.05, 0.1 and 1 mg/kg Administration: 3 days Result: Supressed the effect of nicotine in CPP test.
Molecular Weight 211.26
Formula C13H13N3
CAS No. 249296-44-4

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Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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Keywords

Varenicline 249296-44-4 inhibitor inhibit

 

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