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| 250mg |
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Varenicline Hydrochloride (CP 526555 hydrochloride) is a potent, high affinity, selective α4β2 nicotine acetylcholine receptor (nAChR) partial agonist and full α7 nAChR agonist. Varenicline Hydrochloride is also a potent partial agonist of α6β2 nAChR in striatum of rats with a Ki of 0.12 nM. It is medication used to treat nicotine addiction.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%.
| ln Vivo |
Treatment with varenicline (0.5-2 mg/kg/day; subcutaneous injection; twice daily; for 14 days; male Wistar rats) demonstrated significantly greater availability of DRD2/3 in the ventral striatum, ca. 11%, but rats treated with varenicline alone at doses of 1 mg/kg/day and 2 mg/kg/day showed substantial increases in DRD2/3 availability in the dorsal striatum by 12.5% and 13.2%, respectively. Varenicline can elicit a dose-dependent and sustained rise in DRD2/3 in the rat striatum, notably in the ventral striatum [1].
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| Animal Protocol |
Animal/Disease Models: 80 male Wistar rats (250-300 g) [1]
Doses: 0.5 mg/kg/day, 1 mg/kg/day, or 2 mg/kg/day twice (two times) daily; for 14 days Experimental Results: Abdominal DRD2/3 availability in the lateral striatum was Dramatically increased by approximately 11%, while rats treated with doses of only 1 and 2 mg/kg/day demonstrated a significant increase in DRD2/3 availability in the dorsal striatum of 12.5% , respectively 13.2%. |
| References |
[1]. Crunelle CL, et al. Dose-dependent and sustained effects of varenicline on dopamine D2/3 receptor availability in rats. Eur Neuropsychopharmacol. 2011 Feb;21(2):205-10.
[2]. Kikkawa H, et al. Single- and multiple-dose pharmacokinetics of the selective nicotinic receptor partial agonist, varenicline, in healthy Japanese adult smokers. J Clin Pharmacol. 2011 Apr;51(4):527-37. [3]. Pachas GN, Cather C, Pratt SA et al. Varenicline for Smoking Cessation in Schizophrenia: Safety and Effectiveness in a 12-Week, Open-Label Trial. J Dual Diagn. 2012;8(2):117-125. [4]. Bordia T, Hrachova M, Chin M et al. Varenicline Is a Potent Partial Agonist at α6β2* Nicotinic Acetylcholine Receptors in Rat and Monkey Striatum. J Pharmacol Exp Ther. 2012 Aug;342(2):327-34. |
| Molecular Formula |
C₁₃H₁₄CLN₃
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|---|---|
| Molecular Weight |
247.72
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| CAS # |
230615-23-3
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| Related CAS # |
Varenicline;249296-44-4
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| SMILES |
C1(C2CC3CNC2)=C3C=C(N=CC=N4)C4=C1.Cl
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| Synonyms |
CP-526555 hydrochlorideCP 526555 hydrochlorideCP 526555-18 CP-526555 18 CP 526555 18 CP52655518 Varenicline tartrate Chantix Champix
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ~50 mg/mL (~201.84 mM)
DMSO : ≥ 2.5 mg/mL (~10.09 mM) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.0368 mL | 20.1841 mL | 40.3682 mL | |
| 5 mM | 0.8074 mL | 4.0368 mL | 8.0736 mL | |
| 10 mM | 0.4037 mL | 2.0184 mL | 4.0368 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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