Varenicline

Research use only, not for human use.

Varenicline is a Selective α4β2 nicotinic acetylcholine receptor partial agonist.

Varenicline is a Selective α4β2 nicotinic acetylcholine receptor partial agonist.(In Vitro):Varenicline (1 μM, 24 h ) inhibits LPS-Induced cytokine secretions (IL-1β, IL-6, and TNF α) and cell proliferation rate in RAW 264.7 macrophages.Varenicline (250 nM) evokes action potentials (Aps) in the absence of ACh stimulation in Human adrenal chromaffin cells isolated from male and female organ donors.Varenicline (100 μM, 4 h) promotes migration of HUVECs by lowering the protein expression of VE-cadherin.(In Vivo):Varenicline (Subcutaneous injection, 0.01-1 mg/kg, 3 days) given 10 min prior to nicotine (0.5 mg/kg, s.c.) inhibits nicotine conditioned place preference (CPP).Varenicline (Subcutaneous injection, 2.5 mg/kg, 3 days) results in a place aversion which is dependent on α5 nAChRs but not β2 nAChRs.Varenicline (Subcutaneous injection, 0.1 and 0.5 mg/kg, 3 days) reverses nicotine withdrawal signs such as hyperalgesia and somatic signs and withdrawal-induced aversion in a dose-related manner.

Cell Viability Assay Cell Line:HUVEC Concentration:100, 200, 300, 500 μM Incubation Time:24 h Result:Did not affect cell viability at 100 and 200 μM (96.8 ± 0.1% and 93.9 ± 1.8%, respectively). Decreased cell viability to 85.7 ± 7.5% and 57.8 ± 7.7% for 300 and 500 μM, respectively.Western Blot Analysis Cell Line:HUVEC Concentration:100 μM Incubation Time:1, 5, 10, 15 ,30 ,60 min, 24 h Result:Significantly activated ERK1/2 and p38 signaling with peak activity at 10–15 min and 10–30 min after treatment, respectively, lowered expression of VE-cadherin at 24 h. MLA (100 nM) significantly reversed the Varenicline-induced effects.Cell Migration Assay Cell Line:HUVEC Concentration:100, 200, 300, 500 μM Incubation Time:4 h Result:Significantly increased the number of migrating cells by 2.4-fold compared with vehicle treatment. MLA (100 nM) completely blocked Varenicline-stimulated migration.

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Endocrinology/Hormones

AChR

α4β2 nAChR

Neurological Disease

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866823-63-4

284.18

C13H15Cl2N3

>98% (HPLC)

In Vitro:?DMSO : 62.5 mg/mL (219.93 mM)

Cl.Cl.c1c4c(cc2nccnc12)C3CC4CNC3

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(-20℃)

With Ice Pack

≥ 2 years