866823-63-4
866823-63-4 structure
- Name: Varenicline (CP 526555) dihydrochloride
- Chemical Name: 6,10-Methano-6H-pyrazino[2,3-h][3]benzazepine, 7,8,9,10-tetrahydro-, dihydrochloride
- CAS Number: 866823-63-4
- Molecular Formula: C13H14ClN3
- Molecular Weight: 247.72300
- Catalog: Signaling Pathways Membrane Transporter/Ion Channel nAChR
- Create Date: 2017-09-12 02:26:17
- Modify Date: 2024-01-13 22:59:49
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Varenicline (CP 526555) dihydrochloride is a potent partial agonist for α4β2 nicotinic acetylcholine receptor (nAChR) with an EC50 value of 2.3 μM. Varenicline dihydrochloride is a full agonist for α3β4 and α7 nAChRs with EC50 values of 55 μM and 18 μM, respectively[2]. Varenicline dihydrochloride is a nicotinic ligand based on the structure of cytosine, and has the potential for smoking cessation treatment[5].
| Name | 6,10-Methano-6H-pyrazino[2,3-h][3]benzazepine, 7,8,9,10-tetrahydro-, dihydrochloride |
|---|---|
| Synonyms |
VARENICLINE-D4 DIHYDROCHLORIDE (MAJOR)
7,8,9,10-tetrahydro-6,10-Methano-6H-pyrazino[2,3-h][3]benzazepine dihydrochloride |
| Description | Varenicline (CP 526555) dihydrochloride is a potent partial agonist for α4β2 nicotinic acetylcholine receptor (nAChR) with an EC50 value of 2.3 μM. Varenicline dihydrochloride is a full agonist for α3β4 and α7 nAChRs with EC50 values of 55 μM and 18 μM, respectively[2]. Varenicline dihydrochloride is a nicotinic ligand based on the structure of cytosine, and has the potential for smoking cessation treatment[5]. |
|---|---|
| Related Catalog | |
| Target |
EC50: 2.3 μM (α4β2 nAChR); 18 μM (α7 nAChR); 55 μM (α3β4 nAChR)[2] |
| In Vitro | Varenicline dihydrochloride (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[1]. Varenicline dihydrochloride (250 nM) evokes action potentials (Aps) in the absence of ACh stimulation in Human adrenal chromaffin cells isolated from male and female organ donors[3]. Varenicline dihydrochloride (100 μM, 4 h) promotes migration of HUVECs by lowering the protein expression of VE-cadherin[4]. Cell Proliferation Assay[1] Cell Line: RAW 264.7 murine macrophage cells (treated with 4 μg/mL LPS for 24 h) Concentration: 1 μM Incubation Time: 0-48 h Result: Decreased the LPS-induced cell proliferation rate. Western Blot Analysis[4] Cell Line: HUVECs Concentration: 1, 10, 100 μM Incubation Time: 24 h or 30 min Result: Decreased the protein expression of VE-cadherin and activated ERK1/2, p38 and JNK signaling. |
| In Vivo | Varenicline dihydrochloride (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)[5]. Varenicline dihydrochloride (Subcutaneous injection, 2.5 mg/kg, 3 days) results in a place aversion which is dependent on α5 nAChRs but not β2 nAChRs[5]. Varenicline dihydrochloride (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[5]. Animal Model: ICR male mice[5] Dosage: 0.01-1 mg/kg for 3 days Administration: Subcutaneous injection Result: Inhibited nicotine conditioned place preference (CPP) in a dose dependent manner. |
| References |
| Molecular Formula | C13H14ClN3 |
|---|---|
| Molecular Weight | 247.72300 |
| Exact Mass | 247.08800 |
| PSA | 37.81000 |
| LogP | 2.93470 |
| Storage condition | -20°C |