Varenicline tartrate
Varenicline tartrate
CAS: 375815-87-5
Molecular Formula: C17H19N3O6
Varenicline tartrate - Names and Identifiers
| Name | Varenicline tartrate |
| Synonyms | CS-291 Champix CP 526555-18 Varenicline tartrate VARENICLINE TARTRATE Varenicline Tartarate Varenicline tartrate for research ,10-Methano-6H-pyrazino[2,3-h][3]benzazepine, 7,8,9,10-tetrahydro- 7,8,9,10-Tetrahydro-6,10-methano-6H-pyrazino[2,3-h][3]benzazepine (2R,3R)-2,3- dihydroxybutanedioate |
| CAS | 375815-87-5 |
| EINECS | 638-780-5 |
| InChI | InChI=1/C13H13N3.C4H6O6/c1-2-16-13-5-11-9-3-8(6-14-7-9)10(11)4-12(13)15-1;5-1(3(7)8)2(6)4(9)10/h1-2,4-5,8-9,14H,3,6-7H2;1-2,5-6H,(H,7,8)(H,9,10)/t;1-,2-/m.0/s1 |
| InChIKey | TWYFGYXQSYOKLK-UHFFFAOYSA-N |
Varenicline tartrate - Physico-chemical Properties
| Molecular Formula | C17H19N3O6 |
| Molar Mass | 361.34926 |
| Melting Point | 206-208°C |
| Boling Point | 400.6°C at 760 mmHg |
| Flash Point | 196.1°C |
| Solubility | DMSO: >5mg/mL |
| Vapor Presure | 1.25E-06mmHg at 25°C |
| Appearance | powder |
| Color | white to beige |
| Storage Condition | room temp |
| In vitro study | In the nAChRs-expressing HEK cells, Varenicline is a partial agonist, and the efficacy of alpha3beta4 nAChRs is 45% of the maximum efficacy of nicotine. Varenicline is a potent, partial agonist at the alpha4beta2 receptor with an EC50 of 2.3 mM and an efficacy of 13.4% (relative to acetylcholine). Varenicline has lower efficacy and higher efficacy on the alpha3beta4 receptor, EC50 is 55 mM, the efficacy is 75%. |
| In vivo study | Varenicline stimulates [(3)H]-dopamine release from rat brain slices in vitro with significantly lower efficacy than nicotine (40-60% of nicotine), and increase the release of dopamine from the nucleus accumbens in rats, more effective than nicotine. Varenicline effectively attenuated nicotine-induced dopamine release to the level of effect of Varenicline alone, consistent with a partial agonistic effect. Varenicline reduces nicotine self-administration in rats and has a lower self-administration stop point than nicotine. Varenicline dose-dependently reduced nicotine self-administration and attenuated recovery induced by nicotine and nicotine-binding nicotine pairing cues. Varenicline, a partial agonist of alpha4beta2 nAChRs, reduces nicotine intake and was recently approved to aid smoking cessation. Varenicline selectively reduced ethanol uptake by an effective self-administered drinking regime, but did not affect sucrose uptake, in animals chronically exposed to ethanol for 2 months prior to Varenicline treatment, spontaneous ethanol consumption was also reduced, but water consumption was not affected. |
Varenicline tartrate - Risk and Safety
| Risk Codes | R22 - Harmful if swallowed R50 - Very Toxic to aquatic organisms R39/23/24/25 - R23/24/25 - Toxic by inhalation, in contact with skin and if swallowed. R11 - Highly Flammable |
| Safety Description | S22 - Do not breathe dust. S57 - Use appropriate container to avoid environmental contamination. S45 - In case of accident or if you feel unwell, seek medical advice immediately (show the label whenever possible.) S36/37 - Wear suitable protective clothing and gloves. S16 - Keep away from sources of ignition. S7 - Keep container tightly closed. |
| UN IDs | UN 3077 9 / PGIII |
| WGK Germany | 3 |
Varenicline tartrate - Reference Information
| overview | varenkline tartrate trade name Chang Pei, is a smoking cessation drug developed by Pfizer. Varenkine tartrate can effectively relieve nicotine craving and withdrawal symptoms, and can help reduce the pleasure of smoking during 12 weeks of treatment. |
| apply | varenkline tartrate and its acid addition salt as a drug for the prevention or treatment of the following diseases: inflammatory bowel disease (including but not limited to ulcerative colitis, pyoderma gangrenosum and Crohn's disease), irritable bowel syndrome, spastic dystonia, chronic pain, acute pain, abdominal cavity, vasoconstriction, anxiety, panic disorder, depression, bipolar disorder, autism, sleep disorders, jet lag, amyotrophic lateral sclerosis (ALS), cognitive dysfunction, etc. |
| biological activity | Varenicline Tartrate (CP 526555-18) is a nicotine AChR agonist used to treat smoking addiction. |
| Target | Value |
Last Update：2024-04-09 18:58:34
Supplier List
Product Name: Varenicline L-Tartrate Request for quotation
CAS: 375815-87-5
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
CAS: 375815-87-5
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Product Name: Varenicline L-Tartrate Request for quotation
CAS: 375815-87-5
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
CAS: 375815-87-5
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
View History