Chemical Name: Varenicline Tartrate
CAS No.: 375815-87-5
Molecular Formula: C17H19N3O6
Molecular Weight: 361.35
Varenicline tartrate CAS 375815-87-5
Description
Varenicline Tartrate Quick Details
Chemical Name: Varenicline Tartrate
CAS No.: 375815-87-5
Molecular Formula: C17H19N3O6
Chemical Structure:
Molecular Weight: 361.35
| Varenicline tartrate Chemical Properties |
| Melting point | 206-208°C |
| storage temp. | room temp |
| solubility | DMSO: >5mg/mL |
| form | powder |
| color | white to beige |
| Stability: | Hygroscopic |
| 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-/s3 |
| InChIKey | TWYFGYXQSYOKLK-UHFFFAOYSA-N |
| SMILES | [C@H](O)(C(=O)O)[C@@H](O)C(=O)O.C12=CC3=NC=CN=C3C=C1C1CNCC2C1 |&1:0,5,r| |
Varenicline tartrate Chemical Properties,Uses
Uses
- Nicotinic ??4±2acetylcholine receptor partial agonist. Aid in smoking cessation.
- Nicotinic ??4±2 acetylcholine receptor partial agonist. Aid in smoking cessation.
- Varenicline tartrate is a prescription medication used to treat smoking addiction. Varenicline is a nicotinic receptor partial agonist. In this respect, it is similar to cytisine and different from the nicotinic antagonist, bupropion, and nicotine replacement ther
Definition
ChEBI: A tartrate salt obtained by reaction of varenicline with one equivalent of (R,R)-tartaric acid. A partial agonist for nicotinic cholinergic receptors, it is used as an aid to giving up smoking.
Biological Activity
Orally active, subtype-selective partial agonist at ?? 4 ?? 2 nicotinic receptors (K i values are 0.06, 240, 322 and 3540 nM for ?? 4 ?? 2, ?? 3 ?? 4, ?? 7, ?? 1 ?? ?? ?? receptors respectively). Reduces nicotine-evoked dopamine release in vitro and decreases nicotine self-administration in vivo .
Biochem/physiol Actions
Varenicline tartrate is a partial ??4±2 nicotinic receptor agonist and ??7 full agonist. Varenicline competitively binds to ??4±2 receptors and partially stimulates without creating a full nicotine effect, while simultaneoudly blocking the ability of nicotine to bind to the receptors. Varenicline thus blocks the ability of nicotine to activate ??4±2 receptors and stimulate the central nervous mesolimbic dopamine system, believed to be the neuronal mechanism underlying reinforcement and reward experienced upon smoking.
Storage
Room temperature