Varenicline tartrate

Bezeichnung:Varenicline tartrate

CAS-Nr375815-87-5

Englisch Name:Varenicline tartrate

CBNumberCB91011765

SummenformelC17H19N3O6

Molgewicht361.35

MOL-Datei375815-87-5.mol

Varenicline tartrate physikalisch-chemischer Eigenschaften

Schmelzpunkt	206-208°C
storage temp.	room temp
Löslichkeit	DMSO: >5mg/mL
Aggregatzustand	powder
Farbe	white to beige
Stabilität	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\|

Sicherheit

Kennzeichnung gefährlicher	Xn,N,T,F
R-Sätze:	22-50-39/23/24/25-23/24/25-11
S-Sätze:	22-57-45-36/37-16-7
RIDADR	UN 3077 9 / PGIII
WGK Germany	3

Gefahreninformationscode (GHS)

Varenicline tartrate Chemische Eigenschaften,Einsatz,Produktion Methoden

Chemische Eigenschaften
Tan Solid
Verwenden
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
Verwenden
Nicotinic α4β2 acetylcholine receptor partial agonist. Aid in smoking cessation.
Verwenden
Nicotinic a4? acetylcholine receptor partial agonist. Aid in smoking cessation.
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.
Trademarks
Chantix (Pfizer).
Biologische Aktivität
Orally active, subtype-selective partial agonist at α 4 β 2 nicotinic receptors (K i values are 0.06, 240, 322 and 3540 nM for α 4 β 2, α 3 β 4, α 7, α 1 β γ δ receptors respectively). Reduces nicotine-evoked dopamine release in vitro and decreases nicotine self-administration in vivo .
Biochem/physiol Actions
Varenicline tartrate is a partial α4β2 nicotinic receptor agonist and α7 full agonist. Varenicline competitively binds to α4β2 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 α4β2 receptors and stimulate the central nervous mesolimbic dopamine system, believed to be the neuronal mechanism underlying reinforcement and reward experienced upon smoking.
Lager
Room temperature

Varenicline tartrate Upstream-Materialien And Downstream Produkte

Varenicline tartrate Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

375815-87-5, Varenicline tartrate Verwandte Suche:

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