Varenicline tartrate is an orally active, subtype-selective partial agonist at alpha4beta2 nicotinic receptors with Ki values of 0.06, 240, 322 and 3540 nM for alpha4beta2, alpha3beta4, alpha7, alpha1betaidelta receptors respectively, and a full agonist at alpha7 neuronal nicotinic receptors. In humans, following oral administration, varenicline is almost completely absorbed and has high bioavailability (90%). Varenicline stimulates basal mesolimbic dopamine release to approximately 50% of the maximal effect of nicotine, inhibits nicotine-induced dopamine release, and reduces nicotine self-administration. Varenicline is a clinically useful smoking cessation agent.
Molekulargewicht:
361.35
Reinheit:
>98% by HPLC, NMR conforms
Formulierung:
Yellow solid
CAS Nummer:
[375815-87-5]
Formel:
C13H13N3C4H6O6
Target-Kategorie:
Nicotinic acetylcholine receptors
Anwendungsbeschreibung:
ProductType: Small molecules
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