Varenicline tartrate

Chemical properties

Tan Solid

The Uses of Varenicline tartrate

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

The Uses of Varenicline tartrate

Nicotinic a4? acetylcholine receptor partial agonist. Aid in smoking cessation.

The Uses of Varenicline tartrate

Nicotinic α4β2 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.

brand name

Chantix (Pfizer).

Biological Activity

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.

storage

Room temperature