Varenicline Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
Varenicline, a partial agonist of the a4b2 nicotinic receptor, is a first-in-class
drug launched by Pfizer as an aid to smoking cessation treatment.
Varenicline exhibits dual action by decreasing craving and withdrawal symptoms,
and by decreasing the reinforcement associated with smoking. The addictive
properties of nicotine are thought to be mediated in part through its action as an agonist at α4β2 neuronal nicotinic acetylcholine receptors (nAChRs). Activation
of α4β2 receptors by nicotine increases the release of dopamine in the
mesolimbic system, an effect that is shared by most drugs of abuse. As nicotine
levels decrease, dopamine levels decline, which in turn stimulates the urge to
smoke. Additionally, a reduced dopaminergic tone due to abstinence from
smoking stimulates craving and the withdrawal syndrome. A partial agonist of
α4β2 receptors such as varenicline is expected to elicit a moderate and sustained
increase in dopamine levels to relieve craving and withdrawal symptoms. In
addition, by competitively binding to a4b2 receptors and inhibiting nicotineinduced
dopaminergic activation, a partial agonist could attenuate the pharmacologic
reward associated with smoking.
Verwenden
Varenicline is a useful medication for smoking cessation.
Definition
ChEBI: An organic heterotetracyclic compound that acts as a partial agonist for nicotinic cholinergic receptors and is used (in the form of its tartate salt) as an aid to giving up smoking.
Varenicline Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
