Varenicline - CAS 249296-44-4
Catalog number: B0084-064059
Category: Inhibitor
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Molecular Formula:
C13H13N3
Molecular Weight:
211.26
COA:
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Targets:
nAChR
Description:
Varenicline(CP 526555; Champix; Chantix) is a prescription medication used to treat smoking addiction. As a partial agonist it both reduces cravings for and decreases the pleasurable effects of cigarettes and other tobacco products. Through these mechanisms Varenicline(CP 526555; Champix; Chantix) can assist some patients to quit smoking.
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-064059 1 g $499 In stock
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Purity:
>98%
Synonyms:
CP 526555; Champix; Chantix; CP526555; CP-526555
MSDS:
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InChIKey:
JQSHBVHOMNKWFT-UHFFFAOYSA-N
InChI:
InChI=1S/C13H13N3/c1-2-16-13-5-11-9-3-8(6-14-7-9)10(11)4-12(13)15-1/h1-2,4-5,8-9,14H,3,6-7H2
Canonical SMILES:
C1C2CNCC1C3=CC4=NC=CN=C4C=C23
1. Effectiveness of varenicline versus nicotine replacement therapy for smoking cessation with minimal professional support: evidence from an English population study
Daniel Kotz & Jamie Brown & Robert West. Psychopharmacology (2014) 231:37–42
Several pharmacological treatments can improve the chance of successful quitting. Varenicline, a partial α4β2 receptor agonist, has been shown to be more effective than placebo and bupropion in achieving long-term abstinence from smoking (Gonzales et al. 2006; Jorenby et al. 2006). Few randomised controlled trials, however, have directly compared the efficacy of varenicline with nicotine replacement therapy (NRT), which has been the most widely used smoking cessation drug for decades. One large-scale (N=746) multi-national trial showed that, in the context of intensive behavioural support, varenicline was more effective than NRT transdermal patch in achieving short-term (end-of-treatment) abstinence (Aubin et al.2008). However, this trial as well as a medium-scale (N=272) trial from Iran (Heydari et al. 2012) and a small-scale (N=28) trial from Japan (Tsukahara et al. 2010) did not provide strong evi-dence for the long-term superiority (abstinence at 6 to 12 months post-treatment).
2. Varenicline for smoking cessation in people with schizophrenia: systematic review and meta-analysis
Taro Kishi• Nakao Iwata. Eur Arch Psychiatry Clin Neurosci (2015) 265:259–268
The α4β2 nicotinic acetylcholine receptors (nAChRs) are linked to the reinforcing effects of nicotine and to maintaining smoking behavior. Varenicline, which is a partial agonist ofα4β2 nAChR and a full agonist ofα7 nAChRs, has the potential to relieve nicotine craving and withdrawal symp-toms while decreasing the reinforcing effects of nicotine. To our knowledge, only 1 meta-analysis of double-blind ran-domized placebo-controlled trials (RCTs) on the effects of varenicline adjuvant therapy for smoking cessation among people with schizophrenia has been published. This study showed that varenicline was not superior to placebo in smoking cessation rates (2 RCTs,n=137). Varenicline blocks nicotine from binding to the nAChR and prevents nicotine-induced dopamine release in the ventral tegmental area. The nicotinic receptor, α4β2 nAChR, increases dopa-mine transmission throughout the brain. Therefore, its partial agonism by varenicline is considered to increase the incidence of psychiatric adverse events because dopamine is hypothe-sized to be involved in the development and continuation of various psychiatric illnesses, including schizophrenia and mood disorders. On the other hand, accumulating evidence suggests thatα7 nAChRs plays a role in the path-ogenesis of schizophrenia. Hong et al. reported that in individuals with schizophrenia, treatment with varen-icline reduced the sensory gating deficit and improved exec-utive function compared witha placebo. Lieberman et al. reported that the α7 nAChRs partial agonist TC-5619 shows statistically significant improvements in negative symptoms and cognitive function (executive function) in individuals with schizophrenia compared with a placebo.
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CAS 249296-44-4 Varenicline

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