Varenicline Hydrochloride

Varenicline Hydrochloride is a partial agonist of α4β2 nicotinic receptor for smoking cessation [1].

Varenicline Hydrochloride has been reported to potently inhibit nAChR binding with the Ki values of 0.12±0.02 nM and 0.14±0.01 nM for α6β2* nAChR and α4β2* nAChR, respectively in rat striatum, 0.13±0.01 nM and 0.19±0.11 nM forα6β2* nAChR and α4β2* nAChR, respectively in monkey striatum. In addition, varenicline Hydrochloride has shown to be more potent in stimulating both α6β2* and α4β2* nAChRs compared with nicotine with the EC50 values of 0.007 and 0.086μM, respectively in rat striatum [1].

References:
[1] Bordia T1, Hrachova M, Chin M, McIntosh JM, Quik M. Varenicline is a potent partial agonist at α6β2* nicotinic acetylcholine receptors in rat and monkey striatum. J Pharmacol Exp Ther. 2012 Aug;342(2):327-34. doi: 10.1124/jpet.112.194852. Epub 2012 May 1.

"Impact of Smoking Cessation Treatment" on Lung Function and Response Rate in EGFR Mutated Patients: A Short-Term Cohort Study.[Pubmed:26246248]

Recent Pat Anticancer Drug Discov. 2015;10(3):342-51.

BACKGROUND: Erlotinib is a validated drug "for the treatment of patients affected by advanced unresectable non small cell lung cancer (NSCLC) with EGFR mutations". We want to focus on potential functional benefits deriving from a combined therapy containing TKI (erlotinib) and a nicotinic partial agonist (varenicicline) in smokers. METHODS: we analyzed the records of patients affected by NSCLC treated undergoing "first line therapy with Erlotinib" and smoking cessation (with varenicicline). Response to therapy was evaluated by CT scan. Data concerning clinical history, smoking habit, nicotine dependence were collected after three months from the beginning of the recruitment. Pulmonary function tests including spirometry with pletismographic technique and exhaled carbon monoxide (CO) were performed with recording of resistances, flows, volumes. A group of ten current smokers affected by NSCLC with EGFR activating mutation and concurrent mild COPD undergoing anti-EGFR treatment without smoking cessation was used to compare clinical and functional data. A control group of NSCLC wild type with mild COPD undergoing smoking cessation was assessed for functional data. RESULTS: Twenty-five patients were enrolled. All of them reported partial response at CT re-evaluation. All functional indexes and parameters were improved after combined treatment a significant increase of FEV1 level and a decrease of exhaled CO. In particular, a mean increase of FEV1 from 1.93 (SD 0.48) to 2.03(SD 0.46) liters was recorded. A notable reduction of sRAW (specific resistances) was also observed. The improvement of some parameters such as CO, heart rate (HR), sRAW and FEV1 resulted statistically significant. A better response to therapy was found "in the study group compared to the second group of mutated NSCLC patients". In this second group, we also observed an improvement of functional obstructive parameters although it was less remarkable than study group. Only sRAW and FEF 25/75 were significantly increased. The group of NSCLC wild type undergoing only smoking cessation showed a lower increase of FEV1 by about 50 ml compared to the first group. CONCLUSION: The combination of anti-EGFR treatment and concurrent therapy for smoking cessation seems to be more effective than erlotinib alone in improving lung function and clinical response in advanced NSCLC patients with EGFR-mutations. It is conceivable that erlotinib may potentiate the action of varenicline. We have also outlined some relevant patents concerning varenicline and EGFR-TKI.

Neuroimaging the Effectiveness of Substance Use Disorder Treatments.[Pubmed:27184387]

J Neuroimmune Pharmacol. 2016 Sep;11(3):408-33.

Neuroimaging techniques to measure the function and biochemistry of the human brain such as positron emission tomography (PET), proton magnetic resonance spectroscopy ((1)H MRS), and functional magnetic resonance imaging (fMRI), are powerful tools for assessing neurobiological mechanisms underlying the response to treatments in substance use disorders. Here, we review the neuroimaging literature on pharmacological and behavioral treatment in substance use disorder. We focus on neural effects of medications that reduce craving (e.g., naltrexone, bupropion hydrochloride, baclofen, methadone, varenicline) and that improve cognitive control (e.g., modafinil, N-acetylcysteine), of behavioral treatments for substance use disorders (e.g., cognitive bias modification training, virtual reality, motivational interventions) and neuromodulatory interventions such as neurofeedback and transcranial magnetic stimulation. A consistent finding for the effectiveness of therapeutic interventions identifies the improvement of executive control networks and the dampening of limbic activation, highlighting their values as targets for therapeutic interventions in substance use disorders.

American Psychiatric Association - 168th Annual Meeting (May 16-20, 2015 - Toronto, Canada).[Pubmed:26261851]

Drugs Today (Barc). 2015 Jun;51(6):375-82.

The theme of this year's American Psychiatric Association (APA) meeting was 'Psychiatry: integrating body and mind, heart and soul', with special focus given to advances in basic and cognitive neuroscience and how these may contribute to integrated care of mental health and illness. The program featured numerous tracks and subtracks in areas of interest such as addiction psychiatry, child, adolescent and geriatric psychiatry, and psychosomatic medicine.

Emerging drugs for the treatment of tobacco dependence: 2014 update.[Pubmed:24654737]

Expert Opin Emerg Drugs. 2014 Jun;19(2):243-60.

INTRODUCTION: Tobacco dependence remains a global epidemic and the largest preventable cause of morbidity and mortality around the world. Smoking cessation has benefits at all ages but remains challenging for several reasons, among which are the complexities of nicotine addiction and limitations of available pharmacotherapies. AREAS COVERED: This review summarizes current and emerging pharmacotherapies for the treatment of tobacco dependence, including first- and second-line recommended agents. Medications with alternative primary indications that have been investigated as potential treatments for tobacco dependence are also discussed. Articles reviewed were obtained through searches of PubMed, Ovid MEDLINE, ClinicalTrials.gov and the Pharmaprojects database. EXPERT OPINION: Current evidence suggests that the two most effective pharmacotherapies to treat tobacco dependence are varenicline and combination nicotine replacement therapy. Alternative agents investigated demonstrate mixed rates of success in achieving long-term abstinence from smoking. No single pharmacotherapy will serve as a universally successful treatment given the complex underpinnings of tobacco dependence and individuality of smokers. The ultimate goal of tobacco research with respect to pharmacotherapeutic development continues to be providing clinicians with an armamentarium of drugs to choose from allowing for tailoring of treatment for smokers.

Varenicline Hydrochloride (CP 526555 hydrochloride) is a high affinity, selective α4β2 nicotine acetylcholine receptor (nAChR) partial agonist and full α7 nAChR agonist. Varenicline Hydrochloride is also a potent partial agonist of α6β2 nAChR in striatum of rats with a Ki value of 0.12 nM.

Varenicline Hydrochloride,230615-23-3,CP 526555 hydrochloride; Champix hydrochloride; Chantix hydrochloride,Natural Products,Nicotinic Receptor, buy Varenicline Hydrochloride , Varenicline Hydrochloride supplier , purchase Varenicline Hydrochloride , Varenicline Hydrochloride cost , Varenicline Hydrochloride manufacturer , order Varenicline Hydrochloride , high purity Varenicline Hydrochloride