PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 27613505-3 2016 Varenicline is a nAChR partial agonist that may improve cognitive deficits in both smokers and non-smokers with schizophrenia; however, the mechanism by which varenicline alters cognition in schizophrenia remains unclear. Varenicline 0-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 17-22 27123827-5 2016 In addition, with varenicline, the dopamine D1 receptor (DRD1) antibody titer as well as the percent of baseline calmodulin-dependent protein kinase II (CaM KII) activity dropped significantly. Varenicline 18-29 dopamine receptor D1 Homo sapiens 35-55 27123827-5 2016 In addition, with varenicline, the dopamine D1 receptor (DRD1) antibody titer as well as the percent of baseline calmodulin-dependent protein kinase II (CaM KII) activity dropped significantly. Varenicline 18-29 dopamine receptor D1 Homo sapiens 57-61 27123827-5 2016 In addition, with varenicline, the dopamine D1 receptor (DRD1) antibody titer as well as the percent of baseline calmodulin-dependent protein kinase II (CaM KII) activity dropped significantly. Varenicline 18-29 calcium/calmodulin dependent protein kinase II gamma Homo sapiens 113-151 27123827-5 2016 In addition, with varenicline, the dopamine D1 receptor (DRD1) antibody titer as well as the percent of baseline calmodulin-dependent protein kinase II (CaM KII) activity dropped significantly. Varenicline 18-29 calcium/calmodulin dependent protein kinase II gamma Homo sapiens 153-160 26192545-0 2015 Chronic treatment with varenicline changes expression of four nAChR binding sites in mice. Varenicline 23-34 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 62-67 27012889-0 2016 Effects of varenicline on alpha4-containing nicotinic acetylcholine receptor expression and cognitive performance in mice. Varenicline 11-22 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 44-76 27012889-2 2016 The impact of the smoking cessation aid varenicline, a selective partial alpha4beta2 nAChR agonist, on (1) changes of central protein and mRNA expression of this receptor and (2) on memory deficits in a mouse model of cognitive impairment was investigated. Varenicline 40-51 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 85-90 27012889-8 2016 Varenicline dose-dependently increased protein expression of both the alpha4 and beta2 subunit in cell cultures and brain tissues, respectively, but had no effect on mRNA expression of both subunits. Varenicline 0-11 hemoglobin, beta adult minor chain Mus musculus 81-86 26446070-8 2016 Varenicline versus placebo outcomes demonstrated that varenicline was more effective for women for short and intermediate outcomes (PP-12, CA-12, CA-24; P < .05 sex x medication interaction). Varenicline 54-65 carbonic anhydrase 12 Homo sapiens 139-144 26446070-10 2016 For continuous abstinence, varenicline was 34% (CA-12) and 31% (CA-24) more effective for women. Varenicline 27-38 carbonic anhydrase 12 Homo sapiens 48-53 27089092-1 2016 Varenicline increased smoking cessation at 24 weeks in patients hospitalized with ACS and motivated to quit. Varenicline 0-11 1-aminocyclopropane-1-carboxylate synthase homolog (inactive) Homo sapiens 82-85 26594837-10 2016 From the network meta-analysis, both bupropion and varenicline were more effective than placebo [odds ratio (OR) = 4.51, 95% credible interval (CrI) = 1.45-14.04 and OR = 5.17, 95% CrI = 1.78-15.06, respectively]. Varenicline 51-62 EP300 interacting inhibitor of differentiation 1 Homo sapiens 125-152 26910582-1 2016 The tobacco-dependence pharmacotherapies varenicline and cytisine act as partial alpha4beta2 nAChR agonists. Varenicline 41-52 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 93-98 27028298-3 2016 We report that varenicline, an FDA-approved nicotinic acetylcholine receptor (nAChR) partial agonist that modulates dopamine in the mesolimbic reward pathway of the brain, significantly reduces sucrose consumption, especially in a long-term consumption paradigm. Varenicline 15-26 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 44-76 27028298-3 2016 We report that varenicline, an FDA-approved nicotinic acetylcholine receptor (nAChR) partial agonist that modulates dopamine in the mesolimbic reward pathway of the brain, significantly reduces sucrose consumption, especially in a long-term consumption paradigm. Varenicline 15-26 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 78-83 27028298-6 2016 Taken together, our results suggest that nAChR drugs such as varenicline may represent a novel treatment strategy for reducing sugar consumption. Varenicline 61-72 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 41-46 26192545-3 2015 Varenicline, like nicotine, upregulates the alpha4beta2-nAChR sites; however, it is not known whether varenicline treatment changes expression of the other nAChR subtypes. Varenicline 0-11 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 56-61 26192545-5 2015 RESULTS: The upregulation of alpha4beta2-nAChR sites elicited by chronic varenicline was very similar to that elicited by chronic nicotine. Varenicline 73-84 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 41-46 26192545-8 2015 Varenicline significantly increased both alpha3beta4-and alpha7-nAChR sites while nicotine had less effect on these sites. Varenicline 0-11 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 64-69 25449275-3 2014 In this study, we determined if varenicline increases the risk of cardiovascular events using apolipoprotein E knockout (ApoE KO) mice. Varenicline 32-43 apolipoprotein E Mus musculus 94-110 26049061-0 2015 Analysis of gait in rats with olivocerebellar lesions and ability of the nicotinic acetylcholine receptor agonist varenicline to attenuate impairments. Varenicline 114-125 cholinergic receptor nicotinic alpha 2 subunit Rattus norvegicus 73-105 26142345-2 2015 This study tests whether the coding variant rs16969968 in the CHRNA5 nicotinic receptor gene predicts the effects of combination nicotine replacement therapy (cNRT) and varenicline on treatment outcomes. Varenicline 169-180 cholinergic receptor nicotinic alpha 5 subunit Homo sapiens 62-68 25774163-0 2015 CHRNA4 rs1044396 is associated with smoking cessation in varenicline therapy. Varenicline 57-68 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 0-6 25774163-10 2015 CONCLUSION: The CHRNA4 rs1044396 is associated with smoking cessation in individuals on varenicline therapy. Varenicline 88-99 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 16-22 25475645-5 2015 The allosteric sites found at the extracellular domain (EXD) of halpha3beta4 and halpha4beta2 nAChRs could explain the partial agonistic activity of varenicline on these nAChR subtypes. Varenicline 149-160 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 94-99 25475645-6 2015 Molecular dynamics simulations show that the interaction of varenicline to each allosteric site decreases the capping of Loop C at the halpha4beta2 nAChR, suggesting that these allosteric interactions limit the initial step in the gating process. Varenicline 60-71 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 148-153 25485645-0 2015 The effects of varenicline on sensory gating and exploratory behavior with pretreatment with nicotinic or 5-HT3A receptor antagonists. Varenicline 15-26 5-hydroxytryptamine receptor 3A Homo sapiens 106-112 25485645-3 2015 Varenicline, a nonselective neuronal nicotinic receptor (NNR) agonist and full agonist of 5-HT3A receptors, helps reduce smoking among schizophrenic patients. Varenicline 0-11 5-hydroxytryptamine receptor 3A Homo sapiens 90-96 25485645-8 2015 Collectively, these results indicate that varenicline at low-to-moderate doses may be beneficial against impaired sensory gating in schizophrenia; however, higher doses may induce anxiogenic effects, which can be prevented with antagonists of NNRs or 5-HT3A receptors. Varenicline 42-53 5-hydroxytryptamine receptor 3A Homo sapiens 251-257 25449275-6 2014 Methyllycaconitine, an alpha7 nicotinic acetylcholine receptor (nAChR) antagonist, inhibited varenicline-induced aggravated plaque formation. Varenicline 93-104 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 64-69 25449275-7 2014 Our findings show that varenicline progresses atherosclerotic plaque formation through alpha7 nAChR, and thereby increases the risk of cardiovascular events. Varenicline 23-34 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 87-99 25581658-1 2014 BACKGROUND: Varenicline, a partial nicotinic acetylcholine receptor (nAChR) agonist, is a promising new drug for the treatment of alcohol (ethanol [EtOH]) dependence. Varenicline 12-23 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 35-67 25581658-1 2014 BACKGROUND: Varenicline, a partial nicotinic acetylcholine receptor (nAChR) agonist, is a promising new drug for the treatment of alcohol (ethanol [EtOH]) dependence. Varenicline 12-23 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 69-74 24674749-0 2014 Twelve weeks of smoking cessation therapy with varenicline increases the serum levels of apolipoprotein A-I only in the success group. Varenicline 47-58 apolipoprotein A1 Homo sapiens 89-107 24836728-8 2014 Preclinical and clinical studies also show that the nAChR agonist varenicline improves balance and coordination in various ataxias. Varenicline 66-77 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 52-57 24674749-12 2014 CONCLUSION: These findings suggest that successful smoking cessation therapy with varenicline improves serum apoA-I and HDL-C levels in the short term. Varenicline 82-93 apolipoprotein A1 Homo sapiens 109-115 25063196-11 2014 Varenicline, a partial nicotinic acetylcholine receptor agonist that, like nicotine, induces miR-153 expression, also prevented and reversed the effects of ethanol exposure. Varenicline 0-11 microRNA 153 Mus musculus 93-100 24627467-2 2014 Relative success in abstinence has been found with the nAChR partial agonist varenicline (Chantix; Pfizer, Groton, CT); however, treatment with this drug fails to alleviate anxiety in individuals during nicotine withdrawal. Varenicline 77-88 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 55-60 25071576-3 2014 OBJECTIVE: To evaluate the effects of 12-week varenicline administration on glutamate levels in the dorsal anterior cingulate cortex (dACC) and functional changes within the cognitive control network. Varenicline 46-57 Acetyl-CoA carboxylase Drosophila melanogaster 134-138 25071576-9 2014 CONCLUSIONS: These results suggest possible mechanisms of action for varenicline such as reduction in Glx levels in dACC and shifts in BOLD connectivity between large scale brain networks. Varenicline 69-80 Acetyl-CoA carboxylase Drosophila melanogaster 116-120 24628360-1 2014 BACKGROUND AND PURPOSE: Varenicline, a neuronal nicotinic acetylcholine receptor (nAChR) modulator, decreases ethanol consumption in rodents and humans. Varenicline 24-35 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 48-80 24628360-1 2014 BACKGROUND AND PURPOSE: Varenicline, a neuronal nicotinic acetylcholine receptor (nAChR) modulator, decreases ethanol consumption in rodents and humans. Varenicline 24-35 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 82-87 24406270-0 2014 Functional interactions of varenicline and nicotine with nAChR subtypes implicated in cardiovascular control. Varenicline 27-38 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 57-62 24422997-7 2014 After increasing nAChRs in the rodent brain with chronic nicotine, replacing nicotine with chronic varenicline maintained the increased nAChR binding, as well as the alpha4beta2 subunit proteins measured by western blots. Varenicline 99-110 cholinergic receptor nicotinic beta 1 subunit Rattus norvegicus 17-22 24627467-2 2014 Relative success in abstinence has been found with the nAChR partial agonist varenicline (Chantix; Pfizer, Groton, CT); however, treatment with this drug fails to alleviate anxiety in individuals during nicotine withdrawal. Varenicline 90-97 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 55-60 24418350-16 2014 Also, varenicline for SCA3 patients (level B) can be considered. Varenicline 6-17 ataxin 3 Homo sapiens 22-26 24671929-19 2014 The trial of varenicline did show a significant effect on long-term smoking cessation (RR 1.45; 95% CI 1.01 to 2.07, 1 trial, 286 participants).Seven trials examined the effect of smoking intervention on postoperative complications. Varenicline 13-24 ribonucleotide reductase catalytic subunit M1 Homo sapiens 87-91 24484986-3 2014 Varenicline and cytisine are partial agonists at the alpha4beta2* nicotinic acetylcholine receptor (nAChR). Varenicline 0-11 cholinergic receptor nicotinic beta 1 subunit Rattus norvegicus 100-105 23966067-3 2014 The partial alpha4/alpha6/beta2* nicotinic acetylcholine receptor (nAChR) agonists varenicline and cytisine are widely used as smoking cessation treatments. Varenicline 83-94 cholinergic receptor nicotinic beta 1 subunit Rattus norvegicus 67-72 23639435-7 2013 The Cu,b of the alpha4beta2 nAChR partial agonist varenicline, which has antidepressant-like activity in a murine model, is higher than its IC50 and varenicline is projected to cause ~70% inhibition of alpha4beta2 nAChRs. Varenicline 50-61 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 28-33 23639435-7 2013 The Cu,b of the alpha4beta2 nAChR partial agonist varenicline, which has antidepressant-like activity in a murine model, is higher than its IC50 and varenicline is projected to cause ~70% inhibition of alpha4beta2 nAChRs. Varenicline 149-160 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 28-33 23872372-2 2013 Pre-clinical and clinical studies have shown that neuronal nicotinic acetylcholine receptor (nAChR) partial agonists such as cytisine and its derivative, varenicline, reduce alcohol (ethanol) consumption and seeking behavior. Varenicline 154-165 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 59-91 23872372-2 2013 Pre-clinical and clinical studies have shown that neuronal nicotinic acetylcholine receptor (nAChR) partial agonists such as cytisine and its derivative, varenicline, reduce alcohol (ethanol) consumption and seeking behavior. Varenicline 154-165 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 93-98 23801676-3 2013 We also present a receptor blocking study in a nicotine subject dosed with the alpha4beta2-nAChR-selective partial agonist varenicline. Varenicline 123-134 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 91-96 23344555-0 2013 Varenicline and cytisine: two nicotinic acetylcholine receptor ligands reduce ethanol intake in University of Chile bibulous rats. Varenicline 0-11 cholinergic receptor nicotinic alpha 2 subunit Rattus norvegicus 30-62 23344555-2 2013 Varenicline and cytisine are nAChR partial agonists in clinical use as smoking cessation aids. Varenicline 0-11 cholinergic receptor nicotinic beta 1 subunit Rattus norvegicus 29-34 23352971-0 2013 Varenicline and nicotine enhance GABAergic synaptic transmission in rat CA1 hippocampal and medial septum/diagonal band neurons. Varenicline 0-11 carbonic anhydrase 1 Rattus norvegicus 72-75 23641218-9 2013 The smoking cessation therapeutic and nAChR partial agonist, varenicline, reduces alcohol consumption in heavy drinking smokers and rodent models of alcohol consumption. Varenicline 61-72 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 38-43 23352971-5 2013 KEY FINDINGS: Both varenicline (10 muM) and nicotine (10 muM) applications alone resulted in small but significant increases in amplitude, as well as robustly enhanced frequency of mIPSCs in hippocampal CA1 pyramidal neurons and medial septum/diagonal band (MS/DB) neurons. Varenicline 19-30 carbonic anhydrase 1 Rattus norvegicus 203-206 23042213-4 2013 The alpha7 nAChR agonists varenicline and JN403, but not the alpha4beta2 nAChR agonist cytisine, increased the 3H-PIB binding in autopsy tissue homogenates from AD and control frontal cortex. Varenicline 26-37 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 11-16 23110878-5 2013 During the amygdala reactivity paradigm, nicotinic acetylcholine receptor (nAChR) stimulation by nicotine and varenicline decreased reaction time (RT) in abstinent smokers but not in nonsmokers. Varenicline 110-121 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 41-73 23110878-5 2013 During the amygdala reactivity paradigm, nicotinic acetylcholine receptor (nAChR) stimulation by nicotine and varenicline decreased reaction time (RT) in abstinent smokers but not in nonsmokers. Varenicline 110-121 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 75-80 22899752-8 2012 We used a newly developed method involving radioligand binding to measure the concentrations and nAChR occupancy of saz-A, nicotine, and varenicline in brains from chronically treated rats. Varenicline 137-148 cholinergic receptor nicotinic beta 1 subunit Rattus norvegicus 97-102 22547331-2 2012 The nAChR alpha4beta2 subunit partial agonist varenicline (Chantix ), which is approved by the Food and Drug Administration for smoking cessation, also decreases ethanol consumption in rodents (Steensland et al., Proc Natl Acad Sci U S A 104:12518-12523, 2007) and in human laboratory and open-label studies (Fucito et al., Psychopharmacology (Berl) 215:655-663, 2011; McKee et al., Biol Psychiatry 66:185-190 2009). Varenicline 46-57 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 4-9 22547331-2 2012 The nAChR alpha4beta2 subunit partial agonist varenicline (Chantix ), which is approved by the Food and Drug Administration for smoking cessation, also decreases ethanol consumption in rodents (Steensland et al., Proc Natl Acad Sci U S A 104:12518-12523, 2007) and in human laboratory and open-label studies (Fucito et al., Psychopharmacology (Berl) 215:655-663, 2011; McKee et al., Biol Psychiatry 66:185-190 2009). Varenicline 59-66 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 4-9 22678099-10 2012 Overall, our results suggest that the antagonistic actions of varenicline at low doses are mediated by beta2*-nAChRs and at higher doses as an agonist by alpha3beta4*-nAChRs. Varenicline 62-73 hemoglobin, beta adult minor chain Mus musculus 103-108 22550286-4 2012 Receptor competition studies showed that varenicline inhibited alpha6beta2* nAChR binding (K(i) = 0.12 nM) as potently as alpha4beta2* nAChR binding (K(i) = 0.14 nM) in rat striatal sections and with ~20-fold greater affinity than nicotine. Varenicline 41-52 cholinergic receptor nicotinic beta 1 subunit Rattus norvegicus 76-81 22580377-7 2012 Our data indicated lower efficacy for varenicline and cytisine than expected for beta4-containing receptors, based on previous studies of rodent receptors. Varenicline 38-49 tubulin beta 3 class III Homo sapiens 81-86 22580377-8 2012 We confirm that these therapeutically important alpha4 receptor partial agonists may present different autonomic-based side-effect profiles in humans than will be seen in rodent models, with varenicline being more potent for human than rat receptors and cytisine less potent. Varenicline 191-202 immunoglobulin binding protein 1 Homo sapiens 48-54 22550286-5 2012 Functionally, varenicline was more potent in stimulating alpha6beta2* versus alpha4beta2* nAChR-mediated [(3)H]dopamine release from rat striatal synaptosomes with EC(50) values of 0.007 and 0.086 muM, respectively. Varenicline 14-25 cholinergic receptor nicotinic beta 1 subunit Rattus norvegicus 90-95 22261145-1 2012 INTRODUCTION: Ex vivo storage phosphor imaging rat studies reported increased brain dopamine D2/3 receptor (DRD2/3) availability following treatment with varenicline, a nicotinergic drug. Varenicline 154-165 dopamine receptor D2 Rattus norvegicus 108-114 22261145-7 2012 RESULTS: Significantly increased striatal DRD2/3 availability was found following varenicline treatment compared to saline (time*treatment effect): posttreatment difference in binding potential between groups corrected for initial baseline differences was 2.039 (P=.022), indicating a large effect size (d=1.48). Varenicline 82-93 dopamine receptor D2 Rattus norvegicus 42-46 22261145-8 2012 CONCLUSIONS: Ultra-high-resolution pinhole SPECT can be used to assess varenicline-induced changes in DRD2/3 availability in small laboratory animals over time. Varenicline 71-82 dopamine receptor D2 Rattus norvegicus 102-106 22241831-0 2012 Varenicline blocks beta2*-nAChR-mediated response and activates beta4*-nAChR-mediated responses in mice in vivo. Varenicline 0-11 hemoglobin, beta adult minor chain Mus musculus 19-24 22241831-0 2012 Varenicline blocks beta2*-nAChR-mediated response and activates beta4*-nAChR-mediated responses in mice in vivo. Varenicline 0-11 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 26-31 22241831-0 2012 Varenicline blocks beta2*-nAChR-mediated response and activates beta4*-nAChR-mediated responses in mice in vivo. Varenicline 0-11 basic helix-loop-helix family, member e23 Mus musculus 64-69 22241831-0 2012 Varenicline blocks beta2*-nAChR-mediated response and activates beta4*-nAChR-mediated responses in mice in vivo. Varenicline 0-11 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 71-76 22241831-1 2012 INTRODUCTION: The smoking cessation aid, varenicline, has higher affinity for the alpha4beta2-subtype of the nicotinic acetylcholine receptor (alpha4beta2*-nAChR) than for other subtypes of nAChRs by in vitro assays. Varenicline 41-52 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 156-161 22241831-7 2012 Null mutation of the alpha7- or beta2-nAChR subunit did not decrease the effectiveness of varenicline; however, null mutation of the beta4 subunit significantly decreased the magnitude of the varenicline effect. Varenicline 192-203 basic helix-loop-helix family, member e23 Mus musculus 133-138 22241831-10 2012 Using a dose of nicotine selective for beta2*-nAChR subtype effects with these tests, dose-dependent antagonism by varenicline was seen. Varenicline 115-126 hemoglobin, beta adult minor chain Mus musculus 39-44 22241831-10 2012 Using a dose of nicotine selective for beta2*-nAChR subtype effects with these tests, dose-dependent antagonism by varenicline was seen. Varenicline 115-126 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 46-51 22241831-12 2012 CONCLUSIONS: Varenicline acts as a functional antagonist of beta2*-nAChRs, blocking certain effects of nicotine. Varenicline 13-24 hemoglobin, beta adult minor chain Mus musculus 60-65 22241831-13 2012 At higher doses, varenicline is an agonist of beta4*-nAChRs producing physiological changes in mice. Varenicline 17-28 basic helix-loop-helix family, member e23 Mus musculus 46-51 21778151-7 2012 Over the course of treatment, participants receiving varenicline reduced from 14.1 +- 6.3 (mean +- SD) to 0.9 +- 2.1 cigarettes/day (CPD, 4 achieved abstinence), while those receiving bupropion XL reduced from 15.8 +- 4.4 to 3.1 +- 4.0 CPD (2 achieved abstinence). Varenicline 53-64 inositol polyphosphate-5-phosphatase E Homo sapiens 133-139 22395733-1 2012 The primary objective of this project was to determine the alpha4beta2(*) nicotinic acetylcholine receptor (nAChR) occupancy in human brain of a single low dose of varenicline (0.5 mg), and to explore the relationship between receptor occupancy by varenicline and tobacco withdrawal symptoms ((*)denoting other putative nAChR subunits). Varenicline 164-175 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 74-106 22395733-1 2012 The primary objective of this project was to determine the alpha4beta2(*) nicotinic acetylcholine receptor (nAChR) occupancy in human brain of a single low dose of varenicline (0.5 mg), and to explore the relationship between receptor occupancy by varenicline and tobacco withdrawal symptoms ((*)denoting other putative nAChR subunits). Varenicline 164-175 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 108-113 22323747-1 2012 OBJECTIVE: The objective of this double-blind, placebo-controlled, randomized study was to evaluate the efficacy of varenicline (Chantix), a partial agonist at alpha4beta2 neuronal nicotinic acetylcholine receptors used for smoking cessation, in patients with spinocerebellar ataxia (SCA) 3. Varenicline 116-127 ataxin 3 Homo sapiens 260-290 22323747-6 2012 Improvements were noted in the SARA subsections for gait (p = 0.04), stance (p = 0.03), rapid alternating movements (p = 0.003), and timed 25-foot walk (p = 0.05) and Beck Depression Inventory scores (p = 0.03) in patients taking varenicline compared with those taking placebo at endpoint, with a trend toward improvement in the SARA total score (p = 0.06) in the varenicline group. Varenicline 230-241 zinc finger FYVE-type containing 9 Homo sapiens 31-35 22323747-6 2012 Improvements were noted in the SARA subsections for gait (p = 0.04), stance (p = 0.03), rapid alternating movements (p = 0.003), and timed 25-foot walk (p = 0.05) and Beck Depression Inventory scores (p = 0.03) in patients taking varenicline compared with those taking placebo at endpoint, with a trend toward improvement in the SARA total score (p = 0.06) in the varenicline group. Varenicline 364-375 zinc finger FYVE-type containing 9 Homo sapiens 31-35 22323747-7 2012 CONCLUSIONS: In this controlled study, varenicline significantly improved axial symptoms and rapid alternating movements in patients with SCA3 as measured by SARA subscores and was fairly well tolerated. Varenicline 39-50 zinc finger FYVE-type containing 9 Homo sapiens 158-162 21925806-4 2012 Varenicline was titrated up to a target dose of 1mg BID during the first week of medication. Varenicline 0-11 BH3 interacting domain death agonist Homo sapiens 52-55 22048466-6 2012 For varenicline, continuous abstinence (weeks 9-12) was associated with multiple nAChR subunit genes (including CHRNB2, CHRNA5, and CHRNA4) (OR=1.76; 95% CI: 1.23-2.52) (p<0.005); for bupropion, abstinence was associated with CYP2B6 (OR=1.78; 95% CI: 1.27-2.50) (p<0.001). Varenicline 4-15 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 81-86 22510868-3 2012 Varenicline at a dose of 5 mg/kg was administered to wild-type and Mate1-knockout mice via the jugular vein, and its uptake was measured by high-performance liquid chromatography. Varenicline 0-11 solute carrier family 47, member 1 Mus musculus 67-72 22510868-4 2012 The renal secretory clearance of and systemic exposure to varenicline were significantly decreased (54.6%, p < 0.05) and increased (116%, p < 0.05) respectively, by the genetic disruption of Mate1 in mice. Varenicline 58-69 solute carrier family 47, member 1 Mus musculus 197-202 22510868-6 2012 [(14)C]TEA uptake in HEK293 cells expressing MATE transporters and hOCT2 was decreased in the presence of varenicline. Varenicline 106-117 POU class 2 homeobox 2 Homo sapiens 67-72 22510868-9 2012 Varenicline uptake was significantly increased in HEK293 cells expressing mMATE1, hMATE1, or hMATE2-K cDNA as well as hOCT2 compared to empty vector-transfected cells. Varenicline 0-11 solute carrier family 47, member 1 Mus musculus 74-80 22510868-9 2012 Varenicline uptake was significantly increased in HEK293 cells expressing mMATE1, hMATE1, or hMATE2-K cDNA as well as hOCT2 compared to empty vector-transfected cells. Varenicline 0-11 solute carrier family 47 member 1 Homo sapiens 82-88 22510868-9 2012 Varenicline uptake was significantly increased in HEK293 cells expressing mMATE1, hMATE1, or hMATE2-K cDNA as well as hOCT2 compared to empty vector-transfected cells. Varenicline 0-11 solute carrier family 47 member 2 Homo sapiens 93-99 22510868-9 2012 Varenicline uptake was significantly increased in HEK293 cells expressing mMATE1, hMATE1, or hMATE2-K cDNA as well as hOCT2 compared to empty vector-transfected cells. Varenicline 0-11 POU class 2 homeobox 2 Homo sapiens 118-123 21763340-0 2011 The smoking cessation drug varenicline improves deficient P20-N40 inhibition in DBA/2 mice. Varenicline 27-38 demilune cell and parotid protein 1 Mus musculus 58-61 21763340-1 2011 Varenicline, an FDA approved smoking cessation pharmacotherapy, is an alpha4beta2* nicotinic acetylcholine receptor (nAChR) partial agonist and an alpha7* nAChR full agonist. Varenicline 0-11 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 83-115 21763340-1 2011 Varenicline, an FDA approved smoking cessation pharmacotherapy, is an alpha4beta2* nicotinic acetylcholine receptor (nAChR) partial agonist and an alpha7* nAChR full agonist. Varenicline 0-11 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 117-122 21763340-1 2011 Varenicline, an FDA approved smoking cessation pharmacotherapy, is an alpha4beta2* nicotinic acetylcholine receptor (nAChR) partial agonist and an alpha7* nAChR full agonist. Varenicline 0-11 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 155-160 21763340-8 2011 Selective blockade of either the alpha4beta2* or alpha7* nAChR in competition with 0.6mg/kg varenicline prevented varenicline induced improvements. Varenicline 114-125 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 57-62 21763340-9 2011 In competition with a higher dose of varenicline (3mg/kg) only blockade of the alpha4beta2* nAChR prevented varenicline induced improvement in auditory evoked response inhibition. Varenicline 108-119 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 92-97 21130610-2 2011 We recently showed that rats treated for two weeks with 2mg/kg/day varenicline (a partial agonist at alpha4beta2 nicotinic acetylcholine receptors) showed higher striatal DRD2/3 availability compared to control rats. Varenicline 67-78 dopamine receptor D2 Rattus norvegicus 171-175 21487659-6 2011 beta2* receptor occupancy following acute sazetidine, varenicline, and 5-I-A8350 lasted beyond the duration of action in the forced swim test. Varenicline 54-65 hemoglobin, beta adult minor chain Mus musculus 0-5 21368748-5 2011 Varenicline (VAR), a high-affinity partial agonist at alpha(4)beta(2) and a lower affinity full agonist at alpha(7) neuronal nAChR, injected in doses of 1-5 mg/kg/s.c. Varenicline 0-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 125-130 21239887-1 2011 Recently, we investigated the molecular mechanisms of the smoking cessation drug varenicline, a nicotinic acetylcholine receptor (nAChR) partial agonist, in its ability to decrease voluntary ethanol intake in mice. Varenicline 81-92 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 96-128 21239887-1 2011 Recently, we investigated the molecular mechanisms of the smoking cessation drug varenicline, a nicotinic acetylcholine receptor (nAChR) partial agonist, in its ability to decrease voluntary ethanol intake in mice. Varenicline 81-92 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 130-135 21239887-3 2011 Although varenicline was designed to be a high affinity partial agonist of nAChRs containing the alpha4 and beta2 subunits (designated as alpha4beta2*), at higher concentrations it can also act upon alpha3beta2*, alpha6*, alpha3beta4* and alpha7 nAChRs. Varenicline 9-20 immunoglobulin (CD79A) binding protein 1 Mus musculus 97-103 21239887-3 2011 Although varenicline was designed to be a high affinity partial agonist of nAChRs containing the alpha4 and beta2 subunits (designated as alpha4beta2*), at higher concentrations it can also act upon alpha3beta2*, alpha6*, alpha3beta4* and alpha7 nAChRs. Varenicline 9-20 hemoglobin, beta adult minor chain Mus musculus 108-113 21239887-3 2011 Although varenicline was designed to be a high affinity partial agonist of nAChRs containing the alpha4 and beta2 subunits (designated as alpha4beta2*), at higher concentrations it can also act upon alpha3beta2*, alpha6*, alpha3beta4* and alpha7 nAChRs. Varenicline 9-20 gamma-aminobutyric acid (GABA) A receptor, subunit alpha 6 Mus musculus 213-219 21239887-3 2011 Although varenicline was designed to be a high affinity partial agonist of nAChRs containing the alpha4 and beta2 subunits (designated as alpha4beta2*), at higher concentrations it can also act upon alpha3beta2*, alpha6*, alpha3beta4* and alpha7 nAChRs. Varenicline 9-20 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 239-245 21239887-5 2011 We found that activation of alpha4* nAChRs was necessary and sufficient for varenicline-induced reduction of alcohol consumption. Varenicline 76-87 immunoglobulin (CD79A) binding protein 1 Mus musculus 28-34 21130610-4 2011 DRD2/3 availability in striatal areas was studied in 80 rats following two-week treatment with 0.5, 1 or 2mg/kg/day varenicline or vehicle and survival of the effects of varenicline on DRD2/3 availability up to 2 weeks after treatment discontinuation using (123)I-IBZM storage phosphor imaging. Varenicline 170-181 dopamine receptor D2 Rattus norvegicus 185-189 21130610-5 2011 For all varenicline doses, varenicline treated rats showed a comparable significantly higher DRD2/3 availability in the ventral striatum of approximately 11% compared to control rats, while only the rats treated with 1 and 2mg/kg/day dose showed significantly higher DRD2/3 availability in the dorsal striatum by 12.5% and 13.2% compared to control rats, respectively. Varenicline 27-38 dopamine receptor D2 Rattus norvegicus 93-97 21130610-5 2011 For all varenicline doses, varenicline treated rats showed a comparable significantly higher DRD2/3 availability in the ventral striatum of approximately 11% compared to control rats, while only the rats treated with 1 and 2mg/kg/day dose showed significantly higher DRD2/3 availability in the dorsal striatum by 12.5% and 13.2% compared to control rats, respectively. Varenicline 27-38 dopamine receptor D2 Rattus norvegicus 267-271 21130610-6 2011 Two weeks after discontinuation of the active treatment with 2mg/kg/day varenicline, DRD2/3 binding in ventral, but not dorsal, striatum was still significantly higher (11.7%) compared to vehicle. Varenicline 72-83 dopamine receptor D2 Rattus norvegicus 85-89 21130610-7 2011 Varenicline induces dose-dependent and sustained increases in striatal DRD2/3 in rats, particularly in the ventral striatum. Varenicline 0-11 dopamine receptor D2 Rattus norvegicus 71-75 21130610-8 2011 These observations suggest that increased DRD2/3 availability may contribute to varenicline"s efficacy for smoking cessation and show promise for varenicline as a treatment of other types of drug dependence. Varenicline 80-91 dopamine receptor D2 Rattus norvegicus 42-46 20924754-2 2011 Varenicline, a partial alpha4beta2 nicotinic acetylcholine receptor (nAChR) agonist, is effective in reducing nicotine craving and relapse in smokers, suggesting that alpha4beta2 nAChRs may play a key role in nicotine dependence. Varenicline 0-11 cholinergic receptor nicotinic beta 1 subunit Rattus norvegicus 69-74 20946306-0 2010 The nicotinic acetylcholine receptor partial agonist varenicline increases the ataxic and sedative-hypnotic effects of acute ethanol administration in C57BL/6J mice. Varenicline 53-64 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 4-36 21116052-6 2011 The alpha7 nAChR agonists varenicline and JN403 increased binding of the amyloid ligand [3H]PIB to fibrillar Abeta in AD frontal cortex autopsy tissue. Varenicline 26-37 amyloid beta precursor protein Homo sapiens 109-114 21097981-2 2011 METHODS: We evaluated heteromeric nAChR regulation via [3H]epibatidine binding following cessation of chronic nicotine or varenicline treatment. Varenicline 122-133 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 34-39 20946306-2 2010 Recently, the nicotinic acetylcholine receptor (nAChR) partial agonist varenicline has been shown to decrease ethanol consumption in both humans and animal models. Varenicline 71-82 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 14-46 20946306-2 2010 Recently, the nicotinic acetylcholine receptor (nAChR) partial agonist varenicline has been shown to decrease ethanol consumption in both humans and animal models. Varenicline 71-82 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 48-53 21053991-8 2010 Varenicline is almost exclusively excreted unchanged in urine, primarily through glomerular filtration, with some component of active tubular secretion via human organic cation transporter, hOCT-2. Varenicline 0-11 POU class 2 homeobox 2 Homo sapiens 190-196 20708056-0 2010 The high-affinity nAChR partial agonists varenicline and sazetidine-A exhibit reinforcing properties in rats. Varenicline 41-52 cholinergic receptor nicotinic alpha 2 subunit Rattus norvegicus 18-23 20708056-1 2010 Varenicline (Chantix , Champix ) is a nicotinic acetylcholine receptor (nAChR) partial agonist clinically approved for smoking cessation, yet its potential abuse liability properties have not been fully characterized. Varenicline 0-11 cholinergic receptor nicotinic alpha 2 subunit Rattus norvegicus 38-70 20708056-1 2010 Varenicline (Chantix , Champix ) is a nicotinic acetylcholine receptor (nAChR) partial agonist clinically approved for smoking cessation, yet its potential abuse liability properties have not been fully characterized. Varenicline 0-11 cholinergic receptor nicotinic alpha 2 subunit Rattus norvegicus 72-77 20708056-1 2010 Varenicline (Chantix , Champix ) is a nicotinic acetylcholine receptor (nAChR) partial agonist clinically approved for smoking cessation, yet its potential abuse liability properties have not been fully characterized. Varenicline 13-20 cholinergic receptor nicotinic alpha 2 subunit Rattus norvegicus 38-70 20708056-1 2010 Varenicline (Chantix , Champix ) is a nicotinic acetylcholine receptor (nAChR) partial agonist clinically approved for smoking cessation, yet its potential abuse liability properties have not been fully characterized. Varenicline 13-20 cholinergic receptor nicotinic alpha 2 subunit Rattus norvegicus 72-77 20708056-1 2010 Varenicline (Chantix , Champix ) is a nicotinic acetylcholine receptor (nAChR) partial agonist clinically approved for smoking cessation, yet its potential abuse liability properties have not been fully characterized. Varenicline 23-30 cholinergic receptor nicotinic alpha 2 subunit Rattus norvegicus 38-70 20708056-1 2010 Varenicline (Chantix , Champix ) is a nicotinic acetylcholine receptor (nAChR) partial agonist clinically approved for smoking cessation, yet its potential abuse liability properties have not been fully characterized. Varenicline 23-30 cholinergic receptor nicotinic alpha 2 subunit Rattus norvegicus 72-77 20708056-6 2010 The reinforcing and discriminative stimulus (DS) properties of sazetidine-A, varenicline and nicotine were attenuated by acute pretreatment with the non-selective neuronal non-competitive nAChR antagonist mecamylamine or the alpha4* nAChR-selective antagonist dihydro-beta-erythroidine, but not by the alpha7 nAChR subtype antagonist methyllycaconitine. Varenicline 77-88 cholinergic receptor nicotinic alpha 2 subunit Rattus norvegicus 188-193 20708056-6 2010 The reinforcing and discriminative stimulus (DS) properties of sazetidine-A, varenicline and nicotine were attenuated by acute pretreatment with the non-selective neuronal non-competitive nAChR antagonist mecamylamine or the alpha4* nAChR-selective antagonist dihydro-beta-erythroidine, but not by the alpha7 nAChR subtype antagonist methyllycaconitine. Varenicline 77-88 cholinergic receptor nicotinic alpha 2 subunit Rattus norvegicus 233-238 20708056-6 2010 The reinforcing and discriminative stimulus (DS) properties of sazetidine-A, varenicline and nicotine were attenuated by acute pretreatment with the non-selective neuronal non-competitive nAChR antagonist mecamylamine or the alpha4* nAChR-selective antagonist dihydro-beta-erythroidine, but not by the alpha7 nAChR subtype antagonist methyllycaconitine. Varenicline 77-88 cholinergic receptor nicotinic alpha 2 subunit Rattus norvegicus 233-238 20668200-1 2010 Recently, the smoking cessation therapeutic varenicline, a nicotinic acetylcholine receptor (nAChR) partial agonist, has been shown to reduce alcohol consumption. Varenicline 44-55 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 59-91 20668200-1 2010 Recently, the smoking cessation therapeutic varenicline, a nicotinic acetylcholine receptor (nAChR) partial agonist, has been shown to reduce alcohol consumption. Varenicline 44-55 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 93-98 19959340-0 2010 The nicotinic acetylcholine receptor partial agonist varenicline and the treatment of drug dependence: a review. Varenicline 53-64 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 4-36 20805437-0 2010 Letter by Smolderen and Pelle regarding article, "Efficacy and safety of varenicline for smoking cessation in patients with cardiovascular disease: a randomized trial". Varenicline 73-84 interleukin 1 receptor associated kinase 1 Homo sapiens 24-29 20395358-7 2010 RESULTS: Nicotine and varenicline enhanced mouse P20 amplitude, while nicotine improved P20 habituation by selectively increasing the first-click response. Varenicline 22-33 demilune cell and parotid protein 1 Mus musculus 49-52 20335008-0 2010 Varenicline treatment decreases DNMT1 mRNA expression in lymphocytes of schizophrenic patients who are cigarette smokers. Varenicline 0-11 DNA methyltransferase 1 Homo sapiens 32-37 20331614-7 2010 CONCLUSIONS AND IMPLICATIONS: The data provide a plausible explanation for the higher abstinence rate in smoking cessation trials following treatment with varenicline than with the two other alpha4beta2 nAChR partial agonists. Varenicline 155-166 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 203-208 20373480-1 2010 Varenicline, alpha4beta2 nicotinic acetylcholine receptor (nAChR) partial agonist, is a new class of medications for treating nicotine dependence. Varenicline 0-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 59-64 20373480-2 2010 As an alpha4beta2 nAChR partial agonist, varenicline serves to reduce nicotine withdrawal symptoms, while high-affinity binding of the agonist mitigates the reinforcing effects of smoking. Varenicline 41-52 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 18-23 20373480-3 2010 In the present study, we compared serum brain-derived neurotrophic factor (BDNF) levels of nicotine dependence and nonsmokers, and we investigated changes in serum BDNF levels after 8 weeks of treatment with varenicline. Varenicline 208-219 brain derived neurotrophic factor Homo sapiens 164-168 20167427-4 2010 Nonselective nAChR agonists ABT-594 and varenicline were effective analgesics. Varenicline 40-51 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 13-18 19959340-5 2010 Varenicline, an alpha4beta2 nAChR partial agonist and an alpha7 nAChR full agonist registered for the treatment of nicotine dependence, significantly reduces nicotine craving and prevents relapse. Varenicline 0-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 28-33 19959340-5 2010 Varenicline, an alpha4beta2 nAChR partial agonist and an alpha7 nAChR full agonist registered for the treatment of nicotine dependence, significantly reduces nicotine craving and prevents relapse. Varenicline 0-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 64-69 19887076-0 2010 Effect of the alpha4beta2* nicotinic acetylcholine receptor partial agonist varenicline on dopamine release in beta2 knock-out mice with selective re-expression of the beta2 subunit in the ventral tegmental area. Varenicline 76-87 hemoglobin, beta adult minor chain Mus musculus 111-116 19887076-1 2010 We studied the effects of 1 mg/kg doses of nicotine and the alpha4beta2* nicotinic acetylcholine receptor (nAChR) partial agonist, varenicline, on extracellular dopamine (DA) levels in the nucleus accumbens (NuAcc) of lentivirally vectorized male mice. Varenicline 131-142 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 73-105 19887076-1 2010 We studied the effects of 1 mg/kg doses of nicotine and the alpha4beta2* nicotinic acetylcholine receptor (nAChR) partial agonist, varenicline, on extracellular dopamine (DA) levels in the nucleus accumbens (NuAcc) of lentivirally vectorized male mice. Varenicline 131-142 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 107-112 19887076-3 2010 Our results suggest that the neurochemical effects of varenicline as measured by using microdialysis in awake, freely moving mice are mainly mediated via beta2* nAChR subunits localized in the VTA. Varenicline 54-65 hemoglobin, beta adult minor chain Mus musculus 154-159 19887076-3 2010 Our results suggest that the neurochemical effects of varenicline as measured by using microdialysis in awake, freely moving mice are mainly mediated via beta2* nAChR subunits localized in the VTA. Varenicline 54-65 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 161-166 19959243-2 2010 This pilot study examines the effects of varenicline, an alpha-7 agonist, on the P50 auditory evoked potential in six schizophrenic patients. Varenicline 41-52 nuclear factor kappa B subunit 1 Homo sapiens 81-84 20071853-1 2009 Varenicline, a partial agonist of alpha4beta2 nicotinic acetylcholine receptor (nAChR), is the most recently approved drug for smoking cessation. Varenicline 0-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 80-85 19693492-1 2009 RATIONALE: Varenicline, a partial nicotinic acetylcholine receptor (nAChR) agonist, is approved for smoking cessation. Varenicline 11-22 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 34-66 19693492-1 2009 RATIONALE: Varenicline, a partial nicotinic acetylcholine receptor (nAChR) agonist, is approved for smoking cessation. Varenicline 11-22 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 68-73 19501054-1 2009 The pharmacological properties and pharmacokinetic profile of the alpha4beta2 nicotinic acetylcholine receptor (nAChR) partial agonist varenicline provide an advantageous combination of free brain levels and functional potencies at the target receptor that for a large part explain its efficacy as a smoking cessation aid. Varenicline 135-146 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 112-117 19501054-0 2009 Preclinical pharmacology of the alpha4beta2 nAChR partial agonist varenicline related to effects on reward, mood and cognition. Varenicline 66-77 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 44-49 19501054-2 2009 Since alpha4beta2 and other nAChR subtypes play important roles in mediating central processes that control reward, mood, cognition and attention, there is interest in examining the effects of selective nAChR ligands such as varenicline in preclinical animal models that assess these behaviors. Varenicline 225-236 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 203-208 19494730-1 2009 Two patients with atypical Friedreich ataxia (heterozygotes for a GAA expansion and a G130V point mutation) experienced modest proprioceptive improvements in their extremities within a month of taking varenicline (Chantix), a drug approved for smoking cessation. Varenicline 201-212 alpha glucosidase Homo sapiens 66-69 20071853-3 2009 As a nAChR partial agonist, Varenicline attenuates the craving and withdrawal symptoms that occur with abstinence from nicotine and also reduces the rewarding effects of nicotine obtained from smoking in patients who lapse. Varenicline 28-39 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 5-10 23506178-7 2008 In addition, the neuronal nAChR partial agonist varenicline recently received regulatory approval for use in smoking cessation. Varenicline 48-59 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 26-31 19243716-13 2009 h/mL for varenicline 1 mg BID and 95.7 ng . Varenicline 9-20 BH3 interacting domain death agonist Homo sapiens 26-29 19243716-14 2009 h/mL for varenicline 0.5 mg BID, consistent with values reported previously in adult smokers at the equivalent doses. Varenicline 9-20 BH3 interacting domain death agonist Homo sapiens 28-31 18798299-1 2008 The objective of this study was to evaluate the efficacy of varenicline, a novel partial agonist at alpha 4 beta 2 and full agonist at alpha 7 nicotinic acetylcholine receptor (nAChR) subtypes, in blocking the locomotor effects of acute or repeated treatments with nicotine (0.4 mg/kg, s.c.) in rats. Varenicline 60-71 cholinergic receptor nicotinic beta 1 subunit Rattus norvegicus 177-182 18442345-4 2008 RESULTS: CAR(9-12) was greater for varenicline (44.0%) versus bupropion SR (29.7%; P<0.0001) and placebo (17.7%; P<0.0001). Varenicline 35-46 CXADR pseudogene 1 Homo sapiens 9-12 18442345-5 2008 CAR(9-12) for varenicline versus placebo was not affected by age, gender, or nicotine dependence level. Varenicline 14-25 CXADR pseudogene 1 Homo sapiens 0-3 18078657-1 2007 Varenicline is a new drug for smoking cessation that reduces cravings by binding to the alfa4-beta2-nicotine-achethylcholine receptors in the brain (partial agonist). Varenicline 0-11 potassium calcium-activated channel subfamily M regulatory beta subunit 2 Homo sapiens 94-99 20040957-12 2008 Recently, varenicline, a partial agonist at alpha4beta2 nAChR, has been approved by the FDA (Food and Drug Administration) for smoking cessation. Varenicline 10-21 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 56-61 18625984-12 2008 In our analysis of data from the varenicline trials that included bupropion control arms, we found that varenicline was superior to bupropion (OR 2.18, 95% CrI 1.09-4.08). Varenicline 104-115 EP300 interacting inhibitor of differentiation 1 Homo sapiens 156-161 18411066-2 2008 Varenicline, an alpha4beta2 nicotinic receptor partial agonist and alpha7 nicotinic receptor full agonist prescribed for smoking cessation, has been shown to decrease ethanol consumption. Varenicline 0-11 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 67-92 18463392-1 2008 Varenicline (pronounced va-re-nik-leen) (Champix - Pfizer), a nicotinic receptor partial agonist, is the first medicine of this type licensed for smoking cessation in adults. Varenicline 0-11 mitogen-activated protein kinase kinase kinase 14 Homo sapiens 30-33 18342165-3 2008 Varenicline is the first in a new class of agents for smoking cessation, the alpha(4)beta(2) nicotinic acetylcholine receptor (nAChR) partial agonists. Varenicline 0-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 127-132 18342165-5 2008 As a nAChR partial agonist, varenicline attenuates the craving and withdrawal symptoms that occur with abstinence from nicotine and also reduces the rewarding effects of nicotine obtained from smoking in patients who lapse. Varenicline 28-39 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 5-10 17971819-2 2008 Transporter inhibition assays using human embryonic kidney 293 cells transfected with human renal transporters demonstrated that high concentrations of varenicline inhibited substrate uptake by hOCT2 (IC(50)=890 microM), with very weak or no measurable interactions with the other transporters hOAT1, hOAT3, hOCTN1, and hOCTN2. Varenicline 152-163 POU class 2 homeobox 2 Homo sapiens 194-199 17971819-2 2008 Transporter inhibition assays using human embryonic kidney 293 cells transfected with human renal transporters demonstrated that high concentrations of varenicline inhibited substrate uptake by hOCT2 (IC(50)=890 microM), with very weak or no measurable interactions with the other transporters hOAT1, hOAT3, hOCTN1, and hOCTN2. Varenicline 152-163 solute carrier family 22 member 6 Homo sapiens 294-299 17971819-2 2008 Transporter inhibition assays using human embryonic kidney 293 cells transfected with human renal transporters demonstrated that high concentrations of varenicline inhibited substrate uptake by hOCT2 (IC(50)=890 microM), with very weak or no measurable interactions with the other transporters hOAT1, hOAT3, hOCTN1, and hOCTN2. Varenicline 152-163 solute carrier family 22 member 8 Homo sapiens 301-306 17971819-2 2008 Transporter inhibition assays using human embryonic kidney 293 cells transfected with human renal transporters demonstrated that high concentrations of varenicline inhibited substrate uptake by hOCT2 (IC(50)=890 microM), with very weak or no measurable interactions with the other transporters hOAT1, hOAT3, hOCTN1, and hOCTN2. Varenicline 152-163 solute carrier family 22 member 4 Homo sapiens 308-314 17971819-2 2008 Transporter inhibition assays using human embryonic kidney 293 cells transfected with human renal transporters demonstrated that high concentrations of varenicline inhibited substrate uptake by hOCT2 (IC(50)=890 microM), with very weak or no measurable interactions with the other transporters hOAT1, hOAT3, hOCTN1, and hOCTN2. Varenicline 152-163 solute carrier family 22 member 5 Homo sapiens 320-326 17971819-3 2008 Varenicline was characterized as a moderate-affinity substrate for hOCT2 (K(m)=370 microM) and its hOCT2-mediated uptake was partially inhibited by cimetidine. Varenicline 0-11 POU class 2 homeobox 2 Homo sapiens 67-72 17971819-3 2008 Varenicline was characterized as a moderate-affinity substrate for hOCT2 (K(m)=370 microM) and its hOCT2-mediated uptake was partially inhibited by cimetidine. Varenicline 0-11 POU class 2 homeobox 2 Homo sapiens 99-104 18084743-1 2008 AIMS: To examine the effect of varenicline, a selective alpha4-beta2 nicotinic acetylcholine receptor (nAChR) partial agonist, on craving and withdrawal symptoms in smokers making a quit attempt and the rewarding effects of smoking during a lapse after the target quit date (TQD). Varenicline 31-42 immunoglobulin binding protein 1 Homo sapiens 56-62 17407636-15 2007 CONCLUSIONS: Varenicline 1 mg BID can be safely administered for up to 1 year. Varenicline 13-24 BH3 interacting domain death agonist Homo sapiens 30-33 17692719-2 2007 OBJECTIVE: This study evaluated the efficacy and tolerability of 1 mg BID varenicline, a novel alpha4beta2 nicotinic acetylcholine receptor partial agonist, for smoking cessation in smokers in Taiwan and Korea. Varenicline 74-85 BH3 interacting domain death agonist Homo sapiens 70-73 17692720-13 2007 The highest CAR of 65.4% (85/130) was achieved with varenicline 1 mg BID (odds ratio [OR] [95% CI] = 2.98 [1.78-4.99]; P < 0.001). Varenicline 52-63 BH3 interacting domain death agonist Homo sapiens 69-72 17692720-14 2007 The CAR for weeks 9-52 was significantly greater for varenicline 1 mg BID than placebo (34.6% [45/130] vs 23.3% [30/129]; OR [95% CI] = 1.81 [1.04-3.17]; P = 0.036). Varenicline 53-64 BH3 interacting domain death agonist Homo sapiens 70-73 17692720-16 2007 Treatment-emergent adverse events (AEs) were more prevalent among varenicline-treated subjects (79.1% [121/153] at 0.25 mg BID, 80.6% [125/155] at 0.5 mg BID, and 80.1% [125/156] at 1 mg BID) than placebo subjects (71.4% [110/154]). Varenicline 66-77 BH3 interacting domain death agonist Homo sapiens 123-126 17692720-16 2007 Treatment-emergent adverse events (AEs) were more prevalent among varenicline-treated subjects (79.1% [121/153] at 0.25 mg BID, 80.6% [125/155] at 0.5 mg BID, and 80.1% [125/156] at 1 mg BID) than placebo subjects (71.4% [110/154]). Varenicline 66-77 BH3 interacting domain death agonist Homo sapiens 154-157 17692720-16 2007 Treatment-emergent adverse events (AEs) were more prevalent among varenicline-treated subjects (79.1% [121/153] at 0.25 mg BID, 80.6% [125/155] at 0.5 mg BID, and 80.1% [125/156] at 1 mg BID) than placebo subjects (71.4% [110/154]). Varenicline 66-77 BH3 interacting domain death agonist Homo sapiens 154-157 17692720-17 2007 The 3 most prevalent AEs at varenicline 1 mg BID were nasopharyngitis (35.9% [56/156]), nausea (24.4% [38/156]), and headache (10.3% [16/156]), all of which were of mild or moderate intensity. Varenicline 28-39 BH3 interacting domain death agonist Homo sapiens 45-48 17692720-20 2007 The dose associated with the highest efficacy was varenicline 1 mg BID. Varenicline 50-61 BH3 interacting domain death agonist Homo sapiens 67-70 17353944-2 2007 Varenicline, recently approved by the U.S. Food and Drug Administration and the European Agency for the Evaluation of Medicinal Products as an aid to smoking cessation treatment, has a novel mechanism of action, targeting the specific nicotinic acetylcholine receptor (nAChR) associated with nicotine-induced behaviors (alpha4beta2 nAChR). Varenicline 0-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 235-267 17353944-2 2007 Varenicline, recently approved by the U.S. Food and Drug Administration and the European Agency for the Evaluation of Medicinal Products as an aid to smoking cessation treatment, has a novel mechanism of action, targeting the specific nicotinic acetylcholine receptor (nAChR) associated with nicotine-induced behaviors (alpha4beta2 nAChR). Varenicline 0-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 269-274 17353944-2 2007 Varenicline, recently approved by the U.S. Food and Drug Administration and the European Agency for the Evaluation of Medicinal Products as an aid to smoking cessation treatment, has a novel mechanism of action, targeting the specific nicotinic acetylcholine receptor (nAChR) associated with nicotine-induced behaviors (alpha4beta2 nAChR). Varenicline 0-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 332-337 34582844-15 2022 PKR/STAT3 maybe the potential mechanism, and perioperative varenicline treatment could be an efficient therapeutic strategy for POCD. Varenicline 59-70 eukaryotic translation initiation factor 2-alpha kinase 2 Mus musculus 0-3 17157884-1 2007 The preclinical pharmacology of the alpha4beta2 nicotinic acetylcholine receptor (nAChR) partial agonist varenicline, a novel smoking cessation agent is described. Varenicline 105-116 cholinergic receptor nicotinic beta 1 subunit Rattus norvegicus 82-87 15887955-4 2005 Varenicline displays high alpha4beta2 nAChR affinity and the desired in vivo dopaminergic profile. Varenicline 0-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 38-43 34582844-15 2022 PKR/STAT3 maybe the potential mechanism, and perioperative varenicline treatment could be an efficient therapeutic strategy for POCD. Varenicline 59-70 signal transducer and activator of transcription 3 Mus musculus 4-9 34486130-4 2021 METHODS: The study utilized data from the Phase 2 randomized, double-blind, placebo-controlled multisite 13-week trial of varenicline in alcohol-dependent patients (n = 200) (J Addict Med, 7, 2013, 277). Varenicline 122-133 collagen type IX alpha 3 chain Homo sapiens 184-187 34878065-2 2021 Varenicline, an alpha4beta2 nAChR partial agonist approved for smoking cessation treatments, could be valuable for PD treatment. Varenicline 0-11 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 28-33 34712695-2 2021 This study investigated the effects of varenicline, an alpha7 nicotinic acetylcholine receptor (alpha7nAChR) agonist, on inflammatory cytokine levels, cell proliferation, and migration rates in a lipopolysaccharide (LPS)-induced inflammation model in RAW 264.7 murine macrophage cell lines. Varenicline 39-50 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 96-107 34712695-7 2021 Varenicline decreased LPS-induced cytokines and chemokines including TNFalpha, IL-6, and IL-1beta via alpha7nAChRs to a similar level that observed with dexamethasone. Varenicline 0-11 tumor necrosis factor Mus musculus 69-77 34712695-7 2021 Varenicline decreased LPS-induced cytokines and chemokines including TNFalpha, IL-6, and IL-1beta via alpha7nAChRs to a similar level that observed with dexamethasone. Varenicline 0-11 interleukin 6 Mus musculus 79-83 34712695-7 2021 Varenicline decreased LPS-induced cytokines and chemokines including TNFalpha, IL-6, and IL-1beta via alpha7nAChRs to a similar level that observed with dexamethasone. Varenicline 0-11 interleukin 1 alpha Mus musculus 89-97 34712695-9 2021 On the other hand, the LPS-induced cell migration rate decreased with varenicline via alpha7nAChR. Varenicline 70-81 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 86-97 34366251-5 2021 We identified varenicline as an FDA approved alpha7 nAChR agonist and hypothesized that varenicline administration would decrease long-term testicular atrophy and fibrosis in a murine model of testicular torsion. Varenicline 14-25 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 45-57 34366251-9 2021 RESULTS: 48 h following reperfusion, the testis of animals treated with varenicline demonstrated a significant reduction in the inflammatory response as measured by the acute immune cell infiltrate, myeloperoxidase activity, concentration of reduced glutathione and expression of downstream NF-KB targets. Varenicline 72-83 myeloperoxidase Mus musculus 199-214 32173266-0 2020 Hesperidin blocks varenicline-aggravated atherosclerotic plaque formation in apolipoprotein E knockout mice by downregulating net uptake of oxidized low-density lipoprotein in macrophages. Varenicline 18-29 apolipoprotein E Mus musculus 77-93 33977560-2 2021 As a step towards assessing if alpha4beta2* nicotinic acetylcholine receptor (nAChR) stimulation improves gait-balance function, we assessed target engagement of the alpha4beta2* nAChR partial agonist varenicline. Varenicline 201-212 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 179-184 32776643-9 2021 Female PKCepsilon-/- mice also show reduced immobility time in response to varenicline (1.0 mg/kg i.p.) Varenicline 75-86 protein kinase C, epsilon Mus musculus 7-17 33735416-6 2021 We hypothesize that varenicline treatment (1 mg BID, administered for 12 weeks) would increase quit rates, maintain smoking abstinence up to 1 year after treatment, and be well-tolerated in T2DM smokers intending to quit. Varenicline 20-31 BH3 interacting domain death agonist Homo sapiens 48-51 33713409-12 2021 CONCLUSIONS: Variation in SLCO3A1 may influence the risk for developing nausea in varenicline-treated smokers, which may alter adherence and cessation. Varenicline 82-93 solute carrier organic anion transporter family member 3A1 Homo sapiens 26-33 33713409-15 2021 This pilot genome-wide investigation of nausea, the most common side effect associated with varenicline treatment and an importance cause of treatment discontinuation, suggests the potential involvement of common variation in the SLCO3A1 drug transporter gene. Varenicline 92-103 solute carrier organic anion transporter family member 3A1 Homo sapiens 230-237 31293045-4 2020 Smoking therapy agents, such as the partial nAChR agonist varenicline or the DA/noradrenaline transporter inhibitor bupropion, could potentially also be used for AUD. Varenicline 58-69 cholinergic receptor nicotinic beta 1 subunit Rattus norvegicus 44-49 32209809-6 2020 The partial alpha4beta2* nAChR agonists varenicline and 2"-fluoro-3"-(4-nitro-phenyl)deschloroepibatidine produced 61 and 69% epibatidine-appropriate responding, respectively. Varenicline 40-51 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 25-30 32173266-3 2020 Varenicline progresses atherosclerotic plaque formation in apolipoprotein E knockout (ApoE KO) mice. Varenicline 0-11 apolipoprotein E Mus musculus 59-75 32173266-6 2020 The aim of this study was to examine the effect of hesperidin, a citrus flavonoid, on varenicline-aggravated atherosclerotic plaque formation in apolipoprotein E knockout (ApoE KO) mice. Varenicline 86-97 apolipoprotein E Mus musculus 145-161 32294065-0 2020 Countering Opioid-induced Respiratory Depression in Male Rats with Nicotinic Acetylcholine Receptor Partial Agonists Varenicline and ABT 594. Varenicline 117-128 cholinergic receptor nicotinic alpha 2 subunit Rattus norvegicus 67-99 32494237-0 2020 Safety of varenicline as an aid to smoking cessation in professional drivers and its impact on driving behaviors: An observational cohort study of taxi drivers in Beijing. Varenicline 10-21 activation induced cytidine deaminase Homo sapiens 28-31 32494237-11 2020 CONCLUSIONS: Varenicline appears to be a well-tolerated smoking cessation aid for Beijing taxi drivers and has less impact on driving behaviors. Varenicline 13-24 activation induced cytidine deaminase Homo sapiens 74-77 31096265-2 2020 Varenicline, an alpha4beta2 nicotinic acetylcholine receptor (nAChR) partial agonist, has been shown to increase smoking quit rates compared with nicotine-based products. Varenicline 0-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 62-67 31771811-0 2020 Varenicline aggravates atherosclerotic plaque formation in nicotine-pretreated ApoE knockout mice due to enhanced oxLDL uptake by macrophages through downregulation of ABCA1 and ABCG1 expression. Varenicline 0-11 apolipoprotein E Mus musculus 79-83 32130342-7 2020 In chronic exposure to varenicline, oxidant levels comprising of malondialdehyde (MDA), and myeloperoxidase (MPO) increased and superoxide dismutase (SOD), catalase (CAT), glutathione (GSH) and glutathione peroxidase (GPx) levels, named as antioxidants, decreased significantly when compared to the control group. Varenicline 23-34 myeloperoxidase Rattus norvegicus 92-107 32130342-7 2020 In chronic exposure to varenicline, oxidant levels comprising of malondialdehyde (MDA), and myeloperoxidase (MPO) increased and superoxide dismutase (SOD), catalase (CAT), glutathione (GSH) and glutathione peroxidase (GPx) levels, named as antioxidants, decreased significantly when compared to the control group. Varenicline 23-34 myeloperoxidase Rattus norvegicus 109-112 32130342-7 2020 In chronic exposure to varenicline, oxidant levels comprising of malondialdehyde (MDA), and myeloperoxidase (MPO) increased and superoxide dismutase (SOD), catalase (CAT), glutathione (GSH) and glutathione peroxidase (GPx) levels, named as antioxidants, decreased significantly when compared to the control group. Varenicline 23-34 catalase Rattus norvegicus 156-164 32130342-7 2020 In chronic exposure to varenicline, oxidant levels comprising of malondialdehyde (MDA), and myeloperoxidase (MPO) increased and superoxide dismutase (SOD), catalase (CAT), glutathione (GSH) and glutathione peroxidase (GPx) levels, named as antioxidants, decreased significantly when compared to the control group. Varenicline 23-34 catalase Rattus norvegicus 166-169 32130342-8 2020 MDA and MPO levels were also significantly higher and SOD, CAT, GPx, GSH levels were also significantly lower in chronic varenicline group when compared to acute varenicline group. Varenicline 121-132 catalase Rattus norvegicus 59-62 31771811-0 2020 Varenicline aggravates atherosclerotic plaque formation in nicotine-pretreated ApoE knockout mice due to enhanced oxLDL uptake by macrophages through downregulation of ABCA1 and ABCG1 expression. Varenicline 0-11 ATP-binding cassette, sub-family A (ABC1), member 1 Mus musculus 168-173 31771811-0 2020 Varenicline aggravates atherosclerotic plaque formation in nicotine-pretreated ApoE knockout mice due to enhanced oxLDL uptake by macrophages through downregulation of ABCA1 and ABCG1 expression. Varenicline 0-11 ATP binding cassette subfamily G member 1 Mus musculus 178-183 31771811-2 2020 We previously reported that varenicline aggravates atherosclerosis in apolipoprotein E knockout (ApoE KO) mice. Varenicline 28-39 apolipoprotein E Mus musculus 70-86 31771811-2 2020 We previously reported that varenicline aggravates atherosclerosis in apolipoprotein E knockout (ApoE KO) mice. Varenicline 28-39 apolipoprotein E Mus musculus 97-101 31771811-5 2020 Varenicline caused significant progression of plaque formation in the whole aorta and aortic root and further accelerated the increased formation of a macrophage-rich plaque area in the aortic root in nicotine-pretreated ApoE KO mice. Varenicline 0-11 apolipoprotein E Mus musculus 221-225 31771811-8 2020 Varenicline enhanced nicotine-induced oxLDL uptake in macrophages through decreased expression of cholesterol efflux transporters ABCA1 and ABCG1 and thereby progressed atherosclerotic plaque formation. Varenicline 0-11 ATP-binding cassette, sub-family A (ABC1), member 1 Mus musculus 130-135 31771811-8 2020 Varenicline enhanced nicotine-induced oxLDL uptake in macrophages through decreased expression of cholesterol efflux transporters ABCA1 and ABCG1 and thereby progressed atherosclerotic plaque formation. Varenicline 0-11 ATP binding cassette subfamily G member 1 Mus musculus 140-145 31394567-5 2020 NS9283 increased the potency of varenicline to activate and desensitize (alpha4)3(beta2)2 nAChRs in vitro without affecting other known targets of varenicline. Varenicline 32-43 hemoglobin, beta adult minor chain Mus musculus 73-87 31394567-9 2020 We conclude that compounds targeting the (alpha4)3(beta2)2 subtype of nAChRs can reduce alcohol consumption, and when administered in combination with varenicline, may allow use of lower varenicline doses to decrease varenicline side effects. Varenicline 187-198 hemoglobin, beta adult minor chain Mus musculus 42-56 31394567-9 2020 We conclude that compounds targeting the (alpha4)3(beta2)2 subtype of nAChRs can reduce alcohol consumption, and when administered in combination with varenicline, may allow use of lower varenicline doses to decrease varenicline side effects. Varenicline 187-198 hemoglobin, beta adult minor chain Mus musculus 42-56 31387842-12 2019 CONCLUSIONS: Smoking cessation treatment by varenicline strengthens the effects of bronchial valve implantation and shows up its crucial therapeutic role in severe COPD. Varenicline 44-55 COPD Homo sapiens 164-168 31402421-0 2019 Cytochrome P450 2A6 and 2B6 polymorphisms and smoking cessation success in patients treated with varenicline. Varenicline 97-108 cytochrome P450 family 2 subfamily A member 6 Homo sapiens 0-19 31402421-2 2019 In the scenario of precision medicine, the aim of this study was to evaluate a possible association of cytochrome P450 2A6 and 2B6 polymorphisms with varenicline pharmacotherapy. Varenicline 150-161 cytochrome P450 family 2 subfamily A member 6 Homo sapiens 103-122 31402421-6 2019 RESULTS: Patients with AG or GG genotypes for CYP2B6 rs8109525 had a higher success rate of smoking cessation with varenicline (51.2%) compared with carriers of the AA genotypes (33.3%, P = 0.03, n = 167). Varenicline 115-126 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 46-52 31402421-8 2019 CONCLUSION: CYP2B6 rs8109525 was associated with a higher success rate of smoking cessation with varenicline treatment. Varenicline 97-108 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 12-18 30398980-0 2019 Differential cross-tolerance to the effects of nicotinic acetylcholine receptor drugs in C57BL/6J mice following chronic varenicline. Varenicline 121-132 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 47-79 30398980-1 2019 Varenicline is a smoking cessation pharmacotherapy with a presumed mechanism of action of partial efficacy at the alpha4beta2 nicotinic acetylcholine receptor (nAChR); however, the extent to which daily varenicline use leads to changes in nAChR sensitivity is unclear. Varenicline 0-11 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 126-158 30398980-1 2019 Varenicline is a smoking cessation pharmacotherapy with a presumed mechanism of action of partial efficacy at the alpha4beta2 nicotinic acetylcholine receptor (nAChR); however, the extent to which daily varenicline use leads to changes in nAChR sensitivity is unclear. Varenicline 0-11 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 160-165 30398980-1 2019 Varenicline is a smoking cessation pharmacotherapy with a presumed mechanism of action of partial efficacy at the alpha4beta2 nicotinic acetylcholine receptor (nAChR); however, the extent to which daily varenicline use leads to changes in nAChR sensitivity is unclear. Varenicline 0-11 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 239-244 30472464-8 2019 Further, the smoking cessation agents, nicotine, varenicline and cytisine increased activation of mutant (alpha4)3(beta2)2 receptors, while only nicotine increased activation of mutant (alpha4)2(beta2)3 receptors. Varenicline 49-60 potassium calcium-activated channel subfamily M regulatory beta subunit 2 Homo sapiens 106-120 29498158-1 2019 Varenicline, a nicotinic acetylcholine receptor partial agonist, is used to treat nicotine dependence. Varenicline 0-11 cholinergic receptor nicotinic alpha 2 subunit Rattus norvegicus 15-47 30472464-8 2019 Further, the smoking cessation agents, nicotine, varenicline and cytisine increased activation of mutant (alpha4)3(beta2)2 receptors, while only nicotine increased activation of mutant (alpha4)2(beta2)3 receptors. Varenicline 49-60 potassium calcium-activated channel subfamily M regulatory beta subunit 2 Homo sapiens 186-200 29671814-3 2018 In this study, we investigated whether varenicline, a partial &alpha;4&beta;2*nAChR agonist which reduces nicotine, alcohol and sucrose consumption, can reduce stress, a driving factor in substance use disorders. Varenicline 39-50 immunoglobulin (CD79A) binding protein 1 Mus musculus 67-74 30501536-1 2018 BACKGROUND: Varenicline, a partial agonist of the alpha4beta2 nicotinic acetylcholine receptor (alpha4beta2-nAChR), is currently used to facilitate smoking cessation. Varenicline 12-23 cholinergic receptor nicotinic beta 1 subunit Rattus norvegicus 108-113 29860057-2 2018 This study aimed to determine if varenicline (1 mg BID) resulted in reduced methamphetamine use compared to placebo among treatment-seeking MA-dependent volunteers. Varenicline 33-44 BH3 interacting domain death agonist Homo sapiens 51-54 29860196-1 2018 Varenicline, a partial agonist for alpha4beta2* nicotinic acetylcholine receptors (nAChRs) and a full agonist for alpha3beta4 and alpha7 nAChRs, is approved for smoking cessation treatment. Varenicline 0-11 integrin alpha 7 Mus musculus 130-136 29860196-7 2018 The blockade of nicotine reward by varenicline (0.1 mg/kg) was preserved in alpha7 knockout mice but reduced in alpha5 knockout mice. Varenicline 35-46 integrin alpha 7 Mus musculus 76-82 29059422-2 2018 Unlike US Food and Drug administration approved smoke cessation aids (nicotine and varenicline) which act as nicotinic acetylcholine receptors (nAChRs) agonists, desformylflustrabromine (dFBr) acts as a nAChR positive allosteric modulator with higher selectivity to the alpha4beta2 nAChR. Varenicline 83-94 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 144-149 29059422-2 2018 Unlike US Food and Drug administration approved smoke cessation aids (nicotine and varenicline) which act as nicotinic acetylcholine receptors (nAChRs) agonists, desformylflustrabromine (dFBr) acts as a nAChR positive allosteric modulator with higher selectivity to the alpha4beta2 nAChR. Varenicline 83-94 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 203-208 29064842-2 2018 Varenicline tartrate is a partial agonist at alpha4beta2 and full agonist at alpha7 neuronal nAChR subunits. Varenicline 0-20 cholinergic receptor nicotinic beta 1 subunit Rattus norvegicus 93-98 30042025-6 2018 Our findings demonstrate that varenicline likely has an anti-inflammatory property including reduced inflammatory cell recruitment in lung tissue to protect PPE-induced alveolar expansion via alpha7 nAChR. Varenicline 30-41 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 199-204 29671814-3 2018 In this study, we investigated whether varenicline, a partial &alpha;4&beta;2*nAChR agonist which reduces nicotine, alcohol and sucrose consumption, can reduce stress, a driving factor in substance use disorders. Varenicline 39-50 hemoglobin, beta adult minor chain Mus musculus 79-85 29671814-3 2018 In this study, we investigated whether varenicline, a partial &alpha;4&beta;2*nAChR agonist which reduces nicotine, alcohol and sucrose consumption, can reduce stress, a driving factor in substance use disorders. Varenicline 39-50 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 86-91 29329763-17 2018 In the ITT analysis, varenicline was associated with a higher proportion of patients achieving continuous abstinence over the study period (week 9-48): 18 (15%, 95% CI 8-21) of 123 in the varenicline group versus eight (6%, 2-11) of 124 in the placebo group, adjusted odds ratio (OR) 2 5 (95% CI 1 0-6 1; p=0 041). Varenicline 21-32 olfactory receptor family 3 subfamily A member 4 pseudogene Homo sapiens 268-287 29117796-0 2018 Effects of varenicline therapy in combination with advanced behavioral support on smoking cessation and quality of life in inpatients with acute exacerbation of COPD, bronchial asthma, or community-acquired pneumonia: A prospective, open-label, preference-based, 52-week, follow-up trial. Varenicline 11-22 COPD Homo sapiens 161-165 29117796-13 2018 Varenicline in combination with behavioral support resulted in high abstinence rates inpatients hospitalized for exacerbation of COPD, asthma attack, or CAP, and improved QoL. Varenicline 0-11 COPD Homo sapiens 129-133 28804929-8 2018 At 12 weeks, the relative benefits of varenicline were found to be influenced by the setting in which advice was provided [P < 0.001 for interaction pharmacotherapy x setting; adjusted odds ratio for varenicline x pharmacy setting = 0.53 (95% CI = 0.42, 0.69) and for varenicline x general practice (GP) setting = 0.79 (95% CI = 0.64, 0.98) against a baseline of 1 for varenicline x community setting]. Varenicline 38-49 ring finger protein 130 Homo sapiens 300-302 28804929-11 2018 CONCLUSIONS: Varenicline use was associated with higher smoking cessation rates than nicotine replacement therapy in routine clinical practice, irrespective of a wide range of smoker characteristics, but the difference was less in certain intervention settings, most notably pharmacy but also GP practice, compared with community setting. Varenicline 13-24 ring finger protein 130 Homo sapiens 293-295 28797614-8 2017 Varenicline treatment was associated with reduced EGFP expression and increased GAP43 expression in the striatum of MacGreen mice. Varenicline 0-11 growth associated protein 43 Mus musculus 80-85 29196725-3 2017 To investigate the role of polymorphisms in nAChR genes on smoking quantity and the outcome of smoking-cessation therapies, we carried out an association study on 337 smokers who underwent pharmacotherapy with varenicline, bupropion, nicotine replacement therapy (NRT) alone, or NRT plus bupropion. Varenicline 210-221 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 44-49 28842382-0 2017 Varenicline promotes endothelial cell migration by lowering vascular endothelial-cadherin levels via the activated alpha7 nicotinic acetylcholine receptor-mitogen activated protein kinase axis. Varenicline 0-11 cadherin 5 Homo sapiens 60-89 28842382-6 2017 Varenicline (100muM) markedly promoted migration of HUVECs and decreased expression of vascular endothelial (VE)-cadherin, an endothelial adhesion molecule. Varenicline 0-11 cadherin 5 Homo sapiens 87-121 28842382-7 2017 Extracellular signal-regulated kinase (ERK), p38 and c-Jun N-terminal kinase (JNK) signaling were markedly activated by varenicline. Varenicline 120-131 mitogen-activated protein kinase 1 Homo sapiens 0-37 28842382-7 2017 Extracellular signal-regulated kinase (ERK), p38 and c-Jun N-terminal kinase (JNK) signaling were markedly activated by varenicline. Varenicline 120-131 mitogen-activated protein kinase 1 Homo sapiens 39-42 28842382-7 2017 Extracellular signal-regulated kinase (ERK), p38 and c-Jun N-terminal kinase (JNK) signaling were markedly activated by varenicline. Varenicline 120-131 mitogen-activated protein kinase 14 Homo sapiens 45-48 28842382-7 2017 Extracellular signal-regulated kinase (ERK), p38 and c-Jun N-terminal kinase (JNK) signaling were markedly activated by varenicline. Varenicline 120-131 mitogen-activated protein kinase 8 Homo sapiens 53-76 28842382-7 2017 Extracellular signal-regulated kinase (ERK), p38 and c-Jun N-terminal kinase (JNK) signaling were markedly activated by varenicline. Varenicline 120-131 mitogen-activated protein kinase 8 Homo sapiens 78-81 28842382-10 2017 These findings suggest that varenicline promotes HUVEC migration by lowering VE-cadherin expression due to activated ERK/p38/JNK signaling through alpha7 nAChR. Varenicline 28-39 cadherin 5 Homo sapiens 77-88 28842382-10 2017 These findings suggest that varenicline promotes HUVEC migration by lowering VE-cadherin expression due to activated ERK/p38/JNK signaling through alpha7 nAChR. Varenicline 28-39 mitogen-activated protein kinase 1 Homo sapiens 117-120 28842382-10 2017 These findings suggest that varenicline promotes HUVEC migration by lowering VE-cadherin expression due to activated ERK/p38/JNK signaling through alpha7 nAChR. Varenicline 28-39 mitogen-activated protein kinase 14 Homo sapiens 121-124 28842382-10 2017 These findings suggest that varenicline promotes HUVEC migration by lowering VE-cadherin expression due to activated ERK/p38/JNK signaling through alpha7 nAChR. Varenicline 28-39 mitogen-activated protein kinase 8 Homo sapiens 125-128 28842382-10 2017 These findings suggest that varenicline promotes HUVEC migration by lowering VE-cadherin expression due to activated ERK/p38/JNK signaling through alpha7 nAChR. Varenicline 28-39 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 154-159 28202387-0 2017 Varenicline enhances oxidized LDL uptake by increasing expression of LOX-1 and CD36 scavenger receptors through alpha7 nAChR in macrophages. Varenicline 0-11 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 112-124 28268112-1 2017 Varenicline (Champix , Chantix ) is a partial agonist of the alpha4beta2 nicotinic acetylcholine receptor (nAChR) and a full agonist of the alpha7 nAChR. Varenicline 0-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 107-112 28268112-1 2017 Varenicline (Champix , Chantix ) is a partial agonist of the alpha4beta2 nicotinic acetylcholine receptor (nAChR) and a full agonist of the alpha7 nAChR. Varenicline 0-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 147-152 28268112-1 2017 Varenicline (Champix , Chantix ) is a partial agonist of the alpha4beta2 nicotinic acetylcholine receptor (nAChR) and a full agonist of the alpha7 nAChR. Varenicline 13-20 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 107-112 28268112-1 2017 Varenicline (Champix , Chantix ) is a partial agonist of the alpha4beta2 nicotinic acetylcholine receptor (nAChR) and a full agonist of the alpha7 nAChR. Varenicline 13-20 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 147-152 28268112-1 2017 Varenicline (Champix , Chantix ) is a partial agonist of the alpha4beta2 nicotinic acetylcholine receptor (nAChR) and a full agonist of the alpha7 nAChR. Varenicline 23-30 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 107-112 28268112-1 2017 Varenicline (Champix , Chantix ) is a partial agonist of the alpha4beta2 nicotinic acetylcholine receptor (nAChR) and a full agonist of the alpha7 nAChR. Varenicline 23-30 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 147-152 28268112-3 2017 Varenicline has been associated with adverse cardiovascular (CV) events, including myocardial infarction, which may be caused by activation of the alpha7 nAChR receptor that in turn stimulates parasympathetic output from the brainstem to the heart, release of catecholamines, and has a prothrombotic effect. Varenicline 0-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 154-159 28202387-3 2017 We have reported that varenicline aggravates formation of atherosclerotic plaques through alpha7 nAChR in apolipoprotein E knockout mice. Varenicline 22-33 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 90-102 28202387-10 2017 These effects of varenicline were blocked significantly by an alpha7 nAChR antagonist, methyllycaconitine (MLA) (50nM), but not by an alpha4beta2 nAChR antagonist, dihydro-beta-erythroidine hydrobromide (DHbetaE) (1muM). Varenicline 17-28 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 62-74 28202387-11 2017 These data suggest that varenicline promotes oxLDL uptake by upregulating expression of LOX-1 and CD36 through alpha7 nAChR in macrophages. Varenicline 24-35 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 111-123 28202387-12 2017 We found that varenicline significantly activated extracellular signal-regulated kinase 1/2 (ERK1/2) and nuclear factor-kappa B (NF-kappaB) signaling pathways in RAW264.7 cells. Varenicline 14-25 mitogen-activated protein kinase 3 Mus musculus 50-91 28202387-12 2017 We found that varenicline significantly activated extracellular signal-regulated kinase 1/2 (ERK1/2) and nuclear factor-kappa B (NF-kappaB) signaling pathways in RAW264.7 cells. Varenicline 14-25 mitogen-activated protein kinase 3 Mus musculus 93-99 28202387-12 2017 We found that varenicline significantly activated extracellular signal-regulated kinase 1/2 (ERK1/2) and nuclear factor-kappa B (NF-kappaB) signaling pathways in RAW264.7 cells. Varenicline 14-25 nuclear factor of kappa light polypeptide gene enhancer in B cells 1, p105 Mus musculus 105-127 28202387-12 2017 We found that varenicline significantly activated extracellular signal-regulated kinase 1/2 (ERK1/2) and nuclear factor-kappa B (NF-kappaB) signaling pathways in RAW264.7 cells. Varenicline 14-25 nuclear factor of kappa light polypeptide gene enhancer in B cells 1, p105 Mus musculus 129-138 28202387-14 2017 Therefore, ERK1/2-NF-kappaB signaling pathway is highly likely to be responsible for varenicline-induced upregulation of LOX-1 and CD36 expression through alpha7 nAChR in macrophages. Varenicline 85-96 mitogen-activated protein kinase 3 Mus musculus 11-17 28202387-14 2017 Therefore, ERK1/2-NF-kappaB signaling pathway is highly likely to be responsible for varenicline-induced upregulation of LOX-1 and CD36 expression through alpha7 nAChR in macrophages. Varenicline 85-96 nuclear factor of kappa light polypeptide gene enhancer in B cells 1, p105 Mus musculus 18-27 28202387-14 2017 Therefore, ERK1/2-NF-kappaB signaling pathway is highly likely to be responsible for varenicline-induced upregulation of LOX-1 and CD36 expression through alpha7 nAChR in macrophages. Varenicline 85-96 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 155-167 28028600-11 2017 CONCLUSIONS: These results suggest that alpha4beta2* nAChRs differentially mediate the discriminative stimulus effects of nicotine and varenicline, and suggest that varenicline has substantial non-alpha4beta2 nAChR activity. Varenicline 165-176 cholinergic receptor, nicotinic, alpha polypeptide 7 Mus musculus 53-58 27805736-1 2017 Varenicline is a nicotinic acetylcholine receptor (nAChR) agonist used to treat nicotine addiction, but a live debate persists concerning its mechanism of action in reducing nicotine consumption. Varenicline 0-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 17-49 27805736-1 2017 Varenicline is a nicotinic acetylcholine receptor (nAChR) agonist used to treat nicotine addiction, but a live debate persists concerning its mechanism of action in reducing nicotine consumption. Varenicline 0-11 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 51-56 27805736-2 2017 Although initially reported as alpha4beta2 selective, varenicline was subsequently shown to activate other nAChR subtypes implicated in nicotine addiction including alpha3beta4. Varenicline 54-65 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 107-112 27805736-5 2017 Varenicline and nicotine activated alpha3beta4* nAChRs with EC50 values of 1.8 (1.2-2.7) muM and 19.4 (11.1-33.9) muM, respectively. Varenicline 0-11 latexin Homo sapiens 89-92 27805736-5 2017 Varenicline and nicotine activated alpha3beta4* nAChRs with EC50 values of 1.8 (1.2-2.7) muM and 19.4 (11.1-33.9) muM, respectively. Varenicline 0-11 latexin Homo sapiens 114-117 27617367-9 2016 Varenicline with BT increased abstinence more than other combinations of a pharmacotherapy with BT (varenicline versus bupropion: OR=1.56, 95% credible interval [CrI]=1.07, 2.34; varenicline versus nicotine patch: OR=1.65, 95% CrI=1.10, 2.51; varenicline versus short-acting nicotine-replacement therapies: OR=1.68, 95% CrI=1.15, 2.53). Varenicline 0-11 EP300 interacting inhibitor of differentiation 1 Homo sapiens 227-232 27617367-9 2016 Varenicline with BT increased abstinence more than other combinations of a pharmacotherapy with BT (varenicline versus bupropion: OR=1.56, 95% credible interval [CrI]=1.07, 2.34; varenicline versus nicotine patch: OR=1.65, 95% CrI=1.10, 2.51; varenicline versus short-acting nicotine-replacement therapies: OR=1.68, 95% CrI=1.15, 2.53). Varenicline 0-11 EP300 interacting inhibitor of differentiation 1 Homo sapiens 320-325