PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 19959340-0 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 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 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 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 19501054-2 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 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 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 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 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 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 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