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Auteur Hans Rollema |
Documents disponibles écrits par cet auteur (4)
Ajouter le résultat dans votre panier Affiner la recherchePharmacological profile of the alpha4beta2 nicotinic acetylcholine receptor partial agonist varenicline, an effective smoking cessation tool / Hans Rollema (2007)
Titre : Pharmacological profile of the alpha4beta2 nicotinic acetylcholine receptor partial agonist varenicline, an effective smoking cessation tool Type de document : texte imprimé Auteurs : Hans Rollema, Auteur ; L. K. Chambers, Auteur ; Jotham W. Coe, Auteur Année de publication : 2007 Importance : p. 985-994 Présentation : ill., graph., tab. Langues : Anglais (eng) Catégories : [TABAC] chimie du tabac:constituant:alcaloïde:nicotine:récepteur nicotinique Index. décimale : TA 6.2.3 Approche pharmacologique Résumé : The preclinical pharmacology of the alpha4beta2 nicotinic acetylcholine receptor (nAChR) partial agonist varenicline, a novel smoking cessation agent is described. Varenicline binds with subnanomolar affinity only to alpha4beta2 nAChRs and in vitro functional patch clamp studies in HEK cells expressing nAChRs show that varenicline is a partial agonist with 45% of nicotine's maximal efficacy at alpha4beta2 nAChRs. In neurochemical models varenicline has significantly lower (40-60%) efficacy than nicotine in stimulating [(3)H]-dopamine release from rat brain slices in vitro and in increasing dopamine release from rat nucleus accumbens in vivo, while it is more potent than nicotine. In addition, when combined with nicotine, varenicline effectively attenuates the nicotine-induced dopamine release to the level of the effect of varenicline alone, consistent with partial agonism. Finally, varenicline reduces nicotine self-administration in rats and supports lower self-administration break points than nicotine. These data suggest that varenicline can reproduce to some extent the subjective effects of smoking by partially activating alpha4beta2 nAChRs, while preventing full activation of these receptors by nicotine. Based on these findings, varenicline was advanced into clinical development and recently shown to be an effective and safe aid for smoking cessation treatment. En ligne : https://www.sciencedirect.com/science/article/abs/pii/S0028390806003789?via%3Dih [...] Format de la ressource électronique : PDF, HTML Permalink : https://biblio.fares.be/opac_css/index.php?lvl=notice_display&id=8374 Exemplaires (1)
Code-barres Cote Support Localisation Section Disponibilité TA 006005 TA 6.2.3 ROL P Article/Périodique Bibliothèque FARES Tabac Consultation sur place
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Titre : Rationale, pharmacology and clinical efficacy of partial agonists of alpha4beta2 nACh receptors for smoking cessation Type de document : texte imprimé Auteurs : Hans Rollema, Auteur ; Jotham W. Coe, Auteur ; L. K. Chambers, Auteur ; Raymond S. Hurst, Auteur Editeur : Elsevier Science Direct Année de publication : 2007 Collection : Trends in pharmacological sciences num. 28:7 Importance : p. 316-325 Présentation : ill., graph., tab. Langues : Anglais (eng) Catégories : [TABAC] chimie du tabac:constituant:alcaloïde:nicotine:récepteur nicotinique Index. décimale : TA 6.2.3 Approche pharmacologique Résumé : Most smokers repeatedly fail in their attempts to stop smoking because of the addictive nature of the nicotine in tobacco products. Nicotine dependence is probably mediated through the activation of multiple subtypes of neuronal nicotinic acetylcholine receptor (nAChR), among which the mesolimbic alpha(4)beta(2) subtype has a pivotal role. Here, we discuss the rationale for and the design of alpha(4)beta(2) nAChR partial agonists as novel treatments for tobacco addiction. Such agents are expected to exhibit a dual action by sufficiently stimulating alpha(4)beta(2)-nAChR-mediated dopamine release to reduce craving when quitting and by inhibiting nicotine reinforcement when smoking. Potent and selective alpha(4)beta(2) nAChR partial agonists that exhibit dual agonist and antagonist activity in preclinical models can be identified. The validity of this approach is demonstrated by the clinical efficacy of the alpha(4)beta(2) nAChR partial agonist varenicline, which has significantly better quit rates than do other treatments and offers a new option for smoking cessation pharmacotherapy. En ligne : https://doi.org/10.1016/j.tips.2007.05.003 Format de la ressource électronique : PDF, HTML Permalink : https://biblio.fares.be/opac_css/index.php?lvl=notice_display&id=8367 Exemplaires (1)
Code-barres Cote Support Localisation Section Disponibilité TA 005998 TA 6.2.3 ROL R Article/Périodique Bibliothèque FARES Tabac Consultation sur place
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Titre : Varenicline has antidepressant-like in activity in the forced swim test augments sertraline's effect Type de document : texte imprimé Auteurs : Hans Rollema, Auteur ; Victor Guanowsky, Auteur ; Yann S. Mineur, Auteur Editeur : Elsevier Science Direct Année de publication : 2009 Collection : European Journal of Pharmacology, ISSN 0014-2999 num. Vol 605 Importance : p. 114-116 Présentation : graph. Langues : Anglais (eng) Catégories : [TABAC] étude
[TABAC] sevrage tabagique:méthode de sevrage:méthode individuelle:approche pharmacologique:varéniclineIndex. décimale : TA 6.2.3.1.4 Autres substituts nicotiniques Résumé : Varenicline, an alpha4beta2 nicotinic acetylcholine receptor partial agonist developed as a smoking cessation aid, showed antidepressant-like activity in the forced swim test in two mouse strains. In addition, a low varenicline dose significantly enhanced the effects of moderately active doses of the selective serotonin reuptake inhibitor sertraline. These findings are consistent with the notion that reducing alpha4beta2 nicotinic acetylcholine receptor activity either by antagonists or by partial agonists that can partially activate or desensitize acetylcholine receptors is associated with antidepressant-like properties. These data suggest that varenicline may have antidepressant potential and can, when combined, augment antidepressant responses of selective serotonin reuptake inhibitors. Permalink : https://biblio.fares.be/opac_css/index.php?lvl=notice_display&id=7946 Exemplaires (1)
Code-barres Cote Support Localisation Section Disponibilité TA 005487 TA 6.2.3.1.4 ROL V Article/Périodique Bibliothèque FARES Tabac Consultation sur place
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Titre : Varenicline : new treatment with efficacy in smoking cessation Type de document : texte imprimé Auteurs : Victor I. Reus, Auteur ; R. Scott Obach, Auteur ; Jotham W. Coe, Auteur ; Helene Faessel, Auteur ; Hans Rollema, Auteur ; Eric Watsky, Auteur ; Karen Reeves, Auteur Editeur : Barcelona [Espagne] : Thomson Reuters Année de publication : 2007 Collection : Drugs of today, ISSN 1699-3993 num. 43(2) Importance : p.65-75 Langues : Anglais (eng) Catégories : [TABAC] sevrage tabagique
[TABAC] sevrage tabagique:efficacité du sevrage
[TABAC] sevrage tabagique:méthode de sevrage:méthode individuelle:approche pharmacologique:varéniclineIndex. décimale : TA 6.2.3.1.4 Autres substituts nicotiniques Résumé : Smoking is a significant public health problem, and existing treatments have demonstrated only moderate efficacy in assisting smokers to quit. 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). It has both agonistic and antagonistic properties that together are believed to account for reduction of craving and withdrawal as well as blocking the rewarding effects of smoking. The clinical efficacy and tolerability of varenicline has been demonstrated in phase III clinical trials involving more than 2,000 cigarette smokers. At the end of the treatment period in two 12-week, multicenter, randomized, double-blind, placebo-controlled studies, patients receiving varenicline (1 mg twice daily) experienced an increase in the odds of quitting smoking by nearly fourfold compared with those receiving placebo, and almost twofold compared with the odds for patients receiving 150 mg bupropion SR (sustained release) twice daily. In these two trials where patients were randomized to either varenicline or bupropion, the efficacy of varenicline was consistently superior at 12 weeks; this result sustained significance at 24 weeks in both studies and up to 52 weeks in one study. Nausea, a common adverse event reported in clinical trials, led to few treatment discontinuations. Its targeted mechanism of action, superior efficacy and excellent tolerability make varenicline a welcome and useful addition to the therapeutic options for smoking cessation. En ligne : https://journals.prous.com/journals/servlet/xmlxsl/pk_journals.xml_summary_pr?p_ [...] Format de la ressource électronique : PDF, HTML Permalink : https://biblio.fares.be/opac_css/index.php?lvl=notice_display&id=7932 Aucun avis, veuillez vous identifier pour ajouter le vôtre !
