Search Results - "Kapui, Zoltan"
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Analysis of functional selectivity through G protein-dependent and -independent signaling pathways at the adrenergic α(2C) receptor
Published in Brain research bulletin (01-08-2014)“…Although G protein-coupled receptors (GPCRs) are traditionally categorized as Gs-, Gq-, or Gi/o-coupled, their signaling is regulated by multiple mechanisms…”
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Journal Article -
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Interaction of SSR161421, a novel specific adenosine A(3) receptor antagonist with adenosine A(3) receptor agonists both in vitro and in vivo
Published in European journal of pharmacology (15-01-2013)“…A novel adenosine A(3) receptor antagonist (SSR161421) was characterized by both receptor binding assays and pharmacological tests. Binding studies on cloned…”
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Journal Article -
3
Identification of potential glutaminyl cyclase inhibitors from lead-like libraries by in silico and in vitro fragment-based screening
Published in Molecular diversity (01-02-2017)“…A glutaminyl cyclase (QC) fragment library was in silico selected by disconnection of the structure of known QC inhibitors and by lead-like 2D virtual…”
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Journal Article -
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The influence of 5-HT2A activity on a 5-HT2C specific in vivo assay used for early identification of multiple acting SERT and 5-HT2C receptor ligands
Published in Bioorganic & medicinal chemistry letters (01-02-2016)“…[Display omitted] As a result of our exploratory programme aimed at elaborating dually acting compounds towards the serotonin (5-HT) transporter (SERT) and the…”
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Journal Article -
5
Analysis of functional selectivity through G protein-dependent and -independent signaling pathways at the adrenergic alpha 2C receptor
Published in Brain research bulletin (01-08-2014)“…Although G protein-coupled receptors (GPCRs) are traditionally categorized as Gs-, Gq-, or Gi/o-coupled, their signaling is regulated by multiple mechanisms…”
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Journal Article -
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The influence of 5-HT sub(2A) activity on a 5-HT sub(2C) specific in vivo assay used for early identification of multiple acting SERT and 5-HT sub(2C) receptor ligands
Published in Bioorganic & medicinal chemistry letters (01-02-2016)“…As a result of our exploratory programme aimed at elaborating dually acting compounds towards the serotonin (5-HT) transporter (SERT) and the 5-HT sub(2C)…”
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Journal Article -
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Biochemical and pharmacological characterization of 2-(9-(2-piperidinoethoxy)-4-oxo-4H-pyrido[1,2-a]pyrimidin-2-yloxymethyl)-4-(1-methylethyl)-6-methoxy-1,2-benzisothiazol-3(2H)-one-1,1-dioxide (SSR69071), a novel, orally active elastase inhibitor
Published in The Journal of pharmacology and experimental therapeutics (01-05-2003)“…Human leukocyte elastase (HLE) is a proteinase capable of degrading a variety of proteins. Under normal circumstances, the proteolytic activity of HLE is…”
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A novel orally active inhibitor of HLE
Published in European journal of medicinal chemistry (01-04-2003)“…Human leukocyte elastase (HLE) is a serine proteinase, capable of degrading a variety of structural matrix proteins. SSR69071…”
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Journal Article Conference Proceeding -
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Analysis of functional selectivity through G protein-dependent and -independent signaling pathways at the adrenergic α2C receptor
Published in Brain research bulletin (01-08-2014)“…Highlights • Comparative pharmacology of four α2C -AR related signaling pathways was carried out. • We quantify the level of biased signaling by applying an…”
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Journal Article -
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Poster #S17 ARE DOPAMINE PARTIAL AGONIST ANTIPSYCHOTICS SIMILAR? PRECLINICAL COMPARISON OF ARIPIPRAZOLE, BIFEPRUNOX AND CARIPRAZINE
Published in Schizophrenia research (01-04-2014)Get full text
Journal Article -
11
SSR69071, an elastase inhibitor, reduces myocardial infarct size following ischemia–reperfusion injury
Published in European journal of pharmacology (07-02-2003)“…Neutrophil elastase contributes to the severity of cardiac damage following coronary ischemia and reperfusion. We evaluated the effects of…”
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Interaction of SSR161421, a novel specific adenosine A3 receptor antagonist with adenosine A3 receptor agonists both in vitro and in vivo
Published in European journal of pharmacology (15-01-2013)“…A novel adenosine A3 receptor antagonist (SSR161421) was characterized by both receptor binding assays and pharmacological tests. Binding studies on cloned…”
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Journal Article -
14
Novel Small-Molecule Inhibitors of Phosphodiesterase 4 Isoenzyme and Human Leukocyte Elastase in the Treatment of Airway Diseases
Published 01-01-2009“…Asthma and chronic obstructive pulmonary disease (COPD) are common, severe inflammatory diseases of the respiratory tract for which there is no efficient…”
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Dissertation -
15
The influence of 5-HT(2A) activity on a 5-HT(2C) specific in vivo assay used for early identification of multiple acting SERT and 5-HT(2C) receptor ligands
Published in Bioorganic & medicinal chemistry letters (01-02-2016)“…As a result of our exploratory programme aimed at elaborating dually acting compounds towards the serotonin (5-HT) transporter (SERT) and the 5-HT2C receptor a…”
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Journal Article -
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Experimental studies on guanosine 3', 5'-cyclic monophosphate levels and airway responsiveness of the novel phosphodiesterase type 5 inhibitor SR 265579 in guinea-pigs
Published in Arzneimittel-Forschung (01-08-1999)“…The effect of 1-cyclopentyl-3-ethyl-6-(3-ethoxypyrid-4-yl)- 1H-pyrazolo[3,4-d]pyrimidin-4-one (SR 265579), a potent inhibitor of guanosine 3',5'-cyclic…”
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Journal Article -
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Experimental studies on the antitussive properties of the new xanthine derivative 1H-purine-2,6-dione, 3,7-dihydro-3-methyl-7[(5-methyl-1,2,4-oxadiazol-3-yl)methyl]. 2nd communication: investigations on theophylline-like activities
Published in Arzneimittel-Forschung (01-12-1997)“…CH-13584 (formerly: KHL-8425, 1H-purine-2,6-dione, 3,7-dihydro-3-methyl-7[(5-methyl-1,2,4-oxadiazol-3-yl)methyl], CAS 115779-20-9) is a new xanthine…”
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Journal Article -
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Experimental studies on the antitussive properties of the new xanthine derivative 1H-purine-2,6-dione, 3,7-dihydro-3-methyl-7[(5-methyl-1,2,4-oxadiazol-3-yl) methyl]. 3rd communication: examinations on opioid mechanisms and physical drug dependence
Published in Arzneimittel-Forschung (01-12-1998)“…CH-13584 (formerly: KHL-8425, 1H-purine-2,6-dione, 3,7-dihydro-3-methyl-7[(5-methyl-1,2,4-oxadiazol-3-yl)methyl], CAS 115779-20-9) showed antitussive effect on…”
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Journal Article