Search Results - "Kurkó, Dalma"
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Discovery and Characterization of RGH-122, a Potent, Selective, and Orally Bioavailable V1a Receptor Antagonist
Published in Journal of medicinal chemistry (11-01-2024)“…The V1a receptor is a major contributor in mediating the social and emotional effects of arginine-vasopressin (AVP); therefore it represents a promising target…”
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Controlling receptor function from the extracellular vestibule of G-protein coupled receptors
Published in Chemical communications (Cambridge, England) (25-11-2020)“…Receptor function is traditionally controlled from the orthosteric binding site of G-protein coupled receptors. Here, we show that the functional activity and…”
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New V1a receptor antagonist. Part 1. Synthesis and SAR development of urea derivatives
Published in Bioorganic & medicinal chemistry letters (15-09-2020)“…[Display omitted] Solid preclinical evidence links vasopressin to social behavior in animals, so, extensive work has been initiated to find new vasopressin V1a…”
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Preclinical pharmacodynamic and pharmacokinetic characterization of the major metabolites of cariprazine
Published in Drug design, development and therapy (01-09-2019)“…Cariprazine, a dopamine D -preferring D /D receptor partial agonist and serotonin 5-HT receptor partial agonist, has two major human metabolites,…”
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GluN2B-containing NMDA receptors as possible targets for the neuroprotective and antidepressant effects of fluoxetine
Published in Neurochemistry international (01-01-2012)“…► Whole-cell patch-clamp recordings of cortical neurons and HEK 293 cells were used. ► Inhibitory effect of drugs on GluN2A-containing and GluN2B-containing…”
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Discovery of New Heterocyclic Ring Systems as Novel and Potent V 1A Receptor Antagonists
Published in ACS chemical neuroscience (04-11-2020)Get full text
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Discovery of New Heterocyclic Ring Systems as Novel and Potent V1A Receptor Antagonists
Published in ACS chemical neuroscience (04-11-2020)“…Autism spectrum disorder is a neurodevelopmental disease with increasing occurrence. Recent studies focus on the development of novel V1A receptor antagonists…”
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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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Hit-to-lead optimization of disubstituted oxadiazoles and tetrazoles as mGluR5 NAMs
Published in Bioorganic & medicinal chemistry letters (15-06-2010)“…Here we report the discovery and early SAR of a series of mGluR5 negative allosteric modulators (NAMs). Starting from a moderately active HTS hit we…”
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Carbamoyloximes as novel non-competitive mGlu5 receptor antagonists
Published in Bioorganic & medicinal chemistry letters (01-08-2010)“…Hit-to-lead optimization of a HTS hit led to new carbamoyloxime derivatives. After identification of an advanced hit (8d) the CYP enzyme inhibitory activity of…”
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New V1a receptor antagonist. Part 2. Identification and optimization of triazolobenzazepines
Published in Bioorganic & medicinal chemistry letters (15-09-2020)“…[Display omitted] Solid preclinical evidence links vasopressin to social behavior in animals, so, extensive work has been initiated to find new vasopressin V1a…”
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Cell-based and virtual fragment screening for adrenergic α2C receptor agonists
Published in Bioorganic & medicinal chemistry (15-07-2015)“…[Display omitted] Fragment-based drug discovery has emerged as an alternative to conventional lead identification and optimization strategies generally…”
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Inducible expression and pharmacological characterization of recombinant rat NR1a/NR2A NMDA receptors
Published in Neurochemistry international (01-04-2005)“…In this study, we have established a non-neuronal cell line stably and inducibly expressing recombinant NMDA receptors (NRs) composed of rat NR1a/NR2A…”
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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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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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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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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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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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