Search Results - "Dordal, Alberto"
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N-substituted-1,2,3-triazoles: synthesis, characterization and evaluation as cannabinoid ligands
Published in ARKIVOC (20-05-2010)Get full text
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Chronic 5‐HT6 receptor modulation by E‐6837 induces hypophagia and sustained weight loss in diet‐induced obese rats
Published in British journal of pharmacology (01-08-2006)“…1 E‐6837 is a novel, selective and high‐affinity 5‐HT6 receptor ligand (pKi: 9.13) which in vitro demonstrates partial agonism at a presumably silent rat 5‐HT6…”
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Sleep-Stabilizing Effects of E-6199, Compared to Zopiclone, Zolpidem and THIP in Mice
Published in Sleep (New York, N.Y.) (01-02-2008)“…Gamma aminobutyric acid (GABA)A receptor modulators constitute the majority of clinically used sedative-hypnotics. These compounds have the capacity to…”
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Medicinal Chemistry Driven Approaches Toward Novel and Selective Serotonin 5-HT6 Receptor Ligands
Published in Journal of medicinal chemistry (24-03-2005)“…Based on a medicinal chemistry guided hypothetical pharmacophore model, novel series of indolyl sulfonamides have been designed and prepared as selective and…”
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Chronic 5‐HT 6 receptor modulation by E‐6837 induces hypophagia and sustained weight loss in diet‐induced obese rats
Published in British journal of pharmacology (29-01-2009)“…E‐6837 is a novel, selective and high‐affinity 5‐HT 6 receptor ligand (p K i : 9.13) which in vitro demonstrates partial agonism at a presumably silent rat…”
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Structural–activity relationship study on C-4 carbon atom of the CB 1 antagonist SR141716: synthesis and pharmacological evaluation of 1,2,4-triazole-3-carboxamides
Published in European journal of medicinal chemistry (2006)“…A series of 1,2,4-triazole-3-carboxamides has been prepared from alkyl-1,2,4-triazole-3-carboxylates under mild conditions. The ability of these triazoles to…”
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Discovery of 5-HT sub(6) receptor ligands based on virtual HTS
Published in Bioorganic & medicinal chemistry (01-11-2007)“…Based on a pharmacophore alignment on a 5-HT sub(6) ligand applying 4SCan technology, a new lead series was identified and further structurally investigated. K…”
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Discovery of 5-HT6 receptor ligands based on virtual HTS
Published in Bioorganic & medicinal chemistry letters (15-11-2007)“…Based on a pharmacophore alignment on a 5-HT(6) ligand applying 4SCan technology, a new lead series was identified and further structurally investigated. K(i)s…”
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Structural-activity relationship study on C-4 carbon atom of the CB1 antagonist SR141716 : synthesis and pharmacological evaluation of 1,2,4-triazole-3-carboxamides
Published in European journal of medicinal chemistry (2006)“…A series of 1,2,4-triazole-3-carboxamides has been prepared from alkyl-1,2,4-triazole-3-carboxylates under mild conditions. The ability of these triazoles to…”
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Novel derivatives of 3-alkyl-1,5-diaryl-1H-1,2,4-triazoles and their pharmacological evaluation as CB1 cannabinoid ligands
Published in Monatshefte für Chemie (01-09-2008)“…In a previous study, we have identified 3-alkyl-1,5-diaryl-1 H -1,2,4-triazoles to be a novel class of cannabinoid type-1 (CB 1 ) receptor antagonists…”
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Discovery of 5-HT 6 receptor ligands based on virtual HTS
Published in Bioorganic & medicinal chemistry letters (2007)“…The discovery and SAR studies of 5-HT 6 ligands are described. Based on a pharmacophore alignment on a 5-HT 6 ligand applying 4SCan ® technology, a new lead…”
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Synthesis of New Benzoxazinone Derivatives as Neuropeptide Y5 Antagonists for the Treatment of Obesity
Published in Journal of medicinal chemistry (24-03-2005)“…Screening of our internal chemical collection against the neuropeptide Y5 (NPY Y5) receptor allowed the identification of a benzoxazine derivative 5f as a hit…”
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A Medicinal-Chemistry-Guided Approach to Selective and Druglike Sigma 1 Ligands
Published in ChemMedChem (01-01-2006)“…Based on a medicinal‐chemistry‐guided approach, three novel series of druglike cycloalkyl‐annelated pyrazoles were synthesized and display high affinity (pKi…”
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Medicinal Chemistry Driven Approaches Toward Novel and Selective Serotonin 5-HT 6 Receptor Ligands
Published in Journal of medicinal chemistry (01-03-2005)Get full text
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A preliminary study of the metabolic stability of a series of benzoxazinone derivatives as potent neuropeptide Y5 antagonists
Published in Bioorganic & medicinal chemistry letters (15-08-2005)“…The metabolic stability of benzoxazinone derivatives, a potent series of NPY5 antagonists, has been investigated. This study identified the moieties prone to…”
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Effects of K+ channel blockers and openers on antinociception induced by agonists of 5-HT1A receptors
Published in European journal of pharmacology (11-01-1996)“…The modulation by K+ channel-acting drugs of the antinociceptive effect of several 5-HT1A receptor agonists was examined with the hot plate test in mice. All…”
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Effects of K + channel blockers and openers on antinociception induced by agonists of 5-HT 1A receptors
Published in European journal of pharmacology (1996)“…The modulation by K + channel-acting drugs of the antinociceptive effect of several 5-HT 1A receptor agonists was examined with the hot plate test in mice. All…”
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