Search Results - "Perdona, Elisabetta"
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Novel morpholine scaffolds as selective dopamine (DA) D3 receptor antagonists
Published in Bioorganic & medicinal chemistry letters (15-02-2016)“…[Display omitted] A new series of morpholine derivatives has been identified as selective DA D3 receptor antagonists; their in vitro profile and…”
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Affinity, potency, efficacy, and selectivity of neurokinin A analogs at human recombinant NK2 and NK1 receptors
Published in PloS one (25-10-2018)“…A series of peptide NK2 receptor agonists was evaluated for affinity, potency, efficacy, and selectivity at human recombinant NK2 and NK1 receptors expressed…”
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Functional and binding kinetic studies make a distinction between OX1 and OX2 orexin receptor antagonists
Published in European journal of pharmacology (05-10-2012)“…In this work the pharmacology and the receptor kinetics of the following orexin receptor antagonists SB-649868, ACT-078573, JNJ-10397049, MK-6096 and Roche-Cp…”
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Distinct receptor subtypes mediate arginine vasopressin-dependent ACTH release and intracellular calcium mobilization in rat pituitary cells
Published in European journal of pharmacology (15-03-2012)“…In the present study, adrenocorticotropic hormone (ACTH) release and intracellular calcium ([Ca2+]i) increase induced by arginine vasopressin (AVP) were…”
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In vitro and in vivo characterization of the novel GABA B receptor positive allosteric modulator, 2-{1-[2-(4-chlorophenyl)-5-methylpyrazolo[1,5-a]pyrimidin-7-yl]-2-piperidinyl}ethanol (CMPPE)
Published in Neuropharmacology (01-10-2011)“…There is preclinical evidence supporting the finding that the GABA B receptor orthosteric agonist, baclofen, has significant effects on eating behavior…”
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In vitro and in vivo characterization of the novel GABAB receptor positive allosteric modulator, 2-{1-[2-(4-chlorophenyl)-5-methylpyrazolo[1,5-a]pyrimidin-7-yl]-2-piperidinyl}ethanol (CMPPE)
Published in Neuropharmacology (01-10-2011)“…There is preclinical evidence supporting the finding that the GABA(B) receptor orthosteric agonist, baclofen, has significant effects on eating behavior…”
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Azabicyclo[3.1.0]hexane-1-carbohydrazides as Potent and Selective GHSR1a Ligands Presenting a Specific in vivo Behavior
Published in ChemMedChem (04-11-2011)“…Buon appetito! The synthesis and in vitro and in vivo profiles of a novel series of potent and selective ghrelin ligands is presented. Selected compounds share…”
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Discovery Process and Characterization of Novel Carbohydrazide Derivatives as Potent and Selective GHSR1a Antagonists
Published in ChemMedChem (03-09-2010)“…Ghrelins: don't feed them after dark! A novel class of highly potent and selective growth hormone secretagogue receptor 1a (GHSR1a) antagonists has been…”
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1,2,4-Triazolyl 5‑Azaspiro[2.4]heptanes: Lead Identification and Early Lead Optimization of a New Series of Potent and Selective Dopamine D3 Receptor Antagonists
Published in Journal of medicinal chemistry (22-09-2016)“…A novel series of 1,2,4-triazolyl 5-azaspiro[2.4]heptanes with high affinity and selectivity at the dopamine (DA) D3 receptor (D3R) is described. Some of…”
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Pharmacological characterization of the ghrelin receptor antagonist, GSK1614343 in rat RC-4B/C cells natively expressing GHS type 1a receptors
Published in European journal of pharmacology (10-01-2011)“…A novel growth hormone secretagogues type 1a (GHS1a) receptors antagonist (2R)-N'-[3,5-…”
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Development of novel multipotent compounds modulating endocannabinoid and dopaminergic systems
Published in European journal of medicinal chemistry (01-12-2019)“…Polypharmacology approaches may help the discovery of pharmacological tools for the study or the potential treatment of complex and multifactorial diseases as…”
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Potency, efficacy, and selectivity of GR64349 at human recombinant neurokinin NK2 and NK1 receptors
Published in Neuroscience letters (15-10-2019)“…•The affinity and potency of GR64349 for NK2 and NK1 receptors was examined.•Binding affinity was ˜1200-fold higher for NK2 than NK1 receptors.•Potency was…”
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In vitro and in vivo characterization of the novel GABA sub(B receptor positive allosteric modulator, 2-{1-[2-(4-chlorophenyl)-5-methylpyrazolo[1,5-a]pyrimidin-7-yl]-2- p iperidinyl}ethanol (CMPPE))
Published in Neuropharmacology (01-11-2011)“…There is preclinical evidence supporting the finding that the GABA sub(B receptor orthosteric agonist, baclofen, has significant effects on eating behavior…”
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Evidence that the metabotropic glutamate receptor 5 antagonist MPEP may act as an inhibitor of the norepinephrine transporter in vitro and in vivo
Published in Synapse (New York, N.Y.) (15-12-2003)“…The mechanisms through which blockade of metabotropic glutamate receptors 5 (mGluR5) results in anxiolytic and antidepressant effects are currently unknown. In…”
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Synthesis and pharmacological characterization of constrained analogues of Vestipitant as in vitro potent and orally active NK sub(1) receptor antagonists
Published in Bioorganic & medicinal chemistry letters (15-01-2010)“…A focused exploration targeting conformationally restricted analogues of Vestipitant, resulted in the discovery of novel, in vitro potent NK sub(1)…”
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Synthesis and pharmacological characterization of constrained analogues of Vestipitant as in vitro potent and orally active NK 1 receptor antagonists
Published in Bioorganic & medicinal chemistry letters (2010)“…A focused exploration targeting conformationally restricted analogues of Vestipitant, resulted in the discovery of novel, in vitro potent NK 1 antagonists. In…”
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Synthesis and pharmacological characterization of constrained analogues of Vestipitant as in vitro potent and orally active NK(1) receptor antagonists
Published in Bioorganic & medicinal chemistry letters (15-01-2010)“…A focused exploration targeting conformationally restricted analogues of Vestipitant, resulted in the discovery of novel, in vitro potent NK(1) antagonists. In…”
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Backbone 1H, 13C and 15N resonance assignment of the N-terminal 24 kDa fragment of the gyrase B subunit from E. coli
Published in Journal of biomolecular NMR (01-04-2002)Get full text
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Ciprofloxacin affects conformational equilibria of DNA gyrase A in the presence of magnesium ions
Published in Journal of molecular biology (03-08-2001)“…The conformational equilibria of the A subunit of DNA gyrase (GyrA), of its 59 kDa N-terminal fragment (GyrA59) and of the quinolone-resistant Ser-Trp83 mutant…”
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