Search Results - "Stribling, D. Sloan"
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Ghrelin Neutralization by a Ribonucleic Acid-SPM Ameliorates Obesity in Diet-Induced Obese Mice
Published in Endocrinology (Philadelphia) (01-03-2006)“…Ghrelin, an acylated peptide secreted from the stomach, acts as a short-term signal of nutrient depletion. Ghrelin is an endogenous ligand for the GH…”
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Chronic MCH-1 receptor modulation alters appetite, body weight and adiposity in rats
Published in European journal of pharmacology (15-08-2003)“…Central administration of the neuropeptide melanin-concentrating hormone (MCH) stimulates feeding in rodents. We studied the effects of intracerebroventricular…”
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Furo[2,3- b]pyridine-based cannabinoid-1 receptor inverse agonists: Synthesis and biological evaluation. Part 1
Published in Bioorganic & medicinal chemistry letters (15-02-2010)“…The synthesis, SAR and binding affinities of cannabinoid-1 receptor (CB1R) inverse agonists based on furo[2,3- b]pyridine scaffolds are described. Food intake,…”
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Pyridopyrimidine based cannabinoid-1 receptor inverse agonists: Synthesis and biological evaluation
Published in Bioorganic & medicinal chemistry letters (01-05-2009)“…The synthesis, SAR and binding affinities are described for cannabinoid-1 receptor (CB1R) specific inverse agonists based on pyridopyrimidine and…”
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The triple uptake inhibitor (1R,5S)-(+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0] hexane hydrochloride (DOV 21947) reduces body weight and plasma triglycerides in rodent models of diet-induced obesity
Published in The Journal of pharmacology and experimental therapeutics (01-03-2008)“…Selective inhibitors of biogenic amine (e.g., serotonin, norepinephrine, and dopamine) uptake exhibit varying degrees of safety and efficacy as antiobesity…”
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Synthesis and SAR of 5,6-diarylpyridines as human CB1 inverse agonists
Published in Bioorganic & medicinal chemistry letters (01-02-2005)“…The synthesis and structure–activity relationships for four series of pyridine-based human CB1 inverse agonists are described. Structure–activity relationship…”
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Characterization of a novel and selective cannabinoid CB1 receptor inverse agonist, Imidazole 24b, in rodents
Published in European journal of pharmacology (28-01-2008)“…We document in vitro and in vivo effects of a novel, selective cannabinoid CB(1) receptor inverse agonist, Imidazole 24b…”
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Substituted acyclic sulfonamides as human cannabinoid-1 receptor inverse agonists
Published in Bioorganic & medicinal chemistry letters (15-04-2007)“…Sulfonamide analogues of the potent CB1R inverse agonist 2 (Taranabant) were optimized for CB1R activity. Sulfonamide analogues of the potent CB1R inverse…”
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Protein kinase C beta II specifically binds to and is activated by F-actin
Published in The Journal of biological chemistry (28-06-1996)“…The two most closely related isoenzymes of protein kinase C (PKC), PKC betaI and betaII, are distinct but highly homologous isoenzymes derived via alternative…”
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Lead optimization of 5,6-diarylpyridines as CB1 receptor inverse agonists
Published in Bioorganic & medicinal chemistry letters (01-04-2007)“…The synthesis and biological optimization for 5,6-diarylpyridines as CB1 receptor inverse agonists is described. Optimization of the biological activity for…”
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Discovery of N-[(4R)-6-(4-Chlorophenyl)-7-(2,4-dichlorophenyl)-2,2-dimethyl-3,4-dihydro-2H-pyrano[2,3-b]pyridin-4-yl]-5-methyl-1H-pyrazole-3-carboxamide (MK-5596) as a Novel Cannabinoid-1 Receptor (CB1R) Inverse Agonist for the Treatment of Obesity
Published in Journal of medicinal chemistry (27-05-2010)“…This paper describes the discovery of…”
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Dihydro-pyrano[2,3-b]pyridines and tetrahydro-1,8-naphthyridines as CB1 receptor inverse agonists: Synthesis, SAR and biological evaluation
Published in Bioorganic & medicinal chemistry letters (15-06-2010)“…Synthesis and structure–activity relationships of cannabinoid-1 receptor (CB1R) inverse agonists based on dihydro-pyrano[2,3-b] pyridine and…”
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Discovery of N-[(1S,2S)-3-(4-Chlorophenyl)-2- (3-cyanophenyl)-1-methylpropyl]-2-methyl-2- {[5-(trifluoromethyl)pyridin-2-yl]oxy}propanamide (MK-0364), a Novel, Acyclic Cannabinoid-1 Receptor Inverse Agonist for the Treatment of Obesity
Published in Journal of medicinal chemistry (28-12-2006)“…The discovery of novel acyclic amide cannabinoid-1 receptor inverse agonists is described. They are potent, selective, orally bioavailable, and active in…”
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Synthesis and activity of 4,5-diarylimidazoles as human CB1 receptor inverse agonists
Published in Bioorganic & medicinal chemistry letters (01-03-2005)“…The synthesis and structure–activity relationships for a series of substituted 4,5-diphenylimidazole-2-carboxamide derivatives 2b as selective, orally active…”
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Regulation of Receptor-mediated Protein Kinase C Membrane Trafficking by Autophosphorylation
Published in The Journal of biological chemistry (02-06-2000)“…Signal transduction via protein kinase C (PKC) is closely regulated by its subcellular localization. In response to activation of cell-surface receptors, PKC…”
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Synthesis of functionalized 1,8-naphthyridinones and their evaluation as novel, orally active CB1 receptor inverse agonists
Published in Bioorganic & medicinal chemistry letters (01-02-2006)“…The synthesis, structure–activity relationship, and biological evaluation of a new class of 1,8-naphthyridinone CB1 receptor specific inverse agonists are…”
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Discovery of N -[(4 R )-6-(4-Chlorophenyl)-7-(2,4-dichlorophenyl)-2,2-dimethyl-3,4-dihydro-2 H -pyrano[2,3- b ]pyridin-4-yl]-5-methyl-1 H -pyrazole-3-carboxamide (MK-5596) as a Novel Cannabinoid-1 Receptor (CB1R) Inverse Agonist for the Treatment of Obesity
Published in Journal of medicinal chemistry (27-05-2010)Get full text
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Characterization of a novel and selective cannabinoid CB 1 receptor inverse agonist, Imidazole 24b, in rodents
Published in European journal of pharmacology (2008)“…We document in vitro and in vivo effects of a novel, selective cannabinoid CB 1 receptor inverse agonist, Imidazole 24b (5-(4-chlorophenyl)-…”
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Antiobesity efficacy of a novel cannabinoid-1 receptor inverse agonist, N-[(1S,2S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2-[[5-(trifluoromethyl)pyridin-2-yl]oxy]propanamide (MK-0364), in rodents
Published in The Journal of pharmacology and experimental therapeutics (01-06-2007)“…The cannabinoid-1 receptor (CB1R) has been implicated in the control of energy balance. To explore the pharmacological utility of CB1R inhibition for the…”
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