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Compounds 4a and 10e were formulated as a 25 wt % drug:75 wt % hydroxypropyl methylcellulose acetate succinate-high granular (HPMCAS-HG) SDD in 0.5% methylcellulose
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Compounds 4a and 10e were formulated as a 25 wt % drug:75 wt % hydroxypropyl methylcellulose acetate succinate-high granular (HPMCAS-HG) SDD in 0.5% methylcellulose.
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James, M.K.13
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0023146419
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29
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84862783816
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All procedures were reviewed and approved by the Institutional Animal Care & Use Committee
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All procedures were reviewed and approved by the Institutional Animal Care & Use Committee.
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30
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84862812126
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Stereochemistry of 10e was determined by single crystal X-ray analysis. The crystal structure has been deposited at the Cambridge Crystallographic Data Centre and was allocated the following deposition number: CCDC 855714
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Stereochemistry of 10e was determined by single crystal X-ray analysis. The crystal structure has been deposited at the Cambridge Crystallographic Data Centre and was allocated the following deposition number: CCDC 855714.
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31
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84862812128
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Anorectic activity of 10e in mice was assessed utilizing an overnight fasting-re-feeding paradigm. After an overnight fast, mice were orally given increasing doses of 10e in a SDD formulation and food intake was measured. At the 2-h time point, 0.2 mg/kg was determined to be the minimally efficacious dose, significantly inhibiting food intake by 34% (p <0.05) as compared to vehicle-treated mice. This dose was therefore used to assess gallbladder refilling
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Anorectic activity of 10e in mice was assessed utilizing an overnight fasting-re-feeding paradigm. After an overnight fast, mice were orally given increasing doses of 10e in a SDD formulation and food intake was measured. At the 2-h time point, 0.2 mg/kg was determined to be the minimally efficacious dose, significantly inhibiting food intake by 34% (p <0.05) as compared to vehicle-treated mice. This dose was therefore used to assess gallbladder refilling.
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32
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84862783817
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Significant decreases in food intake relative to vehicle of 19% and 25% were observed at 2 and 6 mg/kg, respectively. No gastrointestinal side-effects were observed
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Significant decreases in food intake relative to vehicle of 19% and 25% were observed at 2 and 6 mg/kg, respectively. No gastrointestinal side-effects were observed.
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