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Volumn 22, Issue 8, 2012, Pages 2943-2947

Discovery of new piperidine amide triazolobenzodiazepinones as intestinal-selective CCK1 receptor agonists

Author keywords

CCK1R; Cholecystokinin 1 receptor; Obesity; Triazolobenzodiazepinone

Indexed keywords

AMIDE; BENZODIAZEPINE DERIVATIVE; CHOLECYSTOKININ 1 RECEPTOR AGONIST; CHOLECYSTOKININ A RECEPTOR; CHOLECYSTOKININ RECEPTOR STIMULATING AGENT; PIPERIDINE DERIVATIVE; TRIAZOLE DERIVATIVE; UNCLASSIFIED DRUG;

EID: 84862806707     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2012.02.049     Document Type: Article
Times cited : (10)

References (32)
  • 20
    • 84862786716 scopus 로고    scopus 로고
    • 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
    • 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.
  • 29
    • 84862783816 scopus 로고    scopus 로고
    • All procedures were reviewed and approved by the Institutional Animal Care & Use Committee
    • All procedures were reviewed and approved by the Institutional Animal Care & Use Committee.
  • 30
    • 84862812126 scopus 로고    scopus 로고
    • 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
    • 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.
  • 31
    • 84862812128 scopus 로고    scopus 로고
    • 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
    • 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.
  • 32
    • 84862783817 scopus 로고    scopus 로고
    • 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
    • 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.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.