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Volumn 20, Issue 11, 2010, Pages 3265-3271

Modulation of 11β-hydroxysteroid dehydrogenase type 1 activity by 1,5-substituted 1H-tetrazoles

Author keywords

11 HSD1; 11 Hydroxysteroid dehydrogenase type 1; Drug discovery; Metabolic syndrome

Indexed keywords

11BETA HYDROXYSTEROID DEHYDROGENASE 1; 11BETA HYDROXYSTEROID DEHYDROGENASE 2; BVT 116429; PF 915275; UNCLASSIFIED DRUG; ENZYME INHIBITOR; TETRAZOLE DERIVATIVE;

EID: 77953284860     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.04.055     Document Type: Article
Times cited : (26)

References (26)
  • 21
    • 77953285506 scopus 로고    scopus 로고
    • note
    • 50) determined by plotting fractional inhibition against log compound concentration. Data were fitted to the four parameter logistic equation. Murine 11β-HSD1 enzyme inhibition was assessed in CHO cells stably transfected with the full length murine hsd11b1 gene. Enzyme inhibition was determined as described for human 11β-HSD1 following a 4-h incubation of cells, compound and substrate.
  • 24
    • 77953284834 scopus 로고    scopus 로고
    • note
    • Male C57BL/6 mice (25-30 g in weight) were group housed and allowed free access to food and water. Compounds was dissolved in 5% DMSO, 3% ethanol, 4 mM cyclodextrin. Animals (n = 3 per group) were dosed intraperitoneally or orally with vehicle or compound at 12-hourly intervals. At 2 h following the third dose mice were killed by cervical dislocation. Liver, adipose and brain samples were removed and frozen until analysis was performed. Inhibition of 11β-HSD1 in each tissue was determined by incubating homogenates with 20 nM tritiated cortisone, 2 mM NADPH and 0.2% glucose in Krebs buffer, pH 7.4. Cortisone and cortisol levels were measured by HPLC and the percentage inhibition determined relative to vehicle treated tissue.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.