지원사업
학술연구/단체지원/교육 등 연구자 활동을 지속하도록 DBpia가 지원하고 있어요.
커뮤니티
연구자들이 자신의 연구와 전문성을 널리 알리고, 새로운 협력의 기회를 만들 수 있는 네트워킹 공간이에요.
초록· 키워드
오류제보하기
KR-67500, trans-4-(2-(4-methyl-1,1-dioxido-6-(2,4,6-trichlorophenyl)-1,2,6-thiadiazinan-2-yl)acetamido)adamantane-1-carboxamide, is a novel $11{\beta}$-HSD1 inhibitor with its therapeutic effects of its anti-diabetic, anti-adipogenic and anti-osteoporotic activity. This study was performed to evaluate in vitro and in vivo pharmacokinetic properties of KR-67500 as a new drug candidate. KR-67500 was stable and highly bound to proteins in rat plasma. The microsomal stabilities of KR-67500 in human and rat liver were high. The inhibitory effect of KR-67500 for five cytochrome P450 enzymes was low. Preclinical pharmacokinetic studies have been carried out with intravenous or oral administrations of KR-67500 (10 mg/kg) to male rats and monkey. KR-67500 showed low clearance (0.68 l/h/kg) and high oral bioavailability (102%) in male rats. These results suggest that KR-67500 has good drug-like pharmacokinetic properties with a low first-pass effect and high bioavailability for an oral therapeutic agent of diabetes and osteoporosis.
목차
등록된 정보가 없습니다.
참고문헌 (13)
참고문헌 신청
Morton, N. M / 2010 / Obesity and corticosteroids: 11betahydroxysteroid type 1 as a cause and therapeutic target in metabolic disease / Mol. Cell Endocrinol 316:154
Walker, B. R / 2006 / Tissue production of cortisol by 11beta-hydroxysteroid dehydrogenase type 1 and metabolic disease / Ann. N. Y. Acad. Sci 1083:165
Wamil, M / 2007 / Inhibition of 11beta-hydroxysteroid dehydrogenase type 1 as a promising therapeutic target / Drug Discov. Today 12:504
Hollis, G / 2011 / 11β-Hydroxysteroid dehydrogenase type 1 inhibition in type 2 diabetes mellitus / Diabetes Obes. Metab 13:1
Harno, E / 2013 / 11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitors still improve metabolic phenotype in male 11β-HSD1 knockout mice suggesting off-target mechanisms / Endocrinology 154:4580
Walker, B. R / 2006 / Tissue production of cortisol by 11beta-hydroxysteroid dehydrogenase type 1 and metabolic disease / Ann. N. Y. Acad. Sci 1083:165
Wamil, M / 2007 / Inhibition of 11beta-hydroxysteroid dehydrogenase type 1 as a promising therapeutic target / Drug Discov. Today 12:504
Hollis, G / 2011 / 11β-Hydroxysteroid dehydrogenase type 1 inhibition in type 2 diabetes mellitus / Diabetes Obes. Metab 13:1
Harno, E / 2013 / 11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitors still improve metabolic phenotype in male 11β-HSD1 knockout mice suggesting off-target mechanisms / Endocrinology 154:4580
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