Orally administered H-Dmt-Tic-Lys-NH-CH2-Ph (MZ-2), a potent mu/delta-opioid receptor antagonist, regulates obese-related factors in mice.
Orally administered H-Dmt-Tic-Lys-NH-CH2-Ph (MZ-2), a potent mu/delta-opioid receptor antagonist, regulates obese-related factors in mice.
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DOI:
10.1016/j.ejphar.2009.06.041
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发表时间:
2009-08-15
影响因子:
5
通讯作者:
Lazarus, Lawrence H.
中科院分区:
文献类型:
--
作者:
Marczak, Ewa D.;Jinsmaa, Yunden;Myers, Page H.;Blankenship, Terry;Wilson, Ralph;Balboni, Gianfranco;Salvadori, Severo;Lazarus, Lawrence H.
关键词:
Orally active dual μ-/δ-opioid receptor antagonist, H-Dmt-Tic-Lys-NH-CH2-Ph (MZ-2) was applied to study body weight gain, fat content, bone mineral density, serum insulin, cholesterol and glucose levels in female ob/ob (B6.V-Lep<ob>/J homozygous) and lean wild mice with or without voluntary exercise on wheels for three weeks, and during a two week post-treatment period under the same conditions. MZ-2 (10 mg/kg/day, p.o.) exhibited the following actions: (1) reduced body weight gain in sedentary obese mice that persisted beyond the treatment period without effect on lean mice; (2) stimulated voluntary running on exercise wheels of both groups of mice; (3) decreased fat content, enhanced bone mineral density (BMD), and decreased serum insulin and glucose levels in obese mice; and (4) MZ-2 (30 μM) increased BMD in human osteoblast cells (MG-63) comparable to naltrexone, while morphine inhibited mineral nodule formation. Thus, MZ-2 has potential application in the clinical management of obesity, insulin and glucose levels, and the amelioration of osteoporosis.
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影响因子:
3.4
作者:
Kas, MJH;van den Bos, R;Spruijt, BM
通讯作者:
Spruijt, BM
影响因子:
3.3
作者:
Hagihara, Y;Fukuda, S;Moriya, H
通讯作者:
Moriya, H
影响因子:
2.5
作者:
Jarosz, Patricia A;Metzger, Bonnie L
通讯作者:
Metzger, Bonnie L
影响因子:
6.1
作者:
KHAWAJA, XZ;BAILEY, CJ;GREEN, IC
通讯作者:
GREEN, IC
影响因子:
--
作者:
Gellner, R.;Domschke, W.
通讯作者:
Domschke, W.