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孕激素对大鼠血脂及脂肪分解的影响:孕酮、醋酸甲地孕酮、醋酸炔诺酮及醋酸诺美孕酮的作用

Effects of progestogens on lipemia and lipolysis in rat: effects of progesterone, megestrol acetate, norethindrone acetate, and nomegestrol acetate.

作者信息

Hazard M C, Clavet M, Chapignac A, Paris J

机构信息

Laboratoires Theramex, Monaco.

出版信息

Fundam Clin Pharmacol. 1987;1(4):233-42. doi: 10.1111/j.1472-8206.1987.tb00562.x.

DOI:10.1111/j.1472-8206.1987.tb00562.x
PMID:3436613
Abstract

Effects of 4 progestogens at equal dosages (5 mg/kg/day) on lipid metabolism and plasma glucose levels of adult female rats were compared. The 4 progestogens studied were progesterone (P) by SC injection, and megestrol acetate (MEG), norethindrone acetate (NOR), and nomegestrol acetate (NOM) PO. MEG, a 17 alpha-hydroxyprogesterone derivative, induced significant increases in glucose, total and high-density lipid (HDL) cholesterol, triglyceride, and phospholipid plasma levels. Treatment with NOR, a 19-nortestosterone derivative, resulted in a reduced gain in body wt and in a marked decrease in all plasma lipid parameters. The 19-norprogesterone derivative NOM, like P, did not alter lipid or glucose metabolism, despite a significant increase in body wt gain. In particular, no reduction in the HDL cholesterol level occurred. Plasma and tissue lipolytic activities remained unchanged. The results of this study confirm interest in the therapeutic class of 19-norprogesterone-derived progestogens, exemplified by NOM, with respect to their lack of metabolic side effects.

摘要

比较了4种剂量相等(5毫克/千克/天)的孕激素对成年雌性大鼠脂质代谢和血糖水平的影响。所研究的4种孕激素分别是皮下注射的孕酮(P),以及口服的醋酸甲地孕酮(MEG)、醋酸炔诺酮(NOR)和醋酸诺美孕酮(NOM)。MEG是一种17α-羟孕酮衍生物,可使血糖、总胆固醇和高密度脂蛋白(HDL)胆固醇、甘油三酯及血浆磷脂水平显著升高。使用19-去甲睾酮衍生物NOR进行治疗,导致体重增加减少,所有血浆脂质参数显著降低。19-去甲孕酮衍生物NOM与P一样,尽管体重增加显著,但并未改变脂质或葡萄糖代谢。特别是,HDL胆固醇水平没有降低。血浆和组织的脂解活性保持不变。本研究结果证实了对以NOM为代表的19-去甲孕酮衍生孕激素治疗类别感兴趣,因为它们缺乏代谢副作用。

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1
Effects of progestogens on lipemia and lipolysis in rat: effects of progesterone, megestrol acetate, norethindrone acetate, and nomegestrol acetate.孕激素对大鼠血脂及脂肪分解的影响:孕酮、醋酸甲地孕酮、醋酸炔诺酮及醋酸诺美孕酮的作用
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引用本文的文献

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Preclinical pharmacological profile of nomegestrol acetate, a synthetic 19-nor-progesterone derivative.醋酸诺美孕酮的临床前药理学特性,一种合成的 19-去甲孕酮衍生物。
Reprod Biol Endocrinol. 2012 Oct 8;10:85. doi: 10.1186/1477-7827-10-85.