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替勃龙

替勃龙用途

替勃龙是一种广谱性腺类固醇激动剂,具有孕激素、雄激素和雌激素活性。替勃龙可用于绝经后骨质疏松症研究[1][2]。

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替勃龙名称

[ CAS 号 ]:
5630-53-5

[ 中文名 ]:
替勃龙

[ 英文名 ]:
Tibolone(Liviella)(Livial)

[中文别名 ]:

[英文别名 ]:

EINECS 227-069-1
Tibolone
7a-Methyl-5,10-norethindrone
LIVIELLA
Org OD 14
7a-Methyl-D5,10-norethindrone
Livial
MFCD00864178

替勃龙生物活性

[ 描述 ]:

替勃龙是一种广谱性腺类固醇激动剂,具有孕激素、雄激素和雌激素活性。替勃龙可用于绝经后骨质疏松症研究[1][2]。

[ 相关类别 ]:

信号通路 >> 其他 >> 雌激素受体/ERR

信号通路 >> 其他 >> 孕激素受体

研究领域 >> 内分泌

信号通路 >> 其他 >> 雄激素受体

[体内研究]

替勃龙(1毫克/天；口服给药；治疗12周)可增强去卵巢大鼠髓内钛植入物的骨整合过程[1]。动物模型：切除卵巢的雌性白化Wistar大鼠[1]剂量：1mg/天给药：口服；每日的12周后的结果：显示整体骨组织显著增加,体重密度显著增加。

[参考文献]

[1]. Dragos Apostu, et al. Tibolone, alendronate, and simvastatin enhance implant osseointegration in a preclinical in vivo model. Clin Oral Implants Res. 2020 Jul;31(7):655-668.

[2]. Marcos García-Juárez, et al. Tibolone induces lordosis behavior, but not concurrent or sequential inhibition, in Sprague Dawley rats. Neurosci Lett. 2021 Apr 24;755:135916.

替勃龙物理化学性质

[ 密度 ]:
1.1±0.1 g/cm3

[ 沸点 ]:
447.4±45.0 °C at 760 mmHg

[ 熔点 ]:
169 °C

[ 分子式 ]:
C₂₁H₂₈O₂

[ 分子量 ]:
312.446

[ 闪点 ]:
190.6±21.3 °C

[ 精确质量 ]:
312.208923

[ PSA ]:
37.30000

[ LogP ]:
4.03

[ 外观性状 ]:
白色至灰白色结晶粉末

[ 蒸汽压 ]:
0.0±2.5 mmHg at 25°C

[ 折射率 ]:
1.570

[ 储存条件 ]:
2-8°C

替勃龙MSDS

详细MSDS(安全技术说明书)

替勃龙安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H319

[ 警示性声明 ]:
P305 + P351 + P338

[ 危害码 (欧洲) ]:
N

[ 风险声明 (欧洲) ]:
R51/53

[ 安全声明 (欧洲) ]:
S22-S24/25-S61

[ 危险品运输编码 ]:
UN 3077 9/PG 3

[ RTECS号 ]:
RC8964020

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替勃龙制备

以7α-甲基-10-甲醛基孕甾-4-烯-3,17-二酮为原料制得。

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替勃龙文献

Tibolone prevents oxidation and ameliorates cholinergic deficit induced by ozone exposure in the male rat hippocampus.

Neurochem. Res. 39(9) , 1776-86, (2014)

Oxidative stress is related to the development of central nervous system diseases involving memory processes. Cholinergic system and memory processes are disrupted by ozone exposure. In rats, ozone in...

Effects of tibolone or continuous combined oestradiol/norethisterone acetate on glucose and insulin metabolism.

Clin. Endocrinol. (Oxf.) 78(2) , 297-302, (2013)

To determine the effects of tibolone or oestradiol (E(2) )/norethisterone acetate (NETA) hormone replacement therapy on glucose and insulin metabolism in postmenopausal women.Single-centre double-blin...

Effects of a continuous-combined regimen of low-dose hormone therapy (oestradiol and norethindrone acetate) and tibolone on the quality of life in symptomatic postmenopausal women: a double-blind, randomised study.

Maturitas 74(2) , 172-8, (2013)

This study compared the effects of a continuous-combined regimen of low-dose hormone therapy (LD-HT) versus tibolone and supplemental calcium/vitamin D3 (control) on quality of life (QoL) in symptomat...

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替勃龙