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首页 / 抑制剂/激动剂 / 代谢酶 / P450 / Metyrapone/美替拉酮

Metyrapone/美替拉酮 {[allProObj[0].p_purity_real_show]}

货号：A341725 同义名： 甲吡酮 / Su-4885; NSC 25265

Metyrapone is an inhibitor of cytochrome P450-mediated ω/ω-1 hydroxylase activity and CYP11B1.

Metyrapone/美替拉酮 化学结构 CAS号：54-36-4
Metyrapone/美替拉酮 化学结构
CAS号：54-36-4
Metyrapone/美替拉酮 3D分子结构
CAS号：54-36-4
Metyrapone/美替拉酮 化学结构 CAS号：54-36-4
Metyrapone/美替拉酮 3D分子结构 CAS号：54-36-4
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Metyrapone/美替拉酮 纯度/质量文件 产品仅供科研

货号：A341725 标准纯度： {[allProObj[0].p_purity_real_show]}
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Metyrapone/美替拉酮 生物活性

描述 Metyrapone is an inhibitor of cytochrome P450-mediated ω/ω-1 hydroxylase activity and CYP11B1. Administration of metyrapone to male rats induces the expression of the cytochrome P450 sub-family 3A (CYP3A)[3]. Metyrapone protects against ischemia- and excitotoxicity-induced brain damages in rodents[4]. Metyrapone is a glucocorticoid synthesis inhibitor largely used to study glucocorticoid involvement in stress and memory processes. Mice received first a saline injection and 2days later a 150mg/kg metyrapone injection. Metyrapone provoked immediately a waking effect together with a 3-h decrease in slow-wave sleep (SWS) and a 5-h decrease in rapid eye movement sleep (REM sleep)[5]. A significant rise in ACTH (adrenocorticotropin) concentration compared to basal values was found at 60 and 120 min following oral metyrapone administration[6]. Metyrapone was well tolerated and did not exacerbate cocaine's physiological effects[7]. Metyrapone (150 mg/kg) acutely reduced stress-induced physiological response in freely behaving rats independently from glucocorticoids and neurosteroids[8].

Metyrapone/美替拉酮 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00004334 - Unknown - United States, Michigan ... 展开 >> University of Michigan Health Systems Recruiting Ann Arbor, Michigan, United States, 48109 Contact: Monica N. Starkman    313-764-6168 收起 <<
NCT00310427 Alcohol Dependence ... 展开 >> Alcoholism 收起 << Phase 2 Completed - United States, Maryland ... 展开 >> National Institutes of Health Clinical Center, 9000 Rockville Pike Bethesda, Maryland, United States, 20892 收起 <<
NCT00310427 - Completed - -

Metyrapone/美替拉酮 参考文献

[1]Park H, Lee S, et al. Structural and dynamical basis of broad substrate specificity, catalytic mechanism, and inhibition of cytochrome P450 3A4. J Am Chem Soc. 2005 Oct 5;127(39):13634-42.

[2]Hays SJ, Tobes MC, et al. Structure-activity relationship study of the inhibition of adrenal cortical 11 beta-hydroxylase by new metyrapone analogues. J Med Chem. 1984 Jan;27(1):15-9.

[3]Wright MC, Paine AJ, Skett P, Auld R. Induction of rat hepatic glucocorticoid-inducible cytochrome P450 3A by metyrapone. J Steroid Biochem Mol Biol. 1994 Feb;48(2-3):271-6

[4]Drouet JB, Fauvelle F, Batandier C, Peinnequin A, Alonso A, Fidier N, Maury R, Poulet L, Buguet A, Cespuglio R, Canini F. Metyrapone effects on systemic and cerebral energy metabolism. Eur J Pharmacol. 2012 May 5;682(1-3):92-8

[5]Drouet JB, Rousset C, Maury R, Michel V, Buguet A, Cespuglio R, Canini F. Single administration of metyrapone modifies sleep-wake patterns in the rat. Eur J Pharmacol. 2011 Feb 10;652(1-3):60-4

[6]Noe S, von Werder A, Iakoubov R, Schneider H, Thaler M, Luppa P, Neu B. Dynamics of Adrenocorticotropin after Application of Metyrapone. Exp Clin Endocrinol Diabetes. 2017 Jan;125(1):53-56

[7]Winhusen T, Somoza E, Harrer JM, Moore E, Ussery T, Kropp F, Singal B, Elkashef A, Mojsiak J. Metyrapone and cocaine: a double-blind, placebo-controlled drug interaction study. Pharmacol Biochem Behav. 2005 Apr;80(4):631-8

[8]Drouet JB, Michel V, Peinnequin A, Alonso A, Fidier N, Maury R, Buguet A, Cespuglio R, Canini F. Metyrapone blunts stress-induced hyperthermia and increased locomotor activity independently of glucocorticoids and neurosteroids. Psychoneuroendocrinology. 2010 Oct;35(9):1299-310

Metyrapone/美替拉酮 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

4.42mL

0.88mL

0.44mL

22.10mL

4.42mL

2.21mL

44.19mL

8.84mL

4.42mL

Metyrapone/美替拉酮 技术信息

CAS号54-36-4
分子式C14H14N2O
分子量 226.27
SMILES Code CC(C1=CC=CN=C1)(C)C(C2=CC=CN=C2)=O
MDL No. MFCD00006397
别名 甲吡酮 ;Su-4885; NSC 25265; Metyrapone, Metopirone, SU 4885, Methbipyranone, Methopyrapone
运输蓝冰
InChI Key FJLBFSROUSIWMA-UHFFFAOYSA-N
Pubchem ID 4174
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Inert atmosphere, room temperature

Tags: Metyrapone | Su-4885;NSC 25265;Metyrapone, Metopirone, SU 4885, Methbipyranone, Methopyrapone | 甲吡酮 | P450 | AmBeed-信号通路专用抑制剂 | Metyrapone/美替拉酮 纯度/质量文件 | Metyrapone/美替拉酮 生物活性 | Metyrapone/美替拉酮 临床数据 | Metyrapone/美替拉酮 参考文献 | Metyrapone/美替拉酮 实验方案 | Metyrapone/美替拉酮 技术信息

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