同义名 :	甲吡酮 ;Su-4885; NSC 25265; Metyrapone, Metopirone, SU 4885, Methbipyranone, Methopyrapone
	CAS号 :	54-36-4
	货号 :	A341725
	分子式 :	C14H14N2O
	纯度 :	95%
	分子量 :	226.27
	MDL号 :	MFCD00006397
	存储条件：	Pure form Inert atmosphere, room temperature In solvent -20°C:3-6个月-80°C:12个月
	溶解度 :	-
	动物实验配方：

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].

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	-	-

实验方案
	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

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