产品说明书

	同义名 :	SA4503;AGY 94806;UNII-9J7A4144BX
	CAS号 :	165377-43-5
	货号 :	A606126
	分子式 :	C23H32N2O2
	纯度 :	98%+
	分子量 :	368.512
	MDL号 :	MFCD09842336
	存储条件：	粉末 Sealed in dry,2-8°C 液体 -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

SA4503 is a potent and selective agonist for the sigma 1 receptor subtype in the brain. SA4503 showed a high affinity for the sigma 1 receptor subtype labeled by (+)-[3H]pentazocine (IC50 = 17.4 +/- 1.9 nM), while it had about 100-fold less affinity for the sigma 2 receptor subtype labeled by [3H]1,3-di(2-tolyl)guanidine ([3H]DTG) in the presence of 200 nM (+)-pentazocine. SA4503 showed little affinity for 36 other receptors, ion channels and second messenger systems[3]. Treatment with SA4503 (0.1-1 μM) dose-dependently inhibited hypertrophy in cultured cardiomyocytes induced by angiotensin II (Ang II). Chronic SA4503 administration also significantly attenuates myocardial hypertrophy and restores ATP production in transverse aortic constriction mice[4]. SA4503 administration rescued PO (pressure overload)-induced σ1R decreases in aortic smooth muscle and endothelial cells. SA4503 treatment also rescued PO-induced impairments in ACh- and clonidine-induced vasodilation without affecting PE- and ET-1-induced vasoconstriction[5]. The administration of SA4503 significantly alters the activity of spontaneously active midbrain DA (dopamine) neurons, particularly those in the VTA (ventral tegmental area) following repeated administration[6].

实验方案
	1mg	5mg	10mg
1 mM 5 mM 10 mM	2.71mL 0.54mL 0.27mL	13.57mL 2.71mL 1.36mL	27.14mL 5.43mL 2.71mL

参考文献

[1]Minabe Y, Matsuno K, et al. Acute and chronic administration of the selective sigma1 receptor agonist SA4503 significantly alters the activity of midbrain dopamine neurons in rats: An in vivo electrophysiological study. Synapse. 1999 Aug;33(2):129-40. [2]Matsuno K, Nakazawa M, et al. Binding properties of SA4503, a novel and selective sigma 1 receptor agonist. Eur J Pharmacol. 1996 Jun 13;306(1-3):271-9. [3]Matsuno K, Nakazawa M, Okamoto K, Kawashima Y, Mita S. Binding properties of SA4503, a novel and selective sigma 1 receptor agonist. Eur J Pharmacol. 1996 Jun 13;306(1-3):271-9 [4]Hirano K, Tagashira H, Fukunaga K. [Cardioprotective effect of the selective sigma-1 receptor agonist, SA4503]. Yakugaku Zasshi. 2014;134(6):707-13. Japanese [5]Tagashira H, Matsumoto T, Taguchi K, Zhang C, Han F, Ishida K, Nemoto S, Kobayashi T, Fukunaga K. Vascular endothelial σ1-receptor stimulation with SA4503 rescues aortic relaxation via Akt/eNOS signaling in ovariectomized rats with aortic banding. Circ J. 2013;77(11):2831-40 [6]Minabe Y, Matsuno K, Ashby CR Jr. Acute and chronic administration of the selective sigma1 receptor agonist SA4503 significantly alters the activity of midbrain dopamine neurons in rats: An in vivo electrophysiological study. Synapse. 1999 Aug;33(2):129-40