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SR59230A

SR59230A用途

SR59230A 是一种有效,选择性的,可透过血脑屏障的 β3-肾上腺素能受体 (β3-adrenergic receptor) 拮抗剂,对 β3,β1 和 β2 受体的 IC50 分别为 40、408 和 648 nM。

SR59230A名称

[ CAS 号 ]:
174689-39-5

[ 中文名 ]:
(S)-1-(2-乙基苯氧基)-3-(((S)-1,2,3,4-四氢萘-1-基)氨基)丙-2-醇草酸盐

[ 英文名 ]:
SR59230A

[英文别名 ]:

SR59230A生物活性

[ 描述 ]:

SR59230A 是一种有效,选择性的,可透过血脑屏障的 β3-肾上腺素能受体 (β3-adrenergic receptor) 拮抗剂,对 β3,β1 和 β2 受体的 IC50 分别为 40、408 和 648 nM。

[ 相关类别 ]:

研究领域 >> 心血管疾病

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 肾上腺素能受体

研究领域 >> 代谢疾病

[ 靶点 ]

IC50: 40 nM (β3 receptor), 408 nM ((β1 receptor), 648 nM (β2 receptor)[2]

[体外研究]

SR59230A(100n M-50μM；24小时)能够以剂量依赖的方式降低Neuro-2A、BE(2)C和SK-N-BE(2)NB细胞系的细胞活力[3]。细胞活力测定[3]细胞系：三种不同的神经母细胞瘤细胞系,一种小鼠(Neuro-2A)和两种人(SK-N-BE(2),BE(2)C)浓度：100n M、1μM、5μM、10μM和50μM培养时间：24小时结果：细胞活力呈剂量依赖性降低,在浓度限值超过1μM时对神经2A细胞和5μM时对SK-N-BE(2)和BE(2)C有显著影响。

[体内研究]

MDMA(20 mg/kg)产生缓慢发展的热疗,在注射后130分钟达到1.8°C的最大增幅。SR59230A(0.5mg/kg)能使缓慢发展的热疗对MDMA产生较小但显著的衰减。SR59230A(5 mg/kg)显示出对MDMA的显著和显著的早期低温反应[4]。动物模型：雄性C-57BL6J野生型小鼠(22-35g)[4]剂量：0.5或5mg/kg给药：注射s.C.；注射s.C.前30min给药(20mg/kg)。结果：MDMA对温度的调节作用涉及α1肾上腺素受体拮抗作用。

[参考文献]

[1]. Nisoli E, et al. Functional studies of the first selective beta 3-adrenergic receptor antagonist SR 59230A in rat brown adipocytes.Mol Pharmacol. 1996 Jan;49(1):7-14.

[2]. Kanzler SA, et al. Involvement of β3-adrenergic receptors in the control of food intake in rats.Braz J Med Biol Res. 2011 Nov;44(11):1141-7.

[3]. Bruno G, et al. β3-adrenoreceptor blockade reduces tumor growth and increases neuronal differentiation in neuroblastoma via SK2/S1P2 modulation.Oncogene. 2020 Jan;39(2):368-384.

[4]. Bexis S, et al. Role of alpha 1- and beta 3-adrenoceptors in the modulation by SR59230A of the effects of MDMA on body temperature in the mouse. Br J Pharmacol. 2009 Sep;158(1):259-66.

SR59230A物理化学性质

[ 沸点 ]:
542.6ºC at 760mmHg

[ 分子式 ]:
C₂₃H₂₉NO₆

[ 分子量 ]:
415.47900

[ 闪点 ]:
281.9ºC

[ 精确质量 ]:
415.19900

[ PSA ]:
116.09000

[ LogP ]:
3.20240

[ 蒸汽压 ]:
1.27E-11mmHg at 25°C

[ 储存条件 ]:
室温

SR59230AMSDS

详细MSDS(安全技术说明书)

SR59230A安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 风险声明 (欧洲) ]:
22-24/25

[ 危险品运输编码 ]:
NONH for all modes of transport

SR59230A文献

Functional evidence of atypical beta 3-adrenoceptors in the human colon using the beta 3-selective adrenoceptor antagonist, SR 59230A.

Br. J. Pharmacol. 117(7) , 1374-6, (1996)

The role of beta 3-adrenoceptors in human colonic circular smooth muscle was assessed in vitro by use of the beta 3-selective antagonist SR 59230A. Isoprenaline, in the presence of the selective beta-...

ALpha1-adrenoceptor antagonist properties of CGP 12177A and other beta-adrenoceptor ligands: evidence against beta(3)- or atypical beta-adrenoceptors in rat aorta.

Br. J. Pharmacol. 142 , 781-787, (2004)

1. The alpha(1)-adrenoceptor antagonist properties of the beta-adrenoceptor nonconventional partial agonist, CGP 12177A, was investigated in functional assays in rat aorta and in radioligand binding a...

Costunolide and Dehydrocostuslactone, two natural sesquiterpene lactones, ameliorate the inflammatory process associated to experimental pleurisy in mice.

Eur. J. Pharmacol. 730 , 107-15, (2014)

The aim of this study was to investigate the effect of costunolide (CS) and dehydrocostuslactone (DCE) a well-known sesquiterpene lactones contained in many plants, in a model of lung injury induced b...

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