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硫丙咪胺马来酸

硫丙咪胺马来酸用途

马来酸硫哌酰胺(MR-12842马来酸)是一种有效的口服脑渗透剂和选择性H3受体拮抗剂,Ki为4.3 nM,用于抑制[3H]组胺释放。马来酸硫哌酰胺抑制[3H]组胺合成,Ki为31 nM[1]。

硫丙咪胺马来酸名称

[ CAS 号 ]:
148440-81-7

[ 中文名 ]:
硫丙咪胺马来酸

[ 英文名 ]:
Thioperamide (maleate)

[英文别名 ]:

Thioperamide Maleate
MFCD00083209

硫丙咪胺马来酸生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 免疫及炎症 >> 组胺受体

研究领域 >> 神经疾病

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 组胺受体

[ 靶点 ]

H3 Receptor

[体外研究]

硫哌酰胺分别以2.1nm和2.0nm的Kis抑制[3H]-(R)α-MeHA结合的大鼠脑和豚鼠肺。硫哌酰胺以4 nM的平均表观Ki竞争性阻断调节[3H]组胺释放的H3自身受体[1]。硫哌酰胺(0.01-100μM；24小时)以浓度依赖性方式促进NE-4C干细胞的活力[2]。硫哌酰胺在人类H4和H3受体上显示出相似的效力(Ki分别为43和60 nM)[3]。细胞活力测定[2]细胞系：NE-4C干细胞浓度：0.01,0.1,1,10,100μM孵育时间：24小时结果：NE-4C干细胞活力在(1μM)给药后显著提高至150.83±6.91%,在10μM和100μM给药后分别提高至145.11±14.52%和132.02±25.65%。

[体内研究]

硫哌酰胺(5-20mg/kg；i、 p.)能够促进C57BL/6J小鼠情境条件恐惧记忆的再巩固[4]。动物模型：天真雌性C57BL/6J小鼠[4]剂量：5、10或20 mg/kg给药：注射(i.p.)结果：促进情境条件恐惧记忆的再巩固。

[参考文献]

[1]. J M Arrang, et al. Highly Potent and Selective Ligands for Histamine H3-receptors. Nature. 1987 May 14-20;327(6118):117-23.

[2]. Na Wang, et al. Histamine H3 Receptor Antagonist Enhances Neurogenesis and Improves Chronic Cerebral Hypoperfusion-Induced Cognitive Impairments. Front Pharmacol. 2020 Jan 21;10:1583.

[3]. Y Charlier, et al. Differential Effects of Histamine H(3) Receptor Inverse Agonist Thioperamide, Given Alone or in Combination With the N-methyl-d-aspartate Receptor Antagonist Dizocilpine, on Reconsolidation and Consolidation of a Contextual Fear Memory in Mice. Neuroscience. 2011 Oct 13;193:132-42.

[4]. Gbahou F, et al. Compared pharmacology of human histamine H3 and H4 receptors: structure-activity relationships of histamine derivatives. Br J Pharmacol. 2006;147(7):744-754.

硫丙咪胺马来酸物理化学性质

[ 分子式 ]:
C₁₉H₂₈N₄O₄S

[ 分子量 ]:
408.515

[ 精确质量 ]:
408.183136

[ PSA ]:
150.64000

[ LogP ]:
2.83690

[ 外观性状 ]:
白色固体

[ 储存条件 ]:
室温

硫丙咪胺马来酸MSDS

详细MSDS(安全技术说明书)

硫丙咪胺马来酸安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H315-H319-H335

[ 警示性声明 ]:
P261-P305 + P351 + P338

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危害码 (欧洲) ]:
Xi

[ 风险声明 (欧洲) ]:
R36/37/38

[ 安全声明 (欧洲) ]:
S26

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

硫丙咪胺马来酸文献

Highly potent and selective ligands for histamine H3-receptors.

Nature 327 , 117, (1987)

New drugs selective for histamine H3-receptors can be used to establish that these receptors are involved in the feedback control of histamine synthesis and release, and to demonstrate their distribut...

Effects of the histamine H3-agonist (R)-alpha-methylhistamine and the antagonist thioperamide on histamine metabolism in the mouse and rat brain.

J. Neurochem. 52 , 1388, (1989)

To study the feedback control by histamine (HA) H3-receptors on the synthesis and release of HA at nerve endings in the brain, the effects of a potent and selective H3-agonist, (R)-alpha-methylhistami...

Effect of thioperamide, a histamine H3 receptor antagonist, on electrically induced convulsions in mice.

Eur. J. Pharmacol. 234(1) , 129-33, (1993)

The effect of thioperamide, a histamine H3 receptor antagonist, on electrically induced convulsions was studied in mice. Thioperamide significantly and dose dependently decreased the duration of each ...

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