S-[2-(4(5)-咪唑基)乙基]异硫脲氢溴酸盐

S-[2-(4(5)-咪唑基)乙基]异硫脲氢溴酸盐用途

Imetit dihydrobromide (VUF 8325 dihydrobromide) 是组胺 H3 和 H4 受体的高亲和力的强激动剂,Ki 值分别为 0.3 和 2.7 nM。Imetit dihydrobromide 模拟组胺对嗜酸性粒细胞形状改变的作用 (EC50=25 nM)。

点击显示

S-[2-(4(5)-咪唑基)乙基]异硫脲氢溴酸盐名称

[ CAS 号 ]:
32385-58-3

[ 中文名 ]:
S-[2-(4(5)-咪唑基)乙基]异硫脲氢溴酸盐

[ 英文名 ]:
Imetit dihydrobromide

[中文别名 ]:

IMETIT 氢溴酸盐

[英文别名 ]:

Imetit dihydrobromide

S-[2-(4(5)-咪唑基)乙基]异硫脲氢溴酸盐生物活性

[ 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:0.3 nM (Ki)

H4 receptor:2.7 nM (Ki)

[体内研究]

二氢溴化乙胺(2.5-10 mg/kg；i.p.)降低阿扑吗啡诱导的舔体反应[4]。动物模型：雄性Sprague-Dawley大鼠[4]剂量：2.5、5、10mg/kg给药：腹腔注射(阿朴吗啡前30min)结果：阿朴吗啡诱导的舔体反应减弱。

[参考文献]

[1]. Liu C, et al. Cloning and pharmacological characterization of a fourth histamine receptor (H(4)) expressed in bone marrow. Mol Pharmacol. 2001 Mar;59(3):420-6.

[2]. Ling P, et al. Histamine H4 receptor mediates eosinophil chemotaxis with cell shape change and adhesion molecule upregulation. Br J Pharmacol. 2004 May;142(1):161-71.

[3]. Garbarg M, et al. S-[2-(4-imidazolyl)ethyl]isothiourea, a highly specific and potent histamine H3 receptor agonist. J Pharmacol Exp Ther. 1992 Oct;263(1):304-10.

[4]. Farzin D, et al. Influence of different histamine receptor agonists and antagonists on apomorphine-induced licking behavior in rat. Eur J Pharmacol. 2000 Sep 15;404(1-2):169-74.

S-[2-(4(5)-咪唑基)乙基]异硫脲氢溴酸盐物理化学性质

[ 沸点 ]:
430.8ºC at 760mmHg

[ 熔点 ]:
206 - 207 °C

[ 分子式 ]:
C₆H₁₂Br₂N₄S

[ 分子量 ]:
332.05900

[ 闪点 ]:
214.3ºC

[ 精确质量 ]:
329.91500

[ PSA ]:
103.85000

[ LogP ]:
3.29510

[ 外观性状 ]:
白色固体

[ 储存条件 ]:
室温

S-[2-(4(5)-咪唑基)乙基]异硫脲氢溴酸盐安全信息

[ 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: Irritant;

[ 风险声明 (欧洲) ]:
36/37/38

[ 安全声明 (欧洲) ]:
26-36

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

[ 海关编码 ]:
2933290090

S-[2-(4(5)-咪唑基)乙基]异硫脲氢溴酸盐海关

[ 海关编码 ]: 2933290090

[ 中文概述 ]:
2933290090. 其他结构含非稠合咪唑环的化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933290090. other compounds containing an unfused imidazole ring (whether or not hydrogenated) in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

S-[2-(4(5)-咪唑基)乙基]异硫脲氢溴酸盐文献

S-[2-(4-imidazolyl)ethyl]isothiourea, a highly specific and potent histamine H3 receptor agonist.

J. Pharmacol. Exp. Ther. 263 , 304, (1992)

The effects of a new agonist of histamine (HA) H3 receptors, Imetit (S-[2-(4-(imidazolyl)ethyl]isothiourea) were investigated in vitro and in vivo and compared to those of (R)-alpha-methylhistamine [(...

更多文献