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抑制剂 > 神经科学 > Metiamide
产品名称:
Metiamide
型号:
CS-01Y76444
生产地址
进口、国产
产品价格
电议
产品简介
质量保证、价格优惠
产品详情

一、概述:

化学性质:                                                                                                             

规格

5mg 10mg 50mg

CAS

34839-70-8

别名

 

化学名

1-methyl-3-[2-[(5-methyl-1H-imidazol-4-yl)methylsulfanyl]ethyl]thiourea

分子式

C9H16N4S2

分子量

244.38

溶解度

Soluble in Water

储存条件

Store at -20°C

General tips

For obtaining a higher solubility , please warm the tube at 37 and shake it in the ultrasonic bath for a while.

Shipping Condition

Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

 

产品描述:                                                                                                            

Metiamide is a high-selective and oral bioavailable antagonist of histamine H2-receptor with ED50 value of 25 μmol/kg [1].

Unlike the traditional antihistaminics which are H1-receptor antagonists, metiamide is an antagonist of H2-receptor. It is developed from burimamide which is a previously found antagonist of H2-receptor. Metiamide acts as a competitive antagonist and blocks the combination of histamine and its receptor. This blockade results in the inhibition of gastric acid secretion stimulated by histamine and other hormone such as pentagastrin and gastrin. Compared with burimamide, metiamide showed higher activity and good oral bioavailability [1 and 2].

In the in vitro assays, metiamide displayed about 10-fold higher activity than burimamide on rat uterine muscle and guinea-pig heart muscle with Kb values of 0.75 and 0.92 μM, respectively. The Kb value of burimamide on the atrial muscle was 7.8 μM. Besides that, metiamide showed no efficacy on H1-receptor and isoprenaline even at the concentration of 1 mM suggested that metiamide was also a selective antagonist. Moreover, metiamide was found to cause increase in chemokinesis and random migration in PMN cells similar to histamine. It was different that metiamide had no effects on the true chemotaxis whereas histamine significantly suppressed the chemotaxis, which demonstrated histamine affected neutrophil motility through the H2-receptor site [1 and 3].

In dogs, the administration of metiamide inhibited acid secretion stimulated by histamine from both the Heidenhain pouch and the gastric fistula. It also inhibited acid secretion stimulated by pentagastrin and liver extract from both the Heidenhain pouch and the main stomach. When metiamide was given by intravenous injection, the doses of it to cause 50% inhibition of the maximal histamine- and pentagastrin-stimulated acid secretion were 3.1 and 6.1 μmol/kg. When metiamide was given by oral administration, the ED50 value of it to cause inhibition was 16 μmol/kg [1 and 2].

特别提醒:                                                                                                              

1. 本产品仅供科研使用。请勿用于医药、临床诊断或治疗,食品及化妆品等用途。请勿存放于普通住宅区。

2. 为了您的安全和健康,请穿好实验服并佩戴一次性手套和口罩操作。

标签:Metiamide 

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