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51598-60-8

中文名称 西托溴铵
英文名称 Cimetropium bromide
CAS 51598-60-8
分子式 C21H28BrNO4
分子量 438.36
MOL 文件 51598-60-8.mol
51598-60-8 结构式 51598-60-8 结构式

基本信息

中文别名
西托溴铵
溴化N-(环丙基甲基)东莨菪碱
英文别名
da3177
Cimetropium
DA-3177:Alginor
Cimetropiumbromid
Cimetronin bromide
CIMETROPIUM BROMIDE
N-Cyclopropvlmethylscopolamine bromide
(7(S)-(1alpha,2beta,4beta,5alpha,7beta))-9-(Cyclopropylmethyl)-7-(3-hydroxy-1-oxo-2-phenylpropoxy)-9-methyl-3-oxa-9-azoniatricyclo(3.3.1.0(sup 2,4))nonane bromide

物理化学性质

外观性状从乙腈结晶,熔点174℃。[α] D20-18.3°(C=3)。
熔点174°
比旋光度D20 -18.3° (c = 3)
储存条件Hygroscopic, -20°C Freezer, Under inert atmosphere
溶解度DMSO(少许)、甲醇(少许)、水(少许)
形态固体
颜色白色

安全数据

危险性符号(GHS)
GHS07
警示词警告
危险性描述H302

应用领域

用途1
能阻断内脏平滑肌的毒蕈碱型受体,因而有抗毒草碱的作用,还有解除平滑肌的痉挛。用于胆石绞痛、肾绞痛、胃肠道痉挛痛、胆道和尿路痉挛痛、痛经、分娩痛等。

制备方法

方法1
由化合物(Ⅰ)和环丙基溴甲烷,在乙腈中回流15~99h,得到西托溴铵。

上下游产品信息

上游原料
溴甲基环丙烷
西托溴铵价格(试剂级)
报价日期产品编号产品名称CAS号包装价格
2024/04/30HY-U00106西托溴铵
Cimetropium Bromide
51598-60-81 mg350元
2024/04/30HY-U00106西托溴铵
Cimetropium Bromide
51598-60-85mg650元
2024/04/30HY-U00106西托溴铵
Cimetropium Bromide
51598-60-810mM * 1mLin Water715元

常见问题列表

生物活性
Cimetropium Bromide (DA-3177) 是一种毒蕈碱受体拮抗剂,用于长期研究肠易激综合征。
靶点

mAChR

体外研究

Cimetropium Bromide behaves as a competitive antagonist of muscarinic-mediated contractions in isolated colonic preparations from both species, with affinity values (pA2) ranging between 7.41 and 7.82. Cimetropium has potent antimuscarinic effect in inhibition of contraction of longitudinal muscle preparations. In the superfusion experiments of the preparation which has been preloaded with labelled choline, Cimetropium decreases the labelled ACh release induced by electrical field stimulation under the muscarinic autoinhibition blocked-condition.

体内研究

When administered intravenously to conscious dogs provided with a colonic Thiry fistula, Cimetropium is a potent inhibitor of large bowel motility evoked by both exogenous and endogenous stimuli. Cimetropium Bromide (10-100 μg/kg) counteracts colonic motor response to neostigmine administration with an ID 50 of 27.9 μg/kg; both tonic and phasic components of contractile response are affected. In a comparable range of doses (3-100μg/kg), the drug inhibits motor activity elicited by intraluminal distension.

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