- 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.
- 化学性质
从乙腈结晶，熔点174℃。[α]
D
20
-18.3°(C=3)。
- 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。
医药
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。
