Cimetropium Bromide (C09-1119-617)

Cimetropium Bromide (DA-3177) is a mAChR antagonist for long-term treatment of irritable bowel syndrome.In VitroCimetropium 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoWhen 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only.Form:SolidIC50& Target:mAChR. Specification: 0.96 Molecular Formula: C21H28BrNO4 Molecular Weight: 438.36 PubChem CID: 20054870 Isomeric SMILES: C[N+]1([C@@H]2CC(C[C@H]1[C@H]3[C@@H]2O3)OC(=O)[C@H](CO)C4=CC=CC=C4)CC5CC5.[Br-]