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Otilonium bromide

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Chemical Structure| 26095-59-0 同义名 : Octylonium bromide;SP63;Octylonium;Otilonium (bromide)
CAS号 : 26095-59-0
货号 : A237499
分子式 : C29H43BrN2O4
纯度 : 98%
分子量 : 563.567
MDL号 : MFCD00211142
存储条件：

粉末 Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(88.72 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 100 mg/mL(177.44 mM)
动物实验配方：

PO 0.5% CMC-Na 100 mg/mL suspension

生物活性
靶点

  • mAChR
描述 Otilonium bromide (OB) is a smooth muscle relaxant used in the treatment of irritable bowel syndrome. Otilonium bromide inhibited the generation of ACh-induced calcium signals in a dose dependent manner (IC50=880 nM)[3]. In experiments with recordings in the same cells of whole-cell IDMPP, Na+ currents (INa) and Ca2+ currents (ICa), 1 mM otilonium blocked 87% IDMPP, 7% INa and 13% ICa. Otilonium inhibited the K+-evoked catecholamine secretory response of superfused bovine chromaffin cells with an IC50 of 10 mM and inhibited the secretory responses induced by 10 s pulses of 50 mM DMPP with an IC50 of 7.4 nM[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.77mL

0.35mL

0.18mL

8.87mL

1.77mL

0.89mL

17.74mL

3.55mL

1.77mL
参考文献

[1]Martinez-Cutillas M, Gil V, et al. Mechanisms of action of otilonium bromide (OB) in human cultured smooth muscle cells and rat colonic strips. Neurogastroenterol Motil. 2013 Dec;25(12):e803-12.

[2]Forte E, Pizzoferrato M, et al. The use of anti-spasmodics in the treatment of irritable bowel syndrome: focus on otilonium bromide. Eur Rev Med Pharmacol Sci. 2012 Jan;16(1):25-37.

[3]Lindqvist S, Hernon J, Sharp P, Johns N, Addison S, Watson M, Tighe R, Greer S, Mackay J, Rhodes M, Lewis M, Stebbings W, Speakman C, Evangelista S, Johnson I, Williams M. The colon-selective spasmolytic otilonium bromide inhibits muscarinic M(3) receptor-coupled calcium signals in isolated human colonic crypts. Br J Pharmacol. 2002 Dec;137(7):1134-42.

[4]Gandía L, Villarroya M, Lara B, Olmos V, Gilabert JA, López MG, Martínez-Sierra R, Borges R, García AG. Otilonium: a potent blocker of neuronal nicotinic ACh receptors in bovine chromaffin cells. Br J Pharmacol. 1996 Feb;117(3):463-470.