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Alverine citrate

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Chemical Structure| 5560-59-8 同义名 : 枸橼酸阿尔维林 ;NSC 35459;Alverine (citrate)
CAS号 : 5560-59-8
货号 : A319955
分子式 : C26H35NO7
纯度 : 98%
分子量 : 473.559
MDL号 : MFCD00035086
存储条件:

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(221.73 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

动物实验配方:

PO 0.5% CMC-Na 30 mg/mL suspension

生物活性
描述 Alverine citrate, as a selective 5-HT1A receptor subtype antagonist, inhibits the rectal hypersensitivity induced by serotonin, a mediator involved in IBS(Irritable bowel syndrome) hyperalgesia[3]. Alverine citrate is thought of as a smooth muscle relaxant, and is currently used as an antispasmodic in irritable bowel syndrome and dysmenorrhoea. Alverine (10 μM) increased the frequency and amplitude of spontaneous action potentials, transient increases in [Ca2+]i and associated contractions. Alverine suppressed contractions produced by high K (40 mM) or ACh (10 μM), without affecting electrical responses and with little suppression of increases in [Ca2+] [4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.11mL

0.42mL

0.21mL

10.56mL

2.11mL

1.06mL

21.12mL

4.22mL

2.11mL

参考文献

[1]Wittmann T, Paradowski L, et al. Clinical trial: the efficacy of alverine citrate/simeticone combination on abdominal pain/discomfort in irritable bowel syndrome--a randomized, double-blind, placebo-controlled study. Aliment Pharmacol Ther. 2010 Mar;31(6):615-24.

[2]Coelho AM, Jacob L, et al. Rectal antinociceptive properties of alverine citrate are linked to antagonism at the 5-HT1A receptor subtype. J Pharm Pharmacol. 2001 Oct;53(10):1419-26.

[3]Ducrotte P, Grimaud JC, Dapoigny M, Personnic S, O'Mahony V, Andro-Delestrain MC. On-demand treatment with alverine citrate/simeticone compared with standard treatments for irritable bowel syndrome: results of a randomised pragmatic study. Int J Clin Pract. 2014 Feb;68(2):245-54. doi: 10.1111/ijcp.12333. Epub 2013 Oct 21. PMID: 24147869; PMCID: PMC4282257.

[4]Hayase M, Hashitani H, Suzuki H, Kohri K, Brading AF. Evolving mechanisms of action of alverine citrate on phasic smooth muscles. Br J Pharmacol. 2007 Dec;152(8):1228-38. doi: 10.1038/sj.bjp.0707496. Epub 2007 Oct 15. PMID: 17934514; PMCID: PMC2190002.