Alverine Citrate - CAS 5560-59-8
Catalog number: 5560-59-8
Category: Inhibitor
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Molecular Formula:
C26H35NO7
Molecular Weight:
473.56
COA:
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Targets:
5-HT Receptor
Description:
Alverine Citrate is a highly potent competitive CXCR4 antagonist with EC50 of 0.3 nM.
Purity:
>98%
Synonyms:
WZ811
MSDS:
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InChIKey:
RYHCACJBKCOBTJ-UHFFFAOYSA-N
InChI:
InChI=1S/C20H27N.C6H8O7/c1-2-21(17-9-15-19-11-5-3-6-12-19)18-10-16-20-13-7-4-8-14-20;7-3(8)1-6(13,5(11)12)2-4(9)10/h3-8,11-14H,2,9-10,15-18H2,1H3;13H,1-2H2,(H,7,8)(H,9,10)(H,11,12)
Canonical SMILES:
CCN(CCCC1=CC=CC=C1)CCCC2=CC=CC=C2.C(C(=O)O)C(CC(=O)O)(C(=O)O)O
1.A rapid and most sensitive liquid chromatography/tandem mass spectrometry method for simultaneous determination of alverine and its major metabolite, para hydroxy alverine, in human plasma: application to a pharmacokinetic and bioequivalence study.
Ghosh C1, Jha V, Ahir R, Shah S, Shinde CP, Chakraborty BS. Drug Test Anal. 2010 Jun;2(6):284-91. doi: 10.1002/dta.130.
A rapid and highly sensitive method for the determination of alverine (ALV) and its metabolite, para hydroxy alverine (PHA), in human plasma using LC-MS/MS in positive ion electrospray ionization (ESI) in multiple reactions monitoring (MRM) mode was developed and validated. The procedure involves a simple solid phase extraction (SPE). Chromatographic separation was carried out on a Hypersil GOLD C(18) column (50 mm x 4.6 mm, 5 microm) with an isocratic mobile phase and a total run time of 1.5 min. The standard calibration curves showed excellent linearity within the range of 0.060-10.051 ng/mL for ALV and 0.059-10.017 ng/mL for PHA (r > or = 0.990). This method was successfully applied to a pharmacokinetic study after oral administration of alverine citrate 120 mg capsule in Indian healthy male volunteers.
2.Pharmacologic Agents for Chronic Diarrhea.
Lee KJ1. Intest Res. 2015 Oct;13(4):306-12. doi: 10.5217/ir.2015.13.4.306. Epub 2015 Oct 15.
Chronic diarrhea is usually associated with a number of non-infectious causes. When definitive treatment is unavailable, symptomatic drug therapy is indicated. Pharmacologic agents for chronic diarrhea include loperamide, 5-hydroxytryptamine type 3 (5-HT3) receptor antagonists, diosmectite, cholestyramine, probiotics, antispasmodics, rifaximin, and anti-inflammatory agents. Loperamide, a synthetic opiate agonist, decreases peristaltic activity and inhibits secretion, resulting in the reduction of fluid and electrolyte loss and an increase in stool consistency. Cholestyramine is a bile acid sequestrant that is generally considered as the first-line treatment for bile acid diarrhea. 5-HT3 receptor antagonists have significant benefits in patients with irritable bowel syndrome (IBS) with diarrhea. Ramosetron improves stool consistency as well as global IBS symptoms. Probiotics may have a role in the prevention of antibiotic-associated diarrhea.
3.Anxiolytic-like effects of alverine citrate in experimental mouse models of anxiety.
Gupta D1, Radhakrishnan M2, Kurhe Y3. Eur J Pharmacol. 2014 Nov 5;742:94-101. doi: 10.1016/j.ejphar.2014.08.033. Epub 2014 Sep 6.
Anxiety disorders are widely spread psychiatric illnesses that are a cause of major concern. Despite a consistent increase in anxiolytics, the prevalence of anxiety is static; this necessitates the development of new compounds with potential activity and minimum unwanted effects. A serotonergic (5HT) system plays an important role in pathogenesis of anxiety and predominantly involves 5HT1A receptor action in mediating anxiety-like behavior; the antagonism of 5HT1A receptor has demonstrated to produce anxiolytic-like effects. Alverine citrate (AVC) is reported as a 5HT1A antagonist; however, its effects on anxiety-like behavior are not investigated. Thus, the present study, by utilizing a neurobehavioral approach, examined the anxiolytic-like effects of AVC in experimental mouse models of anxiety. Mice were acutely treated with AVC (5-20mg/kg, i.p.)/diazepam (DIA, 2mg/kg, i.p.) and subjected to four validated anxiety models viz. elevated plus-maze (EPM), light/dark (L/D), hole-board (HB) and marble burying (MB) tests.
4.Effect of antispasmodic agents, alone or in combination, in the treatment of Irritable Bowel Syndrome: systematic review and meta-analysis.
Martínez-Vázquez MA1, Vázquez-Elizondo G, González-González JA, Gutiérrez-Udave R, Maldonado-Garza HJ, Bosques-Padilla FJ. Rev Gastroenterol Mex. 2012 Apr-Jun;77(2):82-90. doi: 10.1016/j.rgmx.2012.04.002. Epub 2012 Jun 5.
INTRODUCTION: Irritable bowel syndrome (IBS) is characterized by recurrent abdominal pain, bloating, and changes in bowel habit.
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CAS 5560-59-8 Alverine Citrate

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