CAS 5560-59-8|Alverine citrate

Introduction:Basic information about CAS 5560-59-8|Alverine citrate, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
Common NameAlverine citrate
CAS Number5560-59-8Molecular Weight473.55900
Density/Boiling Point358.8ºC at 760mmHg
Molecular FormulaC26H35NO7Melting Point/
MSDSUSAFlash Point174.4ºC

Names

Namealverine citrate
SynonymMore Synonyms

Alverine citrate BiologicalActivity

DescriptionAlverine citrate is a 5-HT1A receptor antagonist, with an IC50 of 101 nM.
Related CatalogSignaling Pathways >>GPCR/G Protein >>5-HT ReceptorSignaling Pathways >>Neuronal Signaling >>5-HT ReceptorResearch Areas >>Metabolic Disease
Target

5-HT1A Receptor:101 nM (IC50)

In VitroAlverine is a drug used for functional gastrointestinal disorders. Alverine acts directly on the muscle in the gut, causing it to relax. Alverine Citrate (20 mg/kg) suppresses the effect of 5-HTP, but not that of 8-OH-DPAT. However, when injected intracerebroventricularly (75 μg/rat) alverine citrate reduces 8-OH-DPAT-induced enhancement of rectal distension-induced abdominal contractions. In-vitro binding studies reveal that Alverine citrate has a high affinity for 5-HT1A receptors and a weak affinity for 5-HT3 and 5-HT4 subtypes[1]. Alverine may increase Ca influx during action potentials due to inhibition of the inactivation of L-type Ca channels, but may also suppress evoked activity by inhibiting the sensitivity of contractile proteins to Ca2+[2].
References

[1]. Coelho, A.M., et al., Rectal antinociceptive properties of alverine citrate are linked to antagonism at the 5-HT1A receptor subtype. J Pharm Pharmacol, 2001. 53(10): p. 1419-26.

[2]. Hayase, M., et al., Evolving mechanisms of action of alverine citrate on phasic smooth muscles. Br J Pharmacol, 2007. 152(8): p. 1228-38.

Chemical & Physical Properties

Boiling Point358.8ºC at 760mmHg
Molecular FormulaC26H35NO7
Molecular Weight473.55900
Flash Point174.4ºC
Exact Mass473.24100
PSA135.37000
LogP3.32540
InChIKeyRYHCACJBKCOBTJ-UHFFFAOYSA-N
SMILESCCN(CCCc1ccccc1)CCCc1ccccc1.O=C(O)CC(O)(CC(=O)O)C(=O)O
Storage condition-20°C

Safety Information

Personal Protective EquipmentEyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter
RIDADRNONH for all modes of transport
WGK Germany3
HS Code2921499090

Customs

HS Code2921499090
Summary2921499090 other aromatic monoamines and their derivatives; salts thereof VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:30.0%

Articles17

More Articles
Validated LC-MS/MS method for determination of Alverine and one of its hydroxy metabolites in human plasma along with its application to a bioequivalence study.

J. Chromatogr. B. Analyt. Technol. Biomed. Life Sci. 877(3) , 197-206, (2009)

The present research work involves a first of its kind rapid and sensitive liquid chromatography-tandem mass spectrometry (LC-MS/MS) method developed and validated for simultaneous analysis of Alverin...

A general practice study to compare alverine citrate with mebeverine hydrochloride in the treatment of irritable bowel syndrome.

Br. J. Clin. Pract. 40(7) , 276-8, (1986)

Alverine citrate, simeticone, and Rome III irritable bowel syndrome.

Aliment. Pharmacol. Ther. 31(7) , 767-8; author reply 768-9, (2010)

Synonyms

N-ethyl-3-phenyl-N-(3-phenylpropyl)propan-1-amine,2-hydroxypropane-1,2,3-tricarboxylic acid
MFCD00035086
EINECS 226-929-3
Alverine Citrate
Alverine (citrate)
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