Alverine-citrate-NSC-35459-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEAlverine citrateCat. No.: HY-B0500CAS No.: 5560-59-8Synonyms: NSC 35459分式: CHNO分量: 473.56作靶點(diǎn): 5-HT Receptor作通路: GPCR/G Protein; Neuronal Signaling儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DM

2、SO : 22 mg/mL (46.46 mM; Need ultrasonic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 2.1117 mL 10.5583 mL 21.1166 mL5 mM 0.4223 mL 2.1117 mL 4.2233 mL10 mM 0.2112 mL 1.0558 mL 2.1117 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Alverine citrate5-HT1A 受體的個(gè)拮抗

3、劑，其 IC50 值為101 nM。IC50 & Target 5-HT1A Receptor101 nM (IC50)體外研究Alverine is a drug used for functional gastrointestinal disorders. Alverine acts directly on the muscle in the1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEgut, causing it to relax. Alverine Citrate (20 mg/kg) suppresses the effect o

4、f 5-HTP, but not that of 8-OH-DPAT. However, when injected intracerebroventricularly (75 g/rat) alverine citrate reduces 8-OH-DPAT-induced enhancement of rectal distension-induced abdominal contractions. In-vitro binding studies revealthat Alverine citrate has a high affinity for 5-HT1A receptors an

5、d a weak affinity for 5-HT3 and 5-HT4subtypes 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 toCa2+ 2.REFERENCES1. Coelho, A.M., et al

6、., Rectal antinociceptive properties of alverine citrate are linked to antagonism at the 5-HT1A receptor subtype. JPharm 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.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: 40