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枸橼酸阿尔维林

枸橼酸阿尔维林用途

Alverine citrate 是 5-HT1A 受体的一个拮抗剂,其 IC50 值为101 nM。

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枸橼酸阿尔维林名称

[ CAS 号 ]:
5560-59-8

[ 中文名 ]:
N-乙基-3,3′-二苯二丙胺

[ 英文名 ]:
Alverine citrate

[中文别名 ]:

枸橼酸阿尔维林

[英文别名 ]:

MFCD00035086
EINECS 226-929-3
Alverine Citrate
Alverine (citrate)

枸橼酸阿尔维林生物活性

[ 描述 ]:

Alverine citrate 是 5-HT1A 受体的一个拮抗剂,其 IC50 值为101 nM。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 5-HT受体

信号通路 >> 神经信号通路 >> 5-HT受体

研究领域 >> 代谢疾病

[ 靶点 ]

5-HT1A Receptor:101 nM (IC50)

[体外研究]

Alverine是一种用于功能性胃肠道疾病的药物。 Alverine直接作用于肠道的肌肉,使其放松。柠檬酸阿尔维林(20mg/kg)抑制5-HTP的作用,但不抑制8-OH-DPAT的作用。然而,当脑室内注射(75μg/大鼠)时,柠檬酸阿维菌素可减少8-OH-DPAT诱导的直肠扩张引起的腹部收缩。体外结合研究表明,Alverine柠檬酸盐对5-HT1A受体具有高亲和力,对5-HT3和5-HT4亚型具有弱亲和力[1]。由于抑制L型Ca通道的失活,Alverine可能在动作电位期间增加Ca流入,但也可能通过抑制收缩蛋白对Ca2 +的敏感性来抑制诱发活性[2]。

[参考文献]

[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.

[相关活性小分子]

枸橼酸阿尔维林物理化学性质

[ 沸点 ]:
358.8ºC at 760mmHg

[ 分子式 ]:
C₂₆H₃₅NO₇

[ 分子量 ]:
473.55900

[ 闪点 ]:
174.4ºC

[ 精确质量 ]:
473.24100

[ PSA ]:
135.37000

[ LogP ]:
3.32540

[ 储存条件 ]:
-20°C

枸橼酸阿尔维林MSDS

详细MSDS(安全技术说明书)

枸橼酸阿尔维林安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

[ 海关编码 ]:
2921499090

枸橼酸阿尔维林海关

[ 海关编码 ]: 2921499090

[ 中文概述 ]:
2921499090 其他芳香单胺及衍生物及它们的盐. 增值税率:17.0% 退税率:9.0% 监管条件:无最惠国关税:6.5% 普通关税:30.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2921499090 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%

枸橼酸阿尔维林文献

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)

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