Alvimopan monohydrate

A μ-opioid receptor antagonist

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库存: 现货

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数量
5mg

￥1037.00

830.00

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10mg

￥1625.00

1300.00

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50mg

￥5612.00

4490.00

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货号: ajce54864
CAS: 1383577-62-5
别名: 爱维莫潘水合物; ADL 8-2698 monohydrate; LY 246736 monohydrate
分子式: C25H34N2O5
分子量: 442.55
纯度: >98%
溶解度: Soluble in DMSO
储存: Store at -20°C
库存: 现货

Background

Alvimopan is a μ-opioid receptor antagonist (K_i = 0.47 nM).¹ It is selective over the κ- and δ-opioid receptors (K_is= 100 nM and 12 nM, respectively). Alvimopan inhibits μ-opioid receptor-mediated GTP binding to CHO cell membranes with an IC₅₀ value of 1.7 nM. It inhibits morphine-induced slowing of colorectal transit in mice with an ED₅₀ value of 0.41 mg/kg.² Alvimopan (0.3 and 1 mg/kg, p.o.) reduces inhibition of gastrointestinal (GI) transit induced by morphine, but not apraclonidine , in rats. Formulations containing alvimopan have been used in the treatment of opioid-induced bowel dysfunction.

1.Le Bourdonnec, B., Barker, W.M., Belanger, S., et al.Novel trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidines as μ opioid receptor antagonists with improved opioid receptor selectivity profilesBioorg. Med. Chem. Lett.18(6)2006-2012(2008) 2.Greenwood-Van Meerveld, B., Gardner, C.J., Little, P.J., et al.Preclinical studies of opioids and opioid antagonists on gastrointestinal functionNeurogastroenterol. Motil.16(Suppl. 2)46-53(2004)