Alvimopan

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Alvimopan

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

156053-89-3

爱维莫潘
ADL 8-2698
LY 246736

Alvimopan (ADL 8-2698) 是一种有效，选择性，具有口服活性和可逆的 μ-阿片受体 (μ-opioid receptor) 拮抗剂，IC₅₀值为 1.7 nM。Alvimopan 对 μ-阿片受体 (K_i=0.47 nM) 的选择性高于 κ- (K_i=100 nM) 和 δ-阿片受体 (K_i=12 nM)。Alvimopan 可用于术后肠梗阻的研究。

生物活性

Alvimopan (ADL 8-2698) is a potent, selective, orally active and reversibleμ-opioid receptorantagonist, with anIC₅₀of 1.7 nM. Alvimopan has selectivity for μ-opioid receptor (K_i=0.47 nM) overκ-andδ-opioid receptors(K_is=100, 12 nM, respectively). Alvimopan can be used for the research of postoperative ileus^[1]^[2]^[3].

IC₅₀& Target

IC50: 1.7 nM (μ-opioid receptor)^[1]

体外研究
(In Vitro)

Alvimopan inhibits the loperamide-stimulated [³⁵S]GTPγS binding to membranes containing the cloned human μ-opioid receptor, with an IC₅₀value of 1.7 nM^[1].

体内研究
(In Vivo)

Alvimopan (0.1-1.0 mg/kg; p.o.) partially antagonizes the slowing of small intestinal transit of¹¹³Sn-labelled microspheres produced by morphine in rats^[3].
Alvimopan (3 mg/kg; p.o.) has no effect on the visceromotor behavioural responses (VMR) induced by noxious colorectal distension (CRD) in conscious rats^[3].

Clinical Trial

分子量

424.53

Formula

C₂₅H₃₂N₂O₄

CAS 号

156053-89-3

中文名称

爱维莫潘；阿维莫泮；爱维莫泮

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.