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Alvimopan dihydrate

CAS No. : 170098-38-1

MCE 站：Alvimopan dihydrate

产品活性：Alvimopan dihydrate (ADL 8-2698 dihydrate) 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 dehydrate 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 dehydrate 可用于术后肠梗阻的研究。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：Opioid Receptor

In Vitro: Alvimopan inhibits the loperamide-stimulated [³⁵S]GTPγS binding to membranes containing the cloned human μ-opioid receptor, with an IC₅₀ of 1.7 nM.

In Vivo: Alvimopan (0.1-1.0 mg/kg; p.o.) partially antagonizes the slowing of small intestinal transit of ¹¹³Sn-labelled microspheres produced by morphine in rats.
Alvimopan (3 mg/kg; p.o.) has no effect on the visceromotor behavioural responses (VMR) induced by noxious colorectal distension (CRD) in conscious rats.

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