爱维莫潘

CAS号:170098-38-1
英文名:2-[[(2S)-2-benzyl-3-[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperi dyl]propanoyl]amino]acetic acid dihydrate
中文名:爱维莫潘
CBNumber:CB21261077
分子式:C25H36N2O6
分子量:460.57
MOL File:170098-38-1.mol

爱维莫潘化学性质

爱维莫潘性质、用途与生产工艺

生物活性 Alvimopan (LY-246736)是一种有效的、相对非选择性的opioid拮抗剂，对μ, δ 和 κ opioid receptors的Ki值分别为0.77、4.4和40 nM，选择性比对其他胺类G蛋白偶联受体高100倍以上
靶点
Target Value
μ-opioid receptor
(Cell-free assay) 0.77 nM(Ki)
δ-opioid receptor
(Cell-free assay) 4.4 nM(Ki)
κ-opioid receptor
(Cell-free assay) 40 nM(Ki)
体外研究

Alvimopan inhibits the loperamide-stimulated [ ³⁵ S]GTPγS binding to membranes containing the cloned human μ-opioid receptor, with an IC ₅₀ of 1.7 nM.
体内研究

Alvimopan (0.1-1.0 mg/kg; p.o.) partially antagonizes the slowing of small intestinal transit of ¹¹³ Sn-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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Target	Value
μ-opioid receptor (Cell-free assay)	0.77 nM(Ki)
δ-opioid receptor (Cell-free assay)	4.4 nM(Ki)
κ-opioid receptor (Cell-free assay)	40 nM(Ki)