Alvimopan

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种选择性外周作用 μ-阿片类拮抗剂，IC50 为 1.7 nM，用于治疗术后肠梗阻。

A selective peripherally acting μ-opioid antagonist with IC50 of 1.7 nM for the treatment of postoperative ileus; prevents gastrointestinal effects of intravenous morphine without affecting analgesia; orally active.Other Indication Approved(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 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.

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

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.

ADL 8-2698 | LY 246736

Endocrinology/Hormones

Opioid Receptor

μ-opioidreceptor

Other Indications

Other Disease

156053-89-3

424.5326

C25H32N2O4

>98% (HPLC)

10 mM in DMSO

O=C(O)CNC([C@H](CN1C[C@H](C)[C@](C)(C2=CC=CC(O)=C2)CC1)CC3=CC=CC=C3)=O

Glycine, N-[(2S)-2-[[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl]-1-oxo-3-phenylpropyl]-

(-20℃)

With Ice Pack

≥ 2 years