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Alvimopan dihydrate Sale

(Synonyms: 爱维莫潘; ADL 8-2698 dihydrate; LY 246736 dihydrate) 目录号 : GC12619

A μ-opioid receptor antagonist

Alvimopan dihydrate Chemical Structure

Cas No.:170098-38-1

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5mg
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50mg
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Sample solution is provided at 25 µL, 10mM.

产品文档

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产品描述

Alvimopan dihydrate is a selective antagonist of opioid receptor with IC50 value of 1.7 nM.
Opioid receptor is a G protein-coupled receptor with opioids as ligands.
The dissociation rate of alvimopan from the micro opioid receptor (t(1/2)=30-44 min) was slower than those of the antagonists N-methylnaltrexone (t(1/2)=0.46 min) and naloxone (t(1/2)=0.82 min), and was similar to that of the long acting partial agonist buprenorphine (t(1/2)=44 min). When preincubation with the micro opioid receptor, the affinity and potency of alvimopan increased apparently, which is consistent with its long duration of action [1].
Patients with opioid induced bowel dysfunction (OBD) orally received alvimopan 0.5 mg twice daily (BID), 1 mg once daily (QD), 1 mg BID, or placebo for 6 weeks. Alvimopan significantly increased spontaneous bowel movements (SBMs) frequency each week in the last three weeks with alvimopan 0.5 mg BID (+1.71 mean SBMs/week), alvimopan 1 mg QD (+1.64) and alvimopan 1 mg BID (+2.52), respectively. While, Alvimopan caused side effects such as abdominal pain, nausea, and diarrhea, which was the same as the placebo. Alvimopan restored GI function and relieved OBD without affecting analgesia [2].
References:
[1]. Cassel JA, Daubert JD, DeHaven RN. [(3)H]Alvimopan binding to the micro opioid receptor: comparative binding kinetics of opioid antagonists. Eur J Pharmacol, 2005, 520(1-3): 29-36.
[2]. Webster L, Jansen JP, Peppin J, et al. Alvimopan, a peripherally acting mu-opioid receptor (PAM-OR) antagonist for the treatment of opioid-induced bowel dysfunction: results from a randomized, double-blind, placebo-controlled, dose-finding study in subjects taking opioids for chronic non-cancer pain. Pain, 2008, 137(2): 428-440.

Chemical Properties

Cas No. 170098-38-1 SDF
别名 爱维莫潘; ADL 8-2698 dihydrate; LY 246736 dihydrate
化学名 2-[[(2S)-2-benzyl-3-[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethylpiperidin-1-yl]propanoyl]amino]acetic acid;dihydrate
Canonical SMILES CC1CN(CCC1(C)C2=CC(=CC=C2)O)CC(CC3=CC=CC=C3)C(=O)NCC(=O)O.O.O
分子式 C25H36N2O6 分子量 460.56
溶解度 DMSO : 92mg/mL 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
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1 mM 2.1713 mL 10.8563 mL 21.7127 mL
5 mM 0.4343 mL 2.1713 mL 4.3425 mL
10 mM 0.2171 mL 1.0856 mL 2.1713 mL
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