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化学性质:
规格 | 5mg 10mg 50mg 500mg |
CAS | 170098-38-1 |
别名 | LY 246736 dihydrate;ADL 8-2698 dihydrate |
化学名 | 2-[[(2S)-2-benzyl-3-[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethylpiperidin-1-yl]propanoyl]amino]acetic acid;dihydrate |
分子式 | C25H36N2O6 |
分子量 | 460.56 |
溶解度 | Soluble in DMSO |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
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].
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原创作者:上海莼试生物技术有限公司
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