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抑制剂 > 内分泌和激素 > Alvimopan dihydrate
产品名称:
Alvimopan dihydrate
型号:
CS-01Y78087
生产地址
国产
产品价格
电议
产品简介
质量保证、价格优惠
产品详情

一、概述:

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
All other available size: ship with RT , or blue ice upon request

 

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].

特别提醒:                                                                                                              

1. 本产品仅供科研使用。请勿用于医药、临床诊断或治疗,食品及化妆品等用途。请勿存放于普通住宅区。

2. 为了您的安全和健康,请穿好实验服并佩戴一次性手套和口罩操作。

标签:Alvimopan dihydrate 

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