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Alvimopan dihydrate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Alvimopan dihydrate图片
CAS NO:170098-38-1
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)460.57
FormulaC25H36N2O6
CAS No.170098-38-1 (di-hydrate);
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 92 mg/mL (199.8 mM)
Water: >1mg/mL
Ethanol:>1mg/mL
Chemical Name((S)-2-benzyl-3-((3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethylpiperidin-1-yl)propanoyl)glycine dihydrate
SynonymsLY246736 dihydrate; LY246736; LY-246736; HSDB 7704; HSDB7704 dihydrate; HSDB-7704; ADL 8-2698; ADL8-2698; ADL-8-2698 dihydrate; Alvimopan dihydrate. Brand name: Entereg.
实验参考方法
In Vitro

In vitro activity: Alvimopan (also known as ADL 8-2698; LY 246736; HSDB-7704) is a novel peripheral micro opioid antagonist in clinical development for the management of post-operative ileus and opioid-induced bowel dysfunction. The long duration of action of alvimopan might be related to a slower dissociation rate from the micro opioid receptor compared to other shorter acting antagonists. The dissociation rate of alvimopan from the micro opioid receptor (t(1/2)=30--44 min) was comparable to that of the long acting partial agonist buprenorphine (t(1/2)=44 min), but was slower than those of the antagonists naloxone (t(1/2)=0.82 min) and N-methylnaltrexone (t(1/2)=0.46 min). Also, increases in the apparent affinities and potencies of buprenorphine and alvimopan, but not of naloxone and methylnaltrexone, were observed upon preincubation with the micro opioid receptor. Consistent with its long duration of action, alvimopan has a slow dissociation rate from the micro opioid receptor compared to other shorter acting antagonists and may be more potent if administered prior to dosing with exogenous opioids.


Kinase Assay: Alvimopan is highly selective (by ≥227-fold) for the human μ receptor over the κ subtype, but has a more modest (≥6-fold) μ/δ receptor selectivity. In the guinea pig isolated ileum, alvimopan is a potent antagonist of morphine, DAMGO or endomorphin-1-induced, and μ opioid receptor-mediated, inhibition of electrically-evoked contractions (pA2 values of 9.6 or 9.7). The δ and κ antagonist potencies of alvimopan are lower in the guinea pig ileum (pA2 values of 8.7 and 7.8, respectively). Alvimopan (1 or 10 μM) has no significant affinity for a broad range of non-opioid receptors, ion channels and enzymes at which it has been tested.


Cell Assay:

In VivoIn animals, alvimopan antagonizes centrally mediated, morphine-induced analgesia only at relatively high doses, with very high plasma concentrations needed to cross the blood-brain barrier. After intravenous administration, alvimopan is approximately 200-times more potent at blocking peripheral verses central μ-receptors. After oral administration, alvimopan is also highly active. In dogs, intravenous administration of alvimopan provided dose-dependent increases in peak plasma concentrations and plasma area under the concentration-time curve. However, as a result of poor systemic absorption, oral doses up to 100 mg/kg produced low plasma concentrations (mean Cmax =92.9 ng/ml), which resulted in an oral bioavailability of approximately 0.03%. The half-life of alvimopan is estimated to be approximately 10 min after intravenous administration in dogs and rabbits.
Animal modeldogs and rabbits
Formulation & Dosage100 mg/kg; i.v.
ReferencesP T. 2008 Oct; 33(10): 574, 580-583; Surg Endosc. 2006 Jan;20(1):64-70; Eur J Pharmacol. 2005 Sep 27;520(1-3):29-36.