| Identification | Back Directory | [Name]
AlviMopan (Monohydrate) | [CAS]
1383577-62-5 | [Synonyms]
AlviMopan (Monohydrate)
((S)-2-benzyl-3-((3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethylpiperidin-1-yl)propanoyl)glycine hydrate
N-[(2S)-2-[[(3R,4R)-4-(3-Hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl]-1-oxo-3-phenylpropyl]glycine hydrate (1:1) | [Molecular Formula]
C25H34N2O5 | [MOL File]
1383577-62-5.mol | [Molecular Weight]
442.548 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in Chloroform,Dichloromethane,Ethyl Acetate,DMSO,Acetone,etc. | [form ]
Powder | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
Alvimopan monohydrate (ADL 8-2698 monohydrate) is a potent, selective, orally active and reversible μ-opioid receptor antagonist, with an IC50 of 1.7 nM. Alvimopan monohydrate has selectivity for μ-opioid receptor (Ki=0.47 nM) over κ- and δ-opioid receptors (Kis=100, 12 nM, respectively). Alvimopan monohydrate can be used for the research of postoperative ileus[1][2][3]. | [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[3].
Alvimopan (3 mg/kg; p.o.) has no effect on the visceromotor behavioural responses (VMR) induced by noxious colorectal distension (CRD) in conscious rats[3]. | [IC 50]
μ Opioid Receptor/MOR | [References]
[1] Bourdonnec BL, et, al. Novel trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidines as mu opioid receptor antagonists with improved opioid receptor selectivity profiles. Bioorg Med Chem Lett. 2008 Mar 15;18(6):2006-12. DOI:10.1016/j.bmcl.2008.01.106
[2] Erowele GI, et, al. Alvimopan (Entereg), a Peripherally Acting mu-Opioid Receptor Antagonist For Postoperative Ileus. P T. 2008 Oct;33(10):574-83. PMID:19750041
[3] Meerveld BG, et, al. Preclinical studies of opioids and opioid antagonists on gastrointestinal function. Neurogastroenterol Motil. 2004 Oct;16 Suppl 2:46-53. DOI:10.1111/j.1743-3150.2004.00555.x |
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