Alvimopan monohydrate  (Synonyms: ADL 8-2698 monohydrate; LY 246736 monohydrate)

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 (K_i=0.47 nM) over κ- and δ-opioid receptors (K_is=100, 12 nM, respectively). Alvimopan monohydrate can be used for the research of postoperative ileus^[1][2][3].

Alvimopan inhibits the loperamide-stimulated [³⁵S]GTPγS binding to membranes containing the cloned human μ-opioid receptor, with an IC₅₀ of 1.7 nM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

442.55

C₂₅H₃₄N₂O₅

1383577-62-5

Solid

White to off-white

OC1=CC=CC([C@@]2(C)[C@@H](C)CN(C[C@H](CC3=CC=CC=C3)C(NCC(O)=O)=O)CC2)=C1.O

Room temperature in continental US; may vary elsewhere.

• [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.  [Content Brief]

  [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.  [Content Brief]

  [3]. Meerveld BG, et, al. Preclinical studies of opioids and opioid antagonists on gastrointestinal function. Neurogastroenterol Motil. 2004 Oct;16 Suppl 2:46-53.  [Content Brief]