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.

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

西域 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.
Alvimopan (3 mg/kg; p.o.) has no effect on the visceromotor behavioural responses (VMR) induced by noxious colorectal distension (CRD) in conscious rats.

西域 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.
Alvimopan (3 mg/kg; p.o.) has no effect on the visceromotor behavioural responses (VMR) induced by noxious colorectal distension (CRD) in conscious rats.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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  . 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]

  . 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]