Naldemedine  (Synonyms: S-297995)

Naldemedine (S-297995) is an orally active μ-opioid receptor antagonist (PAMORA)^[1]. Naldemedine shows potent binding affinities (Ki=0.34, 0.43, 0.94 nM, respectively) and antagonist activities (IC₅₀=25.57, 7.09, 16.1 nM, respectively) for recombinant human μ-, δ-, and κ- opioid receptors^[2]. Naldemedine can be used in opioid-induced constipation (OIC) research^[2]. Naldemedine is predicted to bind to 3CL^pro encoded by SARS-CoV2 genome^[3].

Naldemedine (oral gavage; 0.03-10 mg/kg; once) represses the opioid-induced inhibition of small intestinal transit in rats by subcutaneous morphine and oxycodone^[2].

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

570.64

C₃₂H₃₄N₄O₆

916072-89-4

O[C@@]1(CC(C(NC(C)(C2=NC(C3=CC=CC=C3)=NO2)C)=O)=C4O)[C@@]([C@@]4([H])OC5=C6O)(CC7)C5=C(C=C6)C[C@@]1([H])N7CC8CC8

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• [1]. Hannah A. Blair. Naldemedine: A Review in Opioid-Induced Constipation. Drugs. 2019 Jul;79(11):1241-1247.  [Content Brief]

  [2]. Toshiyuki Kanemasa, et al. Pharmacologic effects of naldemedine, a peripherally acting μ-opioid receptor antagonist, in in vitro and in vivo models of opioid-induced constipation. Neurogastroenterol Motil. 2019 May;31(5):e13563.  [Content Brief]

  [3]. Sugandh Kumar, et al. Identification of multipotent drugs for COVID-19 therapeutics with the evaluation of their SARS-CoV2 inhibitory activity. Comput Struct Biotechnol J. 2021;19:1998-2017.  [Content Brief]