1. GPCR/G Protein
    Neuronal Signaling
  2. Opioid Receptor
  3. Naldemedine

Naldemedine (Synonyms: S-297995)

Cat. No.: HY-19627
Handling Instructions

Naldemedine (S-297995) is an orally active, peripherally acting µ-opioid receptor antagonist. Naldemedine shows potent binding affinities (IC50s = 1.15, 1.11, and 1.5 nM, repectively) and antagonist activities (IC50s= 25.57, 7.09, 16.1 nM, repectively) for recombinant human μ-, δ-, and κ- opioid receptors. Naldemedine tempers opioid-induced constipation (OIC) without compromising opioid analgesia.

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Naldemedine Chemical Structure

Naldemedine Chemical Structure

CAS No. : 916072-89-4

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Description

Naldemedine (S-297995) is an orally active, peripherally acting µ-opioid receptor antagonist. Naldemedine shows potent binding affinities (IC50s = 1.15, 1.11, and 1.5 nM, repectively) and antagonist activities (IC50s= 25.57, 7.09, 16.1 nM, repectively) for recombinant human μ-, δ-, and κ- opioid receptors. Naldemedine tempers opioid-induced constipation (OIC) without compromising opioid analgesia[1].

In Vivo

Naldemedine (S-297995) (0.001-10 mg/kg; p.o.) significantly represses the opioid-induced inhibition of small intestinal transit in rats. In the subcutaneous Morphine-induced inhibition model, the ED50s ± standard error of the mean is 0.03 ± 0.02 mg/kg for Naldemedine. Subcutaneous morphine-inhibited castor oil-induced diarrhea in rats, and pretreatment with Naldemedine 0.03-1 mg/kg significantly reverses this effect[1].

Animal Model: 6-week-old Crlj: WI male rats[1]
Dosage: 0.001-10 mg/kg
Administration: P.o.
Result: Significantly repressed the opioid-induced inhibition of small intestinal transit in rats by subcutaneous morphine (P < 0.05 or P < 0.01 for naldemedine 0.03-10 mg/kg), and oxycodone (P < 0.01 for naldemedine 0.03-3 mg/kg).
Molecular Weight

570.64

Formula

C₃₂H₃₄N₄O₆

CAS No.

916072-89-4

SMILES

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

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Keywords:

NaldemedineS-297995S297995S 297995Opioid ReceptorperipherallyemesisconstipationanalgesiceffectInhibitorinhibitorinhibit

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