916072-89-4
916072-89-4 structure
- Name: S 297995
- Chemical Name: Naldemedine
- CAS Number: 916072-89-4
- Molecular Formula: C32H34N4O6
- Molecular Weight: 570.64
- Catalog: Signaling Pathways GPCR/G Protein Opioid Receptor
- Create Date: 2020-08-11 10:59:20
- Modify Date: 2024-01-12 03:59:53
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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].
| Name | Naldemedine |
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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]. |
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| Related Catalog | |
| 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). |
| References |
| Molecular Formula | C32H34N4O6 |
|---|---|
| Molecular Weight | 570.64 |