| CAS NO: | 916072-89-4 |
| 包装: | 500μg |
| 市场价: | 4914元 |
| Cas No. | 916072-89-4 |
| 别名 | S-297995 |
| Canonical SMILES | OC1=CC=C2C3=C1O[C@](C(O)=C(C(NC(C)(C)C4=NC(C5=CC=CC=C5)=NO4)=O)C6)([H])[C@@]3(CCN7CC8CC8)[C@]6(O)[C@H]7C2 |
| 分子式 | C32H34N4O6 |
| 分子量 | 570.6 |
| 溶解度 | Chloroform: slightly soluble |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | Naldemedine is a peripherally acting opioid receptor antagonist (IC50s = 1.15, 1.11, and 1.5 nM for recombinant human μ-, δ-, and κ-opioid receptors, respectively).1,2 It inhibits opioid-induced emesis and vomiting in ferrets and opioid-induced constipation in rats (ED50 = 0.03 mg/kg for both) without affecting the analgesic effect of morphine in the tail-flick test in rats.1 Naldemedine induces the opioid withdrawal symptoms of diarrhea and teeth chattering, but not jumping, in morphine-dependent rats when administered at doses of 1 and 3 mg/kg, respectively.2 Formulations containing naldemedine have been used in the treatment of opioid-induced constipation. |1. Inagaki, M., Kume, M., Tamura, Y., et al. Discovery of naldemedine: A potent and orally available opioid receptor antagonist for treatment of opioid-induced adverse effects. Bioorg. Med. Chem. Lett. 29(1), 73-77 (2019).|2. Kanemasa, T., Koike, K., Arai, T., 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. 31(5), e13563 (2019). |
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