916072-89-4
中文名稱
Naldemedine
英文名稱
Naldemedine
CAS
916072-89-4
分子式
C32H34N4O6
分子量
570.64
MOL 文件
916072-89-4.mol
更新日期
2025/01/21 09:32:25
916072-89-4 結(jié)構(gòu)式
基本信息
中文別名
S-297995化合物 T33583
英文別名
Morphinan-7-carboxamide, 17-(cyclopropylmethyl)-6,7-didehydro-4,5-epoxy-3,6,14-trihydroxy-N-[1-methyl-1-(3-phenyl-1,2,4-oxadiazol-5-yl)ethyl]-, (5α)-常見問題列表
生物活性
Naldemedine (S-297995) 是一種口服活性、外周作用的 μ-opioid 受體拮抗劑。Naldemedine 對 μ-阿片受體、δ-阿片受體、κ-阿片受體具有較強(qiáng)的結(jié)合親和力 (IC50 分別為1.15、1.11 和 1.5 nM) 和拮抗活性 (IC50 分別為 25.57、7.09 和 16.1 nM)。Naldemedine 在不影響阿片鎮(zhèn)痛作用的情況下緩解阿片類藥物所致便秘 (OIC)。體內(nèi)研究
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 ED 50 s ± 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.
| Animal Model: | 6-week-old Crlj: WI male rats |
| 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). |