Naldemedine
|
|
|
- CAS号:
- 916072-89-4
- 英文名:
- Naldemedine
- 英文别名:
- S297;S 297;S-297;Naldemedine/S-297995;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)-
- 中文名:
- Naldemedine
- 中文别名:
- S-297995;化合物 T33583
- CBNumber:
- CB03368763
- 分子式:
- C32H34N4O6
- 分子量:
- 570.63556
- MOL File:
- 916072-89-4.mol
|
|
|
Naldemedine化学性质
-
储存条件:
-
Store at -20°C
-
|
-
溶解度:
-
Chloroform: slightly soluble
-
|
Naldemedine性质、用途与生产工艺
Naldemedine (S-297995) 是一种口服活性、外周作用的 µ-opioid 受体拮抗剂。Naldemedine 对 μ-阿片受体、δ-阿片受体、κ-阿片受体具有较强的结合亲和力 (IC50 分别为1.15、1.11 和 1.5 nM) 和拮抗活性 (IC50 分别为 25.57、7.09 和 16.1 nM)。Naldemedine 在不影响阿片镇痛作用的情况下缓解阿片类药物所致便秘 (OIC)。
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).
|
Naldemedine
上下游产品信息
上游原料
下游产品
916072-89-4, Naldemedine 相关搜索:
- 化合物 T33583
- S-297995
- 916072-89-4
- Naldemedine/S-297995
- S-297
- S297
- S 297
- 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)-