ChemicalBook CAS数据库列表 Naldemedine
Naldemedine
- CAS号:916072-89-4
- 英文名:Naldemedine
- 中文名:Naldemedine
- 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
- InChIKey :AXQACEQYCPKDMV-RZAWKFBISA-N
Naldemedine性质、用途与生产工艺
- 生物活性 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)。
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体内研究
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).
Naldemedine上下游产品信息
上游原料
下游产品
Naldemedine生产厂家
- 公司名称：Venkatasai Life Sciences
- 联系电话：--
- 电子邮件：info@venkatasailifesciences.com
- 国家：印度
- 产品数：186
- 优势度：58
