111469-81-9
![111469-81-9 结构式](/CAS/GIF/111469-81-9.gif)
基本信息
NaltrindoleHCl
NTI HYDROCHLORIDE
NALTRIDOLE HYDROCHLORIDE
NALTRINDOLE HYDROCHLORIDE
NALTRINDOLE HYDROCHLORIDE (NTI) NON-PEPT IDE DELTA OPI
17-(Cyclopropylmethyl)-6,7-dehydro-4,5α-epoxy-3,14-dihydroxy-6,7-2',3'-indolomorphinanhydrochloride
17-(CYCLOPROPYLMETHYL)-6,7-DEHYDRO-4,5A-EPOXY-3,14-DIHYDROXY-6,7-2',3'-INDOLOMORPHINAN HYDROCHLORIDE
17-(Cyclopropylmethyl)-6,7-dehydro-4,5alpha-epoxy-3,14-dihydroxy-6,7-2',3'-indolomorphinan hydrochloride
报价日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
2022/09/18 | HY-101177 | 纳曲吲哚盐酸盐 Naltrindole hydrochloride | 111469-81-9 | 5mg | 990元 |
2022/09/18 | HY-101177 | 纳曲吲哚盐酸盐 Naltrindole hydrochloride | 111469-81-9 | 10mM * 1mLin DMSO | 1089元 |
2022/09/18 | HY-101177 | 纳曲吲哚盐酸盐 Naltrindole hydrochloride | 111469-81-9 | 10mg | 1350元 |
常见问题列表
Ki: 0.02 nM (δ opioid), 64 nM (μ opioid), 66 nM (κ opioid)
Opioid drugs exert a wide spectrum of physiological and behavioral effects. These effects are mediated via membrane-bound receptors, of which the best characterized are the kappa, delta, and mu receptors. Naltrindole inhibits the proliferation of cultured human U266 MM cells in a time- and dose-dependent manner with an EC 50 of 16 μM. Treatment of U266 cells with naltrindole significantly decreases the level of the active, phosphorylated form of the kinases, extracellular signal-regulated kinase and Akt, which may be related to its antiproliferative activity. Naltrindole inhibits growth and induces apoptosis in the three characteristic SCLC cell lines, NCI-H69, NCI-H345, and NCI-H510. Naltrindole treatment reduces constitutive phosphorylation of Akt/PKB on serine 473 and threonine 308 in cells and also its downstream effectors glycogen synthase kinase-3β and the Forkhead transcription factors AFX and FKHR.
Naltrindole significantly decreases tumor cell volumes in human MM cell xenografts in severe combined immunodeficient mice. In mice, naltrindole at 20 mg/kg s.c. antagonizes the δ-selective agonist effect of [D- Ser, Leu, Thr]enkephalin (DSLET) without blocking the antinociceptive effect of morphine or U50488H. Naltrindole is the only highly selective δ antagonist that is active upon peripheral administration. Acute naltrindole induces significant decreases in external and total ambulation (horizontal activity) and rearing behaviour (vertical activity), as well as a significant increase in grooming frequency. In animals chronically treated with naltrindole there is an increase in total ambulation one day after the discontinuation of the treatment.