纳曲吲哚盐酸盐
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- CAS号:
- 111469-81-9
- 英文名:
- NALTRINDOLE HYDROCHLORIDE
- 英文别名:
- NTI;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
- 中文名:
- 纳曲吲哚盐酸盐
- 中文别名:
- 纳曲吲哚盐酸盐;化合物 T12169
- CBNumber:
- CB3276996
- 分子式:
- C26H27ClN2O3
- 分子量:
- 450.96
- MOL File:
- 111469-81-9.mol
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纳曲吲哚盐酸盐化学性质
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储存条件:
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−20°C
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溶解度:
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methanol: 4.5 mg/mL
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形态:
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solid
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颜色:
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off-white
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纳曲吲哚盐酸盐性质、用途与生产工艺
Naltrindole hydrochloride是高效,选择性的非多肽类 δ opioid 受体拮抗剂,Ki值为0.02 nM。
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.
纳曲吲哚盐酸盐
上下游产品信息
上游原料
下游产品
更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
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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 |
纳曲吲哚盐酸盐
生产厂家
全球有 52家供应商
纳曲吲哚盐酸盐国内生产厂家
111469-81-9, 纳曲吲哚盐酸盐 相关搜索:
- Opioid receptor and opioid-like receptor
- C26H26N2O3HCl
- 化合物 T12169
- 纳曲吲哚盐酸盐
- 111469-81-9
- 17-(Cyclopropylmethyl)-6,7-dehydro-4,5α-epoxy-3,14-dihydroxy-6,7-2',3'-indolomorphinanhydrochloride
- 17-(Cyclopropylmethyl)-6,7-dehydro-4,5alpha-epoxy-3,14-dihydroxy-6,7-2',3'-indolomorphinan hydrochloride
- 17-(CYCLOPROPYLMETHYL)-6,7-DEHYDRO-4,5A-EPOXY-3,14-DIHYDROXY-6,7-2',3'-INDOLOMORPHINAN HYDROCHLORIDE
- NaltrindoleHCl
- NALTRINDOLE HYDROCHLORIDE (NTI) NON-PEPT IDE DELTA OPI
- NTI HYDROCHLORIDE
- NTI
- NALTRINDOLE HYDROCHLORIDE
- NALTRIDOLE HYDROCHLORIDE