MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

Naltrindole hydrochloride

CAS No. : 111469-81-9

MCE 站：Naltrindole hydrochloride

产品活性：Naltrindole hydrochloride是高效，选择性的非多肽类 δ opioid 受体拮抗剂，K_i值为0.02 nM。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：Opioid Receptor

In Vitro: 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 EC₅₀ 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.

In Vivo: 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.

相关产品：Bioactive Compound Library Plus  |  GPCR/G Protein Compound Library  |  Neuronal Signaling Compound Library  |  Anti-Cancer Compound Library  |  Neurotransmitter Receptor Compound Library  |  DAMGO  |  Sinomenine hydrochloride  |  JDTic dihydrochloride  |  Matrine  |  Loperamide hydrochloride  |  Nalfurafine hydrochloride  |  Nociceptin  |  JTC-801  |  [Leu5]-Enkephalin  |  Norbinaltorphimine dihydrochloride  |  Tyr-Gly-Gly-Phe-Met-OH  |  Endomorphin 1  |  CTAP TFA  |  Endomorphin 2 TFA  |  Noscapine  |  LY2795050  |  β-Endorphin, human  |  N-Desmethylclozapine  |  BAN ORL 24  |  Dynorphin A  |  Alvimopan dihydrate  |  Asimadoline  |  Dynorphin A (1-10) (TFA)  |  Corydaline  |  Porcine dynorphin A(1-13)  |  Dermorphin  |  Dynorphin B (1-13) (TFA)  |  Frakefamide TFA

品牌介绍:
•   MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供*新*全的高品质小分子活性化合物；
•   10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种期刊及制药收录了MCE客户的科研成果；
•   专业团队跟踪*新的制药及生命科学研究进展，为您提供全球*新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。