Name | NALTRINDOLE HYDROCHLORIDE |
Synonyms | NTI NaltrindoleHCl NTI HYDROCHLORIDE NALTRIDOLE HYDROCHLORIDE NALTRINDOLE HYDROCHLORIDE NALTRINDOLE HYDROCHLORIDE (NTI) NON-PEPT IDE DELTA OPI 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 |
CAS | 111469-81-9 |
Molecular Formula | C26H27ClN2O3 |
Molar Mass | 450.96 |
Solubility | methanol: 4.5mg/mL |
Appearance | solid |
Color | off-white |
Storage Condition | −20°C |
In vitro study | 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. |
In vivo study | 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. |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.218 ml | 11.088 ml | 22.175 ml |
5 mM | 0.444 ml | 2.218 ml | 4.435 ml |
10 mM | 0.222 ml | 1.109 ml | 2.218 ml |
5 mM | 0.044 ml | 0.222 ml | 0.444 ml |