Antitumoural action of L-733,060 on neuroblastoma and glioma cell lines.

Abstract

We have performed an in vitro study of the growth-inhibitory capacity of the potent and long-acting NK1 receptor antagonist L-733,060, at concentrations ranging from 2.5 microM to 20 microM, against the neuroblastoma cell line SKN-BE(2) and 10 microM to 25 microM for glioma cell line GAMG. Coulter counter was used to determine viable cell numbers, followed by application of the tetrazolium compound [3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)2-(4-sulfophenyl)-2H-tetrazolium], inner salt colorimetric method to evaluate cell viability in this cytotoxicity assay. L-733,060 inhibited the growth of the two cell lines studied in a dose-dependent manner. The IC 50 values were 11.6 microM (30h) and 10.2 microM (72h) for SKN-BE(2); and 21.3 microM (48h) and 19.9 microM (96h) for GAMG. These findings indicate that the NK1 receptor antagonist L-733,060 acts as a broad-spectrum antitumoural agent. This new action, reported here for the first time, suggests that the NK1 receptor antagonist L-733,060 could be a promising therapeutic drug for the treatment of human neuroblastoma and human glioma.

• Authors: M Muñoz, A Pérez, R Coveñas, M Rosso, E Castro
• Journal: Archives italiennes de biologie (Arch Ital Biol) Vol. 142 Issue 2 Pg. 105-12 (Mar 2004) ISSN: 0003-9829 [Print] Italy
• PMID: 15248566 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Antineoplastic Agents
• Neurokinin-1 Receptor Antagonists
• Piperidines
• Receptors, Neurokinin-1
• 3-((3,5-bis(trifluoromethyl)phenyl)methyloxy)-2-phenylpiperidine
• Substance P

Topics

• Antineoplastic Agents (pharmacology, therapeutic use)
• Brain Neoplasms (drug therapy, metabolism)
• Cell Division (drug effects, physiology)
• Cell Line, Tumor
• Dose-Response Relationship, Drug
• Glioma (drug therapy, metabolism)
• Humans
• Neuroblastoma (drug therapy, metabolism)
• Neurokinin-1 Receptor Antagonists
• Piperidines (pharmacology, therapeutic use)
• Receptors, Neurokinin-1 (metabolism)
• Substance P (antagonists & inhibitors, metabolism)