Carbon-11 labelling of the antitumour agent N-[2-(dimethylamino)ethyl]acridine-4-carboxamide (DACA) and determination of plasma metabolites in man.

Abstract

The potential anti-cancer agent N-[2-(dimethylamino)ethyl] acridine-4-carboxamide, DACA has been labelled with carbon-11. N-[2-11C-methyl]DACA was produced in 73% radiochemical yield from [11C]iodomethane in 40 min from EOB. The average radiochemical yield was 3.2 GBq with specific radioactivity of 41.5 GBq mumol-1 at EOS, corresponding to 24 micrograms of stable DACA. The position of labelling was confirmed by co-labelling with [11/13C]iodomethane. PET studies in patients have been performed prior to Phase I trial of DACA and during Phase I trial of DACA. Analysis of serial plasma samples showed that the metabolism of N-[2-11C-methyl]DACA is rapid and extensive in patient plasma.

• Authors: F Brady, S K Luthra, G Brown, S Osman, R J Harte, W A Denny, B C Baguley, T Jones, P M Price
• Journal: Applied radiation and isotopes : including data, instrumentation and methods for use in agriculture, industry and medicine (Appl Radiat Isot) Vol. 48 Issue 4 Pg. 487-92 (Apr 1997) ISSN: 0969-8043 [Print] England
• PMID: 9106990 (Publication Type: Clinical Trial, Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Acridines
• Antineoplastic Agents
• Carbon Radioisotopes
• N-(2'-(dimethylamino)ethyl)acridine-4-carboxamide

Topics

• Acridines (chemical synthesis, metabolism)
• Adult
• Aged
• Aged, 80 and over
• Antineoplastic Agents (blood, chemical synthesis)
• Carbon Radioisotopes (chemistry)
• Dose-Response Relationship, Drug
• Female
• Humans
• Isotope Labeling (methods)
• Male
• Middle Aged
• Neoplasms (blood, diagnostic imaging)
• Tomography, Emission-Computed