Carbon-11 labelling of the antitumour agent N-[2-(dimethylamino)ethyl]acridine-4-carboxamide (DACA) and determination of plasma metabolites in man.
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.
Brady
F
F
MRC Clinical Sciences Centre, Royal Postgraduate Medical School, Hammersmith Hospital, London, UK.
Luthra
S K
SK
Brown
G
G
Osman
S
S
Harte
R J
RJ
Denny
W A
WA
Baguley
B C
BC
Jones
T
T
Price
P M
PM
D000166:Acridines / Q000138:chemical synthesis* / Q000378:metabolism*; D000328:Adult; D000368:Aged; D000369:Aged, 80 and over; D000970:Antineoplastic Agents / Q000097:blood* / Q000138:chemical synthesis*; D002250:Carbon Radioisotopes / Q000737:chemistry*; D004305:Dose-Response Relationship, Drug; D005260:Female; D006801:Humans; D007553:Isotope Labeling / Q000379:methods; D008297:Male; D008875:Middle Aged; D009369:Neoplasms / Q000097:blood / Q000000981:diagnostic imaging; D014055:Tomography, Emission-Computed
D000166:Acridines; D000970:Antineoplastic Agents; D002250:Carbon Radioisotopes; C058332:N-(2'-(dimethylamino)ethyl)acridine-4-carboxamide