Synthesis and characteristics in tumor-bearing mice of N-[11C]methyl-1-deoxynojirimycin and N-[11C]methyl-1-deoxymannojirimycin.
N-[11C]Methyl-1-deoxynojirimycin ([11C]MDNM) and N-[11C]methyl-1-deoxymannojirimycin ([11C]MDMM) were prepared by 11C-methylation of 1-deoxynojirimycin (DNM) and 1-deoxymannojirimycin (DMM), which are specific inhibitors of glucosidase and mannosidase, respectively. In mice bearing Ehrich ascitic tumor, the highest uptake of the [11C]MDNM was observed in the kidney, followed by the liver and small intestine, while the tumor uptake was moderate. By MDNM loading, saturable uptake was observed in these tissues. In homogenates of the kidney and tumor tissues, a considerable amount of radioactivity was detected in a high-molecular weight fraction. These results demonstrate that the [11C]MDNM has a potential for imaging the glucosidase activity by positron emission tomography. On the other hand, [11C]MDMM showed lower uptake than [11C]MDNM in the kidney, liver and small intestine and no effect of carrier DMM, suggesting that the [11C]MDMM would not reflect mannosidase activity.
Ishiwata
K
K
Positron Medical Center, Tokyo Metropolitan Institute of Gerontology, Japan.
Seki
H
H
Sasaki
T
T
Ishii
S
S
Nozaki
T
T
Senda
M
M
D017485:1-Deoxynojirimycin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000493:pharmacokinetics; D000818:Animals; D002250:Carbon Radioisotopes; D002286:Carcinoma, Ehrlich Tumor / Q000378:metabolism*; D005959:Glucosidases / Q000037:antagonists & inhibitors / Q000378:metabolism; D008297:Male; D008361:Mannosidases / Q000037:antagonists & inhibitors / Q000378:metabolism; D051379:Mice; D014018:Tissue Distribution; D014055:Tomography, Emission-Computed
D002250:Carbon Radioisotopes; D017485:1-Deoxynojirimycin; D005959:Glucosidases; D008361:Mannosidases; C033424:N-methyldeoxynojirimycin