In vivo evaluation of the biodistribution of 11C-labeled PD153035 in rats without and with neuroblastoma implants.
The biodistribution of 11C-labeled 4-(3-bromoanilino)-6,7-dimethoxyquinazoline, an inhibitor of the epidermal growth factor (EGF) receptor tyrosine kinase, has been evaluated in vivo in rats using positron emission tomography (PET). Time-activity data obtained after i.v. administration in one rat revealed that the radiotracer rapidly cleared from plasma with subsequent uptake in major organs of the body (brain, heart, liver, gastrointestinal tract and bladder). Uptake in proliferating tissue in rats with human neuroblastoma xenografts indicate that [O-11C-methyl]PD153035 shows promise as a new agent for in vivo imaging of tumors with PET.
Fredriksson
A
A
Karolinska Pharmacy, and Clinical Neuroscience Department, Karolinska Hospital and Institute, Stockholm, Sweden. anna.fredriksson@neuro.ks.se
Johnström
P
P
Thorell
J O
JO
von Heijne
G
G
Hassan
M
M
Eksborg
S
S
Kogner
P
P
Borgström
P
P
Ingvar
M
M
Stone-Elander
S
S
D000818:Animals; D002250:Carbon Radioisotopes; D066246:ErbB Receptors / Q000037:antagonists & inhibitors*; D005069:Evaluation Studies as Topic; D005260:Female; D006801:Humans; D009368:Neoplasm Transplantation; D009447:Neuroblastoma / Q000473:pathology*; D011799:Quinazolines / Q000493:pharmacokinetics*; D051381:Rats; D017207:Rats, Sprague-Dawley; D014018:Tissue Distribution; D014055:Tomography, Emission-Computed; D014407:Tumor Cells, Cultured
D002250:Carbon Radioisotopes; D011799:Quinazolines; D066246:ErbB Receptors; C088860:4-((3-bromophenyl)amino)-6,7-dimethoxyquinazoline