Carbon-11 labelled cholecystokininB antagonists: radiosynthesis and evaluation in rats.
Three cholecystokinin type B (CCKB) receptor antagonists were labelled with 11C and evaluated ex vivo in rat biodistribution studies. The CCKB antagonists were YF 476 and two other compounds of the basic 3-ureido-1,4-benzodiazepine class. Following tail-vein administration of [11C]-YF 476 exceedingly low levels of radioactivity were found in all brain regions from 5 to 60 min post-injection. Similar results were obtained using the other two 11C-labelled CCKB antagonists. In light of the very poor brain penetration of these compounds, reports on the central nervous system activity of this class of CCKB antagonists should be viewed with caution.
PET Centre, The Centre for Addiction and Mental Health, Toronto, Ontario, Canada. aaw@camhpet.on.ca
A A
AA
Wilson
L
L
Jin
A
A
Garcia
J N
JN
DaSilva
S
S
Houle
D000818:Animals; D001570:Benzodiazepinones / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics*; D001921:Brain / Q000378:metabolism; D002250:Carbon Radioisotopes; D006727:Hormone Antagonists / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics*; D007553:Isotope Labeling; D007700:Kinetics; D008297:Male; D010671:Phenylurea Compounds / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics*; D051381:Rats; D017207:Rats, Sprague-Dawley; D011949:Receptors, Cholecystokinin / Q000037:antagonists & inhibitors*; D014018:Tissue Distribution
D001570:Benzodiazepinones; D002250:Carbon Radioisotopes; D006727:Hormone Antagonists; D010671:Phenylurea Compounds; D011949:Receptors, Cholecystokinin; C104428:YF 476