Abstract:
: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.
journal_name
Life Scijournal_title
Life sciencesauthors
Wilson AA,Jin L,Garcia A,DaSilva JN,Houle Sdoi
10.1016/s0024-3205(00)01021-3subject
Has Abstractpub_date
2001-02-02 00:00:00pages
1223-30issue
11eissn
0024-3205issn
1879-0631pii
S0024320500010213journal_volume
68pub_type
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