Carbon-11 labelled cholecystokininB antagonists: radiosynthesis and evaluation in rats.

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 Sci

journal_title

Life sciences

authors

Wilson AA,Jin L,Garcia A,DaSilva JN,Houle S

doi

10.1016/s0024-3205(00)01021-3

subject

Has Abstract

pub_date

2001-02-02 00:00:00

pages

1223-30

issue

11

eissn

0024-3205

issn

1879-0631

pii

S0024320500010213

journal_volume

68

pub_type

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