Abstract:
:In vivo pharmacokinetic and brain binding characteristics of [18F]RP 62203, a selective high-affinity serotonergic 5-HT2A receptor antagonist, were assessed in the rat following intravenous injection of trace amount of the radioligand. The radioactive distribution profile observed in the brain 60 min after injection was characterized by greater than fourfold higher uptake in neocortex as compared to cerebellum (0.38 +/- 0.07% injected dose/g, % ID/g and 0.08 +/- 0.01 ID/g, respectively), consistent with in vivo specific binding to the 5-HT2A receptor. Furthermore, specific [18F]RP 62203 binding significantly correlated with the reported in vitro distribution of 5-HT2A receptors, but not with known concentration profiles of dopaminergic D2 or adrenergic alpha 1 receptors. Finally, detectable specific binding was abolished by pretreatment with large doses of ritanserin, a selective 5-HT2A antagonist, which resulted in uniform uptakes across cortical, striatal and cerebellar tissues. Thus, [18F]RP 62203 appears to be a promising selective tool to visualize and quantify 5-HT2A brain receptors in vivo with positron emission tomography.
journal_name
Nucl Med Bioljournal_title
Nuclear medicine and biologyauthors
Besret L,Dauphin F,Huard C,Lasne MC,Vivet R,Mickala P,Barbelivien A,Baron JCdoi
10.1016/0969-8051(95)02008-xsubject
Has Abstractpub_date
1996-02-01 00:00:00pages
169-71issue
2eissn
0969-8051issn
1872-9614pii
0969-8051(95)02008-Xjournal_volume
23pub_type
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journal_title:Nuclear medicine and biology
pub_type: 杂志文章
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