A SIMPLE PROBE MEASURES THE PHARMACOKINETICS OF [I-125] RTI-55 IN MOUSE-BRAIN IN-VIVO

Citation
T. Mochizuki et al., A SIMPLE PROBE MEASURES THE PHARMACOKINETICS OF [I-125] RTI-55 IN MOUSE-BRAIN IN-VIVO, European journal of pharmacology, 338(1), 1997, pp. 17-23
Citations number
32
Categorie Soggetti
Pharmacology & Pharmacy
ISSN journal
00142999
Volume
338
Issue
1
Year of publication
1997
Pages
17 - 23
Database
ISI
SICI code
0014-2999(1997)338:1<17:ASPMTP>2.0.ZU;2-8
Abstract
A simple external radiation detector system was used to assess brain d opamine and serotonin transporters in mice in vivo using [I-125]RTI-55 . The results were compared to ex vivo dissection data. Methyl 3 beta- (4-iodophenyl) tropane-2 beta-carboxic acid methyl ester (RTI-55 or be ta-CIT), a high-affinity cocaine antagonist, binds to presynaptic dopa mine and serotonin transporters in the brain. Radiotracer accumulation increased for the first 150 min after intravenous injection and their remained constant. When unlabeled RTI-55 was injected, either before or 60 min after radiotracer administration a significant decrease in t racer accumulation was observed [I-125]RTI-55 binding was also displac ed by blocking doses of phenyl)methoxy]ethyl]-4-[3-phenylpropyl]pipera zine dihydrochloride (GBR 12909) and paroxetine. The results were simi lar to the ex vivo dissection data. The results demonstrate the feasib ility of using the probe detector system to study the presynaptic tran sporter system in vivo in the mouse brain. The technique is applicable to other cerebral neurotransmitter systems. (C) 1997 Elsevier Science B.V.