RADIOSYNTHESIS OF A PHOTOAFFINITY PROBE FOR THE COCAINE RECEPTOR OF THE DOPAMINE TRANSPORTER - 3-BETA-(P-CHLOROPHENYL)TROPAN-2-BETA-CARBOXYLIC ACID M-([I-125]-IODO)-P-AZIDOPHENETHYL ESTER ([I-125]-RTI-82)

Authors
LEVER JR CARROLL FI PATEL A ABRAHAM P BOJA J LEWIN A LEW R
Citation
Jr. Lever et al., RADIOSYNTHESIS OF A PHOTOAFFINITY PROBE FOR THE COCAINE RECEPTOR OF THE DOPAMINE TRANSPORTER - 3-BETA-(P-CHLOROPHENYL)TROPAN-2-BETA-CARBOXYLIC ACID M-([I-125]-IODO)-P-AZIDOPHENETHYL ESTER ([I-125]-RTI-82), Journal of labelled compounds & radiopharmaceuticals, 33(12), 1993, pp. 1131-1137
Citations number
19
Categorie Soggetti
Chemistry Analytical","Pharmacology & Pharmacy
Journal title
Journal of labelled compounds & radiopharmaceuticals → ACNP
ISSN journal
03624803
Volume
33
Issue
12
Year of publication
1993
Pages
1131 - 1137
Database
ISI
SICI code
0362-4803(1993)33:12<1131:ROAPPF>2.0.ZU;2-J
Abstract
The tropane alkaloid RTI-82, an iodoarylazide, has been labeled with i odine-125 for use as a photoaffinity probe for the cocaine binding sit e of the dopamine transporter. The one-flask radiosynthesis involves n o-carrier-added electrophilic radioiodination of the corresponding ani line followed by diazotization and treatment with sodium azide. Isolat ion by reverse phase HPLC and solid phase extraction gives [I-125]-RTI -82 in good yield (76 +/- 7%, n = 6), high radiochemical purity (> 99. 8%), and high specific radioactivity (1490 - 1880 mCi/mumol).