Synthesis of [3(R)-amino-2(S)-sulfhydryl-5-sulfonate]-pentanoyl-(S)-3-[I-125]-iodotyrosyl-(S)-aspartic acid: a radiolabelled inhibitor of aminopeptidase A

Authors
David-Basei, C Bischoff, L Fournie-Zaluski, MC Roques, BP
Citation
C. David-basei et al., Synthesis of [3(R)-amino-2(S)-sulfhydryl-5-sulfonate]-pentanoyl-(S)-3-[I-125]-iodotyrosyl-(S)-aspartic acid: a radiolabelled inhibitor of aminopeptidase A, J LABEL C R, 44(1), 2001, pp. 89-98
Citations number
32
Categorie Soggetti
Chemistry & Analysis","Inorganic & Nuclear Chemistry
Journal title
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS
ISSN journal
03624803 → ACNP
Volume
44
Issue
1
Year of publication
2001
Pages
89 - 98
Database
ISI
SICI code
0362-4803(200101)44:1<89:SO[>2.0.ZU;2-#
Abstract
In order to investigate the localization of aminopeptidase A in the central nervous system and peripheral organs, we have synthesized the first radiol abelled inhibitor of this enzyme. This molecule, [3(R)-amino-2(S)-sulfhydry l-5-sulfonate]-pentanoyl-(S)-3-[I-125]-iodotyrosyl-(S)-aspartic acid, exhib ited a Ki value of 4.8 nM for aminopeptidase A. A high purity was obtained with a specific activity of about 2,000 Ci/mmol at the end of the synthesis .