Synthesis of an 125I analog of MK-0591 and characterization of a 5-lipoxygenase activating protein binding assay

Synthesis of an 125I analog of MK-0591 and characterization of a 5-lipoxygenase activating protein binding assay

The 125I analog of MK‐0591, 1, has been prepared for use as a radioligand for developing a 5‐lipoxygenase activating protein (FLAP) binding assay. The radiosynthesis involves a two step oxidative iododestannylation‐saponification procedure. A FLAP binding assay has been developed in human neutrophil...

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Veröffentlicht in:Journal of labelled compounds & radiopharmaceuticals 1994-12, Vol.34 (12), p.1147-1156
Hauptverfasser: Eggler, J. F., Cheng, J. B., Cooper, K., Hanak, L. M., Pillar, J. S., Zdankiewicz, M.
Format: Artikel
Sprache:eng
Schlagworte:
5-lipoxygenase activating protein (FLAP)
Chemistry
Exact sciences and technology
FLAP binding assay
Heterocyclic compounds
Heterocyclic compounds with n hetero atom and also o and/or s, se, te hetero atoms
iodine-125
Organic chemistry
Preparations and properties
radioligand
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Beschreibung
Zusammenfassung:The 125I analog of MK‐0591, 1, has been prepared for use as a radioligand for developing a 5‐lipoxygenase activating protein (FLAP) binding assay. The radiosynthesis involves a two step oxidative iododestannylation‐saponification procedure. A FLAP binding assay has been developed in human neutrophil membranes. The binding of 1 to human neutrophil FLAP is rapid, reversible, of high affinity, saturable and selective for FLAP inhibitors.
ISSN:0362-4803
1099-1344
DOI:10.1002/jlcr.2580341204