Journal article
Synthesis, radiolabelling and biological characterization of (D)-7-iodo-N-(1-phosphonoethyl)-5-aminomethylquinoxaline-2,3-dione, a glycine-binding site antagonist of NMDA receptors.
- Ametamey SM Center for Radiopharmaceutical Science of the ETH, Paul Scherrer Institute and Division of Nuclear Medicine, University Hospital Zurich, Villigen PSI, Switzerland. simon-mensah.ametamey@psi.ch
- Kokic M
- Carrey-Rémy N
- Bläuenstein P
- Willmann M
- Bischoff S
- Schmutz M
- Schubiger PA
- Auberson YP
- 2000-01-15
Published in:
- Bioorganic & medicinal chemistry letters. - 2000
Animals
Anticonvulsants
Binding Sites
Female
Glycine
Inhibitory Concentration 50
Iodine Radioisotopes
Kidney
Mice
Mice, Inbred BALB C
Organophosphonates
Quinoxalines
Radioligand Assay
Radiopharmaceuticals
Receptors, N-Methyl-D-Aspartate
Substrate Specificity
Tissue Distribution
English
(D)-7-Iodo-N-(1-phosphonoethyl)-5-aminomethylquinoxaline-2,3 -dione (I-PAMQX), is a potent, in vivo active antagonist acting at the glycine binding site of the NMDA receptor complex. Radioiodinated [131I]I-PAMQX was prepared with good yields and high specific activity from its 7-bromo analogue. Biodistribution studies of [131I]I-PAMQX in mice showed a relatively slow clearance from the blood. The uptake of radioactivity was highest in the kidneys, moderate in the heart, lung, liver and bones, and low in the brain.
- Language
-
- English
- Open access status
- closed
- Identifiers
-
- DOI 10.1016/s0960-894x(99)00576-4
- PMID 10636248
- Persistent URL
- https://folia.unifr.ch/global/documents/222187
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