Abstract
(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.
MeSH terms
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Animals
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Anticonvulsants / chemical synthesis*
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Anticonvulsants / pharmacokinetics
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Anticonvulsants / pharmacology*
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Binding Sites / drug effects
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Female
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Glycine / metabolism*
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Inhibitory Concentration 50
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Iodine Radioisotopes / chemistry
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Kidney / metabolism
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Mice
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Mice, Inbred BALB C
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Organophosphonates / chemical synthesis*
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Organophosphonates / metabolism
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Organophosphonates / pharmacokinetics
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Organophosphonates / pharmacology*
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Quinoxalines / chemical synthesis*
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Quinoxalines / metabolism
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Quinoxalines / pharmacokinetics
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Quinoxalines / pharmacology*
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Radioligand Assay
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Radiopharmaceuticals / chemical synthesis*
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Radiopharmaceuticals / pharmacokinetics
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Radiopharmaceuticals / pharmacology*
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Receptors, N-Methyl-D-Aspartate / antagonists & inhibitors*
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Receptors, N-Methyl-D-Aspartate / metabolism
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Substrate Specificity
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Tissue Distribution
Substances
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7-iodo-N-(1-phosphonoethyl)-5-aminomethylquinoxaline-2,3-dione
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Anticonvulsants
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Iodine Radioisotopes
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Organophosphonates
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Quinoxalines
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Radiopharmaceuticals
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Receptors, N-Methyl-D-Aspartate
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Glycine