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.
(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.
Ametamey
S M
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
M
Carrey-Rémy
N
N
Bläuenstein
P
P
Willmann
M
M
Bischoff
S
S
Schmutz
M
M
Schubiger
P A
PA
Auberson
Y P
YP
D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology*; D001665:Binding Sites / Q000187:drug effects; D005260:Female; D005998:Glycine / Q000378:metabolism*; D020128:Inhibitory Concentration 50; D007457:Iodine Radioisotopes / Q000737:chemistry; D007668:Kidney / Q000378:metabolism; D051379:Mice; D008807:Mice, Inbred BALB C; D063065:Organophosphonates / Q000138:chemical synthesis* / Q000378:metabolism / Q000493:pharmacokinetics / Q000494:pharmacology*; D011810:Quinoxalines / Q000138:chemical synthesis* / Q000378:metabolism / Q000493:pharmacokinetics / Q000494:pharmacology*; D011869:Radioligand Assay; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology*; D016194:Receptors, N-Methyl-D-Aspartate / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013379:Substrate Specificity; D014018:Tissue Distribution
C404216:7-iodo-N-(1-phosphonoethyl)-5-aminomethylquinoxaline-2,3-dione; D000927:Anticonvulsants; D007457:Iodine Radioisotopes; D063065:Organophosphonates; D011810:Quinoxalines; D019275:Radiopharmaceuticals; D016194:Receptors, N-Methyl-D-Aspartate; D005998:Glycine