(2S,1'S,2'R,3'R)-2(2'-Carboxy-3'-hydroxymethylcyclopropyl)glycine-[3H], a potent and selective radioligand for labeling group 2 and 3 metabotropic glutamate receptors.
We report herein the synthesis of the tritium labeled isotopomer of 1 and its use as a radioligand to label mGlu8 receptors in rat forebrain membranes as well as cloned human recombinant mGlu receptors. [(3)H]-1 was synthesized by the NaBT(4) reduction of an activated analog of 5. [(3)H]-1 bound appreciably to recombinant human mGlu2, mGlu3 and mGlu8 receptors and to rat forebrain membranes and was displaced by L-glutamate and L-(+)-2 amino-4-phosphonobutyric acid. The results indicate that [(3)H]-1 should be a useful ligand for the study of mGluR2, 3, and 8 receptors in cloned cell lines and possibly brain tissue.
Wheeler
William J
WJ
Lilly Research Laboratories, A Division of Eli Lilly and Company, Indianapolis, IN 46285, USA. wheeler_william_joe_dr@lilly.com
Clodfelter
Dean K
DK
Collado
Ivan
I
Kulanthaivel
Palaniappan
P
Pedregal
Concepcion
C
Stoddard
Eli A
EA
Wright
Rebecca A
RA
Schoepp
Darryle D
DD
D000613:Aminobutyrates / Q000494:pharmacology; D000818:Animals; D001921:Brain / Q000187:drug effects* / Q000378:metabolism; D002460:Cell Line; D002462:Cell Membrane / Q000378:metabolism; D003521:Cyclopropanes / Q000737:chemistry* / Q000494:pharmacology; D018698:Glutamic Acid / Q000494:pharmacology; D005998:Glycine / Q000031:analogs & derivatives* / Q000737:chemistry* / Q000494:pharmacology; D006801:Humans; D007553:Isotope Labeling / Q000379:methods*; D008024:Ligands; D051381:Rats; D018094:Receptors, Metabotropic Glutamate / Q000378:metabolism*; D014316:Tritium
C501340:(2S,1'S,2'R,3'R)-2(2'-carboxy-3'-hydroxymethylcyclopropyl)glycine-(3H); D000613:Aminobutyrates; D003521:Cyclopropanes; D008024:Ligands; D018094:Receptors, Metabotropic Glutamate; C108822:metabotropic glutamate receptor 2; C102718:metabotropic glutamate receptor 3; D014316:Tritium; D018698:Glutamic Acid; C012729:2-amino-4-phosphonobutyric acid; D005998:Glycine