A novel metabotropic glutamate receptor agonist: (2S,1'S,2'R,3'R)-2-(2-carboxy-3-methoxymethylcyclopropyl)glycine (cis-MCG-I).
A novel agonist for metabotropic glutamate receptors, (2S,1'S,2'R,3'R)-2-(2-carboxy-3-methoxymethylcyclopropyl)glycine (cis-MCG-I), effectively inhibited monosynaptic excitation in newborn rat spinal cords with EC50 of 3 microM without causing any depolarization. Furthermore, cis-MCG-I inhibited the forskolin-stimulated cyclic AMP formation in rat cultured cortical cells with IC50 of 1.5 microM. cis-MCG-I neither stimulated the phosphoinositide hydrolysis nor activated ionotropic glutamate receptors even in high concentrations. However, after a brief exposure of spinal cords to quisqualate, it caused depolarization in a dose-dependent manner. This compound would provide useful information for elucidating physiological functions of metabotropic glutamate receptors.
Department of Pharmacology, Tokyo Metropolitan Institute of Medical Science, Japan.
M
M
Ishida
T
T
Saitoh
Y
Y
Nakamura
K
K
Kataoka
H
H
Shinozaki
D000818:Animals; D002478:Cells, Cultured; D000242:Cyclic AMP / Q000096:biosynthesis; D018690:Excitatory Amino Acid Agonists / Q000494:pharmacology*; D005998:Glycine / Q000031:analogs & derivatives* / Q000494:pharmacology; D010716:Phosphatidylinositols / Q000378:metabolism; D051381:Rats; D017208:Rats, Wistar; D013116:Spinal Cord / Q000187:drug effects / Q000502:physiology
D018690:Excitatory Amino Acid Agonists; D010716:Phosphatidylinositols; C090522:2-(2-carboxy-3-methoxymethylcyclopropyl)glycine; D000242:Cyclic AMP; D005998:Glycine