A significant increase in intracellular Ca2+ concentration induced by (2S,3R,4S)-2-(carboxycyclopropyl)glycine, a new potent NMDA agonist, in cultured rat hippocampal neurons.
The increase in intracellular Ca2+ concentration, [Ca2+]i, induced by isomers of 2-(carboxycyclopropyl)glycine (CCG) was examined in cultured rat hippocampal neurons. Some CCG isomers and N-methyl-D-aspartate (NMDA) increased [Ca2+]i in a concentration dependent manner. The 2S,3R,4S isomer of CCG (L-CCG-IV) was the most potent in elevating [Ca2+]i, and its activity was more than 100 times higher than that of NMDA and about 10 times higher than that of L-glutamate. The increase in [Ca2+]i was effectively blocked by NMDA blockers and Mg2+, and was markedly augmented by the addition of a low concentration of glycine. L-CCG-IV would be a useful tool for elucidation of functions of NMDA receptors.
Kudo
Y
Y
Department of Neuroscience, Mitsubishi Kasei Institute of Life Science, Tokyo, Japan.
Akita
K
K
Ishida
M
M
Shinozaki
H
H
D000600:Amino Acids, Dicarboxylic / Q000037:antagonists & inhibitors / Q000494:pharmacology*; D000818:Animals; D002118:Calcium / Q000378:metabolism*; D002478:Cells, Cultured; D006624:Hippocampus / Q000166:cytology / Q000378:metabolism*; D016202:N-Methylaspartate / Q000494:pharmacology*; D009474:Neurons / Q000187:drug effects / Q000378:metabolism*; D051381:Rats; D016194:Receptors, N-Methyl-D-Aspartate / Q000187:drug effects*
D000600:Amino Acids, Dicarboxylic; D016194:Receptors, N-Methyl-D-Aspartate; C035261:(alpha-carboxycyclopropyl)glycine; D016202:N-Methylaspartate; D002118:Calcium