A potent metabotropic glutamate receptor agonist: electrophysiological actions of a conformationally restricted glutamate analogue in the rat spinal cord and Xenopus oocytes.
The (2S,3S,4S) isomer of alpha-(carboxycyclopropyl)glycine (L-CCG-I), a conformationally restricted glutamate analogue, caused a marked depolarization of motoneurons in the isolated rat spinal cord, which was almost insensitive to CPP and CNQX. Depolarizing responses to L-CCG-I were markedly decreased by reducing the temperature of the bathing fluid. Similar results were obtained in the case of trans-ACPD, which is a metabotropic glutamate receptor agonist, but the depolarizing action of L-CCG-I was more potent than that of trans-ACPD. In Xenopus oocytes injected with poly(A)+ mRNA extracted from the rat brain, L-CCG-I induced significant oscillatory chloride currents, suggesting that L-CCG-I is a potent agonist for metabotropic-type glutamate receptors.
Ishida
M
M
Tokyo Metropolitan Institute of Medical Science, Japan.
Akagi
H
H
Shimamoto
K
K
Ohfune
Y
Y
Shinozaki
H
H
D000600:Amino Acids, Dicarboxylic / Q000494:pharmacology*; D000818:Animals; D000831:Animals, Newborn / Q000502:physiology; D001921:Brain / Q000502:physiology; D003515:Cycloleucine / Q000031:analogs & derivatives / Q000494:pharmacology; D004594:Electrophysiology; D008968:Molecular Conformation; D009865:Oocytes / Q000378:metabolism*; D012333:RNA, Messenger / Q000494:pharmacology; D051381:Rats; D011919:Rats, Inbred Strains; D017470:Receptors, Glutamate; D017981:Receptors, Neurotransmitter / Q000187:drug effects*; D013116:Spinal Cord / Q000378:metabolism*; D014981:Xenopus
D000600:Amino Acids, Dicarboxylic; D012333:RNA, Messenger; D017470:Receptors, Glutamate; D017981:Receptors, Neurotransmitter; D003515:Cycloleucine; C036361:1-amino-1,3-dicarboxycyclopentane; C035261:(alpha-carboxycyclopropyl)glycine