Glycine antagonist action of 1-aminocyclobutane-1-carboxylate (ACBC) in Xenopus oocytes injected with rat brain mRNA.
ACBC has been reported to have the binding profile of an antagonist at the glycine site of the NMDA receptor. In Xenopus oocytes injected with rat brain mRNA, we have confirmed the antagonist action of ACBC on NMDA responses. ACBC and HA-966, a known glycine antagonist, blocked NMDA responses in a non-competitive manner and blocked the potentiation of NMDA responses by glycine in a competitive manner. We conclude that ACBC blocks NMDA responses via a competitive interaction at the glycine modulatory site.
Watson
G B
GB
CNS Diseases Research, G.D. Searle and Company, St. Louis, MO 63198.
Bolanowski
M A
MA
Baganoff
M P
MP
Deppeler
C L
CL
Lanthorn
T H
TH
D000596:Amino Acids / Q000494:pharmacology*; D000598:Amino Acids, Cyclic; D000818:Animals; D001667:Binding, Competitive; D001921:Brain / Q000378:metabolism*; D004357:Drug Synergism; D005260:Female; D005998:Glycine / Q000037:antagonists & inhibitors*; D009865:Oocytes / Q000187:drug effects*; D011760:Pyrrolidinones / Q000494:pharmacology; D012333:RNA, Messenger / Q000302:isolation & purification / Q000494:pharmacology*; D051381:Rats; D016194:Receptors, N-Methyl-D-Aspartate; D017981:Receptors, Neurotransmitter / Q000378:metabolism*; D014982:Xenopus laevis
D000596:Amino Acids; D000598:Amino Acids, Cyclic; D011760:Pyrrolidinones; D012333:RNA, Messenger; D016194:Receptors, N-Methyl-D-Aspartate; D017981:Receptors, Neurotransmitter; C016987:1-aminocyclobutanecarboxylic acid; C001369:1-hydroxy-3-amino-2-pyrrolidone; D005998:Glycine