Phencyclidine analogues inhibit NMDA-stimulated [3H]GABA release from cultured cortex neurons.
The inhibition of [3H]TCP binding to rat cortical membranes by substances of the PCP/sigma-opiate type was compared with effects of the same compounds on N-methyl-D-aspartate (NMDA) responses in cultured mouse cortex neurons. A new technique of excitatory amino acid-induced [3H]GABA (gamma-amino-butyric acid) release in a continuous superfusion model was used for the purpose. A similar rank order of potencies was found for the substances whether as inhibitors of [3H]TCP binding (MK 801 greater than PCP greater than ketamine-cyclazocine) or as antagonists of NMDA (20 microM)-stimulated [3H]GABA release in the cultured neurons (phencyclidine = MK 801 greater than ketamine greater than cyclazocine).
Drejer
J
J
Ferrosan Research Division, Sydmarken 5, Soeborg, Denmark.
Honoré
T
T
D000818:Animals; D001224:Aspartic Acid / Q000031:analogs & derivatives* / Q000037:antagonists & inhibitors; D001667:Binding, Competitive / Q000187:drug effects; D002540:Cerebral Cortex / Q000187:drug effects / Q000378:metabolism*; D066298:In Vitro Techniques; D016202:N-Methylaspartate; D009474:Neurons / Q000187:drug effects / Q000378:metabolism*; D010622:Phencyclidine / Q000031:analogs & derivatives / Q000494:pharmacology*; D051381:Rats; D005680:gamma-Aminobutyric Acid / Q000378:metabolism*
D001224:Aspartic Acid; D005680:gamma-Aminobutyric Acid; D016202:N-Methylaspartate; C012058:tenocyclidine; D010622:Phencyclidine