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The regional distribution of radioactive ligand binding in rat brain for the different receptors of the gamma-aminobutyric acidA (GABAA)-benzodiazepine receptor/chloride channel complex was measured on tissue sections by autoradiography. Seven ligands were employed including [3H]muscimol for high-affinity GABA agonist sites; [3H]bicuculline methochloride(More)
Felbamate (2-phenyl-1,3-propanediol dicarbamate) is a novel agent effective against maximal electroshock, pentylenetetrazol and other chemically induced seizures in mice and rats. Felbamate has been proposed as a novel anticonvulsant for the treatment of generalized tonic-clonic and complex partial seizures. In addition, felbamate has been shown to have(More)
Conantokin G (Con G) is a 17-amino-acid peptide antagonist of N-methyl-D-aspartate (NMDA) receptors isolated from the venom of the marine cone snail, Conus geographus. The mechanism of action of Con G has not been well defined; both competitive and noncompetitive interactions with the NMDA-binding site have been proposed. In this study the mechanism of(More)
The distribution of dopamine D-1 receptors has been determined in the rat brain by a quantitative in vitro light-microscopic autoradiographic method. The binding of [N-methyl-3H]-SCH 23390 to slide-mounted tissue sections takes place with characteristics expected of a substance that recognizes D-1 receptors. The binding is saturable, has high affinity, and(More)
Chronic treatment of gerbils with 1-aminocyclopropanecarboxylic acid (a high affinity, partial agonist at strychnine-insensitive glycine receptors) resulted in a 3-fold increase in survival, a significant improvement in neurological status, and an extensive protection of vulnerable brain regions following severe forebrain ischaemia. A bolus of(More)
The anticonvulsant compound felbamate (2-phenyl-1,3-propanediol dicarbamate; FBM) appears to inhibit the function of the N-methyl-D-aspartate (NMDA) receptor complex through an interaction with the strychnine-insensitive glycine recognition site. Since we have demonstrated previously that FBM inhibits the binding of [3H]5, 7-dichlorokynurenic acid (DCKA), a(More)
The dicarbamate felbamate has been shown to be capable of competing for the binding of 5,7-[3H]dichlorokynurenic acid ([3H]DCKA) to strychnine-insensitive glycine receptors in sections of human postmortem brain. The IC50 for this interaction was 305.8 microM and the inhibition was complete at 1 mM. Autoradiographic localization of [3H]DCKA binding revealed(More)
Alpha-Conotoxins, peptides produced by predatory species of Conus marine snails, are potent antagonists of nicotinic acetylcholine receptors (nAChRs), ligand-gated ion channels involved in synaptic transmission. We determined the NMR solution structure of the smallest known alpha-conotoxin, ImI, a 12 amino acid peptide that binds specifically to neuronal(More)
Subunit non-selective N-methyl-D-aspartate (NMDA) receptor antagonists reduce injury-induced pain behavior, but generally produce unacceptable side effects. In this study, we examined the antinociceptive and motor effects of cone snail venom-derived peptides, conantokins G and T (conG and conT), which are selective inhibitors of the NR2B or NR2A and NR2B(More)