Identification and initial characterization of high-affinity [3H]dextrorphan binding sites in rat brain.
We have identified specific high-affinity [3H]dextrorphan binding sites in rat forebrain. [3H]Dextrorphan binds saturably and reversibly to an apparently homogenous class of sites characterized by a Bmax of 2.62 +/- 0.06 pmol/mg protein and KD of 60 +/- 4 nM. Glycine and glutamate independently increase [3H]dextrorphan binding in a concentration-dependent manner. The pharmacological profiles of [3H]dextrorphan binding characterized by equilibrium competition experiments together with these data suggest that [3H]dextrorphan labels a site at or near the N-methyl-D-aspartate receptor.
Franklin
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PH
College of Pharmacy, Oregon State University, Corvallis 97331.
Murray
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D000818:Animals; D001665:Binding Sites; D001667:Binding, Competitive; D001921:Brain / Q000648:ultrastructure*; D003917:Dextrorphan / Q000378:metabolism*; D005971:Glutamates / Q000494:pharmacology; D005998:Glycine / Q000494:pharmacology; D007700:Kinetics; D008297:Male; D008566:Membranes / Q000378:metabolism; D051381:Rats; D011919:Rats, Inbred Strains; D013268:Stimulation, Chemical; D014316:Tritium
D005971:Glutamates; D003917:Dextrorphan; D014316:Tritium; D005998:Glycine