Tris inhibits (+)-[3H]SKF-10,047 binding to sigma receptors.
Tris-HCl is the most commonly used buffer in studies of radioligand binding to sigma receptors, with concentrations as high as 50 or 100 mM often used. We report here that these concentrations of Tris substantially inhibit (+)-[3H]SKF-10,047 binding to sigma receptors. The well-established inhibitory effect of Tris-HCl on ligand binding to PCP receptors did not contribute to the presently reported inhibition of (+)-[3H]SKF-10,047 binding. The IC50 of Tris, determined in the presence of 10 mM potassium phosphate buffer, was 15.4 +/- 1.2 mM (n = 3, pH 8.0, 25 degrees C, 1 nM radioligand). Equilibrium saturation studies revealed an apparent competitive inhibition of binding.
McCann
D J
DJ
Neurochemistry Unit, National Institute on Drug Abuse, Baltimore, MD 21224.
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D000818:Animals; D016291:Dizocilpine Maleate / Q000494:pharmacology; D006220:Haloperidol / Q000494:pharmacology; D008099:Liver / Q000378:metabolism; D008297:Male; D010620:Phenazocine / Q000031:analogs & derivatives* / Q000037:antagonists & inhibitors / Q000378:metabolism; D051381:Rats; D017207:Rats, Sprague-Dawley; D017480:Receptors, sigma / Q000378:metabolism*; D013237:Stereoisomerism; D014316:Tritium; D014325:Tromethamine / Q000494:pharmacology*
D017480:Receptors, sigma; D014325:Tromethamine; D014316:Tritium; D016291:Dizocilpine Maleate; C012134:SK&F 10047; D010620:Phenazocine; D006220:Haloperidol