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Stolzki B, Kaiser HO, Mehl EL.
“Heterogeneity of LSD Displacing Factors and Multiple Types of High Affinity LSD-Binding Sites”.
Life Sci.. 1978;23(6):593-97.
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Abstract
The specificity of association of LSD-displacing factors was studied in the rat. Methods Adult Sprague-Dawley rats were decapitated and organs homogenized in distilled water. After centrifugation the extracts were deproteinized and fractionated on Sephadex G-10. LSD-displacing capacity was determined in a microsomal P3 fraction from porcine cerebral cortex using 3H-LSD. In studies with LSD and its 2-bromo derivatives at least 2 types of high affinity LSD-binding sites were indicated. Apamin (Serve) blocked less than 100f the high affinity LSD binding sites with an IC50 value of 1 nM while the rest of the sites were blocked with an IC50, value of 100 mcM. Similar results were obtained after s.c. injection of apamin (3 mcg/kg) in mice. Extracts of whole rat cerebrum contained 5 LSD-displacing fractions, the E fraction in the void volume (fraction 25), the alpha- and beta-fractions (in fractions 32-38), the sigma-fraction (fraction 61) and the gamma-fraction (fraction 7890). Authentic 3H-dopamine co-eluted with the sigma-fraction and authentic 3H-serotonin and 14C-tryptamine co-eluted with the gammafraction. In extracts of the large intestine all LSD-displcing fractions isographic with the cerebral fractions were detected except the sigma-fraction while spleen and cerebellum extracts contained only the E and alpha-fractions. The crude beta-fraction fro bovine brain was found to inhibit high and medium affinity dopamine binding and medium affinity serotonin binding but did not affect high affinity binding of serotonin or spiroperidol (Janssen).
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