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Kang S, Stzelczyk M, Johnson CL, Green JP.
“LSD Binding To Subcellular Fractions Of Rat Brain And Inhibitory Effects Of Ring-substituted Tryptamines”.
Fed. Proc.. 1976;35(3):241.
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Abstract
LSD binds stereospecifically and saturably to the sub cellular fractions of the rat brain homogenates with KD=77.0 nanoM. Among fractions the microsoma7 P3 fraction shows maximum specific binding(7.3 picomoles/mg protein) as well as the highest ratio of specific to nonspecific binding(3.7). Treatments of P3 fraction with the membrane destabilizing agents such as EGTA and phospholipase C, freeze-thawing, and vigorous polytronization markedly increase not only the maximum binding(2.3 picomoles/mg protein for the freeze-thawed P3 fraction), but also the ratio of specific binding to non-specific binding(7.6 for the freeze-thawed P3 fraction). Proteolytic enzymes and solubilizing agents such as TX700 and deoxycholate diminish the LSD binding. The IC50 of serotonin varies with degree of fractionations: with P2 fraction the value is 3.6 micron with P3 fraction 2.3 microM; with freeze-thawed P3 fraction 1.05 microM. The inhibitory effects of the ring-substituted tryptamines normalized to serotonin have the following order: 5-OH, 5-MeO, 4-OH, H, 5-Me, 5,6 di-OH, 5-F, 7-Me, 4-NH2, 7-OH, 7 MeO, 5,7-di-OH, 6,7-di-OH, 5,6-di-MeO.
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| Notes # : Abstr. 195 |
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