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Freedman DX.
“LSD, Psychotogenic Procedures, and Brain Neurohumors”.
Psychopharmacol.Bull.. 1979;15(3):62.
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Abstract
Effect of hallucinogens on brain amines was studied. Methods Rats, mice, cats, rabbits, and monkeys were used. Drugs were given to the subjects; and radioactive serotonin, norepinephrine, dopamine, their precursors and metabolites, and radioactive drugs themselves were injected as tracers. Drug pretreatments, midbrain or hypothalamic lesions, and raphe stimulation were used to probe the LSD-serotonin interaction and amine-behavior interrelationships. Synaptic vesicles can actively accumulate (3H)-serotonin in the presence of Mg++ and ATP. Varying degrees of serotonin uptake inhibition by vesicular preparations were obtained with psychotomimetics (LSD, mescaline, bufotenine, dimethyltryptamine (DMT), psilocybin), antidepressants (chlorimipramine, desipramine), and amphetamine. None of these showed any inhibitory effect in the absence of ATP. Rat brain aryl acylamidase (AAA) activity was inhibited by low concentrations of serotonin and d-LSD, but not by l-LSD. Manipulation of pH values can selectively differentiate and separate at least 2 forms of AAA. The 2 forms, AAA-1 and AAA-Z, showed optimal enzyme activity at pH 7.5 and 5.0, respectively. D-LSD inhibited the activity of both AAA-1 and AAA-2 to a similar extent, but 2 Br-LSD inhibited AAA-1 to a greater extent than AAA-2. Serotonin, bufotenine, tryptamine, 5 MeO-tryptamine, and DMT slightly inhibited both AAA-1 and AAA-Z. d-Amphetamine, mescaline, dopamine, norepinephrine, histamine, and cAMP only moderately inhibited AAA-Z but did not affect AAA-1. Both AAA-1 and AAA-Z might be related to seroto nergic action mechanisms, while AAA-Z (but not AAA-1) might also be related to adrenergic and dopaminergic systems. Tetra hydro-beta-carboline (TH-beta-C) markedly inhibited AAA-1 but only slightly inhibited AAA-Z. 6-MeO-harmalan and 6-MeO harman markedly stimulated AAA-1 and moderately enhanced AAA-2. Pargyline did not affect either AAA-1 or AAA-2. 6 Methoxy-l,Z,3,4-TH-beta-C increased serotonin in the brain. Conclusions Assuming that AAA compounds also act on melatonin or N acetyl-serotonin in viva, stimulation of this enzyme by harmaline, 6-MeO-harmalan, and 6-MeO-harman may explain why the serotonin concentrations were increased after injection of the drug. Whether or not harmaline and the beta-carboline derivatives would stimulate AAA-1 and AAA-Z activity in vivo remains to be determined.
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