Erowid References Database
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Dolphin A, Enjalbert A, Tassin JP, Lucas M, Bockaert J.
“Direct Interaction of LSD with Central "Beta"-Adrenergic Receptors”.
Life Sci.. 1978;22(4):345-51.
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Abstract
The interaction of LSD and serotonin agonists and antagonists with central p-adrenergic receptors was investigated Binding of H-dihydroalprenolol (38-DA) and activity of isoproterenol-sensitive adenylate cyclase were measured in rat cerebral cortex homogenates and C6 glioma cell cultures after incubation with the test substances. The following drugs were tested: LSD, 2-bromo-lysergic acid diethylamide (BOL), methysergide (all Sandoz), alprenolol, phentolamine (both CIBA Geigy), isoproterenol (Sigma-Chem.), dopamine (Calbiochem), methergoline (Farmitalia), methiothepin Roche), 5-methoxy-N,N-dimethyltryptamine, bufotenine (Aegis), fluphenazine (Squibb), sulpiride (Delagrange-), mescaline and serotonin (both Merck-USA). LSD competitively inhibited 311-DA binding with an apparent inhibition constant of 10-7M in cerebral cortex and 10-6M in -C6 glioma cells. LSD completely displaced 3H-DA binding in rat cortex with a dissociation constant of 1.9 x 10-7 M as compared to 1.4 x 10-8M for alprenolol and 5.6 x 10-8M for isoproterenol. BOL, had the same affinity as LSD for a-adrenergic receptors. The other dopamine and serotonin agonists and antagonists had no effect when tested at 10-6 M. The stimulation of adenylate cyclase by isoproterenol was inhibited by LSD with an apparent inhibition constant of l .6 x 10-7M in cerebral cortex homogenates and 5 x 10-6M in the C6 glioma cell system. The central beta-adrenergic receptors are 1 of the multiple sites of action of LSD.
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