Abstract
The specific binding of 3H-serotonin to calf caudate homogenate was studied. The dissociation constant was 2 nM and the number of specific sites was 14 fmoles/mg protein. Of many drugs tested, inhibition of specific 3H-serotonin binding occurred almost exclusively with serotonin agonists and antagonists. The concentrations for 50% inhibition of 3H-serotonin binding by serotonergic agonists follow: bufotenin, 6 nM; 5-methoxytryptamine, 12 nM; psilocin, 35 nM; dimethyltryptamine, 220 nM; and tryptamine, 270 nM. The concentrations for the antagonists were: LSD 9.5 nM; methysergide 16 nM and metergoline 25 nM.
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Azzaro, A. J., Smith, O. J.: The inhibitory action of ketamine HCl on [3H]5-hydroxy-tryptamine accumulation by rat brain synaptosomal-rich fractions: comparison with [3H] catecholamine and [3H] γ-aminobutyric acid uptake. Neuropharmacology 16, 349–356 (1977)
Bennett, J. P., Snyder, S. H.: Serotonin and lysergic acid diethylamide binding in rat brain membranes: relationship to postsynaptic serotonin receptors. Mol. Pharmacol. 12, 373–389 (1976)
Boggan, W. O., Meyer, J. S.: Effects of serotonergic drugs on methaqualone-induced hypothermia. Res. Commun. Chem. Path. Pharmacol. 16, 629–636 (1977)
Burks, T. F., Dafny, N.: Morphine and 5-hydroxytryptamine interactions in rat hypothalamus and pineal body. Exp. Neurol. 55, 458–468 (1977)
Carroll, P. R., Morgans, D., Gloner, W. E.: Blockade by phentolamine of the potentiation of histamine-induced vasoconstriction caused by serotonin and methysergide in the rabbit ear artery. Clin. Exp. Pharmacol. Physiol. 4, 43–48 (1977)
Fillion, G., Fillion, M.-P., Spirakis, C., Bahers, J.-M., Jacob, J.: 5-Hydroxytryptamine binding to synaptic membranes from rat brain. Life Sci. 18, 65–74 (1976)
Hong, E., Sancilio, L. F., Vargas, R., Pardo, E. G.: Similarities between the pharmacological actions of quipazine and serotonin. Eur. J. Pharmacol. 6, 274–280 (1969)
Lovell, R. A., Freedman, D. X.: Stereospecific receptor sites for d-lysergic acid diethylamide in rat brain: effects of neurotransmitters, amine antagonists and other psychotropic drugs. Mol. Pharmacol. 12, 620–630 (1976)
Marchbanks, R. M.: Inhibitory effects of lysergic acid derivatives and reserpine on 5-HT binding to nerve-ending particles. Biochem. Pharmacol. 16, 1971–1979 (1967)
Middlemiss, D. N., Blakeborough, L., Leather, S. R.: Direct evidence for an interaction of beta-adrenergic blockers with the 5-HT receptor. Nature 267, 289–290 (1977)
Neckers, L. M., Bertilsson, L., Costa, E.: The action of fenfluramine and p-chloramphetamine on serotonergic mechanisms: a comparative study in rat brain nuclei. Neurochem. Res. 1, 29–35 (1976)
Sastry, B. S. R., Phillis, J. W.: Metergoline as a selective 5-hydroxytryptamine antagonist in the cerebral cortex. Can. J. Physiol. Pharmacol. 55, 130–133 (1977)
Weinstock, M., Weiss, C., Gitter, S.: Blockade of 5-hydroxytryptamine receptors in the central nervous system by β-adrenoceptor antagonists. Neuropharmacology 16, 273–276 (1971)
Whitaker, P. M., Seeman, P.: Hallucinogen binding to dopamine/neuroleptic receptors. J. Pharm. Pharmacol. 29, 506–507 (1977)
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Whitaker, P.M., Seeman, P. High-affinity 3H-serotonin binding to caudate: Inhibition by hallucinogens and serotoninergic drugs. Psychopharmacology 59, 1–5 (1978). https://doi.org/10.1007/BF00428022
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DOI: https://doi.org/10.1007/BF00428022