Abstract
The hallucinogenic indoleamine drugs N,N-dimethyltryptamine (N,N-DMT), psilocybin, bufotenin, 5-methoxy-N,N-dimethyltryptamine, and N-methyltryptamine, increased rat plasma prolactin (PRL) levels. The increase in plasma PRL produced by N,N-DMT, psilocybin, and bufotenin was inhibited by methysergide, a serotonin receptor blocker. Parachlorophenylalanine (PCPA), an inhibitor of serotonin synthesis, significantly potentiated the increase in PRL produced by N,N-DMT, and psilocybin. Parachloroamphetamine, a relatively selective toxin for serotonin neurons, also stimulated the increase in PRL produced by N,N-DMT. These results suggest that the indole hallucinogens stimulate PRL secretion by a serotonergic agonist mechanism. Bufotenin has been reported to pass the blood-brain barrier poorly, but of the indoles studied it had the most potent effect on PRL secretion. This raises the possibility that the serotonin receptors which promote PRL secretion may be outside the blood-brain barrier or that the central 5-HT receptors which mediate PRL secretion may be especially responsive to bufotenin.
This is a preview of subscription content, log in via an institution to check access.
Similar content being viewed by others
References
Advis, I. P., Simpkins, J. W., Bennett, J., Meites, J.: Serotonergic control of prolactin release in male rats. Endocr. Soc. Abs., p. 254. 59th Annual Meeting, Chicago, Illinois, June, 1977
Andén, N.-E., Corrodi, H., Fuxe, K.: Hallucinogenic drugs of the indolealkylamine type and central monoamine neurons. J. Pharmacol. Exp. Ther. 179, 236–249 (1971)
Chen, H. T., Simpkins, J. W., Mueller, G. P., Meites, J.: Effect of pargyline on hypothalamic biogenic amines and serum prolactin, LH and TSH in male rats. Life Sci. 21, 533–542 (1977)
Creese, I., Burt, D., Snyder, S.: The dopamine receptor: differential binding of d-LSD and related agents to agonist and antagonist states. Life Sci. 17, 1715–1720 (1975)
Domino, E. F.: Search for new treatment approaches in schizophrenia: in vitro studies of potential N-Methyltransferase inhibitors. Arch. int. Pharmacodyn. Ther. 221, 75–86 (1976)
Fabing, H. D., Hawkins, J. R.: Intravenous bufotenine injection in the human being. Science 123, 886–887 (1956)
Gil-Ad, I., Zambotti, F., Carruba, M. O., Vicentini, L., Muller, E. E.: Stimulatory role for brain serotonergic system on prolactin secretion in the male rat. Proc. Soc. Exp. Biol. Med. 151, 512–518 (1976)
Gyermek, L.: 5-Hydroxytryptamine antagonists. Pharmacol. Rev. 13, 399–439 (1961)
Harvey, J. A., McMaster, S. e., Yunger, L. M.: p-Chloroamphetamine: selective neurotoxic agent in brain. Science 187, 841–843 (1975)
Kamberi, I. A., Mical, R. S., Porter, J. C.: Effect of melatonin and serotonin on the release of FSH and prolactin. Endocrinology 88, 1288–1293 (1971)
Koe, B. K., Weissman, A.: Parachlorophenylalanine: a special depletor of brain serotonin. J. Pharmacol. Exp. Ther. 354, 499–576 (1966)
Kordon, C., Blake, C. A., Terkel, J., Sawyer, C. H.: Participation of serotonin-containing neurons in the suckling-induced rise in plasma prolactin levels in lactating rats. Neuroendocrinology 13, 213–223 (1973–74)
Lawson, D. M., Gala, R. R.: The influence of surgery, time of day, blood volume reduction, and anesthetics on plasma prolactin in ovariectomized rats. J. Endocrinol. 62, 75–83 (1974)
Lawson, D. M., Gala, R. R.: The influence of adrenergic, dopaminergic, cholinergic and serotonergic drugs on plasma prolactin levels in ovariectomized, estrogen-treated rats. Endocrinology 96, 313–318 (1975a)
Lawson, D. M., Gala, R. R.: The influence of anaesthetics on basal perphenazine-induced and thyrotropin releasing hormone-induced prolactin secretion in ovariectomized, oestrogen-treated rats. J. Endocrinol 66, 151–157 (1975b)
Lu, K.-H., Meites, J.: Inhibition by l-Dopa and monoamine oxidase inhibitors of pituitary prolactin release; stimulation by methyldopa and d-amphetamine. Proc. Soc. Exp. Biol. Med. 137, 480–483 (1971)
Lu, K.-H., Meites, J.: Effects of serotonin precursors and melatonin on serum prolactin relase in rats. Endocrinology 93, 152–155 (1973)
Malitz, S., Esecover, H., Wilkens, B., Hoch, P. H.: Some observations on psilocybin, a new hallucinogen, in volunteer subjects. Comp. Psychiatry 1, 8–16 (1960)
Meltzer, H. Y., Daniels, S., Fang, V. S.: Clozapine increases rat serum prolactin levels. Life Sci. 17, 339–342 (1975)
Meltzer, H. Y., Fang, V. S.: Effect of apomorphine plus 5-hydroxytryptophan on plasma prolactin levels in male rats. Psychopharmacol. Commun. 2, 189–198 (1976)
Meltzer, D. Y., Fang, V. S., Paul, S. M., Kaluskar, R.: Effect of quipazine on rat plasma prolactin levels. Life Sci. 19, 1073–1078 (1976)
Meltzer, H. Y., Fessler, R. G., Simonovic, M., Fang, V. S.: Effect of indole hallucinogens, mescaline and DMPEA on rat plasma prolactin. Fed. Proc. 36, 984 (1977)
Meltzer, H. Y., Fessler, R. G., Simonovic, M., Fang, V. S.: Lysergic acid diethylamide: evidence for stimulation of pituitary dopamine receptors. Psychopharmacology 54, 39–44 (1977)
Ohgo, S., Kato, Y., Chihara, K., Imura, H., Maeda, K.: Effect of hypothalamic surgery on prolactin release induced by 5-hydroxytryptophan (5-HT) in rats. Endocrinol. Jpn. 23, 458–491 (1976)
Porter, J. C., Mical, R. S., Cramer, O. M.: Effect of serotonin and other indoles on the release of LH, FSH, and prolactin. Horm. Antag. Gynecol. Invest. 2, 13–22 (1971–1972)
Sanders, E., Bush, M. T.: Distribution, metabolism and excretion of bufotenine in the rat with preliminary studies of its O-methyl derivative. J. Pharmacol. Exp. Ther. 157, 340–352 (1967)
Siegel, S.: Nonparametric statistics for the behavioral sciences, pp. 111–116. New York: McGraw-Hill 1956
Talwalker, P. K., Ratner, A., Meites, J.: In vitro inhibition of pituitary prolactin synthesis and release by hypothalamic extracts. Am. J. Physiol. 205, 213–218 (1963)
Trulson, M. E., Eubanks, E. E., Jacobs, B. L.: Behavioral evidence for supersensitivity following destruction of central serotonergic nerve terminals by 5,7-dihydroxytryptamine. J. Pharmacol. Exp. Ther. 198, 23–32 (1976)
Turner, W. J., Merlis, S.: Effect of some indolealkylamines on man. Arch. Neurol. Psychiatry (Chicago) 81, 121–129 (1959)
Udenfriend, S., Witkop, B., Redfield, B. G., Weissbach, H.: Studies with reversible inhibitors of monoamine oxidase: harmaline and related compounds. Biochem. Pharmacol. 1, 160–167 (1958)
Vogel, W. H.: Physiological disposition of 5-methoxytryptamine and the rope climbing performance of rats. Psychopharmacologia (Berl.) 15, 88–95 (1969)
Author information
Authors and Affiliations
Rights and permissions
About this article
Cite this article
Meltzer, H.Y., Fessler, R.G., Simonovic, M. et al. Stimulation of rat prolactin secretion by indolealkylamine hallucinogens. Psychopharmacology 56, 255–259 (1978). https://doi.org/10.1007/BF00432847
Received:
Accepted:
Issue Date:
DOI: https://doi.org/10.1007/BF00432847