Abstract
Cis (α)-flupenthixol and (+)-butaclamol are effective anti-psychotic agents but trans (β)-flupenthixol and (-)-butaclamol are not. α-Flupenthixol was found to be 245 times more active in elevating rat plasma prolactin than the β-isomer. The discrepancy between (+)-butaclamol and (-)-butaclamol was even greater. These results support the hypothesis that the dopamine receptors that mediate the effects of dopamine on prolactin secretion are similar to those that mediate the anti-psychotic effect of neuroleptic drugs.
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Boulin, D. J., Grimes, R. P. J., Orr, M. W.: The action of flupenthixol upon 5-hydroxytryptamine-induced aggregation and the uptake of 5-hydroxytryptamine and dopamine by human blood platelets. Brit. J. Pharmacol. 55, 555–557 (1975)
Burt, D. R., Enna, S. J., Creese, I., Snyder, S. H.: Dopamine receptor binding in the corpus striatum of mammalian brain. Proc. nat. Acad. Sci. (Wash.) 72, 4655–4659 (1975)
Christenson, A. V., Møller-Nielsen, I.: Influence of flupenthixol and flupenthixol decanoate on methylphenidate and apomorphine-induced compulsive gnawing in mice. Psychopharmacologia (Berl.) 34, 119–126 (1974)
Clemens, J. A., Smalstig, E. B., Sawyer, B. D.: Antipsychotic drugs stimulate prolactin release. Psychopharmacologia (Berl.) 40, 123–127 (1974)
Creese, I., Burt, D. R., Snyder, S. H.: Dopamine receptor binding: Differentiation of agonist and antagonist states with 3H-dopamine and 3H-haloperidol. Life Sci. 17, 993–1002 (1975)
Hollister, L. E., Davis, K. L., Berger, P. A.: Butaclamol hydrochloride in newly admitted schizophrenics. Psychopharmacol. Commun. 1, 493–500 (1975)
Iversen, L.: Dopamine receptors in the brain. Science 188, 1084–1089 (1975)
Kleinberg, D. L., Noel, G. L., Frantz, A. G.: Chlorpromazine stimulation and L-dopa suppression of plasma prolactin in man. J. clin. Endocr. Metab. 33, 873–876 (1971)
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)
Lippman, W., Pugsley, T., Merker, J.: Effect of butaclamol and its enantiomers upon striatal homovanillic acid and adenyl cyclase of olfactory tubercle in rats. Life Sci. 16, 213–224 (1975)
Lu, K.-H., Amenomori, Y., Chen, C. L., Meites, J.: Effects of central acting drugs on serum and pituitary prolactin levels in rats. Endocrinology 87, 667–672 (1970)
Meilke, D. H., Gallant, D. M., Oelsner, T., Kessler, C. M., Tomlinson, W. K., Cohen, G. K.: Butaclamol HCl: An early evaluation in severely ill schizophrenics. Dis. nerv. Syst. 36, 7–8 (1975)
Meites, J., Clemens, J.: Hypothalamic control of prolactin secretion. Vitam Horm. 30, 165–221 (1972)
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.: The effect of neuroleptics on serum prolactin in schizophrenic patients. Arch. gen. Psychiat. 33, 279–286 (1976)
Meltzer, H. Y., Sachar, E. J., Frantz, A. A.: Dopamine antagonism by thioridazine in schizophrenia. Biol. Psychiat. 10, 53–57 (1975)
Miller, R. J., Horn, A. S., Iversen, L. L.: Effect of butaclamol on dopamine-sensitive adenylate cyclase in rat striatum. J. Pharm. Pharmacol. 27, 212–213 (1975)
Møller-Nielsen, J., Pedersen, V., Nymack, M., Franck, K. F., Boeck, V., Fjalland, B., Christensen, A. V.: The comparative pharmacology of flupenthixol and some reference neuroleptics. Acta pharmacol. (Kbh.) 33, 353–362 (1973)
Sachar, E.: The use of neuroendocrine techniques in psychopharmacological research. In: Hormones behavior and psychopathology, E. Sachar, ed. New York: Raven Press 1976 (in press)
Seeman, P., Lee, T.: Antipsychotic drugs: direct correlation between clinical potency and presynaptic action on dopamine neurons. Science 188, 1217–1219 (1975)
Smalstig, E. B., Sawyer, B. D., Clemens, J. A.: Inhibition of rat prolactin release by apomorphine in vivo and in vitro. Endocrinology 95, 123–129 (1974)
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Meltzer, H.Y., Paul, S.M. & Fang, V.S. Effect of flupenthixol and butaclamol isomers on prolactin secretion in rats. Psychopharmacology 51, 181–183 (1977). https://doi.org/10.1007/BF00431737
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DOI: https://doi.org/10.1007/BF00431737