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. 1983 Nov;16(5):471–475. doi: 10.1111/j.1365-2125.1983.tb02202.x

Prolactin secretion in man: a useful tool to evaluate the activity of drugs on central 5-hydroxytryptaminergic neurones. Studies with fenfluramine.

A Quattrone, G Tedeschi, U Aguglia, F Scopacasa, G F Direnzo, L Annunziato
PMCID: PMC1428066  PMID: 6639832

Abstract

Acute oral administration of various doses of fenfluramine, a 5-HT releaser, induced a dose-related increase of PRL secretion in nine healthy volunteers. Fenfluramine reached the maximum effect on PRL secretion at 4 h after its administration. This effect was already significant at 2 h and lasted till 8 h. Metergoline, a 5-HT receptor blocker, when administered alone, decreased serum PRL levels in six healthy subjects. The pretreatment with this drug significantly antagonized the PRL-releasing action of fenfluramine (60 mg) suggesting that the effect of fenfluramine on PRL release may be mediated through a 5-HT mechanism in the brain. These findings suggest the possibility that serum PRL levels in humans may represent a useful tool to evaluate, in vivo, the activity of drugs possessing putative 5-hydroxytryptaminergic properties.

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Selected References

These references are in PubMed. This may not be the complete list of references from this article.

  1. Beck-Peccoz P., Ferrari C., Rondena M., Paracchi A., Faglia G. Failure of oral 5-hydroxytryptohan administration to affect prolactin secretion in man. Horm Res. 1976;7(4-5):303–307. doi: 10.1159/000178741. [DOI] [PubMed] [Google Scholar]
  2. Crosignani P. G., Lombroso G. C., Caccamo A., Reschini E., Peracchi M. Suppression of puerperal lactation by metergoline. Obstet Gynecol. 1978 Jan;51(1):113–115. [PubMed] [Google Scholar]
  3. Ferrari C., Caldara R., Rampini P., Telloli P., Romussi M., Bertazzoni A., Polloni G., Mattei A., Crosignani P. G. Inhibition of prolactin release by serotonin antagonists in hyperprolactinemic subjects. Metabolism. 1978 Oct;27(10):1499–1504. doi: 10.1016/s0026-0495(78)80022-5. [DOI] [PubMed] [Google Scholar]
  4. Ferrari C., Paracchi A., Rondena M., Beck-Peccoz P., Faglia G. Effect of two serotonin antagonists on prolactin and thyrotrophin secretion in man. Clin Endocrinol (Oxf) 1976 Sep;5(5):575–578. doi: 10.1111/j.1365-2265.1976.tb01987.x. [DOI] [PubMed] [Google Scholar]
  5. Fuxe K., Farnebo L. O., Hamberger B., Ogren S. O. On the in vivo and in vitro actions of fenfluramine and its derivatives on central monoamine neurons, especially 5-hydroxytryptamine neurons, and their relation to the anorectic activity of fenfluramine. Postgrad Med J. 1975;51 (Suppl 1):35–45. [PubMed] [Google Scholar]
  6. Garattini S., Buczko W., Jori A., Samanin R. The mechanism of action of fenfluramine. Postgrad Med J. 1975;51 (Suppl 1):27–35. [PubMed] [Google Scholar]
  7. Kato Y., Nakai Y., Imura H., Chihara K., Ogo S. Effect of 5-hydroxytryptophan (5-HTP) on plasma prolactin levels in man. J Clin Endocrinol Metab. 1974 Apr;38(4):695–697. doi: 10.1210/jcem-38-4-695. [DOI] [PubMed] [Google Scholar]
  8. Langer G., Sachar E. J., Gruen P. H., Halpern F. S. Human prolactin responses to neuroleptic drugs correlate with antischizophrenic potency. Nature. 1977 Apr 14;266(5603):639–640. doi: 10.1038/266639a0. [DOI] [PubMed] [Google Scholar]
  9. Lu K. H., Meites J. Effects of serotonin precursors and melatonin on serum prolactin release in rats. Endocrinology. 1973 Jul;93(1):152–155. doi: 10.1210/endo-93-1-152. [DOI] [PubMed] [Google Scholar]
  10. Mawson C., Whittington H. Evaluation of the peripheral and central antagonistic activities against 5-hydroxytryptamine of some new agents. Br J Pharmacol. 1970 May;39(1):223P–224P. [PMC free article] [PubMed] [Google Scholar]
  11. Parati E. A., Zanardi P., Cocchi D., Caraceni T., Müller E. E. Neuroendocrine effects of quipazine in man in health state or with neurological disorders. J Neural Transm. 1980;47(4):273–297. doi: 10.1007/BF01247322. [DOI] [PubMed] [Google Scholar]
  12. Quattrone A., Di Renzo G., Schettini G., Tedeschi G., Scopacasa F. Increased plasma prolactin levels induced in rats by d-fenfluramine: relation to central serotonergic stimulation. Eur J Pharmacol. 1978 May 15;49(2):163–167. doi: 10.1016/0014-2999(78)90073-0. [DOI] [PubMed] [Google Scholar]
  13. Quattrone A., Schettini G., Di Renzo G. F., Preziosi P. Pharmacological evidence of an interaction between serotonergic and dopaminergic neurons in the control of prolactin secretion in male rats. Arch Int Pharmacodyn Ther. 1979 Mar;238(1):42–49. [PubMed] [Google Scholar]
  14. Quattrone A., Schettini G., di Renzo G., Tedeschi G., Preziosi P. Effect of midbrain raphe lesion or 5,7-dihydroxytryptamine treatment on the prolactin-releasing action of quipazine and D-fenfluramine in rats. Brain Res. 1979 Sep 28;174(1):71–79. doi: 10.1016/0006-8993(79)90804-7. [DOI] [PubMed] [Google Scholar]
  15. Samanin R., Bernasconi S., Quattrone A. Antinociceptive action of quipazine: relation to central serotonergic receptor stimulation. Psychopharmacologia. 1976 Mar 16;46(2):219–222. doi: 10.1007/BF00421395. [DOI] [PubMed] [Google Scholar]
  16. Shaar C. J., Clemens J. A. The role of catecholamines in the release of anterior pituitary prolactin in vitro. Endocrinology. 1974 Nov;95(5):1202–1212. doi: 10.1210/endo-95-5-1202. [DOI] [PubMed] [Google Scholar]
  17. Sinha Y. N., Selby F. W., Lewis U. J., VanderLaan W. P. A homologous radioimmunoassay for human prolactin. J Clin Endocrinol Metab. 1973 Mar;36(3):509–516. doi: 10.1210/jcem-36-3-509. [DOI] [PubMed] [Google Scholar]
  18. Smalstig E. B., Sawyer B. D., Clemens J. A. Inhibition of rat prolactin release by apomorphine in vivo and in vitro. Endocrinology. 1974 Jul;95(1):123–129. doi: 10.1210/endo-95-1-123. [DOI] [PubMed] [Google Scholar]
  19. Wiebe R. H., Handwerger S., Hammond C. B. Failure of L-tryptophan to stimulate prolactin secretion in man. J Clin Endocrinol Metab. 1977 Dec;45(6):1310–1312. doi: 10.1210/jcem-45-6-1310. [DOI] [PubMed] [Google Scholar]
  20. Woolf P. D., Lee L. Effect of the serotonin precursor, tryptophan, on pituitary hormone secretion. J Clin Endocrinol Metab. 1977 Jul;45(1):123–133. doi: 10.1210/jcem-45-1-123. [DOI] [PubMed] [Google Scholar]
  21. Wuttke W., Björklund A., Baumgarten H. G., Lachenmayer L., Fenske M., Klemm H. P. De- and regeneration of brain serotonin neurons following 5,7-dihydroxytryptamine treatment: effects on serum LH, FSH and prolactin levels in male rats. Brain Res. 1977 Oct 7;134(2):317–331. doi: 10.1016/0006-8993(77)91076-9. [DOI] [PubMed] [Google Scholar]

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