Selective and extremely long inhibition of prolactin release in man by 1-ethyl-3-(3'-dimethylaminopropyl)-3-(6'-allylergoline-8'-β-carbonyl)-urea-d iphosphate (FCE 21336)

A. E. Pontiroli, G. C. Viberti, R. Mangili, L. Cammelli, A. Dubini

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Abstract

1 The effects on anterior pituitary function of FCE 21336 (1-ethyl-3-(3'-dimethylaminopropyl)-3-(6'-allylergoline-8'-β-carbonyl)-urea- diphosphate), a synthetic ergoline derivative with selective dopamine agonistic properties, were studied. 2 Circulating PRL, GH, TSH, cortisol and LH levels were determined up to 96 h after single oral doses of 50, 100, 200 and 300 μg of the compound to eight healthy males, and up to 168 h after single oral doses of 400 and 600 μg to six healthy males, according to double-blind, within subjects, experimental designs vs placebo. Vital signs, ECG, laboratory tests and the appearance of newly observed signs and symptoms were monitored. 3 A dose-related decrease of serum PRL in comparison with both basal and post-placebo levels was observed after 200 μg and greater doses of the compound, with inhibition of spontaneous circadian rhythm. Maximal inhibition (PRL <2 ng ml-1) was observed in one out of five subjects after 200, three out of seven subjects after 300, four out of six after 400 and five out of six and two out of six subjects after 600 μg. The effect was of rapid onset and long duration; the maximum or nearly maximum decrease was observed within 3 h after dosing as well as up to 96 h (200 and 300 μg) and up to 168 h (400 and 600 μg). No modifications of GH, TSH, LH and cortisol as well as of vital signs, ECG and laboratory tests were apparent. No signs or symptoms of clinical relevance were reported; nasal stuffiness and headache occurred in four out of six subjects after the highest dose, respectively. These data indicate that FCE 21336 is a long-lasting and selective inhibitor of PRL secretion in normal man.

Original languageEnglish
Pages (from-to)433-438
Number of pages6
JournalBritish Journal of Clinical Pharmacology
Volume23
Issue number4
Publication statusPublished - 1987

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ASJC Scopus subject areas

  • Pharmacology (medical)
  • Pharmacology, Toxicology and Pharmaceutics(all)

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