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Antero Kallio, Markku Koulu, Harry Scheinin, Jorma Viikari and Mika Scheinin

Abstract. Single iv doses (25, 50 and 100 μg) of medetomidine, a selective α2-adrenoceptor agonist of the imidazole type, were administered to 8 healthy male volunteers in a randomized, double-blind, placebocontrolled study. The concentration of hGH in plasma was powerfully and dose-dependently increased. The plasma level of cortisol was dose-dependently decreased, whereas TSH showed a slight but statistically significant increase. Plasma levels of PRL, FSH and LH were unaffected by the drug. Medetomidine appears to resemble other α2-adrenoceptor agonists, notably clonidine, in its endocrine effects. Its high selectivity and short duration of action make it a suitable tool for studies of the physiology and pharmacology of α2-adrenoceptors in man.