PURPOSE: To provide the compound having a strong dopamine-like action and useful for the therapy of Perkinson disease, hyperprolactinemia, cerebral function insufficiency, etc.
CONSTITUTION: A compound of formula I (R is ethyl, propyl), e.g. (5R,8R,10R-6- ethyl-8-(1,2,4-triazol-1-ylmethyl)ergoline. The compound of formula I is obtained by reacting a compound of formula II (X is an acid residue such as Cl, Br, I, methanesulfonyloxy or p-toluenesufonyloxy as a releasable group) with 1,2,4- triazole in a solvent (e.g. N,N-dimethylformamide) at room temperature to 140°C. The administration dose of the compound is 1-100μg per kg of the body a day in the case of oral administration. The compound of formula I is a low toxic and highly safe medicinal substance capable of reducing emesis and nausea which are the side effects of dopamininergic medicines.
ADACHI YUUKO
TAKAMORI MASAYUKI
MIZUKOSHI SEISHI
NAGASAKA MITSUAKI
ICHIHARA KENJI
KAMEI HIROYUKI
