Inhibition of amine uptake in the mouse heart by some new “thymoleptic” drugs

Abstract

A number of new and established thymoleptic drugs were given to mice. Their inhibitory action on the uptake of [3H]metaraminol and [3H]noradrenaline in the heart was investigated. Among the compounds tested a monomethylamino-derivative was in general 2–3 times more potent than the corresponding dimethyl-amino-derivative. The phthalan derivative 3,3-dimethyl-1-(3-methylaminopropyl)-1-phenylphthalan (Lu 3–010) was as efficient as protriptyline in all the tests performed. Changes in the substitution of the phthalan skeleton influenced the activity critically. As it is devoid of anticholinergic activity Lu 3–010 appears to be the most specific inhibitor of the amine transport mechanism of the adrenergic cell membrane found so far.