Benzofuranyl-tetrahydropyridines and -piperidines, their acid addition salts and antidepressant preparations thereof

Abstract

Abstract The present invention provides new benzofuranyl-tetrahydropyridines and -piperidines of the general formula I ##STR1## in which R 1 and R 2 independently of one another are hydrogen or lower alkyl or together are lower alkylene, R 3 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, cyclo-lower alkyl or cyclo-lower alkyl-lower alkyl and Y 1 and Y 2 are each hydrogen or together are an additional bond, and the ring A is not further substituted or is further substituted by lower alkyl, lower alkoxy, halogen with an atomic number not more than 35, cyano or hydroxyl and the pharmaceutically acceptable acid addition salts thereof, and antidepressant preparations containing these compounds. The compounds according to the invention have valuable pharmacological properties. In particular, they inhibit the absorption of serotonin by mesencephalic synaptosomes, the serotonin depletion induced in the brain of rats by H 75/12, the absorption of noradrenalin by mesencephalic synaptosomes in rats and the noradrenalin depletion induced in the brain of rats by H 77/77. In the same dosage they also effect inhibition of monoamino-oxidase in the brain of rats and in the liver of rats. Furthermore, they intensify the "head twitch" induced by 5-hydroxy-tryptophan, and are distinguished by good tolerance. The compounds of the general formula I and their pharmaceutically acceptable acid addition salts can therefore be used as psychopharmaceuticals and in particular as antidepressants.

Inventors

• 👤 Romeo Paioni
• 👤 Walter Schilling
• 👤 Raymond Bernasconi

Bibliographic Details