6-Piperazino morphanthridine hydrogen maleate - prepd. from 6-chloro-morphanthridine with piperazine in xylene, and having sedative and hypnotic activity

摘要

6-Piperazinomoprhanthridine hydrogen maleate (I) is new. The cpd. is prepd. in pure crystalline form by reaction of 6-chloromorphanthridine with piperazine in xylene to give the free base, then treating the crude base in acetone with maleic acid. The salt is isolated by adding ether. Oral doses of 1.25-5 mg./kg. in the rat cause increases slow-wave sleep markedly only in the first three hrs. whereas the duration of paradoxal sleep hardly varies or increases slightly between the 2nd and 7th hrs. Perfusion of 18.7 mg./kg. i.v. does not significantly affect blood pressure. It does not induce sec. extra-pyramidal effects or neurological effects after 64 mg./kg. orally. The oral LD50 is 1000 mg./kg.