Raubasine (ajmalicine or delta-yohimbine) anti-anoxic derivs. - used for treat cerebral vascular damage, cerebral sclerosis, cranial trauma disorders and depressive states

摘要

Raubasine (ajmalicine or delta-yohimbine) derivs. of formula (I) and their acid addn. salts are new. Cpds. are 1-R1-16,17-didehydro-19 -alpha-methyl-16 -R2-CO-oxayohimbane derivs. R1 is H, 1-4C alkoxycarbonyl, phenoxycarbonyl (where the phenyl ring is opt. substd.by halo or nitro), 1-4C acyl or 1-4C-alkoxycarbonyl-1-4C-alkyl and R2 is O-Me (where Me is an alkali or alkaline earth metal), opt. branched 2-4C alkoxy, 3-6C-cycloalkyl-1-4C-alkoxy, 3-6C-cycloalkoxy, amino, mono- or di-(1-4C alkyl)amino or 3-6C cycloalkyl-amino. (I) are anti-anoxics used to treat vigilance troubles e.g. cerebral vascular damage, cerebral sclerosis in the elderly, cranial trauma disorders and depressive states. They may be administered orally or parenterally in daily doses of 10-200 mg. I.p. LD50 in mice varies from 300-1000 mg/kg and in hypobaric anoxia tests on mice, the mean active dose which increases survival time by 100% was 10-60 mg/kg i.p..