The authors described an experimental approach, specially using oral administration, of drugs used in cerebral metabolic insufficiencies and its application to l-eburnamonine (l-EB). Administered orally, l-EB: (1) significantly increased the cerebral consumption of [14C]-deoxyglucose in normoxic mice; (2) decreased the fall in cerebral energy charge (ECP) of rats after an acute normobaric hypoxia, and (3) stimulated the glycolysis of red blood cells (RBC) in healthy volunteers (repeated administrations) as demonstrated by important increases in 2,3-DPG and ATP, i.e., in factors involved in the bioavailability of oxygen (oxygen transport activity and RBC deformability). The results therefore demonstrate oral activity of l-EB in animals and man. They are in agreement with previous data showing cerebral metabolic stimulant and antihypoxic effects following parenteral administration, in animals. They allow to propose that l-EB acts both at cerebral and extracerebral levels and constitute objective biochemical proof of the activity of l-EB in man. The study of new drugs may be done using the same experimental approach.
l-Eburnamonine - 16-oxoeburnane – assumes experimental cerebral ''oxygenator'' and antihypoxic properties which appear more pronounced than those of vincamine. In anesthetized dogs, l-eburnamonine increases the cerebral oxygen supply and the cerebral oxygen consumption, without cerebral vasodilation; l-eburnamonine improves the cerebral capillary circulation, as observed on the rheoencephalogram. l-Eburnamonine inhibits the effects of hypobaric hypoxia in mice (increase of survival time) and in rats (inhibition of amnesic effects of hypoxia). l-Eburnamonine decreases the electroencephalographic consequences of the acute and iterative asphyxic anoxia in curarized rats and, by means of the protection of the cerebral cortex, inhibits the postischemic increase of thalamic somesthetic evoked potentials in curarized cats. Further studies are necessary to precise the mechanisms involved in these ''cerebral protective'' properties of l-eburnamonine.
Tetralone, z.B. (Ia)‐(Ic), werden durch Beckmann‐Umlagerung der Oxime mit Hilfe von Polyphosphorsäure (PPS), das Tetralon (Id) nach Schmidt mit NaN3 in IRC die Benzazepine (IIa)‐(IIc) bzw. (IId) übergeführt.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.