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Befloxatone, a novel oxazolidinone derivative, inhibited selectively and competitively monoamine oxidase (MAO)-A in human and rat brain, heart, liver and duodenum homogenates with Ki values ranging from 1.9 to 3.6 nM for MAO-A and from 270 to 900 nM for MAO-B. In vitro, befloxatone was more potent at inhibiting MAO-A activity than reference compounds(More)
The pharmacological profile of befloxatone, a reversible, selective and competitive inhibitor of monoamine oxidase-A has been investigated in rodents. In mice, befloxatone was more active at potentiating generalized tremors induced by L-5-hydroxytryptophan (ED50, 0.21 mg/kg p.o.) than phenylethylamine-induced stereotypies (ED50, 58 mg/kg p.o.), indicating a(More)
Single administration of befloxatone (0.75 mg/kg, i.p.) in the rat increased extracellular levels of DA (+300%) in striatum. In frontal cortex, befloxatone (0.75 mg/kg, i.p.) and nialamide (100 mg/kg, i.p.) increased NA by +100% but did not modify 5HT, whereas pargyline (100 mg/kg i.p.) increased extracellular NA and 5HT by 400 and 600%, respectively. At(More)
It is usually postulated that the side chain attached to 17 beta position on the steroid nucleus of the cardioactive glycosides is a major determinant of their pharmacological activity. A new aminosteroid (LND 623) has been prepared. Despite the fact that the structural features quoted above are lacking, the product demonstrates a strong inotropic effect.(More)
Experimental and theoretical physico-chemical methods were used to investigate the interaction between aryl-oxazolidinones and monoamine oxidase (MAO). Several arguments suggest that these compounds interact with the flavin adenine dinucleotide (FAD) cofactor of MAO. The calculation using ab initio molecular orbital methods of the electronic properties of(More)
In vitro and ex-vivo studies show that befloxatone, a new oxazolidinone derivative, is a potent, reversible, competitive and specific MAO-A inhibitor (KiA from 1.9 to 3.6 nM and KiB/KiA ratio between 100 and 400, in the Rat and in Man, depending on the tissue). Befloxatone possesses a marked activity in antidepressant-sensitive behavioral models in rats(More)