Effects of befloxatone, a new potent reversible MAO-A inhibitor, on cortex and striatum monoamines in freely moving rats.
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 these doses, befloxatone inhibited totally and selectively MAO-A, pargyline inhibited totally MAO-A and MAO-B. Increases of tissue and extracellular concentrations of NA and 5HT were highest after Pargyline suggesting that both monoamines may be metabolized by MAO-A and MAO-B. Befloxatone and nialamide potentiated the effects of idazoxan (20 mg/kg, i.p.) on extracellular NA in frontal cortex, which increased from 350% to 2,000 and 1,500% respectively. These results suggest that alpha 2-adrenoceptors play a major role in the regulation of extracellular NA in frontal cortex.
Curet
O
O
Synthelabo Recherche, Rueil Malmaison, France.
Damoiseau
G
G
Labaune
J P
JP
Rovel
V
V
Jarreau
F X
FX
D000818:Animals; D015306:Biogenic Monoamines / Q000378:metabolism*; D002540:Cerebral Cortex / Q000378:metabolism*; D003342:Corpus Striatum / Q000378:metabolism*; D004298:Dopamine / Q000378:metabolism; D008297:Male; D008995:Monoamine Oxidase / Q000378:metabolism*; D008996:Monoamine Oxidase Inhibitors / Q000494:pharmacology*; D009526:Nialamide / Q000494:pharmacology; D009638:Norepinephrine / Q000378:metabolism; D010080:Oxazoles / Q000494:pharmacology*; D010293:Pargyline / Q000494:pharmacology; D051381:Rats; D017207:Rats, Sprague-Dawley; D012701:Serotonin / Q000378:metabolism
D015306:Biogenic Monoamines; D008996:Monoamine Oxidase Inhibitors; D010080:Oxazoles; D012701:Serotonin; C090014:befloxatone; D010293:Pargyline; D008995:Monoamine Oxidase; D009526:Nialamide; D004298:Dopamine; D009638:Norepinephrine