Disease relevance of BEFLOXATONE

• At the doses studied amitriptyline induced miosis but befloxatone did not modify pupil diameter [1].

Psychiatry related information on BEFLOXATONE

• CONCLUSION: Contrary to tricyclic antidepressants, whose deleterious effects are greater in elderly subjects, this study demonstrated the safety of befloxatone on cognition and psychomotor performance in elderly subjects [2].
• However, in view of previous data with panic-modulating compounds on flight behaviours in the MDTB, the present results are in line with clinical results showing that moclobemide is effective in panic disorders and suggest that befloxatone may have some efficacy in the clinical management of panic [3].
• Synthelabo is developing befloxatone, a long-acting selective and reversible monoamine oxidase A (MAO-A) inhibitor, for the treatment of depression, social phobias and panic disorders [4].

High impact information on BEFLOXATONE

• Cognitive performance in elderly subjects after a single dose of befloxatone, a new reversible selective monoamine oxidase A inhibitor [2].
• In vitro, befloxatone inhibits selectively, competitively, and reversibly MAO-A in human tissues [5].
• The inhibitory effects of harmane and befloxatone were reversed by the 5-HT1A antagonist WAY 100 635 [6].
• For quantification of myocardial binding sites (Bmax), [11C]befloxatone was first injected as a tracer dose (2.7-9.3 nmol) and 20 min later injected as a mixture of labeled and unlabeled befloxatone (labeled, 10.3-41.9 nmol; unlabeled, 407-765 nmol) [5].
• Behavioural profiles of the reversible monoamine-oxidase-A inhibitors befloxatone and moclobemide in an experimental model for screening anxiolytic and anti-panic drugs [3].

Biological context of BEFLOXATONE

• Pharmacodynamics and pharmacokinetics of two dose regimens of befloxatone, a new reversible and selective monoamine oxidase inhibitor, at steady state in healthy volunteers [7].
• The extent and the duration of the systolic blood pressure increase did not significantly differ between the placebo and the befloxatone regimens, except for a longer duration with the 20-mg twice daily regimen [8].
• Clinical pharmacology of befloxatone: a brief review [9].
• Befloxatone had an ID50/IC50 ratio four to five times higher than DHP and harmaline [10].
• In a trial of befloxatone in 12 healthy elderly volunteers, an oral dose of 10 mg was administered and psychomotor and cognitive function were assessed using objective tests such as critical flicker fusion (CFF), body sway and learning memory tasks amongst others and subjective tests such as the visual analog scale and a sleep questionnaire [4].

Anatomical context of BEFLOXATONE

• In the brain, liver and duodenum, the inhibition of MAO-A activity by befloxatone was short lasting [11].

Associations of BEFLOXATONE with other chemical compounds

• Effect of the reversible monoamine oxidase-A inhibitor befloxatone on the rat 5-hydroxytryptamine neurotransmission [12].
• Thus, whereas direct agonist activity at 5-HT1A receptors can modulate immobility in the forced swim test, this receptor subtype does not appear to play a major role in the antidepressant-like effects of fluoxetine or befloxatone under the conditions used in this study [13].
• The interaction between tyramine and befloxatone, a new selective, reversible monoamine oxidase-A (MAO-A) inhibitor, was studied in a single-blind, parallel-group study in 30 healthy male volunteers whose fasting tyramine 30 dose (Tyr30) was 400 or 600 mg [8].
• At these doses, befloxatone inhibited totally and selectively MAO-A, pargyline inhibited totally MAO-A and MAO-B [14].
• The reversible MAO-A inhibitor, befloxatone (0.3-3 mg/kg), and the irreversible MAO-A inhibitor, clorgyline (10-30 mg/kg), also reduced ethanol self-administration [15].

Gene context of BEFLOXATONE

• The inhibition of MAO-A by befloxatone was time-dependent and fully reversible after dilution [11].
• Befloxatone (0.5 mg/kg p.o.) decreased MAO-B activity by only 20% in both tissues [11].
• Effects of befloxatone, a new potent reversible MAO-A inhibitor, on cortex and striatum monoamines in freely moving rats [14].
• In rats, befloxatone increased rapid eye movement sleep latency and decreased rapid eye movement sleep duration, without rebound effects [16].

Analytical, diagnostic and therapeutic context of BEFLOXATONE

• METHODS: The effects on cognition and psychomotor performance of single oral doses of befloxatone (10 mg) and amitriptyline (50 mg) were compared in a randomized, double-blind, placebo-controlled, three-way crossover design trial in 12 healthy elderly (65 to 85 years) volunteers [2].
• Befloxatone is a new reversible and selective monoamine oxidase (MAO-A) inhibitor that has been shown to have antidepressant activity in various animal models [1].
• Befloxatone induced dose-related EEG changes which occurred rapidly, peaked between 0.5 and 2 h and lasted at least until 6 h after drug administration [17].

References