OBJECTIVEThe aim of the present study was to evaluate the anxiolytic properties of the new isoxazoline compounds BTG1640 and BTG1675A in comparison with diazepam.MATERIALS AND METHODSWe evaluated the ultrasonic distress emission in both sexes of neonatal rat pups (which seems to be a sensitive indicator of the rat emotional reactivity and represents a valuable tool to screen compounds with expected anxiolytic properties) and the locomotor activity in 30-day old rat pups.RESULTSWe found a significant reduction in the number of emitted ultrasonic calls only after i.p. administration of diazepam 1 mg/kg, while no significant reduction have been detected after i.p. administration of BTG 1640 and BTG 1675A. Furthermore, we found a significant reduction of locomotor activity in the first 10' of the test, only in the group treated with diazepam 0.1 mg.CONCLUSIONSThe tests validating the supposed anxiolytic properties of the new isoxazoline compounds BTG1640 and BTG1675A, in comparison with diazepam, gave negative results.

2009-01-01·Neuropsychobiology4区 · 心理学

Double-Blind, Placebo-Controlled, Multiple-Ascending-Dose Study on the Pharmacodynamics of ABIO-08/01, a New CNS Drug with Potential Anxiolytic Activity

4区 · 心理学

Article

作者: Saletu, Bernd ; Nannipieri, Fabrizio ; Saletu-Zyhlarz, Gerda M. ; Noseda, Emanuele ; Nosiska, Dorothea ; Assandri, Alessandro ; Wolzt, Michael ; Anderer, Peter

Effects of ABIO-08/01, a new potentially anxiolytic isoxazoline, on regional electrical brain generators were investigated by 3-dimensional EEG tomography. In a double- blind, placebo-controlled, multiple-ascending-dose study, 16 healthy males (30.2 ± 5.7 years) received 3 oral drug doses (10, 20, 40 mg) and placebo for 7 days (8-day wash-out) in a randomized non-balanced design for phase-1 studies. A 3-min vigilance-controlled (V) EEG, a 4-min resting (R) EEG with eyes closed, a 1-min eyes-open (EO) EEG and psychometric tests were performed 0, 1 and 6 h after taking the drug on days 1 and 5. Low-resolution brain electromagnetic tomography (LORETA) was computed from the spectrally analyzed EEG data, and differences between drug and placebo were displayed as statistical parametric maps. Data were registered to the Talairach-Tournoux Human Brain Atlas available as a digitized MRI. An overall omnibus significance test followed by a voxel-by-voxel t test demonstrated significant regional EEG changes after ABIO-08/01 versus placebo, dependent on recording condition, dose and time. While in the EO-EEG specifically the lowest dose of ABIO-08/01 induced pronounced sedative effects (delta/theta and beta increase) 1 h after acute and slightly less so after superimposed administration, in the 6th hour a decrease in alpha and beta activity signaled less sedative and more relaxant action. In the V-EEG these changes were less pronounced, in the R-EEG partly opposite. Hemisphere-specific changes were observed, suggesting increases in LORETA power over the left temporal, parietal, superior frontal regions and decreases over the right prefrontal, temporal pole and occipital regions. These LORETA changes are discussed in the light of neuroimaging findings on anxiety and anxiolytics.

2009-01-01·Neuropsychobiology4区 · 心理学

Double-Blind, Placebo-Controlled, Multiple-Ascending-Dose Study on the Pharmacodynamics of ABIO-08/01, a New CNS Drug with Potential Anxiolytic Activity

4区 · 心理学

Article

作者: Nessi, Paola ; Nannipieri, Fabrizio ; Semlitsch, Heribert V. ; Saletu-Zyhlarz, Gerda M. ; Assandri, Alessandro ; Saletu, Bernd ; Rosini, Sergio ; Wolzt, Michael ; Anderer, Peter

In a double-blind, placebo-controlled, multiple-ascending-dose study, the encephalotropic and psychotropic properties of ABIO-08/01, a new potentially anxiolytic and nootropic isoxazoline, were studied in 16 young healthy males. In a randomized nonbalanced phase 1 study, they received 3 oral drug doses (10, 20, 40 mg) and placebo for 7 days (washout period 8 days). EEG mapping and psychometry were carried out at hours 0, 1, 6 of day 1 (acute effect) and day 5 (subacute and superimposed effects). MANOVA/ Hotelling T<sup>2</sup> test demonstrated significant central effects of ABIO-08/01 versus placebo after acute, subacute and superimposed administration of all doses in the resting, vigilance-controlled and eyes-open EEG. Univariate analysis revealed activating patterns in the resting EEG (40 mg > 20 mg > 10 mg), and sedative patterns in the eyes-open EEG (10 mg > 20 mg > 40 mg). In the vigilance-controlled EEG, 40 mg of ABIO-08/01 induced activating patterns, whereas 10 mg induced sedative patterns. Concerning psychometry, ABIO-08/01 improved concentration (40 mg > 20 mg > 10 mg; activating effect) and deteriorated well-being (10 mg > 20 mg > 40 mg; sedative effect). Ten milligrams also improved reaction time performance and psychomotor activity. ABIO-08/01 is well-tolerated and is of interest in anxiety disorders.

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适应症	最高研发状态	国家/地区	公司	日期
焦虑症	临床2期	奥地利	Abiogen Pharma SpA	-
焦虑症	临床2期	-	Abiogen Pharma SpA	-
焦虑症	临床2期	-	BTG International Ltd.	-
惊恐障碍	临床2期	-	BTG International Ltd.	-
惊恐障碍	临床2期	意大利	Abiogen Pharma SpA	-