gs39783  (Tocris)

Journal: International Journal of Molecular Sciences

Article Title: Relationship between GABA-Ergic System and the Expression of Mephedrone-Induced Reward in Rats—Behavioral, Chromatographic and In Vivo Imaging Study

doi: 10.3390/ijms24129958

Figure Lengend Snippet: The impact of GS39783 on the expression of mephedrone-induced CPP ( A ) and animals’ locomotion ( B ). Data represent means ± SEM and are expressed as ( A ) the difference (in s) in time spent in the drug-paired compartment (post-conditioning–pre-conditioning) and ( B ) the distance moved by the animals (in m) during the post-conditioning test. n = 8 rats per group. * p < 0.05, ** p < 0.01; **** p < 0.0001; ns—no statistically significant difference (Tukey’s test).

Article Snippet: In the described experiments, the following compounds were utilized: mephedrone hydrochloride (Tocris Bioscience, Bristol, UK, Cat. No. 4443), baclofen (Sigma Aldrich, Burghausen, Germany, Cat. No. B5399) and GS39783 (Sigma Aldrich, Burghausen, Germany, Cat. No. G5919).

Techniques: Expressing

Journal: Pharmaceuticals

Article Title: Anxiolytic-like Effects of the Positive GABA B Receptor Modulator GS39783 Correlate with Mice’s Individual Basal Anxiety and Stress Reactivity

doi: 10.3390/ph15020233

Figure Lengend Snippet: Diagrams showing the effects of 10 and 30 mg/kg GS39783 on the percent time spent in the bright area of the light–dark box. There were no effects of GS39783 if all animals were analyzed together ( A ). For further analysis, mice were then grouped based on their basal anxiety, i.e., their behavior after vehicle ( B ). If mice were grouped for basal anxiety, 30 mg/kg GS39783 had anxiolytic-like effects in the mice of the most anxious group but not in the average and non-anxious groups ( C ). Furthermore, the individual effects of 30 mg/kg GS39783 were correlated with the behavior after vehicle ( D ). * p < 0.05, comparisons as indicated. Sexes were pooled since there were no effects of sex (numbers in the bars represent group sizes for males (top) and females (bottom)). Y-axis scale and units in panels ( B , C ) are the same as in panel ( A ).

Article Snippet: GS39783, a positive allosteric GABA-B receptor modulator was purchased from Axon MedChem BV (ID: 1820; Groningen, The Netherlands), Tween-80 was purchased from Sigma-Aldrich Chemie (P5188; Taufkirchen, Germany).

Techniques:

Journal: Pharmaceuticals

Article Title: Anxiolytic-like Effects of the Positive GABA B Receptor Modulator GS39783 Correlate with Mice’s Individual Basal Anxiety and Stress Reactivity

doi: 10.3390/ph15020233

Figure Lengend Snippet: Diagrams showing the effects of 10 and 30 mg/kg GS39783 on the percent time spent in the bright area of the light–dark box and on corticosterone plasma levels 10 days after stress by exposure to electric stimuli. There were no main effects of GS39783 treatment ( A ). However, the change of light–dark box behavior after stress was very variable ( B ). Therefore, mice were grouped according to their stress response ( C ). In the high stress-responsive group, GS39783 treatment significantly increased percent time spent in the bright area of the light–dark box. GS39783 treatment had no effects in the groups with average or low stress responsiveness. Of note, individual stress responsiveness was correlated with the effects of 30 mg/kg GS39783 ( D ). Corticosterone plasma levels were increased after the stress as well as after the light–dark box tests but were not affected by stress responsiveness and treatment ( E ). ## p < 0.01, * p < 0.05, comparisons as indicated. Sexes were pooled since there were no effects of sex (numbers in the bars represent group sizes for males (top) and females (bottom)).

Article Snippet: GS39783, a positive allosteric GABA-B receptor modulator was purchased from Axon MedChem BV (ID: 1820; Groningen, The Netherlands), Tween-80 was purchased from Sigma-Aldrich Chemie (P5188; Taufkirchen, Germany).

Techniques: Clinical Proteomics

Journal: Pharmaceuticals

Article Title: Anxiolytic-like Effects of the Positive GABA B Receptor Modulator GS39783 Correlate with Mice’s Individual Basal Anxiety and Stress Reactivity

doi: 10.3390/ph15020233

Figure Lengend Snippet: Extracted ion chromatograms of mass-to-charge ratio ( m / z ) 338.1640 corresponding to [M+H] + ion of GS39783 in positive mode electrospray (ESI) from ( A ) mouse brain extract and ( B ) plasma sample. Peak areas were used for quantitative purposes. Note the values measured in the peak apex ( m / z 338.1647 and m / z 338.1644).

Article Snippet: GS39783, a positive allosteric GABA-B receptor modulator was purchased from Axon MedChem BV (ID: 1820; Groningen, The Netherlands), Tween-80 was purchased from Sigma-Aldrich Chemie (P5188; Taufkirchen, Germany).

Techniques: Clinical Proteomics

Journal: Pharmaceuticals

Article Title: Anxiolytic-like Effects of the Positive GABA B Receptor Modulator GS39783 Correlate with Mice’s Individual Basal Anxiety and Stress Reactivity

doi: 10.3390/ph15020233

Figure Lengend Snippet: Summary of the GS39783 levels found in plasma and brain tissue of selected animals administered with an intraperitoneal dose of 30 mg/kg.

Article Snippet: GS39783, a positive allosteric GABA-B receptor modulator was purchased from Axon MedChem BV (ID: 1820; Groningen, The Netherlands), Tween-80 was purchased from Sigma-Aldrich Chemie (P5188; Taufkirchen, Germany).

Techniques: Clinical Proteomics