BD-1158 is a new 1,4 benzodiazepine derivative. The purpose of the present experiments was to test the spontaneous behaviour (typical of a rabbit) after administration of BD-1158 and thus to define the activity and side effects of this substance under physiological conditions. The experiments were performed for 3 subsequent days in a group of 10 rabbits. On the first day spontaneous behaviour was tested. On the second day 1 ml of 1% starch solution was administered intraperitoneally. On the third day BD-1158 was administered intraperitoneally at a dose 10 mg/kg diluted in 1% starch solution up to 1 ml, 35-40 minutes before the beginning of the experiment. Six phases of behaviour were estimated. It was concluded that BD-1158 has a strong anxiolytic and sedative effect, decreases the state of animal's attention, water and food uptake.
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ACS Chem Neurosci
January 2025
Sensor Engineering Department, Faculty of Science and Engineering, Maastricht University, 6200 MD Maastricht, The Netherlands.
As the main inhibitory neurotransmission system, the GABAergic system poses an interesting yet underutilized target for molecular brain imaging. While PET imaging of postsynaptic GABAergic neurons has been accomplished using radiolabeled benzodiazepines targeting the GABA receptor, the development of presynaptic radioligands targeting GABA transporter 1 (GAT1) has been unsuccessful thus far. Therefore, we developed a novel GAT1-addressing radioligand and investigated its applicability as a PET tracer in rodents.
View Article and Find Full Text PDFSci Justice
January 2025
Leverhulme Research Centre for Forensic Science, School of Science and Engineering, University of Dundee, Nethergate, Dundee DD2 1HD, Scotland, UK.
The assessment of measurement uncertainty of an analytic method is a requirement for forensic toxicologists and drug chemists. There are two main methods for estimating measurement uncertainty: the bottom-up and the top-down approaches. The bottom-up approach has been suggested in current practice guides including 'Guide to the Expression of Uncertainty in Measurement (GUM)' published by ISO, and a guide to 'Quantifying Uncertainty in Analytical Measurement' published by EURACHEM.
View Article and Find Full Text PDFBiochem Biophys Res Commun
January 2025
Molecular Biophysics and Structural Biology (MBSB) Group, Department of Biochemistry, University of Johannesburg, Auckland Park Kingsway Campus, 2006, South Africa. Electronic address:
To address microbial infections and combat drug resistance, we designed, synthesized, and evaluated three novel s-triazine clubbed pharmacophores: 1-acetylpyrazoline (5a-e), 2-aminopyrimidine (6a-e), and 1,5-benzodiazepine (7a-e). These were derived from chalcone (4a-e), showing improved pharmacological profiles. The compounds underwent characterization by FTIR, NMR, and Mass Spectroscopy, and their antimicrobial activities, along with structure-activity relationships (SAR), were assessed using in silico and in vitro methods.
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January 2025
Division of Pharmacotherapy and Translational Science, College of Pharmacy, University of Texas at Austin, San Antonio, Texas.
To evaluate weight change with a combination of olanzapine and samidorphan (OLZ/SAM) versus olanzapine by pooling data across clinical studies. This study was an individual patient data (IPD) meta-analysis of clinical trial data. EMBASE, MEDLINE, and PsycInfo were searched for randomized clinical trials (≥12 weeks) in adults with schizophrenia or bipolar I disorder in which weight change from baseline was the primary or secondary end point.
View Article and Find Full Text PDFChem Commun (Camb)
January 2025
Department of Chemistry, Faculty of Science, Gakushuin University, 1-5-1 Mejiro, Toshima-ku, Tokyo 171-8588, Japan.
We report a cascade synthesis of indole-fused benzodiazepines by the photocatalyzed addition of phenacyl radical, generated from α-acetoxy acetophenone, to 2-(3-methyl-1-indol-1-yl)aniline, and subsequent cyclodehydration. A range of indole-fused benzodiazepines were obtained from readily available substrates.
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