The aim of this research was to investigate the Cyclooxygenase-2 (COX-2) selective inhibition effect on haloperidol-induced catatonia. In this study, the effect of orally, acutely and Sub-chronically administrations of compound 11b [1-(phenyl)-5-(4-methylsulfonylphenyl)-2-ethylthioimidazole] (2, 4 and 8 mg/kg), a newly selective COX-2 inhibitor, was investigated against the haloperidol-induced catatonia phenomenon comparing to the standard drug scopolamine (1 mg/Kg) followed by microdialysis analysis of Striatum dopaminergic neurotransmission. The results showed a great potency for compound 11b in improvement of catalepsy followed by enhancing the dopaminergic neurotransmission p < 0.05. In addition, our statistical analysis showed that the protective effect of compound 11b against haloperidol-induced catatonia was both dose- and time-dependent. These findings are additional pharmacological data that suggest the effectiveness of compound 11b in treatment of schizophrenic drug overdoses and also Parkinson's disease (PD) affiliated rigidity.
Download full-text PDF |
Source |
---|---|
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3813089 | PMC |
Acta Pharm Sin B
December 2024
State Key Laboratory of Anti-Infective Drug Discovery and Development, School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China.
Accurate receptor/ligand binding free energy calculations can greatly accelerate drug discovery by identifying highly potent ligands. By simulating the change from one compound structure to another, the relative binding free energy (RBFE) change can be calculated based on the theoretically rigorous free energy perturbation (FEP) method. However, existing FEP-RBFE approaches may face convergence challenges due to difficulties in simulating non-physical intermediate states, which can lead to increased computational costs to obtain the converged results.
View Article and Find Full Text PDFPharmaceuticals (Basel)
December 2024
Department of Chemistry, Prairie View A&M University, Prairie View, TX 77446, USA.
Background/objectives: The alarming rise in antibiotic resistance necessitates the discovery of novel antimicrobial agents. This study aims to design, synthesize, and evaluate new benzofuran-pyrazole-based compounds for their antimicrobial, antioxidant, and anti-inflammatory properties.
Methods: New benzofuran-pyrazole hybrid molecules were synthesized using the Vilsmeier-Haach reaction and other chemical processes.
Inorg Chem
January 2025
Department of Chemistry, University of California Riverside, Riverside, California 92521, United States.
In the 1970s Hawthorne reported an electrochemical dehydrocoupling reaction of the -carborane anion [HCBH] to form the biscarborane [CBH] . In this Communication we show that the said "Hawthorne Reaction" can be achieved thermally and that it tolerates C-butylation. The new compound was fully characterized by B, H, and C NMR spectroscopies, high-resolution mass spectrometry, and single-crystal X-ray diffraction.
View Article and Find Full Text PDFMagn Reson Chem
December 2024
Institut für Anorganische Chemie, Georg-August-Universität Göttingen, Göttingen, Germany.
We investigate cross-correlation between B quadrupole and B-F dipole-dipole coupling in two BODIPY compounds and one bis(benzoxazol)methanide in partially oriented polystyrene (PS) samples. Especially for the bis(benzoxazol)methanide, the transitions for which the two interactions interfere con- or destructively clearly show distinct linewidths.
View Article and Find Full Text PDFACS Med Chem Lett
December 2024
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo University, Kasr El-Aini Street, Cairo 11562, Egypt.
New derivatives -, , -, -, , , , -, -, and were synthesized and evaluated for their VEGFR-2 inhibition. Compounds , , and showed remarkable enzyme inhibition IC = 57.1, 42.
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!