The selective and systemically active antagonist for the metabotropic glutamate receptor subtype 5 (mGluR5), 2-methyl-6-(phenylethynyl)pyridine (MPEP) was shown to display anxiolytic-like activity in a number of unconditioned assays of stress and anxiety (elevated plus maze, shock probe burying, marble burying, social interaction, and stress-induced hyperthermia) in rodents. In this report, we extend these observations found using unconditioned models of anxiety to include three models of conditioned anxiety, comparing the activity of MPEP to the clinically used anxiolytics, diazepam, and buspirone. MPEP and diazepam, but not buspirone, showed anxiolytic-like activity in the fear-potentiated startle (FPS) model. In a conditioned ultrasonic vocalization (USV) procedure, MPEP, diazepam, and buspirone reduced vocalizations to a similar degree. In the modified Geller-Seifter procedure, MPEP, diazepam, and buspirone displayed statistically significant anxiolytic-like activity, increasing the number of punished responses. Thus, these findings confirm and extend previous reports that MPEP exhibits anxiolytic-like activity in rats, and suggests that development of mGluR5 antagonists may provide a novel approach to treating anxiety disorders.
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http://dx.doi.org/10.1016/s0091-3057(02)00828-6 | DOI Listing |
Synapse
January 2025
Department of Biochemistry & Molecular Biology, Bangabandhu Sheikh Mujibur Rahman Science and Technology University, Gopalganj, Bangladesh.
Sesamol (SES) and linalool (LIN) are aromatic compounds that have neuroprotective effects. The main purpose of this study is to evaluate the anxiolytic activity of LIN and SES co-treatment on Swiss albino mice and analyze its possible mechanism through in silico study. In this sense, the mice were given the gamma-aminobutyric acid type A receptors (GABA) agonist diazepam (DZP; 3 mg/kg, p.
View Article and Find Full Text PDFMolecules
December 2024
Department of Pharmacognosy and Pharmaceutical Chemistry, Faculty of Pharmacy, Medical University of Plovdiv, 4002 Plovdiv, Bulgaria.
L. has been traditionally applied as a remedy for headaches, rheumatism, digestion, respiratory and neurological problems, and other medical conditions. However, the literature data on its effects on cognitive function are scarce.
View Article and Find Full Text PDFPharmacol Rep
December 2024
Department of Clinical Pharmacy, Faculty of Pharmacy, Medical College, Jagiellonian University, Medyczna 9, Kraków, 30-688, Poland.
Background: Research on new candidates for antidepressant/anxiolytic drugs from the long-chain arylpiperazines (LCAPs) group containing a 1,3-dimethylpurine-2,6-dione as a terminal amide fragment fits into the modern exploration trend. This study aimed to examine, for the first time in male Wistar rats, pharmacodynamic (antidepressant- and anxiolytic-like) and pharmacokinetic properties of 7-(5-(4-(3-chlorophenyl)piperazin-1-yl)pentyl)-1,3-dimethyl-3,7-dihydro-1 H-purine-2,6-dione hydrochloride (GR-14).
Methods: Antidepressant- and anxiolytic-like activities have been assessed in the forced swim test (FST) and Vogel conflict drinking test, respectively.
Acta Pharm Sin B
November 2024
Department of Pharmacology, College of Pharmacy, China Pharmaceutical University, Nanjing 211198, China.
Anxiety disorders are one of the most epidemic and chronic psychiatric disorders. An incomplete understanding of anxiety pathophysiology has limited the development of highly effective drugs against these disorders. GPR17 has been shown to be involved in multiple sclerosis and some acute brain injury disorders.
View Article and Find Full Text PDFBrain Behav Immun
December 2024
Department of Biology, Rutgers University, Camden, NJ, USA; Center for Computational and Integrative Biology, Rutgers University, Camden, NJ, USA. Electronic address:
We previously demonstrated that sphingosine-1-phosphate receptor 3 (S1PR3) in the medial prefrontal cortex (mPFC) prevents reductions in sociability normally caused by stress. S1PR3 is a ubiquitously expressed G-protein coupled receptor that regulates immune system function, although its regulation of other biological processes is not well understood. Pharmacological activators of S1PR3 might provide important insights for understanding the neural substrates underlying sociability.
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