The action of a selective 5-HT1A agonist S20244 and its two enantiomers (+)-S20499 and (-)-S20500 were assessed in mice. The animals were confronted with a free exploratory test especially adapted to reveal behavioural sedation, and with a two-box light/dark choice situation validated for the detection of anti-anxiety agents. These drugs were found to have anxiolytic properties at low doses, like benzodiazepines. Furthermore, the drugs exhibited sedative effects at higher doses. These results closely resemble those we found after administration of two other 5-HT1A agonists, 8-OH-DPAT and MDL 73005EF (NeuroReport, 1, 267-270, 1990).
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http://dx.doi.org/10.1097/00001756-199201000-00022 | DOI Listing |
Int J Mol Sci
December 2024
Department of Neurosciences, Lerner Research Institute, Cleveland Clinic, Cleveland, OH 44195, USA.
Spinal cord injury (SCI) results in functional deficits below the injured spinal level. The descending serotonergic system in the spinal cord is critically involved in the control of motor and autonomic functions. Specifically, SCI damages the projections of serotonergic fibers, which leads to reduced serotonin inputs and increased amounts of spinal serotonergic receptors.
View Article and Find Full Text PDFJ Neurodev Disord
January 2025
Graduate Neuroscience Program, University of California, Riverside, CA, USA.
Background: Fragile X syndrome (FXS) is a leading known genetic cause of intellectual disability and autism spectrum disorders (ASD)-associated behaviors. A consistent and debilitating phenotype of FXS is auditory hypersensitivity that may lead to delayed language and high anxiety. Consistent with findings in FXS human studies, the mouse model of FXS, the Fmr1 knock out (KO) mouse, shows auditory hypersensitivity and temporal processing deficits.
View Article and Find Full Text PDFNeuropharmacology
March 2025
Neurolixis, Castres, France.
Serotonin 5-HT receptor agonists are prime candidates for CNS drug discovery due to their involvement physiological and pathological processes relevant to neurology and psychiatry. However, the lack of target specificity of many previously characterized agonists has long been a barrier to pharmacological and therapeutic progress. Some of the obstacles may be overcome through the recent concept of biased agonism, which has attracted considerable attention to the development of novel chemical entities at 5-HT, and particularly 5-HT receptors, by specifically targeting intracellular signalling pathways that may themselves be linked to specific brain regions and therapeutic indications.
View Article and Find Full Text PDFNaunyn Schmiedebergs Arch Pharmacol
December 2024
Department of Pharmaceutics, College of Pharmacy, King Saud University, 11451, Riyadh, Saudi Arabia.
This study investigates the impact of a high-fat-rich diet (HFRD) on behavioral, biochemical, neurochemical, and histopathological studies using the hypothalamus of rats following niacin (NCN) administration. The rats were divided into HFRD and normal diet (ND)-fed groups and administered selected doses of NCN, i.e.
View Article and Find Full Text PDFBiomed Pharmacother
January 2025
School of Pharmacy and Institute of New Drug Development, Jeonbuk National University Jeonju 54896, Republic of Korea. Electronic address:
Fluoxetine is a selective serotonin reuptake inhibitor (SSRI) widely used for depression, but its potential effects on gut microbiota regulation and vagus nerve-mediated serotonin receptor expression have not been well studied. We investigated changes in the gut microbiome regulated by fluoxetine and vagus nerve-mediated expression of several serotonin (5-HT) receptor types associated with anxiety and depression. Oral administration of fluoxetine alleviated lipopolysaccharide (LPS)-induced depressive and anxiety behaviors, increased 5-HT1A, 2 C, and melanocortin 4 (MC4) receptor expression, and the composition of Lactobacillus in mice's gut microbiome.
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