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N-Demethylsinomenine Relieves Neuropathic Pain in Male Mice Mainly via Regulating α2-Subtype GABA Receptors.
CNS Neurosci Ther
January 2025
School of Pharmacy, Nantong University, Nantong, Jiangsu, China.
Aims: N-Demethylsinomenine (NDSM) demonstrates good analgesic efficacy in preclinical pain models. However, how NDSM exerts analgesic actions remains unknown.
Methods: We examined the analgesic effects of NDSM using both pain-evoked and pain-suppressed behavioral assays in two persistent pain models.
Protein phosphatase 2A inhibitors: a possible pharmacotherapy for benzodiazepine dependence.
J Pharm Pharmacol
November 2024
Laboratory of Drug Addiction and Experimental Therapeutics, Department of Pharmacy, School of Pharmacy, Hyogo Medical University, Kobe 650-8530, Japan.
Objectives: Benzodiazepines (BZDs) activate the γ-aminobutyric acid (GABA) subtype A (GABAA) receptors, and thus are widely used medicines for the treatment of anxiety and insomnia. For chronic use, tolerance to BZDs is a major problem. Patients with chronic insomnia that develop tolerance to BZDs lose therapeutic effects but also potentially suffer from BZD dependence resulting in BZD withdrawal.
View Article and Find Full Text PDFThe Role of GABA Receptors in Anesthesia and Sedation: An Updated Review.
CNS Drugs
January 2025
Department of Anesthesiology, Jefferson Surgical Center Endoscopy, Sidney Kimmel Medical College, Jefferson Health, 111 S 11th Street, #7132, Philadelphia, PA, 19107, USA.
GABA (γ-aminobutyric acid) receptors are constituents of many inhibitory synapses within the central nervous system. They are formed by 5 subunits out of 19 various subunits: α1-6, β1-3, γ1-3, δ, ε, θ, π, and ρ1-3. Two main subtypes of GABA receptors have been identified, namely GABAA and GABAB.
View Article and Find Full Text PDFEvaluation of the sedative-motor effects of novel GABAkine imidazodiazepines using quantitative observation techniques in rhesus monkeys.
J Psychopharmacol
December 2024
Department of Psychiatry and Human Behavior, Center for Innovation and Discovery in Addictions, University of Mississippi Medical Center, Jackson, MS, USA.
Article Synopsis
- Benzodiazepines interact with different GABA receptor subtypes, primarily α1GABA and α3GABA, affecting sedative and motor functions in animals.
- The study tested various novel GABAkines on rhesus monkeys to assess their sedative-motor effects, predicting that effectiveness would correlate with their action on α1GABA and α3GABA receptors.
- Results showed that while all compounds produced some sedation, only those targeting α5GABA receptors led to deep sedation, indicating a complex relationship between receptor efficacy and observed behavior.
The Effects of Variation in the GABA Receptor Gene on Anxious Depression are Mediated by the Functional Connectivity Between the Amygdala and Middle Frontal Gyrus.
Neuropsychiatr Dis Treat
September 2024
School of Biological Sciences and Medical Engineering, Southeast University, Nanjing, People's Republic of China.
Background: γ-aminobutyric acid (GABA) and its main receptor, the GABA receptor, are implicated in major depressive disorder (MDD). Anxious depression (AD) is deemed to be a primary subtype of MDD. The amygdala and the dorsolateral prefrontal cortex (DLPFC) are key brain regions involved in emotional regulation.
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