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The substantia gelatinosa (SG) of the trigeminal subnucleus caudalis (Vc) is the first relay site for the orofacial nociceptive inputs the thin myelinated Aδ and unmyelinated C primary afferent fibers. Borneol, one of the valuable timehonored herbal ingredients in traditional Chinese medicine, is a popular treatment for anxiety, anesthesia, and antinociception. However, to date, little is known as to how borneol acts on the SG neurons of the Vc. To close this gap, the whole-cell patch-clamp technique was applied to elucidate the antinociceptive mechanism responding for the actions of borneol on the SG neurons of the Vc in mice. In the voltage-clamp mode, holding at -60 mV, the borneol-induced non-desensitizing inward currents were not affected by tetrodotoxin, a voltage-gated Na channel blocker, 6-cyano-7-nitro-quinoxaline-2,3-dione, a non--methyl-D-aspartate (NMDA) glutamate receptor antagonist and DL-2-amino-5-phosphonopentanoic acid, an NMDA receptor antagonist. However, borneol-induced inward currents were partially decreased in the presence of picrotoxin, a γ-aminobutyric acid (GABA) receptor antagonist, or strychnine, a glycine receptor antagonist, and was almost suppressed in the presence of picrotoxin and strychnine. Though borneol did not show any effect on the glycine-induced inward currents, borneol enhanced GABA-mediated responses. Beside, borneol enhanced the GABA-induced hyperpolarization under the current-clamp mode. Altogether, we suggest that borneol contributes in part toward mediating the inhibitory GABA and glycine transmission on the SG neurons of the Vc and may serve as an herbal therapeutic for orofacial pain ailments.
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http://dx.doi.org/10.4196/kjpp.2020.24.5.433 | DOI Listing |
World J Urol
September 2025
Department of Pharmacology, Faculty of Medical Sciences, University of Campinas (UNICAMP), Campinas, Sao Paulo, Brazil.
Purpose: To evaluate the impact of MRP inhibition by MK571 on prostate hypercontractility in diet-induced obesity, based on the hypothesis that this intervention enhances intracellular cAMP and cGMP signaling.
Methods: Adult C57BL/6 mice were divided into three groups: (i) lean, (ii) obese, and (iii) obese + MK571 (5 mg/kg/day, 14 days). The prostate was isolated for immunohistochemistry, biochemistry and functional assays.
Diabetologia
September 2025
Walther Straub Institute of Pharmacology and Toxicology, LMU Munich, Munich, Germany.
Aims/hypothesis: Unimolecular peptides targeting the receptors for glucagon-like peptide-1 (GLP-1), glucose-dependent insulinotropic polypeptide (GIP) and glucagon (GCG) have been shown to improve glycaemic management in both mice and humans. Yet the identity of the downstream signalling events mediated by these peptides remain to be elucidated. Here, we aimed to assess the mechanisms by which a validated peptide triagonist for GLP-1/GIP/GCG receptors (IUB447) stimulates insulin secretion in murine pancreatic islets.
View Article and Find Full Text PDFElife
September 2025
Department of Neuroscience, Washington University School of Medicine, St Louis, United States.
Peripheral sensory neurons regenerate their axons after injury to regain function, but this ability declines with age. The mechanisms behind this decline are not fully understood. While excessive production of endothelin 1 (ET-1), a potent vasoconstrictor, is linked to many diseases that increase with age, the role of ET-1 and its receptors in axon regeneration is unknown.
View Article and Find Full Text PDFEpilepsia
September 2025
Department of Pharmacology and Neuroscience, Creighton University School of Medicine, Omaha, Nebraska, USA.
The rate of sudden unexpected death in epilepsy (SUDEP) is ~1 per 1000 patients each year. Terminal events reportedly involve repeated and prolonged apnea, suggesting a failure to autoresuscitate. To better understand the mechanisms and identify novel therapeutics, standardized tests to screen for autoresuscitation efficacy are needed in preclinical SUDEP.
View Article and Find Full Text PDFClin Pharmacol Drug Dev
September 2025
Phase I Clinical Research Centre, Wuhan Pulmonary Hospital, Wuhan, China.
Tamsulosin is a highly selective α1A adrenergic receptor antagonist that can relax smooth muscles in the urethra, bladder neck, and prostate and improve urinary disorders. It is therefore widely used to treat lower urinary tract symptoms caused by benign prostatic hyperplasia. The aim of this study is to evaluate the pharmacokinetic (PK) characteristics and bioequivalence of 2 different formulations (tamsulosin sustained-release tablets and tamsulosin sustained-release capsules) in healthy Chinese subjects.
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