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Efficient Reversal of Neuromuscular Blocking Agent-Induced Biological Functions and Side Effects by an Extended Biphen[3]arene Carboxylate.
J Med Chem
December 2024
State Key Laboratory of National Security Specially Needed Medicines, Beijing Institute of Pharmacology and Toxicology, Beijing 100850, P. R. China.
Article Synopsis
- * A new compound called ExBP3C was developed as an effective reversal agent for multiple NMBAs, showing strong binding capabilities with agents like atracurium and rocuronium.
- * ExBP3C demonstrated better efficiency than the existing reversal drug sugammadex, and in tests, it rapidly corrected heart rate issues caused by an overdose of atracurium within two minutes, indicating good safety and biocompatibility.
Voltage dependence of M2 muscarinic receptor antagonists and allosteric modulators.
Biochem Pharmacol
September 2024
Department of Natural Sciences, The Open University of Israel, Ra'anana, Israel. Electronic address:
Muscarinic receptors are G protein-coupled receptors (GPCRs) that play a role in various physiological functions. Previous studies have shown that these receptors, along with other GPCRs, are voltage-sensitive; both their affinity toward agonists and their activation are regulated by membrane potential. To our knowledge, whether the effect of antagonists on these receptors is voltage-dependent has not yet been studied.
View Article and Find Full Text PDFMuscarinic Modulation of Synaptic Transmission and Short-Term Plasticity in the Dorsal and Ventral Hippocampus.
Mol Cell Neurosci
June 2024
Laboratory of Physiology, University of Patras, Department of Medicine, Rion, Greece. Electronic address:
Muscarinic neurotransmission is fundamentally involved in supporting several brain functions by modulating flow of information in brain neural circuits including the hippocampus which displays a remarkable functional segregation along its longitudinal axis. However, how muscarinic neuromodulation contributes to the functional segregation along the hippocampus remains unclear. In this study we show that the nonselective muscarinic receptor agonist carbachol similarly suppresses basal synaptic transmission in the dorsal and ventral CA1 hippocampal field, in a concentration-depended manner.
View Article and Find Full Text PDFNeural Subtype-dependent Cholinergic Modulation of Neural Activities by Activation of Muscarinic 2 Receptors and G Protein-activated Inwardly Rectifying Potassium Channel in Rat Periaqueductal Gray Neurons.
Neuroscience
December 2022
Department of Pharmacology, Nihon University School of Dentistry, 1-8-13 Kanda-Surugadai, Chiyoda-ku, Tokyo 101-8310, Japan; Division of Oral and Craniomaxillofacial Research, Dental Research Centre, Nihon University School of Dentistry, 1-8-13 Kanda-Surugadai, Chiyoda-ku, Tokyo 101-8310, Japan; Molecular Dynamics Imaging Unit, RIKEN Centre for Life Science Technologies, 6-7-3 Minatojima-minamimachi, Chuo-ku, Kobe 650-0047, Japan. Electronic address:
Acetylcholine plays a pivotal role in the regulation of functions such as pain and the sleep and wake cycle by modulating neural activities of the ventrolateral periaqueductal gray (vlPAG). Electrophysiological studies have shown that cholinergic effects are inconsistent among recorded neurons, particularly in the depolarization and hyperpolarization of the resting membrane potential (RMP). This discrepancy may be due to the neural subtype-dependent cholinergic modulation of the RMP.
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