Ro 15-4513 (1.5 mg/kg) decreased the exploratory activity of mice in a holeboard test. This effect was reversed by diazepam (1 mg/kg), ethanol (1 g/kg) and sodium pentobarbital (15 mg/kg). Higher doses of these three agents reduced the number of exploratory head-dips, and Ro 15-4513 antagonised these effects. These observations are consistent with the suggestion that Ro 15-4513 is a partial inverse agonist at benzodiazepine receptors and acts by reducing the efficacy of GABA. Ro 15-4513's interaction with ethanol in the holeboard closely resembled its interaction with the barbiturate.
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http://dx.doi.org/10.1016/0091-3057(87)90015-3 | DOI Listing |
Curr Comput Aided Drug Des
January 2025
Institute of Geriatrics, School of Basic Medicine, Hubei University of Chinese Medicine, Wuhan, 430065, China.
Objective: This study aimed to investigate the medicinal properties of SZS before and after processing and provide novel insights into its potential for treating insomnia.
Methods: This study employed the network pharmacology platform to gather information on the chemical composition of SZS, human targets, genes, molecular networks, and pathways associated with insomnia treatment using SZS. Liquid chromatography-tandem mass spectrometry (LC-MS/ MS) was utilized to analyze the chemical profiles of crude SZS, parched SZS, and their combined decoction.
Respir Res
January 2025
Department of Pulmonary and Critical Care Medicine, Shanghai East Hospital, School of Medicine, Tongji University, Shanghai, 200092, China.
Background: Neuroimmune interaction is an underestimated mechanism for lung diseases, and cryoablation is a competitive advantageous technique than other non-pharmacologic interventions for peripheral nerve innervating the lung. However, a lack of cryodenervation model in laboratory rodents leads to the obscure mechanisms for techniques used in clinic.
Method: Herein, we developed a novel practical method for mouse peripheral nerve cryoablation, named visualized and simple cryodenervation (VSCD).
Pain
December 2024
Department of Cell and Developmental Biology, Institute of Life Sciences, The Hebrew University of Jerusalem, Jerusalem, Israel.
The mesopontine tegmental anesthesia area (MPTA) is a focal brainstem locus which, when exposed to GABAergic agents, induces brain-state transitioning from wakefulness to unconsciousness. Correspondingly, MPTA lesions render animals relatively insensitive to GABAergic anesthetics delivered systemically. Using chemogenetics, we recently identified a neuronal subpopulation within the MPTA whose excitation induces this same pro-anesthetic effect.
View Article and Find Full Text PDFCell Death Dis
January 2025
The First Affiliated Hospital, Cancer Research Institute, Hengyang Medical School, University of South China, Hengyang, Hunan, 421001, PR China.
This research demonstrates that DCC-2036 (Rebastinib), a potent third-generation tyrosine kinase inhibitor (TKI), effectively suppresses tumor growth in colorectal cancer (CRC) models with functional immune systems. The findings underscore the capacity of DCC-2036 to enhance both the activation and cytotoxic functionality of CD8 T cells, which are crucial for facilitating anti-tumor immune responses. Through comprehensive multi-omics investigations, significant shifts in both gene and protein expression profiles were detected, notably a marked decrease in DKK1 levels.
View Article and Find Full Text PDFNutrients
December 2024
Department of Molecular Medicine, School of Medicine, Ewha Womans University, Seoul 07804, Republic of Korea.
: Sleep, a process physiologically vital for mental health, faces disruptions in various sleep disorders linked to metabolic and neurodegenerative risks. seed (Zizy) has long been recognized for its diverse pharmacological attributes, including analgesic, sedative, insomnia, and anxiety alleviation. : In this study, the sleep-prolonging effects of Zizy extract (100, 200 mg/kg), along with their characterizing compounds jujuboside A (JuA) (5, 10 mg/kg), were evaluated in a mouse model under a pentobarbital-induced sleep.
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