Attempts to isolate the putative endogenous ligand for the benzodiazepine receptor from bovine urine resulted in the identification of three isoflavans: equol (1), 3',7-dihydroxyisoflavan (2), and 4'-hydroxy-7-methoxyisoflavan (9), as "diazepam-like" compounds. 3-Chloro-9H-carbazole (17) was found to enhance the binding of diazepam in the benzodiazepine receptor binding assay. Pinosylvine monomethyl ether (18), indigo (20), and indirubin (21) were isolated as inactive compounds.
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http://dx.doi.org/10.1021/np50030a005 | DOI Listing |
J Toxicol Environ Health A
March 2023
Department of Biophysics and Physiology, Laboratory of Experimental Cancerology (LabCancer), Federal University of Piauí, Teresina, Brazil.
ACS Chem Neurosci
September 2020
Department of Chemistry & Biochemistry, Milwaukee Institute for Drug Discovery, University of Wisconsin-Milwaukee, Milwaukee, Wisconsin 53211, United States.
The need for improved medications for the treatment of epilepsy and chronic pain is essential. Epileptic patients typically take multiple antiseizure drugs without complete seizure freedom, and chronic pain is not fully managed with current medications. A positive allosteric modulator (PAM) of α2/3-containing GABA receptors (5-(8-ethynyl-6-(pyridin-2-yl)-4-benzo[]imidazole[1,5-α][1,4]diazepin-3-yl) oxazole or KRM-II-81 () is a lead compound in a series of imidazodiazepines.
View Article and Find Full Text PDFBr J Pharmacol
August 2020
Institute of Pharmacology and Toxicology, NHC and CAMS Key Laboratory of Medical Neurobiology, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, China.
Background And Purpose: Febrile seizures (FS), the most common seizures in childhood and often accompanied by later epileptogenesis, are not well controlled. Inflammatory processes have been implicated in the pathophysiology of epilepsy. However, whether caspase-1 is involved in FS generation and could be a target for the treatment of FS is still unclear.
View Article and Find Full Text PDFToxicol Appl Pharmacol
October 2019
Department of Pharmaceutical Products, Faculty of Pharmacy, Federal University of Minas Gerais, Belo Horizonte 31270-901, Brazil.
Phytomedicine
October 2011
Department of Anesthesiology, Changhua Christian Hospital, Changhua County 500, Taiwan.
Honokiol, an active agent extracted from magnolia bark, has been reported that induces anxiolytic action in a mouse elevated plus-maze test. However, the mechanism of anxiolytic action induced by honokiol remains unclear. This study was to investigate the change in two forms of glutamic acid decarboxylase (GABA synthesized enzymes) GAD(65) and GAD(67) in the cortex and hippocampus areas while the anxiolytic actions induced by chronic administration of honokiol in mice.
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