Ethymisole, or 4,5-di(N-methylcarbamoyl)-1-ethyl-imidazole, is a cognitive enhancer and nootropic drug, the molecular target of which is a multifunctional protein kinase C K2 (casein kinase II). New data about signal pathways and protein substrates of CK2 have been obtained due to research effort of many laboratories. The paper presents a historical sketch of molecular investigations underlying memory enhancer effects of ethymisole; this and the other pharmacological effects of ethymisole are considered in the light of new data.
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Protein kinase CK2 is an important enzyme in the nervous system. The nuclear forms of CK2 regulate chromatin structure and gene expression, the key processes for long-term memory formation. Memory modulators, the Structural Analogues of Etimizole (SAE), were able to increase or decrease the activity of chromatin-associated CK in the cortex and hippocampus of rat brain in vitro.
View Article and Find Full Text PDFEthymisole, or 4,5-di(N-methylcarbamoyl)-1-ethyl-imidazole, is a cognitive enhancer and nootropic drug, the molecular target of which is a multifunctional protein kinase C K2 (casein kinase II). New data about signal pathways and protein substrates of CK2 have been obtained due to research effort of many laboratories. The paper presents a historical sketch of molecular investigations underlying memory enhancer effects of ethymisole; this and the other pharmacological effects of ethymisole are considered in the light of new data.
View Article and Find Full Text PDFThe aim of the study was assessment of ethimizol effects on fatigue of respiratory muscles and ventilatory disorders caused by inspiratory resistive load on respiration. Cat experiments showed that administration of ethimizol in inspiratory fatigue reestablishes total bioelectric activity of the inspiratory muscles and diaphragmatic nerve, diminishes useful respiratory cycle and respiration rate. Thus, ethimizol in a 1 mg/kg dose i.
View Article and Find Full Text PDFStatus of the "protein kinase CK2-HMG14" system in age-related amnesia in rats.
Neurosci Behav Physiol
October 2003
Science Research Institute of Experimental Medicine, Russian Academy of Medical Sciences, 12 Academician Pavlov Street, 197376 St. Petersburg, Russia.
The experiments described here demonstrate that disruption of the phosphorylation of transcription factors of the HMG cAMP/Ca-independent protein kinase CK2 class may be the cause of decreased gene expression in age-related cognitive deficits. Amnesia for a conditioned passive avoidance reaction (CPAR) in aged rats (24 months old) was accompanied by decreases in the synthesis of synaptosomal proteins and transcription in nuclei isolated from cortical, hippocampal, and striatal neurons. There was a decrease in chromatin protein kinase CK2 activity and a significant decrease in the phosphorylation of HMG14 by protein kinase CK2.
View Article and Find Full Text PDF[State of the "protein kinase CK2-HMG14" system in age-dependent amnesia in rats].
Ross Fiziol Zh Im I M Sechenova
May 2002
Institute of Experimental Medicine, Russian Acad. Med. Sci., St. Petersburg, 197376, Acad. Pavlov St., 12, Russia.
It has been shown that a decrease in HMGs transcription factors phosphorylation by protein kinase CK2 may be the cause of a gene expression decline in cognitive disorders. Passive avoidance amnesia in old rats (24 month) was accompanied by a decrease in synaptosomal protein synthesis and transcription in isolated nuclei of cortex, hippocampus, and striatum. A decrease in chromatin protein kinase CK2 activity and a significant decrease in HMG14 phosphorylation by CK2 was found in old rats.
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