Abstract：
:In the present study effects of a new local anaesthetics, pentacaine (trans-2-pyrolidinocyclohexylester of 3-pentyloxyphenylcarbamic acid), and of some chemically related compounds on rat hepatic adenylate cyclase activity were studied under various experimental conditions. As compared with tetracaine, the local anaesthetics tested showed stronger inhibitory effects, regardless of the type of stimulating agents used to activate adenylate cyclase. The most potent effect was observed with pentacaine. Its inhibitory effects on glucagon, guanylylimidodiphosphate (Gpp/NH/p), sodium fluoride or forskolin stimulated activity suggest that it may directly act on the catalytic unit of adenylate cyclase. The same conclusion can be drawn based on its inhibitory effects on adenylate cyclase, regardless ATP concentrations used as the enzyme substrate, and on octylpyranoside solubilized enzyme activated by preincubation of the enzyme preparation with Gpp/NH/p. Structure-activity studies have suggested that the pentacaine molecule as a whole and none of its parts alone or its analogs are responsible for the inhibitory effect. However, the inhibitory effects of these compounds on the rat adenylate cyclase activity do not correlate with their local anaesthetic properties. The possibility of using adenylate cyclase inhibitors to decrease cyclic AMP production under pathological conditions, like in cholera, known to be due to a high adenylate cyclase activity, is discussed.
journal_name
Gen Physiol Biophysjournal_title
General physiology and biophysicsauthors
Hynie S,Wenke M,Klenerová Vsubject
Has Abstractpub_date
1985-10-01 00:00:00pages
517-30issue
5eissn
0231-5882issn
1338-4325journal_volume
4pub_type
杂志文章abstract：:Kinase-targeted therapy is a new and promising approach to disease treatment. However, some kinase inhibitors have been observed to cause an off-target adverse risk for skeletal system by influencing the growth of osteoblasts. It is known that the proliferation and differentiation of osteoblasts are essentially regula...
journal_title：General physiology and biophysics
pub_type： 杂志文章
doi：10.4149/gpb_2018030
更新日期：2019-01-01 00:00:00
abstract：:Culturing the fresh-water alga Hydrodictyon reticulatum for 9 days in the presence of 0.2 and 0.4 mmol/l Ba2+ increases the membrane potential about twice and the plasmalemma resistance 5-10 times without having any significant effect on the cell contents of water and Na+, K+ and Cl- ions. While in control cells the m...
journal_title：General physiology and biophysics
pub_type： 杂志文章
doi：
更新日期：1996-04-01 00:00:00
abstract：:Hyperlipidemia is found to be associated with changes in fatty acid (FA) profiles. The aim of this study was to investigate the effects of AHA-Step-1 dietary treatment and combination of fibrates (gemfibrozil) with dietary intervention on serum and erythrocyte phospholipid FA composition in human hyperlipidemia. 78 st...
journal_title：General physiology and biophysics
pub_type： 临床试验,杂志文章
doi：
更新日期：2009-01-01 00:00:00
abstract：:The effects of both chronic hypoxia and acute intermittent hypoxia (AIH) on cardiovascular system are unclear. We designed this study to develop a rabbit model of hypertension by exposure to chronic hypobaric hypoxia (CHH) and to investigate the effects of AIH on hypertensive rabbits. Present study was performed in 13...
journal_title：General physiology and biophysics
pub_type： 杂志文章
doi：10.4149/gpb_2013070
更新日期：2014-01-01 00:00:00
abstract：:Although high-intensity electric fields (HEF) application is currently the only effective therapy available to terminate ventricular fibrillation, it may cause injury to cardiac cells. In this study we determined the relation between HEF pulse length and cardiomyocyte lethal injury. We obtained lethality curves by sur...
journal_title：General physiology and biophysics
pub_type： 杂志文章
doi：10.4149/gpb_2015047
更新日期：2016-04-01 00:00:00
abstract：:Lidocaine, a use-dependent Na(+) channel blocker, paradoxically evokes neural activation in the slowly adapting stretch receptor organ of crayfish at 5-10 mmol/l concentration. For elucidating the underlying mechanisms of this paradoxical effect, a series of conventional electrophysiological experiments were performed...
journal_title：General physiology and biophysics
pub_type： 杂志文章
doi：
更新日期：2007-03-01 00:00:00
abstract：:Environmental exposure to modern microwave telecommunication electromagnetic fields (EMFs) has increased to unprecedented levels with consequent health complaints and concerns. Many studies have already reported genotoxic effects on a variety of organisms and cell/tissue types. Human peripheral blood lymphocytes from ...
journal_title：General physiology and biophysics
pub_type： 杂志文章
doi：10.4149/gpb_2019032
更新日期：2019-09-01 00:00:00
abstract：:The hydrolytic activity and interaction of acidic and neutral phospholipase A2 (PLA2) with large unilamellar liposomes treated with cobra venom cytotoxin Vc5 (CT Vc5) were studied to more fully understand the modulating effects of cationic membrane-active peptides on PLA2. Studies were done by fluorescence displacemen...
journal_title：General physiology and biophysics
pub_type： 杂志文章
doi：
更新日期：1995-04-01 00:00:00
abstract：:Fusion of neuraminidase or trypsin pretreated human erythrocytes and untreated cells was performed. The obtained doublets had a permanent dipole moment which disappeared as a function of time. Since the dipole moment disappearance is due to protein interdiffusion the lateral diffusion constant may be determined. This ...
journal_title：General physiology and biophysics
pub_type： 杂志文章
doi：
更新日期：1984-06-01 00:00:00
abstract：:For characterization of Na(+),K(+)-ATPase, a key enzyme involved in maintenance of intracellular sodium homeostasis, expression of alpha1 subunit and the ATP- and Na(+)-binding properties were investigated by Western blot analysis and by enzyme kinetics, respectively. Previous studies documented time-dependent alterat...
journal_title：General physiology and biophysics
pub_type： 杂志文章
doi：10.4149/gpb_2010_03_266
更新日期：2010-09-01 00:00:00
abstract：:The dynamics of a bioreactor with a variable volume and an active solute flux based on the thermodynamics of irreversible processes and stability analysis was studied. The active solute flux may control both the bioreactor volume and the hydrostatic pressure as well as the concentration of the solute inside the cell i...
journal_title：General physiology and biophysics
pub_type： 杂志文章
doi：
更新日期：1988-02-01 00:00:00
abstract：:Quercetin and epigallocatechin gallate are two of the most abundant polyphenols in dietary plants, including apples, onions, red wine and green tea. The bioactivity of polyphenols is linked to their ability to interact with cell membranes without being internalized. The aim of the present study was to assess the short...
journal_title：General physiology and biophysics
pub_type： 杂志文章
doi：10.4149/gpb_2012_005
更新日期：2012-03-01 00:00:00
abstract：:Cochlear spiral ganglion neurons provide the only pathway for transmitting sound evoked activity from the hair cells to the central auditory system. Serotonin plays a role in the response properties of central auditory neurons. However, knowledge about the role of serotonin in the peripheral auditory nervous system re...
journal_title：General physiology and biophysics
pub_type： 杂志文章
doi：10.4149/gpb_2013005
更新日期：2013-03-01 00:00:00
abstract：:The effects of different parts of extract from medicinal plant Conyza canadensis, used to control bleeding, on human blood platelet aggregation in vitro were investigated. Aqueous extract of Conyza c. from young or old plants, glycoconjugate part, polysaccharide part and aglycon part at the concentrations above 0.75 m...
journal_title：General physiology and biophysics
pub_type： 杂志文章
doi：
更新日期：2007-06-01 00:00:00
abstract：:Mitochondrial nucleoids (hereafter nucleoids) contain genetic information, mitochondrial DNA, prerequisite for mitochondrial functioning, particularly information required for mitochondrial electron transport. To understand nucleoid functioning, it is imperative to know its ultrastructure and dynamics in the context o...
journal_title：General physiology and biophysics
pub_type： 杂志文章
doi：10.4149/gpb_2016008
更新日期：2016-07-01 00:00:00
abstract：:Lignin, the structural polymer of the plant cell walls, is produced by free radical polymerization of phenolic alcohols, catalyzed by different peroxidases. The mechanism and the structural organization of lignin in the cell have not been completely understood. In this study we applied fractal analysis to images of li...
journal_title：General physiology and biophysics
pub_type： 杂志文章
doi：
更新日期：2000-06-01 00:00:00
abstract：:A number of studies have reported that male reproductive organs are susceptible to electromagnetic fields (EMFs). The aim of this study was to explore the effects of microwave radiation exposures on 6-8 weeks old male Swiss albino mice. Mice were divided into two groups: group I - sham-exposed (Control), and group II ...
journal_title：General physiology and biophysics
pub_type： 杂志文章
doi：10.4149/gpb_2017059
更新日期：2018-07-01 00:00:00
abstract：:Currents through DPI 201-106 modified single cardiac sodium channels in guinea pig ventricular cells were measured using the patch clamp technique in the cell-free configuration to control the sodium concentrations on both sides of the patch membrane. Current-voltage relationships of the single channels were obtained ...
journal_title：General physiology and biophysics
pub_type： 杂志文章
doi：
更新日期：1991-02-01 00:00:00
abstract：:This study investigated time-dependent variations in the activities of adenosine deaminase (ADA), an adenosine-metabolizing enzyme, and myeloperoxidase (MPO), an oxidation reaction-catalyzing enzyme, in control and streptozotocin (STZ)-induced diabetic rat liver. The animals were sacrificed at six different times of d...
journal_title：General physiology and biophysics
pub_type： 杂志文章
doi：
更新日期：2008-03-01 00:00:00
abstract：:Aiming at making the Münch model more adequate to the biological reality we introduce certain modifications and complements. Considering the model within the framework of so-called integrated system of long-distance water transport in plants we present a quantitative analysis based on the Kedem-Katchalsky formalism. A...
journal_title：General physiology and biophysics
pub_type： 杂志文章
doi：
更新日期：2001-06-01 00:00:00
abstract：:Recent research has supported a potential role of immune pathology in the etiopathogenesis of schizophrenic. In the CNS various viruses were identified in the brains of schizophrenic patients. Pro-inflammatory cytokines were found to be associated with the stage of disease. Microglial cells were reported to be activat...
journal_title：General physiology and biophysics
pub_type： 杂志文章,评审
doi：
更新日期：2009-01-01 00:00:00
abstract：:PC12 cells differentiated under the influence of the neuronal growth factor (NGF) serve as a model of both sympathetic neurons and chromaffin cells. NGF-induced differentiation critically depends on elevated intracellular calcium concentration. Main pathway for Ca²⁺ entry in excitable cells is represented by voltage-d...
journal_title：General physiology and biophysics
pub_type： 杂志文章
doi：10.4149/gpb_2014045
更新日期：2015-04-01 00:00:00
abstract：:A growing body of evidence supports the role of free radicals in triggering the functional and metabolic disturbances following transient cerebral ischemia. This study was designed to evaluate whether the extent of reperfusion-induced inhibition of protein synthesis initiation as well as tissue injury can be reduced b...
journal_title：General physiology and biophysics
pub_type： 杂志文章
doi：
更新日期：2004-12-01 00:00:00
abstract：:A new theory termed "tunnel-acid-group-potential" (TAGPT), explaining the effect of pHo and pH(i) on ion conductance through different membrane channels, is presented. It is suggested that shifts in pHo and pH(i) lead to changes in values of negative charges generated by acid groups of side chains of some polar (Glu-,...
journal_title：General physiology and biophysics
pub_type： 杂志文章,评审
doi：
更新日期：1996-10-01 00:00:00
abstract：:Hyperbaric oxygen treatment (HBO) could transiently reverse hypoxia during acute myocardial infarction (AMI). In order to evaluate whether early HBO can identify viable segments after AMI, improvement of wall motion score index (WMSI) after HBO was compared to dobutamine stress echocardiography (DSE). Thirty-one patie...
journal_title：General physiology and biophysics
pub_type： 临床试验,杂志文章
doi：
更新日期：2009-01-01 00:00:00
abstract：:Diabetes mellitus leads to bone disorders such as osteopenia and osteoporosis that can increase fracture risk. On the other hand, sodium tungstate is an inorganic compound which exerts anti-diabetic activity in experimental studies due to its suggested insulin-mimetic or antioxidant activity. Therefore this study was ...
journal_title：General physiology and biophysics
pub_type： 杂志文章
doi：10.4149/gpb_2014020
更新日期：2014-01-01 00:00:00
abstract：:The aim of the study was to examine the effects of epidermal growth factor (EGF) on ram sperm traits following hypothermic storage. Fresh ram ejaculates were diluted in Triladyl extender, pooled and divided into groups according to EGF doses added (0, 100, 200 or 400 ng/ml). Following 72-96 h storage at 4ºC, the sperm...
journal_title：General physiology and biophysics
pub_type： 杂志文章
doi：10.4149/gpb_2011_SI1_36
更新日期：2011-01-01 00:00:00
abstract：:Depression is a brain disorder characterized by severe emotional, cognitive, neuroendocrine and somatic dysfunction. Although the latest generation of antidepressant drugs has improved clinical efficacy and safety, the onset of their clinical effect is significantly delayed after treatment commencement, and a large nu...
journal_title：General physiology and biophysics
pub_type： 杂志文章,评审
doi：10.4149/gpb_2015013
更新日期：2015-10-01 00:00:00
abstract：:Cytochrome P-450 and NADPH: cytochrome P-450 reductase were solubilized by detergents from microsomal fraction of tulip bulbs Tulipa fosteriana L. and purified to electrophoretic homogeneity. The purification was achieved by anion-exchange column chromatography, hydroxyapatite-column chromatography and affinity chroma...
journal_title：General physiology and biophysics
pub_type： 杂志文章
doi：
更新日期：1994-04-01 00:00:00
abstract：:In P-gp-positive cell variants obtained from L1210 cells either by selection with vincristine (L1210/R) or by transfection with the human gene encoding P-gp (L1210/T), we have previously described cross-resistance to tunicamycin (TNM), a protein N-glycosylation inhibitor. Here we studied whether this cross-resistance ...
journal_title：General physiology and biophysics
pub_type： 杂志文章
doi：10.4149/gpb_2016039
更新日期：2016-10-01 00:00:00
