Abstract:
:Electrophysiological effects of bisaramil--a new antiarrhythmic drug under clinical trial--were investigated on isolated heart preparations, at a concentration range of 2.3-23 x 10(-6) M. Bisaramil dose dependently decreased the maximum rate of depolarization (Vmax), action potential amplitude (APA) and overshoot (OS) both in auricle and in papillary muscle of guinea-pig heart. There was no significant and obvious effect on the duration of the action potential and the resting membrane potential was also unchanged. Bisaramil slowed the spontaneous frequency of pacemaker cells in rabbit sinus node preparation due to its inhibitory effect on slow diastolic depolarization (SDD). Bisaramil was able to inhibit slow Ca(2+)-action potentials induced by isoprenaline on K(+)-depolarized papillary muscle. Results obtained with transmembrane current measurements revealed that bisaramil inhibited both fast Na(+)-current and slow Ca(2+)-current in frog sinoauricular fibres at the same concentration. Bisaramil with a mixed mode of the action seems to be a very promising drug.
journal_name
Pharmacol Resjournal_title
Pharmacological researchauthors
Paroczai M,Karpati E,Marko R,Kecskemeti Vdoi
10.1016/s1043-6618(05)80066-0subject
Has Abstractpub_date
1992-01-01 00:00:00pages
75-85issue
1eissn
1043-6618issn
1096-1186pii
S1043-6618(05)80066-0journal_volume
25pub_type
杂志文章abstract::A major focus of contemporary drug screening strategies is the identification of novel anticancer compounds, which often results in underutilization of resources. Current drug evaluation involves in vivo tumor (xenograft) regression as proof-of-principle for cytotoxicity (POC). However, this end-point lacks any assess...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2016.07.018
更新日期:2016-09-01 00:00:00
abstract::Myriocin, a potent inhibitor of serine palmitoyltransferase (SPT), has been shown to reduce plasma sphingolipids, cholesterol and triglycerides in hyperlipidemic apolipoprotein E knockout (apoE KO) mice. We hypothesized that the inhibition of sphingolipid biosynthesis modulates the composition of atherosclerotic plaqu...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2008.06.005
更新日期:2008-07-01 00:00:00
abstract::The molecular complexity of human breast cancer (BC) renders the clinical management of the disease challenging. Long non-coding RNAs (lncRNAs) are promising biomarkers for BC patient stratification, early detection, and disease monitoring. Here, we identified the involvement of the long intergenic non-coding RNA 0108...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2020.105249
更新日期:2020-11-01 00:00:00
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journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/1043-6618(94)80060-x
更新日期:1994-05-01 00:00:00
abstract::It has demonstrated that carteolol can increase the endothelium-dependent vasodilation induced by alpha-2 adrenergic agonist. In order to evaluate the effect of carteolol, and to clarify the mechanism, we examined the effects of 10 microM carteolol on the vasodilation induced by increasing doses (10(-7)-10(-4) M) of c...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/1043-6618(95)80038-7
更新日期:1995-05-01 00:00:00
abstract::Kidney disease is a frequent complication in diabetes, and significant differences have been reported between male and female patients. Our working hypothesis was that diabetes might modify the vascular actions of testosterone in isolated rabbit renal arteries and the mechanisms involved in these actions. Testosterone...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2009.09.002
更新日期:2010-02-01 00:00:00
abstract::As the capacity of the endogenous antioxidative system is limited, pharmacological treatment with antioxidants may help to protect neuronal tissue against increased amount of reactive oxygen species produced during oxidative stress. We attempted to improve resistance of rat hippocampal slices exposed to ischaemia in v...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2005.08.004
更新日期:2006-01-01 00:00:00
abstract::Local microcirculatory dysfunction within the pancreatic gland might be an important factor in the conversion of oedematous to necrotizing pancreatitis. Therapeutic agents, improving the pancreatic blood flow, might be valuable in acute pancreatitis treatment. An influence of nitric oxide, heparin and procaine treatme...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1006/phrs.1997.0200
更新日期:1997-08-01 00:00:00
abstract::In the past two decades, significant advances have been made in the etiology of lipid disorders. Concomitantly, the discovery of liporegulatory functions of certain short-chain fatty acids has generated interest in their clinical applications. In particular, butyric acid (BA) and its derivative, 4-phenylbutyric acid (...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1016/j.phrs.2019.04.002
更新日期:2019-06-01 00:00:00
abstract::The aim of this study is to investigate the acute haemodynamic effect of orally administered nisoldipine. Eight patients with stable angina and normal overall ventricular function were submitted to cardiac catheterization and angiography before and one hour after administration of nisoldipine 20 mg per os. Cardiac out...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/1043-6618(91)90089-g
更新日期:1991-10-01 00:00:00
abstract::The ataxin-2 binding protein 1 (A2BP1) gene is reported to be one of the susceptibility genes in schizophrenia, autism, and obesity. The aim of this study was to explore the association of A2BP1 gene polymorphisms with antipsychotic induced weight gain (AIWG) in Chinese Han population. Three hundred and twenty-eight p...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2015.06.003
更新日期:2015-09-01 00:00:00
abstract::The neurohormonal factor arginine vasopressin (AVP) produces potent systemic vasoconstriction as well as water retention in the kidneys via the V(1a) and V(2) receptors, respectively. Therefore, AVP may be considered as an aggravating factor of cardiac failure. In the present study, the effects of intravenous (i.v.) i...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/s1043661802002062
更新日期:2002-11-01 00:00:00
abstract::Rapid technological advances in genetics have created conceptual chaos regarding the genetics of drug response. Terms for differing concepts are used interchangeably: pharmacogenetics with pharmacogenomics, personalized medicine with personalized prescription. Biomarker has many definitions. The author prefers the con...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1016/j.phrs.2008.10.002
更新日期:2009-02-01 00:00:00
abstract::Myocardial infarction (MI) is a major cause of morbidity and mortality in western countries and the formation of intracoronary thrombi is recognized as a critical determinant of this ischaemic event. Since streptokinase and urokinase cause in vitro lysis of clots, it was though that these drugs were also effective in ...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1016/1043-6618(89)90233-8
更新日期:1989-03-01 00:00:00
abstract::A global transcriptional regulator, MgrA, was previously identified as a key determinant of virulence in Staphylococcus aureus. An 80% EtOH extract of Uncaria gambier was found to attenuate the virulence of S. aureus via its effects on MgrA. Using bioassay-guided fractionation, a polyphenolic polymer, uncariitannin, w...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2019.104328
更新日期:2019-09-01 00:00:00
abstract::In the present study the effect of ketamine, a dissociative anaesthetic, on the GABA- and on the specific GABAA-agonist muscimol-induced responses of the isolated guinea pig ileum was investigated. GABA as well as muscimol produce a concentration-dependent contractile effect on the duodenum, jejunum and ileum. The sen...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/1043-6618(95)80086-7
更新日期:1995-06-01 00:00:00
abstract::Oxidative stress is related to the progression of renal diseases and modulation of oxidative stress can lead to a reduction in vascular events in patients with chronic renal insufficiency (CRI). Indoxyl sulfate (IS) and xanthine oxidase (XO) are related to impaired neovasculogenesis in CRI. Hydralazine is suggested fo...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2019.104509
更新日期:2020-01-01 00:00:00
abstract::Green tea (Camellia sinensis, Theaceace) is the second most popular beverage in the world and has been extensively studied for its putative disease preventive effects. Green tea is characterized by the presence of a high concentrations of polyphenolic compounds known as catechins, with (-)-epigallocatechin-3-gallate (...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1016/j.phrs.2010.12.013
更新日期:2011-08-01 00:00:00
abstract::The metabolism of arachidonic acid by cytochrome P450 (CYP) epoxygenases generates epoxyeicosatrienoic acids (EETs) which affect numerous cellular process including Ca(2+) signaling and the activity of Ca(2+)-dependent K(+) channels. The expression of the CYP epoxygenase(s) that generate EETs in endothelial cells is n...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1016/j.phrs.2003.11.016
更新日期:2004-06-01 00:00:00
abstract::We have shown previously that the antitumor drug, hydroxyurea (HU) is able to induce dose-dependent increases in plasma corticosterone levels in the rat. The drug was administered early in the morning, when the levels of circulating glucocorticoids are low in this species. Normally, in humans under physiological condi...
journal_title:Pharmacological research
pub_type: 临床试验,杂志文章
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更新日期:2000-10-01 00:00:00
abstract::We have previously reported that the dopaminergic projection from A10 ventral tegmental neurons to the central amygdala is, in part, responsible for the facilitatory effect of angiotensin II (AII) and its 3-7 fragment [AII(3-7)] on the retrieval of information in memory motivated affectively and also on recognition me...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1006/phrs.1997.0257
更新日期:1997-11-01 00:00:00
abstract::The principle of mechanopharmacology of airway smooth muscle (ASM) is based on the premise that physical agitation, such as pressure oscillation applied to an airway, is able to induce bronchodilation by reducing contractility and softening the cytoskeleton of ASM. Although the underlying mechanism is not entirely cle...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1016/j.phrs.2020.104995
更新日期:2020-09-01 00:00:00
abstract::Low-doses of fenofibrate and dipyridamole have pleiotropic renoprotective actions in diabetic rats. This study investigated their combined effect relative to their individual treatments and lisinopril in rats with diabetic nephropathy. Streptozotocin (55mg/kg, i.p., once)-administered diabetic rats were allowed for 10...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2014.08.008
更新日期:2014-12-01 00:00:00
abstract::The epidemic of pneumonia (COVID-19) caused by novel coronavirus (SARS-CoV-2) infection has been listed as a public health emergency of international concern by the World Health Organization (WHO), and its harm degree is defined as a global "pandemic". At present, the efforts of various countries focus on the rapid di...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1016/j.phrs.2020.104929
更新日期:2020-08-01 00:00:00
abstract::Based on the role of ATG7 in the initiation of autophagy, autophagy can be divided into ATG7-dependent selective autophagy and ATG7-independent alternative autophagy. However, the detailed roles of two different types of autophagy in antitumor therapy have not been fully elucidated so far. Here, we for the first time ...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2020.105324
更新日期:2021-01-01 00:00:00
abstract::One of the most serious side effects of the immunosuppressive agent, cyclosporin A (CsA), is drug-related hypertension. As it is generally accepted, the sympathetic nervous system may play an important role in the development or maintenance of this abnormal pathophysiological situation. This study is aimed at assessin...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1006/phrs.1999.0572
更新日期:2000-02-01 00:00:00
abstract::Ocotea quixos essential oil was shown to possess significant inhibitory activity of platelet aggregation and clot retraction in rodent plasma. This study is aimed at fully characterizing the antiplatelet activity of the whole essential oil and its main components trans-cinnamaldehyde and methyl cinnamate also in human...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2006.09.009
更新日期:2007-01-01 00:00:00
abstract::Corticosteroids are shown to have deleterious effects on wound healing for various tissues. Arginine metabolism and nitric oxide (NO) synthesis play an important role in many aspects of inflammation and wound healing. The study was designed to evaluate the relationship of dexamethasone impaired healing of tracheal ana...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/s1043-6618(02)00130-5
更新日期:2002-09-01 00:00:00
abstract::Outbreak and pandemic of coronavirus SARS-CoV-2 in 2019/2020 will challenge global health for the future. Because a vaccine against the virus will not be available in the near future, we herein try to offer a pharmacological strategy to combat the virus. There exists a number of candidate drugs that may inhibit infect...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1016/j.phrs.2020.104859
更新日期:2020-07-01 00:00:00
abstract::Gastrointestinal toxicity and red skin discoloration were the major side effects observed in leprosy patients undergoing long-term treatment with clofazimine (CFZ). Hematological and biochemical alterations have been cited among other side effects; however, their real magnitude and clinical significance at the doses c...
journal_title:Pharmacological research
pub_type: 临床试验,杂志文章
doi:10.1016/s1043-6618(02)00086-5
更新日期:2002-08-01 00:00:00