Abstract:
:The electrophysiological and mechanical effects of HNS-32, a novel azulene-1-carboxamidine derivative with antiarrhythmic activity, were studied in isolated guinea-pig myocardial preparations. HNS-32 (10(-6)-10(-4) mol/l) concentration-dependently decreased the maximum rate of rise (V(max)) of action potential in isolated papillary muscle; the potency was the same or slightly higher than that of disopyramide. At 10(-4) mol/l, HNS-32 also shortened the action potential duration (APD) and depolarized the resting membrane potential; these effects were similar to those of 10(-5) mol/l verapamil. HNS-32 (10(-7)-10(-4) mol/l), as well as verapamil (10(-8)-10(-5) mol/l) and disopyramide (10(-6)-10(-3) mol/l), had concentration-dependent negative chronotropic and negative inotropic effects on isolated right atrial and right ventricular papillary muscle preparations, respectively. The concentration-response relationship for the positive chronotropic effect of isoproterenol was not affected by HNS-32 (10(-5) mol/l). In isolated ventricular myocytes, HNS-32 (10(-6)-10(-4) mol/l) concentration-dependently inhibited the peak amplitude of the L-type Ca(2+) current. These results suggest that NHS-32 has V(max) reducing activity on myocardial tissue, which may be responsible for antiarrhythmic effect. The drug may also have additional effect on the Ca(2+) channel at higher concentrations.
journal_name
Pharmacologyjournal_title
Pharmacologyauthors
Noguchi K,Kase J,Saitoh M,Masumiya H,Saitoh M,Nakazawa T,Tanaka Y,Tanaka H,Hashimoto K,Shigenobu Kdoi
10.1159/000056148subject
Has Abstractpub_date
2002-01-01 00:00:00pages
36-42issue
1eissn
0031-7012issn
1423-0313pii
pha64036journal_volume
64pub_type
杂志文章相关文献
PHARMACOLOGY文献大全abstract::The effect of sucralfate treatment (3 g daily for 6 weeks) on gastric HCO3- secretion was investigated in 15 duodenal ulcer patients. After treatment a highly significant (p less than 0.01) increase in gastric bicarbonate output was found. It is suggested that the mode of action of sucralfate includes stimulation of g...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000138136
更新日期:1985-01-01 00:00:00
abstract::There is an ongoing debate about possible advantages of the coadministration of caffeine with cyclooxygenase (COX) inhibitors in the treatment of pain. There are results suggesting interference by caffeine with COX expression and activity in rat immune cells. In the present study, we have used, therefore, human endoto...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000067742
更新日期:2003-02-01 00:00:00
abstract::The influence of repeated administration of histamine on lithium-induced state dependency has been investigated. A single-trial step-down inhibitory avoidance task was used to assess memory in adult male NMRI mice. Intraperitoneal (i.p.) administration of lithium (10 mg/kg), immediately after training (post-training),...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000111760
更新日期:2008-01-01 00:00:00
abstract::Although proton pump inhibitors (PPI) are generally well tolerated, with most adverse effects being minor and self-limiting, there are singular reports on hypersensitivity immune reactions triggered by a PPI or its metabolites. Here we report a case of acute drug-induced fever with leukocytosis and a transient increas...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000364781
更新日期:2014-01-01 00:00:00
abstract::The effects of alpha-adrenergic agonists on 45Ca efflux from slices of rat liver were studied and the results compared to earlier studies on the rabbit aorta. Norepinephrine and phenylephrine (PE) cause a stimulation of 45Ca efflux which was due to alpha 1-receptor activation. The mitochondrial uncoupler dinitrophenol...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000137952
更新日期:1984-01-01 00:00:00
abstract::Prior studies revealed an apparent bimodal distribution of adrenal xenobiotic-metabolizing activities in outbred guinea pigs. High activities were characteristic of most animals but a minority had very low rates of metabolism. The present studies were done to determine the basis for this distribution. Among the enzyma...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000028384
更新日期:2000-08-01 00:00:00
abstract::The temporal effects of vitamin A deficiency on hepatic cytochrome P-450-dependent and conjugation reactions were studied in the rat. Cytochrome P-450 levels and N-methyl-p-chloroaniline N-demethylase activity were significantly reduced in the deficient animals. No other changes in parameters dependent on cytochrome P...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000137457
更新日期:1980-01-01 00:00:00
abstract::This study was designed to determine whether pyrazinoylguanidine (PZG) can attenuate diabetic nephropathy in streptozotocin (STZ)-induced diabetic rats. Diabetes was induced within 1 week after a single intraperitoneal dose of STZ (45 mg/kg in 0.05 mol/l sodium citrate buffer). Diabetic rats were divided into five gro...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000139492
更新日期:1997-05-01 00:00:00
abstract::The absorption into the systemic circulation of compounds administered intraperitoneally in large volumes was investigated in the rat. The influence on absorption of molecular weight, lipid-water partition coefficient (K), and dissociation constant (pKa) was studied. Nine neutral compounds ranging in molecular weight ...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000136874
更新日期:1978-01-01 00:00:00
abstract::The effects of the novel antihypertensive agent, carvedilol, on renal hemodynamics and excretory function have been investigated and compared with the effects of labetalol in conscious, spontaneously hypertensive rats. Sustained intravenous infusion of carvedilol or labetalol at a rate of 10 micrograms/kg/min resulted...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000138719
更新日期:1990-01-01 00:00:00
abstract::The oral bioavailability of two investigational formulations of bicalutamide was compared with the current clinical formulation. The first formulation was amorphous R-/S-bicalutamide in solid dispersion with a polymeric matrix of hydroxypropyl methylcellulose phthalate (HP55S) (R-/S-bicalutamide/HP55S); the second was...
journal_title:Pharmacology
pub_type: 杂志文章,随机对照试验
doi:10.1159/000094599
更新日期:2006-01-01 00:00:00
abstract::A variety of prostaglandin synthetase inhibitors are cooxygenated during arachidonic acid peroxidation catalyzed by rat renal medulla prostaglandin synthetase or soybean lipoxygenase. Phenylbutazone, aminopyrine, 1,3-diphenylisobenzofuran, paracetamol, p-aminophenol, p-phenetidine and other o- and m-substituted aminop...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000137880
更新日期:1983-01-01 00:00:00
abstract::Zopiclone (ZPC; RP 27,267), which is chemically unrelated to benzodiazepines (BZD), was found to have a similar pharmacological profile and to possess in man hypnotic activity similar to that of some BZD such as nitrazepam. It was, therefore, interesting to study the interaction of ZPC with rat brain receptors and spe...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000137912
更新日期:1983-01-01 00:00:00
abstract::Glutathione S-transferases (GSTs) detoxify diverse electrophilic chemicals, including anticancer drugs. Containing at least 100 microM total GST, the adult rat liver has abundant alpha and mu class GST isoenzymes. We utilized primary cultured rat hepatocytes, maintained in chemically defined medium, to examine direct ...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000139312
更新日期:1995-06-01 00:00:00
abstract::The present study was carried out to test bioequivalence between two different oral desmopressin formulations. Sixty healthy volunteers were enrolled in the study and were randomly assigned to receive the test (T) and reference (R) drug in a two-period two-sequence, crossover, analyst-blinded study design. Subjects re...
journal_title:Pharmacology
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1159/000092625
更新日期:2006-01-01 00:00:00
abstract::The calcium channel antagonist, nifedipine (0.1 microM), only slightly inhibited the response to the full alpha 1-adrenoceptor agonist, (-)-norepinephrine, in rat aorta, but nearly completely inhibited the response to the partial alpha 1-adrenoceptor agonist, (-)-dobutamine, indicating that (-)-norepinephrine primaril...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000138906
更新日期:1992-01-01 00:00:00
abstract::We evaluated the effects of sodium alginate (AL-Na) on dextran sulfate sodium (DSS)- and 2,4,6-trinitrobenzene sulfonic acid (TNBS)-induced colitis in mice. DSS was added to the drinking water for 7 days. In another experiment, DSS was added to the drinking water for 5 days and DSS-free water was provided thereafter. ...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000353192
更新日期:2013-01-01 00:00:00
abstract:OBJECTIVE:The aim of this study was to investigate the effects of trichostatin A (TSA) on cervical cancer and the related mechanisms. METHODS:The HeLa and Caski cervical cancer cell lines were treated with different concentrations of TSA. Cell viability was measured by MTT assays. Cell apoptosis was analysed using flo...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000507937
更新日期:2020-11-03 00:00:00
abstract::In isolated perfused rat hearts with coronary occlusion and reperfusion, the effect of adenosine antagonists on the release of adenosine and its degradation products inosine, hypoxanthine, xanthine and uric acid was investigated. An antagonist with high selectivity for the A1 receptor, 8-phenyltheophylline, was applie...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000139444
更新日期:1996-11-01 00:00:00
abstract:BACKGROUND/AIMS:Serotonin (5-hydroxytryptamine, 5-HT)-induced contraction and the involvement of RhoA/Rho-kinase pathway in the 5-HT-induced contraction was investigated isometrically in vitro in both diabetic and nondiabetic human corpus cavernosum (HCC) tissues. METHODS:HCC tissues were obtained from 12 patients. Th...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000221380
更新日期:2009-01-01 00:00:00
abstract::The purpose of the study was to test the hypothesis that the postischemic neuronal damage is accompanied by changes of the electrocorticogram (ECoG) of freely moving rats during long-term recovery after forebrain ischemia. Ten minutes forebrain ischemia was induced in male Wistar rats. ECoG was recorded 1 day before a...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000139287
更新日期:1995-04-01 00:00:00
abstract::The relationship between alpha(1)-adrenoceptor binding in rat tissues and pharmacodynamic effects of continuous infusion of KMD-3213 was examined. In vivo specific binding of [(3)H]KMD-3213 after continuous intravenous infusion of the ligand (100 pmol/kg/min for 10 min, followed by 30 pmol/kg/min for 60 or 90 min) dif...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000056163
更新日期:2002-01-01 00:00:00
abstract::Desferrioxamine (DFO) metabolism and its pharmacokinetics were studied in a swine model using high-performance liquid chromatography. DFO and three iron-binding metabolites occurred in plasma. Interindividual differences in pharmacokinetics and metabolism were observed. Urine analysis in 4 pigs showed three iron-bindi...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000138730
更新日期:1990-01-01 00:00:00
abstract:BACKGROUND/AIMS:Functional linkages between the cannabinoid CB(1) and the dopaminergic systems have been reported although the observations and the mechanisms hypothesizing their interactions at the G protein-coupled receptor (GPCR) functionality level are conflicting. METHODS:Administration of a potent cannabinoid ag...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000335368
更新日期:2012-01-01 00:00:00
abstract::Hyaluronic acid (HA) is an important component of the extracellular matrix of prostate cells. Platelet-derived growth factor bb (PDGFbb) has a mitogenic effect on prostate stromal cells. The effect of PDGFbb on HA production by smooth muscle cells from normal and benign prostatic hyperplasia (BPH) tissue was studied t...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000056079
更新日期:2001-02-01 00:00:00
abstract::The effects of dietary taurine on lipid secretion and ketone body production were examined in the livers of Wistar and Sprague-Dawley rats fed high-cholesterol diets. The weight gain of the Sprague-Dawley rats tended to be higher than that of the Wistar rats, although food intake was comparable between the strains. Th...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000028343
更新日期:2000-01-01 00:00:00
abstract::Feeding a thiamin-deficient diet to male and female rats for 3 weeks alters the mixed function oxidases responsible for metabolizing benzo(a)pyrene and enhances the response of these enzymes to induction by phenobarbital or 3-methylcholanthrene. The caloric restriction observed in thiamin deprivation may be partially ...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000138004
更新日期:1984-01-01 00:00:00
abstract::Cathinone, the active principle of Catha edulis (khat), shows long-lasting analgesic effects when the tail-flick test is used in rats. The involvement of monoamines, endogenous opioids and stress in this analgesic effect was tested. Both early (30 min) and late (24 h) analgesic effects of cathinone were prevented by r...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000138023
更新日期:1984-01-01 00:00:00
abstract::The effect of fenfluramine, administered orally in a daily dose of 1 mg/kg for 40 days, on the disposition and rate of elimination of antipyrine was studied in 15 obese patients. Although the plasma half-life of antipyrine was unchanged, the apparent volume of distribution (1/kg) fell by 11.6% (p less than 0.001) and ...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000136880
更新日期:1975-01-01 00:00:00
abstract::Renal hypoperfusion which occurs in hemorrhagic shock creates an environment in which cellular injury and organ dysfunction can occur during the episode of shock as well as reoxygenation and reperfusion. At the same time, mast cell degranulation which is observed during hemorrhage may have an additional deleterious ef...
journal_title:Pharmacology
pub_type: 杂志文章
doi:10.1159/000139097
更新日期:1993-09-01 00:00:00