Abstract:
:The use-dependent effects of bunazosin on the maximal rate of rise (Vmax) of the action potential and conduction velocity were studied in isolated papillary muscles of guinea-pig. Standard microelectrode techniques were used to monitor the conduction and action potential of the muscles. In the presence of 30 microM bunazosin, the time constants for the start of the use-dependent inhibition of Vmax during a 0.2, 1, 2 and 3 Hz stimulation were (means +/- S.E.M. in s) 30.9 +/- 8.0, 15.0 +/- 1.6, 7.4 +/- 0.9 and 3.9 +/- 0.7 (n = 4) and those for conduction velocity were 17.3 +/- 2.3, 17.3 +/- 5.2, 6.5 +/- 0.9 and 3.4 +/- 0.2, respectively. These results showed that in the cardiac ventricular muscle of the guinea-pigs, bunazosin produces use-dependent changes in conduction velocity with onset kinetics comparable to those measured simultaneously using Vmax. The characteristics of the use-dependent inhibition of conduction velocity induced by bunazosin are similar to those found with slow kinetic drugs such as disopyramide rather than with fast ones.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Hasegawa J,Noguchi N,Sawaguchi M,Doi T,Hisatome I,Kotake H,Mashiba Hdoi
10.1016/0014-2999(90)94170-3subject
Has Abstractpub_date
1990-12-04 00:00:00pages
369-73issue
3eissn
0014-2999issn
1879-0712pii
0014-2999(90)94170-3journal_volume
191pub_type
杂志文章abstract::Endogenous D-serine is known to modulate glutamatergic transmission via interaction with the glycine site of N-methyl-D-aspartate (NMDA) receptors. D-serine is synthesized by racemization of L-serine using an enzymatic reaction catalyzed by serine racemase. Although much attention has been focused on the role of D-ser...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2012.09.011
更新日期:2012-12-05 00:00:00
abstract::To evaluate the possible role of 5-HT 1A and 5-HT 2A receptors in the anticonvulsant effect of swim stress, mice were pre-treated with agonists and antagonists of these receptors prior to exposure to stress and the intravenous infusion of picrotoxin. 8-OH-DPAT ((+/-)-8-hydroxy-2-(di-n-propylamino) tetralin) and WAY-10...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2005.10.021
更新日期:2005-12-19 00:00:00
abstract::Ischemic postconditioning (IPO) had been reported as a promising method against myocardial ischemia-reperfusion (I/R) injury, but IPO was later proved with poor clinical benefit. In this study, we compared the protective effects of pinacidil-postconditioning (PPO) and IPO against myocardial I/R injury. Langendorff rat...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2016.03.027
更新日期:2016-06-05 00:00:00
abstract::The effects of 1,4-dihydropyridine derivatives on divalent cation transients and catecholamine release stimulated by either high K+ or the nicotinic receptor agonist dimethyl-phenyl-piperazinium (DMPP) have been compared in bovine adrenal chromaffin cells. The activation of Ca2+ entry pathways was followed by measurin...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0922-4106(93)90078-n
更新日期:1993-10-15 00:00:00
abstract::Airway responsiveness to histamine, substance P, methacholine and bilateral electrical vagal stimulation was assessed in capsaicin-treated and control guinea pigs. In animals treated with capsaicin (50 mg/kg s.c.) 7 days before experiments, airway responsiveness to histamine, substance P and vagal stimulation was sign...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(90)90148-y
更新日期:1990-01-03 00:00:00
abstract::Bilateral injections of alpha-methylnoradrenaline into the area of the nucleus tractus solitarii of the brain stem caused a dose-dependent decrease of systemic arterial blood pressure and heart rate of anesthetized rats. The effects were prevented and even reversed by a preceding injection of the alpha-adrenoceptor bl...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(75)90305-2
更新日期:1975-06-01 00:00:00
abstract::Metabotropic glutamate mGlu(1) receptors play a modulatory role in the nervous system. They enhance cell excitability, modulate synaptic neurotransmission and are involved in synaptic plasticity. During the last 10 years, several selective metabotropic glutamate mGlu(1) receptor competitive antagonists and potentiator...
journal_title:European journal of pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.ejphar.2009.12.043
更新日期:2010-08-10 00:00:00
abstract::The effects of conditioned fear on gross activity, heart rate, PQ interval, noradrenaline and adrenaline were studied in freely moving rats. Subcutaneous (s.c.) injections of atropine methyl nitrate (0.5 mg/kg) during rest resulted in a significant shortening of the PQ interval, indicating that the PQ interval can be ...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(98)00261-1
更新日期:1998-06-05 00:00:00
abstract::The open field is a very popular animal model of anxiety-like behavior. An overview of the literature on the action elicited by effective or putative anxiolytics in animal subjected to this procedure indicates that classical treatments such as benzodiazepine receptor full agonists or 5-HT(1A) receptor full or partial ...
journal_title:European journal of pharmacology
pub_type: 杂志文章,评审
doi:10.1016/s0014-2999(03)01272-x
更新日期:2003-02-28 00:00:00
abstract::B cell antigen presentation, cytokine production, and antibody production are targets of pharmacological intervention in inflammatory and infectious diseases. Here we review recent pre-clinical evidence demonstrating that pharmacologically relevant levels of n-3 polyunsaturated fatty acids (PUFA) derived from marine f...
journal_title:European journal of pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.ejphar.2015.03.100
更新日期:2016-08-15 00:00:00
abstract::MK-886, an inhibitor of the 5-lipoxygenase-activating protein (FLAP), potently suppresses leukotriene biosynthesis in intact cells and is frequently used to define a role of the 5-lipoxygenase (EC 1.13.11.34) pathway in cellular or animal models of inflammation, allergy, cancer, and cardiovascular disease. Here we sho...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2009.02.023
更新日期:2009-04-17 00:00:00
abstract::Secondary hyperparathyroidism is a common complication in patients with chronic kidney disease and frequently persists after kidney transplantation. Paricalcitol, a selective vitamin D receptor activator, is indicated in the management of this disorder and recent evidences have suggested that this drug has other benef...
journal_title:European journal of pharmacology
pub_type: 杂志文章,随机对照试验
doi:10.1016/j.ejphar.2013.03.040
更新日期:2013-06-05 00:00:00
abstract::Preparations of cauda epididymides were taken from rats unilaterally vasectomised by medial transection of the vas deferens. Responses of preparations from the operated side to field stimulation (10 pulses, 70 V, 1 ms, 0.1-20 Hz) declined in parallel with decreases in catecholamine fluorescence. There were leftward sh...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(89)90315-4
更新日期:1989-12-19 00:00:00
abstract::Pituicytes, the astrocytic glial cells of the neural lobe, are known to secrete interleukin-6 and nitric oxide upon stimulation with various inflammatory mediators, i.e. interleukin-1beta. Nitric oxide is described to modulate the secretion of interleukin-6 in various cell types. The aim of the present study was to in...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2005.06.045
更新日期:2005-09-05 00:00:00
abstract::Several major antiepileptic drugs, including carbamazepine, phenytoin and phenobarbital, induce xenobiotic metabolizing enzymes via activation of nuclear receptors, including pregnane X receptor (NR1I2) and constitutive androstane receptor (NR1I3). Via activation of these xenobiotic sensors, antiepileptic drugs may al...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2009.11.051
更新日期:2010-02-25 00:00:00
abstract::The aim of the present study was to find out the mechanism by which the inflammatory mediator, bradykinin, induces an increase of the cytosolic Ca(2+) concentration ([Ca(2+)](i)) in enteric neurons. For this purpose, ganglia in the isolated submucosa from rat colon were loaded with the Ca(2+)-sensitive dye, fura-2, an...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2012.02.001
更新日期:2012-04-15 00:00:00
abstract::Our recent clinical study indicated that etidronate may inhibit the progression of aortic calcification in hemodialysis patients. To determine whether etidronate inhibits aortic calcification in renal failure rats, renal failure was induced by subtotal nephrectomy, in which 5/6 of the kidneys were removed. Significant...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2006.12.006
更新日期:2007-03-08 00:00:00
abstract::We have examined the effect of ropivacaine, a local anesthetic, on leukocyte-endothelium interactions induced by tumor necrosis factor-alpha (TNF-alpha) in vivo by the use of intravital microscopy in the mouse cremaster microcirculation. It was found that ropivacaine markedly reduced venular leukocyte adhesion and tis...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(00)00108-4
更新日期:2000-03-24 00:00:00
abstract::The muscarinic agonists, xanomeline and carbachol, displayed similar intrinsic activities in stimulating neuronal nitric oxide synthase at muscarinic M1 receptors in Chinese hamster ovary (CHO) cells, with xanomeline being more potent. Pre-incubation (1 h) with 1 microM xanomeline, followed by extensive washing, resul...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(97)01162-x
更新日期:1997-09-03 00:00:00
abstract::It has been shown that α(2)-adrenoceptors mediate vasopressor responses in pithed rats. However, the corresponding α(2)-adrenoceptor subtypes have not been pharmacologically identified. Thus, this study set out to identify the specific subtypes (α(2A), α(2B) and α(2C)) mediating the vasopressor responses to the α(2)-a...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2012.06.011
更新日期:2012-09-15 00:00:00
abstract::Dietary fish oils rich in n-3 polyunsaturated fatty acids can modulate a diverse range of factors contributing to cardiovascular disease. This study examined the relative roles of eicosapentaenoic acid (20:5 n-3; EPA) and docosahexaenoic acid (22:6 n-3; DHA) which are the principal n-3 polyunsaturated fatty acids rega...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(95)00861-6
更新日期:1996-04-04 00:00:00
abstract::In the present study we examined the effect of the cannabinoid receptor agonist, [[1 a,2-(R)-5-(1,1-dimethylheptyl)-2-[5-hydroxy-2-(3-hydroxypropyl)cyc lohexyl]-phenol; CP 55,940] on [14C]acetylcholine and [3H]norepinephrine release from hippocampal slices and on [14C]acetylcholine release from striatal slices. CP 55,...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(97)00082-4
更新日期:1997-04-18 00:00:00
abstract::CPP, administered systemically, elicited four distinct responses characteristic of serotonin-receptor activation in the central nervous system. The crossed extensor reflex in the acutely spinalized rat was enhanced by treatment with CPP, 1-16 mg/kg. CPP, 1.11-10 mg/kg, elicited a dose-related increase in head twitches...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(77)90117-0
更新日期:1977-07-01 00:00:00
abstract::Crocetin, an aglycone of crocin, is found both in the saffron crocus (Crocus starus L.) and in gardenia fruit (Gardenia jasminoides Ellis). We evaluated the protective effects of crocetin against the retinal ischemia induced by 5h unilateral ligation of both the pterygopalatine artery (PPA) and the external carotid ar...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2013.02.007
更新日期:2013-03-05 00:00:00
abstract::N-Methyl-D-aspartate (NMDA)-induced pial artery dilation is reversed to vasoconstriction following fluid percussion brain injury (FPI). This study investigated the contribution of activation of protein tyrosine kinase (PTK) and the extracellular signal-regulated kinase (ERK) and p38 isoforms of mitogen-activated prote...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/s0014-2999(03)02012-0
更新日期:2003-08-08 00:00:00
abstract::The kappa-opioid receptor agonist, U50,488H (trans-(+-)-3,4-dichloro-N-methyl-[2-(1-pyrrolidinyl)-cyclohexyl]- benzeneacetamide), has recently been reported to induce dystonia after s.c. administration of 5-10 mg/kg in guinea pigs. The dystonic movements observed in response to U50,488H resembled those previously repo...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(93)90600-m
更新日期:1993-05-19 00:00:00
abstract::3H-Mepyramine (3H-MEP) binds to slide-mounted tissue sections with characteristics indicating the labelling of a H1-histamine receptor. It is saturable (Bmax 12 pg/g tissue), of a high affinity (KD 0.5 mM) and possesses a drug specificity similar to that observed for H1 receptors in a variety of systems. In agreement ...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(79)90478-3
更新日期:1979-10-01 00:00:00
abstract::A substantial barrier to the treatment of Opioid Use Disorder (OUD) is the elevated relapse rates in affected patients, and a significant contributor to these events of relapse is exposure to cues and contexts that are intensely associated with prior drug abuse. The neurotransmitter dopamine plays a key role in reward...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/j.ejphar.2020.173638
更新日期:2020-12-15 00:00:00
abstract::The specific binding of [3H]desipramine to various brain regions and peripheral tissues of the rat was of high affinity, rapid and reversible. It was inhibited with high affinity only by tricyclic antidepressants and noradrenaline uptake blockers. There was a highly significant correlation between the potencies of a s...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(82)90036-x
更新日期:1982-03-12 00:00:00
abstract::It has been shown that the pancreatic beta-cell monoamines are located in the secretory granules, and that they have an inhibitory influence on insulin secretion. Monoamines are inactivated by the enzyme, monoamine oxidase. We now studied in vivo the relation between adrenergic and cholinergic stimulation, insulin sec...
journal_title:European journal of pharmacology
pub_type: 杂志文章
doi:10.1016/0014-2999(93)90063-n
更新日期:1993-03-23 00:00:00