Abstract：
:Concentration-relaxation curves for pinacidil and cromakalim were obtained in isolated guinea-pig tracheas contracted by histamine. Pinacidil produced complete relaxation with an EC50 value of 2.8 microM. The antidiabetic sulfonylurea, glibenclamide (0.1, 1, 10 microM), caused concentration-dependent rightward shifts (3- to 16-fold) of the concentration-relaxation curve for pinacidil without changing the maximal relaxant response. Cromakalim produced 85% relaxation with an EC50 value of 1.1 microM. Glibenclamide (0.1 microM) displaced the concentration-relaxation curve to the right and at higher concentrations (1-10 microM) caused nearly complete suppression of the maximal relaxant response to cromakalim. Glibenclamide not only prevented the effects of pinacidil and cromakalim but also produced a concentration-dependent and complete reversal of submaximal relaxations produced by these drugs. Glibenclamide was a selective antagonist of the relaxation of airway smooth muscle induced by pinacidil and cromakalim. Concentration-relaxation curves for theophylline, terbutaline and verapamil were unaffected by glibenclamide.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Nielsen-Kudsk JE,Bang L,Brønsgaard AMdoi
10.1016/0014-2999(90)90312-tsubject
Has Abstractpub_date
1990-05-16 00:00:00pages
291-6issue
2-3eissn
0014-2999issn
1879-0712pii
0014-2999(90)90312-Tjournal_volume
180pub_type
杂志文章abstract：:The role of substance P in the cerebral parenchymal circulation was examined in 19 anesthetized cats. The local cerebral blood volume in the temporoparietal cortex was measured by our photoelectric method. Cerebral blood volume reflects the cumulative dimensions of the parenchymal microvessels. Intravenous injection o...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(96)00725-x
更新日期：1996-12-19 00:00:00
abstract：:Four analogues of Phe-Leu-Phe-Gln-Pro-Gln-Arg-Phe-NH2, a mammalian FMRFamide-like peptide with antiopiate properties, were synthesized with N-terminus modifications and were shown to have high affinity for F8Famide binding sites. The degradation rate of these analogues in mouse brain slices was 3 times lower than that...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(92)90463-e
更新日期：1992-11-03 00:00:00
abstract：:The high-level production of nitric oxide (NO) induced by inflammatory cytokines has been shown to play a key role in the pathogenesis of inflammation-mediated osteoporosis. In the present work, we observed that 1mM of the NO donor sodium nitroprusside (SNP) induced an increase of the cytosolic calcium concentration (...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2013.05.009
更新日期：2013-09-05 00:00:00
abstract：:We have shown that the major active agent of Cannabis sativa, Delta(9)-tetrahydrocannabinol, activates peroxisome proliferator-activated receptor gamma [PPARgamma, O'Sullivan, S.E., Tarling, E.J., Bennett, A.J., Kendall, D.A., Randall, M.D., 2005c. Novel time-dependent vascular actions of delta9-tetrahydrocannabinol m...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2009.03.010
更新日期：2009-06-10 00:00:00
abstract：:The present study was carried out to investigate the possibility that noradrenaline (NA) and neuropeptide Y (NPY) are co-released after afferent vagal or saphenous stimulation (1, 5, 10 and 20 Hz) in chloralose-anaesthetized dogs. Electrical stimulation of the vagus elicited an increase in plasma NA levels for the 5, ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(92)90249-4
更新日期：1992-03-17 00:00:00
abstract：:The effects of ketamine and barbiturates (pentobarbital, thiopental, methohexital) were studied in an isolated rabbit Langendorff preparation. All agents tested depressed contractility. Ketamine, as well as the lipophilic barbiturates (thiopental, methohexital), caused a relatively greater depression at higher pacing ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(79)90025-6
更新日期：1979-10-26 00:00:00
abstract：:Two highly selective mu-opioid receptor agonists, endomorphin-1 and endomorphin-2, have been identified and postulated to be endogenous ligands for mu-opioid receptors. Intrathecal (i.t.) administration of endomorphin-1 and endomorphin-2 at doses from 0.039 to 5 nmol dose-dependently produced antinociception with the ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(01)01238-9
更新日期：2001-09-21 00:00:00
abstract：:"Non-adrenoceptor'-binding sites for [3H]clonidine (I1-sites) and [3H]idazoxan (I2-sites) are identified in calf striatum membranes. The pharmacological profile of both subtypes was investigated by competition binding with the imidazolines idazoxan, cirazoline, Bu 224 (2-(4,5-dihydroimidaz-2-yl)-quinoline) and Bu 239 ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(96)00575-4
更新日期：1996-11-07 00:00:00
abstract：:Prenatal exposure to different doses (0.25, or 0.5 or 1.0 mg/kg corresponding to 1/320 th or 1/160 th or 1/80 th of LD50) of deltamethrin to the pregnant Wistar rats from gestation day 5 to 21 were found to produce a dose dependent increase in the activity of cytochrome P450 (CYP) dependent 7-ethoxyresorufin-O-deethyl...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2006.06.042
更新日期：2006-08-21 00:00:00
abstract：:Endothelial dysfunction ensuing inhibition of nitric oxide synthase (NOS) was investigated in male Sprague-Dawley rats given N(omega)-nitro-L-arginine methyl ester (L-NAME) in drinking water for 8 weeks. Age-matched rats served as controls. L-NAME-treated rats, as compared to control animals, showed: (1) a clear-cut i...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(02)02046-0
更新日期：2002-08-16 00:00:00
abstract：:In male Swiss mice, muscimol produced myoclonic jerks. A 3 mg/kg (i.p.) dose induced this response in all of the mice tested and the peak response of 73 jerks per min was observed between 27 and 45 min. Increasing the brain serotonin levels by the administration of 5-hydroxytryptophan (80-160 mg/kg) in combination wit...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(81)90087-x
更新日期：1981-07-17 00:00:00
abstract：:The vasoinhibitory effects of MCI-154 (MCI), a new pyridazione derivative, on contractile responses to alpha 1- and alpha 2-adrenoceptor agonists were examined in isolated rabbit aorta. MCI (10(-8)-10(-5) M) inhibited the maximum contractile responses to clonidine and BHT-920 (BHT) in a concentration-dependent manner,...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(88)90222-1
更新日期：1988-01-12 00:00:00
abstract：:The effects of histamine H(1) receptor antagonists (promethazine, diphenhydramine, chlorphenilamine and triprolidine) on hippocampal theta rhythm during eight-arm radial maze performance were investigated using rats. Promethazine showed a significant increase in the number of total errors and working memory errors at ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2007.08.020
更新日期：2007-12-08 00:00:00
abstract：:It is known that low-dose aspirin is effective in coronary artery therapy, although it has not yet been clarified how it exerts its action. Here, we report that treatment of coronary artery patients with 100 mg/day of aspirin does not attenuate thrombin generation, but reduces free thrombin by favouring the formation ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(02)02925-4
更新日期：2003-01-26 00:00:00
abstract：:Quantitative in vitro autoradiographic techniques were used to localize and characterize 125I-labelled human calcitonin gene-related peptide ([125I]hCGRP) binding sites in sections of bovine left anterior descending coronary artery (LAD). Specific high affinity (Kd 0.4 nM) [125I]hCGRP binding sites were localized to t...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(92)90483-k
更新日期：1992-09-04 00:00:00
abstract：:Long-term treatment with sodium barbital did not alter significantly the responsiveness of the isolated rat vas deferens to noradrenaline. However, three days after barbital withdrawal there was a 4.5-fold increase in the sensitivity and an enhanced maximum response to the neurotransmitter. Pharmacological analysis of...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(82)90550-7
更新日期：1982-08-13 00:00:00
abstract：:The anti-cancer effects of dioscin have been widely reported. However, its effect on laryngeal cancer remains unknown. In the present paper, our results showed that dioscin markedly caused cell apoptosis and DNA damage, increased reactive oxygen species (ROS) level, induced S-phase arrest, and inhibited invasion of hu...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2016.02.009
更新日期：2016-03-05 00:00:00
abstract：:The preparation and the biological activities of the four stereoisomers of 3-[5-(3-amino-1,2,4-oxadiazol)yl]-1-azabicyclo[2.2.1]heptane are described. The most potent stereoisomer, 3a, has the 3R,4R configuration, and in vitro activities in (pD2(% efficacy): ileum 8.8 (87%), hippocampus 9.8 (116%) and ganglion 10.2 (3...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0922-4106(92)90049-2
更新日期：1992-08-03 00:00:00
abstract：:Adenosine relaxes the coronary arteries of various species through A2 receptors. The mechanism(s) by which adenosine causes relaxation of the coronary smooth muscle through changes in intracellular Ca levels is not understood. Therefore, the aim of this study was to evaluate the vasodilatory action of adenosine in nor...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(89)90040-x
更新日期：1989-01-02 00:00:00
abstract：:The rapid breakout of the coronavirus disease of 2019 (COVID-19) has been declared pandemic with serious global concern due to high morbidity and mortality. As we enter the phase beyond limitations there is an urgent need for explicit treatment against COVID-19. To face this immediate global challenge, drug developmen...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2020.173496
更新日期：2020-10-15 00:00:00
abstract：:Posttraumatic nerve recovery remains a challenge in regenerative medicine. As such, there is a need for agents that limit nerve damage and enhance nerve regeneration. Here we investigate rosuvastatin, a 3-hydroxy-3-methylglutaryl coenzyme (HMG-CoA) reductase inhibitor, with anti-inflammatory and antioxidant properties...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2020.173260
更新日期：2020-09-05 00:00:00
abstract：:Pentoxifylline (PTX), a non-specific inhibitor of cAMP phosphodiesterases, is commonly used for treatment of peripheral vascular disorders although its direct action on endothelial cells is not well described. The aim of this study was to determine the influence of PTX on tubule formation and mRNA expression for angio...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2018.03.015
更新日期：2018-05-15 00:00:00
abstract：:Dichlorobenzamil, phenamil and other amiloride analogs (1-100 microM) elicit transient tension in rabbit skinned muscle fibers. Tension requires preloading of Ca(2+) into the sarcoplasmic reticulum, is facilitated by low-[Mg(2+)] solutions, abolished by ruthenium red or by functional disruption of the sarcoplasmic ret...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(00)00058-3
更新日期：2000-03-10 00:00:00
abstract：:Dihydralazine (0.1 mg/kg), injected intravenously into male Sprague-Dawley rats, caused a decrease in mean arterial blood pressure and an increase in renal plasma flow, while urine volume remained unchanged. Dihydralazine had no effect on kallikrein excretion in the urine and on kallikrein activity in the renal cortex...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(82)90239-4
更新日期：1982-02-26 00:00:00
abstract：:Peptide YY (1-36) and peptide YY (3-36) are gut-derived hormones which are involved in feeding control in the hypothalamus. The hypothalamic mechanisms of feeding have been shown to be modulated by aminergic neurotransmitters, which could mediate the anorectic or orexigenic effects of neuropeptides and hormones. We ha...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2005.07.008
更新日期：2005-09-05 00:00:00
abstract：:Local infusions of PYY (3-100 pmol.min-1) caused a slowly developing vasoconstriction of a long duration in the cat submandibular salivary gland. The vasoconstrictor action of PYY was also present after alpha-adrenoceptor blockade and in sympathectomized animals. Local APP infusions caused only weak vasoconstriction. ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(82)90300-4
更新日期：1982-09-10 00:00:00
abstract：:(±)-3,4-Methylenedioxymethamphetamine (MDMA) is an illicit drug that evokes transporter-mediated release of serotonin (5-HT) in the brain. 5-HT transporter (SERT) proteins are also expressed in non-neural tissues (e.g., blood), and evidence suggests that MDMA targets platelet SERT to increase plasma 5-HT. Here we test...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2011.10.033
更新日期：2012-01-15 00:00:00
abstract：:It had previously been shown that D-phenylalanine and hydrocinnamic acid, two in vitro inhibitors of carboxypeptidase A, possess an analgesic action when injected i.p. in mice. We have studied the in vivo effects of indole-3-acetic acid, another carboxypeptidase A inhibitor, and of the following analogs of D-phenylala...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(85)90164-5
更新日期：1985-10-22 00:00:00
abstract：:Calcitonin gene-related peptide (CGRP) is a highly potent vasodilator known to be involved in many physiological functions within the cardiovascular, gastrointestinal, immune, and nervous systems. This study assessed the desensitization of CGRP receptors by measuring agonist-mediated activation of adenylate cyclase in...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2007.08.014
更新日期：2007-12-22 00:00:00
abstract：:The prefrontal cortex and the mediodorsal thalamic nucleus are reciprocally connected through excitatory amino acid pathways. Cortical excitatory responses resulting from activation of either the mediodorsal thalamic nucleus-prefrontal cortex pathway (short latency) or the recurrent collaterals of prefrontal cortex-me...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(95)00377-w
更新日期：1995-10-04 00:00:00
