Abstract：
:The actions of dequalinium have been investigated in cultured rat sympathetic neurones. It produced a rapid and reversible inhibition of the slow apamin-sensitive component of the afterhyperpolarization (AHP) which follows a single action potential in these cells. The IC50 for this effect was 1.1 microM and in voltage clamp experiments, 1 microM dequalinium produced 45% inhibition of the underlying current IAHP. When the small conductance Ca(2+)-activated K+ channels were blocked by 20 nM apamin the slow component of the AHP was abolished, and dequalinium (10 microM) produced no further change in the residual AHP. Dequalinium (10 microM) had no effect on the voltage-activated Ca2+ current in these cells, suggesting that the inhibition of the AHP was the result of a direct interaction with the K+ channels. The A-current as well as a composite current made up of IK and IC were all unaffected by 10 microM dequalinium. However, at this concentration it did produce 18% inhibition of the M-current. These results show dequalinium to be a potent and selective non-peptide blocker of the apamin-sensitive small conductance Ca(2+)-activated K+ channel in rat sympathetic neurones.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Dunn PMdoi
10.1016/0014-2999(94)90596-7subject
Has Abstractpub_date
1994-02-03 00:00:00pages
189-94issue
2eissn
0014-2999issn
1879-0712pii
0014-2999(94)90596-7journal_volume
252pub_type
杂志文章abstract：:In this study, rutaecarpine was tested for its antiplatelet activities in human platelet-rich plasma. In human platelet-rich plasma, rutaecarpine (40-200 microM) inhibited aggregation stimulated by a variety of agonists (i.e., collagen, ADP, adrenaline and arachidonic acid). The antiplatelet activity of rutaecarpine (...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(96)00789-3
更新日期：1996-12-30 00:00:00
abstract：:The contribution of tyrosine kinase activity to vasoreactivity in normotensive Wistar-Kyoto (WKY) and spontaneously hypertensive (SHR) rats was investigated on isolated aortic preparations by the use of two tyrosine kinase inhibitors: methyl-2,5-dihydroxycinnamate (30 microM) and genistein (30 microM). The pretreatmen...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(99)00304-0
更新日期：1999-06-11 00:00:00
abstract：:Recent studies suggested the involvement of the endocannabinoid pathway on insulin secretion in RINm5F cells or rat islets. Animal and clinical studies have reported beneficial effects of the selective cannabinoid 1 receptor antagonist rimonabant on glucose homeostasis. The aim of this study was to investigate the in ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2009.05.024
更新日期：2009-08-15 00:00:00
abstract：:Intravenous amiodarone (Amiodarone i.v.) is widely used to treat cardiac arrhythmias. The most frequent clinical adverse event associated with Amiodarone i.v. administration is systemic hypotension which has been attributed to the cosolvents used in the formulation, polysorbate 80 and benzyl alcohol. To minimize hypot...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2009.02.009
更新日期：2009-04-01 00:00:00
abstract：:The binding of [3H]LSD to serotonergic sites in human brain was studied. The pharmacological profile of [3H]LSD binding in frontal cortex differed to that in hippocampus. Analysis of the inhibition of [3H]LSD binding by serotonin and spiperone was consistent with the presence of two binding sites, which differed in ph...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(82)90555-6
更新日期：1982-08-13 00:00:00
abstract：:Many atypical antipsychotic drugs, such as olanzapine, induce significant weight gain. However, ziprasidone produces minimal weight gain, the mechanism of which remains unclear. The aim of the present study was to investigate whether ziprasidone would reduce the acute effect of olanzapine on feeding behaviour. The res...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2004.10.015
更新日期：2004-11-28 00:00:00
abstract：:Using urethane-anesthetized rats, we examined whether an activation of nuclear factor kappa B is involved in the corticotropin-releasing factor-induced increase in plasma levels of catecholamines. An intracerebroventricularly administered corticotropin-releasing factor (1.5 nmol/animal)-induced increase of plasma cate...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2008.01.037
更新日期：2008-04-14 00:00:00
abstract：:The membrane of bullfrog sympathetic ganglion cells was hyperpolarized by a direct action of ACh (more than 0.5 mM) in a solution containing both nicotine (0.24 mM) and atropine (0.14 mM). This ACh hyperpolarization could be imitated by neither carbachol nor bethanechol, suggesting that the ACh hyperpolarization was t...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(75)90050-3
更新日期：1975-04-01 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(97)01189-8
更新日期：1997-09-24 00:00:00
abstract：:Apolipoprotein B (ApoB) of low-density lipoprotein (LDL) causes endothelial dysfunction in the initial stage of atherogenesis. The present study was designed to explore the underlying molecular mechanisms involved. Rat mesenteric arteries were organ cultured in the presence of different concentrations of ApoB or LDL. ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2014.01.008
更新日期：2014-02-15 00:00:00
abstract：:The origin of the thrombocytopenia and leucopenia induced by protamine-heparin complexes is unknown. We studied the biochemical and cellular effects of protamine (6 mg x kg-1, i.v.) injected after heparin (5 mg x kg-1, i.v.) in New Zealand rabbits. After protamine injection (0.5 min) increases in blood platelet-activa...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(96)00069-6
更新日期：1996-04-29 00:00:00
abstract：:Attempts were made to find whether [3H]batrachotoxinin A 20-alpha-benzoate provides a specific probe for measuring interactions of local anesthetics with the sodium channel complex. [3H]Batrachotoxinin A 20-alpha-benzoate binding, [14C]guanidine and 22Na uptake were investigated in rat brain crude synaptosomal prepara...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(86)90230-x
更新日期：1986-05-27 00:00:00
abstract：:We have developed a model of ischaemia-reperfusion injury in C57BL/6 mice involving ischaemia for 0.5 to 2.5 h with an elastic tourniquet on one hind limb and reperfusion for 24 h, analogous to a well-established model of ischaemia-reperfusion injury in the rat. Viability was assessed in tissue homogenates of the gast...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(97)01101-1
更新日期：1997-08-13 00:00:00
abstract：:In the presence of l-serine borate, salbutamol was much more effective in reversing rather than preventing LTC4-induced contractions of guinea-pig trachea. This suggests that different mechanisms are involved in initiating versus maintaining LTC4-induced contractions. In addition, the ability of salbutamol pretreatmen...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(86)90066-x
更新日期：1986-07-31 00:00:00
abstract：:Migraine is a common painful neurovascular disorder usually associated with several symptoms, such as photophobia, phonophobia, nausea, vomiting and inflammation, and involves immune cells. Mast cells (MCs) are immune cells derived from hematopoietic pluripotent stem cells which migrate and mature close to epithelial,...
journal_title：European journal of pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.ejphar.2018.12.004
更新日期：2019-02-05 00:00:00
abstract：:Intravenous (i.v.) administration of cytidine-5'-diphosphate choline (CDP-choline) (100, 250 and 500 mg/kg) increased blood pressure in normal rats and reversed hypotension in haemorrhagic shock. Choline (54 mg/kg; i.v.), at the dose equimolar to 250 mg/kg CDP-choline decreased blood pressure of rats in both condition...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(03)01602-9
更新日期：2003-05-09 00:00:00
abstract：:Although accumulated data suggest that calcitonin gene-related peptide (CGRP) produces anabolic effects in skeletal tissue by directly acting on osteogenic cells, neither the distribution of CGRP receptor subtypes nor the associated cellular signaling pathways are well understood. In this study, we have pharmacologica...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(03)01763-1
更新日期：2003-06-06 00:00:00
abstract：:The kappa-opioid receptor (kappa Op) from guinea-pig cerebellum membranes has been solubilized in an active form and in good yield (30-40%) with digitonin in 10 mM Tes-KOH buffer, pH 7.4. [3H]Bremazocine (KD = 1.1 nM in the soluble extract) was used to monitor the binding and hydrodynamic characteristics of the digito...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(88)90755-8
更新日期：1988-05-20 00:00:00
abstract：:In neutrophils and several other phagocytes, a pertussis and cholera toxin-sensitive guanine nucleotide-binding protein (G-protein) couples the receptors for formyl methionine-containing chemotactic peptides to stimulation of phospholipase C. We used membranes of myeloid-differentiated HL 60 cells to study the role of...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0922-4106(89)90031-x
更新日期：1989-12-05 00:00:00
abstract：:Substance P and its tachykinin NK(1) receptors are highly expressed in brain regions involved in emotional control. We recently showed that NK(1)-mediated substance P neurotransmission is deeply involved in the control of aggressiveness. To get further insights into the NK(1) receptor/aggression relationship, we studi...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2009.03.050
更新日期：2009-06-02 00:00:00
abstract：:The aim of this study was to characterise the 5-HT receptor(s) mediating secretory responses of isolated human colonic mucosa to 5-HT. Sheets of muscle-stripped mucosa from proximal (ascending) and distal (sigmoid) human colon were set up in Ussing chambers for measurement of short-circuit current (Isc). Serosal appli...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(96)00466-9
更新日期：1996-08-15 00:00:00
abstract：:This study investigates the anti-inflammatory effects of 1-(2-chlorophenyl)-N-methyl-N(1-methylpropyl)-3-isoquinoline carboxamide and 7-chloro-5-(4-chlorophenyl)-1, 3-dihydro-1-methyl-2-H-1,4-benzodiazepin-2-one in paw oedema induced by carrageenan in mice. Pretreatment (24 h) with both ligands inhibited oedema format...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(99)00745-1
更新日期：1999-12-03 00:00:00
abstract：:The role of prejunctional inhibitory and facilitatory muscarinic receptors was investigated in cats with tracheal hyperresponsiveness to vagal stimulation. Intrathoracic airway caliber (total lung resistance (RL) and dynamic compliance (Cdyn] and the diameter of tracheal ring 4 were measured during vagal stimulation a...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(92)90409-w
更新日期：1992-01-21 00:00:00
abstract：:Previous work has demonstrated that neuropeptide tyrosine (NPY), Y(1) receptor and Y(2) receptor are critical in modulation of pain after nerve injury. We hypothesized that NPY was important for nociception after surgical incision. As a model of postoperative pain, rats underwent a plantar incision in one hindpaw. Wes...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2012.10.036
更新日期：2013-01-05 00:00:00
abstract：:We have studied the effects of withdrawal from chronic clonidine treatment in the adult male spontaneously hypertensive rat (SHR). SHR received clonidine, 0.1 mg X kg-1 X day-1 i.v. for 10 days. Clonidine was delivered via osmotic minipumps. After 7 days of treatment there was a 16.5 +/- 2.5 mm Hg fall in mean arteria...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(86)90397-3
更新日期：1986-02-11 00:00:00
abstract：:Terfenadine and astemizole rarely cause cardiac arrhythmias by suppressing the cardiac rapid delayed rectifier K+ channel encoded by the human ether-a-go-go-related gene (HERG). Epinastine, however, has not been reported to have the adverse effect. We have therefore compared the effects of epinastine, terfenadine and ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(99)00375-1
更新日期：1999-06-25 00:00:00
abstract：:Kisspeptin (KP), the endogenous ligand of GPR54, is a mammalian amidated neurohormone, which belongs to the RF-amide peptide family. However, in contrast with the related members of the RF-amide family, little information is available regarding its role in the gastrointestinal motility. With regard to the recent data ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2016.11.041
更新日期：2017-01-05 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：:The pathophysiology of chronic neurodegenerative diseases, as Alzheimer's diseases, has remained inaccessible till recently. But this situation is changing quickly. In the past decades, genes causing familiar forms of the disease have been identified and provided the genetic framework for the emerging amyloid hypothes...
journal_title：European journal of pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.ejphar.2009.10.020
更新日期：2010-01-10 00:00:00
abstract：:Indomethacin and ibuprofen inhibited adrenaline- and calcium ionophore A23187-stimulated 45Ca2+ uptake by isolated human platelets in a concentration-dependent manner. Mediation of these effects by thromboxane A2 (TXA2) inhibition was discounted since under the same experimental conditions, adrenaline did not stimulat...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(90)90351-6
更新日期：1990-10-02 00:00:00
