Abstract：
:The influence of the anti-epileptic drug, valproate, on K conductance (gK) was investigated in voltage-clamped Ranvier nodes of Xenopus laevis. A double pulse method was used in order to eliminate the effect of accumulation of potassium ions in the perinodal space, thus enabling the determination of the 'true' magnitude of gK. Valproate (2.4 mM) had a voltage-dependent action on the magnitude of gK. With small step depolarizations more negative than about -50 mV, valproate increased gK (20 ms after the step) to approximately 12% of the maximal gK, an increase which disappeared due to a relatively rapid (less than 200 ms) inactivation process. However, with step depolarizations more positive than about -50 mV, valproate markedly reduced gK (20 ms after the step) at greater depolarizations, with a maximum of about 40% of the maximal gK. Moreover, at these voltages gK was inactivated completely (less than or equal to 10 s), whereas under control conditions the inactivation was only partial. Both the temporary increase and the steady state decrease of gK could contribute to an anti-epileptic effect by increasing the action potential threshold and by preventing excessive depolarizations of the nerve during epileptic seizures, respectively.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Van Erp MG,Van Dongen AM,Van den Berg RJdoi
10.1016/0014-2999(90)90676-wsubject
Has Abstractpub_date
1990-08-02 00:00:00pages
151-61issue
1eissn
0014-2999issn
1879-0712pii
0014-2999(90)90676-Wjournal_volume
184pub_type
杂志文章abstract：:Oenanthotoxin (OETX) and dihydro-OETX are polyacetylenic diols occurring in Oenanthe crocata and are known to exert proconvulsant effects. We have recently demonstrated that these compounds downregulated GABAergic currents (Appendino et al., 2009) and that OETX induced open channel block and allosterically modulated G...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2012.03.005
更新日期：2012-05-15 00:00:00
abstract：:We reported previously that 18 compounds varying in general anesthetic potency by up to 66 000-fold inhibited, at anesthetic concentrations, the metabolism of arachidonic acid and aminopyrine by cytochrome P450 monooxygenases in rat liver microsomes. Now, we report that P450-mediated para-hydroxylation of aniline is m...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0926-6917(95)00022-4
更新日期：1995-10-06 00:00:00
abstract：:There is a well-described projection from the retrohippocampus (subiculum and entorhinal cortex) to the nucleus accumbens that is involved in the control of psychomotor behaviour, and is implicated in the aetiology of schizophrenia. Cortical abnormalities are widely reported in the brains of schizophrenic patients, bu...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(00)00741-x
更新日期：2000-10-27 00:00:00
abstract：:Systemic administration of the NMDA receptor antagonist phencyclidine (PCP; 4 mg/kg) produced a profound reduction in prepulse inhibition of the acoustic startle response in rats. Pre-treatment with the selective adenosine A1 receptor agonist N6-cyclopentyladenosine (CPA) blocked (0.5 mg/kg) or attenuated (0.1 and 0.2...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(99)00088-6
更新日期：1999-03-26 00:00:00
abstract：:In pentobarbital (35.0 mg/kg) anaesthetised dogs, bolus injections of prazosin into the femoral artery (3.0--300.0 microgram) provoked a dose-related fall in the vascular resistance of the innervated hind limb. In contrast to papaverine, prazosin failed to produce the same effect in dogs under spinal anaesthesia even ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(78)90101-2
更新日期：1978-06-01 00:00:00
abstract：:In Ca-free solution norepinephrine (NE) produced only a phasic contraction in the media-intima layer of rabbit aorta. The second application of NE was almost ineffective. Incubation of the muscle with Ca for a short period (Ca loading) restored the ability to produce a phasic contraction in Ca-free solution. Various i...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(79)90176-6
更新日期：1979-06-15 00:00:00
abstract：:Aspirin (acetylsalicylic acid), the oldest synthetic drug, was originally used as an anti-inflammatory medication. Being an irreversible inhibitor of COX (prostaglandin-endoperoxide synthase) enzymes that produce precursors for prostaglandins and thromboxanes, it has gradually found several other applications. Sometim...
journal_title：European journal of pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.ejphar.2019.172762
更新日期：2020-01-05 00:00:00
abstract：:The present study was conducted to evaluate the effect of L-3, 4-dihydroxyphenylalanine (L-DOPA) on the daily rhythms of temperature, heart rate and locomotor activity in rats that received a 7-day continuous infusion. Our results indicate that L-DOPA does not induce a loss of the daily rhythmicity of temperature, hea...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(00)00422-2
更新日期：2000-07-28 00:00:00
abstract：:In the present work we evaluated the anticonvulsant effects of two novel antagonists of the glycine co-agonist site (glycineB receptor) within the N-methyl-D-aspartate (NMDA) receptor complex, MRZ 2/576 (a tricyclic pyrido-phtalazin dione derivative) and L-701,324 (7-chloro-4-hydroxy-3-(3-phenoxy)phenyl-2(H)quinoline)...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(97)01452-0
更新日期：1998-01-19 00:00:00
abstract：:The impacts of prenatal propofol on cognition and emotion of offspring remain elusive. In the present study, pregnant rats in the second trimester were anesthetized with propofol. Neuronal apoptosis and proliferation was determined in fetuses and postnatal rats by detecting caspase-3 and BrdU expression. The offspring...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2018.11.032
更新日期：2019-01-15 00:00:00
abstract：:In myopathic BIO 8262-hamsters beta1-adrenergic stimulation of cardiac adenylyl cyclase has been found to be markedly reduced compared to that of healthy controls. In order to test the hypothesis that the functional uncoupling of beta1-adrenoceptors in diseased hamster hearts is due to agonist-dependent desensitizatio...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(97)01200-4
更新日期：1997-09-10 00:00:00
abstract：:We have examined the effects of the recently described heptadecapeptide nocistatin on K+-evoked glutamate release from rat cerebrocortical slices in vitro. In vivo, nocistatin reverses the action of nociceptin. Nocistatin (100 nM, n = 7) did not inhibit K+-evoked glutamate release alone. Nociceptin (100 nM) inhibited ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(98)00545-7
更新日期：1998-09-04 00:00:00
abstract：:The effects of procaine, mepivacaine and phenylbutazone on pain perception in the equine were studied using two behavioral assays of nociception; the thermal evoked hoof withdrawal reflex and skin twitch reflex. Pain perception threshold was measured as the latency from onset of thermal stimuli to reflex withdrawal of...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(84)90088-8
更新日期：1984-12-15 00:00:00
abstract：:Coagulopathy is the major cause of organ injury as well as a strong predictor of mortality in septic patients. Systemic inflammatory response and redox imbalance are regarded as the major causes of sepsis-induced coagulopathy. There is growing evidence that a vasodilator hydralazine has beneficial effects on heart fai...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2020.173279
更新日期：2020-09-05 00:00:00
abstract：:In Krebs solution (3.36 mM Ca2+), the maximal contractile response of human ileal and urinary bladder detrusor muscle to acetylcholine (ACh) was 40-60% that to carbachol (CCh). The maximum response to ACh was reached at a bath concentration of about 1 microM and was maintained throughout a range extending to 100 micro...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(86)90698-9
更新日期：1986-04-09 00:00:00
abstract：:The responsiveness of the rat striatal dopamine (DA) receptor system to apomorphine (APO) was assessed after 10 days of antidepressant administration. Desipramine (DMI), dothiepin (DOTH), iprindole (IPR) and nomifensine (NOM) were administered intra-peritoneally, twice daily, to rats for 10 days and 42 h after the las...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(84)90617-4
更新日期：1984-10-15 00:00:00
abstract：:This study was designed to investigate the effects of serotonin on changes in intracellular Ca(2+) concentration ([Ca(2+)](i)) in cultured rat heart endothelial cells. Serotonin stimulated a biphasic change in cytosolic Ca(2+) of rat heart endothelial cells: an initial transient increase, which primarily reflects the ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(99)00672-x
更新日期：1999-11-12 00:00:00
abstract：:The effect of simultaneous topical application of adrenergic agonists was investigated on the polydipsia caused by direct carbachol (CCh) stimulation of the rat brain. In addition, fluid selection (4-choice arrangement) was studied. Noradrenaline and isoprenaline fully antagonized the CCh effect after either intracere...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(81)90342-3
更新日期：1981-10-15 00:00:00
abstract：:A V79 Chinese hamster cell line stably expressing human cytochrome P450 1A1 (CYP1A1) was obtained by chromosomal integration of the human CYP1A1 cDNA under the control of the SV40 early promoter. Chromosomal integration was verified by Southern analysis, and effective transcription of the human CYP1A1 cDNA was demonst...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0926-6917(93)90052-r
更新日期：1993-10-01 00:00:00
abstract：:The present study aims to investigate whether azithromycin reverses P-glycoprotein-dependent anticancer drug resistance in vitro and modifies the hepatobiliary excretion of doxorubicin, a substrate for P-glycoprotein in vivo. Azithromycin increased dose-dependently the intracellular accumulation of doxorubicin in adri...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2003.11.035
更新日期：2004-01-26 00:00:00
abstract：:Substance-related and addictive disorders (SRADs) are characterized by compulsive drug use and recurrent relapse. The persistence of pathological drug-related memories indisputably contributes to a high propensity to relapse. Hence, strategies to disrupt reconsolidation of drug reward memory are currently being pursue...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2021.173911
更新日期：2021-01-24 00:00:00
abstract：:Clonidine and other imidazolines, including phentolamine, inhibited the norepinephrine-elicited accumulation of cyclic AMP in brain slices via blockade or postsynpatic alpha-adrenoceptors. Clonidine (0.0125--0.050 mg/kg, i.p.) antagonized the increase in locomotor activity induced by amphetamine in a dose-dependent ma...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(78)90126-7
更新日期：1978-02-15 00:00:00
abstract：:A series of 26 drugs was tested for in vitro binding to opiate receptors in the presence and absence of 0.1 M NaCl. The results were correlated with assays for in vivo pharmacological potency. Highly significant correlation was found between binding in the presence and absence of sodium ions and analgesic potency. For...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(77)90334-x
更新日期：1977-12-01 00:00:00
abstract：:AY-22,241 (Actodigin) is a new rapid-acting semisynthetic cardiotonic steroid. In experiments on contractility of cat papillary muscle, Actodigin (2 times 10(-7) to 4 times 10(-6) M) produced a dose-dependent positive inotropic effect, a marked increase in the maximum rate of force development, and no change in restin...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(75)90316-7
更新日期：1975-05-01 00:00:00
abstract：:The zebrafish (Danio rerio) has recently become a powerful animal model for cardiovascular research and drug discovery due to its ease of maintenance, genetic manipulability and ability for high-throughput screening. Recent advances in imaging techniques and generation of transgenic zebrafish have greatly facilitated ...
journal_title：European journal of pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.ejphar.2015.10.031
更新日期：2015-12-05 00:00:00
abstract：:Although a number of muscarinic agonists have been used in clinical trials for Alzheimer's Disease, many of these compounds are low in potency and have only limited intrinsic efficacy. The present study describes four non-quaternary oxadiazole based muscarinic agonists from a quinuclidine and a 1-azanorbornane series....
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(90)90006-r
更新日期：1990-10-09 00:00:00
abstract：:The number of prolactin (PRL) receptors in the hypothalamus and substantia nigra of aged rabbits is significantly lower than the number measured in young animals. The treatment of aged rabbits for 30 days with S-adenosyl-L-methionine (SAM) restored the number of PRL binding sites to levels found in the hypothalamus an...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(89)90063-0
更新日期：1989-07-18 00:00:00
abstract：:Enterobacteria are known to deconjugate amino acid-conjugated bile acids in the intestine. Administration of ampicillin (ABPC; 3 days, 100mg/kg) decreased the expression of ileal farnesoid X receptor (Fxr) target genes, and increased the levels of total bile acids in the intestinal lumen. The primary tauro-conjugates ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2012.09.048
更新日期：2012-12-15 00:00:00
abstract：:Honokiol and magnolol, two major phenolic constituents of Magnolia sp., have been known to exhibit antibacterial activities. However, until now, their antibacterial activity against Propionibacterium sp. has not been reported. To this end, the antibacterial activities of honokiol and magnolol were detected using the d...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2004.05.047
更新日期：2004-08-02 00:00:00
abstract：:Nitric oxide can exert either protective or damaging effects on the gastric mucosa. To further explore the role of nitric oxide in the modulation of gastric mucosal defense, the effects of intra-arterial administration of the precursor, L-arginine, on susceptibility of the gastric mucosa to damage induced by topically...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(94)90018-3
更新日期：1994-07-21 00:00:00
