Effects of paxilline on K+ channels in rat mesenteric arterial cells.

Abstract:

:The effects of paxilline, a mycotoxin, on whole-cell outward currents from freshly isolated cells of the rat mesenteric artery were studied. Paxilline inhibited a component of the outward current that was also sensitive to iberiotoxin. Inhibition could be observed at a concentration of 10 nM and complete inhibition of the iberiotoxin-sensitive current was achieved at 300 nM. The inhibition could be described by a single site of interaction with a Ki of 35.7 nM. Paxilline had no effect on the component of the current that was sensitive to 4-aminopyridine. It is concluded that paxilline is a potent inhibitor of large conductance Ca2+ -activated K+ currents in vascular smooth muscle cells.

journal_name

Eur J Pharmacol

authors

Li G,Cheung DW

doi

10.1016/s0014-2999(99)00188-0

keywords:

subject

Has Abstract

pub_date

1999-05-07 00:00:00

pages

103-7

issue

1

eissn

0014-2999

issn

1879-0712

pii

S0014-2999(99)00188-0

journal_volume

372

pub_type

杂志文章
  • Subtype selective regulation of coupling of rat cardiac beta adrenoceptors to adenylate cyclase.

    abstract::There is now evidence from human studies to suggest that cardiac beta-adrenoceptor density and coupling to adenylate cyclase may be regulated in a subtype selective fashion. An animal model was used to investigate this further. Rats were infused for 6 days with the non-selective full agonist isoprenaline (n = 6) or th...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0922-4106(93)90109-m

    authors: Arnold IR,Mistry R,Barnett DB

    更新日期:1993-05-15 00:00:00

  • Differential pharmacology of GABAA and GABAC receptors on rat retinal bipolar cells.

    abstract::GABAA and GABAC receptors were studied on cultured or freshly isolated rat retinal bipolar cells. The cells displayed GABA-induced whole-cell currents, which were only partially blocked by high concentrations (100 microM) of the GABAA receptor antagonist bicuculline. The bicuculline-resistant (GABAC) component was ins...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0922-4106(94)90014-0

    authors: Feigenspan A,Bormann J

    更新日期:1994-12-15 00:00:00

  • Tempol attenuates cocaine-induced death of PC12 cells through decreased oxidative damage.

    abstract::The association between cocaine administration and induction of oxidative stress in different brain regions suggests that oxidative damage is an important factor participating in cocaine disruption of normal central nervous system functions. In order to deal with this topic, brain penetrating exogenous antioxidants we...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2010.10.024

    authors: Numa R,Baron M,Kohen R,Yaka R

    更新日期:2011-01-10 00:00:00

  • Novel p38 MAPK inhibitor ML3403 has potent anti-inflammatory activity in airway smooth muscle.

    abstract::SB203580 is the prototypical p38 MAPK inhibitor; however it cannot be used clinically due to liver toxicity. We developed a structural analogue of SB203580 - ML3403 - with equal in vitro and ex vivo p38alpha MAPK inhibition as SB203580, but with reduced activity towards liver cytochrome P450 enzymes. In addition, we d...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2010.02.037

    authors: Munoz L,Ramsay EE,Manetsch M,Ge Q,Peifer C,Laufer S,Ammit AJ

    更新日期:2010-06-10 00:00:00

  • Effect of idebenone on adenosine outflow and adenine nucleotide level in hippocampal slices under ischemia-like conditions.

    abstract::The effect of idebenone on the changes in adenosine and nucleotide metabolism occurring in hippocampal slices after ischemia-like conditions (superfusion with glucose-free Krebs solution gassed with 95% N2-5% CO2) and during reperfusion with normal Krebs solution was investigated by measuring adenosine and inosine out...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(93)90662-2

    authors: Latini S,Pedata F,Pepeu G

    更新日期:1993-11-02 00:00:00

  • Antagonism of the effects of the hallucinogen DOM and the purported 5-HT agonist quipazine by 5-HT2 antagonists.

    abstract::Rats trained to discriminate 1.0 mg/kg of 1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane (DOM) from saline in a two-lever operant choice task were administered doses of mescaline, LSD, 5-methoxy-N,N-dimethyltryptamine (5-OMe DMT), quipazine, TFMPP and RU-24969. The DOM-stimulus generalized to the three hallucinogenic...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(83)90464-8

    authors: Glennon RA,Young R,Rosecrans JA

    更新日期:1983-07-22 00:00:00

  • DHA supplementation prevent the progression of NASH via GPR120 signaling.

    abstract::Nonalcoholic steatohepatitis (NASH) is one of the most common liver diseases involving chronic accumulation of fat and inflammation, often leading to advanced fibrosis, cirrhosis and carcinoma. However, the pathological mechanism for this is unknown. GPR120/FFAR4 has been recognized as a functional fatty acid receptor...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2017.11.046

    authors: Nakamoto K,Shimada K,Harada S,Morimoto Y,Hirasawa A,Tokuyama S

    更新日期:2018-02-05 00:00:00

  • Central injection of CDP-choline suppresses serum ghrelin levels while increasing serum leptin levels in rats.

    abstract::In this study we aimed to test central administration of CDP-choline on serum ghrelin, leptin, glucose and corticosterone levels in rats. Intracerebroventricular (i.c.v.) 0.5, 1.0 and 2.0 µmol CDP-choline and saline were administered to male Wistar-Albino rats. For the measurement of serum leptin and ghrelin levels, b...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2015.07.014

    authors: Kiyici S,Basaran NF,Cavun S,Savci V

    更新日期:2015-10-05 00:00:00

  • Effects of aging and hypertension on the participation of endothelium-derived constricting factor (EDCF) in norepinephrine-induced contraction of rat femoral artery.

    abstract::Endothelium-dependent contraction elicited by high concentrations of acetylcholine was described in hypertensive as well as in aged normotensive rats. The contribution of endothelium-derived constricting factor (EDCF) to norepinephrine-induced contraction is still unknown. We aimed to compare EDCF participation to nor...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2011.05.031

    authors: Líšková S,Petrová M,Karen P,Kuneš J,Zicha J

    更新日期:2011-09-30 00:00:00

  • Human saphenous vein contains both endothelin ETA and ETB contractile receptors.

    abstract::We have investigated the endothelin receptor subtypes mediating contraction in isolated preparations of human saphenous vein. Endothelin-1 (EC50: 17.8 nM), endothelin-3 (EC50: 82.3 nM) and the endothelin ETB receptor-selective agonists, [Ala1,3,11,15]endothelin-1 (EC50: 63 nM) and sarafotoxin S6c (EC50: 0.75 nM) all p...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(94)90144-9

    authors: White DG,Garratt H,Mundin JW,Sumner MJ,Vallance PJ,Watts IS

    更新日期:1994-05-23 00:00:00

  • Phorbol esters induce oscillatory contractions of intestinal smooth muscles.

    abstract::The actions of tumor-promoting phorbol esters in smooth muscle excitation-contraction coupling were studied in isolated guinea pig ileum in the presence of various contractile agents. Muscarinic agonists, histamine and bradykinin elicited an initial transient phasic contraction and a subsequent sustained tonic contrac...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(91)90348-t

    authors: Xu SF,Collins MA,Chang KJ

    更新日期:1991-08-29 00:00:00

  • The potassium channel opener CGS7184 activates Ca²⁺ release from the endoplasmic reticulum.

    abstract::CGS7184 (ethyl 1-[[(4-chlorophenyl)amino]oxo]-2-hydroxy-6-trifluoromethyl-1H-indole-3-carboxylate) is a synthetic large-conductance Ca(2+)-activated potassium (BK(Ca)) channel opener. The existing literature suggests that potassium channels are involved in cardioprotection, particularly during ischemia-reperfusion eve...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2012.06.029

    authors: Wrzosek A,Tomaskova Z,Ondrias K,Lukasiak A,Szewczyk A

    更新日期:2012-09-05 00:00:00

  • The role of endothelium-derived hyperpolarizing factor and cyclooxygenase pathways in the inhibitory serotonergic response to the pressor effect elicited by sympathetic stimulation in chronic sarpogrelate treated rats.

    abstract::We have demonstrated that the antagonism of 5-HT2 receptors produces an enhancement of serotonergic sympathoinhibitory effect by 5-HT1D and 5-HT7 activation. The aim of this work was to determine mechanisms involved in the 5-hydroxytriptaminergic inhibitory action on the pressor responses elicited by sympathostimulati...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2014.02.043

    authors: García-Pedraza JÁ,García M,Martín ML,San Román L,Morán A

    更新日期:2014-05-15 00:00:00

  • Pharmacological modulation of protein kinases as a new approach to treat addiction to cocaine and opiates.

    abstract::Drug addiction shares brain mechanisms and molecular substrates with learning and memory processes, such as the stimulation of glutamate receptors and their downstream signalling pathways. In the present work we provide an up-to-date review of studies that have demonstrated the implication of the main memory-related c...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/j.ejphar.2016.03.065

    authors: García-Pardo MP,Roger-Sanchez C,Rodríguez-Arias M,Miñarro J,Aguilar MA

    更新日期:2016-06-15 00:00:00

  • Melanocortins and the brain: from effects via receptors to drug targets.

    abstract::The lack of specific receptors (and antagonists) has hampered the research on the neural mechanism of action of adrenocorticotropic hormone (ACTH)- and melanocyte-stimulating hormone (MSH)-like peptides. Yet the original observations in the 1970s already pointed to cAMP as a possible mediator of ACTH/MSH effects in ne...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/s0014-2999(00)00537-9

    authors: Adan RA,Gispen WH

    更新日期:2000-09-29 00:00:00

  • Evidence for a 5-HT1D receptor-mediated hypothermic effect of the alpha 1-adrenoceptor agonist, SDZ NVI-085, in guinea-pigs.

    abstract::The alpha 1-adrenoceptor agonist, SDZ NVI-085 ((-)-(4aR,10aR)-3,4,4a,5,10,10a-hexahydro-6-methoxy-4- methyl-9-(methylthio)-2H-naphth[2,3-b]-1,4-oxazine.HCl; 1 mg/kg i.p.), decreased body temperature of guinea-pigs. Two 5-HT1D receptor antagonists, GR127935 (N-[4-methoxy-3-(4-methyl-1-piperazinyl)phenyl]-2'-methyl-4'-(...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(95)00526-q

    authors: Kalkman HO,Neumann V

    更新日期:1995-10-24 00:00:00

  • Antioxidant effect of erythropoietin on 1-methyl-4-phenylpyridinium-induced neurotoxicity in PC12 cells.

    abstract::The neuroprotective effects of erythropoietin on 1-methyl-4-phenylpyridinium (MPP(+))-induced oxidative stress and apoptosis in cultured PC12 cells as well as the underlying mechanism were investigated. Treatment of PC12 cells with MPP(+) caused the loss of cell viability, which was associated with the elevation in ap...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2007.02.020

    authors: Wu Y,Shang Y,Sun S,Liu R

    更新日期:2007-06-14 00:00:00

  • 3H-noradrenaline outflow induced from isolated aventitia and intima-media of rabbit aorta by electrical field stimulation.

    abstract::Electrical field stimulation of the isolated adventitial and intima-medial layers of rabbit aorta preloaded with 3H-noradrenaline elicited a 3H outflow. The initial 3H outflow from adventitia was independent of external Ca2+ concentration. Each of the subsequent 3H outflows was mainly Ca2+ sensitive. All stimulation-i...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(76)90156-4

    authors: Schrold J,Nedergaard OA

    更新日期:1976-10-01 00:00:00

  • The binding of [3H]leukotriene C4 to guinea-pig lung membranes. The lack of correlation of LTC4 functional activity with binding affinity.

    abstract::High affinity binding sites for [3H]leukotriene C4 ([3H]LTC4) have been identified and characterised in guinea-pig lung membranes. [3H]LTC4 bound to these membranes with a pharmacological specificity totally distinct to that previously observed for [3H]LTD4 binding in guinea-pig lung. Scatchard analysis of saturation ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(87)90456-0

    authors: Norman P,Abram TS,Kluender HC,Gardiner PJ,Cuthbert NJ

    更新日期:1987-11-17 00:00:00

  • Cytokines and nitric oxide synthase inhibitor as mediators of adrenergic refractoriness in cardiac myocytes.

    abstract::We have previously proposed that pro-inflammatory cytokines and nitric oxide (NO) contributed to reversible myocardial depression in patients with sepsis and congestive heart failure. Sepsis and heart failure are also associated with refractoriness to beta-adrenoceptor agonists. Therefore, the chronotropic effects of ...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(96)00912-0

    authors: Oddis CV,Finkel MS

    更新日期:1997-02-12 00:00:00

  • Caffeine inhibits depolarization-activated outward currents in rat ventricular myocytes.

    abstract::The effects of caffeine (10 mM) on depolarization-activated, calcium-independent outward K+ currents were investigated in isolated rat ventricular myocytes, using whole-cell clamping. The external solution contained CoCl2 2 mM and the internal solution contained ethylene glycol-bis(-aminoethyl ether) N,N,N',N'-tetraac...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(92)90551-e

    authors: Sanchez-Chapula J

    更新日期:1992-12-15 00:00:00

  • Steroid receptor coactivator-3 is a pivotal target of gambogic acid in B-cell Non-Hodgkin lymphoma and an inducer of histone H3 deacetylation.

    abstract::Gambogic acid (GA), the active ingredient from gamboges, has been verified as a potent anti-tumor agent in many cancer cells. Nevertheless, its function in lymphoma, especially in B-cell Non-Hodgkin lymphoma (NHL), remains unclear. Amplification and/or overexpression of steroid receptor coactivator-3 (SRC-3) have been...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2016.06.048

    authors: Zhao Z,Zhang X,Wen L,Yi S,Hu J,Ruan J,Zhao F,Cui G,Fang J,Chen Y

    更新日期:2016-10-15 00:00:00

  • Two dopamine receptors: supportive evidence with the rat rotational model.

    abstract::Di-isobutyryl apomorphine (5 mg/kg i.p.) and lergotrile (5 mg/kg i.p.) produce long lasting turning behaviour in rats with 6-hydroxydopamine lesions at the level of the substantia nigra. Haloperidol (1.5 and 3.0 mg/kg p.o.) blocks the rotational behaviour due to the apomorphine ester but has no effect on lergotrile tu...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(77)90063-2

    authors: Tye NC,Horsman L,Wright FC,Large BT,Pullar IA

    更新日期:1977-09-01 00:00:00

  • Vincamine and vincanol are potent blockers of voltage-gated Na+ channels.

    abstract::The effects of three vinca derivatives on [3H]batrachotoxin binding in rat cortical synaptosomes, on the inhibition of whole-cell Na+ currents evoked in voltage-clamped cortical neurones of the rat, on the protection against veratridine-induced cell death in cortical cultures and on the maximal electroshock-induced se...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0014-2999(96)00542-0

    authors: Erdo SA,Molnár P,Lakics V,Bence JZ,Tömösközi Z

    更新日期:1996-10-24 00:00:00

  • Yawning produced by dopamine agonists in rhesus monkeys.

    abstract::Yawning was recorded from five rhesus monkeys restrained in a chair after i.m. injection of dopaminergic compounds: apomorphine (0.03 mg/kg), quinpirole (0.01 mg/kg), and (-)-3-(3-hydroxyphenyl)-N-(1-propyl)piperidine (1 mg/kg). SKF 38393 or physostigmine produced no yawning. Yawning from apomorphine was blocked by ch...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(91)90351-p

    authors: Code RA,Tang AH

    更新日期:1991-08-29 00:00:00

  • 2-(1-Hexyn-1-yl)adenosine-induced intraocular hypertension is mediated via K+ channel opening through adenosine A2A receptor in rabbits.

    abstract::The present study was performed to clarify the mechanism of change in intraocular pressure by 2-(1-hexyn-1-yl)adenosine (2-H-Ado), a selective adenosine A2 receptor agonist, in rabbits. 2-H-Ado (0.1%, 50 microl)-induced ocular hypertension (E(max): 7.7 mm Hg) was inhibited by an adenosine A2A receptor antagonist 1,3,7...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.ejphar.2005.03.002

    authors: Konno T,Uchibori T,Nagai A,Kogi K,Nakahata N

    更新日期:2005-08-22 00:00:00

  • Edematous response caused by [Thi5,8,D-Phe7]bradykinin, a B2 receptor antagonist, is due to mast cell degranulation.

    abstract::[Thi5,8,D-Phe7]bradykinin caused hind-paw edema and degranulation of isolated peritoneal mast cells in a dose-dependent manner. Pretreatment with diphenhydramine/methysergide or compound 48/80 completely suppressed the edematous response caused by [Thi5,8,D-Phe7]bradykinin, whereas bradykinin-induced hind-paw swelling...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(89)90836-4

    authors: Wang JP,Hsu MF,Ouyang CH,Teng CM

    更新日期:1989-02-28 00:00:00

  • Comparison of chronic administration of haloperidol and the atypical neuroleptics, clozapine and raclopride, in an animal model of tardive dyskinesia.

    abstract::Rats were administered haloperidol, clozapine, raclopride, or no drug for either 28 days or 8 months and then withdrawn from drug treatment for 3 weeks. Oral movements were repeatedly recorded, both by a human observer and by a computerized video analysis system which determined mouth openings and closings, or compute...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(90)90077-j

    authors: See RE,Ellison G

    更新日期:1990-06-08 00:00:00

  • Dup 753 prevents the development of puromycin aminonucleoside-induced nephrosis.

    abstract::The appearance of nephrotic syndromes such as proteinuria, hypoalbuminemia, hypercholesterolemia and increase in blood nitrogen urea, induced in rats by injection of puromycin aminonucleoside was markedly inhibited by oral administration of Dup 753 (losartan), a novel angiotensin II receptor antagonist, at a dose of 1...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(93)90609-l

    authors: Yayama K,Kawao M,Tujii H,Itoh N,Okamoto H

    更新日期:1993-05-19 00:00:00

  • The spasmogenic effect of caffeine in trachealis isolated from control and actively sensitized guinea-pigs.

    abstract::The spasmogenic activity of caffeine (10 mM) was evaluated in tracheal strips obtained from control and sensitized guinea-pigs then pretreated with indomethacin (2.8 microM) and cooled to 20 degrees C. The contraction elicited by caffeine was inhibited by verapamil (100 microM), trifluoperazine (100 and 500 microM) an...

    journal_title:European journal of pharmacology

    pub_type: 杂志文章

    doi:10.1016/0014-2999(88)90073-8

    authors: Ortiz JL,Cortijo J,Morcillo EJ,Sanz C,Perpiñá M,Esplugues J

    更新日期:1988-12-13 00:00:00