当前位置： SCI文献检索 > BRITISH JOURNAL OF PHARMACOLOGY期刊下所有文献 > Voltage-dependent block of normal and mutant muscle sodium channels by 4-Chloro-m-Cresol.

Voltage-dependent block of normal and mutant muscle sodium channels by 4-Chloro-m-Cresol.

Abstract：

:1 The effects of 4-Chloro-m-Cresol (4-CmC) were examined on heterologously expressed wild type (WT), Paramyotonia Congenita (R1448H) and Hyperkalemic Periodic Paralysis (M1360V) mutant alpha-subunits of human muscle sodium channels. 2 Block of rested sodium channels caused by 4-CmC was concentration-dependent with an ECR50 of 0.40 mM in WT, 0.45 mM in R1448H and 0.49 mM in M1360V. 3 Inactivation significantly promoted 4-CmC-induced sodium channel block in all clones indicated by 4-CmC-induced shifts of steady-state availability curves, reflecting a higher proportion of channel block at depolarized membrane potentials. Channel block was almost complete (>90%) at concentrations close to the ECR50 (0.5 mM) on application of an inactivating prepulse before the test pulse. 4 4-CmC accelerated the current decay following depolarization and prolonged recovery from inactivation in all clones. Of these, R1448H, the mutant which displayed severely impaired inactivation in the controls, responded to 4-CmC with the most pronounced acceleration of inactivation. Control experiments revealed enhanced recovery from inactivation in the mutants, which was restored to normal in 0.1 mM 4-CmC. 5 4-CmC induced no additional frequency-dependent block. 6 Our results clearly demonstrate that 4-CmC is as effective as lidocaine (Fan et al., 1996) in blocking muscle sodium channels. Low concentrations of the compound (

journal_name

Br J Pharmacol

journal_title

British journal of pharmacology

authors

Haeseler G,Leuwer M,Kavan J,Würz A,Dengler R,Piepenbrock S

doi

10.1038/sj.bjp.0702896

subject

Has Abstract

pub_date

1999-11-01 00:00:00

pages

1259-67

issue

6

eissn

0007-1188

issn

1476-5381

journal_volume

128

pub_type

杂志文章

相关文献

BRITISH JOURNAL OF PHARMACOLOGY文献大全
  • Involvement of protein kinase C in reduced relaxant responses to the NO/cyclic GMP pathway in piglet pulmonary arteries contracted by the thromboxane A2-mimetic U46619.

    abstract：:1. Impairment of nitric oxide (NO)/cyclic GMP production and/or increased activities of thromboxane A2 (TXA2) and endothelin-1 (ET-1) have been associated with pulmonary hypertension. We have analysed the interactions of noradrenaline (NA), the TXA2-mimetic U46619 and ET-1 with the relaxation induced via cyclic GMP in...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1038/sj.bjp.0701257

    authors： Pérez-Vizcaíno F,Villamor E,Duarte J,Tamargo J

    更新日期：1997-08-01 00:00:00

  • High-affinity blockade of voltage-operated skeletal muscle and neuronal sodium channels by halogenated propofol analogues.

    abstract：BACKGROUND AND PURPOSE:Voltage-operated sodium channels constitute major target sites for local anaesthetic-like action. The clinical use of local anaesthetics is still limited by severe side effects, in particular, arrhythmias and convulsions. These side effects render the search for new local anaesthetics a matter of...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1038/bjp.2008.255

    authors： Haeseler G,Karst M,Foadi N,Gudehus S,Roeder A,Hecker H,Dengler R,Leuwer M

    更新日期：2008-09-01 00:00:00

  • Potential importance of alterations in hydrogen sulphide (H2S) bioavailability in diabetes.

    abstract：:Despite its long-standing reputation as a foul smelling and toxic gas that is associated with the decay of biological matter,hydrogen sulphide (H2S) has emerged as an important regulator of cardiovascular homoeostasis. H2S promotes a number of cellular signals that regulate metabolism, cardiac function and cell surviv...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1038/bjp.2008.359

    authors： Lefer DJ

    更新日期：2008-11-01 00:00:00

  • Metergoline and cyproheptadine suppress prolactin release by a non-5-hydroxytryptaminergic, non-dopaminergic mechanism.

    abstract：:A dispersed rat anterior pituitary cell system has been used to investigate the effects of cyproheptadine and metergoline on prolactin secretion. Both drugs were potent inhibitors of prolactin secretion. However, the inhibition was not antagonized by either 5-hydroxytryptamine or a variety of dopamine antagonists. We ...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1980.tb10896.x

    authors： Besser GM,Delitala G,Grossman A,Yeo T

    更新日期：1980-09-01 00:00:00

  • Novel data point to a broader mechanism of action of oxidized ATP: the P2X7 receptor is not the only target.

    abstract：:Oxidized ATP (oATP) is a Schiff-base-forming reagent that has been used for some years as an antagonist at the P2X7 receptor (P2X7R). Preincubation of mononuclear phagocytes with this inhibitor leads to attenuation of several proinflammatory responses triggered by extracellular ATP as well as a few non-nucleotide agon...

    journal_title：British journal of pharmacology

    pub_type： 评论,杂志文章,评审

    doi：10.1038/sj.bjp.0705469

    authors： Di Virgilio F

    更新日期：2003-10-01 00:00:00

  • Stimulation of prostaglandin biosynthesis by drugs: effects in vitro of some drugs affecting gut function.

    abstract：:Low concentrations of several emetic, purgative or irritant drugs in the absence of added co-factors stimulated conversion of arachidonic acid to prostaglandin E2 and F2alpha by prostaglandin synthetase extracted from bull seminal vesicles (BSV prostaglandin synthetase). Their effect was dependent on concentration and...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1976.tb10396.x

    authors： Collier HO,McDonald-Gibson WJ,Saeed SA

    更新日期：1976-10-01 00:00:00

  • Thromboxane (Tx) A2 receptor blockade and TxA2 synthase inhibition alone and in combination: comparison of anti-aggregatory efficacy in human platelets.

    abstract：:1. The present study has compared the relative anti-aggregatory effect of various compounds which interfere with thromboxane (Tx) A2-dependent aggregation of human platelets in whole blood in vitro. These included the cyclo-oxygenase inhibitor aspirin, the TxA2 synthase inhibitor dazoxiben, the TxA2 (TP-) receptor blo...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1991.tb12200.x

    authors： Watts IS,Wharton KA,White BP,Lumley P

    更新日期：1991-02-01 00:00:00

  • Pharmacological characterization of the metabotropic glutamate receptor inhibiting D-[3H]-aspartate output in rat striatum.

    abstract：:1. The effects of several agonists of the metabotropic glutamate receptor (mGluR) were studied in adult rat striatal slices by measuring (i) KCl (30 mM)-induced output of previously taken up D-[3H]-aspartate (Asp), (ii) forskolin (30 microM)-induced adenosine 3':5'-cyclic monophosphate (cyclic AMP) accumulation and (i...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1993.tb13977.x

    authors： Lombardi G,Alesiani M,Leonardi P,Cherici G,Pellicciari R,Moroni F

    更新日期：1993-12-01 00:00:00

  • Electrophysiological effects of the combination of mexiletine and flecainide in guinea-pig ventricular fibres.

    abstract：:1. The effects of flecainide alone, mexiletine alone and their combination at the Na+ channel level were studied in guinea-pig papillary muscles. The maximum upstroke velocity (Vmax) was used as an indirect index of the magnitude of the fast inward Na+ current (INa). 2. In muscles driven at 0.02 Hz, neither mexiletine...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1991.tb09803.x

    authors： Delpón E,Valenzuela C,Tamargo J

    更新日期：1991-06-01 00:00:00

  • Biological activities of a novel selective oestrogen receptor modulator derived from raloxifene (Y134).

    abstract：BACKGROUND AND PURPOSE:Selective oestrogen receptor (ER) modulators (SERMs) are of great value in the treatment of breast cancer and osteoporosis. The aim of this study was to characterize pharmacologically a new class of SERMs synthesized based on the core structure of raloxifene. EXPERIMENTAL APPROACH:Competitive re...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1038/sj.bjp.0706960

    authors： Ning M,Zhou C,Weng J,Zhang S,Chen D,Yang C,Wang H,Ren J,Zhou L,Jin C,Wang MW

    更新日期：2007-01-01 00:00:00

  • Pharmacological modulation of inhaled sodium metabisulphite-induced airway microvascular leakage and bronchoconstriction in the guinea-pig.

    abstract：:1. We have investigated the effects of chlorpheniramine, atropine and capsaicin pretreatment on inhaled sodium metabisulphite (MBS)-induced airway microvascular leakage and bronchoconstriction in anaesthetized guinea-pigs in order to clarify the mechanisms involved in these responses. The effects of frusemide and nedo...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1992.tb12771.x

    authors： Sakamoto T,Elwood W,Barnes PJ,Chung KF

    更新日期：1992-10-01 00:00:00

  • Do motor-nerve terminals have gamma-aminobutyric acid receptors?

    abstract：:1 gamma-Aminobutyric acid (GABA, 0.1 to 1 mM) had no significant effect on the amplitude, rise time, half decay time or frequency of miniature endplate potentials (m.e.p.ps) at the frog or mouse neuromuscular junctions in vitro. 2 Addition of GABA (1 mM) to preparations previously treated with 11 mM K+-Ringer did not ...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1980.tb10937.x

    authors： Smart TG

    更新日期：1980-01-01 00:00:00

  • Effect of sympathomimetic amines on the histamine forming capacity of human leucocytes.

    abstract：:1 The effects of alpha- and beta-adrenoceptor stimulants on the histamine-forming capacity (HFC) of human isolated leucocytes have been studied, in vitro.2 It was confirmed that antigen significantly stimulates the HFC of human leucocytes.3 beta-Adrenoceptor stimulants, such as isoprenaline and salbutamol (10(-6)-10(-...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1974.tb09702.x

    authors： Assem ES

    更新日期：1974-10-01 00:00:00

  • Comparison of the effects of I.C.I. 50172 and propranolol on the cardiovascular responses to adrenaline, isoprenaline and exercise.

    abstract：:1. The intravenous infusion of I.C.I. 50172 in doses up to 20 mg reduced, although not significantly, the increase in heart rate produced by the infusion of isoprenaline in healthy volunteers; the response to adrenaline was significantly reduced. The infusion of 1 mg propranolol abolished these responses2. After the p...

    journal_title：British journal of pharmacology

    pub_type： 临床试验,杂志文章

    doi：10.1111/j.1476-5381.1968.tb07956.x

    authors： Brick I,Hutchison KJ,McDevitt DG,Roddie IC,Shanks RG

    更新日期：1968-09-01 00:00:00

  • Drug displacement from protein binding: isolation of a redistributional drug interaction in vivo.

    abstract：:1. The pharmacokinetic interaction between phenylbutazone and sulphadoxine has been studied in live sheep.2. Intravenous injection of phenylbutazone causes a rapid fall in the concentration of total sulphadoxine together with a simultaneous rise in the concentration of free sulphadoxine in plasma. Both processes are c...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：

    authors： McQueen EG,Wardell WM

    更新日期：1971-10-01 00:00:00

  • Coronary vasoconstrictor and vasodilator actions of arachidonic acid in the isolated perfused heart of the rat.

    abstract：:The administration of arachidonic acid (AA) to the isolated perfused heart of the rat usually produced biphasic coronary responses characterized by initial vasoconstriction followed by prolonged vasodilatation. However, some responses were predominantly vasoconstrictor or vasodilator. The non-steroidal anti-inflammato...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1982.tb08783.x

    authors： Belo SE,Talesnik J

    更新日期：1982-02-01 00:00:00

  • Effect of milacemide on extracellular and tissue concentrations of dopamine and 5-hydroxytryptamine in rat frontal cortex.

    abstract：:1. Milacemide is a glycine prodrug which is both an inhibitor and a substrate for monoamine oxidase-type B (MAO-B) and also an inhibitor of MAO-type A (MAO-A). Its effects on dopamine and 5-hydroxytryptamine (5-HT) metabolism in rat frontal cortex tissue and dialysate were evaluated. 2. Dialysate dopamine concentratio...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1992.tb14210.x

    authors： Semba J,Doheny M,Patsalos PN,Sarna G,Curzon G

    更新日期：1992-01-01 00:00:00

  • Alpha 2-adrenoceptor-mediated inhibition of histamine release from rat cerebral cortical slices.

    abstract：:1. Depolarization of rat cerebral cortical slices, prelabelled with [3H]-histidine, in high potassium (40 mM KCl) medium stimulated the release of [3H]-histamine. The K+-evoked release of [3H]-histamine was attenuated by incubation in calcium-free medium and prevented by prior incubation of brain slices with the selec...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1988.tb11758.x

    authors： Hill SJ,Straw RM

    更新日期：1988-12-01 00:00:00

  • Sominone enhances neurite outgrowth and spatial memory mediated by the neurotrophic factor receptor, RET.

    abstract：BACKGROUND AND PURPOSE:Orally administered withanoside IV (a compound isolated from the roots of Withania somnifera) improved memory deficits in mice with a model of Alzheimer's disease induced by the amyloid peptide Abeta(25-35). Sominone, an aglycone of withanoside IV, was identified as an active metabolite after ora...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.2009.00313.x

    authors： Tohda C,Joyashiki E

    更新日期：2009-08-01 00:00:00

  • nNOS-CAPON blockers produce anxiolytic effects by promoting synaptogenesis in chronic stress-induced animal models of anxiety.

    abstract：BACKGROUND AND PURPOSE:Anxiety disorder is a common mental health disorder. However, there are few safe and fast-acting anxiolytic drugs available that can treat anxiety disorder. We previously demonstrated that the interaction of neuronal NOS (nNOS) with its carboxy-terminal PDZ ligand (CAPON) is involved in regulatin...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/bph.15084

    authors： Zhu LJ,Shi HJ,Chang L,Zhang CC,Si M,Li N,Zhu DY

    更新日期：2020-08-01 00:00:00

  • Importance of membrane-bound catechol-O-methyltransferase in L-DOPA metabolism: a pharmacokinetic study in two types of Comt gene modified mice.

    abstract：BACKGROUND AND PURPOSE:Catechol-O-methyltransferase (COMT) metabolizes compounds containing catechol structures and has two forms: soluble (S-COMT) and membrane-bound (MB-COMT). Here we report the generation of a mouse line that expresses MB-COMT but not S-COMT. We compared the effects of deleting S-COMT only or both C...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.2009.00494.x

    authors： Käenmäki M,Tammimäki A,Garcia-Horsman JA,Myöhänen T,Schendzielorz N,Karayiorgou M,Gogos JA,Männistö PT

    更新日期：2009-12-01 00:00:00

  • Pulmonary metabolism of bradykinin analogues and the contribution of angiotensin converting enzyme to bradykinin inactivation in isolated lungs.

    abstract：:1 The activity and pulmonary metabolism of two peptides, 7-homo Pro-bradykinin and 8-homo Phe-bradykinin were studied in isolated systems. 2 Both analogues were about 50-70 times less active than bradykinin on the guinea-pig ileum and 70-160 times less active on isolated strips of cat terminal ileum. 3 The action of b...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1977.tb06985.x

    authors： Bakhle YS

    更新日期：1977-01-01 00:00:00

  • Effect of 781094, a new selective alpha-adrenoceptor antagonist, on the aggregatory responses of human blood platelets and on binding of [3H]-dihydroergocryptine to these cells.

    abstract：:781094 (2-(2(1, 4-benzodioxanyl))-2-imidazoline hydrochloride) is a potent competitive inhibitor of the aggregatory responses of human platelets induced by adrenaline (pA2 = 7.3) and UK-14304. 781094 is a more potent inhibitor of the pro-aggregatory response to clonidine than of that to methoxamine. The alpha 2/alpha ...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1983.tb11012.x

    authors： Kerry R,Scrutton MC

    更新日期：1983-06-01 00:00:00

  • The effects of combined angiotensin converting enzyme inhibition and beta-adrenoceptor blockade on plasma renin activity in anaesthetized dogs.

    abstract：:1. The effects of beta-adrenoceptor blockade on the changes in plasma renin activity (PRA) following angiotensin enzyme (ACE) inhibition were investigated in pentobarbitone-chloralose anaesthetized dogs. 2. ACE-inhibition, with enalapril (2 mg kg-1), caused a significant reduction in systemic arterial blood pressure (...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1992.tb14338.x

    authors： Cambridge D,Whiting MV,Butterfield LJ,Allan G

    更新日期：1992-06-01 00:00:00

  • Metformin attenuates angiotensin II-induced TGFβ1 expression by targeting hepatocyte nuclear factor-4-α.

    abstract：BACKGROUND AND PURPOSE:Metformin, a small molecule, antihyperglycaemic agent, is a well-known activator of AMP-activated protein kinase (AMPK) and protects against cardiac fibrosis. However, the underlying mechanisms remain elusive. TGFβ1 is a key cytokine mediating cardiac fibrosis. Here, we investigated the effects o...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/bph.13753

    authors： Chen R,Feng Y,Wu J,Song Y,Li H,Shen Q,Li D,Zhang J,Lu Z,Xiao H,Zhang Y

    更新日期：2018-04-01 00:00:00

  • Ventral root responses of the hemisected amphibian spinal cord to perfused amino acids in the presence of procaine.

    abstract：:The use of the procaine-blocked hemisected spinal cord preparation to identify the primary action of amino acids and their antagonists on amphibian mononeurones is described. 2 Apart from an anomalous effect of glycine, the responses of frog spinal motoneurones to amino acids were shown to be similar to those of mamma...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1975.tb07427.x

    authors： Evans RH,Watkins JC

    更新日期：1975-12-01 00:00:00

  • β₁-Adrenoceptor stimulation suppresses endothelial IK(Ca)-channel hyperpolarization and associated dilatation in resistance arteries.

    abstract：BACKGROUND AND PURPOSE:In small arteries, small conductance Ca²⁺-activated K⁺ channels (SK(Ca)) and intermediate conductance Ca²⁺-activated K⁺ channels (IK(Ca)) restricted to the vascular endothelium generate hyperpolarization that underpins the NO- and PGI₂-independent, endothelium-derived hyperpolarizing factor respo...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/bph.12160

    authors： Yarova PL,Smirnov SV,Dora KA,Garland CJ

    更新日期：2013-06-01 00:00:00

  • Neurotoxic activity of venom from the Australian eastern mouse spider (Missulena bradleyi) involves modulation of sodium channel gating.

    abstract：:Mouse spiders represent a potential cause of serious envenomation in humans. This study examined the activity of Missulena bradleyi venom in several in vitro preparations. Whilst female M. bradleyi venom at doses up to 0.05 microl ml(-1) failed to alter twitch or resting tension in all preparations used, male venom (0...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1038/sj.bjp.0703494

    authors： Rash LD,Birinyi-Strachan LC,Nicholson GM,Hodgson WC

    更新日期：2000-08-01 00:00:00

  • Effects of inflammatory agents on endothelial lysosomal fragility and their inhibition by anti-inflammatory drugs.

    abstract：:1. Endothelial cells from human umbilical veins were maintained in tissue culture. The fragility of lysosomal membranes were studied by microdensitometry. 2. Histamine (50 microM to 10 mM), 4-methylhistamine (100 nM to 10 mM) and dimaprit (100 nM to 10 mM) increased lysosomal fragility. 2-Thiazolylethylamine and 2-pyr...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1981.tb09140.x

    authors： Yoffe JR

    更新日期：1981-04-01 00:00:00

  • Excessive stimulation of poly(ADP-ribosyl)ation contributes to endothelial dysfunction in pre-eclampsia.

    abstract：:1. Pre-eclampsia is a serious pregnancy disorder associated with widespread activation of the maternal vascular endothelium. Recent evidence implicates a role for oxidative stress in the aetiology of this condition. 2. Reactive oxygen species, particularly superoxide anions, invokes endothelial cell activation through...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1038/sj.bjp.0706055

    authors： Crocker IP,Kenny LC,Thornton WA,Szabo C,Baker PN

    更新日期：2005-03-01 00:00:00