Inhibition of neuromuscular transmission in the myenteric plexus of guinea-pig ileum by omega-conotoxins GVIA, MVIIA, MVIIC and SVIB.

Abstract:

:1. The effects of a number of Ca2+ channel blockers on the transmural electrical stimulation or receptor agonist-elicited contractile responses of guinea-pig ileum were compared. 2. omega-Conotoxins (MVIIA, GVIA, SVIB and MVIIC), but not omega-agatoxin IVA, completely blocked the twitch responses evoked by low frequency (0.1 Hz) transmural stimulation without inhibition of the contractures evoked by exogenous acetylcholine. The concentration-inhibition curves were shifted by changes of external Ca2+. 3. The tetanic contractures produced by a high frequency (30 Hz) train of stimulation were inhibited by omega-conotoxins by only 25-30%, except for omega-conotoxin MVIIC, which produced about 55% inhibition, all significantly less than that produced by atropine (about 70%) or tetrodotoxin (about 85%). Combinations of omega-conotoxins did not produce additive inhibitory effects. 4. The four omega-conotoxins as well as atropine produced similar partial inhibition (53-62%) of the contractures evoked by dimethylphenylpiperazinium, while tetrodotoxin inhibited the contracture completely. 5. Nifedipine and Ni2+ depressed the nerve stimulation-evoked twitch response and tetanic contracture as well as acetylcholine contracture. 6. These observations suggest that, in the myenteric plexus, a subset of N-type Ca2+ channel dominates under low frequency stimulation, while high frequency stimulation may recruit additional channels and non-cholinergic pathways.

journal_name

Br J Pharmacol

authors

Hong SJ,Roan YF,Chang CC

doi

10.1111/j.1476-5381.1996.tb15470.x

subject

Has Abstract

pub_date

1996-06-01 00:00:00

pages

797-803

issue

3

eissn

0007-1188

issn

1476-5381

journal_volume

118

pub_type

杂志文章
  • Naloxone prevents cell-mediated immune alterations in adult mice following repeated mild stress in the neonatal period.

    abstract::1. Mild stress plus mild pain (solvent injection) applied daily to neonatal mice induces hormonal, behavioural and metabolic changes perduring in the adult life. 2. We investigated whether daily mild stress to neonatal mice induces also long-term defined changes of immune response, and whether immune changes are preve...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0704577

    authors: Loizzo A,Loizzo S,Lopez L,d'Amore A,Renzi P,Spampinato S,Di Carlo S,Bacosi A,Zuccaro P,Pacifici R

    更新日期:2002-03-01 00:00:00

  • Involvement of reactive oxygen species in cyclic stretch-induced NF-kappaB activation in human fibroblast cells.

    abstract::1 Uniaxial cyclic stretch leads to an upregulation of cyclooxygenase (COX)-2 through increases in the intracellular Ca(2+) concentration via the stretch-activated (SA) channel and following nuclear factor kappa B (NF-kappaB) activation in human fibroblasts. However, the signaling mechanism as to how the elevated Ca(2+...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0706182

    authors: Amma H,Naruse K,Ishiguro N,Sokabe M

    更新日期:2005-06-01 00:00:00

  • Haemodynamic actions of a novel sino-atrial node function modulator, ZENECA ZD7288, in the anaesthetized dog: a comparison with zatebradine, atenolol and nitrendipine.

    abstract::1. ZENECA ZD7288 (4-(N-ethyl-N-phenylamino)-1,2-dimethyl-6-(methylamino) pyrimidinium chloride, formerly ICI D7288) is a novel sino-atrial node function modulator which selectively slows sinus node rate. Its effects on haemodynamic function have been studied in pentobarbitone anaesthetized dogs, in comparison with zat...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1994.tb17101.x

    authors: Rouse W,Johnson IR

    更新日期:1994-11-01 00:00:00

  • Rho kinase inhibitor fasudil reduces l-DOPA-induced dyskinesia in a rat model of Parkinson's disease.

    abstract:BACKGROUND AND PURPOSE:Rho kinase (ROCK) activation is involved in neuroinflammatory processes leading to progression of neurodegenerative diseases such as Parkinson's disease. Furthermore, ROCK plays a major role in angiogenesis. Neuroinflammation and angiogenesis are mechanisms involved in developing l-DOPA-induced d...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/bph.15275

    authors: Lopez-Lopez A,Labandeira CM,Labandeira-Garcia JL,Muñoz A

    更新日期:2020-12-01 00:00:00

  • Multiple anti-inflammatory pathways triggered by resveratrol lead to amelioration of staphylococcal enterotoxin B-induced lung injury.

    abstract:BACKGROUND AND PURPOSE:Inhalation of the superantigen,staphylococcal enterotoxin B (SEB), leads to the activation of the host T and invariant natural killer (iNK) T cells, thereby resulting in acute lung inflammation and respiratory failure but the underlying mechanism(s) of disease remain elusive, with limited treatme...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.2012.02063.x

    authors: Rieder SA,Nagarkatti P,Nagarkatti M

    更新日期:2012-11-01 00:00:00

  • Endothelin-1 contributes to the progression of renal injury in sickle cell disease via reactive oxygen species.

    abstract:BACKGROUND AND PURPOSE:Endothelin-1 (ET-1) is increased in patients with sickle cell disease and may contribute to the development of sickle cell nephropathy. The current study was designed to determine whether ET-1 acting via the ETA receptor contributes to renal injury in a mouse model of sickle cell disease. EXPERI...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/bph.13380

    authors: Heimlich JB,Speed JS,O'Connor PM,Pollock JS,Townes TM,Meiler SE,Kutlar A,Pollock DM

    更新日期:2016-01-01 00:00:00

  • Identification of selective, high affinity [125I]-angiotensin and [125I]-bradykinin binding sites in rat intestinal epithelia.

    abstract::Specific [125I]-angiotensin II (AII) and [125I]-bradykinin (Bk) binding sites have been identified within epithelial membranes from rat jejunum and descending colon. These high affinity intestinal sites exhibited KD values of 0.64 +/- 0.16 nM for [125I]-AII and 0.69 +/- 0.13 nM for [125I]-Bk, which were similar to tho...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1986.tb10172.x

    authors: Cox HM,Munday KA,Poat JA

    更新日期:1986-01-01 00:00:00

  • Mechanism of the pro-inflammatory activity of sympathomimetic amines in thermic oedema of the rat paw.

    abstract::1 Thermic oedema induced by heating rat paws at 46.5 degrees C was potentiated by local injection of adrenaline, noradrenaline or high doses of isoprenaline. The pro-inflammatory effect of sympathomimetic amines was antagonized by phenoxybenzamine or phentolamine but not by propranolol.2 The subcutaneous space of heat...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1974.tb08568.x

    authors: Green KL

    更新日期:1974-02-01 00:00:00

  • Vagal mechanisms and the effect of indomethacin on bronchoconstrictor stimuli in the guinea-pig.

    abstract::1. In urethane-anaesthetized guinea-pigs, under spontaneous respiration, indomethacin (1 mg kg-1 i.v., 10-45 min) approximately doubled the bronchoconstrictor effect (increase in airways resistance, R(aw)) of equieffective doses of histamine and 5-hydroxytryptamine (5-HT), but not that of acetylcholine or leukotriene ...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1988.tb11556.x

    authors: Mitchell HW,Adcock J

    更新日期:1988-06-01 00:00:00

  • Pharmacological characterization of nicotine-induced acetylcholine release in the rat hippocampus in vivo: evidence for a permissive dopamine synapse.

    abstract::In this study, the mechanism of nicotine-induced hippocampal acetylcholine (ACh) release in awake, freely moving rats was examined using in vivo microdialysis. Systemic administration of nicotine (0.4 mg kg(-1), s.c.) increased the levels of ACh in hippocampal dialysates. The nicotine-induced hippocampal ACh release w...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0702683

    authors: Reid RT,Lloyd GK,Rao TS

    更新日期:1999-07-01 00:00:00

  • Remodelling of the PDE4 cAMP phosphodiesterase isoform profile upon monocyte-macrophage differentiation of human U937 cells.

    abstract::Monocytes and macrophages provide key targets for the action of novel anti-inflammatory therapeutics targeted at inhibition of PDE4 cAMP-specific phosphodiesterases. PDE4 enzymes provide the dominant cAMP phosphodiesterase activity in U937 human monocytic cells. Differentiation of U937 monocytic cells to a macrophage-...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0705770

    authors: Shepherd MC,Baillie GS,Stirling DI,Houslay MD

    更新日期:2004-05-01 00:00:00

  • Blockade of intracellular actions of calcium may protect against ischaemic damage to the gerbil brain.

    abstract::1. The brain cytoprotective effects of a putative calcium-associated protein kinase inhibitor, HA1077, as well as a calcium entry blocker nicardipine were evaluated in models of cerebral ischaemia in Mongolian gerbils. Morphological changes characterizing delayed neuronal death of selectively vulnerable CA1 pyramidal ...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1991.tb12355.x

    authors: Asano T,Ikegaki I,Satoh S,Mochizuki D,Hidaka H,Suzuki Y,Shibuya M,Sugita K

    更新日期:1991-08-01 00:00:00

  • Impaired response to interferon-gamma in activated macrophages due to tyrosine nitration of STAT1 by endogenous nitric oxide.

    abstract::1. Inducible NO synthase (iNOS) expression and activity were measured in the mouse macrophage cell line J774 after exposure to bacterial lipopolysaccharide (LPS) with or without interferon-gamma (IFN-gamma). 2. Inhibition of NOS activity by concomitant N(G)-monomethyl-L-arginine (L-NMMA) treatment further increased iN...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0703838

    authors: Llovera M,Pearson JD,Moreno C,Riveros-Moreno V

    更新日期:2001-01-01 00:00:00

  • Spinal antinociceptive effects of the novel NOP receptor agonist PWT2-nociceptin/orphanin FQ in mice and monkeys.

    abstract:BACKGROUND AND PURPOSE:Using an innovative chemical approach, peptide welding technology (PWT), a tetrabranched derivative of nociceptin/orphanin FQ (N/OFQ) has been generated and pharmacologically characterized. Both in vitro and in vivo PWT2-N/OFQ displayed the same pharmacological profile to the natural ligand. It w...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/bph.13150

    authors: Rizzi A,Sukhtankar DD,Ding H,Hayashida K,Ruzza C,Guerrini R,Calò G,Ko MC

    更新日期:2015-07-01 00:00:00

  • Characterization of biosynthesis and modes of action of prostaglandin E2 and prostacyclin in guinea pig mesenteric lymphatic vessels.

    abstract:BACKGROUND AND PURPOSE:Rhythmical transient constrictions of the lymphatic vessels provide the means for efficient lymph drainage and interstitial tissue fluid balance. This activity is critical during inflammation, to avoid or limit oedema resulting from increased vascular permeability, mediated by the release of vari...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.2009.00493.x

    authors: Rehal S,Blanckaert P,Roizes S,von der Weid PY

    更新日期:2009-12-01 00:00:00

  • Role of putative neurotransmitters in the central gastric antisecretory effect of prostaglandin E2 in rats.

    abstract::The role of putative neurotransmitters of the central nervous system in the central gastric antisecretory effect of prostaglandin E2 (PGE2) was investigated in pylorus-ligated rats. Pretreatment of the rats with an intracerebroventricular (i.c.v.) injection of 6-hydroxydopamine (6-OHDA) prevented the antisecretory eff...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1985.tb08849.x

    authors: Puurunen J

    更新日期:1985-05-01 00:00:00

  • Inhibitory effect of 1,2,3,4-tetrahydro-9-aminoacridine on the depolarization-induced release of GABA from cerebral cortex.

    abstract::1,2,3,4-Tetrahydro-9-aminoacridine (THA) has an inhibitory effect on the activity of acetylcholinesterase which has led to its use in the treatment of Alzheimer's disease. Other actions of THA include the inhibition of voltage-dependent ion channels. In this paper we describe the effect of THA on the depolarization-in...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1988.tb11615.x

    authors: de Belleroche J,Gardiner IM

    更新日期:1988-08-01 00:00:00

  • Superagonism at G protein-coupled receptors and beyond.

    abstract::Ligands targeting GPCRs can be categorized according to their intrinsic efficacy to trigger a specific, receptor-mediated response. A ligand endowed with the same level of efficacy as the endogenous agonist can be classified as a full agonist, whereas a compound that displays greater efficacy, that is, higher receptor...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1111/bph.13278

    authors: Schrage R,De Min A,Hochheiser K,Kostenis E,Mohr K

    更新日期:2016-10-01 00:00:00

  • Metabolism of prostaglandin E in dog kidneys.

    abstract::1. The biotransformation of prostaglandin E(1) (PGE(1)) was studied in the isolated, perfused dog kidneys.2. An average 43% of PGE(1) was converted into the less polar metabolite I by a single passage through the kidney. As the re-circulation of the perfusate continued, PGE(1) was converted not only into metabolite I ...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1970.tb09924.x

    authors: Nakano J

    更新日期:1970-10-01 00:00:00

  • Non-adrenergic, non-cholinergic contractions in the electrically field stimulated guinea-pig trachea.

    abstract::1. The effects of drugs and altering stimulus parameters on neurogenic responses to electrical field stimulation (EFS) have been investigated in distal and proximal portions of the guinea-pig trachea. 2. In the presence of indomethacin (3 microM) and propranolol (1 microM) two contractile phases were evident in both t...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1990.tb14174.x

    authors: Ellis JL,Undem BJ

    更新日期:1990-12-01 00:00:00

  • Compartmentation of β2 -Adrenergic Receptor Stimulated cAMP Responses by Phosphodiesterases Type 2 and 3 in Cardiac Ventricular Myocytes.

    abstract:BACKGROUND AND PURPOSE:In cardiac myocytes, cAMP produced by both β1 and β2 -adrenergic receptors (ARs) results in an increase in L-type Ca2+ channel activity and myocyte contraction. However, only cAMP produced by β1 ARs is able to enhance myocyte relaxation through phospholamban-dependent regulation of the sarco/endo...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/bph.15382

    authors: Rudokas MW,Post JP,Sataray-Rodriguez A,Sherpa RT,Moshal KS,Agarwal SR,Harvey RD

    更新日期:2021-01-21 00:00:00

  • Assessment of renal dopaminergic system activity in the nitric oxide-deprived hypertensive rat model.

    abstract::1. The present paper reports changes in the urinary excretion of dopamine, 5-hydroxytryptamine and amine metabolites in nitric oxide deprived hypertensive rats during long-term administration of NG-nitro-L-arginine methyl ester (L-NAME). Aromatic L-amino acid decarboxylase (AAAD) activity in renal tissues and the abil...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1995.tb13362.x

    authors: Soares-da-Silva P,Pestana M,Vieira-Coelho MA,Fernandes MH,Albino-Teixeira A

    更新日期:1995-04-01 00:00:00

  • Diverse mechanisms underlying the regulation of ion channels by carbon monoxide.

    abstract::Carbon monoxide (CO) is firmly established as an important, physiological signalling molecule as well as a potent toxin. Through its ability to bind metal-containing proteins, it is known to interfere with a number of intracellular signalling pathways, and such actions can account for its physiological and pathologica...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1111/bph.12760

    authors: Peers C,Boyle JP,Scragg JL,Dallas ML,Al-Owais MM,Hettiarachichi NT,Elies J,Johnson E,Gamper N,Steele DS

    更新日期:2015-03-01 00:00:00

  • The inhibitory effects of iberiotoxin and 4-aminopyridine on the relaxation induced by beta 1- and beta 2-adrenoceptor activation in rat aortic rings.

    abstract::1. In rat aortic rings contracted by phenylephrine, the relaxation induced by isoprenaline was partly inhibited by iberiotoxin, (ibTX), tetraethylammonium, 4-aminopyridine (4-AP) and 1,9-dideoxyforskolin, but not by glibenclamide. 2. In the presence of 4-AP, 1,9-dideoxyforskolin failed to inhibit further the relaxant ...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1996.tb15700.x

    authors: Satake N,Shibata M,Shibata S

    更新日期:1996-10-01 00:00:00

  • Differential inhibition of tumour cell-induced platelet aggregation by the nicotinate aspirin prodrug (ST0702) and aspirin.

    abstract:BACKGROUND AND PURPOSE:Tumour cell-induced platelet aggregation (TCIPA) facilitates cancer cell invasion, angiogenesis and the formation of metastatic foci. TCIPA can be modulated by pharmacological inhibitors of MMP-2 and ADP; however, the COX inhibitor aspirin did not prevent TCIPA. In this study, we have tested the ...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.2011.01794.x

    authors: Medina C,Harmon S,Inkielewicz I,Santos-Martinez MJ,Jones M,Cantwell P,Bazou D,Ledwidge M,Radomski MW,Gilmer JF

    更新日期:2012-06-01 00:00:00

  • Influence of dopamine receptor agonists on gastric acid secretion induced by intraventricular administration of thyrotropin-releasing hormone in the perfused stomach of anaesthetized rats.

    abstract::1 The influence of dopamine receptor agonists on gastric acid secretion stimulated by thyrotropin-releasing hormone (TRH) was studied in the perfused stomach of anaesthetized rats. 2 Intraventricular TRH produced a dose-dependent stimulation of basal gastric acid secretion. 3 Pretreatment with apomorphine, bromocripti...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1983.tb10524.x

    authors: Maeda-Hagiwara M,Watanabe K

    更新日期:1983-05-01 00:00:00

  • 4-bromopropofol decreases action potential generation in spinal neurons by inducing a glycine receptor-mediated tonic conductance.

    abstract:BACKGROUND AND PURPOSE:Impaired function of spinal strychnine-sensitive glycine receptors gives rise to chronic pain states and movement disorders. Therefore, increased activity of glycine receptors should help to treat such disorders. Although compounds targeting glycine receptors with a high selectivity are lacking, ...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/bph.12880

    authors: Eckle VS,Grasshoff C,Mirakaj V,O'Neill PM,Berry NG,Leuwer M,Antkowiak B

    更新日期:2014-12-01 00:00:00

  • Role of CCK and potential utility of CCK1 receptor antagonism in the treatment of pancreatitis induced by biliary tract obstruction.

    abstract:BACKGROUND AND PURPOSE:Cholecystokinin (CCK) stimulates the release of amylase and lipase from the normal pancreas. However, it is not clear to what extent this occurs in the early stages of pancreatitis induced by biliary tract obstruction in the rat and whether CCK initiates an inflammatory cascade in this condition....

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/bjp.2008.44

    authors: Barrett TD,Yan W,Freedman JM,Lagaud GJ,Breitenbucher JG,Shankley NP

    更新日期:2008-04-01 00:00:00

  • Neuroadaptations of presynaptic and postsynaptic GABAB receptor function in the paraventricular nucleus in response to chronic unpredictable stress.

    abstract:BACKGROUND AND PURPOSE:Chronic stress impairs GABAA (GABA type A) receptor-mediated inhibition in the hypothalamic paraventricular nucleus (PVN). It is not clear whether GABAB receptor function is also altered. We hypothesize that chronic stress alters GABAB receptor function in PVN corticotrophin-releasing hormone (CR...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/bph.13924

    authors: Gao Y,Zhou JJ,Zhu Y,Wang L,Kosten TA,Zhang X,Li DP

    更新日期:2017-09-01 00:00:00

  • Pharmacokinetic-pharmacodynamic modelling of the anti-lipolytic and anti-ketotic effects of the adenosine A1-receptor agonist N6-(p-sulphophenyl)adenosine in rats.

    abstract::1. The purpose of this study was to develop and validate an integrated pharmacokinetic-pharmacodynamic model for the anti-lipolytic effects of the adenosine A1-receptor agonist N6-(p-sulphophenyl)adenosine (SPA). Tissue selectivity of SPA was investigated by quantification of haemodynamic and anti-lipolytic effects in...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0701412

    authors: van Schaick EA,de Greef HJ,Langemeijer MW,Sheehan MJ,IJzerman AP,Danhof M

    更新日期:1997-10-01 00:00:00