Influence of epithelium on the inhibition of melittin-induced contraction of guinea-pig isolated trachea by the potassium channel opener NIP-121.

Abstract:

:1. We have investigated the effect of the potassium channel opener, NIP-121, on contraction elicited by melittin (a phospholipase A2 activator) in epithelium-intact and epithelium-denuded trachea isolated from guinea-pigs. The effects of NIP-121 were compared with those of isoprenaline, aminophylline and hydrocortisone. 2. In the presence of the cyclo-oxygenase inhibitor, indomethacin (5 microM), melittin (3 micrograms ml-1) caused time-dependent contraction. The melittin-induced contractile response was significantly augmented by removal of the epithelium and was concentration-dependently and completely inhibited by the phospholipase A2 (PLA2) inhibitor, p-bromophenacyl bromide (BPB 10-100 microM), and the lipoxygenase inhibitor, phenidone (10-300 microM). Similar inhibition of the melittin response by BPB (10 microM) and phenidone (10 microM) was observed in the epithelium-denuded trachea. 3. Concentration-dependent inhibition of the melittin response was induced by preincubation with NIP-121 (0.03 and 0.1 microM), isoprenaline (0.001 and 0.01 microM), aminophylline (30 and 100 microM) and hydrocortisone (100 and 300 microM). The effect of NIP-121 was abolished by glibenclamide (1 microM). 4. The inhibitory effect of NIP-121 on the melittin response was greatly reduced by removing the epithelium while that of the isoprenaline, aminophylline or hydrocortisone was not changed. 5. The inhibition of the melittin response by these drugs was similar to their inhibition of the contraction elicited by a low concentration (3 nM) of leukotriene D4 (LTD4) in the epithelium-intact trachea. Inhibition of the LTD4 response by NIP-121 was not observed in the epithelium-denuded trachea. However, higher concentrations of NIP-121 (0.3 and 1 microM) did inhibit LTD4-induced contractions of epithelium-denuded trachea.6. These findings suggest that melittin causes epithelium-dependent contraction of the guinea-pig isolated trachea which is mediated by products of lipoxygenase activity. NIP-121 may inhibit the melittin response by activating glibenclamide-sensitive potassium channels, which appear to be epithelium-dependent (an indirect effect of NIP-121 apart from its direct effect on the airway smooth muscle) while isoprenaline, aminophylline and hydrocortisone act directly to relax the trachealis smooth muscle.

journal_name

Br J Pharmacol

authors

Shikada K,Tanaka S

doi

10.1111/j.1476-5381.1993.tb13734.x

subject

Has Abstract

pub_date

1993-08-01 00:00:00

pages

1091-6

issue

4

eissn

0007-1188

issn

1476-5381

journal_volume

109

pub_type

杂志文章
  • Endothelium-dependent relaxation to the B1 kinin receptor agonist des-Arg9-bradykinin in human coronary arteries.

    abstract::Des-Arg9-bradykinin (des-Arg9-BK) caused endothelium-dependent relaxations in human, isolated coronary arteries which upregulated with in vitro incubation time. Relaxations to des-Arg9-BK were inhibited by the B1 receptor antagonist, des-Arg9-[Leu3]-BK (pK(B), 6.14 +/- 0.11) but were unaffected by the B2 receptor anta...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1995.tb15108.x

    authors: Drummond GR,Cocks TM

    更新日期:1995-12-01 00:00:00

  • Loperamide mobilizes intracellular Ca2+ stores in insulin-secreting HIT-T15 cells.

    abstract::1 We have investigated the effects of loperamide on intracellular Ca(2+) stores and membrane K(+) channels in insulin-secreting hamster insulinoma (HIT-T15) cells. 2 In cell-attached patch-clamp mode, loperamide (3-250 micro M) activated large single-channel currents. The loperamide-activated currents were tentatively...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0705263

    authors: He LP,Mears D,Atwater I,Rojas E,Cleemann L

    更新日期:2003-05-01 00:00:00

  • Aurora kinase inhibitor tozasertib suppresses mast cell activation in vitro and in vivo.

    abstract:BACKGROUND AND PURPOSE:Mast cells are important in allergic reactions. Here, we assessed the anti-allergic effects of the anti-cancer drug tozasertib specifically regarding regulatory effects on mast cell activation. EXPERIMENTAL APPROACH:Tozasertib effects on mast cell degranulation were determined by measuring β-hex...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/bph.15012

    authors: Zhang LN,Ji K,Sun YT,Hou YB,Chen JJ

    更新日期:2020-06-01 00:00:00

  • Pre- and postjunctional effects of clonidine- and oxymetazoline-like compounds in guinea-pig ileal preparations.

    abstract::1 Noradrenaline and 28 imidazolidine (clonidine-like) and imidazoline (oxymetazoline-like) compounds with various phenyl ring substituents have been examined for their ability to inhibit responses to transmural stimulation and exogenous acetylcholine in ileal preparations from reserpine-treated guinea-pigs.2 The bathi...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1981.tb10429.x

    authors: Malta E,Raper C,Tawa PE

    更新日期:1981-06-01 00:00:00

  • Anti-anhedonic effect of selective serotonin reuptake inhibitors with affinity for sigma-1 receptors in picrotoxin-treated mice.

    abstract:BACKGROUND AND PURPOSE:Prefrontal dopamine release by the combined activation of 5-HT1A and sigma-1 (σ1 ) receptors is enhanced by the GABAA receptor antagonist picrotoxin in mice. Here, we examined whether this neurochemical event was accompanied by behavioural changes. EXPERIMENTAL APPROACH:Male mice were treated wi...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/bph.13692

    authors: Hasebe S,Ago Y,Watabe Y,Oka S,Hiramatsu N,Tanaka T,Umehara C,Hashimoto H,Takuma K,Matsuda T

    更新日期:2017-02-01 00:00:00

  • An examination of 5-hydroxytryptamine receptors in human saphenous vein.

    abstract::We have examined the effects of antagonists on the isometric contraction of the human saphenous vein produced by 5-hydroxytryptamine (5-HT). The 5-HT2-antagonist ketanserin (1 microM) had little effect on the lower part of the concentration-response curve to 5-HT, but markedly shifted the upper part of the curve. Yohi...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1986.tb11122.x

    authors: Docherty JR,Hyland L

    更新日期:1986-09-01 00:00:00

  • Alfuzosin, a selective alpha 1-adrenoceptor antagonist in the lower urinary tract.

    abstract::1. Phenylephrine-induced contractions of rabbit isolated trigone and urethra were antagonized in a competitive manner by alfuzosin (pA2 7.44 and 7.30, respectively) and prazosin. 2. The characteristics of [3H]-prazosin binding to human prostatic adenoma tissue were evaluated. [3H]-prazosin was potently displaced by al...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1993.tb13762.x

    authors: Lefèvre-Borg F,O'Connor SE,Schoemaker H,Hicks PE,Lechaire J,Gautier E,Pierre F,Pimoule C,Manoury P,Langer SZ

    更新日期:1993-08-01 00:00:00

  • Release of a soluble ATPase from the rabbit isolated vas deferens during nerve stimulation.

    abstract::The properties of the ATPase released during electrical field stimulation (EFS) (8 Hz, 25 s) of the sympathetic nerves of the superfused rabbit isolated vas deferens were investigated. Superfusate collected during EFS rapidly metabolised exogenous ATP (100 microM) and 50% was broken down in 5.67+/-0.65 min. The main m...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0703662

    authors: Westfall TD,Menzies JR,Liberman R,Waterston S,Ramphir N,Westfall DP,Sneddon P,Kennedy C

    更新日期:2000-11-01 00:00:00

  • Exacerbation of DSS-induced colitis in mice lacking kinin B(1) receptors through compensatory up-regulation of kinin B(2) receptors: the role of tight junctions and intestinal homeostasis.

    abstract:BACKGROUND AND PURPOSE:Kinins are pro-inflammatory peptides that are released during tissue injury, including that caused by inflammatory bowel disease. Herein, we assessed the role and underlying mechanisms through which the absence of kinin B(1) receptors exacerbates the development of dextran sulfate sodium (DSS)-i...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.2012.02136.x

    authors: Marcon R,Claudino RF,Dutra RC,Bento AF,Schmidt EC,Bouzon ZL,Sordi R,Morais RL,Pesquero JB,Calixto JB

    更新日期:2013-01-01 00:00:00

  • The effects of aldose reductase inhibition with ponalrestat on changes in vascular function in streptozotocin diabetic rats.

    abstract::1. The responses of rat isolated aortae to vasoconstrictor and vasodilator agents have been studied in 14-day streptozotocin-diabetic rats. The effects of treatment with the aldose reductase inhibitor, ponalrestat, on these responses have also been investigated. 2. Maximum contractile responses and aortic sensitivity ...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1994.tb17028.x

    authors: Otter DJ,Chess-Williams R

    更新日期:1994-10-01 00:00:00

  • Inverse agonist and neutral antagonist actions of synthetic compounds at an insect 5-HT1 receptor.

    abstract:BACKGROUND AND PURPOSE:5-Hydroxytryptamine (5-HT) has been shown to control and modulate many physiological and behavioural functions in insects. In this study, we report the cloning and pharmacological properties of a 5-HT(1) receptor of an insect model for neurobiology, physiology and pharmacology. EXPERIMENTAL APPR...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.2010.00638.x

    authors: Troppmann B,Balfanz S,Baumann A,Blenau W

    更新日期:2010-04-01 00:00:00

  • Inhibition of histamine release from human lung in vitro by antihistamines and related drugs.

    abstract::1 A series of cationic, lipophilic histamine H1-receptor antagonists, neuroleptics, antidepressants and monoamine oxidase inhibitors were tested for their effects on anti-IgE-induced histamine release from human lung fragments in vitro. 2 They had a biphasic effect: at low concentrations a dose-related inhibition of h...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1980.tb07919.x

    authors: Church MK,Gradidge CF

    更新日期:1980-08-01 00:00:00

  • Hypoxia activates 15-PGDH and its metabolite 15-KETE to promote pulmonary artery endothelial cells proliferation via ERK1/2 signalling.

    abstract:BACKGROUND AND PURPOSE:Dysfunction and injury of endothelial cells in the pulmonary artery play critical roles in the hypertension induced by chronic hypoxia. One consequence of hypoxia is increased activity of 15-hydroxyprostaglandin dehydrogenase (PGDH). Here, we have explored, in detail, the effects of hypoxia on th...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/bph.12594

    authors: Ma C,Liu Y,Wang Y,Zhang C,Yao H,Ma J,Zhang L,Zhang D,Shen T,Zhu D

    更新日期:2014-07-01 00:00:00

  • Some central effects in mice of compounds related to nicotine.

    abstract::1. Some hydroxy-, amino-, and methoxy- phenylalkyltrimethylammonium compounds, beta-pyridylmethyl- dimethylamine and pyrrolidine, and beta-pyridylethyltrimethylammonium, were tested on avoidance learning in mice and their effects were compared with those of (-)-nicotine.2. The o- and m- hydroxybenzyl-, o-hydroxyphenet...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1970.tb10372.x

    authors: Barlow RB,Oliverio A,Satta M,Thompson GM

    更新日期:1970-07-01 00:00:00

  • Metabolic responses to BRL37344 and clenbuterol in soleus muscle and C2C12 cells via different atypical pharmacologies and beta2-adrenoceptor mechanisms.

    abstract:BACKGROUND AND PURPOSE:Picomolar concentrations of the beta3-adrenoceptor agonist BRL37344 stimulate 2-deoxyglucose uptake in soleus muscle via undefined receptors. Higher concentrations alter uptake, apparently via beta2-adrenoceptors. Effects of BRL37344 and beta2-adrenoceptor agonists are compared. EXPERIMENTAL APP...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/bjp.2008.244

    authors: Ngala RA,O'Dowd J,Wang SJ,Agarwal A,Stocker C,Cawthorne MA,Arch JR

    更新日期:2008-10-01 00:00:00

  • Blockade of adenosine A2B receptors ameliorates murine colitis.

    abstract:BACKGROUND AND PURPOSE:The adenosine 2B (A2B) receptor is the predominant adenosine receptor expressed in the colon. Acting through the A2B receptor, adenosine mediates chloride secretion, as well as fibronectin and interleukin (IL)-6 synthesis and secretion in intestinal epithelial cells. A2B receptor mRNA and protein...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/bjp.2008.227

    authors: Kolachala V,Ruble B,Vijay-Kumar M,Wang L,Mwangi S,Figler H,Figler R,Srinivasan S,Gewirtz A,Linden J,Merlin D,Sitaraman S

    更新日期:2008-09-01 00:00:00

  • Blockade of the 5-HT transporter contributes to the behavioural, neuronal and molecular effects of cocaine.

    abstract:BACKGROUND AND PURPOSE:The psychostimulant cocaine induces complex molecular, cellular and behavioural responses as a consequence of inhibiting presynaptic dopamine, noradrenaline and 5-HT transporters. To elucidate 5-HT transporter (SERT)-specific contributions to cocaine action, we evaluated cocaine effects in the SE...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/bph.13899

    authors: Simmler LD,Anacker AMJ,Levin MH,Vaswani NM,Gresch PJ,Nackenoff AG,Anastasio NC,Stutz SJ,Cunningham KA,Wang J,Zhang B,Henry LK,Stewart A,Veenstra-VanderWeele J,Blakely RD

    更新日期:2017-08-01 00:00:00

  • No proarrhythmic properties of the antibiotics Moxifloxacin or Azithromycin in anaesthetized dogs with chronic-AV block.

    abstract:BACKGROUND & PURPOSE:The therapeutically available quinolone antibiotic moxifloxacin has been used as a positive control for prolonging the QT interval in both clinical and non-clinical studies designed to assess the potential of new drugs to delay cardiac repolarization. Despite moxifloxacin prolonging QT, it has not ...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0706900

    authors: Thomsen MB,Beekman JD,Attevelt NJ,Takahara A,Sugiyama A,Chiba K,Vos MA

    更新日期:2006-12-01 00:00:00

  • Modulation of visceral pain and inflammation by protease-activated receptors.

    abstract::The gastrointestinal (GI) tract is exposed to a large array of proteases, under both physiological and pathophysiological conditions. The discovery of G protein-coupled receptors activated by proteases, the protease-activated receptors (PARs), has highlighted new signaling functions for proteases in the GI tract, part...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1038/sj.bjp.0705750

    authors: Vergnolle N

    更新日期:2004-04-01 00:00:00

  • Proanthocyanidins and hydrolysable tannins: occurrence, dietary intake and pharmacological effects.

    abstract::Tannins are a heterogeneous group of high MW, water-soluble, polyphenolic compounds, naturally present in cereals, leguminous seeds and, predominantly, in many fruits and vegetables, where they provide protection against a wide range of biotic and abiotic stressors. Tannins exert several pharmacological effects, inclu...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1111/bph.13630

    authors: Smeriglio A,Barreca D,Bellocco E,Trombetta D

    更新日期:2017-06-01 00:00:00

  • Chronic exposure of sensory neurones to increased levels of nerve growth factor modulates CB1/TRPV1 receptor crosstalk.

    abstract:BACKGROUND:Anandamide (AEA) activates both cannabinoid CB(1) and TRPV1 receptors, which are expressed on cultured dorsal root ganglion neurones. Increased levels of nerve growth factor (NGF) are associated with chronic pain states. EXPERIMENTAL APPROACH:The aim of this study was to compare of the effects of AEA on CB(...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0707411

    authors: Evans RM,Scott RH,Ross RA

    更新日期:2007-10-01 00:00:00

  • Protease-activated receptor 1 inhibition protects mice against thrombin-dependent respiratory syncytial virus and human metapneumovirus infections.

    abstract:BACKGROUND AND PURPOSE:Protease-activated receptor 1 (PAR1) has been demonstrated to be involved in the pathogenesis of viral diseases. However, its role remains controversial. The goal of our study was to investigate the contribution of PAR1 to respiratory syncytial virus (RSV) and human metapneumovirus (hMPV) infecti...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/bph.14084

    authors: Lê VB,Riteau B,Alessi MC,Couture C,Jandrot-Perrus M,Rhéaume C,Hamelin MÈ,Boivin G

    更新日期:2018-01-01 00:00:00

  • Differential classification of vascular smooth muscle and endothelial cell 5-HT receptors by use of tryptamine analogues.

    abstract::In ring preparations of the rabbit external jugular vein contracted with the thromboxane-mimetic U-46619, submicromolar concentrations of 5-hydroxytryptamine (5-HT) and chemically related analogues produced relaxations that were dependent on the integrity of the vascular endothelium. The receptor mediating endothelium...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1987.tb10287.x

    authors: Leff P,Martin GR,Morse JM

    更新日期:1987-06-01 00:00:00

  • [Nphe1,Arg14,Lys15]nociceptin-NH2, a novel potent and selective antagonist of the nociceptin/orphanin FQ receptor.

    abstract::1. Nociceptin/orphanin FQ (N/OFQ) modulates several biological functions by activating a specific G-protein coupled receptor (NOP). Few molecules are available that selectively activate or block the NOP receptor. Here we describe the in vitro and in vivo pharmacological profile of a novel NOP receptor ligand, [Nphe(1)...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0704706

    authors: Calo G,Rizzi A,Rizzi D,Bigoni R,Guerrini R,Marzola G,Marti M,McDonald J,Morari M,Lambert DG,Salvadori S,Regoli D

    更新日期:2002-05-01 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

  • Nonspecific supersensitivity of the guinea-pig vas deferens produced by decentralization and reserpine treatment.

    abstract::1. The sensitivity of the guinea-pig vas deferens to noradrenaline, histamine, methylfurmethide and potassium was examined in vitro following decentralization and reserpine treatment.2. One day after decentralization or administration of reserpine (1.0 mg/kg daily) the sensitivity of the vas deferens was not increased...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1970.tb09560.x

    authors: Westfall DP

    更新日期:1970-05-01 00:00:00

  • Facilitation by clonidine of purine release induced by high KCl from the rabbit pulmonary artery.

    abstract::1 The effect of clonidine on the 3H-purine release evoked by KCl or (-)-adrenaline was assessed in the superfused helical strip of the rabbit pulmonary artery pretreated with [3H]-adenosine. 2 Clonidine (3 x 10(-5) M to 10(-4) M) significantly enhanced the 3H-purine efflux evoked by 50 mM KCl but not by 3 x 10(-6) M) ...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1981.tb10482.x

    authors: Katsuragi T,Su C

    更新日期:1981-11-01 00:00:00

  • The mechanism of action of cantharidin in smooth muscle.

    abstract::1. The aim of this study was to investigate the mechanism(s) of the vasoconstrictor effect of cantharidin in bovine preparations. 2. Catalytic subunits of protein phosphatase type 1 (PP 1) and type 2A (PP 2A) were immunologically identified in coronary arteries, isolated smooth muscle cells and ventricular myocardium....

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0701668

    authors: Knapp J,Bokník P,Huke S,Lüss H,Müller FU,Müller T,Nacke P,Schmitz W,Vahlensieck U,Neumann J

    更新日期:1998-03-01 00:00:00

  • G protein-coupled oestrogen receptor 1 (GPER1)/GPR30: a new player in cardiovascular and metabolic oestrogenic signalling.

    abstract::Oestrogens are important sex hormones central to health and disease in both genders that have protective effects on the cardiovascular and metabolic systems. These hormones act in complex ways via both genomic and non-genomic mechanisms. The genomic mechanisms are relatively well characterized, whereas the non-genomic...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1111/j.1476-5381.2011.01235.x

    authors: Nilsson BO,Olde B,Leeb-Lundberg LM

    更新日期:2011-07-01 00:00:00

  • Effects of a phosphodiesterase IV inhibitor rolipram on microsphere embolism-induced defects in memory function and cerebral cyclic AMP signal transduction system in rats.

    abstract::The effects of treatment with rolipram, a specific phosphodiesterase IV inhibitor, on learning and memory function and on the cyclic AMP/PKA/CREB signal transduction system were examined in rats with microsphere embolism (ME)-induced cerebral ischaemia. Sustained cerebral ischaemia was induced by the injection of 900 ...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0704629

    authors: Nagakura A,Niimura M,Takeo S

    更新日期:2002-04-01 00:00:00