The potent depolarizing action of palytoxin isolated from Palythoa tubercurosa on the isolated spinal cord of the frog.

Abstract:

:1. The effects of palytoxin (PTX) isolated from Palythoa tubercurosa were tested on the isolated intra-arterially perfused spinal cord of the frog. The resting and evoked potentials were recorded by means of a sucrose-gap technique. 2. PTX caused a marked depolarization of both ventral and dorsal roots. The minimum effective concentration was extremely low, approximately 10(-11) M. During the depolarization the evoked ventral and dorsal root potentials were markedly reduced in amplitude. The ventral root reflex was first augmented and then decreased. 3. The depolarization caused by PTX was markedly reduced when the preparation was perfused with NaCl-deficient medium. However, tetrodotoxin (10(-7) M) only slightly inhibited the depolarization. 4. In a high Ca2+ medium (3.6 mM), the time required to reach the maximum depolarization evoked by PTX was significantly prolonged. In contrast, in a low Ca2+ medium (0.9 mM), PTX caused a marked depolarization soon after application. In a Ca2+-free, Mg2+ (9.0 mM) medium, PTX caused rhythmic oscillatory potentials in both ventral and dorsal roots. 5. The potency of N-acetyl PTX was one hundredth that of the parent compound. 6. It is suggested that PTX may interfere with the stabilizing action of Ca2+ on the neuronal membrane, consequently facilitating Na+ permeability. The primary amine in the PTX molecule may be important for its pharmacological action.

journal_name

Br J Pharmacol

authors

Kudo Y,Shibata S

doi

10.1111/j.1476-5381.1980.tb10975.x

subject

Has Abstract

pub_date

1980-01-01 00:00:00

pages

575-9

issue

2

eissn

0007-1188

issn

1476-5381

journal_volume

71

pub_type

杂志文章
  • Characterization of the postjunctional alpha 2C-adrenoceptor mediating vasoconstriction to UK14304 in porcine pulmonary veins.

    abstract:BACKGROUND AND PURPOSE:In terms of postjunctional alpha(2)-adrenoceptors in the pulmonary circulation, no evidence is available with regard to the receptor subtypes mediating vasoconstriction. Therefore, we characterized the alpha(2)-adrenoceptor subtypes mediating contraction in isolated porcine pulmonary veins. EXPE...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0707221

    authors: Görnemann T,von Wenckstern H,Kleuser B,Villalón CM,Centurión D,Jähnichen S,Pertz HH

    更新日期:2007-05-01 00:00:00

  • Role of 5-HT(1) receptor subtypes in the modulation of pain and synaptic transmission in rat spinal superficial dorsal horn.

    abstract:BACKGROUND AND PURPOSE:5-HT receptor agonists have variable nociceptive effects within the spinal cord. While there is some evidence for 5-HT(1A) spinally-mediated analgesia, the role of other 5-HT(1) receptor subtypes remains unclear. In the present study, we examined the spinal actions of a range of 5-HT(1) agonists,...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.2011.01685.x

    authors: Jeong HJ,Mitchell VA,Vaughan CW

    更新日期:2012-03-01 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

  • Antagonism by fenamates and like-acting drugs of bronchoconstriction induced by bradykinin or antigen in the guinea-pig.

    abstract::1. Nine non-steroidal anti-inflammatory drugs were tested for antagonism of bradykinin-induced bronchoconstriction in guinea-pig lungs in vivo. Only one, benzydamine, was inactive.2. The descending order of potency of the active anti-inflammatory drugs was meclofenamate = Scha 306>Scha 87/2>indoxole>Mi85>indomethacin>...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1968.tb07952.x

    authors: Collier HO,James GW,Piper PJ

    更新日期:1968-09-01 00:00:00

  • Homology-guided mutational analysis reveals the functional requirements for antinociceptive specificity of collapsin response mediator protein 2-derived peptides.

    abstract:BACKGROUND AND PURPOSE:N-type voltage-gated calcium (Cav 2.2) channels are critical determinants of increased neuronal excitability and neurotransmission accompanying persistent neuropathic pain. Although Cav 2.2 channel antagonists are recommended as first-line treatment for neuropathic pain, calcium-current blocking ...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/bph.13737

    authors: Moutal A,Li W,Wang Y,Ju W,Luo S,Cai S,François-Moutal L,Perez-Miller S,Hu J,Dustrude ET,Vanderah TW,Gokhale V,Khanna M,Khanna R

    更新日期:2018-06-01 00:00:00

  • The beta 1- and beta 2-adrenoceptor stimulatory effects of alprenolol, oxprenolol and pindolol: a study in the isolated right atrium and uterus of the rat.

    abstract::The rat isolated right atrium (frequency response) and progesterone-treated rat uterus (relaxation) were used to examine the beta 1- and beta 2-adrenoceptor stimulatory effects of alprenolol, oxprenolol and pindolol. In addition, the beta 1-adrenoceptor stimulatory effect of practolol was studied in the right atrium. ...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1986.tb14582.x

    authors: Abrahamsson T

    更新日期:1986-04-01 00:00:00

  • Phenylglycine derivatives as antagonists of group III metabotropic glutamate receptors expressed on neonatal rat primary afferent terminals.

    abstract::1. Three novel phenylglycine analogues; (RS)-alpha-methyl-3-chloro-4-phosphonophenylglycine (UBP1110), (RS)-alpha-methyl-3-methoxy-4-phosphonophenylglycine (UBP1111) and (RS)-alpha-methyl-3-methyl-4-phosphonophenylglycine (UBP1112) antagonised the depression of the fast component of the dorsal root-evoked ventral root...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0705377

    authors: Miller JC,Howson PA,Conway SJ,Williams RV,Clark BP,Jane DE

    更新日期:2003-08-01 00:00:00

  • Effects of Cl channel blockers on Ca-activated chloride and potassium currents in smooth muscle cells from rabbit portal vein.

    abstract::1. The effects of some chloride channel antagonists were studied on the calcium-activated chloride current (ICl(Ca)) in smooth muscle cells from the rabbit portal vein with the perforated patch technique. 2. 4-Acetamido-4'-isothiocyanatostilbene-2,2'-disulphonic acid (SITS) and 4,4'-diisothiocyanato-stilbene-2,2'-disu...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1994.tb14891.x

    authors: Hogg RC,Wang Q,Large WA

    更新日期:1994-04-01 00:00:00

  • A comparison of the effects of morphine, enkephalin, kyotorphin and D-phenylalanine on rat central neurones.

    abstract::1 Morphine, Met-enkephalin, kyotorphin and D-phenylalanine have been applied by microiontophoresis to neurones in the globus pallidus and cerebral cortex of rats anaesthetized with urethane. 2 In the pallidum, most cells were inhibited by all the agonists, with a high correspondence between cells inhibited by Met-enke...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1983.tb10525.x

    authors: Stone TW

    更新日期:1983-05-01 00:00:00

  • The anti-cancer agent SU4312 unexpectedly protects against MPP(+) -induced neurotoxicity via selective and direct inhibition of neuronal NOS.

    abstract:BACKGROUND AND PURPOSE:SU4312, a potent and selective inhibitor of VEGF receptor-2 (VEGFR-2), has been designed to treat cancer. Recent studies have suggested that SU4312 can also be useful in treating neurodegenerative disorders. In this study, we assessed neuroprotection by SU4312 against 1-methyl-4-phenylpyridinium ...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/bph.12004

    authors: Cui W,Zhang Z,Li W,Hu S,Mak S,Zhang H,Han R,Yuan S,Li S,Sa F,Xu D,Lin Z,Zuo Z,Rong J,Ma ED,Choi TC,Lee SM,Han Y

    更新日期:2013-03-01 00:00:00

  • Rho kinase inhibitors block activation of pancreatic stellate cells.

    abstract::1. In response to pancreatic injury and in cell culture, pancreatic stellate cells (PSCs) are transformed ('activated') into highly proliferative myofibroblast-like cells, which express alpha-smooth muscle actin (alpha-SMA), and produce type I collagen and other extracellular matrix components. There is accumulating e...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0705551

    authors: Masamune A,Kikuta K,Satoh M,Satoh K,Shimosegawa T

    更新日期:2003-12-01 00:00:00

  • Antagonism of adenosine 5'-triphosphate-induced relaxation by 2-2'-pyridylisatogen in the taenia of guinea-pig caecum.

    abstract::1. 2-2' Pyridylisatogen tosylate (PIT) (greater than 2.5 muM) relaxed the guinea-pig isolated taenia caeci by an unknown mechanism. 2. With higher concentrations of PIT (greater than 12.5 muM) subsequent applications of adenosine 5'-triphosphate (ATP) (2-600 muM) revealed a blockade of the ATP receptors. The antagonis...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1975.tb07397.x

    authors: Spedding M,Sweetman AJ,Weetman DF

    更新日期:1975-04-01 00:00:00

  • The effects of glucocorticoids on the distribution and mobilisation of arachidonic acid in fat cell ghosts.

    abstract::1 The prostaglandin synthesizing enzymes were found to be present in fat cell ghosts isolated from rabbit adipose tissue. 2 Prostaglandin E2 (PGE2) and PGF2, were synthesized by ghosts after stimulation with adrenocorticotrophic hormone (ACTH). 3 Indomethacin was found to inhibit this synthesis but not the synthesis o...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:

    authors: Lewis GP,Piper PJ,Vigo C

    更新日期:1979-11-01 00:00:00

  • The antianaphylactic action of histamine H2-receptor agonists in the guinea-pig isolated heart.

    abstract::The effects of histamine and of H1- and H2-receptor agonists on the response to specific antigen were studied in isolated hearts taken from actively sensitized guinea-pigs. Histamine and H2-receptor agonists (dimaprit, impromidine) dose-dependently decrease the positive chronotropic and inotropic effects, and the seve...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1987.tb11195.x

    authors: Blandina P,Brunelleschi S,Fantozzi R,Giannella E,Mannaioni PF,Masini E

    更新日期:1987-03-01 00:00:00

  • Uptake and release of 5-hydroxytryptamine by enteric 5-hydroxytryptaminergic neurones: effects of fluoxetine (Lilly 110140) and chlorimipramine.

    abstract::The effect of fluoxetine on uptake of 5-hydroxytryptamine (5-HT) by enteric 5-hydroxytryptaminergic neurones has been analyzed in order to compare further these neurones with 5-HT neurones of the CNS. In addition, the effects of fluoxetine and chlorimipramine on efflux of [3H]-5-HT from the myenteric plexus were also ...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1979.tb16089.x

    authors: Gershon MD,Jonakait GM

    更新日期:1979-05-01 00:00:00

  • The effects of dimethothiazine on muscle spindle activity in the decerebrate cat.

    abstract::1. The effects of dimethothiazine have been studied on the response of afferent fibres from primary and secondary endings of muscle spindles in the soleus muscle of the decerebrate cat during stretching of the muscle under controlled conditions.2. Dimethothiazine in doses of 1 to 4 mg/kg intravenously reduced the disc...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1970.tb10360.x

    authors: Maxwell DR,Rhodes KF

    更新日期:1970-07-01 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

  • Inhibition of the myocardial Ca(2+)-current (ICa) by the enantiomers of DPI 201-106 and BDF 8784.

    abstract::1. We studied the stereoselectivity of the effects of the enantiomers of the cardiotonic agent DPI 201-106 (4-[3'-(4"-benzhydryl-1"-piperazinyl)-2'-hydroxypropoxy]-1H-indole-2- carbonitrile, DPI) and its methyl-for-carbonitrile analogue BDF 8784 on cardiac calcium currents (ICa) of guinea-pig ventricular myocytes. The...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1991.tb12456.x

    authors: Ravens U,Pfeifer T,Wettwer E,Grundke M

    更新日期:1991-10-01 00:00:00

  • ICI D7114 a novel selective beta-adrenoceptor agonist selectively stimulates brown fat and increases whole-body oxygen consumption.

    abstract::1. ICI D7114 is a novel, beta-adrenoceptor agonist which stimulates whole body oxygen consumption in conscious rats, cats and dogs and brown adipose tissue (BAT) activity in conscious rats. Treatment of rats with ICI D7114 stimulated oxygen consumption (ED50, 0.04 mg kg-1, p.o.) and BAT mitochondrial guanosine diphosp...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1991.tb12391.x

    authors: Holloway BR,Howe R,Rao BS,Stribling D,Mayers RM,Briscoe MG,Jackson JM

    更新日期:1991-09-01 00:00:00

  • Sumatriptan-induced saphenous venoconstriction in the anaesthetized dog through 5-HT1-like receptor activation.

    abstract::1. The role of vasoconstrictor 5-HT1-like receptors in the control of vascular reactivity in vivo has been relatively little studied, particularly with regards to venous function. Using an anaesthetized dog model, we have investigated the haemodynamic profile of the selective 5-HT1-like agonist, sumatriptan, focussing...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1995.tb15055.x

    authors: Drieu la Rochelle C,O'Connor SE

    更新日期:1995-10-01 00:00:00

  • Biphasic responsiveness of rat pial arterioles to dopamine: direct observations on the microcirculation.

    abstract::The effects of local perivascular application of dopamine to rat pial arterioles. (20-40 micrometer i.d.) were examined in situ, at the microcirculatory level, by use of a high-resolution closed circuit television microscope recording system. Local application of very low, physiological doses (1 to 10 pg) of dopamine ...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1980.tb07900.x

    authors: Altura BM,Gebrewold A,Lassoff S

    更新日期:1980-08-01 00:00:00

  • Inhibition of the pulmonary inactivation of prostaglandins in vivo by di-4-phloretin phosphate.

    abstract::1 Inactivation of prostaglandin E2 in the pulmonary circulation of rabbits in vivo was measured by comparing the hypotensive effects of doses given intravenously and intra-arterially. 2 Di-4-phloretin phosphate (DPP) 25-100 mug kg-1 min-1 inhibited the inactivation of prostaglandin E2 in the pulmonary circulation. 3 T...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1975.tb07569.x

    authors: Crutchley DJ,Piper PJ

    更新日期:1975-07-01 00:00:00

  • Effect of sodium metabisulphite on bronchial blood flow in conscious sheep: pharmacological modulation.

    abstract::1. Sodium metabisulphite (MBS) can induce bronchoconstriction in patients with asthma. We investigated the effects of MBS aerosol on bronchial blood velocity (Vbr) and pulmonary resistance in intubated conscious sheep. 2. Bronchial blood velocity was measured by implanting a 20 MHz ultrasonic Doppler flow probe on the...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1994.tb14826.x

    authors: Nichol GM,Parsons GH,Chung KF

    更新日期:1994-03-01 00:00:00

  • Comparative behavioural profile of centrally administered tachykinin NK1, NK2 and NK3 receptor agonists in the guinea-pig.

    abstract::1. The NK1 tachykinin receptor agonists, septide, [Sar9,Met(O2)11]SP and [Pro9]SP produced locomotor hyperactivity (10-20 min) when injected intracerebroventricularly (i.c.v.) in the guinea-pig. The most potent in eliciting this hyperactivity was septide (from 0.63 to 5 micrograms), compared to [Sar9,Met(O2)11]SP, whi...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1995.tb15101.x

    authors: Piot O,Betschart J,Grall I,Ravard S,Garret C,Blanchard JC

    更新日期:1995-11-01 00:00:00

  • Contrasting effects of the imidazol(in)e alpha 2-adrenoceptor agonists, medetomidine, clonidine and UK 14,304 on extraneuronal levels of noradrenaline in the rat frontal cortex: evaluation using in vivo microdialysis and synaptosomal uptake studies.

    abstract::1. In vivo microdialysis in halothane-anaesthetized rats and synaptosomal [3H]-noradrenaline uptake studies in vitro were used to evaluate the effects of imidazole (medetomidine) and imidazoline (clonidine and UK 14,304) alpha 2-adrenoceptor agonists on extraneuronal levels of noradrenaline in the frontal cortex. 2. L...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1995.tb14962.x

    authors: Dalley JW,Stanford SC

    更新日期:1995-04-01 00:00:00

  • Modulating effect of the nootropic drug, piracetam on stress- and subsequent morphine-induced prolactin secretion in male rats.

    abstract::1. The effect of the nootropic drug, piracetam on stress- and subsequent morphine-induced prolactin (PRL) secretion was investigated in vivo in male rats, by use of a stress-free blood sampling and drug administration method by means of a permanent indwelling catheter in the right jugular vein. 2. Four doses of pirace...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1996.tb15218.x

    authors: Matton A,Engelborghs S,Bollengier F,Finné E,Vanhaeist L

    更新日期:1996-02-01 00:00:00

  • The pharmacology of sheep tracheobronchial muscle: a relaxant effect of histamine on the isolated bronchi.

    abstract::1. Histamine contracted the tracheal and major bronchial muscles of sheep and relaxed the muscles of the lesser bronchi and bronchioles.2. The stimulant action of histamine on the trachea was antagonized by mepyramine, whereas the relaxant effect on the bronchial tree was not.3. 5-Hydroxytryptamine contracted the musc...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1969.tb07997.x

    authors: Yre P

    更新日期:1969-07-01 00:00:00

  • P2Y(1) receptors mediate inhibitory neuromuscular transmission in the rat colon.

    abstract:BACKGROUND AND PURPOSE:Inhibitory junction potentials (IJP) are responsible for smooth muscle relaxation in the gastrointestinal tract. The aim of this study was to pharmacologically characterize the neurotransmitters [nitric oxide (NO) and adenosine triphosphate (ATP)] and receptors involved at the inhibitory neuromus...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.2009.00454.x

    authors: Grasa L,Gil V,Gallego D,Martín MT,Jiménez M

    更新日期:2009-11-01 00:00:00

  • Some effects of PCO2 and pH on nerve tissue.

    abstract::1. Rat phrenic nerve preparations were used in vitro to study action potential amplitude and nerve conduction time under varying conditions of Pco(2) and sodium bicarbonate concentration in the surrounding Krebs solution.2. A correlation was found between action potential amplitude and pH but not between action potent...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1969.tb07980.x

    authors: Ellis FR

    更新日期:1969-01-01 00:00:00

  • Pharmacological activity of ACC-7513, a selective alpha-adrenoceptor and 5-hydroxytryptamine receptor blocking agent.

    abstract::The pharmacological activity of N-[2-(2,6-dimethoxyphenoxy) ethyl]-2-(2-methoxyphenoxy) ethanaminium chloride (ACC-7513) was determined in isolated smooth and cardiac muscle and its effect on blood pressure and heart rate assessed in the spontaneously hypertensive rat (SHR). ACC-7513 was found to be a potent alpha-adr...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1985.tb17373.x

    authors: Anderson WG,Kam ST

    更新日期:1985-04-01 00:00:00