The partial purification and bioassay of a toxin present in extracts of the sea anemone, Tealia felina (L.).

Abstract:

:1. Column chromatography with Agarose A50m followed by Sephadex G100 was used to separate a fraction (extract II) in the molecular weight range 12,000 to 14,000 daltons from saline extracts of the sea anemone, Tealia felina. 2. Extract II inhibited histamine-induced contractions of the guinea-pig ileum and produced haemolysis of human blood, effects on which bioassays were based. 3. The potency of extracts was assayed. A standard unit of activity (= AU) was defined such that 100 AU produced 90% inhibition of histamine-induced contractions of the guinea-pig ileum after 30 to 35 min exposure. 4. The relationship between activity of the extracts measured on the ileum and their haemolytic activity was studied, providing a second assay method based on the latter property. 5 Based on values from both methods of assay, the calculated yield in AU at the end of the separation procedure was 0.53 AU for each AU present in the original extract. In crude extract there were 5.0 AU/mg dry weight and 36.7 AU/mg protein, and after separation (extract II) there were 11.2 AU/mg dry weight and 312.2 AU/mg protein. 6 The acute LD50 values determined in mice (i.v.) were: for crude extract 124 mg/kg for extract I, 76 mg/kg and for extract II, 69 mg/kg. 7 Extract II (0.18 to 0.72 AU/ml) produced a slowly developing contraction of guinea-pig ileum. Indomethacin (2.8 x 10(-5) M) substantially reduced this response. 8 Extract II (0.03 AU/ml) reduced the contractile response of the guinea-pig ileum to acetylcholine by 39 +/- 8%, n = 6, and the response to histamine by 26 +/- 6.6%, n = 6. The response to 5-hydroxytryptamine (5-HT) was not reduced by 0.08 AU/ml of extract II, a concentration that actually increased the contractile response to KC1 by 32 +/- 11.2% n = 7. 9 It is proposed that for future work on the extract a new AU should be used. This AU is defined such that 50 AU produce 50% inhibition of histamine-induced contractions of the guinea-pig ileum after 30 to 35 min exposure.

journal_name

Br J Pharmacol

authors

Aldeen SI,Elliott RC,Sheardown M

doi

10.1111/j.1476-5381.1981.tb09115.x

subject

Has Abstract

pub_date

1981-02-01 00:00:00

pages

211-20

issue

2

eissn

0007-1188

issn

1476-5381

journal_volume

72

pub_type

杂志文章
  • Influence of histamine H1- and H2-receptor blockers on sympathetic vasodilator and vasoconstrictor responses in canine paw.

    abstract::1 Vasodilator responses to histamine, bradykinin and sympathetic nerve stimulation were elicited in the perfused paw of dogs treated with bretylium (15-20 mg/kg) and atropine. The H2-receptor blocking agent, burimamide, when administered in the dose of 5 mg/kg intravenously and 4 mg intra-arterially did not depress si...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1975.tb07329.x

    authors: Kraft E,Zimmerman BG

    更新日期:1975-01-01 00:00:00

  • Selective antagonism by benzodiazepines of neuronal responses to excitatory amino acids in the cerebral cortex.

    abstract::1 The recently discovered benzodiazepine receptor exists in high concentration in the cerebral cortex. We have, therefore, examined the effects of diazepam and chlordiazepoxide on cortical neurone responses to excitatory and inhibitory amino acids and acetylcholine, in the cortex of rats anaesthetized with urethane.2 ...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1979.tb08702.x

    authors: Assumpção JA,Bernardi N,Brown J,Stone TW

    更新日期:1979-12-01 00:00:00

  • Participation of protein kinases in staurosporine-induced interleukin-6 production by rat peritoneal macrophages.

    abstract::The incubation of rat peritoneal macrophages in the presence of staurosporine, a non-specific protein kinase inhibitor, induced interleukin-6 (IL-6) production in a time- and concentration-dependent manner at 6.3-63 nM, but at 210 nM, the stimulant effect on IL-6 production was reduced. The levels of IL-6 mRNA as dete...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0702659

    authors: Yamaki K,Ohuchi K

    更新日期:1999-07-01 00:00:00

  • Inhibitors of spasmogen-induced Ca2+ channel suppression in smooth muscle cells from small intestine.

    abstract::1. Whole-cell patch-clamp recordings were made from smooth muscle cells isolated from the longitudinal muscle layer of guinea-pig ileum. Carbachol (acting at muscarinic receptors) or histamine (acting at H1 histamine receptors) suppressed Ca2+ channel current. The effect of either agonist had an initial transient comp...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0702112

    authors: Unno T,Beech DJ,Komori S,Ohashi H

    更新日期:1998-10-01 00:00:00

  • Hypoxia modulates the activity of a series of clinically approved tyrosine kinase inhibitors.

    abstract:BACKGROUND AND PURPOSE:Hypoxia in tumours is known to cause resistance to conventional chemotherapeutic drugs. In contrast, little is known about the effects of hypoxia on targeted anti-cancer drugs. This study evaluated the effect of hypoxia on a series of clinically approved tyrosine kinase inhibitors (TKIs). EXPERI...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/bph.12438

    authors: Ahmadi M,Ahmadihosseini Z,Allison SJ,Begum S,Rockley K,Sadiq M,Chintamaneni S,Lokwani R,Hughes N,Phillips RM

    更新日期:2014-01-01 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

  • Effect of endothelin-1 (1-31) on extracellular signal-regulated kinase and proliferation of human coronary artery smooth muscle cells.

    abstract::1. We have previously found that human chymase cleaves big endothelins (ETs) at the Tyr31-Gly32 bond and produces 31-amino acid ETs (1-31), without any further degradation products. In this study, we investigated the effect of synthetic ET-1 (1-31) on the proliferation of cultured human coronary artery smooth muscle c...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0702141

    authors: Yoshizumi M,Kim S,Kagami S,Hamaguchi A,Tsuchiya K,Houchi H,Iwao H,Kido H,Tamaki T

    更新日期:1998-11-01 00:00:00

  • Post-translational palmitoylation of ionotropic glutamate receptors in excitatory synaptic functions.

    abstract::In the mammalian CNS, glutamate is the major excitatory neurotransmitter. Ionotropic glutamate receptors (iGluRs) are responsible for the glutamate-mediated postsynaptic excitation of neurons. Regulation of glutamatergic synapses is critical for higher brain functions including neural communication, memory formation, ...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1111/bph.15050

    authors: Hayashi T

    更新日期:2020-03-11 00:00:00

  • Impairment of endothelium-dependent relaxation and changes in levels of cyclic GMP in aorta from streptozotocin-induced diabetic rats.

    abstract::1. Acetylcholine (ACh)-induced relaxation of aortic strips with endothelium and production of cyclic GMP between streptozotocin-induced diabetic and age-matched control rats were compared. 2. The concentration-response curve for ACh-induced relaxation was shifted to the right in diabetic rats. IC50 values for ACh were...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1989.tb11993.x

    authors: Kamata K,Miyata N,Kasuya Y

    更新日期:1989-06-01 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

  • Effects of the neuroprotectant lubeluzole on the cytotoxic actions of veratridine, barium, ouabain and 6-hydroxydopamine in chromaffin cells.

    abstract::1. Incubation of bovine adrenal chromaffin cells with veratridine (10-100 microM) during 24 h, caused a concentration-dependent release of the cytosolic lactate dehydrogenase (LDH) into the bathing medium, an indicator of cell death. Lubeluzole or its R(-) enantiomer, R91154, did not enhance LDH release. Both lubeluzo...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0701955

    authors: Cano-Abad MF,López MG,Hernández-Guijo JM,Zapater P,Gandía L,Sánchez-García P,García AG

    更新日期:1998-07-01 00:00:00

  • The effect of capsaicin on voltage-gated calcium currents and calcium signals in cultured dorsal root ganglion cells.

    abstract::1. The effects of capsaicin on voltage-gated Ca2+ currents (ICa), and intracellular Ca2+ concentrations [( Ca2+]i) in cultured dorsal root ganglion (DRG) neurones of the rat were examined in vitro by use of combined patch clamp-microfluorometric recordings. 2. Under voltage-clamp conditions, capsaicin (0.1-10 microM) ...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1990.tb12725.x

    authors: Bleakman D,Brorson JR,Miller RJ

    更新日期:1990-10-01 00:00:00

  • Exercise training as prophylactic strategy in the management of neutropenia during chemotherapy.

    abstract::Chemotherapy-induced immune-suppression is a common, but potential detrimental, adverse reaction in patients undergoing treatment for cancer and strategies with capacity to boost the immune cell populations are needed. Physical exercise training is a potent regulator of immune cell viability and function and may serve...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1111/bph.15141

    authors: Schauer T,Hojman P,Gehl J,Christensen JF

    更新日期:2020-05-25 00:00:00

  • 5-HT3 receptors promote colonic inflammation via activation of substance P/neurokinin-1 receptors in dextran sulphate sodium-induced murine colitis.

    abstract:BACKGROUND AND PURPOSE:5-HT (serotonin) regulates various physiological functions, both directly and via enteric neurons. The present study investigated the role of endogenous 5-HT and 5-HT3 receptors in the pathogenic mechanisms involved in colonic inflammation, especially in relation to substance P (SP) and the neuro...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/bph.13482

    authors: Utsumi D,Matsumoto K,Amagase K,Horie S,Kato S

    更新日期:2016-06-01 00:00:00

  • The effect of parachlorophenylalanine on social interaction of male rats.

    abstract::1. Juvenile male rats treated with parachlorophenylalanine showed hair loss round the head and neck extending down the chest and abdomen.2. Treated isolated rats did not have this loss of hair, while untreated animals living in the same cage as treated rats lost their hair. The loss therefore seems to be caused by inc...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1970.tb08518.x

    authors: Shillito EE

    更新日期:1970-02-01 00:00:00

  • Characterization of adenosine receptors in guinea-pig isolated left atria.

    abstract::1. The effects of purinergic stimulation on action potential, force of contraction, 86Rb efflux and 45Ca uptake were investigated in guinea-pig left atria. 2. Adenosine exerted a negative inotropic effect which was antagonized by adenosine deaminase but enhanced by dipyridamole. 3. The negative inotropic effect of ade...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1989.tb12577.x

    authors: Jahnel U,Nawrath H

    更新日期:1989-08-01 00:00:00

  • Novel roles for β-arrestins in the regulation of pharmacological sequestration to predict agonist-induced desensitization of dopamine D3 receptors.

    abstract:BACKGROUND AND PURPOSE:In addition to typical GPCR kinase (GRK)-/β-arrestin-dependent internalization, dopamine D3 receptor employed an additional GRK-independent sequestration pathway. In this study, we investigated the molecular mechanism of this novel sequestration pathway. EXPERIMENTAL APPROACH:Radioligand binding...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/bph.12357

    authors: Min C,Zheng M,Zhang X,Caron MG,Kim KM

    更新日期:2013-11-01 00:00:00

  • Nitric oxide-mediated modulation of the endothelin-1 signalling pathway in the human cardiovascular system.

    abstract::1. We studied the ability of nitric oxide (NO) to physiologically antagonize endothelin-1 (ET-1) induced constrictions in human internal mammary artery (IMA). We also investigated the hypothesis that NO interacts directly with ET-receptor binding in human heart and aorta. 2. ET-1 potently contracted IMA (EC(50) 6.86 n...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0703834

    authors: Wiley KE,Davenport AP

    更新日期:2001-01-01 00:00:00

  • Preclinical evaluation of [18 F]MA3: a CB2 receptor agonist radiotracer for PET.

    abstract:BACKGROUND AND PURPOSE:Non-invasive in vivo imaging of cannabinoid CB2 receptors using PET is pursued to study neuroinflammation. The purpose of this study is to evaluate the in vivo binding specificity of [18 F]MA3, a CB2 receptor agonist, in a rat model with local overexpression of human (h) CB2 receptors. METHODS:[...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/bph.14564

    authors: Attili B,Celen S,Ahamed M,Koole M,Haute CVD,Vanduffel W,Bormans G

    更新日期:2019-05-01 00:00:00

  • The effect of peptidase inhibitors on bradykinin-induced bronchoconstriction in guinea-pigs in vivo.

    abstract::1. Bradykinin (BK) instilled directly into the airway lumen caused bronchoconstriction in anaesthetized, mechanically ventilated guinea-pigs in the presence of propranolol (1 mg kg-1 i.v.). The geometric mean dose of BK required to produce 100% increase in airway opening pressure (PD100) was 22.9 nmol (95% c.i. 11.7-4...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1990.tb12092.x

    authors: Ichinose M,Barnes PJ

    更新日期:1990-09-01 00:00:00

  • Noradrenaline content of the heart of the adrenal-demedullated rat.

    abstract::1. The noradrenaline (NA) concentration in the "heart" (atria and right ventricle) of male rats was estimated at different periods following adrenal demedullation. For 1-3 weeks after the operation there was, in all rats, a reduction in NA content of the tissue, whereas, after somewhat longer intervals, the concentrat...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1970.tb10335.x

    authors: Borchard F,Vogt M

    更新日期:1970-01-01 00:00:00

  • Acetylcholine and tachykinins involvement in the caffeine-induced biphasic change in intracellular Ca2+ in bovine airway smooth muscle.

    abstract::1. Caffeine has been widely used as a pharmacological tool to evaluate Ca(2+) release from the sarcoplasmic reticulum in isolated smooth muscle cells. However, in nervous tissue this drug also causes neurotransmitters release, which might cause additional effects when smooth muscle strips are evaluated. To assess this...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0705348

    authors: Montaño LM,Carbajal V,Arreola JL,Barajas-López C,Flores-Soto E,Vargas MH

    更新日期:2003-07-01 00:00:00

  • Modification by steroids of pulmonary oedema and prostaglandin E2 pharmacokinetics induced by endotoxin in rats.

    abstract::1. A single i.p. injection of bacterial endotoxin in rats (3.5 mg kg-1) caused lung injury assessed as changes in lung dry:wet weight ratio and leukopaenia over the subsequent 28 h. 2. This treatment also slowed the efflux of 14C from [14C]-prostaglandin E2 (PGE2), i.e., increased t1/2 and increased the survival of PG...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1988.tb11485.x

    authors: Izumi T,Bakhle YS

    更新日期:1988-04-01 00:00:00

  • Effects of 5-HT-receptor and alpha 2-adrenoceptor ligands on the haemodynamic response to acute central hypovolaemia in conscious rabbits.

    abstract::1. We set out to elucidate the pharmacological mechanisms by which alpha 2-adrenoceptor and 5-HT-receptor ligands affect the haemodynamic response to acute central hypovolaemia in conscious rabbits. 2. Acute central hypovolaemia was produced by inflating an inferior vena caval cuff so that cardiac output fell at a con...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1993.tb13528.x

    authors: Evans RG,Haynes JM,Ludbrook J

    更新日期:1993-05-01 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

  • Potentiation by nitric oxide of the ATP-sensitive K+ current induced by K+ channel openers in guinea-pig ventricular cells.

    abstract::1. Modulation by nitric oxide (NO) of the ATP-sensitive K+ channel (KATP) current (IK(ATP)) was investigated in single ventricular cells dissociated from guinea-pig hearts. IK(ATP) was induced by 5-amino-N-[2-(2-chlorophenyl)ethyl]-N'-cyano-3-pyridinecarboxamidine+ ++ (KRN4884) and cromakalim. 2. In the whole-cell pat...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0701069

    authors: Shinbo A,Iijima T

    更新日期:1997-04-01 00:00:00

  • Interleukin-8 production by the human colon epithelial cell line HT-29: modulation by interleukin-13.

    abstract::1. We have determined which cytokines induce and modulate the production of the chemokine interleukin-8 (IL-8) by the human colonic epithelial cell line HT-29. 2. Growth arrested cell cultures were stimulated with the human recombinant cytokines interleukin-1 alpha (IL-1 alpha), tumour necrosis factor-alpha (TNF-alpha...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1996.tb15993.x

    authors: Kolios G,Robertson DA,Jordan NJ,Minty A,Caput D,Ferrara P,Westwick J

    更新日期:1996-09-01 00:00:00

  • Role of the endocannabinoid system in diabetes and diabetic complications.

    abstract:UNLABELLED:Increasing evidence suggests that an overactive endocannabinoid system (ECS) may contribute to the development of diabetes by promoting energy intake and storage, impairing both glucose and lipid metabolism, by exerting pro-apoptotic effects in pancreatic beta cells and by facilitating inflammation in pancre...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1111/bph.13226

    authors: Gruden G,Barutta F,Kunos G,Pacher P

    更新日期:2016-04-01 00:00:00

  • Alterations of the benzodiazepine site of rat alpha 6 beta 2 gamma 2-GABAA receptor by replacement of several divergent amino-terminal regions with the alpha 1 counterparts.

    abstract::1. The benzodiazepine site of the alpha 6 beta 2 gamma 2 subtype of gamma-aminobutyric acidA (GABAA) receptors is distinguishable from that of the alpha 1 beta 2 gamma 2 subtype by its inability to interact with classical benzodiazepines (i.e., diazepam) and its agonistic response to Ro 15-1788, which behaves as an an...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0700931

    authors: Im WB,Pregenzer JF,Binder JA,Alberts GL,Im HK

    更新日期:1997-02-01 00:00:00

  • Pharmacology of LR-B/081, a new highly potent, selective and orally active, nonpeptide angiotensin II AT1 receptor antagonist.

    abstract::1. The pharmacological profile of LR-B/081, (methyl 2-[[4-butyl-2-methyl- 6-oxo-5-[[2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-1(6H)- pyrimidinyl]methyl]-3-thiophenecarboxylate), a novel antagonist at the angiotensin II (AII) AT1-receptor, was studied in vitro and in vivo. 2. In rabbit aortic strips incubated w...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1995.tb13323.x

    authors: Cirillo R,Renzetti AR,Cucchi P,Guelfi M,Salimbeni A,Caliari S,Castellucci A,Evangelista S,Subissi A,Giachetti A

    更新日期:1995-03-01 00:00:00