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 Pharmacoljournal_title
British journal of pharmacologyauthors
Aldeen SI,Elliott RC,Sheardown Mdoi
10.1111/j.1476-5381.1981.tb09115.xsubject
Has Abstractpub_date
1981-02-01 00:00:00pages
211-20issue
2eissn
0007-1188issn
1476-5381journal_volume
72pub_type
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journal_title:British journal of pharmacology
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doi:10.1111/j.1476-5381.1975.tb07329.x
更新日期:1975-01-01 00:00:00
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
更新日期:1979-12-01 00:00:00
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...
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更新日期:1999-07-01 00:00:00
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journal_title:British journal of pharmacology
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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
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doi:10.1111/bph.12438
更新日期:2014-01-01 00:00:00
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journal_title:British journal of pharmacology
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doi:10.1111/j.1476-5381.1988.tb11556.x
更新日期:1988-06-01 00:00:00
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...
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更新日期:1998-11-01 00:00:00
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
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journal_title:British journal of pharmacology
pub_type: 杂志文章
doi:10.1111/j.1476-5381.1989.tb11993.x
更新日期:1989-06-01 00:00:00
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journal_title:British journal of pharmacology
pub_type: 杂志文章
doi:10.1111/j.1476-5381.1991.tb09803.x
更新日期:1991-06-01 00:00:00
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
更新日期:1998-07-01 00:00:00
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journal_title:British journal of pharmacology
pub_type: 杂志文章
doi:10.1111/j.1476-5381.1990.tb12725.x
更新日期:1990-10-01 00:00:00
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...
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更新日期:2020-05-25 00:00:00
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更新日期:2016-06-01 00:00:00
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journal_title:British journal of pharmacology
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doi:10.1111/j.1476-5381.1970.tb08518.x
更新日期:1970-02-01 00:00:00
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journal_title:British journal of pharmacology
pub_type: 杂志文章
doi:10.1111/j.1476-5381.1989.tb12577.x
更新日期:1989-08-01 00:00:00
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...
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doi:10.1111/bph.12357
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journal_title:British journal of pharmacology
pub_type: 杂志文章
doi:10.1111/j.1476-5381.1970.tb10335.x
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journal_title:British journal of pharmacology
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doi:10.1038/sj.bjp.0705348
更新日期:2003-07-01 00:00:00
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journal_title:British journal of pharmacology
pub_type: 杂志文章
doi:10.1111/j.1476-5381.1988.tb11485.x
更新日期:1988-04-01 00:00:00
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...
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doi:10.1111/j.1476-5381.1993.tb13528.x
更新日期:1993-05-01 00:00:00
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
更新日期:2011-07-01 00:00:00
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
更新日期:1997-04-01 00:00:00
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
更新日期:1996-09-01 00:00:00
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
更新日期:2016-04-01 00:00:00
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
更新日期:1997-02-01 00:00:00
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
更新日期:1995-03-01 00:00:00