Abstract：
:1. The uptake of (3)H-digitoxin, (3)H-ouabain and (3)H-dihydro-ouabain by isolated guinea-pig atria has been studied and compared with the inhibition of the sodium pump and with the inotropic effect.2. Analysis of the curve relating the uptake of digitoxin and ouabain at equilibrium to the bath concentration enabled a non-saturable and a saturable binding site to be distinguished.3. The uptake of inactive doses of dihydro-ouabain was only by a non-saturable mechanism.4. The uptake of labelled digitoxin and ouabain was reduced in the presence of another glycoside. The amount of bound glycoside was nearly equivalent to the estimated non-saturable uptake.5. The uptake was reduced at 4 degrees C to the clearance of the non-saturable site.6. ED50 of digitoxin and of ouabain for inhibition of the sodium pump were measured and compared to the ED50 for inotropic effect and to the concentrations producing a half-saturation of the saturable binding site.7. It is concluded that binding to the saturable site may be responsible for the cardiac actions of the glycosides.
journal_name
Br J Pharmacoljournal_title
British journal of pharmacologyauthors
Godfraind T,Lesne Mdoi
10.1111/j.1476-5381.1972.tb08146.xsubject
Has Abstractpub_date
1972-11-01 00:00:00pages
488-97issue
3eissn
0007-1188issn
1476-5381journal_volume
46pub_type
杂志文章abstract：:The effect of the selective serotonin reuptake inhibitor fluoxetine was examined on the 5-HT4 receptor-mediated relaxation in the rat isolated ileum. Fluoxetine unsurmountably antagonized the relaxation to exogenous 5-HT with abolition of the response at 10 microM. Fluoxetine (10 microM) also caused a gradual loss of ...
journal_title：British journal of pharmacology
pub_type： 杂志文章
doi：10.1038/sj.bjp.0704694
更新日期：2002-05-01 00:00:00
abstract：BACKGROUND AND PURPOSE:Obesity is a risk factor for several inflammation-based diseases including arthritis. We investigated the anti-nociceptive and anti-inflammatory effects of the cannabinoid CB1 receptor antagonist rimonabant in lean and diet-induced obese female rats with arthritis induced by complete Freund's adj...
journal_title：British journal of pharmacology
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doi：10.1038/sj.bjp.0707138
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abstract：BACKGROUND AND PURPOSE:Hypoxia/reoxygenation induces synthesis of reactive oxygen species (ROS) which can attack macromolecules and cause brain injury. The transcription factor, nuclear factor (erythroid-derived 2)-like 2, (Nrf2), ia potent activator of genes with an antioxidant responsive element and Nrf2 can countera...
journal_title：British journal of pharmacology
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doi：10.1111/bph.13031
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abstract：:1. Cannabinoids are potent inhibitors of endothelium-derived hyperpolarizing factor (EDHF)-mediated relaxations. We set out to study the mechanism underlying this effect and the possible role of cannabinoid-induced changes in intercellular gap junction communication. 2. In cultured endothelial cells, Delta(9)-tetrahyd...
journal_title：British journal of pharmacology
pub_type： 杂志文章
doi：10.1038/sj.bjp.0704776
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abstract：:The physiological regulation of the immune system encompasses comprehensive anti-inflammatory mechanisms that can be harnessed for the treatment of infectious and inflammatory disorders. Recent studies indicate that the vagal nerve, involved in control of heart rate, hormone secretion and gastrointestinal motility, is...
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doi：10.1038/sj.bjp.0707264
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journal_title：British journal of pharmacology
pub_type： 杂志文章
doi：10.1111/j.1476-5381.1985.tb11078.x
更新日期：1985-08-01 00:00:00
abstract：BACKGROUND AND PURPOSE:We have developed a strategy to target the permanently charged lidocaine derivative lidocaine N-ethyl bromide (QX-314) selectively into nociceptive sensory neurons through the large-pore transient receptor potential cation channel subfamily V (TRPV1) noxious heat detector channel. This involves c...
journal_title：British journal of pharmacology
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doi：10.1111/j.1476-5381.2011.01391.x
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abstract：BACKGROUND AND PURPOSE:Memantine and marijuana smoking have been found to inhibit tremor in parkinsonian patients, although the observed effects were relatively weak. The tremorolytic effects of combinations of memantine and cannabinoids have not been studied. Here, we have evaluated the anti-tremor activity of memanti...
journal_title：British journal of pharmacology
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doi：10.1111/bph.14914
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journal_title：British journal of pharmacology
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doi：10.1111/j.1476-5381.1996.tb15580.x
更新日期：1996-08-01 00:00:00
abstract：:Cannabinoid (CB1) receptor activation acts neuronally, reducing GI motility, diarrhoea, pain, transient lower oesophageal sphincter relaxations (TLESRs) and emesis, and promoting eating. CB2 receptor activation acts mostly via immune cells to reduce inflammation. What are the key questions which now need answering to ...
journal_title：British journal of pharmacology
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doi：10.1038/sj.bjp.0707422
更新日期：2007-11-01 00:00:00
abstract：BACKGROUND AND PURPOSE:Inflammasomes are multimeric complexes that facilitate caspase-1-mediated processing of the pro-inflammatory cytokines IL-1β and IL-18. Clinical hypertension is associated with renal inflammation and elevated circulating levels of IL-1β and IL-18. Therefore, we investigated whether hypertension i...
journal_title：British journal of pharmacology
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doi：10.1111/bph.13230
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journal_title：British journal of pharmacology
pub_type： 杂志文章
doi：10.1111/j.1476-5381.1988.tb11415.x
更新日期：1988-01-01 00:00:00
abstract：:Mitochondrial permeability transition pore (mPTP) opening plays a critical role in cardiac reperfusion injury and its prevention is cardioprotective. Tumour cell mitochondria usually have high levels of hexokinase isoform 2 (HK2) bound to their outer mitochondrial membranes (OMM) and HK2 binding to heart mitochondria ...
journal_title：British journal of pharmacology
pub_type： 杂志文章,评审
doi：10.1111/bph.12899
更新日期：2015-04-01 00:00:00
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doi：10.1038/sj.bjp.0706699
更新日期：2006-05-01 00:00:00
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journal_title：British journal of pharmacology
pub_type： 杂志文章
doi：10.1111/j.1476-5381.1975.tb07323.x
更新日期：1975-01-01 00:00:00
abstract：:1. A series of 5-hydroxytryptamine (5-HT) receptor agonists including 5-HT, 5-carboxamidotryptamine (5-CT) and sumatriptan produced little or no contraction of rabbit isolated mesenteric arteries under resting tone conditions, even at concentrations up to 10(-4) M. 2. When the same agonists were retested in mesenteric...
journal_title：British journal of pharmacology
pub_type： 杂志文章
doi：10.1111/j.1476-5381.1995.tb13228.x
更新日期：1995-01-01 00:00:00
abstract：:1. The aim of the present study was to examine whether ramipril induces delayed myocardial protection against free radical injuries ex vivo and to determine the possible role of the bradykinin B2-nitric oxide (NO) pathway, prostaglandins(PGs) and protein synthesis in this delayed adaptive response. 2. Rats were pretre...
journal_title：British journal of pharmacology
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doi：10.1038/sj.bjp.0702089
更新日期：1998-10-01 00:00:00
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journal_title：British journal of pharmacology
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doi：10.1111/j.1476-5381.1970.tb09560.x
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pub_type： 杂志文章,评审
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更新日期：2020-08-06 00:00:00
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doi：10.1038/sj.bjp.0707175
更新日期：2007-04-01 00:00:00
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journal_title：British journal of pharmacology
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doi：10.1111/j.1476-5381.2010.01081.x
更新日期：2011-03-01 00:00:00
abstract：:1. This study analyses the receptors mediating the effects of bradykinin (BK) and analogues on neurogenic twitch contractions of the mouse isolated vas deferens evoked, in the presence of captopril (3 microM), by electrical field stimulation with trains of 4 rectangular 0.5 ms pulses of supramaximal strength, delivere...
journal_title：British journal of pharmacology
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doi：10.1111/j.1476-5381.1995.tb13372.x
更新日期：1995-04-01 00:00:00
abstract：BACKGROUND AND PURPOSE:Retinoids, through their activation of retinoic acid receptors (RARs) and retinoid X receptors, regulate diverse cellular processes, and pharmacological intervention in their actions has been successful in the treatment of skin disorders and cancers. Despite the many beneficial effects, administr...
journal_title：British journal of pharmacology
pub_type： 杂志文章
doi：10.1111/bph.12543
更新日期：2014-03-01 00:00:00
abstract：:1. Studies in rats suggest that PACAP modulates gastric acid secretion through the release of both histamine and somatostatin. 2. We characterized the effects of exogenous PACAP on gastric acid secretion in urethane-anesthetized mice implanted with a gastric cannula and in conscious 2-h pylorus ligated mice, and deter...
journal_title：British journal of pharmacology
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doi：10.1038/sj.bjp.0705739
更新日期：2004-05-01 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.tb10328.x
更新日期：1988-03-01 00:00:00
abstract：:Chronic itch poses major health care and economic burdens worldwide. In 2013, B-type natriuretic peptide (BNP) was identified as an itch-selective neuropeptide and shown to be both necessary and sufficient to produce itch behaviour in mice. Since then, mechanistic studies of itch have increased, not only at central le...
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pub_type： 杂志文章,评审
doi：10.1111/bph.14952
更新日期：2020-03-01 00:00:00
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journal_title：British journal of pharmacology
pub_type： 杂志文章
doi：10.1111/j.1476-5381.1992.tb14508.x
更新日期：1992-11-01 00:00:00
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journal_title：British journal of pharmacology
pub_type： 杂志文章
doi：10.1111/j.1476-5381.2009.00599.x
更新日期：2010-03-01 00:00:00
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journal_title：British journal of pharmacology
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doi：10.1038/sj.bjp.0703590
更新日期：2000-10-01 00:00:00
