Abstract：
:1. The uptake and release of (3)H-digitoxigenin by electrically driven, guinea-pig isolated atria (frequency 180/min) has been determined for two different medium concentrations of the genin. Both concentrations-1 x 10(-7) and 5 x 10(-7) g/ml.-caused a pronounced increase in contractile force.2. The uptake of (3)H-digitoxigenin reached equilibrium after approximately 2 hr of incubation. At equilibrium, the tissue/medium radioactivity ratio reached a value of about 8 for both concentrations studied. After initial saturation of the atria with (3)H-digitoxigenin, approximately 60% of the accumulated genin was released on wash-out in genin-free Tyrode solution for 2 hr.3. After presaturation of the atria with equimolar concentrations of either digitoxigenin or digitoxin (both non-radioactive) the uptake of (3)H-digitoxigenin occurred more slowly. After 2 hr of incubation approximately 60-70% of the tissue bound digitoxigenin or digitoxin had exchanged against (3)H-digitoxigenin from the medium. Presaturation of the atria with ouabain in equimolar concentration did not significantly affect the uptake of (3)H-digitoxigenin.4. The release process of (3)H-digitoxigenin was not affected by the same concentration of non-radioactive digitoxigenin as used for the accumulation of the genin.5. The kinetic properties of (3)H-digitoxigenin, determined by means of isotope techniques, are very similar to those of (3)H-digitoxin. The discrepancy between kinetic and pharmacological behaviour is, however, much larger for digitoxigenin than for digitoxin. Obviously, the presence or absence of the sugar moieties considerably influences the behaviour of the molecule towards the specific receptors, without particularly affecting the binding to unspecific, cellular structures.
journal_name
Br J Pharmacoljournal_title
British journal of pharmacologyauthors
Kuschinsky K,Lüllmann H,van Zwieten PAdoi
10.1111/j.1476-5381.1968.tb08490.xsubject
Has Abstractpub_date
1968-11-01 00:00:00pages
613-22issue
3eissn
0007-1188issn
1476-5381journal_volume
34pub_type
杂志文章abstract：:1. The affinity of the alpha 1-adrenoceptor antagonist SB 216469 (also known as REC 15/2739) has been determined at native and cloned alpha 1-adrenoceptor subtypes by radioligand binding and at functional alpha 1-adrenoceptor subtypes in isolated tissues. 2. In radioligand binding studies with [3H]-prazosin, SB 216469...
journal_title：British journal of pharmacology
pub_type： 杂志文章
doi：10.1111/j.1476-5381.1996.tb16009.x
更新日期：1996-11-01 00:00:00
abstract：BACKGROUND AND PURPOSE:Catechol-O-methyltransferase (COMT) metabolizes compounds containing catechol structures and has two forms: soluble (S-COMT) and membrane-bound (MB-COMT). Here we report the generation of a mouse line that expresses MB-COMT but not S-COMT. We compared the effects of deleting S-COMT only or both C...
journal_title：British journal of pharmacology
pub_type： 杂志文章
doi：10.1111/j.1476-5381.2009.00494.x
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journal_title：British journal of pharmacology
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doi：10.1111/j.1476-5381.2011.01432.x
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abstract：:1. The pharmacological characteristics of alpha 1-adrenoceptor binding sites in rat pineal gland membranes, detected by use of a selective alpha 1-adrenoceptor antagonist ([125I]-iodo-2-[beta-(4-hydroxyphenyl) ethylaminomethyl]tetralone, [125I]-HEAT), were investigated with the alkylating agent, chloroethylclonidine (...
journal_title：British journal of pharmacology
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doi：10.1111/j.1476-5381.1996.tb15530.x
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abstract：:1. Acute moderate hypoxia modifies the catalytic activity and expression of certain isoenzymes of hepatic cytochrome P450 (P450). The aim of this study was to document whether hypoxia affects hepatic P450 directly or through the release of serum mediators. 2. Rabbits were subjected to a FiO(2) of 8% for 48 h, sacrific...
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abstract：:1. Human mast cell tryptase appears to display considerable variation in activating proteinase-activated receptor 2 (PAR(2)). We found tryptase to be an inefficient activator of wild-type rat-PAR(2) (wt-rPAR(2)) and therefore decided to explore the factors that may influence tryptase activation of PAR(2). 2. Using a 2...
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journal_title：British journal of pharmacology
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doi：10.1111/j.1476-5381.1970.tb10360.x
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更新日期：2001-07-01 00:00:00
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journal_title：British journal of pharmacology
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doi：10.1111/j.1476-5381.1988.tb11470.x
更新日期：1988-04-01 00:00:00
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pub_type： 杂志文章
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更新日期：2011-09-01 00:00:00
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更新日期：2009-06-01 00:00:00
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journal_title：British journal of pharmacology
pub_type： 杂志文章
doi：10.1111/j.1476-5381.1993.tb12797.x
更新日期：1993-02-01 00:00:00
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journal_title：British journal of pharmacology
pub_type： 杂志文章
doi：10.1111/j.1476-5381.1992.tb12771.x
更新日期：1992-10-01 00:00:00
abstract：:1. Desensitization of the myocardial beta-adrenergic signal transduction pathway is an important mechanism which is involved in the progression of hypertensive heart disease. The aim of the present study was to evaluate the differential effects of chronic pharmacotherapy with an angiotensin converting enzyme (ACE)-inh...
journal_title：British journal of pharmacology
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journal_title：British journal of pharmacology
pub_type： 杂志文章
doi：10.1111/j.1476-5381.1995.tb13240.x
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journal_title：British journal of pharmacology
pub_type： 杂志文章
doi：10.1038/sj.bjp.0700890
更新日期：1997-01-01 00:00:00
abstract：:The releases of [3H]5-hydroxytryptamine ([3H]5-HT) and of endogenous glutamic acid and their modulation through presynaptic h5-HT1B autoreceptors and h5-HT1D heteroreceptors have been investigated in synaptosomal preparations from fresh neocortical samples obtained from patients undergoing neurosurgery. The inhibition...
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pub_type： 杂志文章
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更新日期：1999-02-01 00:00:00
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journal_title：British journal of pharmacology
pub_type： 杂志文章
doi：10.1038/sj.bjp.0707284
更新日期：2007-07-01 00:00:00
abstract：BACKGROUND AND PURPOSE:Dehydrodiconiferyl alcohol (DHCA), a lignan compound isolated from Cucurbita moschata, has previously been shown to contain anti-adipogenic and antilipogenic effects on 3T3-L1 cells and mouse embryonic fibroblasts. As some of phytochemicals derived from natural plants show anti-inflammatory or an...
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doi：10.1111/bph.13137
更新日期：2015-07-01 00:00:00
