The uptake of cardiac glycosides by intestinal smooth muscle of the guinea‐pig in relation to digitalis receptors
Summary 1 . The accumulation and release of 3H‐digitoxin, 3H‐digoxin and 3H‐ouabain by isolated guinea‐pig intestinal smooth muscle has been studied and compared with a pharmacological action due to inhibition of the sodium pump. 2 . The uptake of labelled cardiac glycosides can be described by mean...
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| Veröffentlicht in: | British journal of pharmacology 1970-02, Vol.38 (2), p.345-352 |
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| container_title | British journal of pharmacology |
| container_volume | 38 |
| creator | GODFRAIND, T. LESNE, M. |
| description | Summary
1
. The accumulation and release of 3H‐digitoxin, 3H‐digoxin and 3H‐ouabain by isolated guinea‐pig intestinal smooth muscle has been studied and compared with a pharmacological action due to inhibition of the sodium pump.
2
. The uptake of labelled cardiac glycosides can be described by means of an exponential function. The t of uptake was similar for the three compounds and did not depend on the concentration.
3
. Analysis of the curve relating the uptake of cardiac glycosides at equilibrium to the bath concentration enabled a non‐saturable and a saturable binding site to be distinguished.
4
. In contrast to the uptake observations, the onset of the pharmacological effect was dependent on the concentration, and furthermore the t½; for this effect was shorter.
5
. The release of cardiac glycosides proceeded more slowly than the uptake.
6
. The uptake of a labelled glycoside was reduced in the presence of another glycoside. The amount of displaceable glycoside was nearly equivalent to the capacity of the saturable binding site.
7
. The significance of these results is discussed. |
| doi_str_mv | 10.1111/j.1476-5381.1970.tb08522.x |
| format | Article |
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1
. The accumulation and release of 3H‐digitoxin, 3H‐digoxin and 3H‐ouabain by isolated guinea‐pig intestinal smooth muscle has been studied and compared with a pharmacological action due to inhibition of the sodium pump.
2
. The uptake of labelled cardiac glycosides can be described by means of an exponential function. The t of uptake was similar for the three compounds and did not depend on the concentration.
3
. Analysis of the curve relating the uptake of cardiac glycosides at equilibrium to the bath concentration enabled a non‐saturable and a saturable binding site to be distinguished.
4
. In contrast to the uptake observations, the onset of the pharmacological effect was dependent on the concentration, and furthermore the t½; for this effect was shorter.
5
. The release of cardiac glycosides proceeded more slowly than the uptake.
6
. The uptake of a labelled glycoside was reduced in the presence of another glycoside. The amount of displaceable glycoside was nearly equivalent to the capacity of the saturable binding site.
7
. The significance of these results is discussed.</description><identifier>ISSN: 0007-1188</identifier><identifier>EISSN: 1476-5381</identifier><identifier>DOI: 10.1111/j.1476-5381.1970.tb08522.x</identifier><identifier>PMID: 5417857</identifier><language>eng</language><publisher>Oxford, UK: Blackwell Publishing Ltd</publisher><subject>Animals ; Binding Sites ; Cardiac Glycosides - metabolism ; Chromatography, Thin Layer ; Digitoxin - analysis ; Digitoxin - metabolism ; Digoxin - analysis ; Digoxin - metabolism ; Guinea Pigs ; In Vitro Techniques ; Intestinal Mucosa - metabolism ; Muscle, Smooth - analysis ; Muscle, Smooth - metabolism ; Ouabain - analysis ; Ouabain - metabolism ; Receptors, Drug ; Tritium</subject><ispartof>British journal of pharmacology, 1970-02, Vol.38 (2), p.345-352</ispartof><rights>1970 British Pharmacological Society</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c4772-36610f6229fd05e73ce0fde2726eeee5bb63b3c42fbb74f7e22e8b8d5015a5903</citedby><cites>FETCH-LOGICAL-c4772-36610f6229fd05e73ce0fde2726eeee5bb63b3c42fbb74f7e22e8b8d5015a5903</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC1702827/pdf/$$EPDF$$P50$$Gpubmedcentral$$H</linktopdf><linktohtml>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC1702827/$$EHTML$$P50$$Gpubmedcentral$$H</linktohtml><link.rule.ids>230,314,727,780,784,885,27923,27924,53790,53792</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/5417857$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>GODFRAIND, T.</creatorcontrib><creatorcontrib>LESNE, M.</creatorcontrib><title>The uptake of cardiac glycosides by intestinal smooth muscle of the guinea‐pig in relation to digitalis receptors</title><title>British journal of pharmacology</title><addtitle>Br J Pharmacol</addtitle><description>Summary
1
. The accumulation and release of 3H‐digitoxin, 3H‐digoxin and 3H‐ouabain by isolated guinea‐pig intestinal smooth muscle has been studied and compared with a pharmacological action due to inhibition of the sodium pump.
2
. The uptake of labelled cardiac glycosides can be described by means of an exponential function. The t of uptake was similar for the three compounds and did not depend on the concentration.
3
. Analysis of the curve relating the uptake of cardiac glycosides at equilibrium to the bath concentration enabled a non‐saturable and a saturable binding site to be distinguished.
4
. In contrast to the uptake observations, the onset of the pharmacological effect was dependent on the concentration, and furthermore the t½; for this effect was shorter.
5
. The release of cardiac glycosides proceeded more slowly than the uptake.
6
. The uptake of a labelled glycoside was reduced in the presence of another glycoside. The amount of displaceable glycoside was nearly equivalent to the capacity of the saturable binding site.
7
. The significance of these results is discussed.</description><subject>Animals</subject><subject>Binding Sites</subject><subject>Cardiac Glycosides - metabolism</subject><subject>Chromatography, Thin Layer</subject><subject>Digitoxin - analysis</subject><subject>Digitoxin - metabolism</subject><subject>Digoxin - analysis</subject><subject>Digoxin - metabolism</subject><subject>Guinea Pigs</subject><subject>In Vitro Techniques</subject><subject>Intestinal Mucosa - metabolism</subject><subject>Muscle, Smooth - analysis</subject><subject>Muscle, Smooth - metabolism</subject><subject>Ouabain - analysis</subject><subject>Ouabain - metabolism</subject><subject>Receptors, Drug</subject><subject>Tritium</subject><issn>0007-1188</issn><issn>1476-5381</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1970</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqVkcFu1DAQhi0EKtvCIyBZHLgl2E4cJxxApSoUqRIcytlynEnWixMH24HujUfgGXkSHHa1giNzseV__n9G_hB6TklOU73c5bQUVcaLmua0ESSPLak5Y_n9A7Q5SQ_RhhAiMkrr-jE6D2FHSBIFP0NnvKSi5mKDwt0W8DJH9QWw67FWvjNK48HutQumg4DbPTZThBDNpCwOo3Nxi8claPvHEZN_WMwE6tePn7MZUjP2YFU0bsLR4c4MJiprQnrVMEfnwxP0qFc2wNPjeYE-v7u-u7rJbj--_3B1eZvptCXLiqqipK8Ya_qOcBCFBtJ3wASrIBVv26poC12yvm1F2QtgDOq27jihXPGGFBfo9SF3XtoROg1T9MrK2ZtR-b10ysh_lcls5eC-SSoIq5lIAS-OAd59XdIXyNEEDdaqCdwSZF1y0gjWpMZXh0btXQge-tMQSuSKTO7kykWuXOSKTB6Ryftkfvb3mifrkVHS3xz078bC_j-S5dtPN-ut-A2rp6uG</recordid><startdate>197002</startdate><enddate>197002</enddate><creator>GODFRAIND, T.</creator><creator>LESNE, M.</creator><general>Blackwell Publishing Ltd</general><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope><scope>5PM</scope></search><sort><creationdate>197002</creationdate><title>The uptake of cardiac glycosides by intestinal smooth muscle of the guinea‐pig in relation to digitalis receptors</title><author>GODFRAIND, T. ; LESNE, M.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c4772-36610f6229fd05e73ce0fde2726eeee5bb63b3c42fbb74f7e22e8b8d5015a5903</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1970</creationdate><topic>Animals</topic><topic>Binding Sites</topic><topic>Cardiac Glycosides - metabolism</topic><topic>Chromatography, Thin Layer</topic><topic>Digitoxin - analysis</topic><topic>Digitoxin - metabolism</topic><topic>Digoxin - analysis</topic><topic>Digoxin - metabolism</topic><topic>Guinea Pigs</topic><topic>In Vitro Techniques</topic><topic>Intestinal Mucosa - metabolism</topic><topic>Muscle, Smooth - analysis</topic><topic>Muscle, Smooth - metabolism</topic><topic>Ouabain - analysis</topic><topic>Ouabain - metabolism</topic><topic>Receptors, Drug</topic><topic>Tritium</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>GODFRAIND, T.</creatorcontrib><creatorcontrib>LESNE, M.</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><collection>PubMed Central (Full Participant titles)</collection><jtitle>British journal of pharmacology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>GODFRAIND, T.</au><au>LESNE, M.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>The uptake of cardiac glycosides by intestinal smooth muscle of the guinea‐pig in relation to digitalis receptors</atitle><jtitle>British journal of pharmacology</jtitle><addtitle>Br J Pharmacol</addtitle><date>1970-02</date><risdate>1970</risdate><volume>38</volume><issue>2</issue><spage>345</spage><epage>352</epage><pages>345-352</pages><issn>0007-1188</issn><eissn>1476-5381</eissn><abstract>Summary
1
. The accumulation and release of 3H‐digitoxin, 3H‐digoxin and 3H‐ouabain by isolated guinea‐pig intestinal smooth muscle has been studied and compared with a pharmacological action due to inhibition of the sodium pump.
2
. The uptake of labelled cardiac glycosides can be described by means of an exponential function. The t of uptake was similar for the three compounds and did not depend on the concentration.
3
. Analysis of the curve relating the uptake of cardiac glycosides at equilibrium to the bath concentration enabled a non‐saturable and a saturable binding site to be distinguished.
4
. In contrast to the uptake observations, the onset of the pharmacological effect was dependent on the concentration, and furthermore the t½; for this effect was shorter.
5
. The release of cardiac glycosides proceeded more slowly than the uptake.
6
. The uptake of a labelled glycoside was reduced in the presence of another glycoside. The amount of displaceable glycoside was nearly equivalent to the capacity of the saturable binding site.
7
. The significance of these results is discussed.</abstract><cop>Oxford, UK</cop><pub>Blackwell Publishing Ltd</pub><pmid>5417857</pmid><doi>10.1111/j.1476-5381.1970.tb08522.x</doi><tpages>8</tpages><oa>free_for_read</oa></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0007-1188 |
| ispartof | British journal of pharmacology, 1970-02, Vol.38 (2), p.345-352 |
| issn | 0007-1188 1476-5381 |
| language | eng |
| recordid | cdi_pubmedcentral_primary_oai_pubmedcentral_nih_gov_1702827 |
| source | MEDLINE; EZB-FREE-00999 freely available EZB journals; PubMed Central; Alma/SFX Local Collection |
| subjects | Animals Binding Sites Cardiac Glycosides - metabolism Chromatography, Thin Layer Digitoxin - analysis Digitoxin - metabolism Digoxin - analysis Digoxin - metabolism Guinea Pigs In Vitro Techniques Intestinal Mucosa - metabolism Muscle, Smooth - analysis Muscle, Smooth - metabolism Ouabain - analysis Ouabain - metabolism Receptors, Drug Tritium |
| title | The uptake of cardiac glycosides by intestinal smooth muscle of the guinea‐pig in relation to digitalis receptors |
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