Structure-Activity Relationships of an Aminosugar Cardiac Glycoside, ASI-222 HCl, in the Heart-Lung Preparation of the Dog
SynopsisASI-222 [3-β-O-(4-amino-4, 6-dideoxy-β-D-galactopyranosyl) digitoxigenin HCl] is a semisynthetic aminosugar cardiac glycoside that has been shown to have a greater therapeutic index than ouabain or digoxin in dogs. We have compared the effects of ASI, digitoxigenin, digitoxigenin-β-D-galacto...
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| Veröffentlicht in: | Journal of cardiovascular pharmacology 1979-09, Vol.1 (5), p.551-560 |
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| container_end_page | 560 |
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| container_title | Journal of cardiovascular pharmacology |
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| creator | Cook, L Scott Caldwell, Robert W Nash, Clinton B |
| description | SynopsisASI-222 [3-β-O-(4-amino-4, 6-dideoxy-β-D-galactopyranosyl) digitoxigenin HCl] is a semisynthetic aminosugar cardiac glycoside that has been shown to have a greater therapeutic index than ouabain or digoxin in dogs. We have compared the effects of ASI, digitoxigenin, digitoxigenin-β-D-galactose, and digoxin in the dog heart-lung preparation. Minute work and stroke work were calculated. Controls were obtained before and after the hearts were failed with sodium pentobarbital. ASI-222 is about three times more potent than digitoxigenin and about twice as potent as digitoxigenin-β-D-galactose in producing similar increases in the left ventricular stroke work. ASI-222 is about three times more potent than digoxin in increasing left ventricular stroke work. Our results indicate that the addition of an aminosugar group to the genin further increased potency over that observed with the addition of a single neutral sugar and prolonged the duration of activity in failing myocardial tissue. |
| doi_str_mv | 10.1097/00005344-197909000-00007 |
| format | Article |
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We have compared the effects of ASI, digitoxigenin, digitoxigenin-β-D-galactose, and digoxin in the dog heart-lung preparation. Minute work and stroke work were calculated. Controls were obtained before and after the hearts were failed with sodium pentobarbital. ASI-222 is about three times more potent than digitoxigenin and about twice as potent as digitoxigenin-β-D-galactose in producing similar increases in the left ventricular stroke work. ASI-222 is about three times more potent than digoxin in increasing left ventricular stroke work. Our results indicate that the addition of an aminosugar group to the genin further increased potency over that observed with the addition of a single neutral sugar and prolonged the duration of activity in failing myocardial tissue.</description><identifier>ISSN: 0160-2446</identifier><identifier>EISSN: 1533-4023</identifier><identifier>DOI: 10.1097/00005344-197909000-00007</identifier><identifier>PMID: 94411</identifier><language>eng</language><publisher>United States: Lippincott-Raven Publishers</publisher><subject>Aminoglycosides - pharmacology ; Animals ; Blood Pressure - drug effects ; Cardiac Glycosides - pharmacology ; Digitoxigenin - analogs & derivatives ; Digitoxigenin - pharmacology ; Digoxin - pharmacology ; Dogs ; Female ; Heart - drug effects ; In Vitro Techniques ; Lung - physiology ; Male ; Myocardial Contraction - drug effects ; Structure-Activity Relationship ; Time Factors</subject><ispartof>Journal of cardiovascular pharmacology, 1979-09, Vol.1 (5), p.551-560</ispartof><rights>Lippincott-Raven Publishers.</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c3187-123f8ec734fa635b25915717a64ec6b3d18f30700f14506d3e58c6beb1610c233</citedby></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttp://ovidsp.ovid.com/ovidweb.cgi?T=JS&NEWS=n&CSC=Y&PAGE=fulltext&D=ovft&AN=00005344-197909000-00007$$EHTML$$P50$$Gwolterskluwer$$H</linktohtml><link.rule.ids>314,776,780,4594,27903,27904,65210</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/94411$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Cook, L Scott</creatorcontrib><creatorcontrib>Caldwell, Robert W</creatorcontrib><creatorcontrib>Nash, Clinton B</creatorcontrib><title>Structure-Activity Relationships of an Aminosugar Cardiac Glycoside, ASI-222 HCl, in the Heart-Lung Preparation of the Dog</title><title>Journal of cardiovascular pharmacology</title><addtitle>J Cardiovasc Pharmacol</addtitle><description>SynopsisASI-222 [3-β-O-(4-amino-4, 6-dideoxy-β-D-galactopyranosyl) digitoxigenin HCl] is a semisynthetic aminosugar cardiac glycoside that has been shown to have a greater therapeutic index than ouabain or digoxin in dogs. We have compared the effects of ASI, digitoxigenin, digitoxigenin-β-D-galactose, and digoxin in the dog heart-lung preparation. Minute work and stroke work were calculated. Controls were obtained before and after the hearts were failed with sodium pentobarbital. ASI-222 is about three times more potent than digitoxigenin and about twice as potent as digitoxigenin-β-D-galactose in producing similar increases in the left ventricular stroke work. ASI-222 is about three times more potent than digoxin in increasing left ventricular stroke work. Our results indicate that the addition of an aminosugar group to the genin further increased potency over that observed with the addition of a single neutral sugar and prolonged the duration of activity in failing myocardial tissue.</description><subject>Aminoglycosides - pharmacology</subject><subject>Animals</subject><subject>Blood Pressure - drug effects</subject><subject>Cardiac Glycosides - pharmacology</subject><subject>Digitoxigenin - analogs & derivatives</subject><subject>Digitoxigenin - pharmacology</subject><subject>Digoxin - pharmacology</subject><subject>Dogs</subject><subject>Female</subject><subject>Heart - drug effects</subject><subject>In Vitro Techniques</subject><subject>Lung - physiology</subject><subject>Male</subject><subject>Myocardial Contraction - drug effects</subject><subject>Structure-Activity Relationship</subject><subject>Time Factors</subject><issn>0160-2446</issn><issn>1533-4023</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1979</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp1UU1PGzEQtSpQCbS_oBefesLgr7V3j1GgBCkSVWnPluOdTVycdWp7i9Jf300C3JjLaN6beaN5gxBm9IrRRl_TMSohJWGNbmgzVmQP6Q9owiohiKRcnKAJZYoSLqU6Q-c5_6aUyUqrj-i0kZKxCfr3WNLgypCATF3xf33Z4R8QbPGxz2u_zTh22PZ4uvF9zMPKJjyzqfXW4buwczH7Fi7x9PGecM7xfBYuse9xWQOeg02FLIZ-hb8n2Np00NzL7dmbuPqETjsbMnx-yRfo17fbn7M5WTzc3c-mC-IEqzVhXHQ1OC1kZ5WolrxqWKWZtkqCU0vRsroTVFPajadR1Qqo6hGHJVOMOi7EBfp61N2m-GeAXMzGZwch2B7ikI2WjVaMN2NjfWx0KeacoDPb5Dc27QyjZm-6eTXdvJl-gPQ4-uVlx7DcQPs2eHB5ZOWRfY6hQMpPYXiGZNZgQ1mb9z4p_gO2D4ps</recordid><startdate>197909</startdate><enddate>197909</enddate><creator>Cook, L Scott</creator><creator>Caldwell, Robert W</creator><creator>Nash, Clinton B</creator><general>Lippincott-Raven Publishers</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></search><sort><creationdate>197909</creationdate><title>Structure-Activity Relationships of an Aminosugar Cardiac Glycoside, ASI-222 HCl, in the Heart-Lung Preparation of the Dog</title><author>Cook, L Scott ; Caldwell, Robert W ; Nash, Clinton B</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c3187-123f8ec734fa635b25915717a64ec6b3d18f30700f14506d3e58c6beb1610c233</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1979</creationdate><topic>Aminoglycosides - pharmacology</topic><topic>Animals</topic><topic>Blood Pressure - drug effects</topic><topic>Cardiac Glycosides - pharmacology</topic><topic>Digitoxigenin - analogs & derivatives</topic><topic>Digitoxigenin - pharmacology</topic><topic>Digoxin - pharmacology</topic><topic>Dogs</topic><topic>Female</topic><topic>Heart - drug effects</topic><topic>In Vitro Techniques</topic><topic>Lung - physiology</topic><topic>Male</topic><topic>Myocardial Contraction - drug effects</topic><topic>Structure-Activity Relationship</topic><topic>Time Factors</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Cook, L Scott</creatorcontrib><creatorcontrib>Caldwell, Robert W</creatorcontrib><creatorcontrib>Nash, Clinton B</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><jtitle>Journal of cardiovascular pharmacology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Cook, L Scott</au><au>Caldwell, Robert W</au><au>Nash, Clinton B</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Structure-Activity Relationships of an Aminosugar Cardiac Glycoside, ASI-222 HCl, in the Heart-Lung Preparation of the Dog</atitle><jtitle>Journal of cardiovascular pharmacology</jtitle><addtitle>J Cardiovasc Pharmacol</addtitle><date>1979-09</date><risdate>1979</risdate><volume>1</volume><issue>5</issue><spage>551</spage><epage>560</epage><pages>551-560</pages><issn>0160-2446</issn><eissn>1533-4023</eissn><abstract>SynopsisASI-222 [3-β-O-(4-amino-4, 6-dideoxy-β-D-galactopyranosyl) digitoxigenin HCl] is a semisynthetic aminosugar cardiac glycoside that has been shown to have a greater therapeutic index than ouabain or digoxin in dogs. We have compared the effects of ASI, digitoxigenin, digitoxigenin-β-D-galactose, and digoxin in the dog heart-lung preparation. Minute work and stroke work were calculated. Controls were obtained before and after the hearts were failed with sodium pentobarbital. ASI-222 is about three times more potent than digitoxigenin and about twice as potent as digitoxigenin-β-D-galactose in producing similar increases in the left ventricular stroke work. ASI-222 is about three times more potent than digoxin in increasing left ventricular stroke work. Our results indicate that the addition of an aminosugar group to the genin further increased potency over that observed with the addition of a single neutral sugar and prolonged the duration of activity in failing myocardial tissue.</abstract><cop>United States</cop><pub>Lippincott-Raven Publishers</pub><pmid>94411</pmid><doi>10.1097/00005344-197909000-00007</doi><tpages>10</tpages><oa>free_for_read</oa></addata></record> |
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| ispartof | Journal of cardiovascular pharmacology, 1979-09, Vol.1 (5), p.551-560 |
| issn | 0160-2446 1533-4023 |
| language | eng |
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| source | MEDLINE; Journals@Ovid LWW Legacy Archive; Elektronische Zeitschriftenbibliothek - Frei zugängliche E-Journals; Journals@Ovid Ovid Autoload |
| subjects | Aminoglycosides - pharmacology Animals Blood Pressure - drug effects Cardiac Glycosides - pharmacology Digitoxigenin - analogs & derivatives Digitoxigenin - pharmacology Digoxin - pharmacology Dogs Female Heart - drug effects In Vitro Techniques Lung - physiology Male Myocardial Contraction - drug effects Structure-Activity Relationship Time Factors |
| title | Structure-Activity Relationships of an Aminosugar Cardiac Glycoside, ASI-222 HCl, in the Heart-Lung Preparation of the Dog |
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