Heterogeneity of Biochemical Actions Among Vasodilators
Thirty-four vasodilators were screened in several in vitro biochemical assays related to smooth muscle excitation-contraction coupling, binding to β1-, β2-, and α-adrenergic receptors, inhibition of phosphodiesterase activity, and antagonism of calcium accumulation. Isoproterenol and perhexiline onl...
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| Veröffentlicht in: | Journal of pharmaceutical sciences 1982-01, Vol.71 (1), p.94-100 |
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| creator | Greenslade, Forrest C. Newquist, Kathryn L. Krider, Kathryn M. Chasin, Mark Scott, Cynthia K. |
| description | Thirty-four vasodilators were screened in several in vitro biochemical assays related to smooth muscle excitation-contraction coupling, binding to β1-, β2-, and α-adrenergic receptors, inhibition of phosphodiesterase activity, and antagonism of calcium accumulation. Isoproterenol and perhexiline only exhibited binding to β-adrenergic sites. Ergocryptine, tolazoline, and amotriphene only bound to α-adrenergic receptors. Leniquinsin, papaverine, proquazone, dioxyline, hoquizil, quazodine, and theophylline were active only as phosphodiesterase inhibitors. Isoxsuprine, nylidrin, and bencyclane bound to α- and β-receptors. Pentoxifylline bound to β1-sites and inhibited phosphodiesterase. Cyclandelate bound to β2-sites and blocked calcium accumulation. Cinnarizine and flunarizine antagonized calcium accumulation and bound to α-sites. Prazosin bound to α-sites and inhibited phosphodiesterase. Ethaverine and dipyridamole were inhibitors of phosphodiesterase and calcium accumulation. Nafronyl bound to β2- and α-sites and antagonized calcium accumulation. Mebeverine bound to β2- and α-receptors and inhibited phosphodiesterase activity and calcium accumulation. Verapamil bound to α-sites, and blocked phosphodiesterase and calcium accumulation. Quinazosin bound to β2- and α-receptors and antagonized both phosphodiesterase activity and calcium accumulation. Vasodilators that were inactive in all assays included niacin, nicotinyl alcohol, inositol nicotinate, amyl nitrite, sodium nitroprusside, diazoxide, hydralazine, and protoveratrine. Vasodilators should not be considered as a single drug class since they act on various mechanisms related to coupling of neuronal excitation to muscular contractility. |
| doi_str_mv | 10.1002/jps.2600710123 |
| format | Article |
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Isoproterenol and perhexiline only exhibited binding to β-adrenergic sites. Ergocryptine, tolazoline, and amotriphene only bound to α-adrenergic receptors. Leniquinsin, papaverine, proquazone, dioxyline, hoquizil, quazodine, and theophylline were active only as phosphodiesterase inhibitors. Isoxsuprine, nylidrin, and bencyclane bound to α- and β-receptors. Pentoxifylline bound to β1-sites and inhibited phosphodiesterase. Cyclandelate bound to β2-sites and blocked calcium accumulation. Cinnarizine and flunarizine antagonized calcium accumulation and bound to α-sites. Prazosin bound to α-sites and inhibited phosphodiesterase. Ethaverine and dipyridamole were inhibitors of phosphodiesterase and calcium accumulation. Nafronyl bound to β2- and α-sites and antagonized calcium accumulation. Mebeverine bound to β2- and α-receptors and inhibited phosphodiesterase activity and calcium accumulation. Verapamil bound to α-sites, and blocked phosphodiesterase and calcium accumulation. Quinazosin bound to β2- and α-receptors and antagonized both phosphodiesterase activity and calcium accumulation. Vasodilators that were inactive in all assays included niacin, nicotinyl alcohol, inositol nicotinate, amyl nitrite, sodium nitroprusside, diazoxide, hydralazine, and protoveratrine. Vasodilators should not be considered as a single drug class since they act on various mechanisms related to coupling of neuronal excitation to muscular contractility.</description><identifier>ISSN: 0022-3549</identifier><identifier>EISSN: 1520-6017</identifier><identifier>DOI: 10.1002/jps.2600710123</identifier><identifier>PMID: 6276530</identifier><language>eng</language><publisher>Washington: Elsevier Inc</publisher><subject>3',5'-Cyclic-AMP Phosphodiesterases - antagonists & inhibitors ; Adrenergic receptors-α ; Adrenergic receptors—α, β1, and β2, effect of various vasodilators ; and β2 ; Animals ; Biological Transport - drug effects ; Calcium - metabolism ; Calcium-effect of various vasodilators on intracellular accumulation ; Calcium—effect of various vasodilators on intracellular accumulation, red blood cells ; effect of various vasodilators ; Female ; Guinea Pigs ; Humans ; In Vitro Techniques ; Macaca fascicularis ; Muscle, Smooth, Vascular - drug effects ; Muscle, Smooth, Vascular - metabolism ; Phosphodiesterase-inhibition by various vasodilators ; Rabbits ; Rats ; Receptors, Adrenergic, alpha - metabolism ; Receptors, Adrenergic, beta - metabolism ; red blood cells ; Vasodilator Agents - metabolism ; Vasodilator Agents - pharmacology ; Vasodilators-biochemical mechanisms</subject><ispartof>Journal of pharmaceutical sciences, 1982-01, Vol.71 (1), p.94-100</ispartof><rights>1982 Wiley-Liss, Inc., A Wiley Company</rights><rights>Copyright © 1982 Wiley‐Liss, Inc., A Wiley Company</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c4933-6377bfb72bf87e1ee48c922aa05d2a56015f1f4a640a5d688af07a21d8c28b663</citedby><cites>FETCH-LOGICAL-c4933-6377bfb72bf87e1ee48c922aa05d2a56015f1f4a640a5d688af07a21d8c28b663</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://onlinelibrary.wiley.com/doi/pdf/10.1002%2Fjps.2600710123$$EPDF$$P50$$Gwiley$$H</linktopdf><linktohtml>$$Uhttps://onlinelibrary.wiley.com/doi/full/10.1002%2Fjps.2600710123$$EHTML$$P50$$Gwiley$$H</linktohtml><link.rule.ids>314,780,784,1417,27924,27925,45574,45575</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/6276530$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Greenslade, Forrest C.</creatorcontrib><creatorcontrib>Newquist, Kathryn L.</creatorcontrib><creatorcontrib>Krider, Kathryn M.</creatorcontrib><creatorcontrib>Chasin, Mark</creatorcontrib><creatorcontrib>Scott, Cynthia K.</creatorcontrib><title>Heterogeneity of Biochemical Actions Among Vasodilators</title><title>Journal of pharmaceutical sciences</title><addtitle>J. Pharm. Sci</addtitle><description>Thirty-four vasodilators were screened in several in vitro biochemical assays related to smooth muscle excitation-contraction coupling, binding to β1-, β2-, and α-adrenergic receptors, inhibition of phosphodiesterase activity, and antagonism of calcium accumulation. Isoproterenol and perhexiline only exhibited binding to β-adrenergic sites. Ergocryptine, tolazoline, and amotriphene only bound to α-adrenergic receptors. Leniquinsin, papaverine, proquazone, dioxyline, hoquizil, quazodine, and theophylline were active only as phosphodiesterase inhibitors. Isoxsuprine, nylidrin, and bencyclane bound to α- and β-receptors. Pentoxifylline bound to β1-sites and inhibited phosphodiesterase. Cyclandelate bound to β2-sites and blocked calcium accumulation. Cinnarizine and flunarizine antagonized calcium accumulation and bound to α-sites. Prazosin bound to α-sites and inhibited phosphodiesterase. Ethaverine and dipyridamole were inhibitors of phosphodiesterase and calcium accumulation. Nafronyl bound to β2- and α-sites and antagonized calcium accumulation. Mebeverine bound to β2- and α-receptors and inhibited phosphodiesterase activity and calcium accumulation. Verapamil bound to α-sites, and blocked phosphodiesterase and calcium accumulation. Quinazosin bound to β2- and α-receptors and antagonized both phosphodiesterase activity and calcium accumulation. Vasodilators that were inactive in all assays included niacin, nicotinyl alcohol, inositol nicotinate, amyl nitrite, sodium nitroprusside, diazoxide, hydralazine, and protoveratrine. Vasodilators should not be considered as a single drug class since they act on various mechanisms related to coupling of neuronal excitation to muscular contractility.</description><subject>3',5'-Cyclic-AMP Phosphodiesterases - antagonists & inhibitors</subject><subject>Adrenergic receptors-α</subject><subject>Adrenergic receptors—α, β1, and β2, effect of various vasodilators</subject><subject>and β2</subject><subject>Animals</subject><subject>Biological Transport - drug effects</subject><subject>Calcium - metabolism</subject><subject>Calcium-effect of various vasodilators on intracellular accumulation</subject><subject>Calcium—effect of various vasodilators on intracellular accumulation, red blood cells</subject><subject>effect of various vasodilators</subject><subject>Female</subject><subject>Guinea Pigs</subject><subject>Humans</subject><subject>In Vitro Techniques</subject><subject>Macaca fascicularis</subject><subject>Muscle, Smooth, Vascular - drug effects</subject><subject>Muscle, Smooth, Vascular - metabolism</subject><subject>Phosphodiesterase-inhibition by various vasodilators</subject><subject>Rabbits</subject><subject>Rats</subject><subject>Receptors, Adrenergic, alpha - metabolism</subject><subject>Receptors, Adrenergic, beta - metabolism</subject><subject>red blood cells</subject><subject>Vasodilator Agents - metabolism</subject><subject>Vasodilator Agents - pharmacology</subject><subject>Vasodilators-biochemical mechanisms</subject><issn>0022-3549</issn><issn>1520-6017</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1982</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkE1P3DAQhq2qiC5Lr9yQcuot27Ed28lxQYWlQrQSH8vNcpwJGJJ4a2eB_fcNyoqKA-ppDvO8r2YeQg4ozCgA-_6wijMmARQFyvgnMqGCQSqBqs9kMgAs5SIrvpC9GB8AQIIQu2RXMiUFhwlRC-wx-Dvs0PWbxNfJkfP2HltnTZPMbe98F5N567u75MZEX7nG9D7EfbJTmybi1-2ckuuTH1fHi_T81-nZ8fw8tVnBeSq5UmVdKlbWuUKKmOW2YMwYEBUzYjhT1LTOjMzAiErmualBGUar3LK8lJJPybexdxX8nzXGXrcuWmwa06FfR614kYuMFgM4G0EbfIwBa70KrjVhoynoV1N6MKX_mRoCh9vmddli9YZv1Qz7Ytw_uwY3_2nTP39fvutOx6yLPb68ZU141FJxJfTy4lRfLDi7VcuFPhr4fORxUPnkMOhoHXYWKxfQ9rry7qM3_gIBfJWN</recordid><startdate>198201</startdate><enddate>198201</enddate><creator>Greenslade, Forrest C.</creator><creator>Newquist, Kathryn L.</creator><creator>Krider, Kathryn M.</creator><creator>Chasin, Mark</creator><creator>Scott, Cynthia K.</creator><general>Elsevier Inc</general><general>Wiley Subscription Services, Inc., A Wiley Company</general><scope>BSCLL</scope><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>198201</creationdate><title>Heterogeneity of Biochemical Actions Among Vasodilators</title><author>Greenslade, Forrest C. ; Newquist, Kathryn L. ; Krider, Kathryn M. ; Chasin, Mark ; Scott, Cynthia K.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c4933-6377bfb72bf87e1ee48c922aa05d2a56015f1f4a640a5d688af07a21d8c28b663</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1982</creationdate><topic>3',5'-Cyclic-AMP Phosphodiesterases - antagonists & inhibitors</topic><topic>Adrenergic receptors-α</topic><topic>Adrenergic receptors—α, β1, and β2, effect of various vasodilators</topic><topic>and β2</topic><topic>Animals</topic><topic>Biological Transport - drug effects</topic><topic>Calcium - metabolism</topic><topic>Calcium-effect of various vasodilators on intracellular accumulation</topic><topic>Calcium—effect of various vasodilators on intracellular accumulation, red blood cells</topic><topic>effect of various vasodilators</topic><topic>Female</topic><topic>Guinea Pigs</topic><topic>Humans</topic><topic>In Vitro Techniques</topic><topic>Macaca fascicularis</topic><topic>Muscle, Smooth, Vascular - drug effects</topic><topic>Muscle, Smooth, Vascular - metabolism</topic><topic>Phosphodiesterase-inhibition by various vasodilators</topic><topic>Rabbits</topic><topic>Rats</topic><topic>Receptors, Adrenergic, alpha - metabolism</topic><topic>Receptors, Adrenergic, beta - metabolism</topic><topic>red blood cells</topic><topic>Vasodilator Agents - metabolism</topic><topic>Vasodilator Agents - pharmacology</topic><topic>Vasodilators-biochemical mechanisms</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Greenslade, Forrest C.</creatorcontrib><creatorcontrib>Newquist, Kathryn L.</creatorcontrib><creatorcontrib>Krider, Kathryn M.</creatorcontrib><creatorcontrib>Chasin, Mark</creatorcontrib><creatorcontrib>Scott, Cynthia K.</creatorcontrib><collection>Istex</collection><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 pharmaceutical sciences</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Greenslade, Forrest C.</au><au>Newquist, Kathryn L.</au><au>Krider, Kathryn M.</au><au>Chasin, Mark</au><au>Scott, Cynthia K.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Heterogeneity of Biochemical Actions Among Vasodilators</atitle><jtitle>Journal of pharmaceutical sciences</jtitle><addtitle>J. Pharm. Sci</addtitle><date>1982-01</date><risdate>1982</risdate><volume>71</volume><issue>1</issue><spage>94</spage><epage>100</epage><pages>94-100</pages><issn>0022-3549</issn><eissn>1520-6017</eissn><abstract>Thirty-four vasodilators were screened in several in vitro biochemical assays related to smooth muscle excitation-contraction coupling, binding to β1-, β2-, and α-adrenergic receptors, inhibition of phosphodiesterase activity, and antagonism of calcium accumulation. Isoproterenol and perhexiline only exhibited binding to β-adrenergic sites. Ergocryptine, tolazoline, and amotriphene only bound to α-adrenergic receptors. Leniquinsin, papaverine, proquazone, dioxyline, hoquizil, quazodine, and theophylline were active only as phosphodiesterase inhibitors. Isoxsuprine, nylidrin, and bencyclane bound to α- and β-receptors. Pentoxifylline bound to β1-sites and inhibited phosphodiesterase. Cyclandelate bound to β2-sites and blocked calcium accumulation. Cinnarizine and flunarizine antagonized calcium accumulation and bound to α-sites. Prazosin bound to α-sites and inhibited phosphodiesterase. Ethaverine and dipyridamole were inhibitors of phosphodiesterase and calcium accumulation. Nafronyl bound to β2- and α-sites and antagonized calcium accumulation. Mebeverine bound to β2- and α-receptors and inhibited phosphodiesterase activity and calcium accumulation. Verapamil bound to α-sites, and blocked phosphodiesterase and calcium accumulation. Quinazosin bound to β2- and α-receptors and antagonized both phosphodiesterase activity and calcium accumulation. Vasodilators that were inactive in all assays included niacin, nicotinyl alcohol, inositol nicotinate, amyl nitrite, sodium nitroprusside, diazoxide, hydralazine, and protoveratrine. Vasodilators should not be considered as a single drug class since they act on various mechanisms related to coupling of neuronal excitation to muscular contractility.</abstract><cop>Washington</cop><pub>Elsevier Inc</pub><pmid>6276530</pmid><doi>10.1002/jps.2600710123</doi><tpages>7</tpages></addata></record> |
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| ispartof | Journal of pharmaceutical sciences, 1982-01, Vol.71 (1), p.94-100 |
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| subjects | 3',5'-Cyclic-AMP Phosphodiesterases - antagonists & inhibitors Adrenergic receptors-α Adrenergic receptors—α, β1, and β2, effect of various vasodilators and β2 Animals Biological Transport - drug effects Calcium - metabolism Calcium-effect of various vasodilators on intracellular accumulation Calcium—effect of various vasodilators on intracellular accumulation, red blood cells effect of various vasodilators Female Guinea Pigs Humans In Vitro Techniques Macaca fascicularis Muscle, Smooth, Vascular - drug effects Muscle, Smooth, Vascular - metabolism Phosphodiesterase-inhibition by various vasodilators Rabbits Rats Receptors, Adrenergic, alpha - metabolism Receptors, Adrenergic, beta - metabolism red blood cells Vasodilator Agents - metabolism Vasodilator Agents - pharmacology Vasodilators-biochemical mechanisms |
| title | Heterogeneity of Biochemical Actions Among Vasodilators |
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