Vasorelaxant properties of norbormide, a selective vasoconstrictor agent for the rat microvasculature
1 The effects of norbormide on the contractility of endothelium‐deprived rat, guinea‐pig, mouse, and human artery rings, and of freshly isolated smooth muscle cells of rat caudal artery were investigated. In addition, the effect of norbormide on intracellular calcium levels of A7r5 cells was evaluat...
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| Veröffentlicht in: | British journal of pharmacology 1996-03, Vol.117 (6), p.1041-1046 |
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| creator | Bova, Sergio Trevisi, Lucia Debetto, Patrizia Cima, Lorenzo Fumari, Maurizio Luciani, Sisto Padrini, Roberto Cargnelli, Gabriella |
| description | 1
The effects of norbormide on the contractility of endothelium‐deprived rat, guinea‐pig, mouse, and human artery rings, and of freshly isolated smooth muscle cells of rat caudal artery were investigated. In addition, the effect of norbormide on intracellular calcium levels of A7r5 cells was evaluated.
2
In resting rat mesenteric, renal, and caudal arteries, norbormide (0.5–50 μm) induced a concentration‐dependent contractile effect. In rat caudal artery, the contraction was very slowly reversible on washing, completely abolished in the absence of extracellular calcium, and antagonized by high concentrations (10–800 μm) of verapamil. The norbormide effect persisted upon removal of either extracellular Na+ or K+. The contractile effect of norbormide was observed also in single, freshly isolated smooth muscle cells from rat caudal artery.
3
In resting rat and guinea‐pig aortae, guinea‐pig mesenteric artery, mouse caudal artery, and human subcutaneous resistance arteries, norbormide did not induce contraction. When these vessels were contracted by 80 mM KCl, norbormide (10–100 μm) caused relaxation. Norbormide inhibited the response to Ca2+ of rat aorta incubated in 80 mM KCl/Ca2+‐free medium. Norbormide (up to 100 μm) was ineffective in phenylephrine‐contracted guinea‐pig and rat aorta.
4
In A7r5 cells, a cell line from rat aorta, norbormide prevented high K+‐but not 5‐hydro‐xytryptamine‐induced intracellular calcium transients.
5
These findings indicate that in vitro, norbormide induces a myogenic contraction, selective for the rat small vessels, by promoting calcium entry in smooth muscle cells, presumably through calcium channels. In rat aorta and arteries from other mammals, norbormide behaves like a calcium channel entry blocker. |
| doi_str_mv | 10.1111/j.1476-5381.1996.tb16694.x |
| format | Article |
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The effects of norbormide on the contractility of endothelium‐deprived rat, guinea‐pig, mouse, and human artery rings, and of freshly isolated smooth muscle cells of rat caudal artery were investigated. In addition, the effect of norbormide on intracellular calcium levels of A7r5 cells was evaluated.
2
In resting rat mesenteric, renal, and caudal arteries, norbormide (0.5–50 μm) induced a concentration‐dependent contractile effect. In rat caudal artery, the contraction was very slowly reversible on washing, completely abolished in the absence of extracellular calcium, and antagonized by high concentrations (10–800 μm) of verapamil. The norbormide effect persisted upon removal of either extracellular Na+ or K+. The contractile effect of norbormide was observed also in single, freshly isolated smooth muscle cells from rat caudal artery.
3
In resting rat and guinea‐pig aortae, guinea‐pig mesenteric artery, mouse caudal artery, and human subcutaneous resistance arteries, norbormide did not induce contraction. When these vessels were contracted by 80 mM KCl, norbormide (10–100 μm) caused relaxation. Norbormide inhibited the response to Ca2+ of rat aorta incubated in 80 mM KCl/Ca2+‐free medium. Norbormide (up to 100 μm) was ineffective in phenylephrine‐contracted guinea‐pig and rat aorta.
4
In A7r5 cells, a cell line from rat aorta, norbormide prevented high K+‐but not 5‐hydro‐xytryptamine‐induced intracellular calcium transients.
5
These findings indicate that in vitro, norbormide induces a myogenic contraction, selective for the rat small vessels, by promoting calcium entry in smooth muscle cells, presumably through calcium channels. In rat aorta and arteries from other mammals, norbormide behaves like a calcium channel entry blocker.</description><identifier>ISSN: 0007-1188</identifier><identifier>EISSN: 1476-5381</identifier><identifier>DOI: 10.1111/j.1476-5381.1996.tb16694.x</identifier><identifier>PMID: 8882594</identifier><identifier>CODEN: BJPCBM</identifier><language>eng</language><publisher>Oxford, UK: Blackwell Publishing Ltd</publisher><subject>Animals ; Biological and medical sciences ; Ca2+ influx ; Calcium - metabolism ; calcium channel entry blocker ; Cardiovascular system ; Cell Line ; Dose-Response Relationship, Drug ; Guinea Pigs ; Humans ; intracellular Ca2+ levels ; Male ; Medical sciences ; Mice ; Microcirculation - drug effects ; Miscellaneous ; Muscle, Smooth, Vascular - drug effects ; Norbormide ; Norbornanes - pharmacology ; Pharmacology. Drug treatments ; Rats ; Rats, Sprague-Dawley ; vascular smooth muscle cells ; vascular smooth muscle rings ; Vasoconstrictor Agents - pharmacology ; Vasodilation</subject><ispartof>British journal of pharmacology, 1996-03, Vol.117 (6), p.1041-1046</ispartof><rights>1996 British Pharmacological Society</rights><rights>1996 INIST-CNRS</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c5734-5369d0fc5616b30fa3ec14e6bb20f5ff70fd6f077fa6a15f5380d392dcd611c03</citedby><cites>FETCH-LOGICAL-c5734-5369d0fc5616b30fa3ec14e6bb20f5ff70fd6f077fa6a15f5380d392dcd611c03</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/PMC1909795/pdf/$$EPDF$$P50$$Gpubmedcentral$$H</linktopdf><linktohtml>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC1909795/$$EHTML$$P50$$Gpubmedcentral$$H</linktohtml><link.rule.ids>230,314,727,780,784,885,1417,27924,27925,45574,45575,53791,53793</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=3038227$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/8882594$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Bova, Sergio</creatorcontrib><creatorcontrib>Trevisi, Lucia</creatorcontrib><creatorcontrib>Debetto, Patrizia</creatorcontrib><creatorcontrib>Cima, Lorenzo</creatorcontrib><creatorcontrib>Fumari, Maurizio</creatorcontrib><creatorcontrib>Luciani, Sisto</creatorcontrib><creatorcontrib>Padrini, Roberto</creatorcontrib><creatorcontrib>Cargnelli, Gabriella</creatorcontrib><title>Vasorelaxant properties of norbormide, a selective vasoconstrictor agent for the rat microvasculature</title><title>British journal of pharmacology</title><addtitle>Br J Pharmacol</addtitle><description>1
The effects of norbormide on the contractility of endothelium‐deprived rat, guinea‐pig, mouse, and human artery rings, and of freshly isolated smooth muscle cells of rat caudal artery were investigated. In addition, the effect of norbormide on intracellular calcium levels of A7r5 cells was evaluated.
2
In resting rat mesenteric, renal, and caudal arteries, norbormide (0.5–50 μm) induced a concentration‐dependent contractile effect. In rat caudal artery, the contraction was very slowly reversible on washing, completely abolished in the absence of extracellular calcium, and antagonized by high concentrations (10–800 μm) of verapamil. The norbormide effect persisted upon removal of either extracellular Na+ or K+. The contractile effect of norbormide was observed also in single, freshly isolated smooth muscle cells from rat caudal artery.
3
In resting rat and guinea‐pig aortae, guinea‐pig mesenteric artery, mouse caudal artery, and human subcutaneous resistance arteries, norbormide did not induce contraction. When these vessels were contracted by 80 mM KCl, norbormide (10–100 μm) caused relaxation. Norbormide inhibited the response to Ca2+ of rat aorta incubated in 80 mM KCl/Ca2+‐free medium. Norbormide (up to 100 μm) was ineffective in phenylephrine‐contracted guinea‐pig and rat aorta.
4
In A7r5 cells, a cell line from rat aorta, norbormide prevented high K+‐but not 5‐hydro‐xytryptamine‐induced intracellular calcium transients.
5
These findings indicate that in vitro, norbormide induces a myogenic contraction, selective for the rat small vessels, by promoting calcium entry in smooth muscle cells, presumably through calcium channels. In rat aorta and arteries from other mammals, norbormide behaves like a calcium channel entry blocker.</description><subject>Animals</subject><subject>Biological and medical sciences</subject><subject>Ca2+ influx</subject><subject>Calcium - metabolism</subject><subject>calcium channel entry blocker</subject><subject>Cardiovascular system</subject><subject>Cell Line</subject><subject>Dose-Response Relationship, Drug</subject><subject>Guinea Pigs</subject><subject>Humans</subject><subject>intracellular Ca2+ levels</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Mice</subject><subject>Microcirculation - drug effects</subject><subject>Miscellaneous</subject><subject>Muscle, Smooth, Vascular - drug effects</subject><subject>Norbormide</subject><subject>Norbornanes - pharmacology</subject><subject>Pharmacology. Drug treatments</subject><subject>Rats</subject><subject>Rats, Sprague-Dawley</subject><subject>vascular smooth muscle cells</subject><subject>vascular smooth muscle rings</subject><subject>Vasoconstrictor Agents - pharmacology</subject><subject>Vasodilation</subject><issn>0007-1188</issn><issn>1476-5381</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1996</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqVUV2P1CAUJUazjqs_wYQY49NOhdJC8cHobtQ12UQf1FdC6WWXCS0j0HH238s4zUQf5YWbnA_O5SD0gpKKlvN6U9FG8HXLOlpRKXmVe8q5bKr9A7Q6QQ_RihAi1pR23WP0JKUNIQUU7Rk667qubmWzQvBDpxDB672eMt7GsIWYHSQcLJ5C7EMc3QAXWOMEHkx2O8C7IjFhSjk6k0PE-haK1pYp3wGOOuPRmRgKzcxe5znCU_TIap_g2XKfo-8fP3y7ul7ffPn0-er9zdq0gjUlNZcDsabllPeMWM3A0AZ439fEttYKYgduiRBWc01bW7YkA5P1YAZOqSHsHL09-m7nfoTBlFxRe7WNbtTxXgXt1L_I5O7UbdgpKokUsi0GrxaDGH7OkLIaXTLgvZ4gzEmJruGUUFqIb47EsmhKEezpEUrUoSS1UYcm1KEJdShJLSWpfRE__zvmSbq0UvCXC16-UHsb9WRcOtEYYV1di0J7d6T9ch7u_yOAuvx6_WdkvwHm5LNX</recordid><startdate>199603</startdate><enddate>199603</enddate><creator>Bova, Sergio</creator><creator>Trevisi, Lucia</creator><creator>Debetto, Patrizia</creator><creator>Cima, Lorenzo</creator><creator>Fumari, Maurizio</creator><creator>Luciani, Sisto</creator><creator>Padrini, Roberto</creator><creator>Cargnelli, Gabriella</creator><general>Blackwell Publishing Ltd</general><general>Nature Publishing</general><scope>IQODW</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><scope>5PM</scope></search><sort><creationdate>199603</creationdate><title>Vasorelaxant properties of norbormide, a selective vasoconstrictor agent for the rat microvasculature</title><author>Bova, Sergio ; Trevisi, Lucia ; Debetto, Patrizia ; Cima, Lorenzo ; Fumari, Maurizio ; Luciani, Sisto ; Padrini, Roberto ; Cargnelli, Gabriella</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c5734-5369d0fc5616b30fa3ec14e6bb20f5ff70fd6f077fa6a15f5380d392dcd611c03</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1996</creationdate><topic>Animals</topic><topic>Biological and medical sciences</topic><topic>Ca2+ influx</topic><topic>Calcium - metabolism</topic><topic>calcium channel entry blocker</topic><topic>Cardiovascular system</topic><topic>Cell Line</topic><topic>Dose-Response Relationship, Drug</topic><topic>Guinea Pigs</topic><topic>Humans</topic><topic>intracellular Ca2+ levels</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Mice</topic><topic>Microcirculation - drug effects</topic><topic>Miscellaneous</topic><topic>Muscle, Smooth, Vascular - drug effects</topic><topic>Norbormide</topic><topic>Norbornanes - pharmacology</topic><topic>Pharmacology. Drug treatments</topic><topic>Rats</topic><topic>Rats, Sprague-Dawley</topic><topic>vascular smooth muscle cells</topic><topic>vascular smooth muscle rings</topic><topic>Vasoconstrictor Agents - pharmacology</topic><topic>Vasodilation</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Bova, Sergio</creatorcontrib><creatorcontrib>Trevisi, Lucia</creatorcontrib><creatorcontrib>Debetto, Patrizia</creatorcontrib><creatorcontrib>Cima, Lorenzo</creatorcontrib><creatorcontrib>Fumari, Maurizio</creatorcontrib><creatorcontrib>Luciani, Sisto</creatorcontrib><creatorcontrib>Padrini, Roberto</creatorcontrib><creatorcontrib>Cargnelli, Gabriella</creatorcontrib><collection>Pascal-Francis</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><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>Bova, Sergio</au><au>Trevisi, Lucia</au><au>Debetto, Patrizia</au><au>Cima, Lorenzo</au><au>Fumari, Maurizio</au><au>Luciani, Sisto</au><au>Padrini, Roberto</au><au>Cargnelli, Gabriella</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Vasorelaxant properties of norbormide, a selective vasoconstrictor agent for the rat microvasculature</atitle><jtitle>British journal of pharmacology</jtitle><addtitle>Br J Pharmacol</addtitle><date>1996-03</date><risdate>1996</risdate><volume>117</volume><issue>6</issue><spage>1041</spage><epage>1046</epage><pages>1041-1046</pages><issn>0007-1188</issn><eissn>1476-5381</eissn><coden>BJPCBM</coden><abstract>1
The effects of norbormide on the contractility of endothelium‐deprived rat, guinea‐pig, mouse, and human artery rings, and of freshly isolated smooth muscle cells of rat caudal artery were investigated. In addition, the effect of norbormide on intracellular calcium levels of A7r5 cells was evaluated.
2
In resting rat mesenteric, renal, and caudal arteries, norbormide (0.5–50 μm) induced a concentration‐dependent contractile effect. In rat caudal artery, the contraction was very slowly reversible on washing, completely abolished in the absence of extracellular calcium, and antagonized by high concentrations (10–800 μm) of verapamil. The norbormide effect persisted upon removal of either extracellular Na+ or K+. The contractile effect of norbormide was observed also in single, freshly isolated smooth muscle cells from rat caudal artery.
3
In resting rat and guinea‐pig aortae, guinea‐pig mesenteric artery, mouse caudal artery, and human subcutaneous resistance arteries, norbormide did not induce contraction. When these vessels were contracted by 80 mM KCl, norbormide (10–100 μm) caused relaxation. Norbormide inhibited the response to Ca2+ of rat aorta incubated in 80 mM KCl/Ca2+‐free medium. Norbormide (up to 100 μm) was ineffective in phenylephrine‐contracted guinea‐pig and rat aorta.
4
In A7r5 cells, a cell line from rat aorta, norbormide prevented high K+‐but not 5‐hydro‐xytryptamine‐induced intracellular calcium transients.
5
These findings indicate that in vitro, norbormide induces a myogenic contraction, selective for the rat small vessels, by promoting calcium entry in smooth muscle cells, presumably through calcium channels. In rat aorta and arteries from other mammals, norbormide behaves like a calcium channel entry blocker.</abstract><cop>Oxford, UK</cop><pub>Blackwell Publishing Ltd</pub><pmid>8882594</pmid><doi>10.1111/j.1476-5381.1996.tb16694.x</doi><tpages>6</tpages><oa>free_for_read</oa></addata></record> |
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| subjects | Animals Biological and medical sciences Ca2+ influx Calcium - metabolism calcium channel entry blocker Cardiovascular system Cell Line Dose-Response Relationship, Drug Guinea Pigs Humans intracellular Ca2+ levels Male Medical sciences Mice Microcirculation - drug effects Miscellaneous Muscle, Smooth, Vascular - drug effects Norbormide Norbornanes - pharmacology Pharmacology. Drug treatments Rats Rats, Sprague-Dawley vascular smooth muscle cells vascular smooth muscle rings Vasoconstrictor Agents - pharmacology Vasodilation |
| title | Vasorelaxant properties of norbormide, a selective vasoconstrictor agent for the rat microvasculature |
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