Antihypertensive effect of a newly synthesized endothelin antagonist, BQ-123, in a genetic hypertensive model
A newly synthesized ET A-selective antagonist, BQ-123, was examined with respect to its anti-endothelin(ET) action in vitro and in vivo and its effect on blood pressure in Wistar Kyoto rats (WKY), spontaneously hypertensive rats (SHR) and stroke-prone spontaneously hypertensive rats (SHRSP). In isol...
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| Veröffentlicht in: | Life sciences (1973) 1993, Vol.52 (8), p.717-724 |
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| container_title | Life sciences (1973) |
| container_volume | 52 |
| creator | Nishikibe, Masaru Tsuchida, Sonoko Okada, Megumu Fukuroda, Takahiro Shimamoto, Koji Yano, Mitsuo Ishikawa, Kiyofumi Ikemoto, Fumihiko |
| description | A newly synthesized ET
A-selective antagonist, BQ-123, was examined with respect to its anti-endothelin(ET) action in vitro and in vivo and its effect on blood pressure in Wistar Kyoto rats (WKY), spontaneously hypertensive rats (SHR) and stroke-prone spontaneously hypertensive rats (SHRSP). In isolated porcine coronary arteries, BQ-123 (0.07 μM to 6.0 μM) shifted the concentration-response curve for ET-1 to the right without affecting the maximal response of ET-1, its pA
2 value being 7.35. Intravenous infusion of BQ-123 at a rate of 1.2 and 30 mg/kg/hr produced a significant decrease in blood pressure in 20- to 29-week-old SHRSP, but did not alter blood pressure in 13- to 16-week-old WKY or in 18- to 19-week-old and 40-week-old SHR. The hypotensive effect of BQ-123 depended on the pretreatment blood pressure level. These results suggest that ET-1 is involved in part in the maintenance of high blood pressure in malignant hypertension, as exemplified by SHRSP. |
| doi_str_mv | 10.1016/0024-3205(93)90233-S |
| format | Article |
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A-selective antagonist, BQ-123, was examined with respect to its anti-endothelin(ET) action in vitro and in vivo and its effect on blood pressure in Wistar Kyoto rats (WKY), spontaneously hypertensive rats (SHR) and stroke-prone spontaneously hypertensive rats (SHRSP). In isolated porcine coronary arteries, BQ-123 (0.07 μM to 6.0 μM) shifted the concentration-response curve for ET-1 to the right without affecting the maximal response of ET-1, its pA
2 value being 7.35. Intravenous infusion of BQ-123 at a rate of 1.2 and 30 mg/kg/hr produced a significant decrease in blood pressure in 20- to 29-week-old SHRSP, but did not alter blood pressure in 13- to 16-week-old WKY or in 18- to 19-week-old and 40-week-old SHR. The hypotensive effect of BQ-123 depended on the pretreatment blood pressure level. These results suggest that ET-1 is involved in part in the maintenance of high blood pressure in malignant hypertension, as exemplified by SHRSP.</description><identifier>ISSN: 0024-3205</identifier><identifier>EISSN: 1879-0631</identifier><identifier>DOI: 10.1016/0024-3205(93)90233-S</identifier><identifier>PMID: 8446001</identifier><identifier>CODEN: LIFSAK</identifier><language>eng</language><publisher>Amsterdam: Elsevier Inc</publisher><subject>Amino Acid Sequence ; Analysis of Variance ; Animals ; Antihypertensive agents ; Antihypertensive Agents - pharmacology ; Biological and medical sciences ; Cardiovascular system ; Endothelins - antagonists & inhibitors ; Endothelium, Vascular - drug effects ; Hypertension - drug therapy ; Hypertension - genetics ; In Vitro Techniques ; Male ; Medical sciences ; Models, Genetic ; Molecular Sequence Data ; Peptides, Cyclic - pharmacology ; Pharmacology. Drug treatments ; Rats ; Rats, Inbred SHR ; Rats, Inbred WKY ; Swine</subject><ispartof>Life sciences (1973), 1993, Vol.52 (8), p.717-724</ispartof><rights>1993</rights><rights>1993 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c483t-ec9282f846892b74be79e0b8edf98429405c14d7855bee169b37738f5aa9876a3</citedby><cites>FETCH-LOGICAL-c483t-ec9282f846892b74be79e0b8edf98429405c14d7855bee169b37738f5aa9876a3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/0024-3205(93)90233-S$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,780,784,3548,4021,27921,27922,27923,45993</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=4691098$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/8446001$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Nishikibe, Masaru</creatorcontrib><creatorcontrib>Tsuchida, Sonoko</creatorcontrib><creatorcontrib>Okada, Megumu</creatorcontrib><creatorcontrib>Fukuroda, Takahiro</creatorcontrib><creatorcontrib>Shimamoto, Koji</creatorcontrib><creatorcontrib>Yano, Mitsuo</creatorcontrib><creatorcontrib>Ishikawa, Kiyofumi</creatorcontrib><creatorcontrib>Ikemoto, Fumihiko</creatorcontrib><title>Antihypertensive effect of a newly synthesized endothelin antagonist, BQ-123, in a genetic hypertensive model</title><title>Life sciences (1973)</title><addtitle>Life Sci</addtitle><description>A newly synthesized ET
A-selective antagonist, BQ-123, was examined with respect to its anti-endothelin(ET) action in vitro and in vivo and its effect on blood pressure in Wistar Kyoto rats (WKY), spontaneously hypertensive rats (SHR) and stroke-prone spontaneously hypertensive rats (SHRSP). In isolated porcine coronary arteries, BQ-123 (0.07 μM to 6.0 μM) shifted the concentration-response curve for ET-1 to the right without affecting the maximal response of ET-1, its pA
2 value being 7.35. Intravenous infusion of BQ-123 at a rate of 1.2 and 30 mg/kg/hr produced a significant decrease in blood pressure in 20- to 29-week-old SHRSP, but did not alter blood pressure in 13- to 16-week-old WKY or in 18- to 19-week-old and 40-week-old SHR. The hypotensive effect of BQ-123 depended on the pretreatment blood pressure level. These results suggest that ET-1 is involved in part in the maintenance of high blood pressure in malignant hypertension, as exemplified by SHRSP.</description><subject>Amino Acid Sequence</subject><subject>Analysis of Variance</subject><subject>Animals</subject><subject>Antihypertensive agents</subject><subject>Antihypertensive Agents - pharmacology</subject><subject>Biological and medical sciences</subject><subject>Cardiovascular system</subject><subject>Endothelins - antagonists & inhibitors</subject><subject>Endothelium, Vascular - drug effects</subject><subject>Hypertension - drug therapy</subject><subject>Hypertension - genetics</subject><subject>In Vitro Techniques</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Models, Genetic</subject><subject>Molecular Sequence Data</subject><subject>Peptides, Cyclic - pharmacology</subject><subject>Pharmacology. Drug treatments</subject><subject>Rats</subject><subject>Rats, Inbred SHR</subject><subject>Rats, Inbred WKY</subject><subject>Swine</subject><issn>0024-3205</issn><issn>1879-0631</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1993</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkVFrFDEUhYModdv6DxTyIFJhp00mySR5EerSVqEgpe1zyGRu2shMZk2ylfXXd7a7LPiiT5fc-93DzTkIvafklBLanBFS84rVRJxo9lmTmrHq9hWaUSV1RRpGX6PZHnmLDnP-SQgRQrIDdKA4bwihMzScxxIe10tIBWIOT4DBe3AFjx5bHOF3v8Z5Hcsj5PAHOgyxG6dHHyK2sdiHMYZc5vjrTUVrNsebNn6ACCU4_JfsMHbQH6M33vYZ3u3qEbq_vLhbfKuuf1x9X5xfV44rVipwula1V7xRum4lb0FqIK2CzmvFa82JcJR3UgnRAtBGt0xKprywVivZWHaEPm11l2n8tYJczBCyg763EcZVNlJMv2eC_RekzQsoJpBvQZfGnBN4s0xhsGltKDGbOMzGa7Px2mhmXuIwt9Pah53-qh2g2y_t_J_mH3dzm53tfbLRhbzHeKMp0WrCvmwxmEx7CpBMdgGigy6kKSzTjeHfdzwDOiWl_Q</recordid><startdate>1993</startdate><enddate>1993</enddate><creator>Nishikibe, Masaru</creator><creator>Tsuchida, Sonoko</creator><creator>Okada, Megumu</creator><creator>Fukuroda, Takahiro</creator><creator>Shimamoto, Koji</creator><creator>Yano, Mitsuo</creator><creator>Ishikawa, Kiyofumi</creator><creator>Ikemoto, Fumihiko</creator><general>Elsevier Inc</general><general>Elsevier</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>7TK</scope><scope>7X8</scope></search><sort><creationdate>1993</creationdate><title>Antihypertensive effect of a newly synthesized endothelin antagonist, BQ-123, in a genetic hypertensive model</title><author>Nishikibe, Masaru ; Tsuchida, Sonoko ; Okada, Megumu ; Fukuroda, Takahiro ; Shimamoto, Koji ; Yano, Mitsuo ; Ishikawa, Kiyofumi ; Ikemoto, Fumihiko</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c483t-ec9282f846892b74be79e0b8edf98429405c14d7855bee169b37738f5aa9876a3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1993</creationdate><topic>Amino Acid Sequence</topic><topic>Analysis of Variance</topic><topic>Animals</topic><topic>Antihypertensive agents</topic><topic>Antihypertensive Agents - pharmacology</topic><topic>Biological and medical sciences</topic><topic>Cardiovascular system</topic><topic>Endothelins - antagonists & inhibitors</topic><topic>Endothelium, Vascular - drug effects</topic><topic>Hypertension - drug therapy</topic><topic>Hypertension - genetics</topic><topic>In Vitro Techniques</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Models, Genetic</topic><topic>Molecular Sequence Data</topic><topic>Peptides, Cyclic - pharmacology</topic><topic>Pharmacology. Drug treatments</topic><topic>Rats</topic><topic>Rats, Inbred SHR</topic><topic>Rats, Inbred WKY</topic><topic>Swine</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Nishikibe, Masaru</creatorcontrib><creatorcontrib>Tsuchida, Sonoko</creatorcontrib><creatorcontrib>Okada, Megumu</creatorcontrib><creatorcontrib>Fukuroda, Takahiro</creatorcontrib><creatorcontrib>Shimamoto, Koji</creatorcontrib><creatorcontrib>Yano, Mitsuo</creatorcontrib><creatorcontrib>Ishikawa, Kiyofumi</creatorcontrib><creatorcontrib>Ikemoto, Fumihiko</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>Neurosciences Abstracts</collection><collection>MEDLINE - Academic</collection><jtitle>Life sciences (1973)</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Nishikibe, Masaru</au><au>Tsuchida, Sonoko</au><au>Okada, Megumu</au><au>Fukuroda, Takahiro</au><au>Shimamoto, Koji</au><au>Yano, Mitsuo</au><au>Ishikawa, Kiyofumi</au><au>Ikemoto, Fumihiko</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Antihypertensive effect of a newly synthesized endothelin antagonist, BQ-123, in a genetic hypertensive model</atitle><jtitle>Life sciences (1973)</jtitle><addtitle>Life Sci</addtitle><date>1993</date><risdate>1993</risdate><volume>52</volume><issue>8</issue><spage>717</spage><epage>724</epage><pages>717-724</pages><issn>0024-3205</issn><eissn>1879-0631</eissn><coden>LIFSAK</coden><abstract>A newly synthesized ET
A-selective antagonist, BQ-123, was examined with respect to its anti-endothelin(ET) action in vitro and in vivo and its effect on blood pressure in Wistar Kyoto rats (WKY), spontaneously hypertensive rats (SHR) and stroke-prone spontaneously hypertensive rats (SHRSP). In isolated porcine coronary arteries, BQ-123 (0.07 μM to 6.0 μM) shifted the concentration-response curve for ET-1 to the right without affecting the maximal response of ET-1, its pA
2 value being 7.35. Intravenous infusion of BQ-123 at a rate of 1.2 and 30 mg/kg/hr produced a significant decrease in blood pressure in 20- to 29-week-old SHRSP, but did not alter blood pressure in 13- to 16-week-old WKY or in 18- to 19-week-old and 40-week-old SHR. The hypotensive effect of BQ-123 depended on the pretreatment blood pressure level. These results suggest that ET-1 is involved in part in the maintenance of high blood pressure in malignant hypertension, as exemplified by SHRSP.</abstract><cop>Amsterdam</cop><pub>Elsevier Inc</pub><pmid>8446001</pmid><doi>10.1016/0024-3205(93)90233-S</doi><tpages>8</tpages></addata></record> |
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| ispartof | Life sciences (1973), 1993, Vol.52 (8), p.717-724 |
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| language | eng |
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| subjects | Amino Acid Sequence Analysis of Variance Animals Antihypertensive agents Antihypertensive Agents - pharmacology Biological and medical sciences Cardiovascular system Endothelins - antagonists & inhibitors Endothelium, Vascular - drug effects Hypertension - drug therapy Hypertension - genetics In Vitro Techniques Male Medical sciences Models, Genetic Molecular Sequence Data Peptides, Cyclic - pharmacology Pharmacology. Drug treatments Rats Rats, Inbred SHR Rats, Inbred WKY Swine |
| title | Antihypertensive effect of a newly synthesized endothelin antagonist, BQ-123, in a genetic hypertensive model |
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