Differences in the effects of ketanserin and GR127935 on 5-HT-receptor mediated responses in rabbit saphenous vein and guinea-pig jugular vein
Ketanserin has higher affinity for 5-HT 1Dα receptors compared to 5-HT 1Dβ receptors, whereas, GR127935 ( N-[4-methoxy-3-(4-methyl-1-mpiperazinyl)phenyl]-2(methyl-4(-(5-methyl-1,2,4-oxadiazol-3-yl)[1,1-biphenyl]-4-carboxamide), a novel and selective 5-HT 1D receptor antagonist, has higher affinity f...
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| Veröffentlicht in: | European journal of pharmacology 1995-09, Vol.283 (1), p.199-206 |
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| creator | Razzaque, Zerin Longmore, Jeanette Hill, Raymond G. |
| description | Ketanserin has higher affinity for 5-HT
1Dα receptors compared to 5-HT
1Dβ receptors, whereas, GR127935 (
N-[4-methoxy-3-(4-methyl-1-mpiperazinyl)phenyl]-2(methyl-4(-(5-methyl-1,2,4-oxadiazol-3-yl)[1,1-biphenyl]-4-carboxamide), a novel and selective 5-HT
1D receptor antagonist, has higher affinity for 5-HT
1Dβ receptors compared to 5-HT
1Dα receptors. In the present study, we compared the effects of ketanserin and GR127935 on sumatriptan-induced responses of rabbit saphenous vein and guinea-pig jugular vein. In rabbit saphenous vein, contractile responses elicited by sumatriptan were antagonised by ketanserin (pA
2 = 6.76) and GR127935 (apparent pA
2 = 9.4). In guinea-pig jugular vein, concentration-dependent relaxations evoked by sumatriptan were antagonised by ketanserin and GR127935 (apparent pA
2 = 5.9 and 10, respectively). Ketanserin but not GR127935, inhibited Ca
2+-induced contraction of depolarised strips of guinea-pig ileum longitudinal muscle/myenteric plexus, however, in rabbit saphenous vein and guinea-pig jugular vein, 5-HT receptor mediated responses were insensitive to nifedipine (Ca
2+ channel blocker), eliminating the possibility that the inhibitory effects of ketanserin and GR127935 were due to the blockade of voltage-operated Ca
2+ channels. Thus, antagonism by ketanserin and GR127935 confirms the presence of 5-HT
1D receptors in rabbit saphenous vein and guinea-pig jugular vein. The differential effects of ketanserin and GR127935 on responses elicited by sumatriptan in rabbit saphenous vein and guinea-pig jugular vein may reflect either species differences in 5-HT
1D receptors or the involvement of 5-HT
1Dα and 5-HT
1Dβ receptor subtypes. |
| doi_str_mv | 10.1016/0014-2999(95)00349-P |
| format | Article |
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1Dα receptors compared to 5-HT
1Dβ receptors, whereas, GR127935 (
N-[4-methoxy-3-(4-methyl-1-mpiperazinyl)phenyl]-2(methyl-4(-(5-methyl-1,2,4-oxadiazol-3-yl)[1,1-biphenyl]-4-carboxamide), a novel and selective 5-HT
1D receptor antagonist, has higher affinity for 5-HT
1Dβ receptors compared to 5-HT
1Dα receptors. In the present study, we compared the effects of ketanserin and GR127935 on sumatriptan-induced responses of rabbit saphenous vein and guinea-pig jugular vein. In rabbit saphenous vein, contractile responses elicited by sumatriptan were antagonised by ketanserin (pA
2 = 6.76) and GR127935 (apparent pA
2 = 9.4). In guinea-pig jugular vein, concentration-dependent relaxations evoked by sumatriptan were antagonised by ketanserin and GR127935 (apparent pA
2 = 5.9 and 10, respectively). Ketanserin but not GR127935, inhibited Ca
2+-induced contraction of depolarised strips of guinea-pig ileum longitudinal muscle/myenteric plexus, however, in rabbit saphenous vein and guinea-pig jugular vein, 5-HT receptor mediated responses were insensitive to nifedipine (Ca
2+ channel blocker), eliminating the possibility that the inhibitory effects of ketanserin and GR127935 were due to the blockade of voltage-operated Ca
2+ channels. Thus, antagonism by ketanserin and GR127935 confirms the presence of 5-HT
1D receptors in rabbit saphenous vein and guinea-pig jugular vein. The differential effects of ketanserin and GR127935 on responses elicited by sumatriptan in rabbit saphenous vein and guinea-pig jugular vein may reflect either species differences in 5-HT
1D receptors or the involvement of 5-HT
1Dα and 5-HT
1Dβ receptor subtypes.</description><identifier>ISSN: 0014-2999</identifier><identifier>EISSN: 1879-0712</identifier><identifier>DOI: 10.1016/0014-2999(95)00349-P</identifier><identifier>PMID: 7498311</identifier><language>eng</language><publisher>Netherlands: Elsevier B.V</publisher><subject>5-HT 1D receptor ; Animals ; Dose-Response Relationship, Drug ; GR127935 ; Guinea Pigs ; Jugular vein, guinea-pig ; Jugular Veins - drug effects ; Ketanserin ; Ketanserin - pharmacology ; Male ; Myenteric Plexus - drug effects ; Nifedipine - pharmacology ; Oxadiazoles - pharmacology ; Piperazines - pharmacology ; Rabbits ; Saphenous Vein - drug effects ; Saphenous vein, rabbit ; Serotonin - pharmacology ; Serotonin Antagonists - pharmacology ; Sumatriptan - pharmacology</subject><ispartof>European journal of pharmacology, 1995-09, Vol.283 (1), p.199-206</ispartof><rights>1995</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c357t-59af43187e1fdb35ee363d2fe5491775f825c87c48a351969257d61d1489f96d3</citedby><cites>FETCH-LOGICAL-c357t-59af43187e1fdb35ee363d2fe5491775f825c87c48a351969257d61d1489f96d3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://www.sciencedirect.com/science/article/pii/001429999500349P$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,776,780,3537,27901,27902,65306</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/7498311$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Razzaque, Zerin</creatorcontrib><creatorcontrib>Longmore, Jeanette</creatorcontrib><creatorcontrib>Hill, Raymond G.</creatorcontrib><title>Differences in the effects of ketanserin and GR127935 on 5-HT-receptor mediated responses in rabbit saphenous vein and guinea-pig jugular vein</title><title>European journal of pharmacology</title><addtitle>Eur J Pharmacol</addtitle><description>Ketanserin has higher affinity for 5-HT
1Dα receptors compared to 5-HT
1Dβ receptors, whereas, GR127935 (
N-[4-methoxy-3-(4-methyl-1-mpiperazinyl)phenyl]-2(methyl-4(-(5-methyl-1,2,4-oxadiazol-3-yl)[1,1-biphenyl]-4-carboxamide), a novel and selective 5-HT
1D receptor antagonist, has higher affinity for 5-HT
1Dβ receptors compared to 5-HT
1Dα receptors. In the present study, we compared the effects of ketanserin and GR127935 on sumatriptan-induced responses of rabbit saphenous vein and guinea-pig jugular vein. In rabbit saphenous vein, contractile responses elicited by sumatriptan were antagonised by ketanserin (pA
2 = 6.76) and GR127935 (apparent pA
2 = 9.4). In guinea-pig jugular vein, concentration-dependent relaxations evoked by sumatriptan were antagonised by ketanserin and GR127935 (apparent pA
2 = 5.9 and 10, respectively). Ketanserin but not GR127935, inhibited Ca
2+-induced contraction of depolarised strips of guinea-pig ileum longitudinal muscle/myenteric plexus, however, in rabbit saphenous vein and guinea-pig jugular vein, 5-HT receptor mediated responses were insensitive to nifedipine (Ca
2+ channel blocker), eliminating the possibility that the inhibitory effects of ketanserin and GR127935 were due to the blockade of voltage-operated Ca
2+ channels. Thus, antagonism by ketanserin and GR127935 confirms the presence of 5-HT
1D receptors in rabbit saphenous vein and guinea-pig jugular vein. The differential effects of ketanserin and GR127935 on responses elicited by sumatriptan in rabbit saphenous vein and guinea-pig jugular vein may reflect either species differences in 5-HT
1D receptors or the involvement of 5-HT
1Dα and 5-HT
1Dβ receptor subtypes.</description><subject>5-HT 1D receptor</subject><subject>Animals</subject><subject>Dose-Response Relationship, Drug</subject><subject>GR127935</subject><subject>Guinea Pigs</subject><subject>Jugular vein, guinea-pig</subject><subject>Jugular Veins - drug effects</subject><subject>Ketanserin</subject><subject>Ketanserin - pharmacology</subject><subject>Male</subject><subject>Myenteric Plexus - drug effects</subject><subject>Nifedipine - pharmacology</subject><subject>Oxadiazoles - pharmacology</subject><subject>Piperazines - pharmacology</subject><subject>Rabbits</subject><subject>Saphenous Vein - drug effects</subject><subject>Saphenous vein, rabbit</subject><subject>Serotonin - pharmacology</subject><subject>Serotonin Antagonists - pharmacology</subject><subject>Sumatriptan - pharmacology</subject><issn>0014-2999</issn><issn>1879-0712</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1995</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9UctOJCEUJWaMto8_0ITVxFmgUBRFsTExOuokJhqja0LDpUW7q0qgTPwJv1n6EZezIuE84JyD0BGjp4yy5oxSVpNKKXWixB9Kea3IwxaasFYqQiWrfqHJD2UX7aX0SikVqhI7aEfWquWMTdDXVfAeInQWEg4dzi-AodzYnHDv8Rtk0yWIBTGdwzePrJKKC9x3WJDbJxLBwpD7iBfggsngcIQ09EWycotmOg0ZJzO8QNePCX_Axmk2hg4MGcIMv46zcW7iCjtA297MExxuzn30fP336fKW3N3f_Lu8uCOWC5mJUMbXvCQF5t2UCwDecFd5ELViUgrfVsK20tat4YKppoSWrmGO1a3yqnF8H_1e-w6xfx8hZb0IycJ8bjoo_9RSNkoKSQuxXhNt7FOK4PUQw8LET82oXs6glx3rZcdaCb2aQT8U2fHGf5yWan5Em94Lfr7GoYT8CBB1smE5ggul0qxdH_7_wDdEiJb6</recordid><startdate>19950905</startdate><enddate>19950905</enddate><creator>Razzaque, Zerin</creator><creator>Longmore, Jeanette</creator><creator>Hill, Raymond G.</creator><general>Elsevier B.V</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>19950905</creationdate><title>Differences in the effects of ketanserin and GR127935 on 5-HT-receptor mediated responses in rabbit saphenous vein and guinea-pig jugular vein</title><author>Razzaque, Zerin ; Longmore, Jeanette ; Hill, Raymond G.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c357t-59af43187e1fdb35ee363d2fe5491775f825c87c48a351969257d61d1489f96d3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1995</creationdate><topic>5-HT 1D receptor</topic><topic>Animals</topic><topic>Dose-Response Relationship, Drug</topic><topic>GR127935</topic><topic>Guinea Pigs</topic><topic>Jugular vein, guinea-pig</topic><topic>Jugular Veins - drug effects</topic><topic>Ketanserin</topic><topic>Ketanserin - pharmacology</topic><topic>Male</topic><topic>Myenteric Plexus - drug effects</topic><topic>Nifedipine - pharmacology</topic><topic>Oxadiazoles - pharmacology</topic><topic>Piperazines - pharmacology</topic><topic>Rabbits</topic><topic>Saphenous Vein - drug effects</topic><topic>Saphenous vein, rabbit</topic><topic>Serotonin - pharmacology</topic><topic>Serotonin Antagonists - pharmacology</topic><topic>Sumatriptan - pharmacology</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Razzaque, Zerin</creatorcontrib><creatorcontrib>Longmore, Jeanette</creatorcontrib><creatorcontrib>Hill, Raymond G.</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>European journal of pharmacology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Razzaque, Zerin</au><au>Longmore, Jeanette</au><au>Hill, Raymond G.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Differences in the effects of ketanserin and GR127935 on 5-HT-receptor mediated responses in rabbit saphenous vein and guinea-pig jugular vein</atitle><jtitle>European journal of pharmacology</jtitle><addtitle>Eur J Pharmacol</addtitle><date>1995-09-05</date><risdate>1995</risdate><volume>283</volume><issue>1</issue><spage>199</spage><epage>206</epage><pages>199-206</pages><issn>0014-2999</issn><eissn>1879-0712</eissn><abstract>Ketanserin has higher affinity for 5-HT
1Dα receptors compared to 5-HT
1Dβ receptors, whereas, GR127935 (
N-[4-methoxy-3-(4-methyl-1-mpiperazinyl)phenyl]-2(methyl-4(-(5-methyl-1,2,4-oxadiazol-3-yl)[1,1-biphenyl]-4-carboxamide), a novel and selective 5-HT
1D receptor antagonist, has higher affinity for 5-HT
1Dβ receptors compared to 5-HT
1Dα receptors. In the present study, we compared the effects of ketanserin and GR127935 on sumatriptan-induced responses of rabbit saphenous vein and guinea-pig jugular vein. In rabbit saphenous vein, contractile responses elicited by sumatriptan were antagonised by ketanserin (pA
2 = 6.76) and GR127935 (apparent pA
2 = 9.4). In guinea-pig jugular vein, concentration-dependent relaxations evoked by sumatriptan were antagonised by ketanserin and GR127935 (apparent pA
2 = 5.9 and 10, respectively). Ketanserin but not GR127935, inhibited Ca
2+-induced contraction of depolarised strips of guinea-pig ileum longitudinal muscle/myenteric plexus, however, in rabbit saphenous vein and guinea-pig jugular vein, 5-HT receptor mediated responses were insensitive to nifedipine (Ca
2+ channel blocker), eliminating the possibility that the inhibitory effects of ketanserin and GR127935 were due to the blockade of voltage-operated Ca
2+ channels. Thus, antagonism by ketanserin and GR127935 confirms the presence of 5-HT
1D receptors in rabbit saphenous vein and guinea-pig jugular vein. The differential effects of ketanserin and GR127935 on responses elicited by sumatriptan in rabbit saphenous vein and guinea-pig jugular vein may reflect either species differences in 5-HT
1D receptors or the involvement of 5-HT
1Dα and 5-HT
1Dβ receptor subtypes.</abstract><cop>Netherlands</cop><pub>Elsevier B.V</pub><pmid>7498311</pmid><doi>10.1016/0014-2999(95)00349-P</doi><tpages>8</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0014-2999 |
| ispartof | European journal of pharmacology, 1995-09, Vol.283 (1), p.199-206 |
| issn | 0014-2999 1879-0712 |
| language | eng |
| recordid | cdi_proquest_miscellaneous_77697570 |
| source | MEDLINE; ScienceDirect Journals (5 years ago - present) |
| subjects | 5-HT 1D receptor Animals Dose-Response Relationship, Drug GR127935 Guinea Pigs Jugular vein, guinea-pig Jugular Veins - drug effects Ketanserin Ketanserin - pharmacology Male Myenteric Plexus - drug effects Nifedipine - pharmacology Oxadiazoles - pharmacology Piperazines - pharmacology Rabbits Saphenous Vein - drug effects Saphenous vein, rabbit Serotonin - pharmacology Serotonin Antagonists - pharmacology Sumatriptan - pharmacology |
| title | Differences in the effects of ketanserin and GR127935 on 5-HT-receptor mediated responses in rabbit saphenous vein and guinea-pig jugular vein |
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