Pharmacological studies on EB-382, a new non-steroidal antiinflammatory agents: mode of action of the analgesic effects
The analgesic mechanism of (+/-)-2-[p-[(2-methylallyl)amino]phenyl]propionic acid (EB-382), a new non-steroidal antiinflammatory agent, was studied. EB-382 exerted a potent analgesic effect on yeast-induced hyperalgesia in rats and bradykinin-induced writhing in mice, and its potency was superior to...
Gespeichert in:
| Veröffentlicht in: | Chemical & pharmaceutical bulletin 1989, Vol.37 (3), p.775-777 |
|---|---|
| Hauptverfasser: | , , , , |
| Format: | Artikel |
| Sprache: | eng |
| Schlagworte: | |
| Online-Zugang: | Volltext |
| Tags: |
Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
|
| container_end_page | 777 |
|---|---|
| container_issue | 3 |
| container_start_page | 775 |
| container_title | Chemical & pharmaceutical bulletin |
| container_volume | 37 |
| creator | FUJIYOSHI, T IIDA, H MURAKAMI, M KUWASHIMA, M UEMATSU, T |
| description | The analgesic mechanism of (+/-)-2-[p-[(2-methylallyl)amino]phenyl]propionic acid (EB-382), a new non-steroidal antiinflammatory agent, was studied. EB-382 exerted a potent analgesic effect on yeast-induced hyperalgesia in rats and bradykinin-induced writhing in mice, and its potency was superior to that of ibuprofen. EB-382 had a comparatively weak inhibitory effect on the prostaglandin E2 production from arachidonic acid in sheep seminal vesicle microsomal fraction in vitro. EB-382 exhibited a dose-dependent inhibitory effect on the phospholipase A2 activity in 3T3 mouse fibroblast cells with a different mechanism from steroidal agents, although indomethacin and ibuprofen did not reveal any significant inhibition. EB-382 did not affect the bradykinin-induced contraction of isolated rat uterus. Intracisternal injection of EB-382 did not affect the acetic acid-induced writhing response in mice. From these results, it is suggested that the analgesic effect of EB-382 in inflammation is exerted through its direct peripheral action, and inhibition of prostaglandin biosynthesis via phospholipase A2, rather than cyclooxygenase. |
| doi_str_mv | 10.1248/cpb.37.775 |
| format | Article |
| fullrecord | <record><control><sourceid>proquest_cross</sourceid><recordid>TN_cdi_proquest_miscellaneous_79102768</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>15284232</sourcerecordid><originalsourceid>FETCH-LOGICAL-c546t-374827bd541a37af207131e195bedae4d676c12523a4ef5dd88f6105a25afad93</originalsourceid><addsrcrecordid>eNqFkU2LFDEQhoMo6-zqxbuQix7EHvPR6er2psuuCgt60HNTk1RmI93JmGRY9t8b2UGPnqrgfXig6mXshRRbqfrxnT3sthq2AOYR20jdQ2eU0o_ZRggxdUoP-ik7L-WnEMoI0GfsTMEIIMyG3X27xbyiTUvaB4sLL_XoAhWeIr_62OlRveXII93xmGJXKuUUXMMw1hCiX3BdsaZ8z3FPsZb3fE2OePIcbQ3N0bZ6Sw3HZU8lWE7ek63lGXvicSn0_DQv2I_rq--Xn7ubr5--XH646azph9pp6EcFO2d6iRrQKwFSS5KT2ZFD6t0Ag5XKKI09eePcOPpBCoPKoEc36Qv2-sF7yOnXkUqd11AsLQtGSscywySFgmH8LyiNGnulVQPfPIA2p1Iy-fmQw4r5fpZi_lPH3OqYNcytjga_PFmPu5XcX_T0_5a_OuVY2vd9xmhD-WecBmina_0bsyWSow</addsrcrecordid><sourcetype>Aggregation Database</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype><pqid>15284232</pqid></control><display><type>article</type><title>Pharmacological studies on EB-382, a new non-steroidal antiinflammatory agents: mode of action of the analgesic effects</title><source>MEDLINE</source><source>J-STAGE (Japan Science & Technology Information Aggregator, Electronic) Freely Available Titles - Japanese</source><source>EZB-FREE-00999 freely available EZB journals</source><source>Free Full-Text Journals in Chemistry</source><creator>FUJIYOSHI, T ; IIDA, H ; MURAKAMI, M ; KUWASHIMA, M ; UEMATSU, T</creator><creatorcontrib>FUJIYOSHI, T ; IIDA, H ; MURAKAMI, M ; KUWASHIMA, M ; UEMATSU, T</creatorcontrib><description>The analgesic mechanism of (+/-)-2-[p-[(2-methylallyl)amino]phenyl]propionic acid (EB-382), a new non-steroidal antiinflammatory agent, was studied. EB-382 exerted a potent analgesic effect on yeast-induced hyperalgesia in rats and bradykinin-induced writhing in mice, and its potency was superior to that of ibuprofen. EB-382 had a comparatively weak inhibitory effect on the prostaglandin E2 production from arachidonic acid in sheep seminal vesicle microsomal fraction in vitro. EB-382 exhibited a dose-dependent inhibitory effect on the phospholipase A2 activity in 3T3 mouse fibroblast cells with a different mechanism from steroidal agents, although indomethacin and ibuprofen did not reveal any significant inhibition. EB-382 did not affect the bradykinin-induced contraction of isolated rat uterus. Intracisternal injection of EB-382 did not affect the acetic acid-induced writhing response in mice. From these results, it is suggested that the analgesic effect of EB-382 in inflammation is exerted through its direct peripheral action, and inhibition of prostaglandin biosynthesis via phospholipase A2, rather than cyclooxygenase.</description><identifier>ISSN: 0009-2363</identifier><identifier>EISSN: 1347-5223</identifier><identifier>DOI: 10.1248/cpb.37.775</identifier><identifier>PMID: 2787705</identifier><identifier>CODEN: CPBTAL</identifier><language>eng</language><publisher>Tokyo: Maruzen</publisher><subject>Animals ; Anti-Inflammatory Agents, Non-Steroidal - pharmacology ; Biological and medical sciences ; Bones, joints and connective tissue. Antiinflammatory agents ; Female ; ibuprofen ; Male ; Medical sciences ; Mice ; Mice, Inbred Strains ; pain ; Pharmacology. Drug treatments ; Propionates - pharmacology ; Rats ; Rats, Inbred Strains ; Sheep</subject><ispartof>Chemical & pharmaceutical bulletin, 1989, Vol.37 (3), p.775-777</ispartof><rights>1991 INIST-CNRS</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c546t-374827bd541a37af207131e195bedae4d676c12523a4ef5dd88f6105a25afad93</citedby></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,4022,27922,27923,27924</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=19675413$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/2787705$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>FUJIYOSHI, T</creatorcontrib><creatorcontrib>IIDA, H</creatorcontrib><creatorcontrib>MURAKAMI, M</creatorcontrib><creatorcontrib>KUWASHIMA, M</creatorcontrib><creatorcontrib>UEMATSU, T</creatorcontrib><title>Pharmacological studies on EB-382, a new non-steroidal antiinflammatory agents: mode of action of the analgesic effects</title><title>Chemical & pharmaceutical bulletin</title><addtitle>Chem Pharm Bull (Tokyo)</addtitle><description>The analgesic mechanism of (+/-)-2-[p-[(2-methylallyl)amino]phenyl]propionic acid (EB-382), a new non-steroidal antiinflammatory agent, was studied. EB-382 exerted a potent analgesic effect on yeast-induced hyperalgesia in rats and bradykinin-induced writhing in mice, and its potency was superior to that of ibuprofen. EB-382 had a comparatively weak inhibitory effect on the prostaglandin E2 production from arachidonic acid in sheep seminal vesicle microsomal fraction in vitro. EB-382 exhibited a dose-dependent inhibitory effect on the phospholipase A2 activity in 3T3 mouse fibroblast cells with a different mechanism from steroidal agents, although indomethacin and ibuprofen did not reveal any significant inhibition. EB-382 did not affect the bradykinin-induced contraction of isolated rat uterus. Intracisternal injection of EB-382 did not affect the acetic acid-induced writhing response in mice. From these results, it is suggested that the analgesic effect of EB-382 in inflammation is exerted through its direct peripheral action, and inhibition of prostaglandin biosynthesis via phospholipase A2, rather than cyclooxygenase.</description><subject>Animals</subject><subject>Anti-Inflammatory Agents, Non-Steroidal - pharmacology</subject><subject>Biological and medical sciences</subject><subject>Bones, joints and connective tissue. Antiinflammatory agents</subject><subject>Female</subject><subject>ibuprofen</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Mice</subject><subject>Mice, Inbred Strains</subject><subject>pain</subject><subject>Pharmacology. Drug treatments</subject><subject>Propionates - pharmacology</subject><subject>Rats</subject><subject>Rats, Inbred Strains</subject><subject>Sheep</subject><issn>0009-2363</issn><issn>1347-5223</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1989</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkU2LFDEQhoMo6-zqxbuQix7EHvPR6er2psuuCgt60HNTk1RmI93JmGRY9t8b2UGPnqrgfXig6mXshRRbqfrxnT3sthq2AOYR20jdQ2eU0o_ZRggxdUoP-ik7L-WnEMoI0GfsTMEIIMyG3X27xbyiTUvaB4sLL_XoAhWeIr_62OlRveXII93xmGJXKuUUXMMw1hCiX3BdsaZ8z3FPsZb3fE2OePIcbQ3N0bZ6Sw3HZU8lWE7ek63lGXvicSn0_DQv2I_rq--Xn7ubr5--XH646azph9pp6EcFO2d6iRrQKwFSS5KT2ZFD6t0Ag5XKKI09eePcOPpBCoPKoEc36Qv2-sF7yOnXkUqd11AsLQtGSscywySFgmH8LyiNGnulVQPfPIA2p1Iy-fmQw4r5fpZi_lPH3OqYNcytjga_PFmPu5XcX_T0_5a_OuVY2vd9xmhD-WecBmina_0bsyWSow</recordid><startdate>1989</startdate><enddate>1989</enddate><creator>FUJIYOSHI, T</creator><creator>IIDA, H</creator><creator>MURAKAMI, M</creator><creator>KUWASHIMA, M</creator><creator>UEMATSU, T</creator><general>Maruzen</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>8FD</scope><scope>FR3</scope><scope>M7Z</scope><scope>P64</scope><scope>7X8</scope></search><sort><creationdate>1989</creationdate><title>Pharmacological studies on EB-382, a new non-steroidal antiinflammatory agents: mode of action of the analgesic effects</title><author>FUJIYOSHI, T ; IIDA, H ; MURAKAMI, M ; KUWASHIMA, M ; UEMATSU, T</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c546t-374827bd541a37af207131e195bedae4d676c12523a4ef5dd88f6105a25afad93</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1989</creationdate><topic>Animals</topic><topic>Anti-Inflammatory Agents, Non-Steroidal - pharmacology</topic><topic>Biological and medical sciences</topic><topic>Bones, joints and connective tissue. Antiinflammatory agents</topic><topic>Female</topic><topic>ibuprofen</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Mice</topic><topic>Mice, Inbred Strains</topic><topic>pain</topic><topic>Pharmacology. Drug treatments</topic><topic>Propionates - pharmacology</topic><topic>Rats</topic><topic>Rats, Inbred Strains</topic><topic>Sheep</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>FUJIYOSHI, T</creatorcontrib><creatorcontrib>IIDA, H</creatorcontrib><creatorcontrib>MURAKAMI, M</creatorcontrib><creatorcontrib>KUWASHIMA, M</creatorcontrib><creatorcontrib>UEMATSU, T</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>Technology Research Database</collection><collection>Engineering Research Database</collection><collection>Biochemistry Abstracts 1</collection><collection>Biotechnology and BioEngineering Abstracts</collection><collection>MEDLINE - Academic</collection><jtitle>Chemical & pharmaceutical bulletin</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>FUJIYOSHI, T</au><au>IIDA, H</au><au>MURAKAMI, M</au><au>KUWASHIMA, M</au><au>UEMATSU, T</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Pharmacological studies on EB-382, a new non-steroidal antiinflammatory agents: mode of action of the analgesic effects</atitle><jtitle>Chemical & pharmaceutical bulletin</jtitle><addtitle>Chem Pharm Bull (Tokyo)</addtitle><date>1989</date><risdate>1989</risdate><volume>37</volume><issue>3</issue><spage>775</spage><epage>777</epage><pages>775-777</pages><issn>0009-2363</issn><eissn>1347-5223</eissn><coden>CPBTAL</coden><abstract>The analgesic mechanism of (+/-)-2-[p-[(2-methylallyl)amino]phenyl]propionic acid (EB-382), a new non-steroidal antiinflammatory agent, was studied. EB-382 exerted a potent analgesic effect on yeast-induced hyperalgesia in rats and bradykinin-induced writhing in mice, and its potency was superior to that of ibuprofen. EB-382 had a comparatively weak inhibitory effect on the prostaglandin E2 production from arachidonic acid in sheep seminal vesicle microsomal fraction in vitro. EB-382 exhibited a dose-dependent inhibitory effect on the phospholipase A2 activity in 3T3 mouse fibroblast cells with a different mechanism from steroidal agents, although indomethacin and ibuprofen did not reveal any significant inhibition. EB-382 did not affect the bradykinin-induced contraction of isolated rat uterus. Intracisternal injection of EB-382 did not affect the acetic acid-induced writhing response in mice. From these results, it is suggested that the analgesic effect of EB-382 in inflammation is exerted through its direct peripheral action, and inhibition of prostaglandin biosynthesis via phospholipase A2, rather than cyclooxygenase.</abstract><cop>Tokyo</cop><pub>Maruzen</pub><pmid>2787705</pmid><doi>10.1248/cpb.37.775</doi><tpages>3</tpages><oa>free_for_read</oa></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0009-2363 |
| ispartof | Chemical & pharmaceutical bulletin, 1989, Vol.37 (3), p.775-777 |
| issn | 0009-2363 1347-5223 |
| language | eng |
| recordid | cdi_proquest_miscellaneous_79102768 |
| source | MEDLINE; J-STAGE (Japan Science & Technology Information Aggregator, Electronic) Freely Available Titles - Japanese; EZB-FREE-00999 freely available EZB journals; Free Full-Text Journals in Chemistry |
| subjects | Animals Anti-Inflammatory Agents, Non-Steroidal - pharmacology Biological and medical sciences Bones, joints and connective tissue. Antiinflammatory agents Female ibuprofen Male Medical sciences Mice Mice, Inbred Strains pain Pharmacology. Drug treatments Propionates - pharmacology Rats Rats, Inbred Strains Sheep |
| title | Pharmacological studies on EB-382, a new non-steroidal antiinflammatory agents: mode of action of the analgesic effects |
| url | https://sfx.bib-bvb.de/sfx_tum?ctx_ver=Z39.88-2004&ctx_enc=info:ofi/enc:UTF-8&ctx_tim=2025-01-11T08%3A23%3A01IST&url_ver=Z39.88-2004&url_ctx_fmt=infofi/fmt:kev:mtx:ctx&rfr_id=info:sid/primo.exlibrisgroup.com:primo3-Article-proquest_cross&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.genre=article&rft.atitle=Pharmacological%20studies%20on%20EB-382,%20a%20new%20non-steroidal%20antiinflammatory%20agents:%20mode%20of%20action%20of%20the%20analgesic%20effects&rft.jtitle=Chemical%20&%20pharmaceutical%20bulletin&rft.au=FUJIYOSHI,%20T&rft.date=1989&rft.volume=37&rft.issue=3&rft.spage=775&rft.epage=777&rft.pages=775-777&rft.issn=0009-2363&rft.eissn=1347-5223&rft.coden=CPBTAL&rft_id=info:doi/10.1248/cpb.37.775&rft_dat=%3Cproquest_cross%3E15284232%3C/proquest_cross%3E%3Curl%3E%3C/url%3E&disable_directlink=true&sfx.directlink=off&sfx.report_link=0&rft_id=info:oai/&rft_pqid=15284232&rft_id=info:pmid/2787705&rfr_iscdi=true |