Pharmacological study of Mequitazine (LM-209) (I) Antagonistic actions of chemical mediators
Antagonistic activities of Mequitazine (LM-209) on chemical mediators and in particular histamine were investigated in guinea-pigs, mice and rats. The antagonistic activity of LM-209 for histamine in the isolated ileum and trachea of guinea-pigs was less potent than that for clemastine fumarate (CL)...
Gespeichert in:
| Veröffentlicht in: | Folia Pharmacologica Japonica 1981, Vol.78(4), pp.279-289 |
|---|---|
| Hauptverfasser: | , , , , , , , |
| Format: | Artikel |
| Sprache: | jpn |
| Schlagworte: | |
| Online-Zugang: | Volltext |
| Tags: |
Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
|
| container_end_page | 289 |
|---|---|
| container_issue | 4 |
| container_start_page | 279 |
| container_title | Folia Pharmacologica Japonica |
| container_volume | 78 |
| creator | FUJIMURA, Hajime TSURUMI, Kaito YANAGIHARA, Masayoshi HIRAMATSU, Yasuzo TAMURA, Yohei SHIMIZU, Yoan HOJO, Masakazu YOSHIDA, Yoichi |
| description | Antagonistic activities of Mequitazine (LM-209) on chemical mediators and in particular histamine were investigated in guinea-pigs, mice and rats. The antagonistic activity of LM-209 for histamine in the isolated ileum and trachea of guinea-pigs was less potent than that for clemastine fumarate (CL) and chlorpheniramine maleate (CPM) while that for acetylcholine was more potent than CL and CPM. Moreover, the antagonistic activities of these three compounds on serotonin and bradykinin were almost equipotent in the excised ileum. Using a modified Konzett-Rössler method, the bronchodilating effect of LM-209 (p.o.) for histamine was same as CL, but that for acetylcholine was more potent than CL and CPM. The protective activity of LM-209 (p.o.) on acute death induced by histamine and metacholine in mice was the same as CL, but the duration of the anti-histaminic action was markedly longer than CL. LM-209 given orally inhibited markedly the increased vascular permeability by histamine in rats and the diarrhea by 5-HTP in mice, but did not affect on the histamine-induced ulcer in guinea-pigs. From these results, LM-209 appears to have the potent and long acting antagonistic activity on various chemical mediators. |
| doi_str_mv | 10.1254/fpj.78.279 |
| format | Article |
| fullrecord | <record><control><sourceid>pubmed_jstag</sourceid><recordid>TN_cdi_pubmed_primary_6120126</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>6120126</sourcerecordid><originalsourceid>FETCH-LOGICAL-c222t-88889b54bd0b89cbd8f1c2a841fc03c634fec07589d8d673891731f34b6dd8c63</originalsourceid><addsrcrecordid>eNo9kElPAkEQhTtGgwS5eDeZIxwGe5tejoS4kED0oDeTSW8DTWbB6eaAv95WCHWoOnypV_UeAPcIzhAu6GO13824mGEur8AQEcpzQSS_BkMIUZEXTKJbMA7BawgLjjkjaAAGDGGIMBuCr_et6htlurrbeKPqLMSDPWZdla3d98FH9eNbl01W6xxDOc0my2k2b6PadK0P0ZtMmei7NvwtmK1r_iUaZ72KXR_uwE2l6uDG5zkCn89PH4vXfPX2slzMV7nBGMdcpJK6oNpCLaTRVlTIYCUoqgwkhhFaOQN5IaQVlnEiJOIEVYRqZq1IfAQeTrr7g07Hy33vG9Ufy7PLxBcnvgvpdXfhqk8WalemCJGktOSiPLeU5oWalFDpWvILAT9rUw</addsrcrecordid><sourcetype>Index Database</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype></control><display><type>article</type><title>Pharmacological study of Mequitazine (LM-209) (I) Antagonistic actions of chemical mediators</title><source>MEDLINE</source><source>Elektronische Zeitschriftenbibliothek - Frei zugängliche E-Journals</source><creator>FUJIMURA, Hajime ; TSURUMI, Kaito ; YANAGIHARA, Masayoshi ; HIRAMATSU, Yasuzo ; TAMURA, Yohei ; SHIMIZU, Yoan ; HOJO, Masakazu ; YOSHIDA, Yoichi</creator><creatorcontrib>FUJIMURA, Hajime ; TSURUMI, Kaito ; YANAGIHARA, Masayoshi ; HIRAMATSU, Yasuzo ; TAMURA, Yohei ; SHIMIZU, Yoan ; HOJO, Masakazu ; YOSHIDA, Yoichi</creatorcontrib><description>Antagonistic activities of Mequitazine (LM-209) on chemical mediators and in particular histamine were investigated in guinea-pigs, mice and rats. The antagonistic activity of LM-209 for histamine in the isolated ileum and trachea of guinea-pigs was less potent than that for clemastine fumarate (CL) and chlorpheniramine maleate (CPM) while that for acetylcholine was more potent than CL and CPM. Moreover, the antagonistic activities of these three compounds on serotonin and bradykinin were almost equipotent in the excised ileum. Using a modified Konzett-Rössler method, the bronchodilating effect of LM-209 (p.o.) for histamine was same as CL, but that for acetylcholine was more potent than CL and CPM. The protective activity of LM-209 (p.o.) on acute death induced by histamine and metacholine in mice was the same as CL, but the duration of the anti-histaminic action was markedly longer than CL. LM-209 given orally inhibited markedly the increased vascular permeability by histamine in rats and the diarrhea by 5-HTP in mice, but did not affect on the histamine-induced ulcer in guinea-pigs. From these results, LM-209 appears to have the potent and long acting antagonistic activity on various chemical mediators.</description><identifier>ISSN: 0015-5691</identifier><identifier>EISSN: 1347-8397</identifier><identifier>DOI: 10.1254/fpj.78.279</identifier><identifier>PMID: 6120126</identifier><language>jpn</language><publisher>Japan: The Japanese Pharmacological Society</publisher><subject>Acetylcholine - antagonists & inhibitors ; Airway Resistance - drug effects ; Animals ; Bradykinin - antagonists & inhibitors ; Capillary Permeability - drug effects ; Female ; Guinea Pigs ; Histamine H1 Antagonists - pharmacology ; Ileum - drug effects ; In Vitro Techniques ; Male ; Mice ; Muscle Contraction - drug effects ; Muscle, Smooth - drug effects ; Phenothiazines - pharmacology ; Rats ; Rats, Inbred Strains ; Stomach Ulcer - chemically induced ; Stomach Ulcer - prevention & control ; Trachea - drug effects</subject><ispartof>Folia Pharmacologica Japonica, 1981, Vol.78(4), pp.279-289</ispartof><rights>The Japanese PharmacologicalSociety</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c222t-88889b54bd0b89cbd8f1c2a841fc03c634fec07589d8d673891731f34b6dd8c63</citedby></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,776,780,27901,27902</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/6120126$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>FUJIMURA, Hajime</creatorcontrib><creatorcontrib>TSURUMI, Kaito</creatorcontrib><creatorcontrib>YANAGIHARA, Masayoshi</creatorcontrib><creatorcontrib>HIRAMATSU, Yasuzo</creatorcontrib><creatorcontrib>TAMURA, Yohei</creatorcontrib><creatorcontrib>SHIMIZU, Yoan</creatorcontrib><creatorcontrib>HOJO, Masakazu</creatorcontrib><creatorcontrib>YOSHIDA, Yoichi</creatorcontrib><title>Pharmacological study of Mequitazine (LM-209) (I) Antagonistic actions of chemical mediators</title><title>Folia Pharmacologica Japonica</title><addtitle>Nihon Yakurigaku Zasshi</addtitle><description>Antagonistic activities of Mequitazine (LM-209) on chemical mediators and in particular histamine were investigated in guinea-pigs, mice and rats. The antagonistic activity of LM-209 for histamine in the isolated ileum and trachea of guinea-pigs was less potent than that for clemastine fumarate (CL) and chlorpheniramine maleate (CPM) while that for acetylcholine was more potent than CL and CPM. Moreover, the antagonistic activities of these three compounds on serotonin and bradykinin were almost equipotent in the excised ileum. Using a modified Konzett-Rössler method, the bronchodilating effect of LM-209 (p.o.) for histamine was same as CL, but that for acetylcholine was more potent than CL and CPM. The protective activity of LM-209 (p.o.) on acute death induced by histamine and metacholine in mice was the same as CL, but the duration of the anti-histaminic action was markedly longer than CL. LM-209 given orally inhibited markedly the increased vascular permeability by histamine in rats and the diarrhea by 5-HTP in mice, but did not affect on the histamine-induced ulcer in guinea-pigs. From these results, LM-209 appears to have the potent and long acting antagonistic activity on various chemical mediators.</description><subject>Acetylcholine - antagonists & inhibitors</subject><subject>Airway Resistance - drug effects</subject><subject>Animals</subject><subject>Bradykinin - antagonists & inhibitors</subject><subject>Capillary Permeability - drug effects</subject><subject>Female</subject><subject>Guinea Pigs</subject><subject>Histamine H1 Antagonists - pharmacology</subject><subject>Ileum - drug effects</subject><subject>In Vitro Techniques</subject><subject>Male</subject><subject>Mice</subject><subject>Muscle Contraction - drug effects</subject><subject>Muscle, Smooth - drug effects</subject><subject>Phenothiazines - pharmacology</subject><subject>Rats</subject><subject>Rats, Inbred Strains</subject><subject>Stomach Ulcer - chemically induced</subject><subject>Stomach Ulcer - prevention & control</subject><subject>Trachea - drug effects</subject><issn>0015-5691</issn><issn>1347-8397</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1981</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNo9kElPAkEQhTtGgwS5eDeZIxwGe5tejoS4kED0oDeTSW8DTWbB6eaAv95WCHWoOnypV_UeAPcIzhAu6GO13824mGEur8AQEcpzQSS_BkMIUZEXTKJbMA7BawgLjjkjaAAGDGGIMBuCr_et6htlurrbeKPqLMSDPWZdla3d98FH9eNbl01W6xxDOc0my2k2b6PadK0P0ZtMmei7NvwtmK1r_iUaZ72KXR_uwE2l6uDG5zkCn89PH4vXfPX2slzMV7nBGMdcpJK6oNpCLaTRVlTIYCUoqgwkhhFaOQN5IaQVlnEiJOIEVYRqZq1IfAQeTrr7g07Hy33vG9Ufy7PLxBcnvgvpdXfhqk8WalemCJGktOSiPLeU5oWalFDpWvILAT9rUw</recordid><startdate>198110</startdate><enddate>198110</enddate><creator>FUJIMURA, Hajime</creator><creator>TSURUMI, Kaito</creator><creator>YANAGIHARA, Masayoshi</creator><creator>HIRAMATSU, Yasuzo</creator><creator>TAMURA, Yohei</creator><creator>SHIMIZU, Yoan</creator><creator>HOJO, Masakazu</creator><creator>YOSHIDA, Yoichi</creator><general>The Japanese Pharmacological Society</general><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope></search><sort><creationdate>198110</creationdate><title>Pharmacological study of Mequitazine (LM-209) (I) Antagonistic actions of chemical mediators</title><author>FUJIMURA, Hajime ; TSURUMI, Kaito ; YANAGIHARA, Masayoshi ; HIRAMATSU, Yasuzo ; TAMURA, Yohei ; SHIMIZU, Yoan ; HOJO, Masakazu ; YOSHIDA, Yoichi</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c222t-88889b54bd0b89cbd8f1c2a841fc03c634fec07589d8d673891731f34b6dd8c63</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>jpn</language><creationdate>1981</creationdate><topic>Acetylcholine - antagonists & inhibitors</topic><topic>Airway Resistance - drug effects</topic><topic>Animals</topic><topic>Bradykinin - antagonists & inhibitors</topic><topic>Capillary Permeability - drug effects</topic><topic>Female</topic><topic>Guinea Pigs</topic><topic>Histamine H1 Antagonists - pharmacology</topic><topic>Ileum - drug effects</topic><topic>In Vitro Techniques</topic><topic>Male</topic><topic>Mice</topic><topic>Muscle Contraction - drug effects</topic><topic>Muscle, Smooth - drug effects</topic><topic>Phenothiazines - pharmacology</topic><topic>Rats</topic><topic>Rats, Inbred Strains</topic><topic>Stomach Ulcer - chemically induced</topic><topic>Stomach Ulcer - prevention & control</topic><topic>Trachea - drug effects</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>FUJIMURA, Hajime</creatorcontrib><creatorcontrib>TSURUMI, Kaito</creatorcontrib><creatorcontrib>YANAGIHARA, Masayoshi</creatorcontrib><creatorcontrib>HIRAMATSU, Yasuzo</creatorcontrib><creatorcontrib>TAMURA, Yohei</creatorcontrib><creatorcontrib>SHIMIZU, Yoan</creatorcontrib><creatorcontrib>HOJO, Masakazu</creatorcontrib><creatorcontrib>YOSHIDA, Yoichi</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><jtitle>Folia Pharmacologica Japonica</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>FUJIMURA, Hajime</au><au>TSURUMI, Kaito</au><au>YANAGIHARA, Masayoshi</au><au>HIRAMATSU, Yasuzo</au><au>TAMURA, Yohei</au><au>SHIMIZU, Yoan</au><au>HOJO, Masakazu</au><au>YOSHIDA, Yoichi</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Pharmacological study of Mequitazine (LM-209) (I) Antagonistic actions of chemical mediators</atitle><jtitle>Folia Pharmacologica Japonica</jtitle><addtitle>Nihon Yakurigaku Zasshi</addtitle><date>1981-10</date><risdate>1981</risdate><volume>78</volume><issue>4</issue><spage>279</spage><epage>289</epage><pages>279-289</pages><issn>0015-5691</issn><eissn>1347-8397</eissn><abstract>Antagonistic activities of Mequitazine (LM-209) on chemical mediators and in particular histamine were investigated in guinea-pigs, mice and rats. The antagonistic activity of LM-209 for histamine in the isolated ileum and trachea of guinea-pigs was less potent than that for clemastine fumarate (CL) and chlorpheniramine maleate (CPM) while that for acetylcholine was more potent than CL and CPM. Moreover, the antagonistic activities of these three compounds on serotonin and bradykinin were almost equipotent in the excised ileum. Using a modified Konzett-Rössler method, the bronchodilating effect of LM-209 (p.o.) for histamine was same as CL, but that for acetylcholine was more potent than CL and CPM. The protective activity of LM-209 (p.o.) on acute death induced by histamine and metacholine in mice was the same as CL, but the duration of the anti-histaminic action was markedly longer than CL. LM-209 given orally inhibited markedly the increased vascular permeability by histamine in rats and the diarrhea by 5-HTP in mice, but did not affect on the histamine-induced ulcer in guinea-pigs. From these results, LM-209 appears to have the potent and long acting antagonistic activity on various chemical mediators.</abstract><cop>Japan</cop><pub>The Japanese Pharmacological Society</pub><pmid>6120126</pmid><doi>10.1254/fpj.78.279</doi><tpages>11</tpages><oa>free_for_read</oa></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0015-5691 |
| ispartof | Folia Pharmacologica Japonica, 1981, Vol.78(4), pp.279-289 |
| issn | 0015-5691 1347-8397 |
| language | jpn |
| recordid | cdi_pubmed_primary_6120126 |
| source | MEDLINE; Elektronische Zeitschriftenbibliothek - Frei zugängliche E-Journals |
| subjects | Acetylcholine - antagonists & inhibitors Airway Resistance - drug effects Animals Bradykinin - antagonists & inhibitors Capillary Permeability - drug effects Female Guinea Pigs Histamine H1 Antagonists - pharmacology Ileum - drug effects In Vitro Techniques Male Mice Muscle Contraction - drug effects Muscle, Smooth - drug effects Phenothiazines - pharmacology Rats Rats, Inbred Strains Stomach Ulcer - chemically induced Stomach Ulcer - prevention & control Trachea - drug effects |
| title | Pharmacological study of Mequitazine (LM-209) (I) Antagonistic actions of chemical mediators |
| url | https://sfx.bib-bvb.de/sfx_tum?ctx_ver=Z39.88-2004&ctx_enc=info:ofi/enc:UTF-8&ctx_tim=2025-02-02T06%3A43%3A41IST&url_ver=Z39.88-2004&url_ctx_fmt=infofi/fmt:kev:mtx:ctx&rfr_id=info:sid/primo.exlibrisgroup.com:primo3-Article-pubmed_jstag&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.genre=article&rft.atitle=Pharmacological%20study%20of%20Mequitazine%20(LM-209)%20(I)%20Antagonistic%20actions%20of%20chemical%20mediators&rft.jtitle=Folia%20Pharmacologica%20Japonica&rft.au=FUJIMURA,%20Hajime&rft.date=1981-10&rft.volume=78&rft.issue=4&rft.spage=279&rft.epage=289&rft.pages=279-289&rft.issn=0015-5691&rft.eissn=1347-8397&rft_id=info:doi/10.1254/fpj.78.279&rft_dat=%3Cpubmed_jstag%3E6120126%3C/pubmed_jstag%3E%3Curl%3E%3C/url%3E&disable_directlink=true&sfx.directlink=off&sfx.report_link=0&rft_id=info:oai/&rft_id=info:pmid/6120126&rfr_iscdi=true |