Pharmacological studies of FUT-175, nafamstat mesilate: IV. Effects on coagulation, platelets and fibrinolysis
Inhibitory effects of FUT-175 (nafamstat mesilate) on coagulation, platelets and fibrinolysis were examined. 1) FUT-175 prolonged activated partial thromboplastin time, thrombin time and prothrombin time in rabbit plasma. 2) FUT-175 prolonged these coagulation times in human plasma at lower concentr...
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| Veröffentlicht in: | Folia Pharmacologica Japonica 1984, Vol.84(5), pp.417-428 |
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| container_title | Folia Pharmacologica Japonica |
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| creator | KOSHIYAMA, Yoshiko OZEKI, Masayuki MOTOYOSHI, Akemi FUJITA, Mitsunobu IWAKI, Masahiro AOYAMA, Takuo |
| description | Inhibitory effects of FUT-175 (nafamstat mesilate) on coagulation, platelets and fibrinolysis were examined. 1) FUT-175 prolonged activated partial thromboplastin time, thrombin time and prothrombin time in rabbit plasma. 2) FUT-175 prolonged these coagulation times in human plasma at lower concentration than in rabbit plasma. 3) FUT-175 inhibited platelet aggregation induced by a variety of aggregation agents in rabbit plateletrich plasma (PRP). 4) In human PRP, FUT-175 inhibited platelet aggregation induced by a variety of aggregation agents at lower concentration than in rabbit PRP. 5) Lipopolysaccharide induced a dose-dependent platelet aggregation in dog PRP. FUT-175 showed an inhibitory effect on this aggregation. 6) FUT-175 inhibited clot retraction in rabbit plasma. 7) The fibrinolysis activity was measured on fibrinolysis of rabbit plasma activated by urokinase. FUT-175 prolonged this fibrinolysis time. 8) Inhibitory effects on coagulation and fibrinolysis were also found ex vivo. 9) FUT-175 prolonged bleeding time in mice. These results indicate that FUT-175 has potent inhibitory effects on coagulation, platelets and fibrinolysis. |
| doi_str_mv | 10.1254/fpj.84.417 |
| format | Article |
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FUT-175 showed an inhibitory effect on this aggregation. 6) FUT-175 inhibited clot retraction in rabbit plasma. 7) The fibrinolysis activity was measured on fibrinolysis of rabbit plasma activated by urokinase. FUT-175 prolonged this fibrinolysis time. 8) Inhibitory effects on coagulation and fibrinolysis were also found ex vivo. 9) FUT-175 prolonged bleeding time in mice. These results indicate that FUT-175 has potent inhibitory effects on coagulation, platelets and fibrinolysis.</description><identifier>ISSN: 0015-5691</identifier><identifier>EISSN: 1347-8397</identifier><identifier>DOI: 10.1254/fpj.84.417</identifier><identifier>PMID: 6519580</identifier><language>jpn</language><publisher>Japan: The Japanese Pharmacological Society</publisher><subject>Animals ; Anticoagulants ; Antifibrinolytic Agents ; Bleeding Time ; Clot Retraction ; Dogs ; Guanidines - pharmacology ; Humans ; In Vitro Techniques ; Lipopolysaccharides - antagonists & inhibitors ; Male ; Mice ; Mice, Inbred ICR ; Platelet Aggregation - drug effects ; Rabbits ; Species Specificity ; Urokinase-Type Plasminogen Activator - antagonists & inhibitors</subject><ispartof>Folia Pharmacologica Japonica, 1984, Vol.84(5), pp.417-428</ispartof><rights>The Japanese PharmacologicalSociety</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,27922,27923</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/6519580$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>KOSHIYAMA, Yoshiko</creatorcontrib><creatorcontrib>OZEKI, Masayuki</creatorcontrib><creatorcontrib>MOTOYOSHI, Akemi</creatorcontrib><creatorcontrib>FUJITA, Mitsunobu</creatorcontrib><creatorcontrib>IWAKI, Masahiro</creatorcontrib><creatorcontrib>AOYAMA, Takuo</creatorcontrib><title>Pharmacological studies of FUT-175, nafamstat mesilate: IV. Effects on coagulation, platelets and fibrinolysis</title><title>Folia Pharmacologica Japonica</title><addtitle>Nihon Yakurigaku Zasshi</addtitle><description>Inhibitory effects of FUT-175 (nafamstat mesilate) on coagulation, platelets and fibrinolysis were examined. 1) FUT-175 prolonged activated partial thromboplastin time, thrombin time and prothrombin time in rabbit plasma. 2) FUT-175 prolonged these coagulation times in human plasma at lower concentration than in rabbit plasma. 3) FUT-175 inhibited platelet aggregation induced by a variety of aggregation agents in rabbit plateletrich plasma (PRP). 4) In human PRP, FUT-175 inhibited platelet aggregation induced by a variety of aggregation agents at lower concentration than in rabbit PRP. 5) Lipopolysaccharide induced a dose-dependent platelet aggregation in dog PRP. FUT-175 showed an inhibitory effect on this aggregation. 6) FUT-175 inhibited clot retraction in rabbit plasma. 7) The fibrinolysis activity was measured on fibrinolysis of rabbit plasma activated by urokinase. FUT-175 prolonged this fibrinolysis time. 8) Inhibitory effects on coagulation and fibrinolysis were also found ex vivo. 9) FUT-175 prolonged bleeding time in mice. These results indicate that FUT-175 has potent inhibitory effects on coagulation, platelets and fibrinolysis.</description><subject>Animals</subject><subject>Anticoagulants</subject><subject>Antifibrinolytic Agents</subject><subject>Bleeding Time</subject><subject>Clot Retraction</subject><subject>Dogs</subject><subject>Guanidines - pharmacology</subject><subject>Humans</subject><subject>In Vitro Techniques</subject><subject>Lipopolysaccharides - antagonists & inhibitors</subject><subject>Male</subject><subject>Mice</subject><subject>Mice, Inbred ICR</subject><subject>Platelet Aggregation - drug effects</subject><subject>Rabbits</subject><subject>Species Specificity</subject><subject>Urokinase-Type Plasminogen Activator - antagonists & inhibitors</subject><issn>0015-5691</issn><issn>1347-8397</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1984</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNo9kE1Lw0AURQdRaqnduBeycmXqvMz3UoqtQkEX7XqYzLypKUlTM8nCf2-gpZv3Fudy4R5CHoEuoBD8NZ4OC80XHNQNmQLjKtfMqFsypRRELqSBezJPqSopFapQksGETKQAIzSdEvn947rG-bZu95V3dZb6IVSYsjZmq902ByVesqOLrkm967MGU1W7Hh_IXXR1wvnlz8hu9b5dfuSbr_Xn8m2TH0BDnwfPGARDo5RY6uAL0B5pKCWaWBRCgTARWQCjdHQUQ9CUgwQmWDQlYslm5Pnce-ra3wFTb5sqeaxrd8R2SFYJLQXXMAafLsGhbDDYU1c1rvuzl6EjX575Ydyxxyt3XV_5Gu1oEQznVnMrzmcUeqV-lGTxyP4B23dr5w</recordid><startdate>198411</startdate><enddate>198411</enddate><creator>KOSHIYAMA, Yoshiko</creator><creator>OZEKI, Masayuki</creator><creator>MOTOYOSHI, Akemi</creator><creator>FUJITA, Mitsunobu</creator><creator>IWAKI, Masahiro</creator><creator>AOYAMA, Takuo</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><scope>7X8</scope></search><sort><creationdate>198411</creationdate><title>Pharmacological studies of FUT-175, nafamstat mesilate</title><author>KOSHIYAMA, Yoshiko ; OZEKI, Masayuki ; MOTOYOSHI, Akemi ; FUJITA, Mitsunobu ; IWAKI, Masahiro ; AOYAMA, Takuo</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-j181t-dc331d90f66eb8dc218ce0db6e9f2257159fe3d1978fa0edd804161353f9beeb3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>jpn</language><creationdate>1984</creationdate><topic>Animals</topic><topic>Anticoagulants</topic><topic>Antifibrinolytic Agents</topic><topic>Bleeding Time</topic><topic>Clot Retraction</topic><topic>Dogs</topic><topic>Guanidines - pharmacology</topic><topic>Humans</topic><topic>In Vitro Techniques</topic><topic>Lipopolysaccharides - antagonists & inhibitors</topic><topic>Male</topic><topic>Mice</topic><topic>Mice, Inbred ICR</topic><topic>Platelet Aggregation - drug effects</topic><topic>Rabbits</topic><topic>Species Specificity</topic><topic>Urokinase-Type Plasminogen Activator - antagonists & inhibitors</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>KOSHIYAMA, Yoshiko</creatorcontrib><creatorcontrib>OZEKI, Masayuki</creatorcontrib><creatorcontrib>MOTOYOSHI, Akemi</creatorcontrib><creatorcontrib>FUJITA, Mitsunobu</creatorcontrib><creatorcontrib>IWAKI, Masahiro</creatorcontrib><creatorcontrib>AOYAMA, Takuo</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>MEDLINE - Academic</collection><jtitle>Folia Pharmacologica Japonica</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>KOSHIYAMA, Yoshiko</au><au>OZEKI, Masayuki</au><au>MOTOYOSHI, Akemi</au><au>FUJITA, Mitsunobu</au><au>IWAKI, Masahiro</au><au>AOYAMA, Takuo</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Pharmacological studies of FUT-175, nafamstat mesilate: IV. Effects on coagulation, platelets and fibrinolysis</atitle><jtitle>Folia Pharmacologica Japonica</jtitle><addtitle>Nihon Yakurigaku Zasshi</addtitle><date>1984-11</date><risdate>1984</risdate><volume>84</volume><issue>5</issue><spage>417</spage><epage>428</epage><pages>417-428</pages><issn>0015-5691</issn><eissn>1347-8397</eissn><abstract>Inhibitory effects of FUT-175 (nafamstat mesilate) on coagulation, platelets and fibrinolysis were examined. 1) FUT-175 prolonged activated partial thromboplastin time, thrombin time and prothrombin time in rabbit plasma. 2) FUT-175 prolonged these coagulation times in human plasma at lower concentration than in rabbit plasma. 3) FUT-175 inhibited platelet aggregation induced by a variety of aggregation agents in rabbit plateletrich plasma (PRP). 4) In human PRP, FUT-175 inhibited platelet aggregation induced by a variety of aggregation agents at lower concentration than in rabbit PRP. 5) Lipopolysaccharide induced a dose-dependent platelet aggregation in dog PRP. FUT-175 showed an inhibitory effect on this aggregation. 6) FUT-175 inhibited clot retraction in rabbit plasma. 7) The fibrinolysis activity was measured on fibrinolysis of rabbit plasma activated by urokinase. FUT-175 prolonged this fibrinolysis time. 8) Inhibitory effects on coagulation and fibrinolysis were also found ex vivo. 9) FUT-175 prolonged bleeding time in mice. These results indicate that FUT-175 has potent inhibitory effects on coagulation, platelets and fibrinolysis.</abstract><cop>Japan</cop><pub>The Japanese Pharmacological Society</pub><pmid>6519580</pmid><doi>10.1254/fpj.84.417</doi><tpages>12</tpages><oa>free_for_read</oa></addata></record> |
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| ispartof | Folia Pharmacologica Japonica, 1984, Vol.84(5), pp.417-428 |
| issn | 0015-5691 1347-8397 |
| language | jpn |
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| source | MEDLINE; EZB-FREE-00999 freely available EZB journals |
| subjects | Animals Anticoagulants Antifibrinolytic Agents Bleeding Time Clot Retraction Dogs Guanidines - pharmacology Humans In Vitro Techniques Lipopolysaccharides - antagonists & inhibitors Male Mice Mice, Inbred ICR Platelet Aggregation - drug effects Rabbits Species Specificity Urokinase-Type Plasminogen Activator - antagonists & inhibitors |
| title | Pharmacological studies of FUT-175, nafamstat mesilate: IV. Effects on coagulation, platelets and fibrinolysis |
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