The Effects of Orally Administered Y-25130, a Selective Serotonin3-Receptor Antagonist, on Chemotherapeutic Agent-Induced Emesis
The antiemetic effects of orally administered Y-25130, a potent and selective 5-HT3-receptor antagonist, were compared with those of ondansetron, granisetron, metoclopramide and domperidone. Y-25130 (0.1-1.0 mg/kg) dose-dependently prolonged the latency to the first vomiting and decreased the number...
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| Veröffentlicht in: | Japanese journal of pharmacology 1993, Vol.63 (3), p.377-383 |
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| creator | Haga, Keiichiro Inaba, Ken-ichi Shoji, Hidenori Morimoto, Yasuto Fukuda, Takemi Setoguchi, Michihide |
| description | The antiemetic effects of orally administered Y-25130, a potent and selective 5-HT3-receptor antagonist, were compared with those of ondansetron, granisetron, metoclopramide and domperidone. Y-25130 (0.1-1.0 mg/kg) dose-dependently prolonged the latency to the first vomiting and decreased the number of vomitings induced by cisplatin in dogs. The antiemetic effect of Y-25130 against cisplatin-induced vomiting was more potent than that of metoclopramide and ondansetron, but it showed little difference from that of granisetron. The emesis induced by the combined treatment of doxorubicin and cyclophosphamide was also inhibited by Y-25130 (0.1-1 mg/kg) in ferrets. The antiemetic effect of Y-25130 was more potent than that of metoclopramide, almost the same as that of granisetron and less potent than that of ondansetron. Because of a notable difference of potency ranking between Y-25130 and ondansetron in these two tests, a third test was performed to evaluate the inhibitory effect of Y-25130 in ferrets on cisplatin-induced emesis in comparison with that of ondansetron. The antiemetic effect of Y-25130 on cisplatin-induced emesis in ferrets was very similar to that of ondansetron. Domperidone did not inhibit these cytotoxic agents-induced emeses. These results suggest that Y-25130 is an orally active antiemetic compound against cisplatin and doxorubicin/cyclophosphamide-induced emeses; and its the antiemetic potency is similar to those of granisetron and ondansetron, but superior to those of metoclopramide and domperidone. |
| doi_str_mv | 10.1254/jjp.63.377 |
| format | Article |
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Y-25130 (0.1-1.0 mg/kg) dose-dependently prolonged the latency to the first vomiting and decreased the number of vomitings induced by cisplatin in dogs. The antiemetic effect of Y-25130 against cisplatin-induced vomiting was more potent than that of metoclopramide and ondansetron, but it showed little difference from that of granisetron. The emesis induced by the combined treatment of doxorubicin and cyclophosphamide was also inhibited by Y-25130 (0.1-1 mg/kg) in ferrets. The antiemetic effect of Y-25130 was more potent than that of metoclopramide, almost the same as that of granisetron and less potent than that of ondansetron. Because of a notable difference of potency ranking between Y-25130 and ondansetron in these two tests, a third test was performed to evaluate the inhibitory effect of Y-25130 in ferrets on cisplatin-induced emesis in comparison with that of ondansetron. The antiemetic effect of Y-25130 on cisplatin-induced emesis in ferrets was very similar to that of ondansetron. Domperidone did not inhibit these cytotoxic agents-induced emeses. These results suggest that Y-25130 is an orally active antiemetic compound against cisplatin and doxorubicin/cyclophosphamide-induced emeses; and its the antiemetic potency is similar to those of granisetron and ondansetron, but superior to those of metoclopramide and domperidone.</description><identifier>ISSN: 0021-5198</identifier><identifier>EISSN: 1347-3506</identifier><identifier>DOI: 10.1254/jjp.63.377</identifier><identifier>PMID: 8107329</identifier><identifier>CODEN: JJPAAZ</identifier><language>eng</language><publisher>Kyoto: Japanese Pharmacological Society</publisher><subject>5-HT3 receptor ; Administration, Oral ; Animals ; Antiemesis ; Antiemetics - administration & dosage ; Antiemetics - therapeutic use ; Biological and medical sciences ; Bridged Bicyclo Compounds - administration & dosage ; Bridged Bicyclo Compounds - therapeutic use ; Bridged Bicyclo Compounds, Heterocyclic ; Cisplatin ; Cisplatin - toxicity ; Cyclophosphamide - toxicity ; Digestive system ; Dogs ; Domperidone - pharmacology ; Dose-Response Relationship, Drug ; Doxorubicin - toxicity ; Doxorubicin/cyclophosphamide ; Female ; Ferrets ; Granisetron - pharmacology ; Male ; Medical sciences ; Metoclopramide - pharmacology ; Ondansetron - pharmacology ; Oxazines - administration & dosage ; Oxazines - therapeutic use ; Pharmacology. Drug treatments ; Serotonin Antagonists ; Vomiting - chemically induced ; Vomiting - drug therapy ; Y-25130</subject><ispartof>Japanese journal of pharmacology, 1993, Vol.63 (3), p.377-383</ispartof><rights>1993 Elsevier B.V.</rights><rights>1994 INIST-CNRS</rights><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c4747-dc43b750a9d829b7fa05cbd7c8a384781465e334419b2d738c1baba88a7b4a343</citedby><cites>FETCH-LOGICAL-c4747-dc43b750a9d829b7fa05cbd7c8a384781465e334419b2d738c1baba88a7b4a343</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,4024,27923,27924,27925</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=3892065$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/8107329$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Haga, Keiichiro</creatorcontrib><creatorcontrib>Inaba, Ken-ichi</creatorcontrib><creatorcontrib>Shoji, Hidenori</creatorcontrib><creatorcontrib>Morimoto, Yasuto</creatorcontrib><creatorcontrib>Fukuda, Takemi</creatorcontrib><creatorcontrib>Setoguchi, Michihide</creatorcontrib><title>The Effects of Orally Administered Y-25130, a Selective Serotonin3-Receptor Antagonist, on Chemotherapeutic Agent-Induced Emesis</title><title>Japanese journal of pharmacology</title><addtitle>Jpn J Pharmacol</addtitle><description>The antiemetic effects of orally administered Y-25130, a potent and selective 5-HT3-receptor antagonist, were compared with those of ondansetron, granisetron, metoclopramide and domperidone. Y-25130 (0.1-1.0 mg/kg) dose-dependently prolonged the latency to the first vomiting and decreased the number of vomitings induced by cisplatin in dogs. The antiemetic effect of Y-25130 against cisplatin-induced vomiting was more potent than that of metoclopramide and ondansetron, but it showed little difference from that of granisetron. The emesis induced by the combined treatment of doxorubicin and cyclophosphamide was also inhibited by Y-25130 (0.1-1 mg/kg) in ferrets. The antiemetic effect of Y-25130 was more potent than that of metoclopramide, almost the same as that of granisetron and less potent than that of ondansetron. Because of a notable difference of potency ranking between Y-25130 and ondansetron in these two tests, a third test was performed to evaluate the inhibitory effect of Y-25130 in ferrets on cisplatin-induced emesis in comparison with that of ondansetron. The antiemetic effect of Y-25130 on cisplatin-induced emesis in ferrets was very similar to that of ondansetron. Domperidone did not inhibit these cytotoxic agents-induced emeses. These results suggest that Y-25130 is an orally active antiemetic compound against cisplatin and doxorubicin/cyclophosphamide-induced emeses; and its the antiemetic potency is similar to those of granisetron and ondansetron, but superior to those of metoclopramide and domperidone.</description><subject>5-HT3 receptor</subject><subject>Administration, Oral</subject><subject>Animals</subject><subject>Antiemesis</subject><subject>Antiemetics - administration & dosage</subject><subject>Antiemetics - therapeutic use</subject><subject>Biological and medical sciences</subject><subject>Bridged Bicyclo Compounds - administration & dosage</subject><subject>Bridged Bicyclo Compounds - therapeutic use</subject><subject>Bridged Bicyclo Compounds, Heterocyclic</subject><subject>Cisplatin</subject><subject>Cisplatin - toxicity</subject><subject>Cyclophosphamide - toxicity</subject><subject>Digestive system</subject><subject>Dogs</subject><subject>Domperidone - pharmacology</subject><subject>Dose-Response Relationship, Drug</subject><subject>Doxorubicin - toxicity</subject><subject>Doxorubicin/cyclophosphamide</subject><subject>Female</subject><subject>Ferrets</subject><subject>Granisetron - pharmacology</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Metoclopramide - pharmacology</subject><subject>Ondansetron - pharmacology</subject><subject>Oxazines - administration & dosage</subject><subject>Oxazines - therapeutic use</subject><subject>Pharmacology. Drug treatments</subject><subject>Serotonin Antagonists</subject><subject>Vomiting - chemically induced</subject><subject>Vomiting - drug therapy</subject><subject>Y-25130</subject><issn>0021-5198</issn><issn>1347-3506</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1993</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNptkE1LxDAQhoMoun5cvAs5eBK7Jk3apMdlWXVhQfDj4KmkydTN0iYl6Qre_OlGdvHkKRPmmRneB6FLSqY0L_jdZjNMSzZlQhygCWVcZKwg5SGaEJLTrKCVPEGnMW7SVxLKj9GxpESwvJqg79c14EXbgh4j9i1-CqrrvvDM9NbZOEIAg9-zvKCM3GKFX6BLpP2EVAU_emcdy55BwzD6gGduVB_-d-4We4fna-j9uIagBtiOVuPZB7gxWzqz1Wntoodo4zk6alUX4WL_nqG3-8Xr_DFbPT0s57NVprlIgYzmrBEFUZWRedWIVpFCN0ZoqZjkQlJeFsAY57RqciOY1LRRjZJSiYYrxtkZutnt1cHHGKCth2B7Fb5qSupfi3WyWJesThYTfLWDh23Tg_lD99pS_3rfV1Grrg3KaRv_MCarnJRFwvgOgxTs00Koo7bgUngbksbaePvf9R_xt4wd</recordid><startdate>1993</startdate><enddate>1993</enddate><creator>Haga, Keiichiro</creator><creator>Inaba, Ken-ichi</creator><creator>Shoji, Hidenori</creator><creator>Morimoto, Yasuto</creator><creator>Fukuda, Takemi</creator><creator>Setoguchi, Michihide</creator><general>Japanese Pharmacological Society</general><scope>6I.</scope><scope>AAFTH</scope><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></search><sort><creationdate>1993</creationdate><title>The Effects of Orally Administered Y-25130, a Selective Serotonin3-Receptor Antagonist, on Chemotherapeutic Agent-Induced Emesis</title><author>Haga, Keiichiro ; Inaba, Ken-ichi ; Shoji, Hidenori ; Morimoto, Yasuto ; Fukuda, Takemi ; Setoguchi, Michihide</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c4747-dc43b750a9d829b7fa05cbd7c8a384781465e334419b2d738c1baba88a7b4a343</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1993</creationdate><topic>5-HT3 receptor</topic><topic>Administration, Oral</topic><topic>Animals</topic><topic>Antiemesis</topic><topic>Antiemetics - administration & dosage</topic><topic>Antiemetics - therapeutic use</topic><topic>Biological and medical sciences</topic><topic>Bridged Bicyclo Compounds - administration & dosage</topic><topic>Bridged Bicyclo Compounds - therapeutic use</topic><topic>Bridged Bicyclo Compounds, Heterocyclic</topic><topic>Cisplatin</topic><topic>Cisplatin - toxicity</topic><topic>Cyclophosphamide - toxicity</topic><topic>Digestive system</topic><topic>Dogs</topic><topic>Domperidone - pharmacology</topic><topic>Dose-Response Relationship, Drug</topic><topic>Doxorubicin - toxicity</topic><topic>Doxorubicin/cyclophosphamide</topic><topic>Female</topic><topic>Ferrets</topic><topic>Granisetron - pharmacology</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Metoclopramide - pharmacology</topic><topic>Ondansetron - pharmacology</topic><topic>Oxazines - administration & dosage</topic><topic>Oxazines - therapeutic use</topic><topic>Pharmacology. Drug treatments</topic><topic>Serotonin Antagonists</topic><topic>Vomiting - chemically induced</topic><topic>Vomiting - drug therapy</topic><topic>Y-25130</topic><toplevel>online_resources</toplevel><creatorcontrib>Haga, Keiichiro</creatorcontrib><creatorcontrib>Inaba, Ken-ichi</creatorcontrib><creatorcontrib>Shoji, Hidenori</creatorcontrib><creatorcontrib>Morimoto, Yasuto</creatorcontrib><creatorcontrib>Fukuda, Takemi</creatorcontrib><creatorcontrib>Setoguchi, Michihide</creatorcontrib><collection>ScienceDirect Open Access Titles</collection><collection>Elsevier:ScienceDirect:Open Access</collection><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><jtitle>Japanese journal of pharmacology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Haga, Keiichiro</au><au>Inaba, Ken-ichi</au><au>Shoji, Hidenori</au><au>Morimoto, Yasuto</au><au>Fukuda, Takemi</au><au>Setoguchi, Michihide</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>The Effects of Orally Administered Y-25130, a Selective Serotonin3-Receptor Antagonist, on Chemotherapeutic Agent-Induced Emesis</atitle><jtitle>Japanese journal of pharmacology</jtitle><addtitle>Jpn J Pharmacol</addtitle><date>1993</date><risdate>1993</risdate><volume>63</volume><issue>3</issue><spage>377</spage><epage>383</epage><pages>377-383</pages><issn>0021-5198</issn><eissn>1347-3506</eissn><coden>JJPAAZ</coden><abstract>The antiemetic effects of orally administered Y-25130, a potent and selective 5-HT3-receptor antagonist, were compared with those of ondansetron, granisetron, metoclopramide and domperidone. Y-25130 (0.1-1.0 mg/kg) dose-dependently prolonged the latency to the first vomiting and decreased the number of vomitings induced by cisplatin in dogs. The antiemetic effect of Y-25130 against cisplatin-induced vomiting was more potent than that of metoclopramide and ondansetron, but it showed little difference from that of granisetron. The emesis induced by the combined treatment of doxorubicin and cyclophosphamide was also inhibited by Y-25130 (0.1-1 mg/kg) in ferrets. The antiemetic effect of Y-25130 was more potent than that of metoclopramide, almost the same as that of granisetron and less potent than that of ondansetron. Because of a notable difference of potency ranking between Y-25130 and ondansetron in these two tests, a third test was performed to evaluate the inhibitory effect of Y-25130 in ferrets on cisplatin-induced emesis in comparison with that of ondansetron. The antiemetic effect of Y-25130 on cisplatin-induced emesis in ferrets was very similar to that of ondansetron. Domperidone did not inhibit these cytotoxic agents-induced emeses. These results suggest that Y-25130 is an orally active antiemetic compound against cisplatin and doxorubicin/cyclophosphamide-induced emeses; and its the antiemetic potency is similar to those of granisetron and ondansetron, but superior to those of metoclopramide and domperidone.</abstract><cop>Kyoto</cop><pub>Japanese Pharmacological Society</pub><pmid>8107329</pmid><doi>10.1254/jjp.63.377</doi><tpages>7</tpages><oa>free_for_read</oa></addata></record> |
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| ispartof | Japanese journal of pharmacology, 1993, Vol.63 (3), p.377-383 |
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| language | eng |
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| source | MEDLINE; Elektronische Zeitschriftenbibliothek - Frei zugängliche E-Journals; J-STAGE (Japan Science & Technology Information Aggregator, Electronic) Freely Available Titles - Japanese; Free Full-Text Journals in Chemistry |
| subjects | 5-HT3 receptor Administration, Oral Animals Antiemesis Antiemetics - administration & dosage Antiemetics - therapeutic use Biological and medical sciences Bridged Bicyclo Compounds - administration & dosage Bridged Bicyclo Compounds - therapeutic use Bridged Bicyclo Compounds, Heterocyclic Cisplatin Cisplatin - toxicity Cyclophosphamide - toxicity Digestive system Dogs Domperidone - pharmacology Dose-Response Relationship, Drug Doxorubicin - toxicity Doxorubicin/cyclophosphamide Female Ferrets Granisetron - pharmacology Male Medical sciences Metoclopramide - pharmacology Ondansetron - pharmacology Oxazines - administration & dosage Oxazines - therapeutic use Pharmacology. Drug treatments Serotonin Antagonists Vomiting - chemically induced Vomiting - drug therapy Y-25130 |
| title | The Effects of Orally Administered Y-25130, a Selective Serotonin3-Receptor Antagonist, on Chemotherapeutic Agent-Induced Emesis |
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