High affinity binding of Y-25130 for serotonin 3 receptor
The binding of Y-25130 on serotonin 3 (5-HT3) receptors was evaluated by examining its effect on 3H-BRL 43694 (3H-granisetron) binding to rat cerebral cortex membranes in comparison with those of granisetron, ondansetron and metoclopramide. Y-25130, granisetron, ondansetron, metoclopramide, 5-HT and...
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| Veröffentlicht in: | Folia Pharmacologica Japonica 1992/08/01, Vol.100(2), pp.137-142 |
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| container_title | Folia Pharmacologica Japonica |
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| creator | SAKAMORI, Masamitsu TAKEHARA, Shuzo SETOGUCHI, Michihide |
| description | The binding of Y-25130 on serotonin 3 (5-HT3) receptors was evaluated by examining its effect on 3H-BRL 43694 (3H-granisetron) binding to rat cerebral cortex membranes in comparison with those of granisetron, ondansetron and metoclopramide. Y-25130, granisetron, ondansetron, metoclopramide, 5-HT and 2-methyl-5-HT displaced the specific binding of 3H-granisetron to the synaptosomal membranes in a concentration-dependent manner. The rank order of potency for inhibition of 3H-granisetron binding by the test compounds was Y-25130≅granisetron > ondansetron> 2-methyl- 5-HT≅5-HT≅metoclopramide. To determine the manner of interaction between Y-25130 and 5-HT3 receptors, Scatchard analysis of 3H-granisetron specific binding to the membranes of the cerebral cortex in the absence or presence of various concentrations of Y-25130 was performed. It was indicated that Y-25130 exerted a typical competitive-type inhibition of 3H-granisetron binding. The present study indicates that Y-25130 binds competitively to 5-HT3 receptors with high affinity. |
| doi_str_mv | 10.1254/fpj.100.137 |
| format | Article |
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Y-25130, granisetron, ondansetron, metoclopramide, 5-HT and 2-methyl-5-HT displaced the specific binding of 3H-granisetron to the synaptosomal membranes in a concentration-dependent manner. The rank order of potency for inhibition of 3H-granisetron binding by the test compounds was Y-25130≅granisetron > ondansetron> 2-methyl- 5-HT≅5-HT≅metoclopramide. To determine the manner of interaction between Y-25130 and 5-HT3 receptors, Scatchard analysis of 3H-granisetron specific binding to the membranes of the cerebral cortex in the absence or presence of various concentrations of Y-25130 was performed. It was indicated that Y-25130 exerted a typical competitive-type inhibition of 3H-granisetron binding. The present study indicates that Y-25130 binds competitively to 5-HT3 receptors with high affinity.</description><identifier>ISSN: 0015-5691</identifier><identifier>EISSN: 1347-8397</identifier><identifier>DOI: 10.1254/fpj.100.137</identifier><identifier>PMID: 1330854</identifier><language>jpn</language><publisher>Japan: The Japanese Pharmacological Society</publisher><subject>Animals ; Antiemetics - metabolism ; Binding, Competitive ; Bridged Bicyclo Compounds - metabolism ; Bridged Bicyclo Compounds, Heterocyclic ; Cerebral Cortex - metabolism ; Granisetron ; In Vitro Techniques ; Indazoles - metabolism ; Male ; Ondansetron - metabolism ; Oxazines - metabolism ; Rats ; Rats, Wistar ; Receptors, Serotonin - metabolism ; Synaptic Membranes - metabolism</subject><ispartof>Folia Pharmacologica Japonica, 1992/08/01, Vol.100(2), pp.137-142</ispartof><rights>The Japanese PharmacologicalSociety</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c440t-285947a1f58d2a459587d546e138c13b10b3f6b82ebfb0fff7935d29a5d150423</citedby></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,27924,27925</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/1330854$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>SAKAMORI, Masamitsu</creatorcontrib><creatorcontrib>TAKEHARA, Shuzo</creatorcontrib><creatorcontrib>SETOGUCHI, Michihide</creatorcontrib><title>High affinity binding of Y-25130 for serotonin 3 receptor</title><title>Folia Pharmacologica Japonica</title><addtitle>Nihon Yakurigaku Zasshi</addtitle><description>The binding of Y-25130 on serotonin 3 (5-HT3) receptors was evaluated by examining its effect on 3H-BRL 43694 (3H-granisetron) binding to rat cerebral cortex membranes in comparison with those of granisetron, ondansetron and metoclopramide. Y-25130, granisetron, ondansetron, metoclopramide, 5-HT and 2-methyl-5-HT displaced the specific binding of 3H-granisetron to the synaptosomal membranes in a concentration-dependent manner. The rank order of potency for inhibition of 3H-granisetron binding by the test compounds was Y-25130≅granisetron > ondansetron> 2-methyl- 5-HT≅5-HT≅metoclopramide. To determine the manner of interaction between Y-25130 and 5-HT3 receptors, Scatchard analysis of 3H-granisetron specific binding to the membranes of the cerebral cortex in the absence or presence of various concentrations of Y-25130 was performed. It was indicated that Y-25130 exerted a typical competitive-type inhibition of 3H-granisetron binding. The present study indicates that Y-25130 binds competitively to 5-HT3 receptors with high affinity.</description><subject>Animals</subject><subject>Antiemetics - metabolism</subject><subject>Binding, Competitive</subject><subject>Bridged Bicyclo Compounds - metabolism</subject><subject>Bridged Bicyclo Compounds, Heterocyclic</subject><subject>Cerebral Cortex - metabolism</subject><subject>Granisetron</subject><subject>In Vitro Techniques</subject><subject>Indazoles - metabolism</subject><subject>Male</subject><subject>Ondansetron - metabolism</subject><subject>Oxazines - metabolism</subject><subject>Rats</subject><subject>Rats, Wistar</subject><subject>Receptors, Serotonin - metabolism</subject><subject>Synaptic Membranes - metabolism</subject><issn>0015-5691</issn><issn>1347-8397</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1992</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNpFkD1PwzAURS0EKlXpxIzkiQWl2H52HI-oKhSpEgsMTJGd2K2rNC52OvTfkxIoy_vQuTrDReiWkhllgj-6_XZGSf-AvEBjClxmBSh5icaEUJGJXNFrNE3JG0KEZDIHOkIjCkAKwcdILf16g7VzvvXdERvf1r5d4-DwZ8YEBYJdiDjZGLrQ-hYDjray-y7EG3TldJPs9HdP0Mfz4n2-zFZvL6_zp1VWcU66jBVCcampE0XNNBdKFLIWPLcUioqCocSAy03BrHGGOOekAlEzpUVNBeEMJuh-8O5j-DrY1JU7nyrbNLq14ZBKCcA4kafgwxCsYkgpWlfuo9_peCwpKU9dlX1X_d0_IPv03a_2YHa2_s8OzfR8MfBt6vTanrmOna8ae3JRxfmPj_1NkGdebXQsbQvf4YJ5mQ</recordid><startdate>19920801</startdate><enddate>19920801</enddate><creator>SAKAMORI, Masamitsu</creator><creator>TAKEHARA, Shuzo</creator><creator>SETOGUCHI, Michihide</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>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope></search><sort><creationdate>19920801</creationdate><title>High affinity binding of Y-25130 for serotonin 3 receptor</title><author>SAKAMORI, Masamitsu ; TAKEHARA, Shuzo ; SETOGUCHI, Michihide</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c440t-285947a1f58d2a459587d546e138c13b10b3f6b82ebfb0fff7935d29a5d150423</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>jpn</language><creationdate>1992</creationdate><topic>Animals</topic><topic>Antiemetics - metabolism</topic><topic>Binding, Competitive</topic><topic>Bridged Bicyclo Compounds - metabolism</topic><topic>Bridged Bicyclo Compounds, Heterocyclic</topic><topic>Cerebral Cortex - metabolism</topic><topic>Granisetron</topic><topic>In Vitro Techniques</topic><topic>Indazoles - metabolism</topic><topic>Male</topic><topic>Ondansetron - metabolism</topic><topic>Oxazines - metabolism</topic><topic>Rats</topic><topic>Rats, Wistar</topic><topic>Receptors, Serotonin - metabolism</topic><topic>Synaptic Membranes - metabolism</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>SAKAMORI, Masamitsu</creatorcontrib><creatorcontrib>TAKEHARA, Shuzo</creatorcontrib><creatorcontrib>SETOGUCHI, Michihide</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>Folia Pharmacologica Japonica</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>SAKAMORI, Masamitsu</au><au>TAKEHARA, Shuzo</au><au>SETOGUCHI, Michihide</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>High affinity binding of Y-25130 for serotonin 3 receptor</atitle><jtitle>Folia Pharmacologica Japonica</jtitle><addtitle>Nihon Yakurigaku Zasshi</addtitle><date>1992-08-01</date><risdate>1992</risdate><volume>100</volume><issue>2</issue><spage>137</spage><epage>142</epage><pages>137-142</pages><issn>0015-5691</issn><eissn>1347-8397</eissn><abstract>The binding of Y-25130 on serotonin 3 (5-HT3) receptors was evaluated by examining its effect on 3H-BRL 43694 (3H-granisetron) binding to rat cerebral cortex membranes in comparison with those of granisetron, ondansetron and metoclopramide. Y-25130, granisetron, ondansetron, metoclopramide, 5-HT and 2-methyl-5-HT displaced the specific binding of 3H-granisetron to the synaptosomal membranes in a concentration-dependent manner. The rank order of potency for inhibition of 3H-granisetron binding by the test compounds was Y-25130≅granisetron > ondansetron> 2-methyl- 5-HT≅5-HT≅metoclopramide. To determine the manner of interaction between Y-25130 and 5-HT3 receptors, Scatchard analysis of 3H-granisetron specific binding to the membranes of the cerebral cortex in the absence or presence of various concentrations of Y-25130 was performed. It was indicated that Y-25130 exerted a typical competitive-type inhibition of 3H-granisetron binding. The present study indicates that Y-25130 binds competitively to 5-HT3 receptors with high affinity.</abstract><cop>Japan</cop><pub>The Japanese Pharmacological Society</pub><pmid>1330854</pmid><doi>10.1254/fpj.100.137</doi><tpages>6</tpages><oa>free_for_read</oa></addata></record> |
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| identifier | ISSN: 0015-5691 |
| ispartof | Folia Pharmacologica Japonica, 1992/08/01, Vol.100(2), pp.137-142 |
| issn | 0015-5691 1347-8397 |
| language | jpn |
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| source | MEDLINE; Elektronische Zeitschriftenbibliothek - Frei zugängliche E-Journals |
| subjects | Animals Antiemetics - metabolism Binding, Competitive Bridged Bicyclo Compounds - metabolism Bridged Bicyclo Compounds, Heterocyclic Cerebral Cortex - metabolism Granisetron In Vitro Techniques Indazoles - metabolism Male Ondansetron - metabolism Oxazines - metabolism Rats Rats, Wistar Receptors, Serotonin - metabolism Synaptic Membranes - metabolism |
| title | High affinity binding of Y-25130 for serotonin 3 receptor |
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