Comparison of Anticonvulsant Potencies of Cyheptamide, Carbamazepine, and Phenytoin
Carbamazepine and cyheptamide have certain stereo-chemical features in common with phenytoin; when superimposed, two bulky hydrophobic groups in each permit the approximate apposition of two electron donor atoms. The anticonvulsant activity of each compound was determined in mice using a standard ma...
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Veröffentlicht in: | Journal of pharmaceutical sciences 1981-06, Vol.70 (6), p.618-620 |
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description | Carbamazepine and cyheptamide have certain stereo-chemical features in common with phenytoin; when superimposed, two bulky hydrophobic groups in each permit the approximate apposition of two electron donor atoms. The anticonvulsant activity of each compound was determined in mice using a standard maximal electroshock procedure, and the relative potencies are expressed in terms of the blood and brain concentrations as well as the intraperitoneal dosage. Although cyheptamide was much less potent than carbamazepine or phenytoin on the basis of intraperitoneal dosage, the difference in potency was much less when blood or brain concentrations were compared. These data should be of value for quantitative structure-activity relationship studies. |
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The anticonvulsant activity of each compound was determined in mice using a standard maximal electroshock procedure, and the relative potencies are expressed in terms of the blood and brain concentrations as well as the intraperitoneal dosage. Although cyheptamide was much less potent than carbamazepine or phenytoin on the basis of intraperitoneal dosage, the difference in potency was much less when blood or brain concentrations were compared. These data should be of value for quantitative structure-activity relationship studies.</description><identifier>ISSN: 0022-3549</identifier><identifier>EISSN: 1520-6017</identifier><identifier>DOI: 10.1002/jps.2600700611</identifier><identifier>PMID: 7252802</identifier><language>eng</language><publisher>Washington: Elsevier Inc</publisher><subject>and phenytoin compared for anticonvulsant activity ; Animals ; Anticonvulsant activity-carbamazepine ; Anticonvulsant activity—carbamazepine, cyheptamide, phenytoin, blood and brain concentrations ; Anticonvulsants - metabolism ; blood and brain concentrations ; Brain - metabolism ; Carbamazepine - pharmacology ; Carbamazepine-anticonvulsant activity ; Carbamazepine—anticonvulsant activity, intraperitoneal dosage, blood and brain concentrations ; cyheptamide ; Cyheptamide-anticonvulsant activity ; Cyheptamide—anticonvulsant activity, intraperitoneal dosage, blood and brain concentrations ; Dibenzocycloheptenes - pharmacology ; Electroshock ; intraperitoneal dosage ; Male ; Mice ; Molecular Conformation ; phenytoin ; Phenytoin - pharmacology ; Phenytoin-anticonvulsant activity ; Phenytoin—anticonvulsant activity, intraperitoneal dosage, blood and brain concentrations ; Structure-Activity Relationship ; Structure-activity relationships-carbamazepine ; Structure-activity relationships—carbamazepine, cyheptamide, and phenytoin compared for anticonvulsant activity</subject><ispartof>Journal of pharmaceutical sciences, 1981-06, Vol.70 (6), p.618-620</ispartof><rights>1981 Wiley-Liss, Inc., A Wiley Company</rights><rights>Copyright © 1981 Wiley‐Liss, Inc., A Wiley Company</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c4271-fa67f72133d3b27ac476bc0e41b9bb9a91cbf5ebef664fcb12e1b08f003701943</citedby><cites>FETCH-LOGICAL-c4271-fa67f72133d3b27ac476bc0e41b9bb9a91cbf5ebef664fcb12e1b08f003701943</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://onlinelibrary.wiley.com/doi/pdf/10.1002%2Fjps.2600700611$$EPDF$$P50$$Gwiley$$H</linktopdf><linktohtml>$$Uhttps://onlinelibrary.wiley.com/doi/full/10.1002%2Fjps.2600700611$$EHTML$$P50$$Gwiley$$H</linktohtml><link.rule.ids>314,776,780,1411,27901,27902,45550,45551</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/7252802$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Jones, Gary L.</creatorcontrib><creatorcontrib>Amato, Robert J.</creatorcontrib><creatorcontrib>Wimbish, Gary H.</creatorcontrib><creatorcontrib>Peyton, Gaylon A.</creatorcontrib><title>Comparison of Anticonvulsant Potencies of Cyheptamide, Carbamazepine, and Phenytoin</title><title>Journal of pharmaceutical sciences</title><addtitle>J. Pharm. Sci</addtitle><description>Carbamazepine and cyheptamide have certain stereo-chemical features in common with phenytoin; when superimposed, two bulky hydrophobic groups in each permit the approximate apposition of two electron donor atoms. The anticonvulsant activity of each compound was determined in mice using a standard maximal electroshock procedure, and the relative potencies are expressed in terms of the blood and brain concentrations as well as the intraperitoneal dosage. Although cyheptamide was much less potent than carbamazepine or phenytoin on the basis of intraperitoneal dosage, the difference in potency was much less when blood or brain concentrations were compared. These data should be of value for quantitative structure-activity relationship studies.</description><subject>and phenytoin compared for anticonvulsant activity</subject><subject>Animals</subject><subject>Anticonvulsant activity-carbamazepine</subject><subject>Anticonvulsant activity—carbamazepine, cyheptamide, phenytoin, blood and brain concentrations</subject><subject>Anticonvulsants - metabolism</subject><subject>blood and brain concentrations</subject><subject>Brain - metabolism</subject><subject>Carbamazepine - pharmacology</subject><subject>Carbamazepine-anticonvulsant activity</subject><subject>Carbamazepine—anticonvulsant activity, intraperitoneal dosage, blood and brain concentrations</subject><subject>cyheptamide</subject><subject>Cyheptamide-anticonvulsant activity</subject><subject>Cyheptamide—anticonvulsant activity, intraperitoneal dosage, blood and brain concentrations</subject><subject>Dibenzocycloheptenes - pharmacology</subject><subject>Electroshock</subject><subject>intraperitoneal dosage</subject><subject>Male</subject><subject>Mice</subject><subject>Molecular Conformation</subject><subject>phenytoin</subject><subject>Phenytoin - pharmacology</subject><subject>Phenytoin-anticonvulsant activity</subject><subject>Phenytoin—anticonvulsant activity, intraperitoneal dosage, blood and brain concentrations</subject><subject>Structure-Activity Relationship</subject><subject>Structure-activity relationships-carbamazepine</subject><subject>Structure-activity relationships—carbamazepine, cyheptamide, and phenytoin compared for anticonvulsant activity</subject><issn>0022-3549</issn><issn>1520-6017</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1981</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkc1v1DAQxS0EKtvClRtSTpzI1h9xvDmWCArVql2xII6W7YxVl8RO7Wzp8tfjKqsiDqin0ej93pPmDUJvCF4SjOnpzZiWtMZYYFwT8gwtCKe4rDERz9EiA7RkvGpeouOUbnBmMOdH6EhQTleYLtC2DcOookvBF8EWZ35yJvi7XZ-Un4pNmMAbB-lBa_fXME5qcB28L1oVtRrUbxidz6vyXbG5Br-fgvOv0Aur-gSvD_MEff_08Vv7uVxfnX9pz9alqaggpVW1sIISxjqmqVCmErU2GCqiG60b1RCjLQcNtq4razShQDReWYyZwKSp2Al6N-eOMdzuIE1ycMlA3ysPYZekYJznM0UGlzNoYkgpgpVjdIOKe0mwfGhR5hbl3xaz4e0heacH6B7xQ21Zb2b9l-th_0SavNhs_8kuZ69LE9w_elX8KWvBBJc_Ls_l5Wa7_ko-VJJlfjXzkKu8cxBlyh_xBjoXwUyyC-5_Z_wB96Ogbg</recordid><startdate>198106</startdate><enddate>198106</enddate><creator>Jones, Gary L.</creator><creator>Amato, Robert J.</creator><creator>Wimbish, Gary H.</creator><creator>Peyton, Gaylon A.</creator><general>Elsevier Inc</general><general>Wiley Subscription Services, Inc., A Wiley Company</general><scope>BSCLL</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>7X8</scope></search><sort><creationdate>198106</creationdate><title>Comparison of Anticonvulsant Potencies of Cyheptamide, Carbamazepine, and Phenytoin</title><author>Jones, Gary L. ; Amato, Robert J. ; Wimbish, Gary H. ; Peyton, Gaylon A.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c4271-fa67f72133d3b27ac476bc0e41b9bb9a91cbf5ebef664fcb12e1b08f003701943</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1981</creationdate><topic>and phenytoin compared for anticonvulsant activity</topic><topic>Animals</topic><topic>Anticonvulsant activity-carbamazepine</topic><topic>Anticonvulsant activity—carbamazepine, cyheptamide, phenytoin, blood and brain concentrations</topic><topic>Anticonvulsants - metabolism</topic><topic>blood and brain concentrations</topic><topic>Brain - metabolism</topic><topic>Carbamazepine - pharmacology</topic><topic>Carbamazepine-anticonvulsant activity</topic><topic>Carbamazepine—anticonvulsant activity, intraperitoneal dosage, blood and brain concentrations</topic><topic>cyheptamide</topic><topic>Cyheptamide-anticonvulsant activity</topic><topic>Cyheptamide—anticonvulsant activity, intraperitoneal dosage, blood and brain concentrations</topic><topic>Dibenzocycloheptenes - pharmacology</topic><topic>Electroshock</topic><topic>intraperitoneal dosage</topic><topic>Male</topic><topic>Mice</topic><topic>Molecular Conformation</topic><topic>phenytoin</topic><topic>Phenytoin - pharmacology</topic><topic>Phenytoin-anticonvulsant activity</topic><topic>Phenytoin—anticonvulsant activity, intraperitoneal dosage, blood and brain concentrations</topic><topic>Structure-Activity Relationship</topic><topic>Structure-activity relationships-carbamazepine</topic><topic>Structure-activity relationships—carbamazepine, cyheptamide, and phenytoin compared for anticonvulsant activity</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Jones, Gary L.</creatorcontrib><creatorcontrib>Amato, Robert J.</creatorcontrib><creatorcontrib>Wimbish, Gary H.</creatorcontrib><creatorcontrib>Peyton, Gaylon A.</creatorcontrib><collection>Istex</collection><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>Journal of pharmaceutical sciences</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Jones, Gary L.</au><au>Amato, Robert J.</au><au>Wimbish, Gary H.</au><au>Peyton, Gaylon A.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Comparison of Anticonvulsant Potencies of Cyheptamide, Carbamazepine, and Phenytoin</atitle><jtitle>Journal of pharmaceutical sciences</jtitle><addtitle>J. Pharm. Sci</addtitle><date>1981-06</date><risdate>1981</risdate><volume>70</volume><issue>6</issue><spage>618</spage><epage>620</epage><pages>618-620</pages><issn>0022-3549</issn><eissn>1520-6017</eissn><abstract>Carbamazepine and cyheptamide have certain stereo-chemical features in common with phenytoin; when superimposed, two bulky hydrophobic groups in each permit the approximate apposition of two electron donor atoms. The anticonvulsant activity of each compound was determined in mice using a standard maximal electroshock procedure, and the relative potencies are expressed in terms of the blood and brain concentrations as well as the intraperitoneal dosage. Although cyheptamide was much less potent than carbamazepine or phenytoin on the basis of intraperitoneal dosage, the difference in potency was much less when blood or brain concentrations were compared. These data should be of value for quantitative structure-activity relationship studies.</abstract><cop>Washington</cop><pub>Elsevier Inc</pub><pmid>7252802</pmid><doi>10.1002/jps.2600700611</doi><tpages>3</tpages></addata></record> |
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subjects | and phenytoin compared for anticonvulsant activity Animals Anticonvulsant activity-carbamazepine Anticonvulsant activity—carbamazepine, cyheptamide, phenytoin, blood and brain concentrations Anticonvulsants - metabolism blood and brain concentrations Brain - metabolism Carbamazepine - pharmacology Carbamazepine-anticonvulsant activity Carbamazepine—anticonvulsant activity, intraperitoneal dosage, blood and brain concentrations cyheptamide Cyheptamide-anticonvulsant activity Cyheptamide—anticonvulsant activity, intraperitoneal dosage, blood and brain concentrations Dibenzocycloheptenes - pharmacology Electroshock intraperitoneal dosage Male Mice Molecular Conformation phenytoin Phenytoin - pharmacology Phenytoin-anticonvulsant activity Phenytoin—anticonvulsant activity, intraperitoneal dosage, blood and brain concentrations Structure-Activity Relationship Structure-activity relationships-carbamazepine Structure-activity relationships—carbamazepine, cyheptamide, and phenytoin compared for anticonvulsant activity |
title | Comparison of Anticonvulsant Potencies of Cyheptamide, Carbamazepine, and Phenytoin |
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