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
Hauptverfasser: Jones, Gary L., Amato, Robert J., Wimbish, Gary H., Peyton, Gaylon A.
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container_title Journal of pharmaceutical sciences
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creator Jones, Gary L.
Amato, Robert J.
Wimbish, Gary H.
Peyton, Gaylon A.
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. 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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. 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ispartof Journal of pharmaceutical sciences, 1981-06, Vol.70 (6), p.618-620
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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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