Relationship between the brain levels and the anticonvulsant activity of denzimol after its acute and repeated administration to mice
The relationship between the brain concentration of denzimol and its anticonvulsant activity was studied in mice after acute and repeated administration (14 days) of this drug to mice. Anticonvulsant activity was assessed against maximal electroshock seizures (MES). When denzimol was administered at...
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| Veröffentlicht in: | Pharmacological research communications 1987-02, Vol.19 (2), p.153-161 |
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| container_title | Pharmacological research communications |
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| creator | Abbiati, G.A. Restelli, G.V. Schiavi, S. Ceserani, R. Testa, R. |
| description | The relationship between the brain concentration of denzimol and its anticonvulsant activity was studied in mice after acute and repeated administration (14 days) of this drug to mice. Anticonvulsant activity was assessed against maximal electroshock seizures (MES). When denzimol was administered at 30 mg/kg p.o. to repeatedly treated mice, its brain concentration and anticonvulsant activity were reduced in comparison to non-treated mice and
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β was significantly changed from 2.10 to 1.53 hr. Tonic hindlimb extension was completely abolished at a brain denzimol concentration higher than 15 mcg/g, whereas the minimum effective brain concentration was between 2–3 mcg/g both in acute and repeatedly treated animals.
The brain concentration of denzimol is closely correlated with its anticonvulsant effect both in acute and repeatedly treated animals. Futhermore these findings seem to suggest that the decreased anticonvulsant activity of denzimol, following repeated administration, might be due to a development of pharmacokinetic tolerance. |
| doi_str_mv | 10.1016/0031-6989(87)90005-1 |
| format | Article |
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β was significantly changed from 2.10 to 1.53 hr. Tonic hindlimb extension was completely abolished at a brain denzimol concentration higher than 15 mcg/g, whereas the minimum effective brain concentration was between 2–3 mcg/g both in acute and repeatedly treated animals.
The brain concentration of denzimol is closely correlated with its anticonvulsant effect both in acute and repeatedly treated animals. Futhermore these findings seem to suggest that the decreased anticonvulsant activity of denzimol, following repeated administration, might be due to a development of pharmacokinetic tolerance.</description><identifier>ISSN: 0031-6989</identifier><identifier>EISSN: 1879-2936</identifier><identifier>DOI: 10.1016/0031-6989(87)90005-1</identifier><identifier>PMID: 3588651</identifier><language>eng</language><publisher>Orlando, FL: Elsevier B.V</publisher><subject>Animals ; Anticonvulsants - administration & dosage ; Anticonvulsants - metabolism ; Anticonvulsants. Antiepileptics. Antiparkinson agents ; Biological and medical sciences ; Brain - metabolism ; Dose-Response Relationship, Drug ; Drug Administration Schedule ; Electroshock ; Imidazoles - administration & dosage ; Imidazoles - metabolism ; Medical sciences ; Mice ; Neuropharmacology ; Pharmacology. Drug treatments ; Seizures - prevention & control</subject><ispartof>Pharmacological research communications, 1987-02, Vol.19 (2), p.153-161</ispartof><rights>1987</rights><rights>1987 INIST-CNRS</rights><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c417t-7f7b5f208b7b4f5a8438f7d97f16e7f08ad611f7aa20c847f4bc06c46010ffe43</citedby><cites>FETCH-LOGICAL-c417t-7f7b5f208b7b4f5a8438f7d97f16e7f08ad611f7aa20c847f4bc06c46010ffe43</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,776,780,27901,27902</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=8325600$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/3588651$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Abbiati, G.A.</creatorcontrib><creatorcontrib>Restelli, G.V.</creatorcontrib><creatorcontrib>Schiavi, S.</creatorcontrib><creatorcontrib>Ceserani, R.</creatorcontrib><creatorcontrib>Testa, R.</creatorcontrib><title>Relationship between the brain levels and the anticonvulsant activity of denzimol after its acute and repeated administration to mice</title><title>Pharmacological research communications</title><addtitle>Pharmacol Res Commun</addtitle><description>The relationship between the brain concentration of denzimol and its anticonvulsant activity was studied in mice after acute and repeated administration (14 days) of this drug to mice. Anticonvulsant activity was assessed against maximal electroshock seizures (MES). When denzimol was administered at 30 mg/kg p.o. to repeatedly treated mice, its brain concentration and anticonvulsant activity were reduced in comparison to non-treated mice and
t
1
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β was significantly changed from 2.10 to 1.53 hr. Tonic hindlimb extension was completely abolished at a brain denzimol concentration higher than 15 mcg/g, whereas the minimum effective brain concentration was between 2–3 mcg/g both in acute and repeatedly treated animals.
The brain concentration of denzimol is closely correlated with its anticonvulsant effect both in acute and repeatedly treated animals. Futhermore these findings seem to suggest that the decreased anticonvulsant activity of denzimol, following repeated administration, might be due to a development of pharmacokinetic tolerance.</description><subject>Animals</subject><subject>Anticonvulsants - administration & dosage</subject><subject>Anticonvulsants - metabolism</subject><subject>Anticonvulsants. Antiepileptics. Antiparkinson agents</subject><subject>Biological and medical sciences</subject><subject>Brain - metabolism</subject><subject>Dose-Response Relationship, Drug</subject><subject>Drug Administration Schedule</subject><subject>Electroshock</subject><subject>Imidazoles - administration & dosage</subject><subject>Imidazoles - metabolism</subject><subject>Medical sciences</subject><subject>Mice</subject><subject>Neuropharmacology</subject><subject>Pharmacology. Drug treatments</subject><subject>Seizures - prevention & control</subject><issn>0031-6989</issn><issn>1879-2936</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1987</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkUuLFDEURoMoY9v6DxSyENFFaW5VKkltBBl8wYAgug6p5IaJpFJtkmoZ9_5vqx_0Uld53PN9CRxCngJ7DQzEG8Y6aMSghpdKvhoYY30D98gGlByadujEfbK5IA_Jo1J-rMdWALsiV12vlOhhQ_58xWhqmFO5DTs6Yv2FmGi9RTpmExKNuMdYqEnueGlSDXZO-yWWdUuNrWEf6h2dPXWYfodpjtT4ipmGuqbsUvGYzbhDU9FR46aQQqn5-CitM52CxcfkgTex4JPzuiXfP7z_dv2pufny8fP1u5vGcpC1kV6OvW-ZGuXIfW8U75SXbpAeBErPlHECwEtjWmYVl56PlgnLBQPmPfJuS16cend5_rlgqXoKxWKMJuG8FC1lL0DC_0HoGR8GKVeQn0Cb51Iyer3LYTL5TgPTB0364EAfHGgl9VGThjX27Ny_jBO6S-jsZZ0_P89NsSb6bJIN5YKpru3FWrwlb0_Y6gj3AbMuNmCy6EJGW7Wbw7__8Rf3ILDY</recordid><startdate>19870201</startdate><enddate>19870201</enddate><creator>Abbiati, G.A.</creator><creator>Restelli, G.V.</creator><creator>Schiavi, S.</creator><creator>Ceserani, R.</creator><creator>Testa, R.</creator><general>Elsevier B.V</general><general>Academic Press</general><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><scope>7TK</scope><scope>7X8</scope></search><sort><creationdate>19870201</creationdate><title>Relationship between the brain levels and the anticonvulsant activity of denzimol after its acute and repeated administration to mice</title><author>Abbiati, G.A. ; Restelli, G.V. ; Schiavi, S. ; Ceserani, R. ; Testa, R.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c417t-7f7b5f208b7b4f5a8438f7d97f16e7f08ad611f7aa20c847f4bc06c46010ffe43</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1987</creationdate><topic>Animals</topic><topic>Anticonvulsants - administration & dosage</topic><topic>Anticonvulsants - metabolism</topic><topic>Anticonvulsants. Antiepileptics. Antiparkinson agents</topic><topic>Biological and medical sciences</topic><topic>Brain - metabolism</topic><topic>Dose-Response Relationship, Drug</topic><topic>Drug Administration Schedule</topic><topic>Electroshock</topic><topic>Imidazoles - administration & dosage</topic><topic>Imidazoles - metabolism</topic><topic>Medical sciences</topic><topic>Mice</topic><topic>Neuropharmacology</topic><topic>Pharmacology. Drug treatments</topic><topic>Seizures - prevention & control</topic><toplevel>online_resources</toplevel><creatorcontrib>Abbiati, G.A.</creatorcontrib><creatorcontrib>Restelli, G.V.</creatorcontrib><creatorcontrib>Schiavi, S.</creatorcontrib><creatorcontrib>Ceserani, R.</creatorcontrib><creatorcontrib>Testa, R.</creatorcontrib><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><collection>Neurosciences Abstracts</collection><collection>MEDLINE - Academic</collection><jtitle>Pharmacological research communications</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Abbiati, G.A.</au><au>Restelli, G.V.</au><au>Schiavi, S.</au><au>Ceserani, R.</au><au>Testa, R.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Relationship between the brain levels and the anticonvulsant activity of denzimol after its acute and repeated administration to mice</atitle><jtitle>Pharmacological research communications</jtitle><addtitle>Pharmacol Res Commun</addtitle><date>1987-02-01</date><risdate>1987</risdate><volume>19</volume><issue>2</issue><spage>153</spage><epage>161</epage><pages>153-161</pages><issn>0031-6989</issn><eissn>1879-2936</eissn><abstract>The relationship between the brain concentration of denzimol and its anticonvulsant activity was studied in mice after acute and repeated administration (14 days) of this drug to mice. Anticonvulsant activity was assessed against maximal electroshock seizures (MES). When denzimol was administered at 30 mg/kg p.o. to repeatedly treated mice, its brain concentration and anticonvulsant activity were reduced in comparison to non-treated mice and
t
1
2
β was significantly changed from 2.10 to 1.53 hr. Tonic hindlimb extension was completely abolished at a brain denzimol concentration higher than 15 mcg/g, whereas the minimum effective brain concentration was between 2–3 mcg/g both in acute and repeatedly treated animals.
The brain concentration of denzimol is closely correlated with its anticonvulsant effect both in acute and repeatedly treated animals. Futhermore these findings seem to suggest that the decreased anticonvulsant activity of denzimol, following repeated administration, might be due to a development of pharmacokinetic tolerance.</abstract><cop>Orlando, FL</cop><cop>London</cop><pub>Elsevier B.V</pub><pmid>3588651</pmid><doi>10.1016/0031-6989(87)90005-1</doi><tpages>9</tpages></addata></record> |
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| ispartof | Pharmacological research communications, 1987-02, Vol.19 (2), p.153-161 |
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| subjects | Animals Anticonvulsants - administration & dosage Anticonvulsants - metabolism Anticonvulsants. Antiepileptics. Antiparkinson agents Biological and medical sciences Brain - metabolism Dose-Response Relationship, Drug Drug Administration Schedule Electroshock Imidazoles - administration & dosage Imidazoles - metabolism Medical sciences Mice Neuropharmacology Pharmacology. Drug treatments Seizures - prevention & control |
| title | Relationship between the brain levels and the anticonvulsant activity of denzimol after its acute and repeated administration to mice |
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