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Neuropharmacological profile of l -pGlu-(1-benzyl)- l -His- l -ProNH2 , a newer thyrotropin-releasing hormone analog: Effects on seizure models, sodium current, cerebral blood flow and behavioral parameters
Summary In the present study, l -pGlu-(1-benzyl)- l -His- l -ProNH2 (NP-355), a newer CNS active thyrotropin-releasing hormone (TRH) analog was evaluated for its antiepileptic potential. NP-355 (5, 10 and 20 μmol/kg; i.v.) pretreatment significantly delayed onset and reduced the frequency of convuls...
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| Published in: | Epilepsy research 2009-12, Vol.87 (2), p.223-233 |
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| container_end_page | 233 |
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| container_start_page | 223 |
| container_title | Epilepsy research |
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| creator | Rajput, Satyendra Kumar Singh, Jitendra Narain Ingole, Shubhada Jain, Gaurav Kaur, Navneet Monga, Vikramdeep Meena, Chhuttan Lal Jain, Rahul Sharma, Shyam Sunder |
| description | Summary In the present study, l -pGlu-(1-benzyl)- l -His- l -ProNH2 (NP-355), a newer CNS active thyrotropin-releasing hormone (TRH) analog was evaluated for its antiepileptic potential. NP-355 (5, 10 and 20 μmol/kg; i.v.) pretreatment significantly delayed onset and reduced the frequency of convulsions in pentylenetetrazole-induced seizures. NP-355 was also found to be protective against picrotoxin- and kainic acid-induced seizures. Maximum electroshock-induced seizures were not protected even at 20 μmol/kg in mice. Effects of NP-355 on functional observation battery did not exhibit any undesirable effects. Moreover, the antiepileptic activity produced by NP-355 was observed without significantly altering mean arterial blood pressure. NP-355 significantly increases the CBF to 17 ± 3% as compared to saline (6 ± 2%). NP-355 (100, 300 and 1000 μM) produces a concentration-dependent depression (16%, 63% and 77%, respectively) of the peak sodium current. NP-355 did not alter neurobehavioral parameters. This study demonstrates that NP-355 has potential antiepileptic activity and devoid of undesirable effects. |
| doi_str_mv | 10.1016/j.eplepsyres.2009.09.007 |
| format | article |
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NP-355 (5, 10 and 20 μmol/kg; i.v.) pretreatment significantly delayed onset and reduced the frequency of convulsions in pentylenetetrazole-induced seizures. NP-355 was also found to be protective against picrotoxin- and kainic acid-induced seizures. Maximum electroshock-induced seizures were not protected even at 20 μmol/kg in mice. Effects of NP-355 on functional observation battery did not exhibit any undesirable effects. Moreover, the antiepileptic activity produced by NP-355 was observed without significantly altering mean arterial blood pressure. NP-355 significantly increases the CBF to 17 ± 3% as compared to saline (6 ± 2%). NP-355 (100, 300 and 1000 μM) produces a concentration-dependent depression (16%, 63% and 77%, respectively) of the peak sodium current. NP-355 did not alter neurobehavioral parameters. This study demonstrates that NP-355 has potential antiepileptic activity and devoid of undesirable effects.</description><identifier>ISSN: 0920-1211</identifier><identifier>EISSN: 1872-6844</identifier><identifier>DOI: 10.1016/j.eplepsyres.2009.09.007</identifier><identifier>PMID: 19833480</identifier><language>eng</language><publisher>Netherlands: Elsevier B.V</publisher><subject>Analysis of Variance ; Animals ; Anticonvulsants - administration & dosage ; Behavior, Animal - drug effects ; Blood Pressure - drug effects ; Brain - drug effects ; Brain - physiopathology ; Cardiovascular system ; Cerebral blood flow ; Cerebrovascular Circulation - drug effects ; Dose-Response Relationship, Drug ; DRG neurons ; Electrophysiology ; Electroshock ; Functional observation battery ; Ganglia, Spinal - cytology ; Ganglia, Spinal - drug effects ; Kainic Acid - toxicity ; Male ; Mice ; Motor Activity - drug effects ; Neurology ; Neurons - drug effects ; Pentylenetetrazole - toxicity ; Picrotoxin - toxicity ; Rats ; Rats, Sprague-Dawley ; Seizure ; Seizures - drug therapy ; Seizures - etiology ; Sodium current ; Statistics, Nonparametric ; Thyrotropin-Releasing Hormone - administration & dosage ; Thyrotropin-Releasing Hormone - analogs & derivatives</subject><ispartof>Epilepsy research, 2009-12, Vol.87 (2), p.223-233</ispartof><rights>Elsevier B.V.</rights><rights>2009 Elsevier B.V.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c343t-519bde794892fae9857496b94992dadbae2981b54824ac917a7b39aba8fa06483</citedby><cites>FETCH-LOGICAL-c343t-519bde794892fae9857496b94992dadbae2981b54824ac917a7b39aba8fa06483</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>315,783,787,27936,27937</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/19833480$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Rajput, Satyendra Kumar</creatorcontrib><creatorcontrib>Singh, Jitendra Narain</creatorcontrib><creatorcontrib>Ingole, Shubhada</creatorcontrib><creatorcontrib>Jain, Gaurav</creatorcontrib><creatorcontrib>Kaur, Navneet</creatorcontrib><creatorcontrib>Monga, Vikramdeep</creatorcontrib><creatorcontrib>Meena, Chhuttan Lal</creatorcontrib><creatorcontrib>Jain, Rahul</creatorcontrib><creatorcontrib>Sharma, Shyam Sunder</creatorcontrib><title>Neuropharmacological profile of l -pGlu-(1-benzyl)- l -His- l -ProNH2 , a newer thyrotropin-releasing hormone analog: Effects on seizure models, sodium current, cerebral blood flow and behavioral parameters</title><title>Epilepsy research</title><addtitle>Epilepsy Res</addtitle><description>Summary In the present study, l -pGlu-(1-benzyl)- l -His- l -ProNH2 (NP-355), a newer CNS active thyrotropin-releasing hormone (TRH) analog was evaluated for its antiepileptic potential. NP-355 (5, 10 and 20 μmol/kg; i.v.) pretreatment significantly delayed onset and reduced the frequency of convulsions in pentylenetetrazole-induced seizures. NP-355 was also found to be protective against picrotoxin- and kainic acid-induced seizures. Maximum electroshock-induced seizures were not protected even at 20 μmol/kg in mice. Effects of NP-355 on functional observation battery did not exhibit any undesirable effects. Moreover, the antiepileptic activity produced by NP-355 was observed without significantly altering mean arterial blood pressure. NP-355 significantly increases the CBF to 17 ± 3% as compared to saline (6 ± 2%). NP-355 (100, 300 and 1000 μM) produces a concentration-dependent depression (16%, 63% and 77%, respectively) of the peak sodium current. NP-355 did not alter neurobehavioral parameters. This study demonstrates that NP-355 has potential antiepileptic activity and devoid of undesirable effects.</description><subject>Analysis of Variance</subject><subject>Animals</subject><subject>Anticonvulsants - administration & dosage</subject><subject>Behavior, Animal - drug effects</subject><subject>Blood Pressure - drug effects</subject><subject>Brain - drug effects</subject><subject>Brain - physiopathology</subject><subject>Cardiovascular system</subject><subject>Cerebral blood flow</subject><subject>Cerebrovascular Circulation - drug effects</subject><subject>Dose-Response Relationship, Drug</subject><subject>DRG neurons</subject><subject>Electrophysiology</subject><subject>Electroshock</subject><subject>Functional observation battery</subject><subject>Ganglia, Spinal - cytology</subject><subject>Ganglia, Spinal - drug effects</subject><subject>Kainic Acid - toxicity</subject><subject>Male</subject><subject>Mice</subject><subject>Motor Activity - drug effects</subject><subject>Neurology</subject><subject>Neurons - drug effects</subject><subject>Pentylenetetrazole - toxicity</subject><subject>Picrotoxin - toxicity</subject><subject>Rats</subject><subject>Rats, Sprague-Dawley</subject><subject>Seizure</subject><subject>Seizures - drug therapy</subject><subject>Seizures - etiology</subject><subject>Sodium current</subject><subject>Statistics, Nonparametric</subject><subject>Thyrotropin-Releasing Hormone - administration & dosage</subject><subject>Thyrotropin-Releasing Hormone - analogs & derivatives</subject><issn>0920-1211</issn><issn>1872-6844</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2009</creationdate><recordtype>article</recordtype><recordid>eNqNUtFqFDEUHUSxtfoLkjcVdtYkk91JfBC01K5QqqA-hyRzp5s1MxlvZlq2H-k3mXEXCj4JFy4k555zuecUBWF0yShbv90tYQgwpD1CWnJK1XIuWj8qTpmsebmWQjwuTqnitGScsZPiWUo7mhFUiKfFCVOyqoSkp8Xva5gwDluDnXExxBvvTCADxtYHILElgZTDZZjK16y00N_vw5tyftv49Ld_xXi94WRBDOnhDpCM2z3GMVP6vkQIYJLvb8g2Yhd7IKY3WeMduWhbcGMisScJ_P2EQLrYQEgLkmLjp464CRH6cUEcIFjMS9kQY0PaEO8yTUMsbM2tj_PPYNB0MAKm58WT1oQEL479rPjx6eL7-aa8-nL5-fzDVekqUY3liinbQK2EVLw1oOSqFmptlVCKN6axBriSzK6E5MI4xWpT20oZa2Rr6FrI6qx4deDNl_o1QRp155ODEEwPcUq6rgRbVbKmGSkPSIcxJYRWD-g7g3vNqJ7N1Dv9YKaezdRz0TqPvjyKTLaD5mHw6F4GfDwA8uHg1gPq5Dz0DhqP-by6if5_VN7_Q-KC7-cY_IQ9pF2cMJuWNNOJa6q_zaGaM0UVpXzFRPUHq2nNvg</recordid><startdate>200912</startdate><enddate>200912</enddate><creator>Rajput, Satyendra Kumar</creator><creator>Singh, Jitendra Narain</creator><creator>Ingole, Shubhada</creator><creator>Jain, Gaurav</creator><creator>Kaur, Navneet</creator><creator>Monga, Vikramdeep</creator><creator>Meena, Chhuttan Lal</creator><creator>Jain, Rahul</creator><creator>Sharma, Shyam Sunder</creator><general>Elsevier B.V</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>200912</creationdate><title>Neuropharmacological profile of l -pGlu-(1-benzyl)- l -His- l -ProNH2 , a newer thyrotropin-releasing hormone analog: Effects on seizure models, sodium current, cerebral blood flow and behavioral parameters</title><author>Rajput, Satyendra Kumar ; Singh, Jitendra Narain ; Ingole, Shubhada ; Jain, Gaurav ; Kaur, Navneet ; Monga, Vikramdeep ; Meena, Chhuttan Lal ; Jain, Rahul ; Sharma, Shyam Sunder</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c343t-519bde794892fae9857496b94992dadbae2981b54824ac917a7b39aba8fa06483</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2009</creationdate><topic>Analysis of Variance</topic><topic>Animals</topic><topic>Anticonvulsants - administration & dosage</topic><topic>Behavior, Animal - drug effects</topic><topic>Blood Pressure - drug effects</topic><topic>Brain - drug effects</topic><topic>Brain - physiopathology</topic><topic>Cardiovascular system</topic><topic>Cerebral blood flow</topic><topic>Cerebrovascular Circulation - drug effects</topic><topic>Dose-Response Relationship, Drug</topic><topic>DRG neurons</topic><topic>Electrophysiology</topic><topic>Electroshock</topic><topic>Functional observation battery</topic><topic>Ganglia, Spinal - cytology</topic><topic>Ganglia, Spinal - drug effects</topic><topic>Kainic Acid - toxicity</topic><topic>Male</topic><topic>Mice</topic><topic>Motor Activity - drug effects</topic><topic>Neurology</topic><topic>Neurons - drug effects</topic><topic>Pentylenetetrazole - toxicity</topic><topic>Picrotoxin - toxicity</topic><topic>Rats</topic><topic>Rats, Sprague-Dawley</topic><topic>Seizure</topic><topic>Seizures - drug therapy</topic><topic>Seizures - etiology</topic><topic>Sodium current</topic><topic>Statistics, Nonparametric</topic><topic>Thyrotropin-Releasing Hormone - administration & dosage</topic><topic>Thyrotropin-Releasing Hormone - analogs & derivatives</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Rajput, Satyendra Kumar</creatorcontrib><creatorcontrib>Singh, Jitendra Narain</creatorcontrib><creatorcontrib>Ingole, Shubhada</creatorcontrib><creatorcontrib>Jain, Gaurav</creatorcontrib><creatorcontrib>Kaur, Navneet</creatorcontrib><creatorcontrib>Monga, Vikramdeep</creatorcontrib><creatorcontrib>Meena, Chhuttan Lal</creatorcontrib><creatorcontrib>Jain, Rahul</creatorcontrib><creatorcontrib>Sharma, Shyam Sunder</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>Epilepsy research</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Rajput, Satyendra Kumar</au><au>Singh, Jitendra Narain</au><au>Ingole, Shubhada</au><au>Jain, Gaurav</au><au>Kaur, Navneet</au><au>Monga, Vikramdeep</au><au>Meena, Chhuttan Lal</au><au>Jain, Rahul</au><au>Sharma, Shyam Sunder</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Neuropharmacological profile of l -pGlu-(1-benzyl)- l -His- l -ProNH2 , a newer thyrotropin-releasing hormone analog: Effects on seizure models, sodium current, cerebral blood flow and behavioral parameters</atitle><jtitle>Epilepsy research</jtitle><addtitle>Epilepsy Res</addtitle><date>2009-12</date><risdate>2009</risdate><volume>87</volume><issue>2</issue><spage>223</spage><epage>233</epage><pages>223-233</pages><issn>0920-1211</issn><eissn>1872-6844</eissn><abstract>Summary In the present study, l -pGlu-(1-benzyl)- l -His- l -ProNH2 (NP-355), a newer CNS active thyrotropin-releasing hormone (TRH) analog was evaluated for its antiepileptic potential. NP-355 (5, 10 and 20 μmol/kg; i.v.) pretreatment significantly delayed onset and reduced the frequency of convulsions in pentylenetetrazole-induced seizures. NP-355 was also found to be protective against picrotoxin- and kainic acid-induced seizures. Maximum electroshock-induced seizures were not protected even at 20 μmol/kg in mice. Effects of NP-355 on functional observation battery did not exhibit any undesirable effects. Moreover, the antiepileptic activity produced by NP-355 was observed without significantly altering mean arterial blood pressure. NP-355 significantly increases the CBF to 17 ± 3% as compared to saline (6 ± 2%). NP-355 (100, 300 and 1000 μM) produces a concentration-dependent depression (16%, 63% and 77%, respectively) of the peak sodium current. NP-355 did not alter neurobehavioral parameters. This study demonstrates that NP-355 has potential antiepileptic activity and devoid of undesirable effects.</abstract><cop>Netherlands</cop><pub>Elsevier B.V</pub><pmid>19833480</pmid><doi>10.1016/j.eplepsyres.2009.09.007</doi><tpages>11</tpages></addata></record> |
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| ispartof | Epilepsy research, 2009-12, Vol.87 (2), p.223-233 |
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| subjects | Analysis of Variance Animals Anticonvulsants - administration & dosage Behavior, Animal - drug effects Blood Pressure - drug effects Brain - drug effects Brain - physiopathology Cardiovascular system Cerebral blood flow Cerebrovascular Circulation - drug effects Dose-Response Relationship, Drug DRG neurons Electrophysiology Electroshock Functional observation battery Ganglia, Spinal - cytology Ganglia, Spinal - drug effects Kainic Acid - toxicity Male Mice Motor Activity - drug effects Neurology Neurons - drug effects Pentylenetetrazole - toxicity Picrotoxin - toxicity Rats Rats, Sprague-Dawley Seizure Seizures - drug therapy Seizures - etiology Sodium current Statistics, Nonparametric Thyrotropin-Releasing Hormone - administration & dosage Thyrotropin-Releasing Hormone - analogs & derivatives |
| title | Neuropharmacological profile of l -pGlu-(1-benzyl)- l -His- l -ProNH2 , a newer thyrotropin-releasing hormone analog: Effects on seizure models, sodium current, cerebral blood flow and behavioral parameters |
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