Synthesis and central none-opioid analgesic activity of SIPI5047
Compound SIPI5047 was synthesize by using piperazine as starting material in five reaction steps, and its central none-opioid analgesic activity was studied. Its analgesic activity, pharmacological mechanism, action type and drug dependence were well studied in vivo and in vitro. The results show th...
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| Veröffentlicht in: | Yao hsüeh hsüeh pao 2008-06, Vol.43 (6), p.611 |
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| container_title | Yao hsüeh hsüeh pao |
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| creator | Li, Jian-Qi Huang, Li-Ying Chen, Xin-Jian Weng, Zhi-Jie Zhang, Chun-Nian |
| description | Compound SIPI5047 was synthesize by using piperazine as starting material in five reaction steps, and its central none-opioid analgesic activity was studied. Its analgesic activity, pharmacological mechanism, action type and drug dependence were well studied in vivo and in vitro. The results show that SIPI5047 has potent analgesic activities in vivo, which is quite similar to morphine and also much more powerful than paracetamol. SIPI5047 has no efficacy to reduce fever or inflammation, but has an obvious action on central nervous system. SIPI5057 has no apparent affinity with the mu-receptor and it is an antagonist that acts on the polyamine site of the NMDA receptor. SIPI5057 appears no drug dependence. SIPI5047 is a novel central none-opioid analgesic agent and more worthy of further research as a new drug candidate. |
| format | Article |
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Its analgesic activity, pharmacological mechanism, action type and drug dependence were well studied in vivo and in vitro. The results show that SIPI5047 has potent analgesic activities in vivo, which is quite similar to morphine and also much more powerful than paracetamol. SIPI5047 has no efficacy to reduce fever or inflammation, but has an obvious action on central nervous system. SIPI5057 has no apparent affinity with the mu-receptor and it is an antagonist that acts on the polyamine site of the NMDA receptor. SIPI5057 appears no drug dependence. SIPI5047 is a novel central none-opioid analgesic agent and more worthy of further research as a new drug candidate.</description><identifier>ISSN: 0513-4870</identifier><identifier>PMID: 18822964</identifier><language>chi</language><publisher>China</publisher><subject>Analgesics - chemical synthesis ; Analgesics - pharmacology ; Analgesics - toxicity ; Animals ; Female ; Male ; Mice ; Motor Activity - drug effects ; Pain Measurement - methods ; Piperazines - chemical synthesis ; Piperazines - pharmacology ; Piperazines - toxicity ; Random Allocation ; Rats ; Rats, Sprague-Dawley ; Receptors, N-Methyl-D-Aspartate - antagonists & inhibitors ; Receptors, Opioid, mu - metabolism ; Substance-Related Disorders - etiology</subject><ispartof>Yao hsüeh hsüeh pao, 2008-06, Vol.43 (6), p.611</ispartof><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,776,780</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/18822964$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Li, Jian-Qi</creatorcontrib><creatorcontrib>Huang, Li-Ying</creatorcontrib><creatorcontrib>Chen, Xin-Jian</creatorcontrib><creatorcontrib>Weng, Zhi-Jie</creatorcontrib><creatorcontrib>Zhang, Chun-Nian</creatorcontrib><title>Synthesis and central none-opioid analgesic activity of SIPI5047</title><title>Yao hsüeh hsüeh pao</title><addtitle>Yao Xue Xue Bao</addtitle><description>Compound SIPI5047 was synthesize by using piperazine as starting material in five reaction steps, and its central none-opioid analgesic activity was studied. Its analgesic activity, pharmacological mechanism, action type and drug dependence were well studied in vivo and in vitro. The results show that SIPI5047 has potent analgesic activities in vivo, which is quite similar to morphine and also much more powerful than paracetamol. SIPI5047 has no efficacy to reduce fever or inflammation, but has an obvious action on central nervous system. SIPI5057 has no apparent affinity with the mu-receptor and it is an antagonist that acts on the polyamine site of the NMDA receptor. SIPI5057 appears no drug dependence. SIPI5047 is a novel central none-opioid analgesic agent and more worthy of further research as a new drug candidate.</description><subject>Analgesics - chemical synthesis</subject><subject>Analgesics - pharmacology</subject><subject>Analgesics - toxicity</subject><subject>Animals</subject><subject>Female</subject><subject>Male</subject><subject>Mice</subject><subject>Motor Activity - drug effects</subject><subject>Pain Measurement - methods</subject><subject>Piperazines - chemical synthesis</subject><subject>Piperazines - pharmacology</subject><subject>Piperazines - toxicity</subject><subject>Random Allocation</subject><subject>Rats</subject><subject>Rats, Sprague-Dawley</subject><subject>Receptors, N-Methyl-D-Aspartate - antagonists & inhibitors</subject><subject>Receptors, Opioid, mu - metabolism</subject><subject>Substance-Related Disorders - etiology</subject><issn>0513-4870</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2008</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNo1j11LwzAYRnMxcXP6F0b-QODNR_smd5PhR2GgML0eaZJqRpeWJgr99w7UqwcOhwPPgqyg4pIpjbAkNzmfABQ3Ul-TJddaCFOrFdke5lQ-Q46Z2uSpC6lMtqdpSIENYxyiv3Dbf1wMR60r8TuWmQ4dPTSvTQUKb8lVZ_sc7v52Td4fH952z2z_8tTs7vds5EIVpsA4A642tUVwaFqUWnjVdj7I2nDphUPHPYCxSkneIaLnAaoKURgtW7kmm9_u-NWegz-OUzzbaT7-X5E_vtNCaA</recordid><startdate>200806</startdate><enddate>200806</enddate><creator>Li, Jian-Qi</creator><creator>Huang, Li-Ying</creator><creator>Chen, Xin-Jian</creator><creator>Weng, Zhi-Jie</creator><creator>Zhang, Chun-Nian</creator><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope></search><sort><creationdate>200806</creationdate><title>Synthesis and central none-opioid analgesic activity of SIPI5047</title><author>Li, Jian-Qi ; Huang, Li-Ying ; Chen, Xin-Jian ; Weng, Zhi-Jie ; Zhang, Chun-Nian</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-p124t-409c90c696a70c79b7382d4bfde36913d2c7c1d009a4431f777d1e055772983b3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>chi</language><creationdate>2008</creationdate><topic>Analgesics - chemical synthesis</topic><topic>Analgesics - pharmacology</topic><topic>Analgesics - toxicity</topic><topic>Animals</topic><topic>Female</topic><topic>Male</topic><topic>Mice</topic><topic>Motor Activity - drug effects</topic><topic>Pain Measurement - methods</topic><topic>Piperazines - chemical synthesis</topic><topic>Piperazines - pharmacology</topic><topic>Piperazines - toxicity</topic><topic>Random Allocation</topic><topic>Rats</topic><topic>Rats, Sprague-Dawley</topic><topic>Receptors, N-Methyl-D-Aspartate - antagonists & inhibitors</topic><topic>Receptors, Opioid, mu - metabolism</topic><topic>Substance-Related Disorders - etiology</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Li, Jian-Qi</creatorcontrib><creatorcontrib>Huang, Li-Ying</creatorcontrib><creatorcontrib>Chen, Xin-Jian</creatorcontrib><creatorcontrib>Weng, Zhi-Jie</creatorcontrib><creatorcontrib>Zhang, Chun-Nian</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><jtitle>Yao hsüeh hsüeh pao</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Li, Jian-Qi</au><au>Huang, Li-Ying</au><au>Chen, Xin-Jian</au><au>Weng, Zhi-Jie</au><au>Zhang, Chun-Nian</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Synthesis and central none-opioid analgesic activity of SIPI5047</atitle><jtitle>Yao hsüeh hsüeh pao</jtitle><addtitle>Yao Xue Xue Bao</addtitle><date>2008-06</date><risdate>2008</risdate><volume>43</volume><issue>6</issue><spage>611</spage><pages>611-</pages><issn>0513-4870</issn><abstract>Compound SIPI5047 was synthesize by using piperazine as starting material in five reaction steps, and its central none-opioid analgesic activity was studied. Its analgesic activity, pharmacological mechanism, action type and drug dependence were well studied in vivo and in vitro. The results show that SIPI5047 has potent analgesic activities in vivo, which is quite similar to morphine and also much more powerful than paracetamol. SIPI5047 has no efficacy to reduce fever or inflammation, but has an obvious action on central nervous system. SIPI5057 has no apparent affinity with the mu-receptor and it is an antagonist that acts on the polyamine site of the NMDA receptor. SIPI5057 appears no drug dependence. SIPI5047 is a novel central none-opioid analgesic agent and more worthy of further research as a new drug candidate.</abstract><cop>China</cop><pmid>18822964</pmid></addata></record> |
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| ispartof | Yao hsüeh hsüeh pao, 2008-06, Vol.43 (6), p.611 |
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| language | chi |
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| source | MEDLINE; Alma/SFX Local Collection |
| subjects | Analgesics - chemical synthesis Analgesics - pharmacology Analgesics - toxicity Animals Female Male Mice Motor Activity - drug effects Pain Measurement - methods Piperazines - chemical synthesis Piperazines - pharmacology Piperazines - toxicity Random Allocation Rats Rats, Sprague-Dawley Receptors, N-Methyl-D-Aspartate - antagonists & inhibitors Receptors, Opioid, mu - metabolism Substance-Related Disorders - etiology |
| title | Synthesis and central none-opioid analgesic activity of SIPI5047 |
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