Antihyperalgesic activity of a novel synthesized analogue of lidocaine in diabetic rats
Objectives The purpose of this study was to assess the antinociceptive and antihyperalgesic effects of a lidocaine analogue N‐(2,6‐dichlorophenyl)‐2‐(4‐methyl‐1‐piperidinyl)acetamide (LIA). Methods The structure of LIA was established by elemental analysis and compatible IR, 1H NMR, 13C NMR, and spe...
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Veröffentlicht in: | Journal of pharmacy and pharmacology 2013-05, Vol.65 (5), p.689-696 |
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creator | García-Hernández, Liliana Navarrete-Vázquez, Gabriel González-Trujano, María Eva López-Muñoz, Francisco Javier Déciga-Campos, Myrna |
description | Objectives
The purpose of this study was to assess the antinociceptive and antihyperalgesic effects of a lidocaine analogue N‐(2,6‐dichlorophenyl)‐2‐(4‐methyl‐1‐piperidinyl)acetamide (LIA).
Methods
The structure of LIA was established by elemental analysis and compatible IR, 1H NMR, 13C NMR, and spectral data. Nociceptive and hyperalgesic activity were evaluated in normoglycaemic and streptozocin‐induced diabetic rats using the formalin test. Formalin‐evoked flinching, an indication of nociception and hyperalgesia, was increased in diabetic rats (using 0.5% formalin) compared with nondiabetic rats (using 1% formalin).
Key findings
Local administration of LIA into the dorsal surface of the right hind paw (0.18–5.6 mg per paw) significantly reduced the formalin‐induced nociceptive and hyperalgesic behaviour of nondiabetic and diabetic rat. The antinociceptive effect of LIA was higher than that of lidocaine injection, furthermore this effect was higher than that of gabapentin.
Conclusions
LIA may have potential as a treatment for diabetic hyperalgesia. Further investigations of the antinociceptive mechanisms and the safety of this new compound are necessary. |
doi_str_mv | 10.1111/jphp.12025 |
format | Article |
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The purpose of this study was to assess the antinociceptive and antihyperalgesic effects of a lidocaine analogue N‐(2,6‐dichlorophenyl)‐2‐(4‐methyl‐1‐piperidinyl)acetamide (LIA).
Methods
The structure of LIA was established by elemental analysis and compatible IR, 1H NMR, 13C NMR, and spectral data. Nociceptive and hyperalgesic activity were evaluated in normoglycaemic and streptozocin‐induced diabetic rats using the formalin test. Formalin‐evoked flinching, an indication of nociception and hyperalgesia, was increased in diabetic rats (using 0.5% formalin) compared with nondiabetic rats (using 1% formalin).
Key findings
Local administration of LIA into the dorsal surface of the right hind paw (0.18–5.6 mg per paw) significantly reduced the formalin‐induced nociceptive and hyperalgesic behaviour of nondiabetic and diabetic rat. The antinociceptive effect of LIA was higher than that of lidocaine injection, furthermore this effect was higher than that of gabapentin.
Conclusions
LIA may have potential as a treatment for diabetic hyperalgesia. Further investigations of the antinociceptive mechanisms and the safety of this new compound are necessary.</description><identifier>ISSN: 0022-3573</identifier><identifier>EISSN: 2042-7158</identifier><identifier>DOI: 10.1111/jphp.12025</identifier><identifier>PMID: 23600386</identifier><identifier>CODEN: JPPMAB</identifier><language>eng</language><publisher>England: Blackwell Publishing Ltd</publisher><subject>Amines - pharmacology ; Amines - therapeutic use ; Analgesics - chemistry ; Analgesics - pharmacology ; Analgesics - therapeutic use ; analogue of lidocaine ; Animals ; Behavior, Animal - drug effects ; Cyclohexanecarboxylic Acids - pharmacology ; Cyclohexanecarboxylic Acids - therapeutic use ; Diabetes ; Diabetes Complications - drug therapy ; Diabetes Mellitus, Experimental - complications ; Diabetes Mellitus, Experimental - drug therapy ; diabetic painful neuropathy ; Formaldehyde ; gamma-Aminobutyric Acid - pharmacology ; gamma-Aminobutyric Acid - therapeutic use ; hyperalgesia ; Hyperalgesia - chemically induced ; Hyperalgesia - drug therapy ; Lidocaine - analogs & derivatives ; Lidocaine - chemistry ; Lidocaine - pharmacology ; Lidocaine - therapeutic use ; Molecular Structure ; nociception ; Nociceptive Pain - chemically induced ; Nociceptive Pain - drug therapy ; Pain - chemically induced ; Pain - drug therapy ; Pain Measurement ; Rats ; Reference Values ; Rodents</subject><ispartof>Journal of pharmacy and pharmacology, 2013-05, Vol.65 (5), p.689-696</ispartof><rights>2013 The Authors. JPP © 2013 Royal Pharmaceutical Society</rights><rights>2013 The Authors. JPP © 2013 Royal Pharmaceutical Society.</rights><rights>Copyright © 2013 Royal Pharmaceutical Society</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c3955-402b3f50ba08e5d0162576564772b25fb01170d5151be886331b6df94238dfef3</citedby><cites>FETCH-LOGICAL-c3955-402b3f50ba08e5d0162576564772b25fb01170d5151be886331b6df94238dfef3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://onlinelibrary.wiley.com/doi/pdf/10.1111%2Fjphp.12025$$EPDF$$P50$$Gwiley$$H</linktopdf><linktohtml>$$Uhttps://onlinelibrary.wiley.com/doi/full/10.1111%2Fjphp.12025$$EHTML$$P50$$Gwiley$$H</linktohtml><link.rule.ids>314,780,784,1417,27924,27925,45574,45575</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/23600386$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>García-Hernández, Liliana</creatorcontrib><creatorcontrib>Navarrete-Vázquez, Gabriel</creatorcontrib><creatorcontrib>González-Trujano, María Eva</creatorcontrib><creatorcontrib>López-Muñoz, Francisco Javier</creatorcontrib><creatorcontrib>Déciga-Campos, Myrna</creatorcontrib><title>Antihyperalgesic activity of a novel synthesized analogue of lidocaine in diabetic rats</title><title>Journal of pharmacy and pharmacology</title><addtitle>J Pharm Pharmacol</addtitle><description>Objectives
The purpose of this study was to assess the antinociceptive and antihyperalgesic effects of a lidocaine analogue N‐(2,6‐dichlorophenyl)‐2‐(4‐methyl‐1‐piperidinyl)acetamide (LIA).
Methods
The structure of LIA was established by elemental analysis and compatible IR, 1H NMR, 13C NMR, and spectral data. Nociceptive and hyperalgesic activity were evaluated in normoglycaemic and streptozocin‐induced diabetic rats using the formalin test. Formalin‐evoked flinching, an indication of nociception and hyperalgesia, was increased in diabetic rats (using 0.5% formalin) compared with nondiabetic rats (using 1% formalin).
Key findings
Local administration of LIA into the dorsal surface of the right hind paw (0.18–5.6 mg per paw) significantly reduced the formalin‐induced nociceptive and hyperalgesic behaviour of nondiabetic and diabetic rat. The antinociceptive effect of LIA was higher than that of lidocaine injection, furthermore this effect was higher than that of gabapentin.
Conclusions
LIA may have potential as a treatment for diabetic hyperalgesia. Further investigations of the antinociceptive mechanisms and the safety of this new compound are necessary.</description><subject>Amines - pharmacology</subject><subject>Amines - therapeutic use</subject><subject>Analgesics - chemistry</subject><subject>Analgesics - pharmacology</subject><subject>Analgesics - therapeutic use</subject><subject>analogue of lidocaine</subject><subject>Animals</subject><subject>Behavior, Animal - drug effects</subject><subject>Cyclohexanecarboxylic Acids - pharmacology</subject><subject>Cyclohexanecarboxylic Acids - therapeutic use</subject><subject>Diabetes</subject><subject>Diabetes Complications - drug therapy</subject><subject>Diabetes Mellitus, Experimental - complications</subject><subject>Diabetes Mellitus, Experimental - drug therapy</subject><subject>diabetic painful neuropathy</subject><subject>Formaldehyde</subject><subject>gamma-Aminobutyric Acid - pharmacology</subject><subject>gamma-Aminobutyric Acid - therapeutic use</subject><subject>hyperalgesia</subject><subject>Hyperalgesia - chemically induced</subject><subject>Hyperalgesia - drug therapy</subject><subject>Lidocaine - analogs & derivatives</subject><subject>Lidocaine - chemistry</subject><subject>Lidocaine - pharmacology</subject><subject>Lidocaine - therapeutic use</subject><subject>Molecular Structure</subject><subject>nociception</subject><subject>Nociceptive Pain - chemically induced</subject><subject>Nociceptive Pain - drug therapy</subject><subject>Pain - chemically induced</subject><subject>Pain - drug therapy</subject><subject>Pain Measurement</subject><subject>Rats</subject><subject>Reference Values</subject><subject>Rodents</subject><issn>0022-3573</issn><issn>2042-7158</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2013</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kE1P3DAQhi3UChbKpT-gitQLQgod2_HHHgHBbltEQeLjaDnJhPU2mwQ7AcKvb8IChx6YyxzmeR9pXkK-Ujigw_xYNovmgDJgYoNMGCQsVlToT2QCwFjMheJbZDuEJQAoKeUm2WJcAnAtJ-T2sGrdom_Q2_IOg8sim7XuwbV9VBeRjar6Acso9FW7GK7PmEe2smV91-F4L11eZ9ZVGLkqyp1NsR0M3rbhC_lc2DLg7uveIdenJ1fH8_jsz-zn8eFZnPGpEHECLOWFgNSCRpEDlUwoKWSiFEuZKFKgVEEuqKApai05p6nMi2nCuM4LLPgO2Vt7G1_fdxhas3Ihw7K0FdZdMJRzzaeJgmRAv_-HLuvOD9-MFNMJm1I9UvtrKvN1CB4L03i3sr43FMxYtxnrNi91D_C3V2WXrjB_R9_6HQC6Bh5dif0HKvPrYn7xJo3XGRdafHrPWP_XSMWVMLfnMyNu4PLodP7bzPg_D4eYLA</recordid><startdate>201305</startdate><enddate>201305</enddate><creator>García-Hernández, Liliana</creator><creator>Navarrete-Vázquez, Gabriel</creator><creator>González-Trujano, María Eva</creator><creator>López-Muñoz, Francisco Javier</creator><creator>Déciga-Campos, Myrna</creator><general>Blackwell Publishing Ltd</general><general>Wiley Subscription Services, Inc</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>7QP</scope><scope>7TK</scope><scope>7U9</scope><scope>H94</scope><scope>K9.</scope><scope>M7N</scope><scope>7X8</scope></search><sort><creationdate>201305</creationdate><title>Antihyperalgesic activity of a novel synthesized analogue of lidocaine in diabetic rats</title><author>García-Hernández, Liliana ; Navarrete-Vázquez, Gabriel ; González-Trujano, María Eva ; López-Muñoz, Francisco Javier ; Déciga-Campos, Myrna</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c3955-402b3f50ba08e5d0162576564772b25fb01170d5151be886331b6df94238dfef3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2013</creationdate><topic>Amines - pharmacology</topic><topic>Amines - therapeutic use</topic><topic>Analgesics - chemistry</topic><topic>Analgesics - pharmacology</topic><topic>Analgesics - therapeutic use</topic><topic>analogue of lidocaine</topic><topic>Animals</topic><topic>Behavior, Animal - drug effects</topic><topic>Cyclohexanecarboxylic Acids - pharmacology</topic><topic>Cyclohexanecarboxylic Acids - therapeutic use</topic><topic>Diabetes</topic><topic>Diabetes Complications - drug therapy</topic><topic>Diabetes Mellitus, Experimental - complications</topic><topic>Diabetes Mellitus, Experimental - drug therapy</topic><topic>diabetic painful neuropathy</topic><topic>Formaldehyde</topic><topic>gamma-Aminobutyric Acid - pharmacology</topic><topic>gamma-Aminobutyric Acid - therapeutic use</topic><topic>hyperalgesia</topic><topic>Hyperalgesia - chemically induced</topic><topic>Hyperalgesia - drug therapy</topic><topic>Lidocaine - analogs & derivatives</topic><topic>Lidocaine - chemistry</topic><topic>Lidocaine - pharmacology</topic><topic>Lidocaine - therapeutic use</topic><topic>Molecular Structure</topic><topic>nociception</topic><topic>Nociceptive Pain - chemically induced</topic><topic>Nociceptive Pain - drug therapy</topic><topic>Pain - chemically induced</topic><topic>Pain - drug therapy</topic><topic>Pain Measurement</topic><topic>Rats</topic><topic>Reference Values</topic><topic>Rodents</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>García-Hernández, Liliana</creatorcontrib><creatorcontrib>Navarrete-Vázquez, Gabriel</creatorcontrib><creatorcontrib>González-Trujano, María Eva</creatorcontrib><creatorcontrib>López-Muñoz, Francisco Javier</creatorcontrib><creatorcontrib>Déciga-Campos, Myrna</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>Calcium & Calcified Tissue Abstracts</collection><collection>Neurosciences Abstracts</collection><collection>Virology and AIDS Abstracts</collection><collection>AIDS and Cancer Research Abstracts</collection><collection>ProQuest Health & Medical Complete (Alumni)</collection><collection>Algology Mycology and Protozoology Abstracts (Microbiology C)</collection><collection>MEDLINE - Academic</collection><jtitle>Journal of pharmacy and pharmacology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>García-Hernández, Liliana</au><au>Navarrete-Vázquez, Gabriel</au><au>González-Trujano, María Eva</au><au>López-Muñoz, Francisco Javier</au><au>Déciga-Campos, Myrna</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Antihyperalgesic activity of a novel synthesized analogue of lidocaine in diabetic rats</atitle><jtitle>Journal of pharmacy and pharmacology</jtitle><addtitle>J Pharm Pharmacol</addtitle><date>2013-05</date><risdate>2013</risdate><volume>65</volume><issue>5</issue><spage>689</spage><epage>696</epage><pages>689-696</pages><issn>0022-3573</issn><eissn>2042-7158</eissn><coden>JPPMAB</coden><abstract>Objectives
The purpose of this study was to assess the antinociceptive and antihyperalgesic effects of a lidocaine analogue N‐(2,6‐dichlorophenyl)‐2‐(4‐methyl‐1‐piperidinyl)acetamide (LIA).
Methods
The structure of LIA was established by elemental analysis and compatible IR, 1H NMR, 13C NMR, and spectral data. Nociceptive and hyperalgesic activity were evaluated in normoglycaemic and streptozocin‐induced diabetic rats using the formalin test. Formalin‐evoked flinching, an indication of nociception and hyperalgesia, was increased in diabetic rats (using 0.5% formalin) compared with nondiabetic rats (using 1% formalin).
Key findings
Local administration of LIA into the dorsal surface of the right hind paw (0.18–5.6 mg per paw) significantly reduced the formalin‐induced nociceptive and hyperalgesic behaviour of nondiabetic and diabetic rat. The antinociceptive effect of LIA was higher than that of lidocaine injection, furthermore this effect was higher than that of gabapentin.
Conclusions
LIA may have potential as a treatment for diabetic hyperalgesia. Further investigations of the antinociceptive mechanisms and the safety of this new compound are necessary.</abstract><cop>England</cop><pub>Blackwell Publishing Ltd</pub><pmid>23600386</pmid><doi>10.1111/jphp.12025</doi><tpages>8</tpages></addata></record> |
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subjects | Amines - pharmacology Amines - therapeutic use Analgesics - chemistry Analgesics - pharmacology Analgesics - therapeutic use analogue of lidocaine Animals Behavior, Animal - drug effects Cyclohexanecarboxylic Acids - pharmacology Cyclohexanecarboxylic Acids - therapeutic use Diabetes Diabetes Complications - drug therapy Diabetes Mellitus, Experimental - complications Diabetes Mellitus, Experimental - drug therapy diabetic painful neuropathy Formaldehyde gamma-Aminobutyric Acid - pharmacology gamma-Aminobutyric Acid - therapeutic use hyperalgesia Hyperalgesia - chemically induced Hyperalgesia - drug therapy Lidocaine - analogs & derivatives Lidocaine - chemistry Lidocaine - pharmacology Lidocaine - therapeutic use Molecular Structure nociception Nociceptive Pain - chemically induced Nociceptive Pain - drug therapy Pain - chemically induced Pain - drug therapy Pain Measurement Rats Reference Values Rodents |
title | Antihyperalgesic activity of a novel synthesized analogue of lidocaine in diabetic rats |
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