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
Hauptverfasser: García-Hernández, Liliana, Navarrete-Vázquez, Gabriel, González-Trujano, María Eva, López-Muñoz, Francisco Javier, Déciga-Campos, Myrna
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container_end_page 696
container_issue 5
container_start_page 689
container_title Journal of pharmacy and pharmacology
container_volume 65
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
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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 &amp; 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. 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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 ; 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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 &amp; 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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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source MEDLINE; Access via Wiley Online Library; Oxford University Press Journals All Titles (1996-Current)
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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