The use of carbetapentane for spinal anesthesia and use-dependent block of sodium currents
Although carbetapentane produces skin (peripheral) infiltrative analgesia, the underlying mechanism of carbetapentane in local anesthesia is not well understood. The purpose of the study was to examine the effect of carbetapentane on voltage-gated Na+ channels and its efficacy on spinal (central) an...
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| Veröffentlicht in: | European journal of pharmacology 2013-08, Vol.714 (1-3), p.366-372 |
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| container_title | European journal of pharmacology |
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| creator | Leung, Yuk-Man Tzeng, Jann-Inn Kuo, Chang-Shin Chen, Yu-Wen Chu, Chin-Chen Wang, Jhi-Joung |
| description | Although carbetapentane produces skin (peripheral) infiltrative analgesia, the underlying mechanism of carbetapentane in local anesthesia is not well understood. The purpose of the study was to examine the effect of carbetapentane on voltage-gated Na+ channels and its efficacy on spinal (central) anesthesia. We evaluated the effects of carbetapentane on rat motor and pain behavior (when administered intrathecally) and on voltage-gated sodium channels in differentiated neuronal NG108-15 cells. Carbetapentane exhibited dose-dependent spinal blockade with a more sensory-selective action over motor blockade (P |
| doi_str_mv | 10.1016/j.ejphar.2013.07.013 |
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The purpose of the study was to examine the effect of carbetapentane on voltage-gated Na+ channels and its efficacy on spinal (central) anesthesia. We evaluated the effects of carbetapentane on rat motor and pain behavior (when administered intrathecally) and on voltage-gated sodium channels in differentiated neuronal NG108-15 cells. Carbetapentane exhibited dose-dependent spinal blockade with a more sensory-selective action over motor blockade (P<0.05). Carbetapentane was more potent than lidocaine (P<0.05) in spinal anesthesia. Intrathecal 5% dextrose (vehicle) elicited no spinal anesthesia. Lidocaine, used as a positive control, demonstrated concentration- and state-dependent effects on tonic block of voltage-gated Na+ currents (IC50 of 49.6 and 194.6µM at holding potentials of −70 and −100mV, respectively). Carbetapentane was more potent (IC50 of 36.3 and 62.2µM at holding potentials of −70 and −100mV, respectively). Carbetapentane showed a much stronger frequency-dependence of block than lidocaine: with high frequency stimulation (3.33Hz), 50µM lidocaine produced an additional 30% blockade, while the same concentration of carbetapentane produced 70% more block. These results revealed carbetapentane had a more potent and prolonged spinal blockade with a more sensory/nociceptive-selective action over motor blockade in comparison with lidocaine. Spinal anesthesia with carbetapentane could be through inhibition of voltage-gated Na+ currents.</description><identifier>ISSN: 0014-2999</identifier><identifier>EISSN: 1879-0712</identifier><identifier>DOI: 10.1016/j.ejphar.2013.07.013</identifier><identifier>PMID: 23872380</identifier><language>eng</language><publisher>Netherlands: Elsevier B.V</publisher><subject>analgesia ; anesthesia ; Anesthesia, Spinal ; Animals ; Behavior, Animal - drug effects ; Behavior, Animal - physiology ; Carbetapentane ; Cell Line ; Cyclopentanes - pharmacology ; Electrophysiological Phenomena - drug effects ; glucose ; inhibitory concentration 50 ; Intrathecal ; Lidocaine ; Male ; Motor Activity - drug effects ; Motor Activity - physiology ; pain ; pharmacology ; Rats ; Rats, Sprague-Dawley ; sodium ; Sodium - metabolism ; sodium channels ; Sodium currents ; Spinal anesthesia ; Voltage-Gated Sodium Channels - metabolism</subject><ispartof>European journal of pharmacology, 2013-08, Vol.714 (1-3), p.366-372</ispartof><rights>2013 Elsevier B.V.</rights><rights>2013 Elsevier B.V. All rights reserved.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c412t-210ef74445ad7190fb2e001407f824c9d0ccf953527a69c749992a0f29b805473</citedby><cites>FETCH-LOGICAL-c412t-210ef74445ad7190fb2e001407f824c9d0ccf953527a69c749992a0f29b805473</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://www.sciencedirect.com/science/article/pii/S0014299913005232$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,776,780,3536,27903,27904,65309</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/23872380$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Leung, Yuk-Man</creatorcontrib><creatorcontrib>Tzeng, Jann-Inn</creatorcontrib><creatorcontrib>Kuo, Chang-Shin</creatorcontrib><creatorcontrib>Chen, Yu-Wen</creatorcontrib><creatorcontrib>Chu, Chin-Chen</creatorcontrib><creatorcontrib>Wang, Jhi-Joung</creatorcontrib><title>The use of carbetapentane for spinal anesthesia and use-dependent block of sodium currents</title><title>European journal of pharmacology</title><addtitle>Eur J Pharmacol</addtitle><description>Although carbetapentane produces skin (peripheral) infiltrative analgesia, the underlying mechanism of carbetapentane in local anesthesia is not well understood. The purpose of the study was to examine the effect of carbetapentane on voltage-gated Na+ channels and its efficacy on spinal (central) anesthesia. We evaluated the effects of carbetapentane on rat motor and pain behavior (when administered intrathecally) and on voltage-gated sodium channels in differentiated neuronal NG108-15 cells. Carbetapentane exhibited dose-dependent spinal blockade with a more sensory-selective action over motor blockade (P<0.05). Carbetapentane was more potent than lidocaine (P<0.05) in spinal anesthesia. Intrathecal 5% dextrose (vehicle) elicited no spinal anesthesia. Lidocaine, used as a positive control, demonstrated concentration- and state-dependent effects on tonic block of voltage-gated Na+ currents (IC50 of 49.6 and 194.6µM at holding potentials of −70 and −100mV, respectively). Carbetapentane was more potent (IC50 of 36.3 and 62.2µM at holding potentials of −70 and −100mV, respectively). Carbetapentane showed a much stronger frequency-dependence of block than lidocaine: with high frequency stimulation (3.33Hz), 50µM lidocaine produced an additional 30% blockade, while the same concentration of carbetapentane produced 70% more block. These results revealed carbetapentane had a more potent and prolonged spinal blockade with a more sensory/nociceptive-selective action over motor blockade in comparison with lidocaine. Spinal anesthesia with carbetapentane could be through inhibition of voltage-gated Na+ currents.</description><subject>analgesia</subject><subject>anesthesia</subject><subject>Anesthesia, Spinal</subject><subject>Animals</subject><subject>Behavior, Animal - drug effects</subject><subject>Behavior, Animal - physiology</subject><subject>Carbetapentane</subject><subject>Cell Line</subject><subject>Cyclopentanes - pharmacology</subject><subject>Electrophysiological Phenomena - drug effects</subject><subject>glucose</subject><subject>inhibitory concentration 50</subject><subject>Intrathecal</subject><subject>Lidocaine</subject><subject>Male</subject><subject>Motor Activity - drug effects</subject><subject>Motor Activity - physiology</subject><subject>pain</subject><subject>pharmacology</subject><subject>Rats</subject><subject>Rats, Sprague-Dawley</subject><subject>sodium</subject><subject>Sodium - metabolism</subject><subject>sodium channels</subject><subject>Sodium currents</subject><subject>Spinal anesthesia</subject><subject>Voltage-Gated Sodium Channels - metabolism</subject><issn>0014-2999</issn><issn>1879-0712</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2013</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kD-P1DAQxS0E4paFb4AgJU3C2HHWcYOETscf6SQK7hoay7HHrJfsOtgJEt-eiXJQUljPY_1m5vkx9pJDw4Ef3p4aPE1HmxsBvG1ANSSP2I73SteguHjMdgBc1kJrfcWelXICgE6L7im7Em2v6MCOfbs7YrUUrFKonM0DznbCy2wvWIWUqzLFix0rKst8xBItXf3K1x6J84RWw5jcj7W_JB-Xc-WWnOm9PGdPgh0LvnjQPbv_cHN3_am-_fLx8_X729pJLuZacMCgpJSd9YprCIPA1Tio0AvptAfngu7aTih70E5J-o-wEIQeeuikavfszTZ3yunnQkbNORaH40iu01IMl0IfWt1CT6jcUJdTKRmDmXI82_zbcDBrquZktlTNmqoBZUio7dXDhmU4o__X9DdGAl5vQLDJ2O85FnP_lSZ0FLnkHS3fs3cbgZTEr4jZFBfx4tDHjG42PsX_e_gD6SSS2g</recordid><startdate>20130815</startdate><enddate>20130815</enddate><creator>Leung, Yuk-Man</creator><creator>Tzeng, Jann-Inn</creator><creator>Kuo, Chang-Shin</creator><creator>Chen, Yu-Wen</creator><creator>Chu, Chin-Chen</creator><creator>Wang, Jhi-Joung</creator><general>Elsevier B.V</general><scope>FBQ</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>7X8</scope></search><sort><creationdate>20130815</creationdate><title>The use of carbetapentane for spinal anesthesia and use-dependent block of sodium currents</title><author>Leung, Yuk-Man ; Tzeng, Jann-Inn ; Kuo, Chang-Shin ; Chen, Yu-Wen ; Chu, Chin-Chen ; Wang, Jhi-Joung</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c412t-210ef74445ad7190fb2e001407f824c9d0ccf953527a69c749992a0f29b805473</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2013</creationdate><topic>analgesia</topic><topic>anesthesia</topic><topic>Anesthesia, Spinal</topic><topic>Animals</topic><topic>Behavior, Animal - drug effects</topic><topic>Behavior, Animal - physiology</topic><topic>Carbetapentane</topic><topic>Cell Line</topic><topic>Cyclopentanes - pharmacology</topic><topic>Electrophysiological Phenomena - drug effects</topic><topic>glucose</topic><topic>inhibitory concentration 50</topic><topic>Intrathecal</topic><topic>Lidocaine</topic><topic>Male</topic><topic>Motor Activity - drug effects</topic><topic>Motor Activity - physiology</topic><topic>pain</topic><topic>pharmacology</topic><topic>Rats</topic><topic>Rats, Sprague-Dawley</topic><topic>sodium</topic><topic>Sodium - metabolism</topic><topic>sodium channels</topic><topic>Sodium currents</topic><topic>Spinal anesthesia</topic><topic>Voltage-Gated Sodium Channels - metabolism</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Leung, Yuk-Man</creatorcontrib><creatorcontrib>Tzeng, Jann-Inn</creatorcontrib><creatorcontrib>Kuo, Chang-Shin</creatorcontrib><creatorcontrib>Chen, Yu-Wen</creatorcontrib><creatorcontrib>Chu, Chin-Chen</creatorcontrib><creatorcontrib>Wang, Jhi-Joung</creatorcontrib><collection>AGRIS</collection><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>European journal of pharmacology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Leung, Yuk-Man</au><au>Tzeng, Jann-Inn</au><au>Kuo, Chang-Shin</au><au>Chen, Yu-Wen</au><au>Chu, Chin-Chen</au><au>Wang, Jhi-Joung</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>The use of carbetapentane for spinal anesthesia and use-dependent block of sodium currents</atitle><jtitle>European journal of pharmacology</jtitle><addtitle>Eur J Pharmacol</addtitle><date>2013-08-15</date><risdate>2013</risdate><volume>714</volume><issue>1-3</issue><spage>366</spage><epage>372</epage><pages>366-372</pages><issn>0014-2999</issn><eissn>1879-0712</eissn><abstract>Although carbetapentane produces skin (peripheral) infiltrative analgesia, the underlying mechanism of carbetapentane in local anesthesia is not well understood. The purpose of the study was to examine the effect of carbetapentane on voltage-gated Na+ channels and its efficacy on spinal (central) anesthesia. We evaluated the effects of carbetapentane on rat motor and pain behavior (when administered intrathecally) and on voltage-gated sodium channels in differentiated neuronal NG108-15 cells. Carbetapentane exhibited dose-dependent spinal blockade with a more sensory-selective action over motor blockade (P<0.05). Carbetapentane was more potent than lidocaine (P<0.05) in spinal anesthesia. Intrathecal 5% dextrose (vehicle) elicited no spinal anesthesia. Lidocaine, used as a positive control, demonstrated concentration- and state-dependent effects on tonic block of voltage-gated Na+ currents (IC50 of 49.6 and 194.6µM at holding potentials of −70 and −100mV, respectively). Carbetapentane was more potent (IC50 of 36.3 and 62.2µM at holding potentials of −70 and −100mV, respectively). Carbetapentane showed a much stronger frequency-dependence of block than lidocaine: with high frequency stimulation (3.33Hz), 50µM lidocaine produced an additional 30% blockade, while the same concentration of carbetapentane produced 70% more block. These results revealed carbetapentane had a more potent and prolonged spinal blockade with a more sensory/nociceptive-selective action over motor blockade in comparison with lidocaine. Spinal anesthesia with carbetapentane could be through inhibition of voltage-gated Na+ currents.</abstract><cop>Netherlands</cop><pub>Elsevier B.V</pub><pmid>23872380</pmid><doi>10.1016/j.ejphar.2013.07.013</doi><tpages>7</tpages></addata></record> |
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| subjects | analgesia anesthesia Anesthesia, Spinal Animals Behavior, Animal - drug effects Behavior, Animal - physiology Carbetapentane Cell Line Cyclopentanes - pharmacology Electrophysiological Phenomena - drug effects glucose inhibitory concentration 50 Intrathecal Lidocaine Male Motor Activity - drug effects Motor Activity - physiology pain pharmacology Rats Rats, Sprague-Dawley sodium Sodium - metabolism sodium channels Sodium currents Spinal anesthesia Voltage-Gated Sodium Channels - metabolism |
| title | The use of carbetapentane for spinal anesthesia and use-dependent block of sodium currents |
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