Dantrolene, a Direct Acting Skeletal Muscle Relaxant
Dantrolene causes skeletal muscle relaxation in animals without prominent CNS actions, and it has little or no measurable effect on smooth or cardiac muscle. Dantrolene reduces rigidity in decerebrate cats. Unlike centrally acting muscle relaxants, it has no preferential effect on polysynaptic flexo...
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Veröffentlicht in: | Journal of pharmaceutical sciences 1973-06, Vol.62 (6), p.948-951 |
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creator | Ellis, K.O. Castellion, A.W. Honkomp, L.J. Wessels, F.L. Carpenter, J.F. Halliday, R.P. |
description | Dantrolene causes skeletal muscle relaxation in animals without prominent CNS actions, and it has little or no measurable effect on smooth or cardiac muscle. Dantrolene reduces rigidity in decerebrate cats. Unlike centrally acting muscle relaxants, it has no preferential effect on polysynaptic flexor reflexes and still produces its maximum effect on the muscle twitch in an isolated, neurally intact, perfused hindlimb. Dantrolene blocks the twitch response when stimulated through the motor nerve in a way different from the action of tubocurarine or decamethonium. It inhibits direct twitch responses in denervated muscle and is equally effective in attenuating the direct and indirect twitch responses. It is hypothesized that dantrolene causes skeletal muscle relaxation by a direct action on muscle at a site beyond the neuromuscular junction. |
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Dantrolene reduces rigidity in decerebrate cats. Unlike centrally acting muscle relaxants, it has no preferential effect on polysynaptic flexor reflexes and still produces its maximum effect on the muscle twitch in an isolated, neurally intact, perfused hindlimb. Dantrolene blocks the twitch response when stimulated through the motor nerve in a way different from the action of tubocurarine or decamethonium. It inhibits direct twitch responses in denervated muscle and is equally effective in attenuating the direct and indirect twitch responses. It is hypothesized that dantrolene causes skeletal muscle relaxation by a direct action on muscle at a site beyond the neuromuscular junction.</description><identifier>ISSN: 0022-3549</identifier><identifier>EISSN: 1520-6017</identifier><identifier>DOI: 10.1002/jps.2600620619</identifier><identifier>PMID: 4712630</identifier><language>eng</language><publisher>Washington: Elsevier Inc</publisher><subject>and smooth or cardiac muscle ; Animals ; Blood Pressure - drug effects ; Cats ; Cholinesterase Inhibitors - pharmacology ; CNS ; Dantrolene - administration & dosage ; Dantrolene - pharmacology ; Dantrolene-effects on skeletal muscle ; Dantrolene—effects on skeletal muscle, CNS, and smooth or cardiac muscle ; Decamethonium Compounds - pharmacology ; Dogs ; Dose-Response Relationship, Drug ; Female ; Heart Rate - drug effects ; Hexobarbital - pharmacology ; Hydantoins - pharmacology ; Male ; Mice ; Muscle Contraction - drug effects ; Muscle Relaxants, Central - pharmacology ; Paraldehyde - pharmacology ; Physostigmine - pharmacology ; potential-dantrolene ; proposed site of action ; Rats ; Reflex - drug effects ; Skeletal muscle relaxants ; Skeletal muscle relaxants, potential— dantrolene, proposed site of action ; Sleep - drug effects ; Time Factors ; Tubocurarine - pharmacology</subject><ispartof>Journal of pharmaceutical sciences, 1973-06, Vol.62 (6), p.948-951</ispartof><rights>1973 Wiley‐Liss, Inc., A Wiley Company</rights><rights>Copyright © 1973 Wiley‐Liss, Inc., A Wiley Company</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c4279-8ec00baa2582d433e1c235abd9060a2adf1dc9c31afebb7babe166b6cb2e52ac3</citedby><cites>FETCH-LOGICAL-c4279-8ec00baa2582d433e1c235abd9060a2adf1dc9c31afebb7babe166b6cb2e52ac3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://onlinelibrary.wiley.com/doi/pdf/10.1002%2Fjps.2600620619$$EPDF$$P50$$Gwiley$$H</linktopdf><linktohtml>$$Uhttps://onlinelibrary.wiley.com/doi/full/10.1002%2Fjps.2600620619$$EHTML$$P50$$Gwiley$$H</linktohtml><link.rule.ids>314,778,782,1414,27907,27908,45557,45558</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/4712630$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Ellis, K.O.</creatorcontrib><creatorcontrib>Castellion, A.W.</creatorcontrib><creatorcontrib>Honkomp, L.J.</creatorcontrib><creatorcontrib>Wessels, F.L.</creatorcontrib><creatorcontrib>Carpenter, J.F.</creatorcontrib><creatorcontrib>Halliday, R.P.</creatorcontrib><title>Dantrolene, a Direct Acting Skeletal Muscle Relaxant</title><title>Journal of pharmaceutical sciences</title><addtitle>J. Pharm. Sci</addtitle><description>Dantrolene causes skeletal muscle relaxation in animals without prominent CNS actions, and it has little or no measurable effect on smooth or cardiac muscle. Dantrolene reduces rigidity in decerebrate cats. Unlike centrally acting muscle relaxants, it has no preferential effect on polysynaptic flexor reflexes and still produces its maximum effect on the muscle twitch in an isolated, neurally intact, perfused hindlimb. Dantrolene blocks the twitch response when stimulated through the motor nerve in a way different from the action of tubocurarine or decamethonium. It inhibits direct twitch responses in denervated muscle and is equally effective in attenuating the direct and indirect twitch responses. It is hypothesized that dantrolene causes skeletal muscle relaxation by a direct action on muscle at a site beyond the neuromuscular junction.</description><subject>and smooth or cardiac muscle</subject><subject>Animals</subject><subject>Blood Pressure - drug effects</subject><subject>Cats</subject><subject>Cholinesterase Inhibitors - pharmacology</subject><subject>CNS</subject><subject>Dantrolene - administration & dosage</subject><subject>Dantrolene - pharmacology</subject><subject>Dantrolene-effects on skeletal muscle</subject><subject>Dantrolene—effects on skeletal muscle, CNS, and smooth or cardiac muscle</subject><subject>Decamethonium Compounds - pharmacology</subject><subject>Dogs</subject><subject>Dose-Response Relationship, Drug</subject><subject>Female</subject><subject>Heart Rate - drug effects</subject><subject>Hexobarbital - pharmacology</subject><subject>Hydantoins - pharmacology</subject><subject>Male</subject><subject>Mice</subject><subject>Muscle Contraction - drug effects</subject><subject>Muscle Relaxants, Central - pharmacology</subject><subject>Paraldehyde - pharmacology</subject><subject>Physostigmine - pharmacology</subject><subject>potential-dantrolene</subject><subject>proposed site of action</subject><subject>Rats</subject><subject>Reflex - drug effects</subject><subject>Skeletal muscle relaxants</subject><subject>Skeletal muscle relaxants, potential— dantrolene, proposed site of action</subject><subject>Sleep - drug effects</subject><subject>Time Factors</subject><subject>Tubocurarine - pharmacology</subject><issn>0022-3549</issn><issn>1520-6017</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1973</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkTtPwzAURi0EKuWxsiFlYiLFj8RJRtTyhoJaEGyW7dwiFzcpdsrj32NIBWJATB7u-T5dn4vQDsE9gjE9mM59j3KMOcWcFCuoS1KKY45Jtoq6AaAxS5NiHW14P8UBw2naQZ0kI5Qz3EXJQFaNqy1UsB_JaGAc6CY61I2pHqPxE1hopI2uFl5biEZg5Vvgt9DaRFoP28t3E90dH932T-PL65Oz_uFlrBOaFXEOGmMlJU1zWiaMAdGUpVKVRVhDUllOSKkLzYicgFKZkgoI54prRSGlUrNNtNf2zl39vADfiJnxGqyVFdQLL3JSsIzlNIC9FtSu9t7BRMydmUn3LggWn5pE0CR-NIXA7rJ5oWZQfuNLL2FetPNXY-H9nzZxfjP-1R23WeMbePvOSvckeMayVNwPT0R2MewPL0aFeAh83vIQVL4YcMJrA5WG8usYoqzNX9_4AF7HlVg</recordid><startdate>197306</startdate><enddate>197306</enddate><creator>Ellis, K.O.</creator><creator>Castellion, A.W.</creator><creator>Honkomp, L.J.</creator><creator>Wessels, F.L.</creator><creator>Carpenter, J.F.</creator><creator>Halliday, R.P.</creator><general>Elsevier Inc</general><general>Wiley Subscription Services, Inc., A Wiley Company</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>7X8</scope></search><sort><creationdate>197306</creationdate><title>Dantrolene, a Direct Acting Skeletal Muscle Relaxant</title><author>Ellis, K.O. ; Castellion, A.W. ; Honkomp, L.J. ; Wessels, F.L. ; Carpenter, J.F. ; Halliday, R.P.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c4279-8ec00baa2582d433e1c235abd9060a2adf1dc9c31afebb7babe166b6cb2e52ac3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1973</creationdate><topic>and smooth or cardiac muscle</topic><topic>Animals</topic><topic>Blood Pressure - drug effects</topic><topic>Cats</topic><topic>Cholinesterase Inhibitors - pharmacology</topic><topic>CNS</topic><topic>Dantrolene - administration & dosage</topic><topic>Dantrolene - pharmacology</topic><topic>Dantrolene-effects on skeletal muscle</topic><topic>Dantrolene—effects on skeletal muscle, CNS, and smooth or cardiac muscle</topic><topic>Decamethonium Compounds - pharmacology</topic><topic>Dogs</topic><topic>Dose-Response Relationship, Drug</topic><topic>Female</topic><topic>Heart Rate - drug effects</topic><topic>Hexobarbital - pharmacology</topic><topic>Hydantoins - pharmacology</topic><topic>Male</topic><topic>Mice</topic><topic>Muscle Contraction - drug effects</topic><topic>Muscle Relaxants, Central - pharmacology</topic><topic>Paraldehyde - pharmacology</topic><topic>Physostigmine - pharmacology</topic><topic>potential-dantrolene</topic><topic>proposed site of action</topic><topic>Rats</topic><topic>Reflex - drug effects</topic><topic>Skeletal muscle relaxants</topic><topic>Skeletal muscle relaxants, potential— dantrolene, proposed site of action</topic><topic>Sleep - drug effects</topic><topic>Time Factors</topic><topic>Tubocurarine - pharmacology</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Ellis, K.O.</creatorcontrib><creatorcontrib>Castellion, A.W.</creatorcontrib><creatorcontrib>Honkomp, L.J.</creatorcontrib><creatorcontrib>Wessels, F.L.</creatorcontrib><creatorcontrib>Carpenter, J.F.</creatorcontrib><creatorcontrib>Halliday, R.P.</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>MEDLINE - Academic</collection><jtitle>Journal of pharmaceutical sciences</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Ellis, K.O.</au><au>Castellion, A.W.</au><au>Honkomp, L.J.</au><au>Wessels, F.L.</au><au>Carpenter, J.F.</au><au>Halliday, R.P.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Dantrolene, a Direct Acting Skeletal Muscle Relaxant</atitle><jtitle>Journal of pharmaceutical sciences</jtitle><addtitle>J. Pharm. Sci</addtitle><date>1973-06</date><risdate>1973</risdate><volume>62</volume><issue>6</issue><spage>948</spage><epage>951</epage><pages>948-951</pages><issn>0022-3549</issn><eissn>1520-6017</eissn><abstract>Dantrolene causes skeletal muscle relaxation in animals without prominent CNS actions, and it has little or no measurable effect on smooth or cardiac muscle. Dantrolene reduces rigidity in decerebrate cats. Unlike centrally acting muscle relaxants, it has no preferential effect on polysynaptic flexor reflexes and still produces its maximum effect on the muscle twitch in an isolated, neurally intact, perfused hindlimb. Dantrolene blocks the twitch response when stimulated through the motor nerve in a way different from the action of tubocurarine or decamethonium. It inhibits direct twitch responses in denervated muscle and is equally effective in attenuating the direct and indirect twitch responses. It is hypothesized that dantrolene causes skeletal muscle relaxation by a direct action on muscle at a site beyond the neuromuscular junction.</abstract><cop>Washington</cop><pub>Elsevier Inc</pub><pmid>4712630</pmid><doi>10.1002/jps.2600620619</doi><tpages>4</tpages></addata></record> |
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subjects | and smooth or cardiac muscle Animals Blood Pressure - drug effects Cats Cholinesterase Inhibitors - pharmacology CNS Dantrolene - administration & dosage Dantrolene - pharmacology Dantrolene-effects on skeletal muscle Dantrolene—effects on skeletal muscle, CNS, and smooth or cardiac muscle Decamethonium Compounds - pharmacology Dogs Dose-Response Relationship, Drug Female Heart Rate - drug effects Hexobarbital - pharmacology Hydantoins - pharmacology Male Mice Muscle Contraction - drug effects Muscle Relaxants, Central - pharmacology Paraldehyde - pharmacology Physostigmine - pharmacology potential-dantrolene proposed site of action Rats Reflex - drug effects Skeletal muscle relaxants Skeletal muscle relaxants, potential— dantrolene, proposed site of action Sleep - drug effects Time Factors Tubocurarine - pharmacology |
title | Dantrolene, a Direct Acting Skeletal Muscle Relaxant |
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