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
Hauptverfasser: Ellis, K.O., Castellion, A.W., Honkomp, L.J., Wessels, F.L., Carpenter, J.F., Halliday, R.P.
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container_end_page 951
container_issue 6
container_start_page 948
container_title Journal of pharmaceutical sciences
container_volume 62
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.
doi_str_mv 10.1002/jps.2600620619
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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. 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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 &amp; 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. ; 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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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