Naunyn-Schmiedeberg's Archives of Pharmacology

, Volume 301, Issue 3, pp 237–240 | Cite as

Muscle relaxant properties of the identified metabolites of dantrolene

  • K. O. Ellis
  • F. L. Wessels


Identified metabolites of dantrolene, a skeletal muscle relaxant, were studied for inhibition of skeletal muscle contractions. Inhibition of muscle contractions were studied in vivo in the rat gastrocnemius muscle preparation, and in vitro using isolated rat diaphragm strips. Dantrolene (D) and 5-hydroxydantrolene (5-HD) inhibited muscle contraction responses in a dose dependent manner, both in vivo and in vitro. 5-HD was less potent than D.

Key words

Dantrolene Skeletal muscle relaxant 5-Hydroxydantrolene 


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  1. Birkmayer, W., Danieldzyk, W., Werner, H.: In: DMSO Symposium, Vienna, (G. Laudahn and K. Gerick, eds.). Berlin (West): Saladruck 1966Google Scholar
  2. Conklin, J. D., Sobers, R. J.: Qualitative method for dantrolene and a related metabolite in urine. J. Pharm. Sci. 62, 1024 (1973)Google Scholar
  3. Cox, P. L., Heotis, J. P., Polin, D., Rose, G. M.: Quantitative determination of dantrolene sodium and its metabolites by differential pulse polarography. J. Pharm. Sci. 58, 987 (1969)Google Scholar
  4. Ellis, K. O., Butterfield, J. L., Wessels, F. L., Carpenter, J. F.: A comparison of skeletal, cardiac, and smooth muscle actions of dantrolene sodium—a muscle relaxant. Arch. Int. Pharmacoldyn. Ther. 224, 118 (1976)Google Scholar
  5. Ellis, K. O., Carpenter, J. F.: Studies on the mechanism of action of dantrolene sodium. Naunyn-Schmiedeberg's Arch. Pharmacol. 275, 83 (1972)Google Scholar
  6. Ellis, K. O., Carpenter, J. F.: A comparative study of dantrolene sodium and other skeletal muscle relaxants in the Straub tail mouse. Neuropharmacology 13, 211 (1974)Google Scholar
  7. Ellis, K. O., Castellion, A. W., Honkomp, L. J., Wessels, F. L., Carpenter, J. F., Halliday, R. P.: Dantrolene, a direct acting skeletal muscle relaxant. J. Pharm. Sci. 62, 948 (1973)Google Scholar
  8. Graybill, F. A.: An introduction to linear statistical models, Vol. 1. New York: McGraw-Hill Book Co., Inc. 1961Google Scholar
  9. Hollifield, R. D., Conklin, J. D.: Determination of dantrolene in biological specimens containing drug-related metabolites. J. Pharm. Sci. 62, 271 (1973)Google Scholar
  10. Honkomp, L. J., Halliday, R. P., Wessels, F. L.: Dantrolene, 1-[5-(p-nitrophenyl)furfurylidene]aminohydrantoin, an unique skeletal muscle relaxant. Pharmacologist 12, 301 (1970)Google Scholar
  11. Kligman, A. M.: Topical pharmacology and toxicology of dimethylsulfoxide, Part 1. J. Am. Med. Assoc. 193, 796 (1965a)Google Scholar
  12. Kligman, A. M.: Dimethylsulfoxide, Part 2. J. Am. Med. Assoc. 193, 923 (1965b)Google Scholar
  13. Lietman, P. S., Haslam, R. H. A., Walchar, J. R.: Pharmacology of dantrolene sodium in children. Arch. Phys. Med. Rehabil. 55, 388 (1974)Google Scholar
  14. Maibach, H. E., Feldman, R. J.: The effect of DMSO on percutaneous penetration of hypercortisone and testosterone in man. Ann. N.Y. Acad. Sci. 141, 423 (1967)Google Scholar
  15. Sams, W. M., Jr., Carroll, N. V., Crantz, P. L.: Effect of dimethylsulfoxide on isolated-innervated skeletal, smooth and cardiac muscle. Proc. Soc. Exp. Biol. Med. 122, 103 (1966)Google Scholar
  16. Snedecor, G. W., Cochran, G. W.: Statistical methods, 6th Ed. pp. 432–436 Ames Univ. Iowa Press, 1967Google Scholar
  17. White, R. L., Schwan, T. J.: Synthesis of 5-hydroxy-1-[[5-(p-nitrophenyl)furfurylidene]amino]hydantoin, a metabolite of dantrolene. J. Pharm. Sci. 65, 135 (1976)Google Scholar

Copyright information

© Springer-Verlag 1978

Authors and Affiliations

  • K. O. Ellis
    • 1
  • F. L. Wessels
    • 1
  1. 1.Division of Morton-Norwich Products, Inc.Scientific Affairs Department, Norwich-Eaton PharmaceuticalsNorwichUSA

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