A comparison of the potency and specificity of the direct muscle relaxant activity of azumolene and dantrolene

@article{Dhillon1992ACO,
  title={A comparison of the potency and specificity of the direct muscle relaxant activity of azumolene and dantrolene},
  author={D S Dhillon and Schwe Fang Pong and Thomas John Moorehead},
  journal={Drug Development Research},
  year={1992},
  volume={25}
}
Dantrolene is a unique directly acting skeletal muscle relaxant that is clinically useful in the treatment of chronic muscle spasticity and malignant hyperthermia. Azumolene is a new dantrolene‐like drug that has better aqueous solubility and that may also be of use in the treatment of acute muscle spasm. Potency of both compounds was determined in the anesthetized, curarized rat gastrocnemius (using different routes of administration) and the isolated chick biventer muscle preparations. The… 
Identification of Dantrolene Binding Sites in Porcine Skeletal Muscle Sarcoplasmic Reticulum (*)
TLDR
It is suggested that dantrolene inhibits calcium release from the sarcoplasmic reticulum by either direct or indirect interaction with the ryanodine receptor.
Physico-Chemical Characterization and Analytical Development for Sodium Azumolene, a Potential Drug Designed to Fight Malignant Hyperthermia
Sodium azumolene is a drug designed to fight Malignant Hyperthermia (MH), which is characterized by genetic predisposition and triggered by the use of inhalational anesthetics. This drug is shown as
Dantrolene Inhibition of Sarcoplasmic Reticulum Ca2+Release by Direct and Specific Action at Skeletal Muscle Ryanodine Receptors*
TLDR
Evidence is provided of a high-affinity, monophasic inhibition by dantrolene of ryanodine receptor Ca2+ channel function in isolated sarcoplasmic reticulum vesicles prepared from malignant hyperthermia-susceptible and normal pig skeletal muscle and a mechanism of action is suggested in which danterolene may act directly at the skeletal muscle ryanODine receptor complex to limit its activation by calmodulin and Ca2+.
In vitro testing of calcium channel blockers and cytotoxic chemotherapy in B-cell low-grade non-Hodgkin's lymphoma.
TLDR
Dantrolene and azumolene were potent inducers of cell death in both systems reducing the viable cell count by 70-90% in comparison with normal controls and Nimodipine, in comparison, appeared to have no significant effect.
Biochemical and physiological mechanisms of creatine kinase release from avian skeletal muscle during acute stress
TLDR
It is proposed that CK loss occurs as a consequence of Ca2+ mediated alterations in muscle cell membrane permeability, possibly caused by Ca2 + -activated phospholipase A2 (PLA2).

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