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

  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},
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 (*)
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*
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.
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
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).


Site of action of dantrolene in frog sartorius muscle.
Data suggest that dantrolene owes its effect, at least in part, to an inhibition of the "triggering" step in excitation-contraction coupling.
Sodium Nitroprusside: A Review of Its Clinical Effectiveness as a Hypotensive Agent
  • I. Tuzel
  • Medicine
    Journal of clinical pharmacology
  • 1974
Intravenous sodium nitroprusside causes an immediate and potent hypotensivc response, and continuous intravenous infusions of the drug are required to sustain the hypotensive response.
Effect of dantrolene sodium on excitation-contraction coupling in frog skeletal muscle.
The results suggested that dantrolene acts on the membrane of transverse tubules and possibly the triadic junction and that it inhibits the inward movement of Ca and subsequently decreases the release of activator Ca from sarcoplasmic reticulum.
Dantrolene, a direct acting skeletal muscle relaxant.
It is hypothesized that dantrolene causes skeletal muscle relaxation by a direct action on muscle at a site beyond the neuromuscular junction.
Effect of dantrolene sodium on excitation-contraction coupling of frog toe muscle
The possibility that the drug acts mainly by inhibiting the movement of “trigger calcium” which in turn releases calcium from the sarcoplasmic reticulum is discussed.
Reactions of strips of rabbit aorta to epinephrine, isopropylarterenol, sodium nitrite and other drugs.
The relation of the observed curves to theoretical curves predicted by Clark9s equation has been discussed and the time-characteristics of contraction on addition, and of relaxation after washout, of epinephrine and certain other drugs have been described.
Pharmacology of spasticity
This review will assess the pharmacologic features of some of these compounds from a particular point of view-that is, the drugs will be considered for their basic pharmacologic actions on neurons in the spinal cord and in the peripheral spinal reflex apparatus.
Sulfhydryl requirement for relaxation of vascular smooth muscle.
There appears to be two distinct vasodilation responses, one activated by direct interaction with a specific receptor site and not necessarily requiring SH oxidation as a primary event, and a second group of nonspecific vasodilators in which vasodillation is correlated with ability to react with SH groups.