Abstract
We tested whether the hydantoin muscle relaxants dantrolene, azumolene, or aminodantrolene could alter the binding of [ 3H]PN200-110 to transverse tubule dihydropyridine receptors or the binding of [ 3H]ryanodine to junctional sarcoplasmic reticulum Ca 2+ release channels. All three drugs inhibited [ 3H]PN200-110 binding with azumolene (IC 50≈20 μM) 3–5 times more potent than dantrolene or aminodantrolene. In contrast, 100 μM azumolene and dantrolene produced a small inhibition of [ 3H]ryanodine binding (<25%) while amino- dantrolene was essentially inert. Hence there was a preferential interaction of hydantoins with dihydropyrdine receptors instead of ryanodine receptors. Skeletal muscle dihydropyridine receptors may participate in the mechanism of action of dantrolene and azumolene.
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More From: Biochemical and Biophysical Research Communications
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