Ionophoretic and inhibitory action of the analgesic, diflunisal, on sarcoplasmic reticulum.
Diflunisal decreased the ATP-dependent transport rate and calcium accumulation by the sarcoplasmic reticulum. Inhibition of calcium transport by diflunisal was pH dependent, and a pKa of 6.7 to 6.9 was observed for the carboxylic acid group. In sealed sarcoplasmic reticulum vesicles, diflunisal at concentrations below 1 mM increased the rate of Ca2+-dependent hydrolysis of ATP; above 1 mM, the Ca2+-ATPase activity was inhibited. In purified Ca2+-ATPase, diflunisal acted only as an inhibitor. Methylation of the phenolic group of diflunisal eliminated both its analgesic and ionophoretic properties.[1]References
- Ionophoretic and inhibitory action of the analgesic, diflunisal, on sarcoplasmic reticulum. Holguín, J.A. Biochem. Pharmacol. (1988) [Pubmed]
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