The effect of dantrolene sodium on rat skeletal muscle in relation to the plasma concentration

In Vitro and in Vivo Effects of Dantrolene on Carbonic Anhydrase Enzyme Activities

“…These results showed that there is a correlation between the plasma half-life of dantrolene and inhibition of CA enzyme activity. 30) Our data showed that there is accordance between in vivo and in vitro effects of dantrolene on CA activity.…”

Binding of dantrolene sodium to muscle intracellular membranes

“…Various suggestions have been made as to the possible of action of dantrolene sodium, but one hypothesis that has gained momentum in recent years is that of an inhibition of the release of calcium from muscle intracellular stores, particularly the sarcoplasmic reticulum. On the basis of pharmacological evidence, the existence of an intracellular compartment able to bind dantrolene sodium with high affinity was postulated [9].…”

Brain Penetration of WEB 2086 (Apafant) and Dantrolene in Mdr1a (P-Glycoprotein) and Bcrp Knockout Rats

“…Dantrolene was selected as a specific BCRP substrate based on data from in vitro and in vivo literature (Enokizono et al, 2008;Kodaira et al, 2010;Xiao et al, 2012). Both [ 14 C]WEB 2086 and dantrolene are known to exhibit a short mean residence time (MRT) in rats: MRT of WEB 2086 is 0.44 hour (V. Haeselbarth, G. Schoenfels, and H. Foerster, unpublished data), and MRT of dantrolene was reported to be 0.52 hour by Meyler et al (1979) and 3.1 hours by Karan et al (1996). Thus, it was expected that close to steady-state conditions would be achieved after a combined intravenous infusion of [ 14 C]WEB 2086 and dantrolene for 2 hours, enabling the function of both brain efflux transporters to be assessed in the s This article has supplemental material available at dmd.aspetjournals.org.…”