tcsc2617 PMSF

PMSF is an irreversible serine/cysteine protease inhibitor.

In Vitro: PMSF (2 mM) inhibits carbachol-stimulated inositol phosphate accumulation in the presence of Li⁺ by only 15%-19%. PMSF inhibition of phosphoinositide turnover is due to one or more steps following phosphoinositide breakdown^[1]. PMSF inhibits the acylation of the inositol residue of GPI intermediates in bloodstream form T. brucei. PMSF inhihits the formntion of glycolipid C but does not inhibit fatty acid remodeling in vitro. PMSF inhihits GPI acylation and ethanolamine phosphatp addition in procyclic trypanosomes but not in Hela cells^[2].

In Vivo: PMSF (0.1 mL/10 g b.wt, i.p.) produces antinociception as indicated by the dose-responsive increase in % MPE in the tail-flick latency evaluation, but fails to produce a clear dose-responsive inhibition of locomotion. Mice receiving i.p. injections of PMSF exhibit cannabinoid effects that includes antinociception, hypothermia and immobility with ED₅₀ values of 86, 224 and 206 mg/kg, respectively. PMSF (30 mg/kg) pretreatment potentiates the effects of anandamide on tail-flick response (antinociception), spontaneous activity and mobility by 5-, 10- and 8-fold, respectively^[3].