A PDE4 inhibitor
(–)-Rolipram is a phosphodiesterase 4 (PDE4) inhibitor (IC50 = 0.22 ?M for the guinea pig eosinophil enzyme) and an enantiomer of (±)-rolipram .1 It enhances isoprenaline-induced cAMP accumulation in isolated guinea pig eosinophils (EC50 = 0.19 ?M). (–)-Rolipram (1-1,000 ?M) inhibits TNF and INF-γ production in L1402 CD4+ encephalitogenic rat T cells.2 It inhibits ovalbumin-induced contraction of tracheal rings isolated from ovalbumin-sensitized guinea pigs when used at a concentration of 1 ?M.3 (–)-Rolipram inhibits ovalbumin-induced bronchoconstriction in guinea pigs (ED50 = 0.25 mg/kg).
1.Souness, J.E., and Scott, L.C.Stereospecificity of rolipram actions on eosinophil cyclic AMP-specific phosphodiesteraseBiochem. J.291(Pt 1)(Pt 2)389-395(1993) 2.Sommer, N., L?shmann, P.-A., Northoff, G.H., et al.The antidepressant rolipram suppresses cytokine production and prevents autoimmune encephalomyelitisNat. Med.1(3)244-248(1995) 3.Underwood, D.C., Osborn, R.R., Novak, L.B., et al.Inhibition of antigen-induced bronchoconstriction and eosinophil infiltration in the guinea pig by the cyclic AMP-specific phosphodiesterase inhibitor, rolipramJ. Pharmacol. Exp. Ther.266(1)306-313(1993)
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