rolipram

Rolipram (SB 95952) is a phosphodiesterase 4 inhibitor with antidepressant properties.

(S)-(+)-Rolipram ((+)-Rolipram) inhibits human monocyte cyclic AMP-specific PDE4 with an IC50 of 0.75 μM and exhibits anti-inflammatory and anti-depressant activity in the central nervous system, though it is less potent than its R enantiomer.

(R)-(-)-Rolipram ((-)-Rolipram) is an R-enantiomer of Rolipram which is a PDE4 inhibitor.

Bemoradan is an inhibitor of the rolipram-insensitive cyclic AMP phosphodiesterase from canine heart tissue

PDE4-IN-9 (Compound 5j) is a potent PDE4 inhibitor with an IC50 value of 1.4 μM against PDE4 in vitro enzyme assays, which is lower than the 2.0 μM of parent rolipram, and demonstrates good in vivo activity in LPS-induced animal models of asthma COPD and sepsis [1].

NEO214, an autophagy inhibitor and a covalent conjugate of the PDE4 inhibitor Rolipram and perillyl alcohol, exhibits anti-cancer activity and blood-brain barrier (BBB) permeability. It prevents autophagy-lysosome fusion, blocking autophagic flux and triggering glioma cell death via mTOR activation and TFEB (Transcription Factor EB) aggregation. NEO214 inhibition of Macroautophagy autophagy in glioblastoma cells may overcome chemotherapy resistance in glioblastoma [1].