rolipram

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

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.

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].

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

NEO214 is an autophagy inhibitor obtained by covalently conjugating rolipram, a PDE4 inhibitor, with perillyl alcohol. It possesses anticancer activity and blood-brain barrier (BBB) permeability, blocks autophagosome-lysosome fusion, thereby inhibiting autophagic flux and inducing glioma cell death, which is associated with mTOR activation and aggregation of the transcription factor TFEB. NEO214 inhibits macroautophagy/autophagy in glioblastoma cells and has the potential to overcome chemoresistance in glioblastoma.