S- (+)-Rolipram 85416-73-5

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Molecular Weight:

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






Biological Activity


S-(+)-Rolipram suppresses LPS-induced TNFα expression from human monocyte through inhibiting PDE4 with IC50 about 2 μM. 1 μM S-(+)-Rolipram significantly antagonizes ovalbumin (OA) induced
concentration-related contractions of tracheal rings which are isolated
from OA-sensitized guinea pigs. S-(+)-Rolipram inhibits
PDE4 activity in a CHO-K1 cell line which stably expresses a recombinant
full length human PDE-4a with IC50 at 450 nM.


Treatment
of the human glioma cell line A-172 with Rolipram (including both R- and
S-enantiomers of Rolipram) results in increased expression of the cell
cycle Inhibitors p21 [Cip1] and p27 [Kip1], and
decreased activity of cdk2, a cyclindependent kinase essential for cell
cycle progression.


As a result, the proliferation of A-172 cells is
inhibited, with induction of a G1 block. Eventually, Rolipram-treated
A-172 cells undergo differentiation, which is followed by apoptotic cell
death.


In anesthetized, ventilated OA-sensitive guinea pigs, S-(+)-Rolipram
reduces OA-induced bronchoconstriction with ID50 values of approximately
0.25 mg/kg i.v. Histamine- and leukotriene D4-induced
bronchoconstriction are not affected by doses of S-(+)-Rolipram which
abolishes the response to OA. Higher doses (3-10 mg/kg) reduce
histamine-, but not the leukotriene D4-induced bronchoconstriction.


In
conscious OA-sensitive guinea pigs, intragastric pretreatment with
S-(+)-Rolipram dose-dependently reduces both the OA-induced decreases in
specific conductance as well as the corresponding pulmonary eosinophil
influx as assessed by both bronchoalveolar lavage and histological
evaluation.

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