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Neurotropic effects of the optical isomers of the selective adenosine cyclic 3′,5′‐monophosphate phosphodiesterase inhibitor rolipram in rats in‐vivo

The efficacy of the selective adenosine cyclic 3′,5′‐monophosphate (cAMP) phosphodiesterase (PDE) inhibitor (±)‐rolipram and its optical isomers (0·006 to 25 mg kg−1) in inducing characteristic behavioural changes like hypothermia, hypoactivity, forepaw shaking, grooming and head twitches in rats has been examined. (+)‐Rolipram was found some 15 times less potent than the racemate suggesting a stereoselective interaction with a rat brain cAMP phosphodiesterase isoenzyme. Following their intracerebral administration, the stereoisomers also demonstrated their unusual potency ratio. These findings suggested that (+)‐rolipram is a less potent neurotropic PDE inhibitor in‐vivo than its (‐)‐enantiomer.