Neurotropic effects of the optical isomers of the selective adenosine cyclic 3',5'-monophosphate phosphodiesterase inhibitor rolipram in rats in-vivo.

Abstract

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.

• Authors: H Wachtel
• Journal: The Journal of pharmacy and pharmacology (J Pharm Pharmacol) Vol. 35 Issue 7 Pg. 440-4 (Jul 1983) ISSN: 0022-3573 [Print] England
• PMID: 6136585 (Publication Type: Journal Article)

Chemical References

• Pyrrolidinones
• 3',5'-Cyclic-AMP Phosphodiesterases
• Rolipram

Topics

• 3',5'-Cyclic-AMP Phosphodiesterases (antagonists & inhibitors)
• Animals
• Behavior, Animal (drug effects)
• Body Temperature (drug effects)
• Brain (drug effects)
• Injections, Intraventricular
• Male
• Motor Activity (drug effects)
• Pyrrolidinones (pharmacology)
• Rats
• Rats, Inbred Strains
• Rolipram
• Stereoisomerism