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Rolipram attenuates bleomycin A5‐induced pulmonary fibrosis in rats
Respirology, 2009ABSTRACTBackground and objective: Pulmonary fibrosis has a poor prognosis. The pathogenesis of fibrotic disorders is unclear, but the extent of lung damage due to persistent inflammation is regarded as a critical factor. Rolipram inhibits inflammation induced by various stimuli, as well as the chemotaxis of fibroblasts.
Yu Hong Hou, Guojun Zhang, Jin Bing Pan
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Pharmacokinetics of (+)-rolipram and (?)-rolipram in healthy volunteers
European Journal of Clinical Pharmacology, 1990Plasma levels of S-(+)-rolipram and R-(-)-rolipram in six healthy male volunteers were measured by radioimmunoassay after intravenous injection of 0.1 mg and oral administration of 1.0 mg of the pure enantiomers. Following i.v. treatment, plasma levels of both isomers declined in three phases, with half-lives of 0.2 h, 0.6-0.9 h and 6-8 h.
W. Krause, G. Kühne, N. Sauerbrey
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HETEROCYCLES, 2003
AbstractFor Abstract see ChemInform Abstract in Full Text.
Shui-Tein Chen+3 more
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AbstractFor Abstract see ChemInform Abstract in Full Text.
Shui-Tein Chen+3 more
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Efficient synthesis of (−)-(R)- and (+)-(S)-rolipram
Tetrahedron Letters, 2017Abstract A novel, efficient and protecting group free enantioselective synthetic approach of (−)-( R )- 1 and (+)-( S )-rolipram 2 is described employing the organocatalyzed asymmetric Michael addition, Henry condensation, Wittig olefination and reductive lactamization reactions as key steps.
Satyendra Kumar Pandey, Ramandeep Kaur
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Pharmacokinetics of the Antidepressant Rolipram in Healthy Volunteers
Xenobiotica, 19891. The pharmacokinetics of rolipram were studied in healthy male volunteers using 3H-rolipram and a radioimmunoassay for measurement of unchanged drug. 2. Rolipram was rapidly and completely absorbed after an oral dose of 1 mg. Bioavailability was 73%. 3. Plasma levels of the unchanged drug declined with a terminal half-life of 2 h. The total clearance
W. Krause, H. Matthes, G Kühne
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2006 IEEE Nuclear Science Symposium Conference Record, 2006
The PET tracers (R)-[11C] rolipram and (S)-[11C] rolipram have been proposed to measure phosphodiesterase-4 (PDE4) density as an indirect index of cAMP-mediated cell signaling, which is altered in many cardiac pathologies. The aim of this study was to determine which of the following models (if any) describe the kinetics of these tracers in normal dog ...
R.S. Beanlands+5 more
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The PET tracers (R)-[11C] rolipram and (S)-[11C] rolipram have been proposed to measure phosphodiesterase-4 (PDE4) density as an indirect index of cAMP-mediated cell signaling, which is altered in many cardiac pathologies. The aim of this study was to determine which of the following models (if any) describe the kinetics of these tracers in normal dog ...
R.S. Beanlands+5 more
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Effects of rolipram on in vivo dopamine receptor binding [PDF]
In order to clarify whether changes in brain concentrations of the second messenger cyclic AMP (cAMP) affect in vivo receptor binding in the brain, the effects of rolipram, a selective inhibitor of phosphodiesterase type 4 (PDE(4)), on dopamine receptor binding in the mouse brain were studied.
Hosoi, R+6 more
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Rolipram inhibition of phosphodiesterase-4 activation
European Journal of Pharmacology: Molecular Pharmacology, 1995Rolipram inhibited U937 cell phosphodiesterase-4 in either the presence or absence of saturating (100 micrograms/ml) phosphatidic acid in an apparently phospholipid-independent manner, exhibiting similar kinetics (Ki values = 0.41 and 0.59 microM, respectively).
Richard J. Heaslip, Michael E. DiSanto
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