Molecular structure of R-(−)-Rolipram, CAS Number: 85416-75-7
R-(−)-Rolipram (CAS 85416-75-7)
Application:
R-(−)-Rolipram is a PDE IV inhibitor and anti-inflammatory agent
CAS Number:
85416-75-7
Molecular Weight:
275.34
Molecular Formula:
C16H21NO3
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
R-(−)-Rolipram is the R-entantiomer of rolipram. This compound has been shown to strongly inhibit the catalytic activities of PDE4 (phosphodiesterase 4), which is selective for cAMP, an important secondary messenger molecule in signal transduction. Experiments have revealed that high-affinity binding sites require residues within the catalytic domains and residues flanking the N-/C-terminal to the catalytic region of amino acids. Other studies suggest that the deactivation of PDE4 has been reported to affect other cellular functions.
R-(−)-Rolipram (CAS 85416-75-7) References
- Characterization of r-[11C]rolipram for PET imaging of phosphodieterase-4: in vivo binding, metabolism, and dosimetry studies in rats. | Lourenco, CM., et al. 2001. Nucl Med Biol. 28: 347-58. PMID: 11395307
- Coexpression of human cAMP-specific phosphodiesterase activity and high affinity rolipram binding in yeast. | Torphy, TJ., et al. 1992. J Biol Chem. 267: 1798-804. PMID: 1309798
- Behaviour of [11C]R(-)- and [11C]S(+)-rolipram in vitro and in vivo, and their use as PET radiotracers for the quantificative assay of PDE4. | Parker, CA., et al. 2005. Synapse. 55: 270-9. PMID: 15668983
- In vivo selective binding of (R)-[11C]rolipram to phosphodiesterase-4 provides the basis for studying intracellular cAMP signaling in the myocardium and other peripheral tissues. | Kenk, M., et al. 2007. Nucl Med Biol. 34: 71-7. PMID: 17210463
- PET measurement of the in vivo affinity of 11C-(R)-rolipram and the density of its target, phosphodiesterase-4, in the brains of conscious and anesthetized rats. | Itoh, T., et al. 2009. J Nucl Med. 50: 749-56. PMID: 19372471
- PET of (R)-11C-rolipram binding to phosphodiesterase-4 is reproducible and sensitive to increased norepinephrine in the rat heart. | Thomas, AJ., et al. 2011. J Nucl Med. 52: 263-9. PMID: 21270457
- Analysis of (R)- and (S)-[(11)C]rolipram kinetics in canine myocardium for the evaluation of phosphodiesterase-4 with PET. | Lortie, M., et al. 2012. Mol Imaging Biol. 14: 225-36. PMID: 21424298
- PET measurements of cAMP-mediated phosphodiesterase-4 with (R)-[11C]rolipram. | Kenk, M., et al. 2011. Curr Radiopharm. 4: 44-58. PMID: 22191614
- Multistep continuous-flow synthesis of (R)- and (S)-rolipram using heterogeneous catalysts. | Tsubogo, T., et al. 2015. Nature. 520: 329-32. PMID: 25877201
- Prevention by phosphodiesterase inhibitors of antigen-induced contraction of guinea-pig colonic smooth muscle. | Grous, M. and Barnette, M. 1994. Br J Pharmacol. 111: 259-63. PMID: 7516803
- Inhibition of antigen-induced bronchoconstriction and eosinophil infiltration in the guinea pig by the cyclic AMP-specific phosphodiesterase inhibitor, rolipram. | Underwood, DC., et al. 1993. J Pharmacol Exp Ther. 266: 306-13. PMID: 8392555
- Detailed characterization of a purified type 4 phosphodiesterase, HSPDE4B2B: differentiation of high- and low-affinity (R)-rolipram binding. | Rocque, WJ., et al. 1997. Protein Expr Purif. 9: 191-202. PMID: 9056484
- Inhibitory effects of rolipram on partially purified phosphodiesterase 4 from rat brains. | Ohsawa, F., et al. 1998. Jpn J Pharmacol. 77: 147-54. PMID: 9681571
Inhibitor of:
PDE.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
R-(−)-Rolipram, 5 mg | sc-201199 | 5 mg | $158.00 |