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Join us! · InformexUSA 2012 · New Orleans, Louisiana · February 14-17, 2012 · Booth 2514

Rolipram

Cayman Chemical Item Number 10011132

ZK 62711; SB 95952 (CAS 61413-54-5)

Rolipram (CAS 61413-54-5)

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Description

Type 4 cyclic nucleotide phosphodiesterases (PDE4) isoforms selectively inactivate the second messenger cAMP by hydrolyzing the phosphodiester bond, producing AMP. Rolipram is a cell-permeable selective PDE4 inhibitor. Since PDE4 is abundant in leukocytes, rolipram inhibits inflammation by suppressing leukocyte function, inhibiting C5a-stimulated LTC4 synthesis in eosinophils (IC50 = 200 nM),1 and lipopolysaccharide-induced TNF synthesis in monocytes (IC50 = 360 nM).2 Rolipram also enhances neuronal survival,3 has antipsychotic effects in mice,4 and suppresses bone loss in ovariectomized rats.5

1 Tenor, H., Hatzelmann, A., Church, M.K., et al. Effects of theophylline and rolipram on leukotriene C4 (LTC4) synthesis and chemotaxis of human eosinophils from normal and atopic subjects. Br J Pharmacol 118 1727-1735 (1996).

2 Souness, J.E., Griffin, M., Maslen, C., et al. Evidence that cyclic AMP phosphodiesterase inhibitors suppress TNFa generation from human monocytes by interacting with a 'low-affinity' phosphodiesterase 4 conformer. Br J Pharmacol 118 649-658 (1996).

3 Sasaki, T., Kitagawa, K., Omura-Matsuoka, E., et al. The phosphodiesterase inhibitor rolipram promotes survival of newborn hippocampal neurons after ischemia. Stroke 38 1597-1605 (2007).

4 Kanes, S.J., Tokarczyk, J., Siegel, S.J., et al. Rolipram: A specific phosphodiesterase 4 inhibitor with potential antipsychotic activity. Neuroscience 144 239-246 (2007).

5 Yao, W., Tian, X.Y., Chen, J., et al. Rolipram, a phosphodiesterase 4 inhibitor, prevented cancellous and cortical bone loss by inhibiting endosteal bone resorption and maintaining the elevated periosteal bone formation in adult ovariectomized rats. J Musculoskelet Neuronal Interact 7(2) 119-130 (2007).

Synonyms
  • ZK 62711
  • SB 95952
Formal Name 4-​[3-​(cyclopentyloxy)-​4-​methoxyphenyl]-​2-​pyrrolidinone
CAS Number 61413-54-5
Molecular Formula C16H21NO3
Formula Weight 275.3
Formulation A crystalline solid
Purity ≥98%
Stability 2 years
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
SMILES
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COC(C=CC(C1CC(NC1)​=O)​=C2)​=C2OC3CCCC3

Background Reading

Yao, W., Tian, X.Y., Chen, J., et al. Rolipram, a phosphodiesterase 4 inhibitor, prevented cancellous and cortical bone loss by inhibiting endosteal bone resorption and maintaining the elevated periosteal bone formation in adult ovariectomized rats. J Musculoskelet Neuronal Interact 7(2) 119-130 (2007).

Kanes, S.J., Tokarczyk, J., Siegel, S.J., et al. Rolipram: A specific phosphodiesterase 4 inhibitor with potential antipsychotic activity. Neuroscience 144 239-246 (2007).

Sasaki, T., Kitagawa, K., Omura-Matsuoka, E., et al. The phosphodiesterase inhibitor rolipram promotes survival of newborn hippocampal neurons after ischemia. Stroke 38 1597-1605 (2007).

Tenor, H., Hatzelmann, A., Church, M.K., et al. Effects of theophylline and rolipram on leukotriene C4 (LTC4) synthesis and chemotaxis of human eosinophils from normal and atopic subjects. Br J Pharmacol 118 1727-1735 (1996).

Souness, J.E., Griffin, M., Maslen, C., et al. Evidence that cyclic AMP phosphodiesterase inhibitors suppress TNFa generation from human monocytes by interacting with a 'low-affinity' phosphodiesterase 4 conformer. Br J Pharmacol 118 649-658 (1996).

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Size Price Quantity Subtotal
5 mg $22.00 $0.00
10 mg $42.00 $0.00
25 mg $99.00 $0.00
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Cart Total $0.00

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Pricing updated 2012-02-10. Prices are subject to change without notice.

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Warning This product is not for human or veterinary use.

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