Cayman Chemical | Rolipram | Description • ZK 62711; SB 95952 (CAS 61413-54-5)

10011132 Rolipram

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

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• See more Inhibitors; Allergy/Asthma; Arthritis; Bone-Related Research; Immunology; Inflammation; Neuroscience

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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).

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Pricing updated 2010-03-19.
Prices are subject to change without notice.

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Stability of this item is suitable for room temperature overnight shipping. If shipment on ice is desired, it must be requested when the order is placed.