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Rolipram

Cayman Chemical Item Number 10011132

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

Rolipram (CAS 61413-54-5)

See more	Inhibitors (546) Allergy/Asthma (98) Arthritis (32) Bone-Related Research (35) Immunology (187) Inflammation (396) Neuroscience (725)

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	Copy SMILES to clipboard 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
Bulk	Contact
		Cart Total	$0.00

Pricing updated 2012-05-25. Prices are subject to change without notice.

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