5-[4-methoxy-3-[(2S)-norbornan-2-yl]oxy-phenyl]-1,3-diazinan-2-one

Uses

CP 80633 is a selective inhibitor of phosphodiesterase type 4.

Uses

Phosphodiesterases (PDE) enzymatically convert the cyclic nucleotide second messengers cAMP and cGMP to 5’-AMP and 5’-GMP, respectively, thus terminating signal transduction. The cAMP-specific PDE4 isoforms may be particularly important in certain respiratory and neurological diseases. CP 80,633 is a selective inhibitor of PDE4 (IC50 = 1.27 μM for PDE4 versus. >100 μM for PDE1, PDE2, PDE3, and PDE5). It potentiates PGE1-dependent increases in cAMP levels in eosinophils, monocytes, and T-cells, inhibits eosinophil superoxide production (IC50 < 0.6 μM), and blocks LPS-induced TNF-α release from monocytes (IC50 = 0.22 μM). CP 80,633 (1 mg/kg) significantly reduces antigen-induced airway inflammation in atopic guinea pigs, monkeys, and mice.[Cayman Chemical]

Definition

ChEBI: 2(1h)-pyrimidinone, 5-[3-[(1s,2s,4r)-bicyclo[2.2.1]hept-2-yloxy]-4-methoxyphenyl]tetrahydro- is a monoterpenoid.

Biological Activity

Selective inhibitor of phosphodiesterase type 4 (IC 50 values are 1.9, > 100, > 100, > 100 and > 100 μ M for human lung PDE4, lung PDE1, lung PDE2, heart PDE3 and platelet PDE-V respectively) that displays no significant PDE4 isozyme selectivity. Inhibits hydrolysis of cAMP in isolated human peripheral blood monocytes, eosinophils and T cells.? Displays anti-inflammatory and bronchodilatory effects in vivo .