| Target Validation Information | |||||
|---|---|---|---|---|---|
| Target ID | T47941 | ||||
| Target Name | PDE4 | ||||
| Target Type | Successful |
||||
| Drug Potency against Target | Cilomilast | Drug Info | IC50 = 120 nM | ||
| Arofylline | Drug Info | IC50 = 5500 nM | [552224] | ||
| Action against Disease Model | Cilomilast | Cilomilast has an IC50 value of 30 nM against PDE4 from U937 cells and inhibits the LPS-induced TNF-a release in whole blood with an IC50 of 7.3 uM. | [552261] | Drug Info | |
| The Effect of Target Knockout, Knockdown or Genetic Variations | Knockout mice showed a significant reduction in prepulse inhibition. Spontaneous locomotor activity was decreased (16%) in knockout mice. Furthermore, when challenged with amphetamine, both groups of mice responded similarly to a low dose of d-amphetamine (1.0 mg/kg), but knockout mice showed an enhanced response to a higher dose (1.78 mg/kg). Decreases in baseline levels ofmonoamines and their metabolites within the striat uM of knockout mice were also observed. Phosphodiesterases(PDE)4B knockout mice showed a modest decrease in immobility time in the forced swim test that approached significance. In several other tests, including the elevated plus maze, hot plate, passive avoidance, and Morris water maze, wild-type and knockout mice performed similarly.These data further support a role for PDE4B in psychiatric diseases and striatal function | ||||
| References | |||||
| Ref 552224 | Phosphodiesterase 4 inhibitors, structurally unrelated to rolipram, as promising agents for the treatment of asthma and other pathologies. Eur J Med Chem. 2000 May;35(5):463-80. | ||||
| Ref 552261 | The next generation of PDE4 inhibitors. Curr Opin Chem Biol. 2001 Aug;5(4):432-8. | ||||
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