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PiclamilastCat. No. 4525 |
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Alternative Name: RP 73401 Chemical Name: 3-(Cyclopentyloxy)-N-(3,5-dichloro-4-pyridinyl)-4-methoxybenzamide |
Biological Activity
Potent and selective inhibitor of phosphodiesterase (PDE) 4 (IC50 = 1 nM at PDE4 from human neutrophils). Displays >19,000-fold selectivity over other PDE isoenzymes. Exhibits anti-inflammatory effects in models of allergic inflammation. Also inhibits LTB4 synthesis in human neutrophils (IC50 = 2 nM).Certificate of Analysis / Safety Data Sheet
References
Raeburn et al (1994) Anti-inflammatory and bronchodilator properties of RP 73401, a novel and selective phosphodiesterase type IV inhibitor. Br.J.Pharmacol. 113 1423. PMID: 7889300.
Hatzelmann and Schudt (2001) Anti-inflammatory and immunomodulatory potential of the novel PDE4 inhibitor roflumilast in vitro. J.Pharmacol.Exp.Ther. 297 267. PMID: 11259554.
Zhao et al (2003) Inhibitor binding to type 4 phosphodiesterase (PDE4) assessed using [3H]piclamilast and [3H]rolipram. J.Pharmacol.Exp.Ther. 305 565. PMID: 12704225.
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Keywords: Piclamilast, supplier, RP73401, phosphodiesterases, pde4, potent, selective, inhibitors
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