A 33 是一种具有口服活性的选择性 PDE4B 抑制剂，IC50 为 15 nM。
Potent and selective PDE4B inhibitor (IC50 = 15 nM); exhibits >100-fold selectivity for PDE4B over 4D. Regulates cAMP in inflammatory cells. Inhibits LPS-induced TNF-α production and neutrophil accumulation in mouse lungs. Reduces microglial and neutrophil activation, and improves behavioral deficits in a traumatic brain injury model in vivo. Also exhibits antidepressant-like effects. Orally bioavailable.
Naganuma et al (2009) Discovery of selective PDE4B inhibitors. Bioorg.Med.Chem.Lett. 19 3174 PMID:19447034 |Zhang et al (2017) Comparison of the pharmacological profiles of selective PDE4B and PDE4D inhibitors in the central nervous system. Sci.Rep. 7 40115 PMID:28054669 |Wilson et al (2017) Therapeutic benefits of phosphodiesterase 4B inhibition after traumatic brain injury. PLoS One 12 e0178013 PMID:28542295
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