GSK356278 is a potent, selective, brain-penetrant and orally bioavailable phosphodiesterase 4 (PDE4) inhibitor with pIC50 of 8.8 (PDE4B).
GSK356278 equally inhibits PDE4A and PDE4Dwith pIC50 of 8.6 and 8.7, exhibits >100-fold selectivity for PDE4B over the other 10 PDEs.
GSK356278 inhibits LPS-induced release of TNF-α in human whole blood with pIC50 of 7.6, demonstrates anxiolytic and cognition-enhancing effects without inducing side effects in models of anxiety.
