D159687

D159687 is a negative allosteric modulator of phosphodiesterase 4D (PDE4D; IC₅₀ = 28 nM for the human enzyme).¹ It is selective for PDE4D over PDE4B (IC₅₀ = 562 nM for the human enzyme), as well as 14 other PDE isoforms (IC₅₀s = >1.4 µM). D159687 decreases forskolin-induced cAMP hydrolysis in HEK293 cells (IC₅₀ = 253 nM) and dextran gel-induced increases in leukotriene E₄ production in isolated human whole blood (IC₅₀ = 44 nM). It impairs novel object recognition in mice when administered at a dose of 3 mg/kg but does not increase anesthesia duration, a proxy measure of emesis induction, in mice at 3 or 10 mg/kg.²

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1. Burgin, A.B., Magnusson, O.T., Singh, J., et al. Design of phosphodiesterase 4D (PDE4D) allosteric modulators for enhancing cognition with improved safety. Nat. Biotechnol. 28(1), 63-70 (2010).

2. Zhang, C., Xu, Y., Zhang, H.-T., et al. Comparison of the Pharmacological Profiles of Selective PDE4B and PDE4D Inhibitors in the Central Nervous System. Sci. Rep. 7, 40115 (2017).