BPN14770

BPN14770 is a selective phosphodiesterase 4D (PDE4D) allosteric inhibitor with IC50s of 7.8 nM and 7.4 nM for PDE4D7 and PDE4D3 (two different dimeric forms of PDE4D), respectively[1].

Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphodiesterase (PDE)

Research Areas >> Neurological Disease

PDE4D3:7.4 nM (IC50)

PDE4D7:7.8 nM (IC50)

BPN14770 increases brain cAMP, increases phosphorylation of CREB and increases production of brain-derived neurotrophic factor (BDNF) in hippocampus[1]. BPN14770 (0.1-30 mg/kg; p.o.; 24 hours) provides cognitive benefit in the mouse novel object recognition (NOR) at doses above 0.3 mg/kg[2]. Animal Model: C57Bl6 mice[2] Dosage: 0.1, 0.3, 1, 3, 10, 30 mg/kg Administration: p.o.; 24 hours Result: Significantly improved novel object discrimination at doses above 0.3 mg/kg.

[1]. Ricciarelli R, et al. Memory-enhancing effects of GEBR-32a, a new PDE4D inhibitor holding promise for the treatment of Alzheimer's disease. Sci Rep. 2017 Apr 12;7:46320.

[2]. Gurney ME, et al. Design and Synthesis of Selective Phosphodiesterase 4D (PDE4D) Allosteric Inhibitors for the Treatment of Fragile X Syndrome and Other Brain Disorders. J Med Chem. 2019 May 23;62(10):4884-4901.