Bioactivity | Zatolmilast (BPN14770) is a selective phosphodiesterase 4D (PDE4D) allosteric inhibitor with IC50s of 7.8 nM and 7.4 nM for PDE4D7 and PDE4D3, respectively[1]. | ||||||||||||
In Vivo | Zatolmilast increases brain cAMP, increases phosphorylation of CREB and increases production of brain-derived neurotrophic factor (BDNF) in hippocampus[1].Zatolmilast (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: | ||||||||||||
Name | Zatolmilast | ||||||||||||
CAS | 1606974-33-7 | ||||||||||||
Formula | C21H15ClF3NO2 | ||||||||||||
Molar Mass | 405.80 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [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. |