PF-04447943

Short Summary : PDE9 inhibitor

Category : Metabolism|PDE

Purity : 0.98

CAS Number : 1082744-20-4

Formula : C20H25N7O2

Molecular Weight : 395.46

SMILE : CC1CN(CC2=NC=CC=N2)CC1C3=NC(C4=CNN(C5CCOCC5)C4=N3)=O

Solubility : DMSO

Storage : Store at -20°C

Description : PF-04447943 is a potent and selective inhibitor of PDE9 [1]. Phosphodiesterase 9 (PDE9) selectively degrades cGMP and limits the cGMP-mediated signal transduction which occurs following glutamate binding to NMDA receptors. PDE9 in cortex and hippocampus of rodents and humans play an important role in memory and learning [1]. PF-04447943 have high affinity with Ki of 2.8, 4.5 and 18 nM for human, rhesus and rat recombinant PDE9 respectively and high selectivity for PDE9 versus PDEs1- 8 and 10 -11. In cultured hippocampal neurons, PF-04447943 (30-100 nM) significantly increased neurite outgrowth and synapse formation. Also, PF-04447943 (100 nM) significantly facilitated hippocampal slice LTP evoked by a weak tetanic stimulus [1]. In mice model, PF-04447943 (1 mg/kg) significantly reduced the time spent interacting with the female mouse during the second encounter 24 h later compared to the first encounter, which suggested that PF-04447943 enhanced recognition memory. While, PF-04447943 (3 or 10 mg/kg) didnt change the interaction times for each encounter. These results suggested that PF-04447943 enhanced memory with an inverted U-shaped dose-response efficacy curve [1]. Reference:[1]Hutson PH, Finger EN, Magliaro BC, et al. The selective phosphodiesterase 9 (PDE9) inhibitor PF-04447943(6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one) enhances synaptic plasticity and cognitive function in rodents. Neuropharmacology, 2011, 61(4): 665-676.

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