Thursday, September 14, 2017

Drugs in Clinical Pipeline: BI 409306 | PDE9A Inhibitor | Phosphodiesterase 9A Inhibitors | Treatment for Alzheimer's Disease

Phosphodiesterases (PDEs) in the brain have shown to play an important role in synaptic plasticity and cognitive function. Among those PDEs is PDE9A, which specifically regulates the second messenger cGMP in neurons related to NMDA receptor signaling and is expressed in cognition relevant regions of the brain. Thus, PDE9A inhibitors are hypothesized to improve cognitive function via increasing NMDA receptor related cGMP signalling pathway to strengthen synaptic plasticity.

BI 409306 is a potent PDE9A inhibitor, which strengthens synaptic plasticity as demonstrated by increased hippocampal long-term potentiation (LTP). Systemic application of BI 409306 to rats increased cGMP levels in the CSF and brain indicating functional target engagement. Moreover, BI 409306 shows low nanomolar potency against PDE9A.

Regarding cognition, BI 409306 improved memory performance in the object recognition task, which addresses episodic memory function.
For more details, order the pdf by sending an email at Report has all the features that this site has provided to its users such as structure, synthesis, and activity results.
Or else wait for 60 days, when a part of the report will be available free.

For FAQ’s