ZD7288

ZD7288 is a selective phosphodiesterase 10 (PDE10) inhibitor, a type of medication that targets the enzyme phosphodiesterase 10, which plays a crucial role in the regulation of intracellular signaling pathways. This enzyme is involved in various cellular processes, including the modulation of neural activity.

Preclinical studies have shown that ZD7288 has a high affinity and selectivity for PDE10, with a K(inh) value of approximately 34 nM. The compound has been demonstrated to inhibit PDE10 activity in a reversible and time-dependent manner, with an IC(50) value of 0.2 μM.

ZD7288 has been explored for its potential therapeutic applications in various neurological disorders, including Huntington's disease, Parkinson's disease, and bipolar disorder. The mechanisms by which ZD7288 exerts its effects are believed to involve the enhancement of cyclic adenosine monophosphate (cAMP) levels within cells, which can lead to changes in neural activity and excitability. In particular, the compound has been shown to increase the activity of cAMP-dependent protein kinase (PKA), a key enzyme involved in signal transduction pathways.

Pharmacokinetic studies have shown that ZD7288 is rapidly absorbed following oral administration and has a high clearance rate, resulting in a relatively short half-life. The compound is primarily metabolized by the liver and is eliminated via the kidneys. Overall, ZD7288 represents a promising lead compound for the development of PDE10 inhibitors, with potential applications in the treatment of neurological disorders.