JTP-4819 is a potent and selective prolyl endopeptidase (PEP) inhibitor with potential for treating Alzheimers disease. At nanomolar concentrations, it inhibited the degradation of substance P, arginine-vasopressin, and thyrotropin-releasing hormone by PEP in supernatants of the rat cerebral cortex and hippocampus. Repeated administration of JTP-4819 reversed the aging-induced decrease in brain substance P-like and thyrotropin-releasing hormone-like immunoreactivity, suggesting it may improve the imbalance of peptidergic neuronal systems that develops with senescence by inhibiting PEP activity. Additionally, JTP-4819 increased acetylcholine release from the frontal cortex and hippocampus, regions closely associated with memory, in both young and aged rats.
Molekulargewicht:
359.42
CAS Nummer:
[162203-65-8]
Formel:
C19H25N3O4
Target-Kategorie:
Others|||Prolyl Endopeptidase (PREP)
T70365
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