ITI-214 phosphate is an orally active, potent and selective inhibitors of PDE1, exhibits potent PDE1 inhibitory activity (Ki = 58 pM). ITI-214 demonstrated excellent selectivity against all other PDE families.
ITI-214 showed good efficacy in vivo, it is found to significantly enhance memory performance in the test with a minimum effective dose of 3 mg/kg.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Solubility||DMSO ≥ 15 mg/mL|
 Li P, et al. J Med Chem. Discovery of Potent and Selective Inhibitors of Phosphodiesterase 1 for the Treatment of Cognitive Impairment Associated with Neurodegenerative and Neuropsychiatric Diseases.
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