ITI-214

ITI-214 is a potent, CNS-active, orally bioavailable PDE1 inhibitor ( K i of 58 pM) with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters and ion channels. ITI-214 inhibits recombinant full-length human PDE1A, PDE1B and PDE1C with K i s of 33 pM, 380 pM and 35 pM, respectively. ITI-214 shows efficacy in various animal models of motor and cognitive functions In Vitro ITI-214 expresses >1000-fold greater activity toward PDE1 isoforms compared with the next nearest PDE family enzyme, PDE4D (K i =?33 nM) and 10,000-300,000-fold selectivity toward all other PDE enzyme families. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo ITI-214 significantly enhances memory performance in the test with a minimum effective dose of 3 mg/kg . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male Sprague-Dawley rats Dosage: 0.1-10 mg/kg Administration: p.o. Result: Significantly enhanced memory performance in the test with a minimum effective dose of 3 mg/kg. IC50& Target:PDE1 58 pM (Ki) PDE1A 33 pM (Ki) PDE1B 380 pM (Ki) PDE1C 35 pM (Ki)

No numbering system information yet

No physical and chemical property information yet

No safety information yet

No production method and use information yet

No upstream information yet

No downstream information yet

No related product information yet