"目录号: HY-14550
Metabolic Enzyme/Protease-
TP-10是PDE10A 抑制剂, IC50 为0.8 nM。
Phosphodiesterase (PDE)
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生物活性
Description
TP-10 is a PDE10A inhibitor with IC50 of 0.8 nM.IC50 value: 0.8 nM [1]Target: PDE10ATP-10 has extremely potent PDE10A inhibitory activity and highselectivity against other PDEs, and be active in the mouse behavioral model for positive symptoms. TP-10 demonstrats good in vitro and in vivo activity, the intrinsic clearance (CLint) of these compounds in mouse liver microsomes (MLM) was extremely high in assay (CLint>1000 mL/min/kg). [1]
Clinical Trial
NCT02302755
University of Iowa
Dense Deposit Disease
November 2014
Phase 1
NCT00082121
Avant Immunotherapeutics
Myocardial Ischemia-Coronary Arteriosclerosis-Aortic Valve Insufficiency-Mitral Valve Insufficiency
April 2004
Phase 2
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References
[1].Hamaguchi W, et al. Synthesis and in vivo evaluation of novel quinoline derivatives as phosphodiesterase 10A inhibitors. Chem Pharm Bull (Tokyo). 2014;62(12):1200-1213.
[2].Verhoest PR, et al. Discovery of a novel class of phosphodiesterase 10A inhibitors and identification of clinical candidate 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the treatment of schizophrenia. J Med Chem