61335-37-3Relevant academic research and scientific papers
Pyrazoloquinolines as PDE10A inhibitors: Discovery of a tool compound
McElroy, William T.,Tan, Zheng,Basu, Kallol,Yang, Shu-Wei,Smotryski, Jennifer,Ho, Ginny D.,Tulshian, Deen,Greenlee, William J.,Mullins, Deborra,Guzzi, Mario,Zhang, Xiaoping,Bleickardt, Carina,Hodgson, Robert
scheme or table, p. 1335 - 1339 (2012/03/26)
A series of pyrazoloquinolines, possessing (hetero)arylhydroxymethyl substituents at the quinoline C-4 position were evaluated as PDE10A inhibitors. Among these, methylpyrimidyl analogue 15 was identified as having good rodent and monkey exposure, and a MED of 10 mg/kg in an in vivo model.
Discovery of orally active pyrazoloquinolines as potent PDE10 inhibitors for the management of schizophrenia
Yang, Shu-Wei,Smotryski, Jennifer,McElroy, William T.,Tan, Zheng,Ho, Ginny,Tulshian, Deen,Greenlee, William J.,Guzzi, Mario,Zhang, Xiaoping,Mullins, Deborra,Xiao, Li,Hruza, Alan,Chan, Tze-Ming,Rindgen, Diane,Bleickardt, Carina,Hodgson, Robert
, p. 235 - 239 (2012/02/16)
A series of pyrazoloquinoline analogs have been synthesized and shown to bind to PDE10 with high affinity. From the SAR study and our lead optimization efforts, compounds 16 and 27 were found to possess potent oral antipsychotic activity in the MK-801 induced hyperactive rat model.
