Zobrazeno 1 - 4
of 4
pro vyhledávání: '"Kelly Brush"'
Autor:
Cathy Dantzman, William E. Palmer, Peter N. Dorff, Charles S. Elmore, Christer Halldin, Valerie Hoesch, Kelly Brush, Magnus Schou, Thomas J. Hudzik, James E. Hall, Mark E. Powell
Publikováno v:
Journal of Labelled Compounds and Radiopharmaceuticals. 54:847-854
In support of a program to develop a treatment for depression, four labeled forms of a delta opioid agonist were prepared. The [2H4] labeled form was prepared using a relatively straightforward conversion of [2H4]bromoethanol to [2H4]N-methyl-2-hydro
Autor:
Michael Balestra, Francis M. McLaren, Julie Wilson, Linda A. Sygowski, Nathan Spear, James Kang, John P. McCauley, Lindsay Hinkley, Becky Brockel, Laura M. Panko, Valerie Hoesch, James Woods, Jalaj Arora, Kelly Brush, Minli Zhang, Thomas R. Simpson, Caprice Hightower, Dean G. Brown, Todd Andrew Brugel, Megan M. King, Abdelmalik Slassi, Vijay Chhajlani, Reed W. Smith, Gerard M. Koether, Reto Gadient, Hui Xiong, Methvin Isaac, Nathalie Breysse
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:7381-7384
Positive allosteric modulation of metabotropic glutamate receptor 5 (mGluR5) is regarded as a potential novel treatment for schizophrenic patients. Herein we report the synthesis and SAR of 4-aryl piperazine and piperidine amides as potent mGluR5 pos
Autor:
William E. Palmer, Steven Wesolowski, James M. Hulsizer, Jay Liu, Megan M. King, Khanh Bui, John P. McCauley, Thomas J. Hudzik, Valerie Hoesch, Kelly Brush, Xia Wang, Donald Andisik, Cathy Dantzman, William Frietze, Glen Ernst, Kenneth Doring
Publikováno v:
Bioorganicmedicinal chemistry letters. 22(2)
A novel series of piperazine derivatives exhibits sub-nanomolar binding and enhanced subtype selectivity as δ-opioid agonists. The synthesis and SAR are described as well as the application of computational models to improve in vitro ADME and safety