1007457-06-8Relevant academic research and scientific papers
Discovery of 8-azabicyclo[3.2.1]octan-3-yloxy-benzamides as selective antagonists of the kappa opioid receptor. Part 1
Brugel, Todd A.,Smith, Reed W.,Balestra, Michael,Becker, Christopher,Daniels, Thalia,Hoerter, Tiffany N.,Koether, Gerard M.,Throner, Scott R.,Panko, Laura M.,Folmer, James J.,Cacciola, Joseph,Hunter, Angela M.,Liu, Ruifeng,Edwards, Philip D.,Brown, Dean G.,Gordon, John,Ledonne, Norman C.,Pietras, Mark,Schroeder, Patricia,Sygowski, Linda A.,Hirata, Lee T.,Zacco, Anna,Peters, Matthew F.
, p. 5847 - 5852 (2010)
Initial high throughput screening efforts identified highly potent and selective kappa opioid receptor antagonist 3 (κ IC50 = 77 nM; μ:κ and δ:κ IC50 ratios >400) which lacked CNS exposure in vivo. Modification of this scaffold resulted in development of a series of 8-azabicyclo[3.2.1]octan-3-yloxy-benzamides showing potent and selectivity κ antagonism as well as good brain exposure. Analog 6c (κ IC50 = 20 nM; μ:κ = 36, δ:κ = 415) was also shown to reverse κ-agonist induced rat diuresis in vivo.
Therapeutic Agents
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Page/Page column 13, (2008/06/13)
The present invention provides compounds of formula I, processes for preparing such compounds, their use in the treatment of obesity, psychiatric disorders, cognitive disorders, memory disorders, schizophrenia, epilepsy, and related conditions, type II di
