norbinaltorphimine and Depressive-Disorder--Major

norbinaltorphimine has been researched along with Depressive-Disorder--Major* in 1 studies

Other Studies

1 other study(ies) available for norbinaltorphimine and Depressive-Disorder--Major

Article	Year
SAR development of a series of 8-azabicyclo[3.2.1]octan-3-yloxy-benzamides as kappa opioid receptor antagonists. Part 2. Bioorganic & medicinal chemistry letters, 2010, Sep-15, Volume: 20, Issue:18 Further structure activity relationship studies on a previously reported 8-azabicyclo[3.2.1]octan-3-yloxy-benzamide series of potent and selective kappa opioid receptor antagonists is discussed. Modification of the pendant N-substitution to include a cyclohexylurea moiety produced analogs with greater in vitro opioid and hERG selectivity such as 12 (kappa IC50=172 nM, mu:kappa ratio=93, delta:kappa ratio=>174, hERG IC50=>33 microM). Changes to the linker conformation and identity as well as to the benzamide ring moiety were also investigated. Topics: Animals; Antidepressive Agents; Benzamides; Brain; Bridged Bicyclo Compounds; Depressive Disorder, Major; Humans; Microsomes, Liver; Rats; Receptors, Opioid, kappa; Structure-Activity Relationship	2010

Article

Year

SAR development of a series of 8-azabicyclo[3.2.1]octan-3-yloxy-benzamides as kappa opioid receptor antagonists. Part 2.

Bioorganic & medicinal chemistry letters, 2010, Sep-15, Volume: 20, Issue:18

Further structure activity relationship studies on a previously reported 8-azabicyclo[3.2.1]octan-3-yloxy-benzamide series of potent and selective kappa opioid receptor antagonists is discussed. Modification of the pendant N-substitution to include a cyclohexylurea moiety produced analogs with greater in vitro opioid and hERG selectivity such as 12 (kappa IC50=172 nM, mu:kappa ratio=93, delta:kappa ratio=>174, hERG IC50=>33 microM). Changes to the linker conformation and identity as well as to the benzamide ring moiety were also investigated.

Topics: Animals; Antidepressive Agents; Benzamides; Brain; Bridged Bicyclo Compounds; Depressive Disorder, Major; Humans; Microsomes, Liver; Rats; Receptors, Opioid, kappa; Structure-Activity Relationship

2010