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2.
Bioorg Med Chem Lett ; 20(19): 5847-52, 2010 Oct 01.
Article in English | MEDLINE | ID: mdl-20727752

ABSTRACT

Initial high throughput screening efforts identified highly potent and selective kappa opioid receptor antagonist 3 (κ IC(50)=77 nM; µ:κ and δ:κ IC(50) 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 IC(50)=20 nM; µ:κ=36, δ:κ=415) was also shown to reverse κ-agonist induced rat diuresis in vivo.


Subject(s)
Benzamides/chemistry , Receptors, Opioid, kappa/antagonists & inhibitors , Tropanes/chemistry , Animals , Benzamides/chemical synthesis , Benzamides/pharmacokinetics , Cell Line, Tumor , Diuresis/drug effects , Drug Evaluation, Preclinical , High-Throughput Screening Assays , Humans , Microsomes, Liver/metabolism , Rats , Receptors, Opioid, kappa/metabolism , Structure-Activity Relationship , Tropanes/chemical synthesis , Tropanes/pharmacokinetics
4.
Org Lett ; 20(6): 1481-1482, 2018 03 16.
Article in English | MEDLINE | ID: mdl-29544253
5.
Org Lett ; 17(12): 2867-9, 2015 Jun 19.
Article in English | MEDLINE | ID: mdl-26087893
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