- 4-[aryl(8-azabicyclo[3.2.1]octan-3-yl)]aminobenzoic acid derivatives
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4-[aryl(8-azabicyclo[3.2.1]octan-3yl)]aminobenzoic acid derivatives are delta-opioid receptor modulators. As delta-opioid receptor agonists, such compounds are useful as analgesics. Depending on their antagonist effect, such compounds may also be useful immunosuppressants, antiinflammatory agents, agents for the treatment of neurological and psychiatric conditions, medicaments for drug and alcohol abuse, agents for treating gastritis and diarrhea, cardiovascular agents and agents for the treatment of respiratory diseases.
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- Synthesis and binding affinities of 4-diarylaminotropanes, a new class of delta opioid agonists
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A series of 4-diarylaminotropanes has been prepared. Both endo and exo diastereomeric forms bound to the delta opioid receptor but the endo isomers were more potent and selective versus the μ opioid receptor than the exo isomers. The most potent delta opioid agonist (14) exhibited a delta opioid K(i) of 0.2 nM and was 860-fold selective over mu. (C) 2000 Elsevier Science Ltd. All rights reserved.
- Boyd, Robert E.,Carson, John R.,Codd, Ellen E.,Gauthier, A. Diane,Neilson, Lou Anne,Zhang, Sui-Po
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p. 1109 - 1111
(2007/10/03)
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