287720-99-4Relevant academic research and scientific papers
Synthesis and binding affinities of 4-diarylaminotropanes, a new class of delta opioid agonists
Boyd, Robert E.,Carson, John R.,Codd, Ellen E.,Gauthier, A. Diane,Neilson, Lou Anne,Zhang, Sui-Po
, p. 1109 - 1111 (2007/10/03)
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.
4-[(8-Alkyl-8-azabicyclo[3.2.1]octyl-3-yl)-3-arylanilino]-N,N-diethylbenz amides: High affinity, selective ligands for the delta opioid receptor illustrate factors important to antagonist activity
Thomas, James B.,Atkinson, Robert N.,Rothman, Richard B.,Burgess, Jason P.,Mascarella, S. Wayne,Dersch, Christina M.,Xu, Heng,Carroll, F. Ivy
, p. 1281 - 1284 (2007/10/03)
The tropane derived compounds, 4-[(8-alkyl-8-azabicyclo[3.2.1]octyl-3-yl)-3-arylanilino]-N,N-diethylbenzamides (5a-d), were synthesized and found to have high affinity and selectivity for the δ receptor. Compounds 5a-d are structurally similar to the full agonist (-)-RTI-5989-54 (3); yet, efficacy studies for compounds in this series (5a-d) reveal greatly diminished agonist activity as well as antagonism not found in piperidine-based compounds like 3. (C) 2000 Elsevier Science Ltd. All rights reserved.
