Bioorganic and Medicinal Chemistry Letters p. 1281 - 1284 (2000)
Update date:2022-09-26
Topics:
Thomas, James B.
Atkinson, Robert N.
Rothman, Richard B.
Burgess, Jason P.
Mascarella, S. Wayne
Dersch, Christina M.
Xu, Heng
Carroll, F. Ivy
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.
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