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4-[(8-Alkyl-8-azabicyclo[3.2.1]octyl-3-yl)-3-arylanilino]-N,N-diethylbenzamides: high affinity, selective ligands for the delta opioid receptor illustrate factors important to antagonist activity.

Authors
  • Thomas, J B
  • Atkinson, R N
  • Rothman, R B
  • Burgess, J P
  • Mascarella, S W
  • Dersch, C M
  • Xu, H
  • Carroll, F I
Type
Published Article
Journal
Bioorganic & Medicinal Chemistry Letters
Publisher
Elsevier
Publication Date
Jun 05, 2000
Volume
10
Issue
11
Pages
1281–1284
Identifiers
PMID: 10866400
Source
Medline
License
Unknown

Abstract

The tropane derived compounds, 4-[(8-alkyl-8-azabicyclo[3.2.1]octyl-3-yl)-3-arylanilino]-N,N-d iethylbenzamides (5a-d), were synthesized and found to have high affinity and selectivity for the delta 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.

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