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Bioorg Med Chem Lett. 2000 May 15;10(10):1109-11.

Synthesis and binding affinities of 4-diarylaminotropanes, a new class of delta opioid agonists.

Author information

1
Drug Discovery, R. W. Johnson Pharmaceutical Research Institute, Spring House, Philadelphia, PA 19477, USA.

Abstract

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 mu opioid receptor than the exo isomers. The most potent delta opioid agonist (14) exhibited a delta opioid Ki of 0.2 nM and was 860-fold selective over mu.

PMID:
10843229
DOI:
10.1016/s0960-894x(00)00182-7
[Indexed for MEDLINE]

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