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Effect of ring-constrained phenylpropyloxyethylamines on sigma receptors.

Abstract：

:A series of ring-constrained phenylpropyloxyethylamines, partial opioid structure analogs and derivatives of a previously studied sigma (σ) receptor ligand, was synthesized and evaluated at σ and opioid receptors for receptor selectivity. The results of this study identified several compounds with nanomolar affinity at both σ receptor subtypes. Compounds 6 and 9 had the highest selectivity for both σ receptor subtypes, compared to μ opioid receptors. In addition, compounds 6 and 9 significantly reduced the convulsive effects of cocaine in mice, which would be consistent with antagonism of σ receptors.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Stavitskaya L,Seminerio MJ,Healy JR,Noorbakhsh B,Matsumoto RR,Coop A

doi

10.1016/j.bmc.2013.06.068

subject

Has Abstract

pub_date

2013-09-01 00:00:00

pages

4923-7

issue

17

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(13)00608-1

journal_volume

21

pub_type

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