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Differential signaling properties at the kappa opioid receptor of 12-epi-salvinorin A and its analogues.

Abstract：

:The kappa opioid receptor (KOPR) has been identified as a potential drug target to prevent or alter the course of mood, anxiety and addictive disorders or reduce response to stress. In a search for highly potent and selective KOPR partial agonists as pharmacological tools, we have modified 12-epi-salvinorin A, a compound which we have previously observed to be a KOPR partial agonist. Five analogues of 12-epi-salvinorin A were synthesized and their effects on G protein activation as well as β-arrestin2 recruitment were evaluated. Only 12-epi-salvinorin A (1) partially activated signaling through G proteins, yet acted as a full agonist in the β-arrestin 2 DiscoveRx assay. Other salvinorin analogues tested in these functional assays were full agonists in both assays of KOPR activation. By comparison, the non-selective opioid ligand nalbuphine, known to be a partial agonist for G-protein activation, was also a partial agonist for the β-arrestin mediated signaling pathway activated through KOPR.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Béguin C,Potuzak J,Xu W,Liu-Chen LY,Streicher JM,Groer CE,Bohn LM,Carlezon WA Jr,Cohen BM

doi

10.1016/j.bmcl.2011.11.128

subject

Has Abstract

pub_date

2012-01-15 00:00:00

pages

1023-6

issue

2

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(11)01672-6

journal_volume

22

pub_type

杂志文章

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