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4-Phenyl-4-[1H-imidazol-2-yl]-piperidine derivatives, a novel class of selective delta-opioid agonists.

Abstract：

:A novel series of 4-phenyl-4-[1H-imidazol-2-yl]-piperidine derivatives has been prepared and their synthesis described herein. In vitro affinities for delta-, mu-, and kappa-opioid receptors, as well as the functional activity in the [(35)S]GTPgammaS assay are reported. The most potent and selective delta-opioid agonist 18a exhibited a K(i) of 18 nM, and was >258-fold and 28-fold selective over mu- and kappa-receptors, respectively; the compound is a full agonist with an EC(50) value of 14 nM.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Trabanco AA,Pullan S,Alonso JM,Alvarez RM,Andrés JI,Boeckx I,Fernández J,Gómez A,Iturrino L,Janssens FE,Leenaerts JE,De Lucas AI,Matesanz E,Meert T,Steckler T

doi

10.1016/j.bmcl.2005.09.025

subject

Has Abstract

pub_date

2006-01-01 00:00:00

pages

146-9

issue

1

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(05)01193-5

journal_volume

16

pub_type

杂志文章

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