Synthesis and agonist properties of novel quinoline and isoquinoline derivatives toward the cannabinoid receptor CB2

Bastien Reux; Tapio Nevalainen; Katri H. Raitio; Ari M.P. Koskinen

doi:10.1016/j.bmc.2009.05.013

Synthesis and agonist properties of novel quinoline and isoquinoline derivatives toward the cannabinoid receptor CB2

Bastien Reux
, Tapio Nevalainen
, Katri H. Raitio
, Ari M.P. Koskinen

Research output: Contribution to journal › Article › Scientific › peer-review

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Abstract

A series of quinolinyl and isoquinolinyl phenyl ketones was synthesized and their CB2 receptor-dependent G-protein activities were determined using the [35S]GTPcS binding assay. Both quinoline and isoquinoline derivatives exhibited similar CB2 receptor agonist activity, the most potent ligands being the 2-(Me2N)-phenyl substituted derivatives, which were also full agonists at the CB2-receptor.

Original language	English
Pages (from-to)	4441-4447
Journal	Bioorganic and Medicinal Chemistry
Volume	17
Issue number	13
DOIs	https://doi.org/10.1016/j.bmc.2009.05.013
Publication status	Published - 2009
MoE publication type	A1 Journal article-refereed

Keywords

cannabinoid
receptor CB2
quinoline
isoquinoline

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10.1016/j.bmc.2009.05.013

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title = "Synthesis and agonist properties of novel quinoline and isoquinoline derivatives toward the cannabinoid receptor CB2",

abstract = "A series of quinolinyl and isoquinolinyl phenyl ketones was synthesized and their CB2 receptor-dependent G-protein activities were determined using the [35S]GTPcS binding assay. Both quinoline and isoquinoline derivatives exhibited similar CB2 receptor agonist activity, the most potent ligands being the 2-(Me2N)-phenyl substituted derivatives, which were also full agonists at the CB2-receptor.",

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author = "Bastien Reux and Tapio Nevalainen and Raitio, \{Katri H.\} and Koskinen, \{Ari M.P.\}",

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language = "English",

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journal = "Bioorganic and Medicinal Chemistry",

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AU - Reux, Bastien

AU - Nevalainen, Tapio

AU - Raitio, Katri H.

AU - Koskinen, Ari M.P.

PY - 2009

Y1 - 2009

N2 - A series of quinolinyl and isoquinolinyl phenyl ketones was synthesized and their CB2 receptor-dependent G-protein activities were determined using the [35S]GTPcS binding assay. Both quinoline and isoquinoline derivatives exhibited similar CB2 receptor agonist activity, the most potent ligands being the 2-(Me2N)-phenyl substituted derivatives, which were also full agonists at the CB2-receptor.

AB - A series of quinolinyl and isoquinolinyl phenyl ketones was synthesized and their CB2 receptor-dependent G-protein activities were determined using the [35S]GTPcS binding assay. Both quinoline and isoquinoline derivatives exhibited similar CB2 receptor agonist activity, the most potent ligands being the 2-(Me2N)-phenyl substituted derivatives, which were also full agonists at the CB2-receptor.

KW - cannabinoid

KW - receptor CB2

KW - quinoline

KW - isoquinoline

U2 - 10.1016/j.bmc.2009.05.013

DO - 10.1016/j.bmc.2009.05.013

M3 - Article

SN - 0968-0896

VL - 17

SP - 4441

EP - 4447

JO - Bioorganic and Medicinal Chemistry

JF - Bioorganic and Medicinal Chemistry

IS - 13

ER -

Synthesis and agonist properties of novel quinoline and isoquinoline derivatives toward the cannabinoid receptor CB2

Abstract

Keywords

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