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Complanadine A, a selective agonist for the Mas-related G protein-coupled receptor X2.

Abstract：

:The first biological target for the natural product complanadine A has been determined. The pseudosymmetric alkaloid functions as a selective agonist for the Mas-related G protein-coupled receptor X2 (MrgprX2), a G protein-coupled receptor that is highly expressed in neurons. Given the potential of MrgprX2 to function as a modulator of pain, complanadine A represents a new chemical probe to selectively interrogate the physiological function of MrgprX2 as well as a potential lead for the development of antihyperalgesics for the treatment of persistent pain. While complanadine A possess agonistic activity the related natural product lycodine, representing half of complanadine A, lacks activity providing a cursory description of the structural requirements for agonistic activity.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Johnson T,Siegel D

doi

10.1016/j.bmcl.2014.05.060

subject

Has Abstract

pub_date

2014-08-01 00:00:00

pages

3512-5

issue

15

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(14)00560-5

journal_volume

24

pub_type

杂志文章

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