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

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

  • Bioorg Med Chem Lett. 2014 Aug 1;24(15):3512-5. doi: 10.1016/j.bmcl.2014.05.060.
Trevor Johnson 1,  Dionicio Siegel 2
Affiliations

Affiliations

  • 1 Department of Chemistry, The University of Texas at Austin, Austin, TX 78712, United States.
  • 2 Department of Chemistry, The University of Texas at Austin, Austin, TX 78712, United States. Electronic address: [email protected].
PMID: 24930830 DOI: 10.1016/j.bmcl.2014.05.060
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.

Keywords

Agonist; Complanadine A; Lycodine; Mas-related G protein-coupled receptor X2; Pain management.

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