title: 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.
authors.affiliation: Department of Chemistry, The University of Texas at Austin, Austin, TX 78712, United States.
authors.forename: Trevor
authors.initials: T
authors.lastname: Johnson
authors.affiliation: Department of Chemistry, The University of Texas at Austin, Austin, TX 78712, United States. Electronic address: dsiegel@cm.utexas.edu.
authors.forename: Dionicio
authors.initials: D
authors.lastname: Siegel
mesh_terms: D004305:Dose-Response Relationship, Drug; D006576:Heterocyclic Compounds, 4 or More Rings / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D015394:Molecular Structure; D009419:Nerve Tissue Proteins / Q000819:agonists*; D043562:Receptors, G-Protein-Coupled / Q000819:agonists*; D018013:Receptors, Neuropeptide / Q000819:agonists*; D013329:Structure-Activity Relationship
chemical_list: D006576:Heterocyclic Compounds, 4 or More Rings; C480039:MRGPRX2 protein, human; D009419:Nerve Tissue Proteins; D043562:Receptors, G-Protein-Coupled; D018013:Receptors, Neuropeptide; C550939:complanadine A
keywords: Agonist; Complanadine A; Lycodine; Mas-related G protein-coupled receptor X2; Pain management