title: The discovery of a selective, small molecule agonist for the MAS-related gene X1 receptor.
abstract: The novel 7-transmembrane receptor MrgX1 is located predominantly in the dorsal root ganglion and has consequently been implicated in the perception of pain. Here we describe the discovery and optimization of a small molecule agonist and initial docking studies of this ligand into the receptor in order to provide a suitable lead and tool compound for the elucidation of the physiological function of the receptor.
authors.affiliation: GlaxoSmithKline Pharmaceuticals, New Frontiers Science Park (North), Third Avenue, Harlow, Essex CM19 5AW, United Kingdom.
authors.forename: Berthold
authors.initials: B
authors.lastname: Wroblowski
authors.forename: Mark J
authors.initials: MJ
authors.lastname: Wigglesworth
authors.forename: Philip G
authors.initials: PG
authors.lastname: Szekeres
authors.forename: Graham D
authors.initials: GD
authors.lastname: Smith
authors.forename: Shahzad S
authors.initials: SS
authors.lastname: Rahman
authors.forename: Neville H
authors.initials: NH
authors.lastname: Nicholson
authors.forename: Alison I
authors.initials: AI
authors.lastname: Muir
authors.forename: Adrian
authors.initials: A
authors.lastname: Hall
authors.forename: Jag P
authors.initials: JP
authors.lastname: Heer
authors.forename: Stephen L
authors.initials: SL
authors.lastname: Garland
authors.forename: William J
authors.initials: WJ
authors.lastname: Coates
mesh_terms: D001713:Biphenyl Compounds / Q000138:chemical synthesis / Q000494:pharmacology; D002118:Calcium / Q000378:metabolism; D020650:Combinatorial Chemistry Techniques; D015195:Drug Design; D006801:Humans; D010879:Piperazines / Q000138:chemical synthesis* / Q000494:pharmacology; D011724:Pyridazines / Q000138:chemical synthesis* / Q000494:pharmacology; D043562:Receptors, G-Protein-Coupled / Q000819:agonists* / Q000502:physiology; D013329:Structure-Activity Relationship
chemical_list: D001713:Biphenyl Compounds; D010879:Piperazines; D011724:Pyridazines; D043562:Receptors, G-Protein-Coupled; C510803:mas-related gene-X1 receptor, human; D002118:Calcium