The Discovery of a Selective, Small Molecule Agonist for the Mas-Related Gene X1 Receptor

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 or...

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Bibliographic Details
Published in:Journal of medicinal chemistry 2009-02, Vol.52 (3), p.818-825
Main Authors: Wroblowski, Berthold, Wigglesworth, Mark J, Szekeres, Philip G, Smith, Graham D, Rahman, Shahzad S, Nicholson, Neville H, Muir, Alison I, Hall, Adrian, Heer, Jag P, Garland, Stephen L, Coates, William J
Format: Article
Language:English
Subjects:
Biological and medical sciences
Biphenyl Compounds - chemical synthesis
Biphenyl Compounds - pharmacology
Calcium - metabolism
Combinatorial Chemistry Techniques
Drug Design
Humans
Medical sciences
Miscellaneous
Neuropharmacology
Neurotransmitters. Neurotransmission. Receptors
Pharmacology. Drug treatments
Piperazines - chemical synthesis
Piperazines - pharmacology
Pyridazines - chemical synthesis
Pyridazines - pharmacology
Receptors, G-Protein-Coupled - agonists
Receptors, G-Protein-Coupled - physiology
Structure-Activity Relationship
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Summary: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.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm800962k