Journal
CHEMMEDCHEM
Volume 10, Issue 1, Pages 57-61Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cmdc.201402277
Keywords
chronic pain; ML382; MLPCN; molecular probes; MrgX1; positive allosteric modulators
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Funding
- US National Institutes of Health (NIH)/Molecular Libraries Probe Centers Network (MLPCN) [U54 MH084659, U54 MH084691, R03 DA033176, R01 NS054791]
- NIH [R03 MH090837-01, R03 MH090849-01, R03 A031670-01]
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Previous studies have shown that the activation of mouse MrgC11, a G-protein-coupled receptor, by its peptide ligand BAM8-22 can inhibit chronic pain. A large-scale screen has been carried out to isolate small-molecule allosteric agonists of MrgX1, the human homologue of MrgC11. The goal of this study is to improve the efficacy and potency of positive allosteric modulators (PAMs) with therapeutic implications in combating chronic pain. Herein we report an iterative parallel synthesis effort and a structure-activity relationship study of a series of arylsulfonamides which led to the discovery of the first PAM of MrgX1, ML382.
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