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Neuropathic pain medication
Abstract
The investigators discovered potent AT2 antagonists for non-addictive pain relief. Several new lead compounds displayed better potency than the previous clinical candidate EMA401 (EC50=0.16nM vs 4.9nM). All compounds tested had good solubility, acceptable hepatocyte clearance and CYP inhibition profiles, as well...
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Improved analgesic drugs
Abstract
USC researchers have identified two similar DOR-selective bitopic ligands that provide analgesia while minimizing seizure risk. These ligands, which target the conserved sodium site in DORs, have high affinity and potency for the DOR in G-protein pathways, but not arrestin pathways. In a mouse model, these ligands...
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