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TRPA1 and TRPV1 are ion channels crucial for pain sensation. In this issue of Neuron, Weng et al. (2015) demonstrate that the activity of TRPA1-TRPV1 heteromers is governed by Tmem100 and that disabling Tmem100 may be a novel pharmacologic strategy to combat pain.
TRPM8 has been implicated in pain and migraine based on dorsal root- and trigeminal ganglion-enriched expression, upregulation in preclinical models of pain, knockout mouse studies, and human genetics. Here, we evaluated the therapeutic potential in pain of AMG2850 (( R )-8-(4-(trifluoromethyl)phenyl)- N -(( S )-1,1,1-trifluoropropan-2-yl)-5,6-dihydro-1,7-naphthyridine-7(8H)-carboxamide),...
Therapeutic use of general sodium channel blockers, such as lidocaine, can substantially reduce the enhanced activity in sensory neurons that accompanies chronic pain after nerve or tissue injury. However, because these general blockers have significant side effects, there is great interest in developing inhibitors that specifically target subtypes of sodium channels. Moreover, some idiopathic small-fiber...
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