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A selective, high-affinity A2B adenosine receptor (AR) antagonist will be useful as a pharmacological tool to help determine the role of the A2BAR in inflammatory diseases and angiogenic diseases. Based on early A2BAR-selective ligands with nonoptimal pharmaceutical properties, such as 15 (MRS 1754: $${K}_{\mathrm{i}}(\mathrm{h{A}_{2B}})\;=\;2\,\mathrm{nM};\ {K}_{\mathrm{i}}({\mathrm{hA}}_{1})\;=\;403\,\mathrm{nM};\...
The transient receptor potential ankyrin 1 (TRPA1) channel is activated by a series of by-products of oxidative/nitrative stress, produced under inflammatory conditions or in the case of tissue damage, thus generating inflammatory and neuropathic pain and neurogenic inflammatory responses. These findings have identified TRPA1 as an emerging opportunity for the design and synthesis of selective inhibitors...
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