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ABT-102 is a potent and selective small molecule antagonist of the transient receptor potential vanilloid type 1 (TRPV1) receptor, also known as the capsaicin receptor. TRPV1 is a ligand-gated ion channel involved in the detection and regulation of body temperature and pain sensation. By antagonizing TRPV1, ABT-102 blocks multiple modes of receptor activation (including by capsaicin, protons, heat, and endogenous ligands), thereby attenuating nociceptive signaling associated with inflammatory, post-operative, osteoarthritic, and bone cancer pain in preclinical models. The drug was developed for oral administration primarily for pain management but its clinical development was discontinued after phase 1 trials due to class-related safety concerns such as thermosensory impairment[1][2][3][4][7][8].
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