TAN-452 is a selective, orally active δ-opioid receptor antagonist, exhibiting a Ki of 0.47 nM and a Kb of 0.21 nM. This reagent also shows antagonistic properties toward μ-opioid receptors, with a Ki of 36.56 nM, and κ-opioid receptors, with a Ki of 5.31 nM. TAN-452 is designed to attenuate morphine-induced side effects while maintaining analgesic efficacy, making it valuable for research in pain management and opioid-related studies. Its low brain penetrability further supports peripheral applications, minimizing central nervous system interactions.
TAN-452 is a selective, orally active δ-opioid receptor antagonist, exhibiting a Ki of 0.47 nM and a Kb of 0.21 nM. This reagent also shows antagonistic properties toward μ-opioid receptors, with a Ki of 36.56 nM, and κ-opioid receptors, with a Ki of 5.31 nM. TAN-452 is designed to attenuate morphine-induced side effects while maintaining analgesic efficacy, making it valuable for research in pain management and opioid-related studies. Its low brain penetrability further supports peripheral applications, minimizing central nervous system interactions.
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