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Nalfurafine is a κ-opioid receptor (KOR) agonist (EC50 = 0.05 nM for human receptors expressed in CHO cell membranes). [1]  It is selective for κ-opioid over μ- and δ-opioid receptors (EC50s = 0.72 and 74.1 nM, respectively). Nalfurafine (≥30 μg/kg) reduces scratching behavior induced by chloroquine in mice, as well as locomotor activity when administered at a dose of 100 μg/kg.[2]  In rats, nalfurafine (≥0.01 mg/kg) reduces intracranial self-stimulation, lactic acid-induced stretching behavior, and scratching behavior induced by intradermal administration of serotonin . [3] Nalfurafine is also an orexin 1 receptor (OX1R) antagonist (Ki = 250 nM).[4]

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