Nalfurafine is a κ-opioid receptor (KOR) agonist (EC50 = 0.05 nM for human receptors expressed in CHO cell membranes).
CAS:152657-84-6
分子式:C28H32N2O5
分子量:476.6
纯度:98%
存储:Store at -20°C
Background:
Nalfurafine is a κ-opioid receptor (KOR) agonist (EC50 = 0.05 nM for human receptors expressed in CHO cell membranes). 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. 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 . Nalfurafine is also an orexin 1 receptor (OX1R) antagonist (Ki = 250 nM).