85-5072-86　［取扱停止］Nalfurafine (TRK-820) 10mg　CAS No:152657-84-6　422220

特徴

• Nalfurafine is a κ-opioid receptor (KOR) agonist (EC50 = 0.05nM 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 74.1nM, respectively). Nalfurafine (≥30ug/kg) reduces scratching behavior induced by chloroquine in mice, as well as locomotor activity when administered at a dose of 100ug/kg.2 In rats, nalfurafine (≥0.01mg/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 = 250nM).4
• Synonyms:(2E)-N-[(5α,6β)-17-(cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxymorphinan-6-yl]-3-(3-furanyl)-N-methyl-2-propenamide; TRK-820
• Molecular Formula:C28H32N2O5
• Molecular Weight:476.56
• Appearance:White to off-white solid
• Purity:≥95%
• Melting Point:165-167°C
• Solubility:DMSO (Slightly), Methanol (Slightly)
• Storage and Stability:Store at -20°C under inert atmosphere. For maximum recovery of product, centrifuge the original vial prior to removing the cap.