A KOR agonist (EC50 = 0.05 nM for human receptors expressed in CHO cell membranes); selective for κ-opioid over μ- and δ-opioid receptors (EC50s = 0.72 and 74.1 nM

Nalfurafine – 1 mg

Brand:
Cayman
CAS:
152657-84-6
Storage:
-20
UN-No:
Non-Hazardous - /

Nalfurafine is a κ-opioid receptor (KOR) agonist (EC50 = 0.05 nM for human receptors expressed in CHO cell membranes).{49051} 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 (CQ; Item No. 14194) in mice, as well as locomotor activity when administered at a dose of 100 μg/kg.{49053} 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 (5-HT; Item No. 14332).{49054} Nalfurafine is also an orexin 1 receptor (OX1R) antagonist (Ki = 250 nM).{49052}  

 

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SKU: 23186 - 1 mg Category:

Description

A KOR agonist (EC50 = 0.05 nM for human receptors expressed in CHO cell membranes); selective for κ-opioid over μ- and δ-opioid receptors (EC50s = 0.72 and 74.1 nM, respectively); reduces CQ-induced scratching behavior induced in mice at ≥30 μg/kg, as well as locomotor activity at 100 μg/kg; reduces intracranial self-stimulation, lactic-acid induced stretching behavior, and 5-HT-induced scratching behavior in rats at ≥0.01 mg/kg; an OX1R antagonist (Ki = 250 nM)

Formal name: (2E)-N-[(5α,6β)-17-(cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxymorphinan-6-yl]-3-(3-furanyl)-N-methyl-2-propenamide

Synonyms:  TRK-820

Molecular weight: 476.6

CAS: 152657-84-6

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Neuroscience|Pain Research

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