Nalfurafine hydrochloride, a selective κ opioid receptor agonist, has no reinforcing effect on intravenous self-administration in rhesus monkeys

Journal of Pharmacological Sciences
Kaoru NakaoTomoji Yanagita

Abstract

Nalfurafine hydrochloride [(E)-N-[17-(cyclopropylmethyl)-4,5α-epoxy-3,14-dihydroxymorphinan-6β-yl]-3-(furan-3-yl)-N-methylprop-2-enamide monohydrochloride; nalfurafine] is used in Japan as an antipruritic for the treatment of intractable pruritus in patients undergoing hemodialysis or with chronic liver disease. It is a potent and selective agonist at the κ opioid receptor, but also has weak and partial agonist activity at μ opioid receptors. Opioids, especially those acting at μ receptors, carry a risk of abuse. This is an important factor in the consideration of therapeutic risk vs. benefit in clinical use and the potential for misuse as a public health problem. It is therefore necessary to carefully evaluate the reinforcing effects of nalfurafine. To this end, we investigated intravenous self-administration of nalfurafine in rhesus monkeys. The number of self-administration of nalfurafine at doses of 0.0625, 0.125 and 0.25 μg/kg/infusion was not higher than that of saline in rhesus monkeys that frequently self-administered pentazocine (0.25 mg/kg/infusion). These results indicate that nalfurafine has no reinforcing effect in rhesus monkeys in the intravenous self-administration paradigm.

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Citations

Jun 2, 2009·Harm Reduction Journal·Simon H BudmanStephen F Butler
Feb 22, 2007·PloS One·Bernard Le FollSteven R Goldberg
Jun 19, 2012·Neuropharmacology·Britta HahnRobert W Buchanan
Feb 1, 2005·Trends in Pharmacological Sciences·Anne-Noël Samaha, Terry E Robinson
Apr 6, 2017·British Journal of Pharmacology·Thomas GüntherStefan Schulz
Oct 14, 2018·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Bronwyn M KivellThomas E Prisinzano
Jan 17, 2021·Experimental Neurology·Huiping Ding, Mei-Chuan Ko
Mar 24, 2021·Annual Review of Biochemistry·Tao Che, Bryan L Roth

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