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Norbinaltorphimine for ADHD

Norbinaltorphimine for ADHD

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Norbinaltorphimine is an opioid antagonist that has so far only been used in scientific research. Norbinaltorphimine is one of the few available highly selective kappa-opioid antagonists with a long-lasting effect.1
It is a non-stimulant.

A preclinical study in nicotine-exposed mice indicated a possible helpful effect of norbinaltorphimine in ADHD.2

Norbinaltorphimine increased dopamine and noradrenaline in the PFC in a similar way to methylphenidate, but with a significantly longer effect. At the same time, dopamine was not increased in the nucleus accumbens, which indicates a low risk of addiction.3

  1. Chavkin C, Cohen JH, Land BB (2019): Repeated Administration of Norbinaltorphimine Produces Cumulative Kappa Opioid Receptor Inactivation. Front Pharmacol. 2019 Feb 6;10:88. doi: 10.3389/fphar.2019.00088. PMID: 30787880; PMCID: PMC6373456. ↥

  2. McCarthy DM, Spencer TJ, Bhide PG (2023): Preclinical Models of Attention Deficit Hyperactivity Disorder: Neurobiology, Drug Discovery, and Beyond. J Atten Disord. 2023 Dec 12:10870547231215286. doi: 10.1177/10870547231215286. PMID: 38084074. ↥

  3. Zhang L, McCarthy DM, Eskow Jaunarajs KL, Biederman J, Spencer TJ, Bhide PG (2021): Frontal Cortical Monoamine Release, Attention, and Working Memory in a Perinatal Nicotine Exposure Mouse Model Following Kappa Opioid Receptor Antagonism. Cereb Cortex. 2021 Jan 1;31(1):483-496. doi: 10.1093/cercor/bhaa238. PMID: 32869057. ↥