Drug intelligence / Profile preview

norbinaltorphimine

Development stage
Preclinical
Lead developer
University of Washington
Modality
Small Molecules
Administration
Intraperitoneal, Subcutaneous, Intracerebroventricular
01

Overview

norbinaltorphimine is a highly selective, long-acting κ-opioid receptor antagonist and inverse agonist used exclusively in scientific research. It blocks the effects of κ-opioids, resulting in antidepressant-like and anxiolytic-like effects in animal models[1][6][11]. Norbinaltorphimine's mechanism involves cumulative and persistent inactivation of κ-opioid receptors, with doses producing pharmacological effects that last for weeks or months[1][7]. Unlike stimulants, it increases monoamines such as dopamine and noradrenaline in the prefrontal cortex, potentially relevant for ADHD, with a low risk of addiction[4]. It has been studied for potential in stress, anxiety, depression, and substance abuse relapse[5][13].

Other names
norbinaltorphiminenor-BNInBNI
02

Targets

KOR (Kappa opioid receptor)

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