Drug intelligence / Profile preview

R-norketamine

Development stage
Preclinical
Lead developer
ATAI Life Sciences
Modality
Small Molecules
Administration
Intravenous
01

Overview

R-norketamine is the (R)-enantiomer of norketamine, which is a major active metabolite of the dissociative anesthetic ketamine. It is a small molecule that acts as an N-methyl-D-aspartate (NMDA) receptor antagonist, though it exhibits lower potency at this receptor compared to its (S)-enantiomer. Beyond direct NMDA receptor modulation, R-norketamine has been shown to decrease intracellular D-serine concentrations and alter the expression of serine racemase. Preclinical research suggests that R-norketamine may possess potent and sustained antidepressant-like effects and analgesic properties, potentially with a lower risk of psychotomimetic side effects and abuse liability than (R,S)-ketamine or (S)-ketamine. While it is currently a subject of significant neuropharmacological interest for treatment-resistant depression and chronic pain, it is primarily available as a research tool and is not yet developed as a branded therapeutic product.

Other names
(R)-norketamine(R)-2-amino-2-(2-chlorophenyl)cyclohexanone(R)-2-amino-2-(2-chlorophenyl)cyclohexan-1-one
02

Targets

SRR (Serine racemase)NMDAR (Glutamate receptor ionotropic, NMDA)

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