Drug intelligence / Profile preview

AEX-2

Development stage
Preclinical
Lead developer
NLS Pharmaceutics
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Intraperitoneal (preclinical Studies)
01

Overview

AEX-2 is a non-sulfonamide dual orexin receptor agonist (DOXA) developed by NLS Pharmaceutics and originally by Aexon Labs. It acts as an agonist at both orexin receptor type 1 (OX1R) and orexin receptor type 2 (OX2R), with additional activity at the Sigma-1 receptor. Preclinical studies have shown that AEX-2 enhances wakefulness, preserves REM sleep architecture, and reduces cataplexy episodes in models of narcolepsy type 1. Unlike traditional stimulants or sulfonamide-based orexin agonists, it maintains stable sleep-wake patterns without REM suppression or wake fragmentation. The drug is being explored for narcolepsy and other central nervous system diseases such as neuroinflammation, ALS, Parkinson's disease, and diabetes-associated neurological disorders due to its multi-target mechanism involving both orexin receptors and Sigma-1 modulation[1][6][2].

02

Targets

SIGMAR1 (Sigma non-opioid intracellular receptor 1)HCRTR2 (Orexin/hypocretin receptor type 2)HCRTR1 (Orexin/hypocretin receptor type 1)

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