Drug intelligence / Profile preview

NE-100

Development stage
Unknown
Modality
Small Molecules
Administration
Oral
01

Overview

NE-100 is a **selective antagonist** of the sigma-1 receptor, one of the earliest such ligands reported and widely used as a pharmacological tool[1][3][7][9]. It exhibits **high affinity for the sigma-1 receptor** (Ki ≈ 1 nM) and markedly lower affinity for other receptors such as sigma-2, dopamine, and serotonin receptors[1][3]. NE-100 has been studied for its **potential antipsychotic activity without the typical motor side effects of neuroleptics**, and it shows neuroprotective and procognitive properties in preclinical models[3][5][7][9][15]. NE-100 is primarily used in research; it is not an approved pharmaceutical for clinical use and is known as a tool compound for investigating sigma-1 receptor physiology and pharmacology[1][3][5][9][13][15].

Other names
4-methoxy-3-(2-phenylethoxy)-N,N-dipropylbenzeneethanamineN,N-dipropyl-2-[4-methoxy-3-(2-phenylethoxy)phenyl]-ethylamine monohydrochloride
02

Targets

SIGMAR1 (Sigma non-opioid intracellular receptor 1)TMEM97 (Sigma-2 receptor complex (TMEM97/PGRMC1))

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