Drug intelligence / Profile preview

FGIN-1-27

Development stage
Preclinical
Modality
Small Molecules
Administration
Unknown (preclinical Studies Suggest Oral, Parenteral, And Topical: Studies In Animals Via Injection/oral, Topical In Dermatology Studies)
01

Overview

FGIN-1-27 is a synthetic **small molecule** originally developed as a potent and selective **agonist of the mitochondrial diazepam binding inhibitor receptor (MDR)**, also known as the peripheral benzodiazepine receptor or translocator protein (**TSPO**). It is *blood-brain barrier permeable* and has shown **anxiolytic, anti-convulsant, pro-apoptotic, and steroidogenic activities** across various studies. FGIN-1-27 was initially recognized for its interaction with TSPO, leading to increased production of **neurosteroids** (such as pregnenolone) and modulation of **Leydig cell testosterone** synthesis without suppressing spermatogenesis. More recent data demonstrate that its immunomodulatory actions—such as **inhibition of IL-17 production, suppression of pathogenic Th17 cell differentiation, and amelioration of autoimmune responses (notably EAE, a model of multiple sclerosis)**—occur independently of TSPO and instead result from **metabolic reprogramming** (shifting glycolytic and amino acid metabolism and activating amino acid starvation response signaling in Th17 cells). FGIN-1-27 also exhibits **anti-melanogenic** effects by suppressing the PKA/CREB, PKC-β, and MAPK pathways in melanocytes, suggesting possible application as a skin depigmenting agent.

Other names
N,N-dihexyl-2-(4-fluorophenyl)indole-3-acetamide
02

Targets

TSPO (Translocator Protein (18 kDa))

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