PCB2

PCB2 is a small molecule Sigma-1 receptor (S1R) agonist developed by researchers at the Università degli Studi "G. d'Annunzio" di Chieti-Pescara. It is a synthetic amino-enone derivative specifically designed to target the Sigma-1 receptor, a molecular chaperone located at the endoplasmic reticulum-mitochondrion interface that plays a critical role in calcium signaling, protein folding, and neuroplasticity. Preclinical studies have demonstrated that PCB2 exerts rapid and sustained antidepressant-like effects in animal models, particularly in those representing treatment-resistant depression (TRD). Its mechanism of action involves the stabilization of the Sigma-1 receptor in its active conformation, which subsequently modulates glutamatergic neurotransmission and enhances the expression of brain-derived neurotrophic factor (BDNF), potentially reversing the synaptic deficits associated with chronic stress and depression.

Other names

(E)-1-phenyl-3-(cyclohexylamino)-2-buten-1-one