Sigma2 Receptor Antagonists Small Molecules and Peptides

σ2 receptors are members of the sigma (σ) family of receptors that also includes σ1 receptors. Originally thought to be opioid receptors or the phencyclidine binding site on the NMDA receptor, more recently σ2 receptors have been identified as the endoplasmic reticulum transmembrane protein, TMEM97.

This protein regulates the sterol transporter Niemann-Pick disease protein (NPC1), and is involved in cholesterol homeostasis. An inherited mutation in the gene for NPC1 causes ...