Sigma1 Receptor Antagonists Small Molecules and Peptides

σ₁ receptors are members of the σ family of receptors that also includes σ₂ receptors. Originally thought to be opioid receptors or the phencyclidine binding site on the NMDA receptor, they are now known to be distinct targets. These receptors are distinguished from σ₂ receptors as they exhibit high affinity and stereoselectivity for the (+)-isomers of pentazocine, SK&F 10047 and cyclazocine, as well as having different tissue distribution patterns and subcellular ...