Sigma 1 Receptor Modulator

Sigma-1 receptor modulator-1 is a sigma-1 receptor modulator and acetylcholinesterase (AChE) inhibitor. Sigma-1 receptor modulator-1 binds to sigma-1 receptors in guinea pigs with a K_i of 1.8 nM. Sigma-1 receptor modulator-1 modulates chaperone proteins, restores calcium homeostasis, and controls ROS production. Sigma-1 receptor modulator-1 inhibits AChE activity and scavenges free radicals. Sigma-1 receptor modulator-1 can be used for research on neurodegenerative diseases.

SKF83959 is a potent and selective dopamine D₁-like receptor partial agonist. SKF83959 K_i values for rat D₁, D₅, D₂ and D₃ receptors are 1.18, 7.56, 920 and 399 nM, respectively. SKF83959 is a potent allosteric modulator of sigma (σ)-1 receptor. SKF83959 belongs to benzazepine family and has improvements on cognitive dysfunction. SKF83959 can be used for the research of Alzheimer's disease and depression.

Phenyltoloxamine (Bistrimin) is an antihistamine agent with sedative and analgesic effects. Phenyltoloxamine also has potent Sigma-1 receptor binding affinity (K_i: 160 nM).