Sigma-LIGAND-1

Sigma-LIGAND-1 is a selective sigma receptor ligand, has receptor IC50s of 16 nM at the DTG site, 19 nM at the PPP site, and a Ki of 4000 nM at the dopamine D2 receptor.

Signaling Pathways >> GPCR/G Protein >> Sigma Receptor

Research Areas >> Neurological Disease

IC50: 16 nM (DTG site of sigma receptor), 19 nM (PPP site of sigma receptor)[1] Ki: 4000 nM (Dopamine D2 receptor)[1]

Administration of Sigma-LIGAND-1 would reverse amphetamine-induced hyperlocomotion in mice, a behavioral model sensitive to antipsychotic compounds. Sigma-LIGAND-1 and its structural analogues have the potential antipsychotic activity[1].

[1]. Erickson RH, et al. (Aminoalkoxy)chromones. Selective sigma receptor ligands. J Med Chem. 1992 May 1;35(9):1526-35.

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