Sigma-LIGAND-1是σ受体(sigmareceptor)的选择性配体,在DTG和PPP位点的IC50值分别为16和19nM,在多巴胺受体D2的Ki值为4000nM。
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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.
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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