Therapeutic Targets Database
BIDD Pharmainformatics Databases


Target Validation Information
Target NameSigma(1)-type opioid receptor    
Type of TargetSuccessful target    
Drug Potency against TargetDextromethorphanIC50 = 2500 nM[1]
OPC-14523IC50 = 2.3 nM[2]
OPC-14523IC50 = 2.3 nM[3]
E-5842IC50 > 100000 nM[4]
Ref 1Curr Top Med Chem. 2006;6(8):749-70.N-methyl-D-aspartate receptor (NMDA) antagonists as potential pain therapeutics. To Reference
Ref 2Neuropharmacology. 2001 Dec;41(8):976-88.Antidepressant-like responses to the combined sigma and 5-HT1A receptor agonist OPC-14523. To Reference
Ref 3Curr Top Med Chem. 2008;8(12):1008-23.5-HT1 receptor augmentation strategies as enhanced efficacy: therapeutics for psychiatric disorders. To Reference
Ref 4Mini Rev Med Chem. 2008 Oct;8(12):1243-51.Recent advances in the research of HIV-1 RNase H inhibitors. To Reference
Ref 5J Med Chem. 1994 Jun 10;37(12):1737-9.Synthesis and characterization of [125I]-N-(N-benzylpiperidin-4-yl)-4- iodobenzamide, a new sigma receptor radiopharmaceutical: high-affinity binding to MCF-7 breast tumor cells. To Reference


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