Therapeutic Targets Database
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TTD Target ID: TTDS00129

Target Information
NameSigma(1)-type opioid receptor    
Type of targetSuccessful target    
SynonymsOPRS1 protein    
Opioid receptor, sigma 1, isoform 1    
SR31747 binding protein 1    
DiseaseNeuropsychiatric disorders    [1][2]
Drug(s)DextromethorphanApprovedCough and Pain[3]
OPC-14523Phase IIBulimia nervosa OCD MDD, Severe Mood Disorders[4]
ANAVEX 2-73Phase IAlzheimer¡¯s disease[5]
OPC-14523Phase IFemale sexual dysfunction[4]
SSR-125047Phase ISchizophrenia[6]
E-6276DiscontinuedSchizophrenia[6]
PRX-00023Discontinued in Phase IISevere Mood Disorders[7]
RimcazoleDiscontinuedSchizophrenia[6]
SR-31742ADiscontinuedSchizophrenia[6]
E-5842No development reportedSchizophrenia[6]
MS-377No development reportedSchizophrenia[6]
NE-100No development reportedSchizophrenia[6]
Sigma antagonistNo development reportedSchizophrenia[6]
ANAVEX 1-41PreclinicalAlzheimer¡¯s disease[5]
ANAVEX 1007PreclinicalMelanoma, prostate cancer, pancreatic cancer[5]
BioChemical ClassTransmembrane protein    
UniProt IDQ99720
SequenceMQWAVGRRWAWAALLLAVAAVLTQVVWLWLGTQSFVFQREEIAQLARQYAGLDHELAFSR LIVELRRLHPGHVLPDEELQWVFVNAGGWMGAMCLLHASLSEYVLLFGTALGSRGHSGRY WAEISDTIISGTFHQWREGTTKSEVFYPGETVVHGPGEATAVEWGPNTWMVEYGRGVIPS TLAFALADTVFSTQDFLTLFYTLRSYARGLRLELTTYLFGQDP
Target ValidationClick to Find Target Validation Information.    
QSAR ModelClick to Find Target QSAR Model.    
InhibitorDITOLYLGUANIDINE[8]
Dimethyltryptamine[9]
AgonistANAVEX 1-41[5]
ANAVEX 1007[5]
ANAVEX 2-73[5]
Dextromethorphan[3]
Dimemorfan[10]
Igmesine[11][1][2]
OPC-14523[4]
PRX-00023[7]
AntagonistMS-377[6]
NE-100[6]
Rimcazole[6]
Sigma antagonist[6]
BinderE-5842[6]
E-6276[6]
SR-31742A[6]
SSR-125047[6]
MultitargetANAVEX 1007[5]
OPC-14523[4]
PRX-00023[7]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Sigma-1 receptor ligands: potential in the treatment of neuropsychiatric disorders. CNS Drugs. 2004;18(5):269-84. To Reference
Ref 2Strain differences in sigma(1) receptor-mediated behaviours are related to neurosteroid levels. Eur J Neurosci. 2002 May;15(9):1523-34. To Reference
Ref 3Dextromethorphan/quinidine: AVP 923, dextromethorphan/cytochrome P450-2D6 inhibitor, quinidine/dextromethorphan. Drugs R D. 2005;6(3):174-7. To Reference
Ref 4Emerging drugs for eating disorder treatment. Expert Opin Emerg Drugs. 2006 May;11(2):315-36. To Reference
Ref 52011 Pipeline of Anavex. To Reference
Ref 6The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22. Epub 2007 Jul 31. To Reference
Ref 7Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92. Epub 2008 Jan 2. To Reference
Ref 8J 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
Ref 9Strassman RJ, Qualls CR: Dose-response study of N,N-dimethyltryptamine in humans. I. Neuroendocrine, autonomic, and cardiovascular effects. Arch Gen Psychiatry. 1994 Feb;51(2):85-97. To Reference
Ref 10Dimemorfan protects rats against ischemic stroke through activation of sigma-1 receptor-mediated mechanisms by decreasing glutamate accumulation. J Neurochem. 2008 Jan;104(2):558-72. To Reference
Ref 11Antiamnesic and neuroprotective effects of donepezil against learning impairments induced in mice by exposure to carbon monoxide gas. J Pharmacol Exp Ther. 2006 Jun;317(3):1307-19. Epub 2006 Mar 21. To Reference



 

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