Target Information
Target General Infomation | |||||
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Target ID |
T46360
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Former ID |
TTDS00129
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Target Name |
Sigma(1)-type opioid receptor
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Gene Name |
SIGMAR1
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Synonyms |
OPRS1 protein; Opioid receptor, sigma 1, isoform 1; SR31747 binding protein 1; SIGMAR1
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Target Type |
Successful
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Disease | Aging skin [ICD10: L00-L99] | ||||
Alzheimer disease [ICD9: 331; ICD10: G30] | |||||
Anxiety disorder [ICD9: 300, 311; ICD10: F32, F40-F42] | |||||
Brain injury [ICD10: S09.90] | |||||
Breast cancer [ICD9: 174, 175; ICD10: C50] | |||||
Bulimia nervosa; Severe mood disorders [ICD9: 296, 307.51; ICD10: F30-F39, F50.2] | |||||
Cough; Pain [ICD9: 338, 786.2,780; ICD10: R05, R52, G89] | |||||
Central nervous system disease [ICD10: G00-G99] | |||||
Drug abuse [ICD9: 303-304; ICD10: F10-F19] | |||||
Dry cough [ICD10: R05] | |||||
Excessive daytime sleepiness [ICD9: 291.82, 292.85, 307.43-307.44, 327.1, 780.53-780.54; ICD10: F51.1, G47.1] | |||||
Female sexual dysfunction [ICD9: 302.7; ICD10: F52] | |||||
Immuno-modulator [ICD9: 135, 691.8, 692.9, 710-719, 714; ICD10: D86, L20, L20-L30, M00-M25, M05-M06] | |||||
Major depressive disorder [ICD9: 296.2, 296.3, 710.0; ICD10: F32, F33, M32] | |||||
Melanoma; Prostate cancer; Pancreatic cancer [ICD9: 140-229, 157, 172, 185; ICD10: C25, C43, C61] | |||||
Mood disorder [ICD10: F30-F39] | |||||
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89] | |||||
Psychotic disorders [ICD9: 290-299; ICD10: F20-F29] | |||||
Peptic ulcer [ICD9: 531-534; ICD10: K25-K27] | |||||
Pollakiuria [ICD10: R35] | |||||
Schizophrenia [ICD9: 295; ICD10: F20] | |||||
BioChemical Class |
Transmembrane protein
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Target Validation |
T46360
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UniProt ID | |||||
Sequence |
MQWAVGRRWAWAALLLAVAAVLTQVVWLWLGTQSFVFQREEIAQLARQYAGLDHELAFSR
LIVELRRLHPGHVLPDEELQWVFVNAGGWMGAMCLLHASLSEYVLLFGTALGSRGHSGRY WAEISDTIISGTFHQWREGTTKSEVFYPGETVVHGPGEATAVEWGPNTWMVEYGRGVIPS TLAFALADTVFSTQDFLTLFYTLRSYARGLRLELTTYLFGQDP |
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Drugs and Mode of Action | |||||
Drug(s) | Dextromethorphan | Drug Info | Approved | Cough; Pain | [536631], [541989] |
Dextromethorphan Polistirex | Drug Info | Approved | Dry cough | [551871] | |
ADX N05 | Drug Info | Phase 3 | Mood disorder | [548910] | |
CM-2395 | Drug Info | Phase 3 | Schizophrenia | [551513] | |
ADX N05 | Drug Info | Phase 2 | Excessive daytime sleepiness | [548910] | |
ANAVEX 2-73 | Drug Info | Phase 2 | Breast cancer | [531153], [532266] | |
Igmesine | Drug Info | Phase 2 | Major depressive disorder | [544891] | |
OPC-14523 | Drug Info | Phase 2 | Bulimia nervosa; Severe mood disorders | [536493] | |
ANAVEX 2-73 | Drug Info | Phase 1 | Alzheimer disease | [549727] | |
AVP-786 | Drug Info | Phase 1 | Pain | [526642], [532713] | |
OPC-14523 | Drug Info | Phase 1 | Female sexual dysfunction | [536493] | |
SA-5845 | Drug Info | Phase 1 | Central nervous system disease | [526642], [527279], [532713] | |
SSR-125047 | Drug Info | Phase 1 | Schizophrenia | [536463] | |
SSR-125329A | Drug Info | Phase 1 | Immuno-modulator | [526469] | |
ANAVEX 1-41 | Drug Info | Preclinical | Alzheimer disease | [549727] | |
ANAVEX 1007 | Drug Info | Preclinical | Melanoma; Prostate cancer; Pancreatic cancer | [549727] | |
Cutamesine | Drug Info | Preclinical | Major depressive disorder | [546327] | |
SA-5845 | Drug Info | Preclinical | Psychotic disorders | [525883] | |
BMS-181100 | Drug Info | Discontinued in Phase 3 | Psychotic disorders | [542913], [544706] | |
KB-5492 | Drug Info | Discontinued in Phase 2 | Peptic ulcer | [544799] | |
OxycoDex | Drug Info | Discontinued in Phase 2 | Pain | [547593] | |
Panamesine | Drug Info | Discontinued in Phase 2 | Psychotic disorders | [544890] | |
DUP-734 | Drug Info | Discontinued in Phase 1 | Psychotic disorders | [544981] | |
Gevotroline | Drug Info | Discontinued in Phase 1 | Psychotic disorders | [544877] | |
AH-9700 | Drug Info | Terminated | Pollakiuria | [546850] | |
CNS-1307 | Drug Info | Terminated | Schizophrenia | [545363] | |
E-5842 | Drug Info | Terminated | Schizophrenia | [536463] | |
E-6276 | Drug Info | Terminated | Schizophrenia | [536463] | |
FH-510 | Drug Info | Terminated | Psychotic disorders | [545084] | |
HydrocoDex | Drug Info | Terminated | Pain | [526642], [532713] | |
LU-29252 | Drug Info | Terminated | Anxiety disorder | [545515] | |
MS-377 | Drug Info | Terminated | Schizophrenia | [536463] | |
NE-033 | Drug Info | Terminated | Psychotic disorders | [545663] | |
NE-100 | Drug Info | Terminated | Schizophrenia | [536463], [541784] | |
NPC-16377 | Drug Info | Terminated | Psychotic disorders | [545059] | |
PRE-084 | Drug Info | Terminated | Aging skin | [532130], [541783] | |
Rimcazole | Drug Info | Terminated | Schizophrenia | [536463] | |
SR-31742A | Drug Info | Terminated | Schizophrenia | [536463] | |
Agonist | (+)-SK&F10047 | Drug Info | [543646] | ||
(RS)-PPCC | Drug Info | [528705] | |||
1,3-ditolylguanidine | Drug Info | [528020] | |||
ANAVEX 1-41 | Drug Info | [549727] | |||
ANAVEX 1007 | Drug Info | [549727] | |||
ANAVEX 2-73 | Drug Info | [549727] | |||
C-10068 | Drug Info | [526642], [532713] | |||
CM-2395 | Drug Info | [548980] | |||
Cutamesine | Drug Info | [526642], [532713], [534601] | |||
Dextromethorphan | Drug Info | [536078] | |||
Dimemorfan | Drug Info | [536581] | |||
Igmesine | Drug Info | [535460], [535948], [536208] | |||
MC-113 | Drug Info | [526642], [532713] | |||
MC-116 | Drug Info | [526642], [532713] | |||
[3H]pentazocine | Drug Info | [543646] | |||
Modulator | ADX N05 | Drug Info | [551695] | ||
AH-9700 | Drug Info | [525959] | |||
AVP-786 | Drug Info | [526642], [532713] | |||
BMS-181100 | Drug Info | ||||
CNS-1169 | Drug Info | [526642], [532713] | |||
CNS-1307 | Drug Info | [526642], [532713] | |||
Dextromethorphan Polistirex | Drug Info | [556264] | |||
DUP-734 | Drug Info | ||||
FH-510 | Drug Info | [526642], [532713], [533898] | |||
Gevotroline | Drug Info | ||||
HydrocoDex | Drug Info | [526642], [532713] | |||
LU-29252 | Drug Info | [525460], [526642], [532713] | |||
NE-033 | Drug Info | [526642], [532713], [545664] | |||
NPC-16377 | Drug Info | [526642], [532713], [533992] | |||
OPC-14523 | Drug Info | [552279] | |||
OxycoDex | Drug Info | [526642], [532713] | |||
PRE-084 | Drug Info | [526642], [530642], [532713] | |||
Antagonist | BD-1047 | Drug Info | [534090] | ||
CM-156 | Drug Info | [526642], [532713] | |||
KB-5492 | Drug Info | [526642], [532713], [533921] | |||
MS-377 | Drug Info | [536463] | |||
NE-100 | Drug Info | [536463] | |||
Rimcazole | Drug Info | [536463] | |||
Inhibitor | Dimethyltryptamine | Drug Info | [551401] | ||
DITOLYLGUANIDINE | Drug Info | [533852] | |||
Binder | E-5842 | Drug Info | [536463] | ||
E-6276 | Drug Info | [536463] | |||
Panamesine | Drug Info | [525495], [526642], [532713] | |||
SA-5845 | Drug Info | [526642], [527279], [532713] | |||
SR-31742A | Drug Info | [536463] | |||
SSR-125047 | Drug Info | [536463] | |||
SSR-125329A | Drug Info | [526469], [526642], [532713] | |||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
References | |||||
Ref 525883 | Preclinical evaluation of [11C]SA4503: radiation dosimetry, in vivo selectivity and PET imaging of sigma1 receptors in the cat brain. Ann Nucl Med. 2000 Aug;14(4):285-92. | ||||
Ref 526469 | SSR125329A, a high affinity sigma receptor ligand with potent anti-inflammatory properties. Eur J Pharmacol. 2002 Dec 5;456(1-3):123-31. | ||||
Ref 526642 | Dextromethorphan antagonizes the acute depletion of brain serotonin by p-chloroamphetamine and H75/12 in rats. Brain Res. 1992 Oct 30;594(2):323-6. | ||||
Ref 527279 | Tumor imaging with 2 sigma-receptor ligands, 18F-FE-SA5845 and 11C-SA4503: a feasibility study. J Nucl Med. 2004 Nov;45(11):1939-45. | ||||
Ref 531153 | Anti-amnesic and neuroprotective potentials of the mixed muscarinic receptor/sigma 1 (?1) ligand ANAVEX2-73, a novel aminotetrahydrofuran derivative. J Psychopharmacol. 2011 Aug;25(8):1101-17. | ||||
Ref 532130 | Self-administration of cocaine induces dopamine-independent self-administration of sigma agonists. Neuropsychopharmacology. 2013 Mar;38(4):605-15. | ||||
Ref 532266 | Blockade of Tau hyperphosphorylation and Abeta?????? generation by the aminotetrahydrofuran derivative ANAVEX2-73, a mixed muscarinic and ???receptor agonist, in a nontransgenic mouse model of Alzheimer's disease. Neuropsychopharmacology. 2013 Aug;38(9):1706-23. | ||||
Ref 536463 | The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22. Epub 2007 Jul 31. | ||||
Ref 536493 | Designing drugs for the treatment of female sexual dysfunction. Drug Discov Today. 2007 Sep;12(17-18):757-66. Epub 2007 Aug 27. | ||||
Ref 536631 | Molecular insights and therapeutic targets in amyotrophic lateral sclerosis. CNS Neurol Disord Drug Targets. 2008 Feb;7(1):11-9. | ||||
Ref 541783 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6678). | ||||
Ref 541784 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6679). | ||||
Ref 541989 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6953). | ||||
Ref 542913 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 8). | ||||
Ref 544706 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000679) | ||||
Ref 544799 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001141) | ||||
Ref 544877 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001398) | ||||
Ref 544890 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001428) | ||||
Ref 544891 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001429) | ||||
Ref 544981 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001777) | ||||
Ref 545059 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001997) | ||||
Ref 545084 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002069) | ||||
Ref 545363 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003010) | ||||
Ref 545515 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003571) | ||||
Ref 545663 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004064) | ||||
Ref 546327 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007486) | ||||
Ref 546850 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010610) | ||||
Ref 547593 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800017613) | ||||
Ref 548910 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800030225) | ||||
Ref 525460 | Involvement of sigma receptors in the modulation of the glutamatergic/NMDA neurotransmission in the dopaminergic systems. Eur J Pharmacol. 1999 Mar 5;368(2-3):183-96. | ||||
Ref 525495 | Efficacy and safety of the sigma receptor ligand EMD 57445 (panamesine) in patients with schizophrenia: an open clinical trial. Pharmacopsychiatry. 1999 Mar;32(2):68-72. | ||||
Ref 525959 | Pharmacological actions of AH-9700 on micturition reflex in anesthetized rats. Eur J Pharmacol. 2001 Jan 26;412(2):171-9. | ||||
Ref 526469 | SSR125329A, a high affinity sigma receptor ligand with potent anti-inflammatory properties. Eur J Pharmacol. 2002 Dec 5;456(1-3):123-31. | ||||
Ref 526642 | Dextromethorphan antagonizes the acute depletion of brain serotonin by p-chloroamphetamine and H75/12 in rats. Brain Res. 1992 Oct 30;594(2):323-6. | ||||
Ref 527279 | Tumor imaging with 2 sigma-receptor ligands, 18F-FE-SA5845 and 11C-SA4503: a feasibility study. J Nucl Med. 2004 Nov;45(11):1939-45. | ||||
Ref 528020 | Sigma1 and sigma2 receptor binding affinity and selectivity of SA4503 and fluoroethyl SA4503. Synapse. 2006 May;59(6):350-8. | ||||
Ref 528705 | Novel sigma receptor ligands: synthesis and biological profile. J Med Chem. 2007 Mar 8;50(5):951-61. Epub 2007 Feb 13. | ||||
Ref 530642 | Antidepressant-like effect of PRE-084, a selective sigma1 receptor agonist, in Albino Swiss and C57BL/6J mice. Pharmacol Rep. 2009 Nov-Dec;61(6):1179-83. | ||||
Ref 533852 | J 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. | ||||
Ref 533898 | FH-510, a potent and selective ligand for rat brain sigma recognition sites. Eur J Pharmacol. 1993 Jul 6;238(1):89-92. | ||||
Ref 533921 | Sigma receptor-mediated effects of a new antiulcer agent, KB-5492, on experimental gastric mucosal lesions and gastric alkaline secretion in rats. J Pharmacol Exp Ther. 1994 May;269(2):799-805. | ||||
Ref 533992 | Effects of the selective sigma receptor ligand, 6-[6-(4-hydroxypiperidinyl)hexyloxy]-3-methylflavone (NPC 16377), on behavioral and toxic effects of cocaine. J Pharmacol Exp Ther. 1993 Aug;266(2):473-82. | ||||
Ref 534090 | Characterization of two novel sigma receptor ligands: antidystonic effects in rats suggest sigma receptor antagonism. Eur J Pharmacol. 1995 Jul 14;280(3):301-10. | ||||
Ref 534601 | Effect of SA4503, a novel sigma1 receptor agonist, against glutamate neurotoxicity in cultured rat retinal neurons. Eur J Pharmacol. 1998 Jan 19;342(1):105-11. | ||||
Ref 535460 | Strain differences in sigma(1) receptor-mediated behaviours are related to neurosteroid levels. Eur J Neurosci. 2002 May;15(9):1523-34. | ||||
Ref 535948 | Sigma-1 receptor ligands: potential in the treatment of neuropsychiatric disorders. CNS Drugs. 2004;18(5):269-84. | ||||
Ref 536078 | Dextromethorphan/quinidine: AVP 923, dextromethorphan/cytochrome P450-2D6 inhibitor, quinidine/dextromethorphan. Drugs R D. 2005;6(3):174-7. | ||||
Ref 536208 | Antiamnesic 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. | ||||
Ref 536463 | The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22. Epub 2007 Jul 31. | ||||
Ref 536581 | Dimemorfan 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. | ||||
Ref 543646 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 2552). | ||||
Ref 545664 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004064) | ||||
Ref 548980 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031127) | ||||
Ref 551401 | Dose-response study of N,N-dimethyltryptamine in humans. I. Neuroendocrine, autonomic, and cardiovascular effects. Arch Gen Psychiatry. 1994 Feb;51(2):85-97. |
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