Target Information
| Target General Information | Top | |||||
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| Target ID |
T46360
(Former ID: TTDS00129)
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| Target Name |
Opioid receptor sigma 1 (OPRS1)
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| Synonyms |
hSigmaR1; Sigma1R; Sigma1-receptor; Sigma non-opioid intracellular receptor 1; Sigma 1-type opioid receptor; SRBP; SR31747-binding protein; SR31747 binding protein 1; SR-BP; SIG-1R; Opioid receptor, sigma 1, isoform 1; OPRS1 protein; Aging-associated gene 8 protein; AAG8
Click to Show/Hide
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| Gene Name |
SIGMAR1
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 1 Target-related Diseases | + | ||||
| 1 | Cough [ICD-11: MD12] | |||||
| Function |
Involved in the regulation of different receptors it plays a role in BDNF signaling and EGF signaling. Also regulates ion channels like the potassium channel and could modulate neurotransmitter release. Plays a role in calcium signaling through modulation together with ANK2 of the ITP3R-dependent calcium efflux at the endoplasmic reticulum. Plays a role in several other cell functions including proliferation, survival and death. Originally identified for its ability to bind various psychoactive drugs it is involved in learning processes, memory and mood alteration. Necessary for proper mitochondrial axonal transport in motor neurons, in particular the retrograde movement of mitochondria. Plays a role in protecting cells against oxidative stress-induced cell death via its interaction with RNF112. Functions in lipid transport from the endoplasmic reticulum and is involved in a wide array of cellular functions probably through regulation of the biogenesis of lipid microdomains at the plasma membrane.
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| BioChemical Class |
GPCR rhodopsin
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| UniProt ID | ||||||
| Sequence |
MQWAVGRRWAWAALLLAVAAVLTQVVWLWLGTQSFVFQREEIAQLARQYAGLDHELAFSR
LIVELRRLHPGHVLPDEELQWVFVNAGGWMGAMCLLHASLSEYVLLFGTALGSRGHSGRY WAEISDTIISGTFHQWREGTTKSEVFYPGETVVHGPGEATAVEWGPNTWMVEYGRGVIPS TLAFALADTVFSTQDFLTLFYTLRSYARGLRLELTTYLFGQDP Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | PDB | ||||
| ADReCS ID | BADD_A01381 | |||||
| HIT2.0 ID | T70U24 | |||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Approved Drug(s) | [+] 2 Approved Drugs | + | ||||
| 1 | Dextromethorphan | Drug Info | Approved | Cough | [2], [3] | |
| 2 | Dextromethorphan Polistirex | Drug Info | Approved | Dry cough | [4] | |
| Clinical Trial Drug(s) | [+] 7 Clinical Trial Drugs | + | ||||
| 1 | ADX N05 | Drug Info | Phase 3 | Mood disorder | [9] | |
| 2 | Igmesine | Drug Info | Phase 2 | Major depressive disorder | [10] | |
| 3 | OPC-14523 | Drug Info | Phase 2 | Mood disorder | [11] | |
| 4 | ANAVEX 2-73 | Drug Info | Phase 1 | Alzheimer disease | [7], [8] | |
| 5 | SA-5845 | Drug Info | Phase 1 | Central nervous system disease | [13], [14], [15] | |
| 6 | SSR-125047 | Drug Info | Phase 1 | Schizophrenia | [16] | |
| 7 | SSR-125329A | Drug Info | Phase 1 | Immune System disease | [17] | |
| Discontinued Drug(s) | [+] 17 Discontinued Drugs | + | ||||
| 1 | BMS-181100 | Drug Info | Discontinued in Phase 3 | Psychotic disorder | [18], [19] | |
| 2 | KB-5492 | Drug Info | Discontinued in Phase 2 | Peptic ulcer | [20] | |
| 3 | OxycoDex | Drug Info | Discontinued in Phase 2 | Pain | [21] | |
| 4 | Panamesine | Drug Info | Discontinued in Phase 2 | Psychotic disorder | [22] | |
| 5 | Gevotroline | Drug Info | Discontinued in Phase 1 | Psychotic disorder | [24] | |
| 6 | AH-9700 | Drug Info | Terminated | Pollakiuria | [29] | |
| 7 | E-5842 | Drug Info | Terminated | Schizophrenia | [16] | |
| 8 | E-6276 | Drug Info | Terminated | Schizophrenia | [16] | |
| 9 | HydrocoDex | Drug Info | Terminated | Pain | [14], [15] | |
| 10 | LU-29252 | Drug Info | Terminated | Anxiety disorder | [30] | |
| 11 | MS-377 | Drug Info | Terminated | Schizophrenia | [16] | |
| 12 | NE-033 | Drug Info | Terminated | Psychotic disorder | [31] | |
| 13 | NE-100 | Drug Info | Terminated | Schizophrenia | [32], [16] | |
| 14 | NPC-16377 | Drug Info | Terminated | Psychotic disorder | [33] | |
| 15 | PRE-084 | Drug Info | Terminated | Aging skin | [34], [35] | |
| 16 | Rimcazole | Drug Info | Terminated | Schizophrenia | [16] | |
| 17 | SR-31742A | Drug Info | Terminated | Schizophrenia | [16] | |
| Preclinical Drug(s) | [+] 3 Preclinical Drugs | + | ||||
| 1 | ANAVEX 1-41 | Drug Info | Preclinical | Alzheimer disease | [25] | |
| 2 | ANAVEX 1007 | Drug Info | Preclinical | Pancreatic cancer | [25] | |
| 3 | Cutamesine | Drug Info | Preclinical | Major depressive disorder | [26] | |
| Mode of Action | [+] 6 Modes of Action | + | ||||
| Agonist | [+] 14 Agonist drugs | + | ||||
| 1 | Dextromethorphan | Drug Info | [1] | |||
| 2 | Igmesine | Drug Info | [38], [39], [40] | |||
| 3 | ANAVEX 2-73 | Drug Info | [25] | |||
| 4 | ANAVEX 1-41 | Drug Info | [25] | |||
| 5 | ANAVEX 1007 | Drug Info | [25] | |||
| 6 | Cutamesine | Drug Info | [14], [15], [50] | |||
| 7 | (+)-SK&F10047 | Drug Info | [56] | |||
| 8 | (RS)-PPCC | Drug Info | [57] | |||
| 9 | 1,3-ditolylguanidine | Drug Info | [58], [59] | |||
| 10 | C-10068 | Drug Info | [14], [15] | |||
| 11 | Dimemorfan | Drug Info | [62] | |||
| 12 | MC-113 | Drug Info | [14], [15] | |||
| 13 | MC-116 | Drug Info | [14], [15] | |||
| 14 | [3H]pentazocine | Drug Info | [56] | |||
| Modulator | [+] 13 Modulator drugs | + | ||||
| 1 | Dextromethorphan Polistirex | Drug Info | [36] | |||
| 2 | ADX N05 | Drug Info | [37] | |||
| 3 | OPC-14523 | Drug Info | [41] | |||
| 4 | BMS-181100 | Drug Info | [44], [45] | |||
| 5 | OxycoDex | Drug Info | [14], [15] | |||
| 6 | Gevotroline | Drug Info | [48], [49] | |||
| 7 | AH-9700 | Drug Info | [51] | |||
| 8 | HydrocoDex | Drug Info | [14], [15] | |||
| 9 | LU-29252 | Drug Info | [14], [15], [52] | |||
| 10 | NE-033 | Drug Info | [14], [15], [53] | |||
| 11 | NPC-16377 | Drug Info | [14], [15], [54] | |||
| 12 | PRE-084 | Drug Info | [14], [15], [55] | |||
| 13 | CNS-1169 | Drug Info | [14], [15] | |||
| Binder | [+] 7 Binder drugs | + | ||||
| 1 | SA-5845 | Drug Info | [13], [14], [15] | |||
| 2 | SSR-125047 | Drug Info | [16] | |||
| 3 | SSR-125329A | Drug Info | [14], [15], [17] | |||
| 4 | Panamesine | Drug Info | [14], [15], [47] | |||
| 5 | E-5842 | Drug Info | [16] | |||
| 6 | E-6276 | Drug Info | [16] | |||
| 7 | SR-31742A | Drug Info | [16] | |||
| Inhibitor | [+] 4 Inhibitor drugs | + | ||||
| 1 | 1,2,4-triazole derivative 3 | Drug Info | [42] | |||
| 2 | 1,2,4-triazole derivative 4 | Drug Info | [42] | |||
| 3 | Pyrazole derivative 86 | Drug Info | [42] | |||
| 4 | 2-(1H-indol-3-yl)-N,N-dimethylethanamine | Drug Info | [60] | |||
| Antagonist | [+] 8 Antagonist drugs | + | ||||
| 1 | Aryl alkanolamine derivative 1 | Drug Info | [42] | |||
| 2 | Aryl alkanolamine derivative 2 | Drug Info | [42] | |||
| 3 | KB-5492 | Drug Info | [14], [15], [46] | |||
| 4 | MS-377 | Drug Info | [16] | |||
| 5 | NE-100 | Drug Info | [16] | |||
| 6 | Rimcazole | Drug Info | [16] | |||
| 7 | BD-1047 | Drug Info | [61] | |||
| 8 | CM-156 | Drug Info | [14], [15] | |||
| Ligand | [+] 19 Ligand drugs | + | ||||
| 1 | Benzamide derivative 10 | Drug Info | [43] | |||
| 2 | Benzamide derivative 7 | Drug Info | [43] | |||
| 3 | Benzamide derivative 8 | Drug Info | [43] | |||
| 4 | Benzamide derivative 9 | Drug Info | [43] | |||
| 5 | Isoindoline derivative 1 | Drug Info | [43] | |||
| 6 | Isoindoline derivative 2 | Drug Info | [43] | |||
| 7 | Isoindoline derivative 3 | Drug Info | [43] | |||
| 8 | Isoindoline derivative 4 | Drug Info | [43] | |||
| 9 | Isoindoline derivative 5 | Drug Info | [43] | |||
| 10 | Phenylpropylamine derivative 1 | Drug Info | [42] | |||
| 11 | Phenylpropylamine derivative 2 | Drug Info | [42] | |||
| 12 | Phenylpropylamine derivative 3 | Drug Info | [42] | |||
| 13 | Phenylpropylamine derivative 4 | Drug Info | [42] | |||
| 14 | Phenylpropylamine derivative 5 | Drug Info | [42] | |||
| 15 | Piperazine derivative 7 | Drug Info | [42] | |||
| 16 | Piperidine derivative 6 | Drug Info | [42] | |||
| 17 | PMID28051882-Compound-XIV | Drug Info | [42] | |||
| 18 | PMID30185082-Compound-57 | Drug Info | [43] | |||
| 19 | PMID30185082-Compound-64 | Drug Info | [43] | |||
| Cell-based Target Expression Variations | Top | |||||
|---|---|---|---|---|---|---|
| Cell-based Target Expression Variations | ||||||
| Drug Binding Sites of Target | Top | |||||
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| Ligand Name: Haloperidol | Ligand Info | |||||
| Structure Description | Human sigma-1 receptor bound to haloperidol | PDB:6DJZ | ||||
| Method | X-ray diffraction | Resolution | 3.08 Å | Mutation | No | [63] |
| PDB Sequence |
RWAWAALLLA
17 VAAVLTQVVW27 LWLGTQSFVF37 QREEIAQLAR47 QYAGLDHELA57 FSRLIVELRR 67 LHPGHVLPDE77 ELQWVFVNAG87 GWMGAMCLLH97 ASLSEYVLLF107 GTALGSRGHS 117 GRYWAEISDT127 IISGTFHQWR137 EGTTKSEVFY147 PGETVVHGPG157 EATAVEWGPN 167 TWMVEYGRGV177 IPSTLAFALA187 DTVFSTQDFL197 TLFYTLRSYA207 RGLRLELTTY 217 LF
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VAL84
4.653
TRP89
4.113
MET93
3.576
LEU95
4.728
TYR103
3.588
LEU105
3.719
PHE107
4.605
HIS116
4.788
SER117
3.315
TYR120
3.113
ILE124
3.917
ASP126
2.818
PHE133
3.811
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| Ligand Name: PD-144418 | Ligand Info | |||||
| Structure Description | Human sigma-1 receptor bound to PD144418 | PDB:5HK1 | ||||
| Method | X-ray diffraction | Resolution | 2.51 Å | Mutation | No | [64] |
| PDB Sequence |
RWAWAALLLA
17 VAAVLTQVVW27 LWLGTQSFVF37 QREEIAQLAR47 QYAGLDHELA57 FSRLIVELRR 67 LHPGHVLPDE77 ELQWVFVNAG87 GWMGAMCLLH97 ASLSEYVLLF107 GTALGSRGHS 117 GRYWAEISDT127 IISGTFHQWR137 EGTTKSEVFY147 PGETVVHGPG157 EATAVEWGPN 167 TWMVEYGRGV177 IPSTLAFALA187 DTVFSTQDFL197 TLFYTLRSYA207 RGLRLELTTY 217 LF
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VAL84
3.971
TRP89
3.866
MET93
3.828
LEU95
4.451
ALA98
4.674
TYR103
3.988
LEU105
3.531
PHE107
3.577
SER117
3.796
TYR120
3.374
ILE124
3.639
ASP126
3.067
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| Click to View More Binding Site Information of This Target with Different Ligands | ||||||
| Different Human System Profiles of Target | Top |
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Human Similarity Proteins
of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.
A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs
(Brief Bioinform, 21: 649-662, 2020).
Human Tissue Distribution
of target is determined from a proteomics study that quantified more than 12,000 genes across 32 normal human tissues. Tissue Specificity (TS) score was used to define the enrichment of target across tissues.
The distribution of targets among different tissues or organs need to be taken into consideration when assessing the target druggability, as it is generally accepted that the wider the target distribution, the greater the concern over potential adverse effects
(Nat Rev Drug Discov, 20: 64-81, 2021).
Biological Network Descriptors
of target is determined based on a human protein-protein interactions (PPI) network consisting of 9,309 proteins and 52,713 PPIs, which were with a high confidence score of ≥ 0.95 collected from STRING database.
The network properties of targets based on protein-protein interactions (PPIs) have been widely adopted for the assessment of target’s druggability. Proteins with high node degree tend to have a high impact on network function through multiple interactions, while proteins with high betweenness centrality are regarded to be central for communication in interaction networks and regulate the flow of signaling information
(Front Pharmacol, 9, 1245, 2018;
Curr Opin Struct Biol. 44:134-142, 2017).
Human Similarity Proteins
Human Tissue Distribution
Biological Network Descriptors
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There is no similarity protein (E value < 0.005) for this target
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Note:
If a protein has TS (tissue specficity) scores at least in one tissue >= 2.5, this protein is called tissue-enriched (including tissue-enriched-but-not-specific and tissue-specific). In the plots, the vertical lines are at thresholds 2.5 and 4.
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| Degree | 7 | Degree centrality | 7.52E-04 | Betweenness centrality | 3.73E-04 |
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| Closeness centrality | 2.09E-01 | Radiality | 1.36E+01 | Clustering coefficient | 4.76E-02 |
| Neighborhood connectivity | 1.56E+01 | Topological coefficient | 1.58E-01 | Eccentricity | 11 |
| Download | Click to Download the Full PPI Network of This Target | ||||
| Chemical Structure based Activity Landscape of Target | Top |
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| Drug Property Profile of Target | Top | |
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| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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| "RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five | ||
| Co-Targets | Top | |||||
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| Co-Targets | ||||||
| Target Poor or Non Binders | Top | |||||
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| Target Poor or Non Binders | ||||||
| Target Regulators | Top | |||||
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| Target-regulating microRNAs | ||||||
| Target Profiles in Patients | Top | |||||
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| Target Expression Profile (TEP) | ||||||
| Target Affiliated Biological Pathways | Top | |||||
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| WikiPathways | [+] 2 WikiPathways | + | ||||
| 1 | miR-targeted genes in squamous cell - TarBase | |||||
| 2 | miR-targeted genes in lymphocytes - TarBase | |||||
| Target-Related Models and Studies | Top | |||||
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| Target Validation | ||||||
| Target QSAR Model | ||||||
| References | Top | |||||
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| REF 1 | Dextromethorphan/quinidine: AVP 923, dextromethorphan/cytochrome P450-2D6 inhibitor, quinidine/dextromethorphan. Drugs R D. 2005;6(3):174-7. | |||||
| REF 2 | URL: 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 3 | Molecular insights and therapeutic targets in amyotrophic lateral sclerosis. CNS Neurol Disord Drug Targets. 2008 Feb;7(1):11-9. | |||||
| REF 4 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
| REF 5 | Pharmaceutical Research Companies Are Developing More Than 300 Medicines to Treat Mental Illnesses. Pharmaceutical Research and Manufacturers of America report.2010. | |||||
| REF 6 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 7 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 8 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 9 | 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 10 | 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 11 | Designing drugs for the treatment of female sexual dysfunction. Drug Discov Today. 2007 Sep;12(17-18):757-66. | |||||
| REF 12 | ClinicalTrials.gov (NCT04442945) A Double-blind, Randomized, Placebo-controlled, Phase 1 Safety and Tolerability, and Pharmacokinetics Study of ANAVEX3-71. U.S.National Institutes of Health. | |||||
| REF 13 | 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 14 | Antitussives and substance abuse. Subst Abuse Rehabil. 2013 Nov 6;4:75-82. | |||||
| REF 15 | 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 16 | The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22. | |||||
| REF 17 | SSR125329A, a high affinity sigma receptor ligand with potent anti-inflammatory properties. Eur J Pharmacol. 2002 Dec 5;456(1-3):123-31. | |||||
| REF 18 | URL: 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 19 | 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 20 | 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 21 | 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 22 | 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 23 | 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 24 | 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 25 | 2011 Pipeline of Anavex. | |||||
| REF 26 | 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 27 | 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 28 | 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 29 | 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 30 | 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 31 | 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 32 | URL: 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 33 | 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 34 | URL: 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 35 | Self-administration of cocaine induces dopamine-independent self-administration of sigma agonists. Neuropsychopharmacology. 2013 Mar;38(4):605-15. | |||||
| REF 36 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. | |||||
| REF 37 | Clinical pipeline report, company report or official report of SK BioPhamaceuticals. | |||||
| REF 38 | 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. | |||||
| REF 39 | Sigma-1 receptor ligands: potential in the treatment of neuropsychiatric disorders. CNS Drugs. 2004;18(5):269-84. | |||||
| REF 40 | Strain differences in sigma(1) receptor-mediated behaviours are related to neurosteroid levels. Eur J Neurosci. 2002 May;15(9):1523-34. | |||||
| REF 41 | Antidepressant-like responses to the combined sigma and 5-HT1A receptor agonist OPC-14523. Neuropharmacology. 2001 Dec;41(8):976-88. | |||||
| REF 42 | Are sigma modulators an effective opportunity for cancer treatment A patent overview (1996-2016).Expert Opin Ther Pat. 2017 May;27(5):565-578. | |||||
| REF 43 | The sigma-2 (-2) receptor: a review of recent patent applications: 2013-2018.Expert Opin Ther Pat. 2018 Sep;28(9):655-663. | |||||
| REF 44 | BMY 14802, a sigma receptor ligand for the treatment of schizophrenia. Neuropsychopharmacology. 1994 Feb;10(1):37-40. | |||||
| REF 45 | The effects of BMY-14802 against L-DOPA- and dopamine agonist-induced dyskinesia in the hemiparkinsonian rat | |||||
| REF 46 | 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 47 | 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 48 | Sigma receptor ligands alter concentrations of corticosterone in plasma in the rat. Neuropharmacology. 1991 Jan;30(1):79-87. | |||||
| REF 49 | Neuroendocrinological and neurochemical effects of sigma ligands. Neuropharmacology. 1992 Feb;31(2):157-62. | |||||
| REF 50 | 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 51 | Pharmacological actions of AH-9700 on micturition reflex in anesthetized rats. Eur J Pharmacol. 2001 Jan 26;412(2):171-9. | |||||
| REF 52 | 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 53 | 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 54 | 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 55 | 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 56 | URL: 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 57 | Novel sigma receptor ligands: synthesis and biological profile. J Med Chem. 2007 Mar 8;50(5):951-61. | |||||
| REF 58 | Sigma1 and sigma2 receptor binding affinity and selectivity of SA4503 and fluoroethyl SA4503. Synapse. 2006 May;59(6):350-8. | |||||
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