SIGMAR1

Summary

Gene Symbol: SIGMAR1
Description: sigma non-opioid intracellular receptor 1
Alias: ALS16, OPRS1, SR-BP1, SRBP, SIG-1R, SR-BP, SR31747 binding protein 1, aging-associated gene 8 protein, hSigmaR1, sigma 1-type opioid receptor, sigma1R
Species: human

Top Publications

  1. ncbi Expression pattern of sigma receptor 1 mRNA and protein in mammalian retina
    M S Ola
    Department of Cellular Biology and Anatomy, Medical College of Georgia, Augusta, GA 30912, USA
    Brain Res Mol Brain Res 95:86-95. 2001
  2. ncbi Cloning and functional expression of the human type 1 sigma receptor (hSigmaR1)
    R Kekuda
    Department of Biochemistry and Molecular Biology, Medical College of Georgia, Augusta 30912 2100, USA
    Biochem Biophys Res Commun 229:553-8. 1996
  3. ncbi Colocalization of sterol isomerase and sigma(1) receptor at endoplasmic reticulum and nuclear envelope level
    D Dussossoy
    Sanofi Recherche, Montpellier, France Sanofi Recherche, Labege, France
    Eur J Biochem 263:377-86. 1999
  4. ncbi Role of sigma-1 receptor C-terminal segment in inositol 1,4,5-trisphosphate receptor activation: constitutive enhancement of calcium signaling in MCF-7 tumor cells
    Zhiping Wu
    Department of Molecular Pharmacology, Physiology and Biotechnology, Division of Biology and Medicine, Brown University, Providence, Rhode Island 02912, USA
    J Biol Chem 283:28198-215. 2008
  5. ncbi Irreversible blockade of sigma-1 receptors by haloperidol and its metabolites in guinea pig brain and SH-SY5Y human neuroblastoma cells
    Enrique J Cobos
    Department of Pharmacology and Institute of Neuroscience, Faculty of Medicine, University of Granada, Granada, Spain
    J Neurochem 102:812-25. 2007
  6. ncbi Expression pattern of the type 1 sigma receptor in the brain and identity of critical anionic amino acid residues in the ligand-binding domain of the receptor
    P Seth
    Department of Biochemistry and Molecular Biology, Medical College of Georgia, Augusta 30912, USA
    Biochim Biophys Acta 1540:59-67. 2001
  7. ncbi The expression and functional characterization of sigma (sigma) 1 receptors in breast cancer cell lines
    Ebru Aydar
    Division of Cell and Molecular Biology, Imperial College London, Sir Alexander Fleming Building, South Kensington Campus, London SW7 2AZ, UK
    Cancer Lett 242:245-57. 2006
  8. ncbi Regulating ankyrin dynamics: Roles of sigma-1 receptors
    T Hayashi
    Cellular Pathobiology Unit, Cellular Neurobiology Research Branch, Intramural Research Program, National Institute on Drug Abuse National Institutes of Health, 5500 Nathan Shock Drive, Baltimore, MD 21224, USA
    Proc Natl Acad Sci U S A 98:491-6. 2001
  9. ncbi Prevention of excitotoxicity in primary retinal ganglion cells by (+)-pentazocine, a sigma receptor-1 specific ligand
    Ying Dun
    Department of Cellular Biology and Anatomy, Medical College of Georgia, Augusta, Georgia 30912 2000, USA
    Invest Ophthalmol Vis Sci 48:4785-94. 2007
  10. ncbi In vivo protection against retinal neurodegeneration by sigma receptor 1 ligand (+)-pentazocine
    Sylvia B Smith
    Departments of Cellular Biology and Anatomy, Medical College of Georgia, Augusta, Georgia, USA
    Invest Ophthalmol Vis Sci 49:4154-61. 2008

Research Grants

  1. Sigma Receptor Structure /Function /K+ Channel Modulation
    ARNOLD RUOHO; Fiscal Year: 2007
  2. SIGMA LIGANDS FOR THE TREATMENT OF COCAINE OVERDOSE
    Rae Matsumoto; Fiscal Year: 2007
  3. SYNTHESIS AND PHARMACOLOGY OF NOVEL OPIATE LIGANDS
    Gavril Pasternak; Fiscal Year: 2002
  4. Synthesis and pharmacology of novel opiates and their modulatory systems
    Gavril W Pasternak; Fiscal Year: 2010
  5. MOLECULAR BASIS OF REOVIRUS PATHOGENESIS
    Terence Dermody; Fiscal Year: 2007
  6. OPIATE RECEPTOR PHARMACOLOGY
    Gavril Pasternak; Fiscal Year: 2007
  7. Synthesis & Pharmacology of Novel Opiates and Systems
    Gavril Pasternak; Fiscal Year: 2007
  8. Structural Analysis of Reovirus Attachment Mechanisms
    Thilo Stehle; Fiscal Year: 2004
  9. Structural Analysis of Reovirus Attachment Mechanisms
    Terence Dermody; Fiscal Year: 2006
  10. RETINAL PIGMENT EPITHELIUM: VECTORIAL TRANSPORT FUNCTION
    Sylvia Smith; Fiscal Year: 2003

Scientific Experts

Detail Information

Publications104 found, 100 shown here

  1. ncbi Expression pattern of sigma receptor 1 mRNA and protein in mammalian retina
    M S Ola
    Department of Cellular Biology and Anatomy, Medical College of Georgia, Augusta, GA 30912, USA
    Brain Res Mol Brain Res 95:86-95. 2001
    ..Our findings suggest that retinal ganglion cells may be amenable to the neuroprotective effects of sigma ligands under conditions of neurotoxicity such as occurs in diabetes...
  2. ncbi Cloning and functional expression of the human type 1 sigma receptor (hSigmaR1)
    R Kekuda
    Department of Biochemistry and Molecular Biology, Medical College of Georgia, Augusta 30912 2100, USA
    Biochem Biophys Res Commun 229:553-8. 1996
    ..The hSigmaR1 cDNA predicts a protein of 223 amino acids with a single putative transmembrane domain...
  3. ncbi Colocalization of sterol isomerase and sigma(1) receptor at endoplasmic reticulum and nuclear envelope level
    D Dussossoy
    Sanofi Recherche, Montpellier, France Sanofi Recherche, Labege, France
    Eur J Biochem 263:377-86. 1999
    ..Taken together our results suggest that both SR31747A-binding proteins not only play a role in sterol metabolism but indirectly affect lipoprotein functions...
  4. ncbi Role of sigma-1 receptor C-terminal segment in inositol 1,4,5-trisphosphate receptor activation: constitutive enhancement of calcium signaling in MCF-7 tumor cells
    Zhiping Wu
    Department of Molecular Pharmacology, Physiology and Biotechnology, Division of Biology and Medicine, Brown University, Providence, Rhode Island 02912, USA
    J Biol Chem 283:28198-215. 2008
    ..These results suggest that sigma-1R overexpression drives sigma agonist-independent dissociation of ANK 220 from IP3R-3, resulting in activation. The C-terminal segment plays a key role in the interaction...
  5. ncbi Irreversible blockade of sigma-1 receptors by haloperidol and its metabolites in guinea pig brain and SH-SY5Y human neuroblastoma cells
    Enrique J Cobos
    Department of Pharmacology and Institute of Neuroscience, Faculty of Medicine, University of Granada, Granada, Spain
    J Neurochem 102:812-25. 2007
    ..These results suggest that HP may irreversibly inactivate sigma(1) receptors in guinea pig and human cells, probably after metabolism to reduced HP...
  6. ncbi Expression pattern of the type 1 sigma receptor in the brain and identity of critical anionic amino acid residues in the ligand-binding domain of the receptor
    P Seth
    Department of Biochemistry and Molecular Biology, Medical College of Georgia, Augusta 30912, USA
    Biochim Biophys Acta 1540:59-67. 2001
    The type 1 sigma receptor (sigmaR1) has been shown to participate in a variety of functions in the central nervous system...
  7. ncbi The expression and functional characterization of sigma (sigma) 1 receptors in breast cancer cell lines
    Ebru Aydar
    Division of Cell and Molecular Biology, Imperial College London, Sir Alexander Fleming Building, South Kensington Campus, London SW7 2AZ, UK
    Cancer Lett 242:245-57. 2006
    ..This data suggests sigma1 receptor plays a role in proliferation and adhesion of breast cancer cells. Therefore, it is likely to be a potential target for the diagnosis and therapy of breast cancer...
  8. ncbi Regulating ankyrin dynamics: Roles of sigma-1 receptors
    T Hayashi
    Cellular Pathobiology Unit, Cellular Neurobiology Research Branch, Intramural Research Program, National Institute on Drug Abuse National Institutes of Health, 5500 Nathan Shock Drive, Baltimore, MD 21224, USA
    Proc Natl Acad Sci U S A 98:491-6. 2001
    ....
  9. ncbi Prevention of excitotoxicity in primary retinal ganglion cells by (+)-pentazocine, a sigma receptor-1 specific ligand
    Ying Dun
    Department of Cellular Biology and Anatomy, Medical College of Georgia, Augusta, Georgia 30912 2000, USA
    Invest Ophthalmol Vis Sci 48:4785-94. 2007
    ..1 mM) of the excitatory amino acids glutamate (Glu) and homocysteine (Hcy) and demonstrated that the sigmaR1 ligand (+)-pentazocine ((+)-PTZ) could protect against cell death...
  10. ncbi In vivo protection against retinal neurodegeneration by sigma receptor 1 ligand (+)-pentazocine
    Sylvia B Smith
    Departments of Cellular Biology and Anatomy, Medical College of Georgia, Augusta, Georgia, USA
    Invest Ophthalmol Vis Sci 49:4154-61. 2008
    To evaluate the neuroprotective properties of the sigma receptor 1 (sigmaR1) ligand, (+)-pentazocine in an in vivo model of retinal neurodegeneration.
  11. ncbi Expression, subcellular localization, and regulation of sigma receptor in retinal muller cells
    Guoliang Jiang
    Department of Cellular Biology and Anatomy, Medical College of Georgia, Augusta, GA 30912 2000, USA
    Invest Ophthalmol Vis Sci 47:5576-82. 2006
    ..Type 1 sigmaR1 (sigmaR1) is expressed in brain oligodendrocytes, but its expression and binding capacity have not been analyzed ..
  12. ncbi Expression of sigma receptor 1 mRNA and protein in rat retina
    L L Liu
    Institute of Neurobiology, Institute of Brain Science and State Key Laboratory of Medical Neurobiology, Fudan University, 138 Yixueyuan Road, Shanghai 200032, PR China
    Neuroscience 167:1151-9. 2010
    ..Two types of sigmaRs have been identified: sigmaR1 and sigmaR2...
  13. ncbi Rapid reduction of sigma1-receptor binding and 18F-FDG uptake in rat gliomas after in vivo treatment with doxorubicin
    Aren van Waarde
    Department of Nuclear Medicine and Molecular Imaging, University Medical Center Groningen, University of Groningen, Groningen, The Netherlands
    J Nucl Med 48:1320-6. 2007
    ....
  14. ncbi In vivo functional interaction between phencyclidine binding sites and sigma receptors to produce head-weaving behavior in rats
    K Kitaichi
    Department of Neuropsychopharmacology and Hospital Pharmacy, Nagoya University School of Medicine, Showa Ku, Japan
    Eur J Pharmacol 318:205-11. 1996
    ..o.). These results suggest that PCP binding sites and sigma receptors are involved in PCP-induced head weaving behavior, and that sigma1 receptors play an important role in modulation of the head-weaving behavior...
  15. ncbi [Anti-amnesic effects of sigma (sigma)-receptor agonists]
    K Matsuno
    Discovery Research Division, Santen Pharmaceutical Co, Ltd, Osaka, Japan
    Nihon Yakurigaku Zasshi 114:25-33. 1999
    ..However, the sigma-receptor family is still considered to be enigmatic molecular targets. More molecular cloning and biochemical studies on the sigma-receptor family are needed...
  16. ncbi Cloning of an emopamil-binding protein (EBP)-like protein that lacks sterol delta8-delta7 isomerase activity
    Fabian F Moebius
    Institut fur Biochemische Pharmakologie, Peter Mayr Strasse 1, A 6020 Innsbruck, Austria
    Biochem J 374:229-37. 2003
    ..We propose that EBPL has a yet-to-be-discovered function other than cholesterol biosynthesis...
  17. ncbi [Sigma-receptor ligands and anti-stress actions]
    Y Noda
    Department of Neuropsychopharmacology, Nagoya University Graduate School of Medicine, Japan
    Nihon Yakurigaku Zasshi 114:43-9. 1999
    ....
  18. ncbi Sigma receptor agonists provide neuroprotection in vitro by preserving bcl-2
    Sufang Yang
    Department of Anesthesiology and Peri Operative Medicine, Oregon Health Sciences University, Portland, Oregon 97239 3098, USA
    Anesth Analg 104:1179-84, tables of contents. 2007
    ..We tested the hypothesis that the potent, prototypical sigma(1)-receptor agonist, 4-phenyl-1-(4-phenylbutyl) piperidine (PPBP), protects neurons by a mechanism involving the antiapoptotic protein bcl-2...
  19. ncbi Molecular cloning and pharmacological characterization of the rat sigma1 receptor
    J Mei
    The Cotzias Laboratory of Neuro Oncology, Memorial Sloan Kettering Cancer Center, Program in Neurosciences, Cornell University Graduate School of Medical Sciences, 1275 York Avenue, New York, NY 10021, USA
    Biochem Pharmacol 62:349-55. 2001
    ..Thus, rs2-2.HA encodes a high-affinity [3H](+)-pentazocine binding site with characteristics of a rat sigma1 receptor...
  20. ncbi Induction of micronuclei in mouse bone-marrow erythrocytes in association with hypothermia after administration of the sigma receptor ligand E-5842
    Antonio Guzman
    Department of Toxicology, ESTEVE, Mare de Deu de Montserrat 221, 08041 Barcelona, Spain
    Mutat Res 565:11-22. 2004
    ..The results suggest that the slight increase in MNPCE frequency observed 48 h after administration of a 200 mg/kg dose of E-5842 is due to a hypothermic effect and not to a direct effect of E-5842 on DNA...
  21. ncbi The attenuation of learning impairments induced after exposure to CO or trimethyltin in mice by sigma (sigma) receptor ligands involves both sigma1 and sigma2 sites
    T Maurice
    INSERM U 336, Developpement, Plasticite et Vieillissement du Systeme Nerveux, ENSCM, Montpellier, France
    Br J Pharmacol 127:335-42. 1999
    ..The particular pattern of neurodegeneration observed in these lesional models may explain these differences...
  22. ncbi Sigma receptors and cancer: possible involvement of ion channels
    Ebru Aydar
    Department of Biological Sciences, Sir Alexander Fleming Building, Imperial College, South Kensington Campus, London SW7 2AZ, United Kingdom
    Cancer Res 64:5029-35. 2004
    ....
  23. ncbi Yeast sterol C8-C7 isomerase: identification and characterization of a high-affinity binding site for enzyme inhibitors
    F F Moebius
    Institut fur Biochemische Pharmakologie, Universitat Innsbruck, Austria
    Biochemistry 35:16871-8. 1996
    ..Our results demonstrate that the yeast sterol C8-C7 isomerase has a polyvalent high-affinity drug binding site similar to mammalian sigma receptors and that in yeast sigma ligands inhibit sterol biosynthesis...
  24. ncbi Design, synthesis, and structure-affinity relationships of regioisomeric N-benzyl alkyl ether piperazine derivatives as sigma-1 receptor ligands
    Iman A Moussa
    School of Chemistry, Discipline of Medical Radiation Sciences, University of Sydney, Sydney, NSW, Australia
    J Med Chem 53:6228-39. 2010
    ..The in vivo evaluation of [11C]13 indicates that this radiotracer is a suitable candidate for imaging the sigma1 receptor in neurodegenerative processes...
  25. ncbi The sigma1 receptor interacts with N-alkyl amines and endogenous sphingolipids
    Subramaniam Ramachandran
    Department of Pharmacology, University Wisconsin Madison, School of Medicine and Public Health, 1300 University Ave, Madison, WI 53706, USA
    Eur J Pharmacol 609:19-26. 2009
    ..The data presented here strongly supports sphingosine as an endogenous modulator of the sigma1 receptor...
  26. ncbi Evaluation of spirocyclic 3-(3-fluoropropyl)-2-benzofurans as sigma1 receptor ligands for neuroimaging with positron emission tomography
    Eva Grosse Maestrup
    Institut fur Pharmazeutische und Medizinische Chemie der Westfalischen Wilhelms Universitat Munster, Munster, Germany
    J Med Chem 52:6062-72. 2009
    ..Target specificity of [(18)F]7a was validated in blocking studies by preapplication of haloperidol, and significant reduction in the uptake of radioactivity was observed in the brain and peripheral organs expressing sigma(1) receptors...
  27. ncbi 5D-QSAR for spirocyclic sigma1 receptor ligands by Quasar receptor surface modeling
    Christoph Oberdorf
    Institut für Pharmazeutische und Medizinische Chemie der Universität Münster, Hittorfstrasse 58 62, D 48149 Munster, Germany
    Eur J Med Chem 45:3116-24. 2010
    ..8). Thus, in addition to novel insights into the requirements for binding of spirocyclic piperidines to the sigma(1) receptor, the presented model can be used successfully in the rational design of new sigma(1) ligands...
  28. ncbi Involvement of the sigma1 receptor in inhibiting activity of fluvoxamine on marble-burying behavior: comparison with paroxetine
    Nobuaki Egashira
    Department of Neuropharmacology, Faculty of Pharmaceutical Sciences, Fukuoka University, Fukuoka and Department of Pharmacy, Kyushu University Hospital, Fukuoka 812 8582, Japan
    Eur J Pharmacol 563:149-54. 2007
    ....
  29. ncbi High occupancy of sigma-1 receptors in the human brain after single oral administration of fluvoxamine: a positron emission tomography study using [11C]SA4503
    Masatomo Ishikawa
    Division of Clinical Neuroscience, Chiba University Center for Forensic Mental Health, Chiba, Japan
    Biol Psychiatry 62:878-83. 2007
    ..The present study was undertaken to examine whether fluvoxamine binds to sigma-1 receptors in living human brain...
  30. ncbi Sigma1 receptor modulation of opioid analgesia in the mouse
    Jianfeng Mei
    The Laboratory of Molecular Neuropharmacology, Memorial Sloan Kettering Cancer Center, Program in Neurosciences, Cornell University Graduate School of Medical Sciences, New York, New York 10021, USA
    J Pharmacol Exp Ther 300:1070-4. 2002
    ..This enhanced response following antisense treatment was similar to that seen with haloperidol. These observations confirm the importance of sigma1 receptors as a modulatory system influencing the analgesic activity of opioid drugs...
  31. ncbi Involvement of the sigma 1 receptor in the modulation of dopaminergic transmission by amantadine
    Magali Peeters
    Laboratoire de Pharmacologie Expérimentale FARL, Universite Catholique de Louvain, 54 10, Avenue Hippocrate 54, B 1200 Brussels, Belgium
    Eur J Neurosci 19:2212-20. 2004
    ..Together, these data demonstrate that aminoadamantanes behave as sigma1 receptor agonists, and confirm an involvement of this receptor in modulating dopamine receptors exerted by therapeutically relevant concentrations of amantadine...
  32. ncbi Local anesthetic procaine protects rat pheochromocytoma PC12 cells against beta-amyloid-induced neurotoxicity
    Laurent Lecanu
    Department of Biochemistry and Molecular Biology, Georgetown University Medical Center, Washington, DC 20057, USA
    Pharmacology 74:65-78. 2005
    ..In conclusion, these data suggest that procaine exerts neuroprotective properties and may serve either as a treatment for AD or as a starting point for the development of novel therapies for AD...
  33. ncbi Inhibition of hyperpolarization-activated cation currents by phencyclidine and some sigma ligands in rat hippocampal CA1 pyramidal neurons in vitro
    Mitsuo Tanabe
    Laboratory of CNS Pharmacology, Graduate School of Pharmaceutical Sciences, Nagoya City University, 3 1 Tanabe dori, Mizuho ku, Nagoya 467 8603, Japan
    Neuropharmacology 53:406-14. 2007
    ..The results of this study suggest that PCP and some sigma ligands could modulate cell excitability partly through their action on Ih...
  34. ncbi Cloning and characterization of a mouse sigma1 receptor
    Y X Pan
    Cotzias Laboratory of Neuro Oncology, Memorial Sloan Kettering Cancer Center, New York, New York 10021, USA
    J Neurochem 70:2279-85. 1998
    ..HA encodes a high-affinity (+)-[3H]pentazocine binding site with characteristics of a murine sigma1 receptor. An antisense oligodeoxynucleotide designed from S2-1a potentiated opioid analgesia in vivo...
  35. ncbi Dextromethorphan attenuates trimethyltin-induced neurotoxicity via sigma1 receptor activation in rats
    Eun Joo Shin
    Neuropsychopharmacology and Toxicology Program, College of Pharmacy, Kangwon National University, Chunchon 200 701, South Korea
    Neurochem Int 50:791-9. 2007
    ..These results suggest that DM prevents TMT-induced neurotoxicity, at least in part, via sigma(1) receptor stimulation...
  36. ncbi Antiproliferative and cytotoxic effects of some sigma2 agonists and sigma1 antagonists in tumour cell lines
    Nicola Antonio Colabufo
    Dipartimento Farmaco Chimico, via Orabona, 4, 70126 Bari, Italy
    Naunyn Schmiedebergs Arch Pharmacol 370:106-13. 2004
    ....
  37. ncbi Pharmacological and metabolic characterisation of the potent sigma1 receptor ligand 1'-benzyl-3-methoxy-3H-spiro[[2]benzofuran-1,4'-piperidine]
    Christian Wiese
    Institut für Pharmazeutische und Medizinische Chemie der Universität Münster, Munster, Germany
    J Pharm Pharmacol 61:631-40. 2009
    ..The pharmacology and metabolism of the potent sigma1 receptor ligand 1'-benzyl-3-methoxy-3H-spiro[[2]benzofuran-1,4'-piperidine] were evaluated...
  38. ncbi Intracellular sigma1 receptor modulates phospholipase C and protein kinase C activities in the brainstem
    M P Morin-Surun
    Institut Alfred Fessard, Avenue de la Terrasse, 91198 Gif sur Yvette, France
    Proc Natl Acad Sci U S A 96:8196-9. 1999
    ..This might be an example of a mechanism by which an intracellular receptor modulates metabotropic responses...
  39. ncbi 4-IBP, a sigma1 receptor agonist, decreases the migration of human cancer cells, including glioblastoma cells, in vitro and sensitizes them in vitro and in vivo to cytotoxic insults of proapoptotic and proautophagic drugs
    Véronique Megalizzi
    Laboratoire de Toxicologie, Institut de Pharmacie, Universite Libre de Bruxelles, Brussels, Belgium
    Neoplasia 9:358-69. 2007
    ..In vivo, 4-IBP increased the antitumor effects of temozolomide and irinotecan in immunodeficient mice that were orthotopically grafted with invasive cancer cells...
  40. ncbi An unambiguous assay for the cloned human sigma1 receptor reveals high affinity interactions with dopamine D4 receptor selective compounds and a distinct structure-affinity relationship for butyrophenones
    Ivan T Lee
    Department of Pharmacology and Neuroscience, University of North Texas Health Science Center, Fort Worth, TX 79107, USA
    Eur J Pharmacol 578:123-36. 2008
    ..The antidepressant fluvoxamine, the drug of abuse methamphetamine, and the neurosteroid progesterone were amongst the many ligands whose interactions with the sigma(1) receptor were confirmed with our screening assay...
  41. ncbi Sigma1-receptor stimulation with fluvoxamine ameliorates transverse aortic constriction-induced myocardial hypertrophy and dysfunction in mice
    Hideaki Tagashira
    Department of Pharmacology, Graduate School of Pharmaceutical Sciences, Tohoku University, Sendai, Japan
    Am J Physiol Heart Circ Physiol 299:H1535-45. 2010
    ..This is the first report of a potential role for ?(1)R stimulation by fluvoxamine in attenuating cardiac hypertrophy and restoring contractility in TAC mice...
  42. ncbi Involvement of the sigma1 (sigma1) receptor in the anti-amnesic, but not antidepressant-like, effects of the aminotetrahydrofuran derivative ANAVEX1-41
    J Espallergues
    CNRS, FRE2693, Montpellier, France
    Br J Pharmacol 152:267-79. 2007
    ..we have here analysed the sigma (1) component in the behavioural effects of anavex1-41...
  43. ncbi Genetic polymorphisms in sigma-1 receptor and apolipoprotein E interact to influence the severity of Alzheimer's disease
    Yue Huang
    Department of Neurology and Institute of Neurology, Ruijin Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai 200025, China
    Curr Alzheimer Res 8:765-70. 2011
    Apolipoprotein E (APOE) ?4 allele and sigma-1 receptor (SIGMAR1) c.5C (Q2P) polymorphisms have been acknowledged as risk factors for developing Alzheimer's disease (AD)...
  44. ncbi The SIGMAR1 gene is associated with a risk of schizophrenia and activation of the prefrontal cortex
    Kazutaka Ohi
    Department of Psychiatry, Osaka University Graduate School of Medicine, Osaka, Japan
    Prog Neuropsychopharmacol Biol Psychiatry 35:1309-15. 2011
    Several studies have identified the possible involvement of sigma non-opioid intracellular receptor 1 (SIGMAR1) in the pathogenesis of schizophrenia...
  45. ncbi Sigma1 receptor antagonist BD1047 enhances reversal of conditioned place preference from cocaine to social interaction
    Michael Fritz
    Experimental Psychiatry Unit, Medical University Innsbruck, Innsbruck, Austria
    Pharmacology 87:45-8. 2011
    ..Our findings indicate that sigma1 blockade may be used therapeutically to enhance treatment adherence in social interaction-based rehabilitation programs...
  46. ncbi Synthesis and evaluation of fluorine-18-labeled SA4503 as a selective sigma1 receptor ligand for positron emission tomography
    Kazunori Kawamura
    Positron Medical Center, Tokyo Metropolitan Institute of Gerontology, Itabashi ku, Tokyo 173 0022, Japan
    Nucl Med Biol 34:571-7. 2007
    ..18)F]FM-SA4503 showed specific binding to sigma(1) receptors in mice and monkeys; therefore, [(18)F]FM-SA4503 has the potential for mapping sigma(1) receptors in the brain...
  47. ncbi AVP-923, a combination of dextromethorphan hydrobromide and quinidine sulfate for the treatment of pseudobulbar affect and neuropathic pain
    Nicholas Olney
    University of California, San Francisco, Department of Neurology, Memory and Aging Center, Suite 706, San Francisco, CA 94143, USA
    IDrugs 13:254-65. 2010
    ..Pending approval of the data from the FDA, AVP-923 would be the first FDA-approved treatment for PBA...
  48. ncbi Association analysis of SIGMAR1 with major depressive disorder and SSRI response
    Taro Kishi
    Department of Psychiatry, Fujita Health University School of Medicine, Toyoake, Aichi 470 1192, Japan
    Neuropharmacology 58:1168-73. 2010
    ..To evaluate the association of sigma 1 receptor gene (SIGMAR1) and MDD and SSRIs therapeutic response in MDD, we conducted a case-control study of Japanese samples (466 MDD ..
  49. ncbi An update on the development of drugs for neuropsychiatric disorders: focusing on the sigma 1 receptor ligand
    Teruo Hayashi
    IRP, NIDA NIH, Cellular Pathobiology Unit, Development and Plasticity Section, Cellular Neurobiology Research Branch, Room 3418, Triad building, 333 Cassell Drive, Baltimore, MD 21224, USA
    Expert Opin Ther Targets 12:45-58. 2008
    ..Ligands for the sigma1 receptor may constitute a new class of therapeutic drugs targeting an endoplasmic reticular protein...
  50. ncbi Synthesis of spirocyclic sigma1 receptor ligands as potential PET radiotracers, structure-affinity relationships and in vitro metabolic stability
    Eva Grosse Maestrup
    Institut für Pharmazeutische und Medizinische Chemie der Universität Münster, Hittorfstrasse 58 62, D 48149 Munster, Germany
    Bioorg Med Chem 17:3630-41. 2009
    ..For the synthesis of the potential PET tracers [(18)F]2a and [(18)F]2e two different radiosynthetic approaches were followed...
  51. ncbi Association between sigma-1 receptor gene polymorphism and prefrontal hemodynamic response induced by cognitive activation in schizophrenia
    Ryu Takizawa
    Department of Neuropsychiatry, Graduate School of Medicine, The University of Tokyo, Japan
    Prog Neuropsychopharmacol Biol Psychiatry 33:491-8. 2009
    ..Our findings also suggest that the prefrontal hemodynamic response assessed by noninvasive and less demanding NIRS is a useful intermediate phenotype for translational research in schizophrenia...
  52. ncbi Voltage-gated sodium channel modulation by sigma-receptors in cardiac myocytes and heterologous systems
    Molly Johannessen
    Dept of Physiology, University of Wisconsin School of Medicine and Public Health, Madison, WI 53706, USA
    Am J Physiol Cell Physiol 296:C1049-57. 2009
    ..The modulation of Na(v)1.5 channels by sigma-receptors in the heart suggests an important pathway by which drugs can alter cardiac excitability and rhythmicity...
  53. ncbi Sigma1 receptor antagonists determine the behavioral pattern of the methamphetamine-induced stereotypy in mice
    J Kitanaka
    Department of Pharmacology, Hyogo College of Medicine, 1 1 Mukogawa cho, Nishinomiya, Hyogo, 663 8501, Japan
    Psychopharmacology (Berl) 203:781-92. 2009
    ..The effects of sigma receptor antagonists on methamphetamine (METH)-induced stereotypy have not been examined. We examined the effects of sigma antagonists on METH-induced stereotypy in mice...
  54. ncbi Dual DAT/sigma1 receptor ligands based on 3-(4-(3-(bis(4-fluorophenyl)amino)propyl)piperazin-1-yl)-1-phenylpropan-1-ol
    Jianjing Cao
    Medicinal Chemistry Section, National Institute on Drug Abuse Intramural Research Program, National Institutes of Health, 333 Cassell Drive, Baltimore, MD 21224, USA
    Bioorg Med Chem Lett 18:5238-41. 2008
    ....
  55. ncbi Alterations in fos-related antigen 2 and sigma1 receptor gene and protein expression are associated with the development of cocaine-induced behavioral sensitization: time course and regional distribution studies
    Yun Liu
    Department of Pharmaceutical Sciences, University of Oklahoma Health Sciences Center, Oklahoma City, Oklahoma, USA
    J Pharmacol Exp Ther 327:187-95. 2008
    ..These data suggest that repeated exposure to cocaine elicits alterations in fra-2 and sigma(1) receptor-mediated mechanisms, which ultimately manifest as altered behavioral responses to cocaine...
  56. ncbi Synthesis, biological evaluation, and three-dimensional in silico pharmacophore model for sigma(1) receptor ligands based on a series of substituted benzo[d]oxazol-2(3H)-one derivatives
    Daniele Zampieri
    Department of Pharmaceutical Sciences, Piazzale Europa 1, University of Trieste, 34127 Trieste, Italy
    J Med Chem 52:5380-93. 2009
    ....
  57. ncbi On the mechanism of antidepressant-like action of berberine chloride
    Shrinivas K Kulkarni
    Pharmacology Division, University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh, India
    Eur J Pharmacol 589:163-72. 2008
    ..Further, nitric oxide pathway and/or sigma receptors are involved in mediating its antidepressant-like activity in mouse forced swim test...
  58. ncbi Selective sigma-1 (sigma1) receptor antagonists: emerging target for the treatment of neuropathic pain
    Jose Luis Diaz
    Department of Chemistry, ESTEVE, Av Mare de Déu de Montserrat 221, 08041 Barcelona, Spain
    Cent Nerv Syst Agents Med Chem 9:172-83. 2009
    ..Functional data in pain models are presented mainly on one series that provide evidence to consider selective sigma(1) receptor antagonists an innovative and alternative approach for treating neuropathic pain...
  59. ncbi Anti-inflammatory effects of dimemorfan on inflammatory cells and LPS-induced endotoxin shock in mice
    Y H Wang
    Department of Pharmacy, Taipei Veterans General Hospital, Taipei, Taiwan
    Br J Pharmacol 154:1327-38. 2008
    ..Dimemorfan (a sigma1 receptor agonist) showed neuroprotective properties in animal models of inflammation-mediated neurodegenerative conditions, but its effects on inflammatory cells and systemic inflammation remain unclear...
  60. ncbi Detergent-resistant microdomains determine the localization of sigma-1 receptors to the endoplasmic reticulum-mitochondria junction
    Teruo Hayashi
    Cellular Pathobiology Section, Cellular Neurobiology Research Branch, Intramural Research Program, National Institute on Drug Abuse, National Institutes of Health, Department of Health and Human Services, Baltimore, MD 21224, USA
    Mol Pharmacol 77:517-28. 2010
    ..These findings suggest that the MAM, bearing cholesterol and ceramide-enriched microdomains at the ER, may use the microdomains to anchor Sig-1Rs to the location; thus, it serves to stage Sig-1R at ER-mitochondria junctions...
  61. ncbi Involvement of sigma (sigma1) receptors in modulating the anti-depressant effect of neurosteroids (dehydroepiandrosterone or pregnenolone) in mouse tail-suspension test
    A Dhir
    Pharmacology Division, University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh, India
    J Psychopharmacol 22:691-6. 2008
    ..The treatments and their combination did not alter the motor activity in mice. These data suggested a role for the central sigma receptors particularly sigma-1 (sigma1) receptors in the anti-depressant-like effects of neurosteroids...
  62. ncbi Synthesis of bicyclic sigma receptor ligands with cytotoxic activity
    Christian Geiger
    Institut fur Pharmazeutische und Medizinische Chemie, University Munster, Hittorfstrasse 58 62, Munster, Germany
    J Med Chem 50:6144-53. 2007
    ..The IC50-values of methyl ethers ent-17 and ent-22 are in the range of the antitumor drugs cisplatin and oxaliplatin. Binding assays show that the investigated tumor cell lines express considerable amounts of sigma1 and sigma2 receptors...
  63. ncbi SA4503, a novel cognitive enhancer with sigma1 receptor agonist properties, facilitates NMDA receptor-dependent learning in mice
    T Maurice
    Unité 336 de l Institut National de la Santé et de la Recherche Médicale, Developpement, Plasticite et Vieillissement du Systeme Nerveux, E N S C M, Montpellier, France
    Eur J Pharmacol 328:9-18. 1997
    ..Pertinent informations on the potential mechanism of the anti-amnesic effects of sigma1 receptor ligands were also obtained...
  64. ncbi Dimemorfan enhances acetylcholine release from rat hippocampal slices
    Hui Hung Wang
    Department and Institute of Pharmacology, National Yang Ming University, No 155, Sec 2, Li Nong Street, Taipei, Taiwan
    Brain Res 1008:113-5. 2004
    ..3 microM)...
  65. ncbi Enhanced antidepressant efficacy of sigma1 receptor agonists in rats after chronic intracerebroventricular infusion of beta-amyloid-(1-40) protein
    Alexandre Urani
    INSERM U 336, Behavioural Neuropharmacology Group, Institut de Biologie, 4, bvd Henri IV, 34060 Montpellier, France
    Eur J Pharmacol 486:151-61. 2004
    ..The present study suggests that sigma(1) receptor agonists, due to their enhanced efficacy in a nontransgenic animal model, may alleviate Alzheimer's disease-associated depressive symptoms...
  66. ncbi Improving the comparative map of porcine chromosome 10 with respect to human chromosomes 1, 9 and 10
    J Aldenhoven
    Centre for Advanced Technologies in Animal Genetics and Reproduction, Faculty of Veterinary Science, University of Sydney, Sydney, NSW, Australia
    Cytogenet Genome Res 102:121-7. 2003
    ..were physically mapped: fifteen to SSC10 (ACO1, ATP5C1, BMI1, CYB5R1, DCTN3, DNAJA1, EPHX1, GALT, GDI2, HSPC177, OPRS1, NUDT2, PHYH, RGS2, VIM), eleven to SSC1 (ADFP, ALDHIB1, CLTA, CMG1, HARC, PLAA, STOML2, RRP40, TESK1, VCP and ..
  67. ncbi Protein kinase C-dependent potentiation of intracellular calcium influx by sigma1 receptor agonists in rat hippocampal neurons
    F P Monnet
    Hôpital Charcot, and Institut National de la Santé et de la Recherche Médicale INSERM Unité 488, 80 rue du General Leclerc, F 94276 Kremlin Bicêtre cedex, France
    J Pharmacol Exp Ther 307:705-12. 2003
    ..Our results provide further support for a general mechanism for the intracellular sigma1 receptor to regulate Ca2+-dependent signal transduction and protein phosphorylation...
  68. ncbi The anti-amnesic effects of sigma1 (sigma1) receptor agonists confirmed by in vivo antisense strategy in the mouse
    T Maurice
    INSERM U 336, Behavioral Neuropharmacology Group, Institut de Biologie, 4, Boulevard Henri IV, 34060, Montpellier, France
    Brain Res 898:113-21. 2001
    ..The anti-amnesic effects of PRE-084 or SA4503, observed after saline- or mODN-treatment, were blocked after aODN administration. These observations bring a molecular basis to the modulatory role of sigma1 receptors in memory processes...
  69. ncbi Preclinical evaluation of [11C]SA4503: radiation dosimetry, in vivo selectivity and PET imaging of sigma1 receptors in the cat brain
    K Kawamura
    Positron Medical Center, Tokyo Metropolitan Institute of Gerontology, Itabashi, Japan
    Ann Nucl Med 14:285-92. 2000
    ..We have concluded that [11C]SA4503 has the potential for mapping sigma1 receptor by PET...
  70. ncbi Substituted 1-phenyl-2-cyclopropylmethylamines with high affinity and selectivity for sigma sites
    G Ronsisvalle
    Department of Pharmaceutical Sciences, University of Catania, Italy
    Bioorg Med Chem 8:1503-13. 2000
    ..Moreover, modifications of carboxyl groups provided compounds with the highest affinities in the series. In particular, compound 25 with reverse-type ester showed a Ki of 0.6 and 4.05 nM for sigma1 and sigma2 binding sites, respectively...
  71. ncbi A sigma-1 receptor selective analogue of BD1008. A potential substitute for (+)-opioids in sigma receptor binding assays
    D Y Maeda
    Department of Pharmaceutical Sciences, University of Maryland School of Pharmacy, Baltimore, USA
    Bioorg Med Chem Lett 10:17-8. 2000
    ..A simple, achiral monoamine sigma-1 (sigma1) receptor selective ligand (sigma2Ki/sigma1Ki>2000) is described, which could replace the chiral (+)-pentazocine or dextrallorphan as a sigma1 masking agent in sigma2 binding assays...
  72. ncbi [Atypical antipsychotic profiles of sigma receptor ligands]
    S Okuyama
    1st Laboratory, Taisho Pharmaceutical Co, Ltd, Saitama, Japan
    Nippon Yakurigaku Zasshi 114:13-23. 1999
    ..Panamesine and SL 82.0714 showed favorable efficacy in the open studies, but BMY 14802 showed no efficacy in clinical trials...
  73. ncbi Modulation of steroidal levels by adrenalectomy/castration and inhibition of neurosteroid synthesis enzymes affect sigma1 receptor-mediated behaviour in mice
    V L Phan
    INSERM U 336, Developpement, Plasticite et Vieillissement du Systeme Nerveux, ENSCM, 8 rue de lEcole Normale, 34296 Montpellier Cedex 5, France
    Eur J Neurosci 11:2385-96. 1999
    ..These results confirmed that endogenous neurosteroidal levels modulate sigma1 receptor-mediated behaviour directly, and revealed that, among neurosteroids, progesterone may be the main modulator of sigma1 receptors...
  74. ncbi Molecular and ligand-binding characterization of the sigma-receptor in the Jurkat human T lymphocyte cell line
    M E Ganapathy
    Department of Medicine, Medical College of Georgia, Augusta, USA
    J Pharmacol Exp Ther 289:251-60. 1999
    ..This splice variant was found to be nonfunctional in ligand binding assays. This constitutes the first report on the molecular characterization of the sigma-receptor in immune cells...
  75. ncbi Potent sigma1-receptor ligand 4-phenyl-1-(4-phenylbutyl) piperidine modulates basal and N-methyl-D-aspartate-evoked nitric oxide production in vivo
    A Bhardwaj
    Department of Neurology, Johns Hopkins University School of Medicine, and National Institute on Drug Abuse, Baltimore, MD 21287, USA
    Stroke 29:2404-10; discussion 2411. 1998
    ....
  76. ncbi Sigma1 receptor subtype does not interact with stereotyped behaviors in rats
    T Kobayashi
    Central Research Laboratories, Santen Pharmaceutical Co, Ltd, Higashiyodogawa, Osaka, Japan
    Pharmacol Biochem Behav 61:381-4. 1998
    ..We thus suggest that the induction of PCP-like stereotyped behaviors elicited by (+)-SKF-10,047 closely interacts with NMDA/PCP receptor channel complex but not with the sigma1 receptor subtype...
  77. ncbi Sigma receptor ligands (+)-SKF10,047 and SA4503 improve dizocilpine-induced spatial memory deficits in rats
    L B Zou
    Department of Neuropsychopharmacology and Hospital Pharmacy, Nagoya University School of Medicine, Japan
    Eur J Pharmacol 355:1-10. 1998
    ..These results suggest that the interaction of sigma1 receptors with NMDA receptors modulates spatial memory in rats...
  78. ncbi 2(3H)-benzoxazolone and 2(3H)-benzothiazolone derivatives: novel, potent and selective sigma1 receptor ligands
    H Ucar
    Unite de Chimie pharmaceutique et de Radiopharmacie, Ecole de Pharmacie, Universite Catholique de Louvain, Brussels, Belgium
    Eur J Pharmacol 335:267-73. 1997
    ..Compound 1, administered intraperitoneally, was the most effective against maximal electroshock-induced seizures and was devoid of significant neurotoxic effects...
  79. ncbi No association found between the type 1 sigma receptor gene polymorphisms and methamphetamine abuse in the Japanese population: a collaborative study by the Japanese Genetics Initiative for Drug Abuse
    T Inada
    Department of Psychiatry and Psychobiology, Nagoya University Graduate School of Medicine, Nagoya, Japan
    Ann N Y Acad Sci 1025:27-33. 2004
    ..This study suggests that type 1 sigma receptor gene is unlikely to play a major role in substance abuse liability and/or the development of MAP psychosis...
  80. ncbi Involvement of kappa-opioid receptors and sigma receptors in memory function demonstrated using an antisense strategy
    Masayuki Hiramatsu
    Laboratory of Neuropsychopharmacology, Graduate School of Environmental and Human Sciences, Meijo University, Tenpaku ku, Nagoya 468 8503, Japan
    Brain Res 1030:247-55. 2004
    ....
  81. ncbi A feasibility study of [11C]SA4503-PET for evaluating sigmal receptor occupancy by neuroleptics: the binding of haloperidol to sigma1 and dopamine D2-like receptors
    Kiichi Ishiwata
    Positron Medical Center, Tokyo Metropolitan Institute of Gerontology, Japan
    Ann Nucl Med 20:569-73. 2006
    ..dopamine D2-like receptor (D2R) as well as to be a representative non-selective antagonist for sigma1 receptor (sigma1R), was selected as a model drug...
  82. ncbi Trishomocubanes: novel sigma ligands modulate cocaine-induced behavioural effects
    Xiang Liu
    Department of Pharmacology, University of Sydney, NSW 2006, Australia
    Eur J Pharmacol 555:37-42. 2007
    ..The differential effect of TC1 and TC4 warrants further study of the mechanism of these actions. Present data also suggests a potential role for trishomocubane analogues in developing medication or research tools for cocaine addiction...
  83. ncbi Effect of BD 1047, a sigma1 receptor antagonist, in the animal models predictive of antipsychotic activity
    Grazyna Skuza
    Department of Pharmacology, Institute of Pharmacology, Polish Academy of Sciences, Smetna 12, Pl 31 343 Krakow, Poland
    Pharmacol Rep 58:626-35. 2006
    ..Summing up, BD 1047 shows a moderate activity in models used in this study suggesting that its usefulness as an antipsychtic drug is doubtful. However, more detailed studies are required for definitive confirmation of this conclusion...
  84. ncbi Dopamine-1 receptor agonist, but not cocaine, modulates sigma(1) gene expression in SVG cells
    Oren Ben-Ami
    Faculty of Life Sciences, Bar Ilan University, Ramat Gan, Israel
    J Mol Neurosci 29:169-76. 2006
    ..This (+)-SKF38393-induced effect was blocked by the D(1)R selective antagonist (+)-SCH23390. These results suggest that the effect of cocaine on sigma(1) gene expression in the brain might be indirect and mediated through D(1)R...
  85. ncbi The synergistic effect of selective sigma receptor agonists and uncompetitive NMDA receptor antagonists in the forced swim test in rats
    G Skuza
    Department of Pharmacology, Institute of Pharmacology, Polish Academy of Sciences, Krakow, Poland
    J Physiol Pharmacol 57:217-29. 2006
    ..Combined treatment with sigma ligands and AMA or MEM (applied in the clinic) may be an alternative to the treatment of antidepressant-resistant depressive patients in the future...
  86. ncbi A novel adamantane derivative attenuates retinal ischemia-reperfusion damage in the rat retina through sigma1 receptors
    Claudio Bucolo
    Department of Experimental and Clinical Pharmacology, School of Medicine, University of Catania, Catania, Viale A Doria 6, I 95125 Catania, Italy
    Eur J Pharmacol 536:200-3. 2006
    ..The protective effect of (-)-MR22 on ischemic retina was confirmed by the histological analysis. These findings suggest that (-)-MR22 serves as a retinal neuroprotective agent and acts as a sigma1 receptor agonist...
  87. ncbi Differential effects of sigma1 receptor blockade on self-administration and conditioned reinstatement motivated by cocaine vs natural reward
    Remi Martin-Fardon
    Molecular and Integrative Neurosciences Department, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA
    Neuropsychopharmacology 32:1967-73. 2007
    ..The findings support a role for sigma(1) receptors in regulating conditioned responses to cocaine-related contextual stimuli and identify this receptor as a potential treatment target for the prevention of craving and relapse...
  88. ncbi Sigma receptor ligands protect human retinal cells against oxidative stress
    Claudio Bucolo
    Department of Experimental and Clinical Pharmacology, School of Medicine, University of Catania, Catania, Italy
    Neuroreport 17:287-91. 2006
    ..The results suggest that sigma1 receptors play an important role against retinal damage, even though sigma2 receptor involvement cannot be excluded...
  89. ncbi Effects of progesterone and norethisterone on cephalexin transport and peptide transporter PEPT1 expression in human intestinal cell line Caco-2
    Kazuhiro Watanabe
    Hokkaido Pharmaceutical University, School of Pharmacy, Hokkaido, Japan
    Biol Pharm Bull 29:90-5. 2006
    ..Further studies are needed to clarify whether the inhibition of the PEPT1 gene transcription by progesterone pretreatment proceeds via sigma1-receptor or progesterone receptor...
  90. ncbi Formalin-induced pain is reduced in sigma(1) receptor knockout mice
    Cruz Miguel Cendan
    Department of Pharmacology and Institute of Neurosciences, School of Medicine, University of Granada, Avenida de Madrid 12, 18012 Granada, Spain
    Eur J Pharmacol 511:73-4. 2005
    ..These results suggest that the tonic pain induced by formalin is altered in mice lacking sigma1 receptors, and highlight the potential usefulness of further studies of the role of sigma1 receptors in models of non-acute pain...
  91. ncbi Age-related expression of sigma1 receptors and antidepressant efficacy of a selective agonist in the senescence-accelerated (SAM) mouse
    Vân Ly Phan
    INSERM U 336, Behavioral Neuropharmacology Group, Montpellier, France
    J Neurosci Res 79:561-72. 2005
    ..Preserved sigma1 receptor expression and enhanced behavioral efficacy of sigma1 agonists were measured in SAM animals, confirming the therapeutic opportunities for selective ligands against age-related mood disorders...
  92. ncbi Pharmacophore identification for sigma-1 (sigma1) receptor binding: application of the "deconstruction-reconstruction-elaboration" approach
    R A Glennon
    Department of Medicinal Chemistry, School of Pharmacy, Medical College of Virginia Campus, Virginia Commonwealth University, Richmond, Virginia 23298 0540, USA
    Mini Rev Med Chem 5:927-40. 2005
    ..A structural feature common to high-affinity (Ki <10 nM) sigma1 ligands is: C-N(R)-X-Ph; both C and Ph are associated with regions of bulk tolerance. Numerous other ligands bind, but typically do so with lower affinity...
  93. ncbi Exon-intron structure, analysis of promoter region, and chromosomal localization of the human type 1 sigma receptor gene
    P D Prasad
    Department of Biochemistry and Molecular Biology, Medical College of Georgia, Augusta 30912 2100, USA
    J Neurochem 70:443-51. 1998
    ....
  94. ncbi Immunohistochemical localization of the sigma1 receptor in Schwann cells of rat sciatic nerve
    Gabriel Palacios
    Histopathology Unit, Research Center, Laboratorios del Dr Esteve, S A, Av Mare de Déu de Montserrat 221, 08041 Barcelona, Spain
    Brain Res 1007:65-70. 2004
    ....
  95. ncbi High occupancy of sigma1 receptors in the human brain after single oral administration of donepezil: a positron emission tomography study using [11C]SA4503
    Masatomo Ishikawa
    Division of Clinical Neuroscience, Chiba University Center for Forensic Mental Health, Chiba, Japan
    Int J Neuropsychopharmacol 12:1127-31. 2009
    ..This study demonstrated that donepezil binds to sigma1 receptors in the living human brain at therapeutic doses. Therefore, sigma1 receptors may be implicated in the pharmacological mechanism of donepezil in the human brain...
  96. ncbi Antidepressant-like effect of PRE-084, a selective sigma1 receptor agonist, in Albino Swiss and C57BL/6J mice
    Grazyna Skuza
    Department of Pharmacology, Institute of Pharmacology, Polish Academy of Sciences, Smetna 12, Pl 31 343 Krakow, Poland
    Pharmacol Rep 61:1179-83. 2009
    ..These results support the idea that sigma(1)-receptors, but not sigma(2)-receptors, contribute to the mechanism of antidepressant activity of sigma agonists in FST...
  97. ncbi Neuro(active)steroids actions at the neuromodulatory sigma1 (sigma1) receptor: biochemical and physiological evidences, consequences in neuroprotection
    Tangui Maurice
    INSERM U 710, Montpellier, F 34095 France University of Montpellier II, Montpellier, F 34095 France c EPHE, Paris, F 75007 France
    Pharmacol Biochem Behav 84:581-97. 2006
    ..Biochemical and physiological arguments for an interaction of neuro(active)steroids with the sigma(1) receptor are analyzed and the impact on physiopathological outcomes in neuroprotection is illustrated...
  98. ncbi Functional polymorphisms in the sigma1 receptor gene associated with alcoholism
    Ryosuke Miyatake
    Institute of Clinical Research, National Alcoholism Center Kurihama Hospital, Kanagawa, Japan
    Biol Psychiatry 55:85-90. 2004
    ..Two polymorphisms (GC-241-240TT and Gln2Pro) in the sigma1 receptor gene (SIGMAR1) have been identified...
  99. ncbi Sigma receptor type 1 gene variation in a group of Polish patients with Alzheimer's disease and mild cognitive impairment
    Aleksandra Maruszak
    Department of Neurodegenerative Disorders, Medical Research Centre, Polish Academy of Sciences, Warsaw, Poland
    Dement Geriatr Cogn Disord 23:432-8. 2007
    The sigma-1 receptor (SIGMAR1) is a subtype of a nonopioid sigma receptor family and is implicated in numerous functions connected with Alzheimer's disease (AD)...
  100. ncbi No association between the sigma receptor type 1 gene and schizophrenia: results of analysis and meta-analysis of case-control studies
    Naohiko Uchida
    Department of Neuropsychiatry, Okayama University Graduate School of Medicine and Dentistry, Shikata cho 2 5 1, Okayama, 700 8558, Japan
    BMC Psychiatry 3:13. 2003
    ..An association study provided genetic evidence that the sigma receptor type 1 gene (SIGMAR1) was a possible susceptibility factor for schizophrenia, however, it was not replicated by a subsequent study...
  101. ncbi A variant of the sigma receptor type-1 gene is a protective factor for Alzheimer disease
    Naohiko Uchida
    Department of Neuropsychiatry, Okayama University Graduate School of Medicine, Dentistry, and Pharmaceutical Sciences, Shikata cho 2 5 1, Okayama 700 8558, Japan
    Am J Geriatr Psychiatry 13:1062-6. 2005
    ..The authors provide here genetic evidence that the sigma receptor type 1 (SIGMAR1) gene is involved in susceptibility to AD.

Research Grants52

  1. Sigma Receptor Structure /Function /K+ Channel Modulation
    ARNOLD RUOHO; Fiscal Year: 2007
    ..4 potassium channels and other protein partners. These experiments will be performed through the combined use of photoactivatable molecules, electrophysiology, and recombinant and fusion proteins. ..
  2. SIGMA LIGANDS FOR THE TREATMENT OF COCAINE OVERDOSE
    Rae Matsumoto; Fiscal Year: 2007
    ..It is anticipated that the results of this project will facilitate the development of new and effective treatments for cocaine abuse. ..
  3. SYNTHESIS AND PHARMACOLOGY OF NOVEL OPIATE LIGANDS
    Gavril Pasternak; Fiscal Year: 2002
    ..Finally, we will continue our efforts to synthesize radiolabeled affinity labels. ..
  4. Synthesis and pharmacology of novel opiates and their modulatory systems
    Gavril W Pasternak; Fiscal Year: 2010
    ....
  5. MOLECULAR BASIS OF REOVIRUS PATHOGENESIS
    Terence Dermody; Fiscal Year: 2007
    ..These studies will yield a precise understanding of reovirus cell-attachment and provide novel insights into mechanisms by which reoviruses and other neurotropic viruses select cellular targets and produce disease. ..
  6. OPIATE RECEPTOR PHARMACOLOGY
    Gavril Pasternak; Fiscal Year: 2007
    ..By examining both the receptors themselves and modulatory systems, we hope to extend our understanding of opioid analgesics and gain insights into how to use them appropriately and minimize their abuse. ..
  7. Synthesis & Pharmacology of Novel Opiates and Systems
    Gavril Pasternak; Fiscal Year: 2007
    ..By understanding how opioids and their modulatory systems interact, we hope to develop better approaches towards the management of pain and the discovery of new agents. ..
  8. Structural Analysis of Reovirus Attachment Mechanisms
    Thilo Stehle; Fiscal Year: 2004
    ....
  9. Structural Analysis of Reovirus Attachment Mechanisms
    Terence Dermody; Fiscal Year: 2006
    ....
  10. RETINAL PIGMENT EPITHELIUM: VECTORIAL TRANSPORT FUNCTION
    Sylvia Smith; Fiscal Year: 2003
    ..The results obtained from these studies will be the first data available on the mechanisms involved in vectorial transport of folate across RPE. ..
  11. Analysis of neural retina transport function
    Sylvia Smith; Fiscal Year: 2009
    ..We will determine whether the Hcy-induced retinopathy in cbs mutant mice is due solely to lack of adequate folate or is due to a complexity of cellular insults including oxidative stress, excitotoxic damage, ER stress, and DNA damage. ..
  12. Analysis of neural retina transport function
    Sylvia B Smith; Fiscal Year: 2010
    ..We will determine whether the Hcy-induced retinopathy in cbs mutant mice is due solely to lack of adequate folate or is due to a complexity of cellular insults including oxidative stress, excitotoxic damage, ER stress, and DNA damage. ..
  13. Diabetic retinopathy: sigma receptor 1 (??R1) as a novel therapeutic target.
    Sylvia B Smith; Fiscal Year: 2010
    ..The proposed project will extend these findings to understand the mechanism of this protection with the ultimate goal of determining whether (+)- pentazocine may be useful clinically for retinopathy in humans. ..
  14. Analysis of neural retina transport function
    Sylvia Smith; Fiscal Year: 2007
    ..We will determine whether the Hcy-induced retinopathy in cbs mutant mice is due solely to lack of adequate folate or is due to a complexity of cellular insults including oxidative stress, excitotoxic damage, ER stress, and DNA damage. ..
  15. Diabetic retinopathy: aR1 as a novel therapeutic target
    Sylvia Smith; Fiscal Year: 2007
    ..Type 1 sigma receptor (sigmaR1) is a nonopiate, nonphencyclidine binding site that demonstrates robust neuroprotective properties including ..
  16. SP004, a sigma-1 ligand with AchE inhibition properties
    Laurent Lecanu; Fiscal Year: 2004
    ..Our goal in this Phase I STTR application is to prove the concept that a dual activity compound, such as SP004, is efficacious in an in vivo settings simulating human neuropathology. ..