Cited by 184Pharmacological Receptor Mechanisms and EffectsDementia and Cognitive Impairment ResearchAlzheimer's disease research and treatments

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Low density of sigma1 receptors in early Alzheimer’s disease

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Mishina, Masahiro, Ohyama, Masashi, Ishii, Kenji, Kitamura, Shin, Kimura, Yuichi, Oda, Kei-ichi, Kawamura, Kazunori, Sasaki, Toru, Kobayashi, Shiro, Katayama, Yasuo, Ishiwata, Kiichi·2008·Annals of Nuclear Medicine

DOI 10.1007/s12149-007-0094-z

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Abstract

Objective The sigma(1) receptor is considered to be involved in cognitive function. A postmortem study reported that the sigma(1) receptors were reduced in the hippocampus in Alzheimer's disease (AD). However, in vivo imaging of sigma(1) receptors in the brain of AD patients has not been reported. The aim of this study is to investigate the mapping of sigma(1) receptors in AD using [(11)C]SA4503 positron emission tomography (PET).Methods We studied five AD patients and seven elderly volunteers. A dynamic series of decay-corrected PET data acquisition was performed for 90 min starting at the time of the injection of 500 MBq of [(11)C]SA4503. A two-tissue three-compartment model was used to estimate K (1), k (2), k (3), k (4), and the delay between metabolite-corrected plasma and tissue time activity using a Gauss-Newton algorithm. The ratio of k (3) to k (4) was computed as the binding potential (BP), which is linearly related to the density of sigma(1) receptors. Unpaired t tests were used to compare K (1) and BP in patients with AD and normal subjects.Results As compared with normals, BP in the AD was significantly lower in the frontal, temporal, and occipital lobe, cerebellum and thalamus, whereas K (1) was significantly lower in the parietal lobe.Conclusions [(11)C]SA4503 PET can demonstrate that the density of cerebral and cerebellar sigma(1) receptors is reduced in early AD.

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Tripathi, P., Guo, H., Yamoah, A., Doukas, P., Alam, M. M., Dreser, A., Jesse, C. M., Aronica, E., Hermann, A., Steinbusch, H. W. M., et al. (2026) · Research Square · doi:10.21203/rs.3.rs-8428187/v1
Design, synthesis, and characterization of F-18 sigma-1 receptor radiotracers for Alzheimer disease
Jiang, H., Jadhav, S. B., Soda, A. K., Zhou, W., Chen, H., Xu, S., Qiu, L., Huang, T., Xing, Z., Zhao, L., et al. (2026) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2026.118647
VAPB confers selective neuroprotection by driving autophagic degradation of pathogenic aggregates in ALS
Tripathi, P., Guo, H., Yamoah, A., Mathur, R., Doukas, P., Dreser, A., Jesse, C. M., Aronica, E., Hermann, A., Steinbusch, H. W. M., et al. (2026) · Acta Neuropathologica Communications · doi:10.1186/s40478-026-02298-8
“Moreover, these proteins are abnormally modified in neurodegenerative conditions such as AD [20, 39, 67, 109], PD [67], HD [66], and ALS [21, 29, 43], diseases that feature distinct ultrastructural ER alterations and defective protein degradation pathways [16, 49, 103].”
Sigma-1 Receptor Ligand Blarcamesine (ANAVEX 2-73) for Alzheimer’s Disease: A Systematic Review
Brimson, S., Thitilertdecha, P., Kumaree, K., & Brimson, J. (2026) · CNS Drugs · doi:10.1007/s40263-026-01327-3
From Structurally Diverse Sigma-1 (σ1) Receptor Reference Ligands to Live-Cell Probes: Fluorescent Phenoxyalkylpiperidines for the Detection of σ1 Receptor
Musillo, G. R., Abatematteo, F. S., Stiller, B., Majellaro, M., Gioé-Gallo, C., Ortigueira, S., Niso, M., Liturri, A., Perrone, M. G., Vavers, E., et al. (2026) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.6c02423
TDP-43 and ALS - what's wrong with my membranes?
Dahlhaus, R., Yalcin, I., Tischer, J., & Braun, R. J. (2026) · Neurobiology of Disease · doi:10.1016/j.nbd.2026.107630
BindingDB Entry 50033343: Synthesis and biological evaluation of novel 4-benzylpiperazine ligands for sigma-1 receptor imaging.
BindingDB (2011) · UC San Diego · doi:10.7270/q2qj7hn1
BindingDB Entry 50042323: Synthesis and biological evaluation of¹8F labeled fluoro-oligo-ethoxylated 4-benzylpiperazine derivatives for sigma-1 receptor imaging.
BindingDB (2013) · UC San Diego · doi:10.7270/q2vm4dkp
BindingDB Entry 50040665: New positron emission tomography (PET) radioligand for imagings-1 receptors in living subjects.
BindingDB (2013) · UC San Diego · doi:10.7270/q2v40wb0
BindingDB Entry 50032751: Synthesis, pharmacological activity and structure affinity relationships of spirocyclics(1) receptor ligands with a (2-fluoroethyl) residue in 3-position.
BindingDB (2011) · UC San Diego · doi:10.7270/q23f4pwg
BindingDB Entry 50039479: Arylamides hybrids of two high-affinitys2 receptor ligands as tools for the development of PET radiotracers.
BindingDB (2013) · UC San Diego · doi:10.7270/q2b56kq5
BindingDB Entry 50042877: Synthesis and evaluation of novel (18)F-labeled spirocyclic piperidine derivatives ass1 receptor ligands for positron emission tomography imaging.
BindingDB (2013) · UC San Diego · doi:10.7270/q28w3fn3
BindingDB Entry 50034412: Synthesis, radiofluorination and pharmacological evaluation of a fluoromethyl spirocyclic PET tracer for centrals1 receptors and comparison with fluoroalkyl homologs.
BindingDB (2012) · UC San Diego · doi:10.7270/q2ng4r2v
BindingDB Entry 50042819: Investigation ofs receptors agonist/antagonist activity through N-(6-methoxytetralin-1-yl)- and N-(6-methoxynaphthalen-1-yl)alkyl derivatives of polymethylpiperidines.
BindingDB (2013) · UC San Diego · doi:10.7270/q2s75hp7
BindingDB Entry 50033818: Fluorescent derivatives ofs receptor ligand 1-cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]piperazine (PB28) as a tool for uptake and cellular localization studies in pancreatic tumor cells.
BindingDB (2012) · UC San Diego · doi:10.7270/q2kk9c5z
BindingDB Entry 50030624: Evaluation of spirocyclic 3-(3-fluoropropyl)-2-benzofurans as sigma1 receptor ligands for neuroimaging with positron emission tomography.
BindingDB (2010) · UC San Diego · doi:10.7270/q2kh0nd9
BindingDB Entry 50012661: Small Molecules Selectively Targeting Sigma-1 Receptor for the Treatment of Neurological Diseases.
BindingDB (2022) · UC San Diego · doi:10.7270/q2xd15ch
BindingDB Entry 50043283: Structure activity relationship study of benzo[d]thiazol-2(3H)one baseds receptor ligands.
BindingDB (2014) · UC San Diego · doi:10.7270/q2tq62zz
BindingDB Entry 50032929: Analogues ofs receptor ligand 1-cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]piperazine (PB28) with added polar functionality and reduced lipophilicity for potential use as positron emission tomography radiotracers.
BindingDB (2011) · UC San Diego · doi:10.7270/q20v8d3k

Authors: Mishina, M., Ohyama, M., Ishii, K., Kitamura, S., Kimura, Y., Oda, K.-I., Kawamura, K., Sasaki, T., Kobayashi, S., Katayama, Y., & Ishiwata, K.
Affiliations: Tokyo Metropolitan Institute of Gerontology (JP)
Nippon Medical School Musashi Kosugi Hospital (JP)
Chiba Hokusou Hospital (JP)
Nippon Medical School (JP)
Corresponding author: Mishina, Masahiro
ORCID: Mishina, Masahiro
Ishii, Kenji
Kitamura, Shin
Kimura, Yuichi
Kawamura, Kazunori
Sasaki, Toru
Ishiwata, Kiichi
Venue: Annals of Nuclear Medicine
Publisher: Springer Science and Business Media LLC
Published: 2008-04
Volume: 22
Issue: 3
Pages: 151-156
ISSN: 0914-7187 (ISSN-L)
1864-6433
DOI: 10.1007/s12149-007-0094-z
OpenAlex: W2169525045
Cited by: 172
References: 45
Citations by year: 2026: 9 · 2025: 4 · 2024: 7 · 2023: 11 · 2022: 11 · 2021: 10 · 2020: 14 · 2019: 7 · 2018: 4 · 2017: 14 · 2016: 8 · 2015: 10 · 2014: 20 · 2013: 12 · 2012: 7
FWCI: 3.84
Type: journal article
Language: en
Open access: green
repo.qst.go.jp
Licence: cc-by-nc-nd
www.springer.com/tdm (tdm)
Locations: Annals of Nuclear Medicine (publishedVersion)
PubMed (publishedVersion)
Institutional Repositories DataBase (IRDB) (submittedVersion, cc-by-nc-nd)
QST-Repository (National Institutes for Quantum and Radiological Science and Technology) (submittedVersion)
Topics: Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmacology › Pharmacological Receptor Mechanisms and Effects
Health Sciences › Medicine › Psychiatry and Mental health › Dementia and Cognitive Impairment Research
Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Alzheimer's disease research and treatments
Keywords: sigma-1 receptor, Alzheimer's disease, early Alzheimer's disease, receptor binding potential, receptor density
MeSH terms: Aged, Alzheimer Disease, Brain Chemistry, Carbon Radioisotopes, Cerebellum, Cerebral Cortex, Female, Humans, Male, Piperazines, Thalamus, Tissue Distribution, Receptors, sigma, Radiopharmaceuticals, Positron-Emission Tomography

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Low density of sigma1 receptors in early Alzheimer’s disease

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