New positron emission tomography (PET) radioligand for imaging σ-1 receptors in living subjects.

No abstract is available for this paper.

• Publication year

  2012

• Venue

  Journal of Medicinal Chemistry

• Publication date

  2012-10-11

• Fields of study

  Medicine, Chemistry

• Identifiers
  DOI 10.1021/jm300371cPMID 22853801PMCID PMC4106900
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• Pharmacological properties of S1RA, a new sigma‐1 receptor antagonist that inhibits neuropathic pain and activity‐induced spinal sensitization

  2012cited by this paper
• Is cocaine a social drug? Exploration of the stereo-structure of cocaine’s pharmacophore

  2012cited by this paper
• Synthesis and Pharmacological Evaluation of 6-Acetyl-3-(4-(4-(4-fluorophenyl)piperazin-1-yl)butyl)benzo[d]oxazol-2(3H)-one (SN79), a Cocaine Antagonist, in Rodents

  2011cited by this paper
• Molecular imaging of σ receptors: synthesis and evaluation of the potent σ1 selective radioligand [18F]fluspidine

  2011cited by this paper
• Sigma receptors and cocaine abuse.

  2011cited by this paper
• Synthesis and characterization of [³H]-SN56, a novel radioligand for the σ₁ receptor.

  2011cited by this paper
• New methodologies for in vitro analysis of binding and functional activity of sigma receptor ligands

  2011cited by this paper
• A Novel Substituted Piperazine, CM156, Attenuates the Stimulant and Toxic Effects of Cocaine in Mice

  2010cited by this paper
• Novel highly potent and selective sigma 1 receptor antagonists related to spipethiane.

  2010cited by this paper
• The sigma-1 receptor is enriched in postsynaptic sites of C-terminals in mouse motoneurons. An anatomical and behavioral study.

  2010cited by this paper
• Design, synthesis, and structure-affinity relationships of regioisomeric N-benzyl alkyl ether piperazine derivatives as sigma-1 receptor ligands.

  2010cited by this paper
• Synthesis and biological activities of Schiff bases of gabapentin with different aldehydes and ketones: a structure–activity relationship study

  2010cited by this paper
• Cholesterol at the endoplasmic reticulum: roles of the sigma-1 receptor chaperone and implications thereof in human diseases.

  2010cited by this paper
• Evaluation of spirocyclic 3-(3-fluoropropyl)-2-benzofurans as sigma1 receptor ligands for neuroimaging with positron emission tomography.

  2009cited by this paper
• Imaging of sigma1 receptors in the human brain using PET and [11C]SA4503.

  2009cited by this paper
• The pharmacology of sigma-1 receptors.

  2009cited by this paper
• The role of sigma-1 receptors in the pathophysiology of neuropsychiatric diseases

  2009cited by this paper
• Selective sigma-1 (sigma1) receptor antagonists: emerging target for the treatment of neuropathic pain.

  2009cited by this paper
• Attenuation of methamphetamine-induced effects through the antagonism of sigma (sigma) receptors: Evidence from in vivo and in vitro studies.

  2008cited by this paper
• Low density of sigma1 receptors in early Alzheimer’s disease

  2008cited by this paper
• Synthesis and evaluation of fluorine-18-labeled SA4503 as a selective sigma1 receptor ligand for positron emission tomography.

  2007cited by this paper
• igh Occupancy of Sigma-1 Receptors in the Human rain after Single Oral Administration of Fluvoxamine : Positron Emission Tomography Study Using 11 C ] SA 4503

  2007cited by this paper
• High occupancy of sigma-1 receptors in the human brain after single oral administration of fluvoxamine: a positron emission tomography study using [11C]SA4503.

  2007cited by this paper
• Imaging sigma receptors: applications in drug development.

  2007cited by this paper
• Synthesis and binding affinities of methylvesamicol analogs for the acetylcholine transporter and sigma receptor.

  2006cited by this paper
• Preclinical Acute Toxicity Studies and Dosimetry Estimates of the Novel Sigma-1 Receptor Radiotracer, [18F]SFE

  2006cited by this paper
• In vivo evaluation in rats of [(18)F]1-(2-fluoroethyl)-4-[(4-cyanophenoxy)methyl]piperidine as a potential radiotracer for PET assessment of CNS sigma-1 receptors.

  2006cited by this paper
• Novel 2(3H)-Benzothiazolones as Highly Potent and Selective Sigma-1 Receptor Ligands

  2005cited by this paper
• Methyl substitution on the piperidine ring of N-[omega-(6-methoxynaphthalen-1-yl)alkyl] derivatives as a probe for selective binding and activity at the sigma(1) receptor.

  2005cited by this paper
• Sigma receptors: biology and therapeutic potential

  2004cited by this paper
• Determination of acid dissociation constants by capillary electrophoresis.

  2004cited by this paper
• Expression of sigma 1 receptor in human breast cancer

  2004cited by this paper
• Clinical trials with sigma ligands.

  2004cited by this paper
• Expression of sigma 1 receptor in human breast cancer

  2004cited by this paper
• AMIDE: a free software tool for multimodality medical image analysis.

  2003cited by this paper
• Improving Alzheimer's Disease-Related Cognitive Deficits with sigma1 Receptor Agonists.

  2002cited by this paper
• NMR (Nuclear Magnetic Resonance)

  2002cited by this paper
• A multireceptorial binding reinvestigation on an extended class of σ ligands: N-[ω-(indan-1-yl and tetralin-1-yl)alkyl] derivatives of 3,3-dimethylpiperidine reveal high affinities towards σ1 and EBP sites

  2001cited by this paper
• A multireceptorial binding reinvestigation on an extended class of sigma ligands: N-[omega-(indan-1-yl and tetralin-1-yl)alkyl] derivatives of 3,3-dimethylpiperidine reveal high affinities towards sigma1 and EBP sites.

  2001cited by this paper
• Correlation between neuroleptic binding to σ1 and σ2 receptors and acute dystonic reactions

  2000cited by this paper
• sigma(1)-receptor ligand 4-phenyl-1-(4-phenylbutyl)-piperidine affords neuroprotection from focal ischemia with prolonged reperfusion.

  2000cited by this paper
• In vivo evaluation of [11C]SA4503 as a PET ligand for mapping CNS sigma1 receptors

  2000cited by this paper
• In vivo evaluation of [(11)C]SA4503 as a PET ligand for mapping CNS sigma(1) receptors.

  2000cited by this paper
• Correlation between neuroleptic binding to sigma(1) and sigma(2) receptors and acute dystonic reactions.

  2000cited by this paper
• Ameliorative effect of SA4503, a novel cognitive enhancer, on the basal forebrain lesion-induced impairment of the spatial learning performance in rats.

  1998cited by this paper
• 1'-Benzyl-3,4-dihydrospiro[2H-1- benzothiopyran-2,4'-piperidine] (spipethiane), a potent and highly selective sigma1 ligand.

  1998cited by this paper
• In vivo evaluation of [18F]1-(3-fluoropropyl)-4-(4-cyanophenoxymethyl)piperidine: a selective sigma-1 receptor radioligand for PET.

  1997cited by this paper
• 2(3H)-benzoxazolone and 2(3H)-benzothiazolone derivatives: novel, potent and selective sigma1 receptor ligands.

  1997cited by this paper
• Release of [3 H]dopamine from guinea pig striatal slices is modulated by sigma1 receptor agonists

  1997cited by this paper
• Methods for determiningn-octanol-water partition constants

  1996cited by this paper
• Binding properties of SA4503, a novel and selective σ1 receptor agonist

  1996cited by this paper
• Enhancement of acetylcholine release by SA4503, a novel sigma 1 receptor agonist, in the rat brain.

  1996cited by this paper
• Binding properties of SA4503, a novel and selective sigma 1 receptor agonist.

  1996cited by this paper
• Sigma-1 and sigma-2 receptors are expressed in a wide variety of human and rodent tumor cell lines.

  1995cited by this paper
• Rat liver and kidney contain high densities of sigma 1 and sigma 2 receptors: characterization by ligand binding and photoaffinity labeling.

  1994cited by this paper
• Sigma‐1 and Sigma‐2 sites in rat brain: Comparison of regional, ontogenetic, and subcellular patterns

  1994cited by this paper
• RLH-033, a novel, potent and selective ligand for the sigma 1 recognition site.

  1994cited by this paper
• Rat liver and kidney contain high densities of σ1 and σ2 receptors: characterization by ligand binding and photoaffinity labeling

  1994cited by this paper
• RLH-033, a novel, potent and selective ligand for the σ1 recognition site

  1994cited by this paper
• Delineating biochemical and functional properties of sigma receptors: emerging concepts.

  1993cited by this paper
• Sigma receptor-active neuroleptics are cytotoxic to C6 glioma cells in culture.

  1993cited by this paper
• Delineating biochemical and functional properties of sigma receptors: emerging concepts.

  1993cited by this paper
• A proposal for the classification of sigma binding sites.

  1992cited by this paper
• Sigma receptors: biology and function.

  1990cited by this paper
• A steric theory of opioid agonists, antagonists, agonist-antagonists, and partial agonists.

  1984cited by this paper
• A steric theory of opioid agonists, antagonists, agonist-antagonists, and partial agonists.

  1984cited by this paper
• The effects of morphine- and nalorphine- like drugs in the nondependent and morphine-dependent chronic spinal dog.

  1976cited by this paper

• The Sigma1 receptor antagonist CM304 potentiates the antinociceptive effects of the cannabinoid receptor agonist delta9-tetrahydrocannabinol in rats and mice.

  2026cites this paper
• Neuromelanin-targeted 18F-P3BZA PET/MR imaging of the substantia nigra in rhesus macaques

  2025cites this paper
• A Full-Spectrum Evaluation of Sigma-1 Receptor (S1R) Positron Emission Tomography (PET) Radioligands from Binding Affinity to Clinical Imaging

  2025influential citation
• Structural Features of Tetrabutylammonium Salts of bis-2-Mercaptothiazoles: Ionic Complex and One-Dimensional Hydrogen-Bonded Organic Framework

  2025cites this paper
• Development of Carbon‐11 Labeled Pyrimidine Derivatives as Novel Positron Emission Tomography (PET) Agents Enabling Brain Sigma‐1 Receptor Imaging

  2025cites this paper
• Sigma-1 receptor as an emerging target for painful diabetic neuropathy—a review

  2025cites this paper
• Structurally isomeric ditopic 2-mercaptobenzoxazole and 2-hydroxybenzothiazole as ligands for design of 2D sodium-based luminescent coordination polymers.

  2025cites this paper
• Recent Advances in the Development of Sigma Receptor (Radio)Ligands and Their Application in Tumors.

  2025cites this paper
• Recent developments and challenges in positron emission tomography imaging of gliosis in chronic neuropathic pain.

  2024cites this paper
• A facile synthesis of precursor for the σ-1 receptor PET radioligand [18 F]FTC-146 and its radiofluorination.

  2024cites this paper
• RETRACTED ARTICLE: Neuromelanin-targeted 18 F-P3BZA PET/MR imaging of the substantia nigra in rhesus macaques

  2024cites this paper
• Imaging brain glucose metabolism in vivo reveals propionate as a major anaplerotic substrate in pyruvate dehydrogenase deficiency.

  2024cites this paper
• Imaging of Pain using Positron Emission Tomography.

  2024cites this paper
• Current status of PET tracers for the early diagnosis of Alzheimer's disease

  2024cites this paper
• Advances with the discovery and development of novel sigma 1 receptor antagonists for the management of pain

  2023cites this paper
• Improved protocol for the radiosynthesis of [18 F]FTC-146: A potent and selective sigma-1 receptor radioligand.

  2023cites this paper
• Up-and-coming Radiotracers for Imaging Pain Generators

  2023cites this paper
• Sigma Receptor Ligands Prevent COVID Mortality In Vivo: Implications for Future Therapeutics

  2023cites this paper
• Development and Initial Assessment of [^18F]OP-801: a Novel Hydroxyl Dendrimer PET Tracer for Preclinical Imaging of Innate Immune Activation in the Whole Body and Brain

  2023cites this paper
• Recent advances in drug discovery efforts targeting the sigma 1 receptor system: Implications for novel medications designed to reduce excessive drug and food seeking

  2023cites this paper
• Discovery of RC-752, a Novel Sigma-1 Receptor Antagonist with Antinociceptive Activity: A Promising Tool for Fighting Neuropathic Pain

  2023cites this paper
• Candidate 3-benzazepine-1-ol type GluN2B receptor radioligands (11C-NR2B-Me enantiomers) have high binding in cerebellum but not to σ1 receptors

  2023cites this paper
• PET Molecular Imaging in Drug Development: The Imaging and Chemistry Perspective

  2022cites this paper
• Examination of the Novel Sigma-1 Receptor Antagonist, SI 1/28, for Antinociceptive and Anti-allodynic Efficacy against Multiple Types of Nociception with Fewer Liabilities of Use

  2022cites this paper
• Sigma-1 receptor: A potential target for the development of antidepressants.

  2022cites this paper
• Evaluation of (rac)-, (R)-, and (S)-18F-OF-NB1 for Imaging GluN2B Subunit–Containing N-Methyl-d-Aspartate Receptors in Nonhuman Primates

  2022influential citation
• Development of a PET radioligand for α2δ-1 subunit of calcium channels for imaging neuropathic pain

  2022cites this paper
• Comparison of three novel radiotracers for GluN2B-containing NMDA receptors in non-human primates: (R)-[11C]NR2B-Me, (R)-[18F]of-Me-NB1, and (S)-[18F]of-NB1

  2022cites this paper
• Effects of the sigma-1 receptor agonist blarcamesine in a murine model of fragile X syndrome: neurobehavioral phenotypes and receptor occupancy

  2021cites this paper
• Characterization in Non-human Primates of (R)-[18F]OF-Me-NB1 and (S)-[18F]OF-Me-NB1 for Imaging the GluN2B Subunits of the NMDA Receptor

  2021influential citation
• Characterization in nonhuman primates of (R)-[18F]OF-Me-NB1 and (S)-[18F]OF-Me-NB1 for imaging the GluN2B subunits of the NMDA receptor

  2021cites this paper
• NRM 2021 Abstract Booklet

  2021cites this paper
• Highly Specific Sigma Receptor Ligands Exhibit Anti-Viral Properties in SARS-CoV-2 Infected Cells

  2021cites this paper
• A Clinical PET Imaging Tracer ([18F]DASA-23) to Monitor Pyruvate Kinase M2–Induced Glycolytic Reprogramming in Glioblastoma

  2021cites this paper
• Multi-Target Directed Ligands (MTDLs) Binding the σ1 Receptor as Promising Therapeutics: State of the Art and Perspectives

  2021cites this paper
• Involvement of Chaperone Sigma1R in the Anxiolytic Effect of Fabomotizole

  2021cites this paper
• In Vivo Receptor Visualization and Evaluation of Receptor Occupancy with Positron Emission Tomography.

  2021cites this paper
• Physiological blood–brain transport is impaired with age by a shift in transcytosis

  2020cites this paper
• Evaluation of 11C-NR2B-SMe and Its Enantiomers as PET Radioligands for Imaging the NR2B Subunit Within the NMDA Receptor Complex in Rats

  2020cites this paper
• Demarcation of Sepsis-Induced Peripheral and Central Acidosis with pH (Low) Insertion Cycle Peptide

  2020cites this paper
• Approaches to PET Imaging of Glioblastoma

  2020cites this paper
• Distinct Regulation of σ1 Receptor Multimerization by Its Agonists and Antagonists in Transfected Cells and Rat Liver Membranes

  2020influential citation
• Positron Emission Tomography Imaging Evaluation of a Novel 18F-Labeled Sigma-1 Receptor Radioligand in Cynomolgus Monkeys.

  2020cites this paper
• Evaluation of 18F-IAM6067 as a sigma-1 receptor PET tracer for neurodegeneration in vivo in rodents and in human tissue

  2020cites this paper
• Exploring 1-adamantanamine as an alternative amine moiety for metabolically labile azepane ring in newly synthesized benzo[d]thiazol-2(3H)one σ receptor ligands

  2020cites this paper
• Discovery of a Highly Selective Sigma-2 Receptor Ligand, 1-(4-(6,7-Dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)butyl)-3-methyl-1H-benzo[d]imidazol-2(3H)-one (CM398), with Drug-Like Properties and Antinociceptive Effects In Vivo

  2020cites this paper
• Identifying Musculoskeletal Pain Generators Using Clinical PET

  2020cites this paper
• Chaperone Sigma1R and Antidepressant Effect

  2020cites this paper
• Knocking Out Sigma-1 Receptors Reveals Diverse Health Problems

  2020cites this paper
• In vitro and in vivo sigma 1 receptor imaging studies in different disease states.

  2020cites this paper
• Characterization of Sigma 1 Receptor Antagonist CM-304 and Its Analog, AZ-66: Novel Therapeutics Against Allodynia and Induced Pain

  2019cites this paper
• Distinct regulation of sigma‐1 receptor multimerization by its agonists and antagonists

  2019influential citation
• Synthesis, in vitro and in vivo characterization of new benzoxazole and benzothiazole-based sigma receptor ligands.

  2019cites this paper
• Novel radioligands for imaging sigma-1 receptor in brain using positron emission tomography (PET)

  2019cites this paper
• Acetylated Benzothiazolone as Homobivalent SPECT Metallo-Radiopharmaceutical 99mTc-(6-AcBTZ)2DTPA: Design, Synthesis, and Preclinical Evaluation for Mapping 5-HT1A/7 Receptors

  2019cites this paper
• Imaging Sigma-1 Receptor (S1R) Expression Using Iodine-124-Labeled 1-(4-Iodophenyl)-3-(2-adamantyl)guanidine ([124I]IPAG)

  2019cites this paper
• TSPO–PET imaging using [18F]PBR06 is a potential translatable biomarker for treatment response in Huntington’s disease: preclinical evidence with the p75NTR ligand LM11A-31

  2018cites this paper
• Assessment of sigma-1 receptor occupancy in mice with non-radiolabelled FTC-146 as a tracer

  2018cites this paper
• Synthesis, radiolabelling, and evaluation of [11C]PB212 as a radioligand for imaging sigma-1 receptors using PET.

  2018cites this paper
• Quantification of highly selective sigma-1 receptor antagonist CM304 using liquid chromatography tandem mass spectrometry and its application to a pre-clinical pharmacokinetic study.

  2017cites this paper
• A Role for Sigma Receptors in Stimulant Self-Administration and Addiction.

  2017cites this paper
• [18F]GE-180 PET Detects Reduced Microglia Activation After LM11A-31 Therapy in a Mouse Model of Alzheimer's Disease

  2017cites this paper
• Medicinal Chemistry of σ1 Receptor Ligands: Pharmacophore Models, Synthesis, Structure Affinity Relationships, and Pharmacological Applications.

  2017cites this paper
• PET Imaging Evaluation of Four σ1 Radiotracers in Nonhuman Primates

  2017cites this paper
• Fluorinated PET Tracers for Molecular Imaging of σ1 Receptors in the Central Nervous System.

  2017cites this paper
• Biodistribution and Radiation Dosimetry of 18F-FTC-146 in Humans

  2017cites this paper
• Imaging B Cells in a Mouse Model of Multiple Sclerosis Using 64Cu-Rituximab PET

  2017cites this paper
• 1-(4-[18F]Fluorobenzyl)-4-[(tetrahydrofuran-2-yl)methyl]piperazine: A Novel Suitable Radioligand with Low Lipophilicity for Imaging σ1 Receptors in the Brain.

  2017cites this paper
• Radiosynthesis and First-In-Human PET/MRI Evaluation with Clinical-Grade [18F]FTC-146

  2017cites this paper
• Production of diverse PET probes with limited resources: 24 18F-labeled compounds prepared with a single radiosynthesizer

  2017influential citation
• The sigma-1 receptor modulates dopamine transporter conformation and cocaine binding and may thereby potentiate cocaine self-administration in rats

  2017cites this paper
• Human umbilical cord plasma proteins revitalize hippocampal function in aged mice

  2017cites this paper
• Visualizing Nerve Injury in a Neuropathic Pain Model with [18F]FTC-146 PET/MRI

  2017cites this paper
• Blockade of Cocaine or Sigma Receptor Agonist Self-Administration by Subtype- Selective Sigma Receptor Antagonists

  2016cites this paper
• Synthesis and evaluation of a (18) F-labeled 4-phenylpiperidine-4-carbonitrile radioligand for σ1 receptor imaging.

  2016cites this paper
• Blockade of Cocaine or σ Receptor Agonist Self Administration by Subtype-Selective σ Receptor Antagonists

  2016cites this paper
• Synthesis and Biological Evaluation of Novel σ1 Receptor Ligands for Treating Neuropathic Pain: 6-Hydroxypyridazinones.

  2016cites this paper
• Potential applications for sigma receptor ligands in cancer diagnosis and therapy.

  2015cites this paper
• Design and Synthesis of Sigma-1 Probe for Positron Emission Tomography (PET) Imaging

  2015cites this paper
• Neuropathic Pain Mechanisms and Imaging

  2015cites this paper
• PET imaging of tumor glycolysis downstream of hexokinase through noninvasive measurement of pyruvate kinase M2

  2015cites this paper
• PET Imaging of Translocator Protein (18 kDa) in a Mouse Model of Alzheimer's Disease Using N-(2,5-Dimethoxybenzyl)-2-18F-Fluoro-N-(2-Phenoxyphenyl)Acetamide

  2015cites this paper
• Further validation to support clinical translation of ( 18 F)FTC-146 for imaging

  2015cites this paper
• DESIGN AND SYNTHESIS OF SIGMA-1 PROBE FOR POSITRON EMISSION TOMOGRAPHY (PET) IMAGING

  2015cites this paper
• Selective sigma-1 receptor antagonists for the treatment of pain.

  2014cites this paper
• Synthesis and evaluation of a 18F-labeled spirocyclic piperidine derivative as promising σ1 receptor imaging agent.

  2014cites this paper
• Cognitive Enhancers (Nootropics). Part 1: Drugs interacting with Receptors. Update 2014

  2014cites this paper
• Evaluation of σ-1 Receptor Radioligand 18F-FTC-146 in Rats and Squirrel Monkeys Using PET

  2014influential citation
• Novel Treatment Strategies for Cocaine and Opioid Abuse

  2014cites this paper
• Importance of ADME and Bioanalysis in the Drug Discovery

  2013cites this paper
• The development of radiotracers for imaging sigma (σ) receptors in the central nervous system (CNS) using positron emission tomography (PET).

  2013cites this paper
• Molecular imaging: an innovative force in musculoskeletal radiology.

  2013cites this paper
• Structure activity relationship study of benzo[d]thiazol-2(3H)one based σ receptor ligands.

  2013cites this paper
• Molecular imaging of σ1 receptors in vivo: current status and perspectives.

  2013cites this paper
• A Role for Sigma Receptors in Stimulant Self Administration and Addiction

  2011cites this paper