111 articles for thisTarget
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An insight on synthetic and medicinal aspects of pyrazolo[1,5-a]pyrimidine scaffold.
University of Kwazulu-Natal
Discovery of benzimidazole derivatives as modulators of mitochondrial function: A potential treatment for Alzheimer's disease.
Korea Institute of Science and Technology
Synthesis and in vitro characterization of novel fluorinated derivatives of the translocator protein 18 kDa ligand CfO-DPA-714.
Institute of Biomedical Imaging (I2Bm)
Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH
Jagiellonian University Medical College
Structure-Based Scaffold Repurposing for G Protein-Coupled Receptors: Transformation of Adenosine Derivatives into 5HT
National Institute of Diabetes and Digestive and Kidney Diseases
New structure-activity relationships of N-acetamide substituted pyrazolopyrimidines as pharmacological ligands of TSPO.
Vanderbilt University
Lead Optimization of 2-Phenylindolylglyoxylyldipeptide Murine Double Minute (MDM)2/Translocator Protein (TSPO) Dual Inhibitors for the Treatment of Gliomas.
University of Pisa
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.
Jagiellonian University Medical College
Synthesis and evaluation of aporphine analogs containing C1 allyl isosteres at the h5-HT(2A) receptor.
City University of New York
First Demonstration of Positive Allosteric-like Modulation at the Human Wild Type Translocator Protein (TSPO).
University of New South Wales
Discovery of potent and selective cytotoxic activity of new quinazoline-ureas against TMZ-resistant glioblastoma multiforme (GBM).
Korea University of Science and Technology (Ust)
Synthesis and in vitro characterization of novel fluorinated derivatives of the TSPO 18 kDa ligand SSR180575.
Institute of Biomedical Imaging (I2Bm)
C4 phenyl aporphines with selective h5-HT(2B) receptor affinity.
City University of New York
Deepening the Topology of the Translocator Protein Binding Site by Novel N,N-Dialkyl-2-arylindol-3-ylglyoxylamides.
University of Pisa
Ether analogues of DPA-714 with subnanomolar affinity for the translocator protein (TSPO).
Stanford University School of Medicine
Synthesis, Characterization, and in Vitro Evaluation of a New TSPO-Selective Bifunctional Chelate Ligand.
University of Bari Aldo Moro
Discovery of a neuroprotective chemical, (S)-N-(3-(3,6-dibromo-9H-carbazol-9-yl)-2-fluoropropyl)-6-methoxypyridin-2-amine [(-)-P7C3-S243], with improved druglike properties.
University of Texas Southwestern Medical Center
Structure-activity relationship refinement and further assessment of 4-phenylquinazoline-2-carboxamide translocator protein ligands as antiproliferative agents in human glioblastoma tumors.
University of Salerno
Preparation and evaluation of novel pyrazolo[1,5-a]pyrimidine acetamides, closely related to DPA-714, as potent ligands for imaging the TSPO 18kDa with PET.
Cea
Synthesis and evaluation in monkey of [(18)F]4-fluoro-N-methyl-N-(4-(6-(methylamino)pyrimidin-4-yl)thiazol-2-yl)benzamide ([(18)F]FIMX): a promising radioligand for PET imaging of brain metabotropic glutamate receptor 1 (mGluR1).
National Institute of Mental Health
Identification of a novel benzoxazolone derivative as a selective, orally active 18 kDa translocator protein (TSPO) ligand.
Dainippon Sumitomo Pharma
Discovery of ML314, a Brain Penetrant Non-Peptidicβ-Arrestin Biased Agonist of the Neurotensin NTR1 Receptor.
Sanford-Burnham Medical Research Institute
Synthesis and structure-activity relationships of 5,6,7-substituted pyrazolopyrimidines: discovery of a novel TSPO PET ligand for cancer imaging.
Vanderbilt University Institute of Imaging Science (Vuiis)
Design, synthesis and structure-activity relationship of novel tricyclic benzimidazolone derivatives as potent 18 kDa translocator protein (TSPO) ligands.
Dainippon Sumitomo Pharma
Design, synthesis and structure-activity relationships of novel benzoxazolone derivatives as 18 kDa translocator protein (TSPO) ligands.
Dainippon Sumitomo Pharma
Novel 2-phenylimidazo[1,2-a]pyridine derivatives as potent and selective ligands for peripheral benzodiazepine receptors: synthesis, binding affinity, and in vivo studies.
University of Bari Aldo Moro
Genetic neural networks for quantitative structure-activity relationships: improvements and application of benzodiazepine affinity for benzodiazepine/GABAA receptors.
Harvard University
Synthesis and evaluation of novel carbon-11 labeled oxopurine analogues for positron emission tomography imaging of translocator protein (18 kDa) in peripheral organs.
National Institute of Radiological Sciences
Exploration of the structure-activity relationship of the diaryl anilide class of ligands for translocator protein--potential novel positron emitting tomography imaging agents.
Ge Healthcare
Synthesis and biological evaluation of 4-phenylquinazoline-2-carboxamides designed as a novel class of potent ligands of the translocator protein.
University of Salerno
Tertiary amides with a five-membered heteroaromatic ring as new probes for the translocator protein.
University of Naples Federico II
Synthesis of 6-[¹8F]fluoro-PBR28, a novel radiotracer for imaging the TSPO 18 kDa with PET.
Cea
N-(4-cyanotetrahydro-2H-pyran-4-yl) and N-(1-cyanocyclohexyl) derivatives of 1,5-diarylpyrazole-3-carboxamides showing high affinity for 18 kDa translocator protein and/or cannabinoid receptors.
National Institute of Mental Health
Evaluation of novel N1-methyl-2-phenylindol-3-ylglyoxylamides as a new chemotype of 18 kDa translocator protein-selective ligand suitable for the development of positron emission tomography radioligands.
National Institute of Mental Health
Pyrazolo[1,5-a]pyrimidine acetamides: 4-Phenyl alkyl ether derivatives as potent ligands for the 18 kDa translocator protein (TSPO).
University of Sydney
New iodinated quinoline-2-carboxamides for SPECT imaging of the translocator protein.
University of Glasgow
[18F]FEAC and [18F]FEDAC: Two novel positron emission tomography ligands for peripheral-type benzodiazepine receptor in the brain.
National Institute of Radiological Sciences
The translocator protein (18 kDa): central nervous system disease and drug design.
Brain and Mind Research Institute
Anxiolytic-like effects of N,N-dialkyl-2-phenylindol-3-ylglyoxylamides by modulation of translocator protein promoting neurosteroid biosynthesis.
University of Pisa
2-Phenyl-imidazo[1,2-a]pyridine compounds containing hydrophilic groups as potent and selective ligands for peripheral benzodiazepine receptors: synthesis, binding affinity and electrophysiological studies.
Universita Degli Studi Di Bari
Synthesis, fluorine-18 radiolabeling, and in vitro characterization of 1-iodophenyl-N-methyl-N-fluoroalkyl-3-isoquinoline carboxamide derivatives as potential PET radioligands for imaging peripheral benzodiazepine receptor.
Emory University
Synthesis and structure-activity relationship studies in peripheral benzodiazepine receptor ligands related to alpidem.
University of Siena
Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain.
Abbott Laboratories
N-(5-Fluoro-2-phenoxyphenyl)-N-(2-[(131)I]iodo-5-me thoxybenzyl)acetamide: a potent iodinated radioligand for the peripheral-type benzodiazepine receptor in brain.
National Institute of Radiological Sciences
[2-11C]isopropyl-, [1-11C]ethyl-, and [11C]methyl-labeled phenoxyphenyl acetamide derivatives as positron emission tomography ligands for the peripheral benzodiazepine receptor: radiosynthesis, uptake, and in vivo binding in brain.
National Institute of Radiological Sciences
Development of a new radioligand, N-(5-fluoro-2-phenoxyphenyl)-N-(2-[18F]fluoroethyl-5-methoxybenzyl)acetamide, for pet imaging of peripheral benzodiazepine receptor in primate brain.
National Institute of Radiological Sciences
N,N-dialkyl-2-phenylindol-3-ylglyoxylamides. A new class of potent and selective ligands at the peripheral benzodiazepine receptor.
University of Pisa
Structure-activity relationships in carboxamide derivatives based on the targeted delivery of radionuclides and boron atoms by means of peripheral benzodiazepine receptor ligands.
University of Siena
Mapping and fitting the peripheral benzodiazepine receptor binding site by carboxamide derivatives. Comparison of different approaches to quantitative ligand-receptor interaction modeling.
Magna Graecia University of Catanzaro
Synthesis and binding affinity of 2-phenylimidazo[1,2-alpha]pyridine derivatives for both central and peripheral benzodiazepine receptors. A new series of high-affinity and selective ligands for the peripheral type.
University of Bari Aldo Moro
Mapping the peripheral benzodiazepine receptor binding site by conformationally restrained derivatives of 1-(2-chlorophenyl)-N-methyl-N-(1-methylpropyl)-3- isoquinolinecarboxamide (PK11195).
University of Siena
Synthesis, biological activity, and SARs of pyrrolobenzoxazepine derivatives, a new class of specific"peripheral-type" benzodiazepine receptor ligands.
University of Siena
Cardiovascular characterization of pyrrolo[2,1-d][1,5]benzothiazepine derivatives binding selectively to the peripheral-type benzodiazepine receptor (PBR): from dual PBR affinity and calcium antagonist activity to novel and selective calcium entry blockers.
University of Siena
A concerted study using binding measurements, X-ray structural data, and molecular modeling on the stereochemical features responsible for the affinity of 6-arylpyrrolo[2,1-d][1,5]benzothiazepines toward mitochondrial benzodiazepine receptors.
University of Ferrara
A comparative molecular field analysis model for 6-arylpyrrolo[2,1-d] [1,5]benzothiazepines binding selectively to the mitochondrial benzodiazepine receptor.
University of Naples Federico II
Novel ligands specific for mitochondrial benzodiazepine receptors: 6-arylpyrrolo[2,1-d][1,5]benzothiazepine derivatives. Synthesis, structure-activity relationships, and molecular modeling studies.
University of Siena
(+/-)8-Amino-5,6,7,8-tetrahydroisoquinolines as novel antinociceptive agents.
Virginia Commonwealth University
[¹¿?¿F]GE-180: a novel fluorine-18 labelled PET tracer for imaging Translocator protein 18 kDa (TSPO).
Ge Healthcare
Synthesis and structure-activity relationship studies in translocator protein ligands based on a pyrazolo[3,4-b]quinoline scaffold.
University of Siena
1,5-benzodiazepines, a novel class of hepatitis C virus polymerase nonnucleoside inhibitors.
Tibotec
Novel irreversible fluorescent probes targeting the 18 kDa translocator protein: synthesis and biological characterization.
University of Pisa
Synthesis, structure and affinity of novel 3-alkoxy-1,2-dihydro-3H-1,4-benzodiazepin-2-ones for CNS central and peripheral benzodiazepine receptors.
Institute of The National Academy of Sciences of Ukraine
Synthesis and in vitro autoradiographic evaluation of a novel high-affinity radioiodinated ligand for imaging brain cannabinoid subtype-1 receptors.
National Institute of Mental Health
Single-step high-yield radiosynthesis and evaluation of a sensitive 18F-labeled ligand for imaging brain peripheral benzodiazepine receptors with PET.
National Institute of Mental Health
Synthesis and biological evaluation of substituted [18F]imidazo[1,2-a]pyridines and [18F]pyrazolo[1,5-a]pyrimidines for the study of the peripheral benzodiazepine receptor using positron emission tomography.
Radiopharmaceuticals Research Institute
Synthesis and evaluation in monkey of two sensitive 11C-labeled aryloxyanilide ligands for imaging brain peripheral benzodiazepine receptors in vivo.
National Institute of Mental Health
2-Amino-5-arylethynyl-thiophen-3-yl-(phenyl)methanones as A
National Institute of Diabetes and Digestive and Kidney Disease
Targeting the Translocator Protein (18 kDa) in Cardiac Diseases: State of the Art and Future Opportunities.
National Research Council of Italy
Synthesis and characterization of a platinum(II) complex tethered to a ligand of the peripheral benzodiazepine receptor.
Università
Exploring Translocator Protein (TSPO) Medicinal Chemistry: An Approach for Targeting Radionuclides and Boron Atoms to Mitochondria.
Rottapharm Biotech
Synthesis and Biological Characterization of a Series of 2-Sulfonamidebenzamides as Allosteric Modulators of MrgX1.
University of Nebraska Medical Center
An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression.
Predix Pharmaceuticals
Synthesis, in vitro and in vivo evaluation of [O-methyl-11C] 2-{4-[4-(3-methoxyphenyl)piperazin-1-yl]-butyl}-4-methyl-2H-[1,2,4]-triazine-3,5-dione: a novel agonist 5-HT1A receptor PET ligand.
Columbia University College of Physicians and Surgeons
The Alpha Keto Amide Moiety as a Privileged Motif in Medicinal Chemistry: Current Insights and Emerging Opportunities.
Niddk
Glioblastoma: Current Status, Emerging Targets, and Recent Advances.
Taipei Medical University
An update into the medicinal chemistry of translocator protein (TSPO) ligands.
University of Pisa
Structure-Activity Studies of 1
National Institute of Diabetes and Digestive and Kidney Diseases
Structure-activity relationships and effects on neuroactive steroid synthesis in a series of 2-phenylimidazo[1,2-a]pyridineacetamide peripheral benzodiazepine receptors ligands.
Università
Bridged Piperidine Analogues of a High Affinity Naphthalene-Based P2Y
National Institute of Diabetes and Digestive and Kidney Diseases
Structure-Activity Relationship of Heterocyclic P2Y
National Institute of Diabetes and Digestive and Kidney Diseases
Discovery, structure-activity relationship study and biological evaluation of 2-thioureidothiophene-3-carboxylates as a novel class of C-X-C chemokine receptor 2 (CXCR2) antagonists.
University of Michigan
[18F]FMDAA1106 and [18F]FEDAA1106: two positron-emitter labeled ligands for peripheral benzodiazepine receptor (PBR).
National Institute of Radiological Sciences
Relating the structure, activity, and physical properties of ultrashort-acting benzodiazepine receptor agonists.
Glaxosmithkline
Synthesis of new molecular probes for investigation of steroid biosynthesis induced by selective interaction with peripheral type benzodiazepine receptors (PBR).
Universita' Degli Studi Di Siena
Tricyclic heterocycles display diverse sensitivity to the A147T TSPO polymorphism.
Faculty of Science and The University of Sydney
Exploration of Alternative Scaffolds for P2Y
National Institute of Diabetes and Digestive and Kidney Diseases
Imidazopyridine-based selective and multifunctional ligands of biological targets associated with psychiatric and neurodegenerative diseases.
Palack£
Truncated (N)-Methanocarba Nucleosides as Partial Agonists at Mouse and Human A
Medical College of Wisconsin
First Nondiscriminating Translocator Protein Ligands Produced from a Carbazole Scaffold.
Macquarie University
Modulation of melphalan resistance in glioma cells with a peripheral benzodiazepine receptor ligand-melphalan conjugate.
University of Kansas
Molecular basis of peripheral vs central benzodiazepine receptor selectivity in a new class of peripheral benzodiazepine receptor ligands related to alpidem.
Università
(S)-(-)-4-[4-[2-(isochroman-1-yl)ethyl]-piperazin-1-yl] benzenesulfonamide, a selective dopamine D4 antagonist.
Pharmacia & Upjohn
Chemistry, binding affinities, and behavioral properties of a new class of"antineophobic" mitochondrial DBI receptor complex (mDRC) ligands.
Mayo Foundation
Exploration of the structure-activity relationship of a novel tetracyclic class of TSPO ligands-potential novel positron emitting tomography imaging agents.
Ge Healthcare
Structure-Guided Modification of Heterocyclic Antagonists of the P2Y
National Institute of Diabetes and Digestive and Kidney Diseases
Discovery of furan and dihydrofuran-fused tricyclic benzo[d]imidazole derivatives as potent and orally efficacious microsomal prostaglandin E synthase-1 (mPGES-1) inhibitors: Part-1.
Glenmark Pharmaceuticals
Radioiodinated benzodiazepines: agents for mapping glial tumors.
University of Michigan Medical Center
Investigating isoindoline, tetrahydroisoquinoline, and tetrahydrobenzazepine scaffolds for their sigma receptor binding properties.
University of Texas At Austin
Discovery of thienopyrrolotriazine derivatives to protect mitochondrial function against Aβ-induced neurotoxicity.
Korea Institute of Science & Technology (Kist)
Discovery of N-(4-(2,4-Difluorophenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl)ethanesulfonamide (ABBV-075/Mivebresib), a Potent and Orally Available Bromodomain and Extraterminal Domain (BET) Family Bromodomain Inhibitor.
Abbvie
Lazaroids U83836E and U74389G are potent, time-dependent inhibitors of caspase-1.
Depaul University