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1. Full Text Discovery of molecular switches that modulate modes of metabotropic glutamate receptor subtype 5 (mGlu5) pharmacology in vitro and in vivo within a series of functionalized, regioisomeric 2- and 5-(phenylethynyl) pyrimidines
by Sharma, Sameer and Kedrowski, Jeffrey and Rook, Jerri M and Smith, Randy L and Jones, Carrie K and Rodriguez, Alice L and Conn, P. Jeffrey and Lindsley, Craig W
Journal of Medicinal Chemistry, ISSN 0022-2623, 07/2009, Volume 52, Issue 14, pp. 4103 - 4106
We describe the synthesis and SAR of a series or analogues of the mGlu(5) partial antagonist 5-(phenylethynyl)pyrimidine. New molecular switches are identified... 
POTENT | CHEMISTRY, MEDICINAL | ALLOSTERIC MODULATORS | ANTAGONIST | SAR | MTEP | MPEP | GLUTAMATE-RECEPTOR-SUBTYPE-5 | Pyrimidines - chemical synthesis | Stereoisomerism | Allosteric Regulation | Humans | Rats | Structure-Activity Relationship | Pyrimidines - pharmacology | Pyrimidines - chemistry | Dose-Response Relationship, Drug | Animals | Inhibitory Concentration 50 | Receptor, Metabotropic Glutamate 5 | Receptors, Metabotropic Glutamate - antagonists & inhibitors | Index Medicus
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2. Full Text Imaging Glutamate Homeostasis in Cocaine Addiction with the Metabotropic Glutamate Receptor 5 Positron Emission Tomography Radiotracer [11 C]ABP688 and Magnetic Resonance Spectroscopy
by Martinez, Diana and Slifstein, Mark and Nabulsi, Nabeel and Grassetti, Alexander and Urban, Nina B.L and Perez, Audrey and Liu, Fei and Lin, Shu-Fei and Ropchan, Jim and Mao, Xiangling and Kegeles, Lawrence S and Shungu, Dikoma C and Carson, Richard E and Huang, Yiyun
Biological Psychiatry, ISSN 0006-3223, 2014, Volume 75, Issue 2, pp. 165 - 171
Background Preclinical studies demonstrate that glutamate homeostasis in the striatum is disrupted following cocaine exposure, including a decrease in... 
Psychiatry | cocaine self-administration | magnetic resonance spectroscopy | Addiction | positron emission tomography | cocaine | metabotropic glutamate receptor 5 | SQUIRREL-MONKEYS | INDUCED REINSTATEMENT | PSYCHIATRY | DEPENDENT PATIENTS | MGLUR5 ANTAGONIST MPEP | NEUROSCIENCES | PREFRONTAL CORTEX | NUCLEUS-ACCUMBENS | FUNCTIONAL SUBDIVISIONS | IN-VIVO | INDUCED DOPAMINE RELEASE | GAMMA-AMINOBUTYRIC-ACID | Oximes | Pyridines | Brain - diagnostic imaging | Choice Behavior - drug effects | Magnetic Resonance Spectroscopy | Humans | Glutamine - metabolism | Homeostasis | Male | Positron-Emission Tomography | Receptor, Metabotropic Glutamate 5 - metabolism | Corpus Striatum - metabolism | Case-Control Studies | Brain - metabolism | Young Adult | Cocaine - administration & dosage | Self Administration | Cocaine-Related Disorders - metabolism | Functional Neuroimaging | Cocaine-Related Disorders - diagnostic imaging | Adult | Glutamic Acid - metabolism | Corpus Striatum - diagnostic imaging | Carbon Radioisotopes | Drug abuse | Medical colleges | PET imaging | Nuclear magnetic resonance spectroscopy | Amino acids | Cocaine | Glutamate
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3. Full Text Discovery of novel positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu 5)
by Varnes, Jeffrey G and Marcus, Andrew P and Mauger, Russell C and Throner, Scott R and Hoesch, Valerie and King, Megan M and Wang, Xia and Sygowski, Linda A and Spear, Nathan and Gadient, Reto and Brown, Dean G and Campbell, James B
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 2011, Volume 21, Issue 5, pp. 1402 - 1406
Positive allosteric modulators of mGlu are described. Novel in vitro mGlu positive allosteric modulators with good potency, solubility, and low lipophilicity... 
mGlu5 | Schizophrenia | NMDAr | Positive allosteric modulator | N-Methyl- d-aspartate receptor | Glutamate | Metabotropic glutamate receptor 5 | N-Methyl-d-aspartate receptor | CHEMISTRY, MEDICINAL | CHEMISTRY, ORGANIC | POTENT | IN-VIVO | PROGRESS | MGLUR5 | N-Methyl-D-aspartate receptor | Inhibitory Concentration 50 | Receptor, Metabotropic Glutamate 5 | Receptors, Metabotropic Glutamate - metabolism | Allosteric Regulation | Drug Design | Index Medicus | Allosteric properties | Solubility | carbonyls | Nitrogen | ketones | phenylacetylene | Glutamic acid receptors (metabotropic)
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4. Full Text Test–retest variability of [11C]ABP688 estimates of metabotropic glutamate receptor subtype 5 availability in humans
by Smart, Kelly and Cox, Sylvia M. L and Nagano‐Saito, Atsuko and Rosa‐Neto, Pedro and Leyton, Marco and Benkelfat, Chawki
Synapse, ISSN 0887-4476, 09/2018, Volume 72, Issue 9, pp. e22041 - n/a
[ 11 C]ABP688 is a positron emission tomography (PET) radioligand that binds selectively to metabotropic glutamate type 5 receptors (mGluR5). The use of this... 
test–retest | positron emission tomography | C]ABP688 | metabotropic glutamate receptor type 5 | PET TRACER | test-retest | VALIDATION | C-11-ABP688 | [C-11]ABP688 | NEUROSCIENCES | REPRODUCIBILITY | IN-VIVO VARIATION | POSITRON-EMISSION-TOMOGRAPHY | MGLUR5 | HEALTHY-VOLUNTEERS | BINDING | BRAIN | Glutamate | Analysis | Menstruation | Mood | Amygdala | Menstrual cycle | Cortex | Neostriatum | Glutamic acid receptors | Anxiety | Hydrocortisone | Glutamic acid receptors (metabotropic) | Positron emission tomography
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5. Full Text Test–retest reproducibility of the metabotropic glutamate receptor 5 ligand [18F]FPEB with bolus plus constant infusion in humans
by Park, Eunkyung and Sullivan, Jenna M and Planeta, Beata and Gallezot, Jean-Dominique and Lim, Keunpoong and Lin, Shu-Fei and Ropchan, Jim and McCarthy, Timothy J and Ding, Yu-Shin and Morris, Evan D and Williams, Wendol A and Huang, Yiyun and Carson, Richard E
European Journal of Nuclear Medicine and Molecular Imaging, ISSN 1619-7070, 9/2015, Volume 42, Issue 10, pp. 1530 - 1541
[18F]FPEB is a promising PET radioligand for the metabotropic glutamate receptor 5 (mGluR5), a potential target for the treatment of neuropsychiatric diseases.... 
Human | Medicine & Public Health | Reproducibility | Orthopedics | Oncology | Nuclear Medicine | Imaging / Radiology | Cardiology | [ 18 F]FPEB | Metabotropic glutamate receptor 5 | Positron emission tomography | F]FPEB | QUANTITATION | RADIOTRACER | [F-18\]FPEB | IN-VITRO | POSITRON-EMISSION-TOMOGRAPHY | TRACER | MGLUR5 | TARGETS | BINDING | RADIOLOGY, NUCLEAR MEDICINE & MEDICAL IMAGING | PET | Brain - diagnostic imaging | Reproducibility of Results | Pyridines - administration & dosage | Radiopharmaceuticals - pharmacokinetics | Humans | Pyridines - pharmacokinetics | Male | Molecular Imaging - methods | Positron-Emission Tomography - methods | Receptor, Metabotropic Glutamate 5 - metabolism | Nitriles - pharmacokinetics | Brain - metabolism | Nitriles - administration & dosage | Radiopharmaceuticals - administration & dosage | Tissue Distribution | Young Adult | Sensitivity and Specificity | Adult | Infusions, Intravenous | Tomography | Brain | Neurotransmitters | Medical imaging
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6. Full Text Biased mGlu(5)-Positive Allosteric Modulators Provide In Vivo Efficacy without Potentiating mGlu(5) Modulation of NMDAR Currents
by Rook, JM and Xiang, ZX and Lv, XH and Ghoshal, A and Dickerson, JW and Bridges, TM and Johnson, KA and Foster, DJ and Gregory, KJ and Vinson, PN and Thompson, AD and Byun, N and Collier, RL and Bubser, M and Nedelcovych, MT and Gould, RW and Stauffer, SR and Daniels, JS and Niswender, CM and Lavreysen, H and Mackie, C and Conde-Ceide, S and Alcazar, J and Bartolome-Nebreda, JM and Macdonald, GJ and Talpos, JC and Steckler, T and Jones, CK and Lindsley, CW and Conn, PJ
NEURON, ISSN 0896-6273, 05/2015, Volume 86, Issue 4, pp. 1029 - 1040
Schizophrenia is associated with disruptions in N-methyl-D-aspartate glutamate receptor subtype (NMDAR)-mediated excitatory synaptic signaling. The... 
GLUTAMATE-RECEPTOR 5 | PROTEIN-KINASE-C | SIGNALING PATHWAYS | BEHAVIORAL-MODELS | PREPULSE INHIBITION | COGNITIVE ENHANCEMENT | LOCOMOTOR-ACTIVITY | RAT HIPPOCAMPAL SLICES | NEUROSCIENCES | METHYL-D-ASPARTATE | ANTIPSYCHOTIC-LIKE
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7. Full Text Kinetic Analysis of the Metabotropic Glutamate Subtype 5 Tracer [18F]FPEB in Bolus and Bolus-Plus-Constant-Infusion Studies in Humans
by Sullivan, Jenna M and Lim, Keunpoong and Labaree, David and Lin, Shu-fei and McCarthy, Timothy J and Seibyl, John P and Tamagnan, Gilles and Huang, Yiyun and Carson, Richard E and Ding, Yu-Shin and Morris, Evan D
Journal of Cerebral Blood Flow & Metabolism, ISSN 0271-678X, 4/2013, Volume 33, Issue 4, pp. 532 - 541
[18F]FPEB is a positron emission tomography tracer which, in preclinical studies, has shown high specificity and selectivity toward the metabotropic glutamate... 
scan duration | binding potential (BPND) | mGluR5 | glutamate | bolus-plus-constant-infusion | total volume of distribution (V | VIVO | RECEPTOR | REFERENCE TISSUE MODELS | NEUROSCIENCES | total volume of distribution (V-T) | IN-VITRO | POSITRON-EMISSION-TOMOGRAPHY | ENDOCRINOLOGY & METABOLISM | METABOTROPIC-GLUTAMATE-RECEPTOR-SUBTYPE-5 | HEMATOLOGY | BINDING | PET | BRAIN | Radioactive Tracers | Models, Biological | Humans | Receptor, Metabotropic Glutamate 5 | Adult | Female | Male | Kinetics | Positron-Emission Tomography - methods | Receptors, Metabotropic Glutamate - agonists | total volume of distribution (VT) | Original
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8. Full Text Automated cGMP‐compliant radiosynthesis of [18F]‐(E)‐PSS232 for brain PET imaging of metabotropic glutamate receptor subtype 5
by Park, Jun Young and Son, Jeongmin and Yun, Mijin and Ametamey, Simon M and Chun, Joong‐Hyun
Journal of Labelled Compounds and Radiopharmaceuticals, ISSN 0362-4803, 01/2018, Volume 61, Issue 1, pp. 30 - 37
( E )‐3‐(Pyridin‐2‐yl ethynyl)cyclohex‐2‐enone O ‐(3‐(2‐[ 18 F]‐fluoroethoxy)propyl) oxime ([ 18 F]‐( E )‐PSS232, [ 18 F] 2a ) is a recently developed... 
mGlu | fluorine‐18 | automation | PET imaging | F | radiopharmaceutical | PSS232 | F]-(E)-PSS232 | fluorine-18 | CHEMISTRY, ANALYTICAL | CHEMISTRY, MEDICINAL | [F-18]-(E)-PSS232 | RADIOLIGAND | BIOCHEMICAL RESEARCH METHODS | C-11-ABP688 | PATHOGENESIS | POSITRON-EMISSION-TOMOGRAPHY | PHARMACOLOGY | MGLUR5 | DISEASE | RAT-BRAIN | METABOTROPIC-GLUTAMATE-RECEPTOR-SUBTYPE-5 | PRECLINICAL EVALUATION | Glutamate | Pets | Neuroimaging | Brain | Automation | Purification | Mental disorders | Fluorine | Positron emission | Glutamic acid receptors | High-performance liquid chromatography | Cyclotrons | Fluoride | Synthesis | Cyclic GMP | Dimethyl sulfoxide | Radiochemistry | Tomography | Diagnostic systems | Glutamic acid receptors (metabotropic) | Positron emission tomography | High performance liquid chromatography
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9. Full Text The metabotropic glutamate receptor 5 radioligand [11C]AZD9272 identifies unique binding sites in primate brain
by Varnäs, Katarina and Juréus, Anders and Finnema, Sjoerd J and Johnström, Peter and Raboisson, Patrick and Amini, Nahid and Takano, Akihiro and Stepanov, Vladimir and Halldin, Christer and Farde, Lars
Neuropharmacology, ISSN 0028-3908, 06/2018, Volume 135, pp. 455 - 463
The metabotropic glutamate receptor 5 (mGluR5) is a target for drug development and for imaging studies of the glutamate system in neurological and psychiatric... 
Autoradiography | Fenobam | PET imaging | Negative allosteric modulator | Metabotropic glutamate receptor 5 | AZD9272 | POSITIVE ALLOSTERIC MODULATOR | NERVOUS-SYSTEM | NONHUMAN PRIMATE | SCHIZOPHRENIA | NONBENZODIAZEPINE | NEUROSCIENCES | IN-VITRO | SUBTYPE-5 | PHARMACOLOGY | PHARMACOLOGY & PHARMACY | PET | Binding, Competitive | Brain - diagnostic imaging | Radiopharmaceuticals - pharmacokinetics | Allosteric Regulation | Macaca fascicularis | Pyridines - pharmacokinetics | Male | Receptor, Metabotropic Glutamate 5 - antagonists & inhibitors | Imidazoles - pharmacology | Positron-Emission Tomography | Receptor, Metabotropic Glutamate 5 - metabolism | Brain - metabolism | Animals | Female | Oxadiazoles - pharmacokinetics | Binding Sites | Primates | Amino acids | Glutamate | Mental illness
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10. Full Text Synthesis and preliminary biological evaluation of 3‐[18F]fluoro‐5‐(2‐pyridinylethynyl)benzonitrile as a PET radiotracer for imaging metabotropic glutamate receptor subtype 5
by Wang, Ji‐Quan and Tueckmantel, Werner and Zhu, Aijun and Pellegrino, Daniela and Brownell, Anna‐Liisa
Synapse, ISSN 0887-4476, 12/2007, Volume 61, Issue 12, pp. 951 - 961
The metabotropic glutamate receptor subtype 5 (mGluR5) has been reported to be implicated in various neurological disorders in the central nervous system.To... 
radiotracer | F]FPEB | metabotropic glutamate receptor | mGluR5 | PET | Radiotracer | Metabotropic glutamate receptor | METABOTROPIC GLUTAMATE-RECEPTOR | ALLOSTERIC MODULATORS | MPEP | NEUROSCIENCES | POTENT | SUBTYPE-5 | [F-18]FPEB | DERIVATIVES | BINDING | MGLUR5 ANTAGONIST | BRAIN | IN-VIVO CHARACTERIZATION | Brain - diagnostic imaging | Male | Nitriles - chemical synthesis | Nitriles - pharmacokinetics | Radiopharmaceuticals - chemical synthesis | Thiazoles - pharmacokinetics | Brain - metabolism | Piperidines - pharmacology | Reaction Time - drug effects | Receptor, Metabotropic Glutamate 5 | Whole Body Imaging - methods | Tissue Distribution - drug effects | Radiopharmaceuticals - pharmacokinetics | Rats | Excitatory Amino Acid Antagonists - pharmacology | Positron-Emission Tomography - methods | Rats, Sprague-Dawley | Brain - drug effects | Animals | Thiazoles - chemical synthesis | Benzimidazoles - pharmacology | Pyridines - pharmacology | Thiazoles - pharmacology | Evaluation Studies as Topic | Receptors, Metabotropic Glutamate - analysis
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11. Full Text Spectrin mutations cause spinocerebellar ataxia type 5
by Clark, H Brent and Armbrust, Karen R and Stevanin, Giovanni and Day, John W and Schut, Lawrence J and Weatherspoon, Marcy R and Ikeda, Yoshio and Dürr, Alexandra and Brice, Alexis and Dalton, Joline C and Gincel, Dan and Rothstein, Jeffrey D and Bürk, Katrin and Ranum, Laura P W and Zühlke, Christine and Dick, Katherine A
Nature Genetics, ISSN 1061-4036, 02/2006, Volume 38, Issue 2, pp. 184 - 190
We have discovered that β-III spectrin (SPTBN2) mutations cause spinocerebellar ataxia type 5 (SCA5) in an 11-generation American kindred descended from... 
GLUTAMATE-RECEPTOR GENE | PURKINJE-CELLS | PATHOGENESIS | TRANSPORT | LURCHER | MEMBRANE | DYNACTIN | DISEASE | GENETICS & HEREDITY | NEURONS | FEATURES | Spectrin | Cytoskeletal Proteins - genetics | Humans | Middle Aged | Spinocerebellar Ataxias - classification | Molecular Sequence Data | Male | Case-Control Studies | Nerve Tissue Proteins - chemistry | Amino Acid Transport System X-AG - metabolism | Aged, 80 and over | Adult | Female | Child | Spinocerebellar Ataxias - genetics | Amino Acid Sequence | Cell Line | Chromosome Mapping | Cytoskeletal Proteins - chemistry | Nerve Tissue Proteins - genetics | Cerebellum - pathology | Animals | Pedigree | Excitatory Amino Acid Transporter 4 - metabolism | Adolescent | Aged | Mice | Complications and side effects | Genetic aspects | Diagnosis | Gene mutations | Spinocerebellar ataxia | Risk factors | Proteins | Cell culture | Membranes | Genetics | Nervous system | Heredity | Mutation | Gene expression
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12. Full Text Preparation of the metabotropic glutamate receptor 5 (mGluR5) PET tracer [18F]FPEB for human use: An automated radiosynthesis and a novel one-pot synthesis of its radiolabeling precursor
by Lim, Keunpoong and Labaree, David and Li, Songye and Huang, Yiyun
Applied Radiation and Isotopes, ISSN 0969-8043, 12/2014, Volume 94, pp. 349 - 354
The radiotracer 3-[ F]fluoro-5-(2-pyridinylethynyl)benzonitrile, or [ F]FPEB, is a promising PET imaging agent for the metabotropic glutamate subtype 5... 
Suzuki coupling | Radiotracer synthesis | [18F]FPEB | mGluR5 | PET | F]FPEB | MGluR5 | NUCLEAR SCIENCE & TECHNOLOGY | METABOTROPIC-GLUTAMATE-RECEPTOR-SUBTYPE-5 | [F-18]FPEB | RADIOLOGY, NUCLEAR MEDICINE & MEDICAL IMAGING | CHEMISTRY, INORGANIC & NUCLEAR | Radiopharmaceuticals - pharmacokinetics | Humans | Pyridines - chemical synthesis | Pyridines - pharmacokinetics | Molecular Imaging - methods | Nitriles - chemical synthesis | Positron-Emission Tomography - methods | Receptor, Metabotropic Glutamate 5 - metabolism | Nitriles - pharmacokinetics | Radiopharmaceuticals - chemical synthesis | Isotope Labeling - methods | Fluorine Radioisotopes - pharmacokinetics | Robotics - methods | Fluorine Radioisotopes - chemistry | Pets | Nitriles | Tracers (Biology) | Glutamate | Production processes | Medical colleges | Synthesis | Organic compounds
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13. Full Text Block of Long-Term Potentiation by Naturally Secreted and Synthetic Amyloid β-Peptide in Hippocampal Slices Is Mediated via Activation of the Kinases c-Jun N-Terminal Kinase, Cyclin-Dependent Kinase 5, and p38 Mitogen-Activated Protein Kinase as well as Metabotropic Glutamate Receptor Type 5
by Wang, Qinwen and Walsh, Dominic M and Rowan, Michael J and Selkoe, Dennis J and Anwyl, Roger
Journal of Neuroscience, ISSN 0270-6474, 03/2004, Volume 24, Issue 13, pp. 3370 - 3378
The mechanisms of action of human synthetic and naturally secreted cell-derived amyloid beta-peptide (Abeta)(1-42) on the induction of long-term potentiation... 
Metabotropic glutamate receptors | Cdk5 | JNK | LTP | Amyloid β-protein | Alzheimer's disease | p38 MAPK | Hippocampus | NEURONAL APOPTOSIS | hippocampus | ALZHEIMERS-DISEASE | MAP KINASE | metabotropic glutamate receptors | amyloid beta-protein | SYNAPTIC PLASTICITY | FREQUENCY STIMULATION | AREA CA1 | NEUROSCIENCES | IN-VITRO | PATHWAY | MICE | PRECURSOR PROTEIN | Receptors, Metabotropic Glutamate - drug effects | Cyclin-Dependent Kinases - metabolism | Amyloid beta-Peptides - pharmacology | Humans | Amyloid beta-Peptides - secretion | Peptide Fragments - pharmacology | Receptors, Metabotropic Glutamate - metabolism | Hippocampus - drug effects | Ovary - cytology | Excitatory Postsynaptic Potentials - drug effects | Cyclin-Dependent Kinases - drug effects | Dose-Response Relationship, Drug | Excitatory Postsynaptic Potentials - physiology | Long-Term Potentiation - drug effects | Amyloid beta-Peptides - genetics | JNK Mitogen-Activated Protein Kinases | Long-Term Potentiation - physiology | Receptor, Metabotropic Glutamate 5 | Female | Electric Stimulation - methods | Peptide Fragments - genetics | p38 Mitogen-Activated Protein Kinases | CHO Cells | Ovary - metabolism | Cricetinae | Enzyme Inhibitors - pharmacology | Peptide Fragments - secretion | Rats | Excitatory Amino Acid Antagonists - pharmacology | Cyclin-Dependent Kinase 5 | Animals | Ovary - secretion | Hippocampus - physiology | In Vitro Techniques | Mitogen-Activated Protein Kinases - drug effects | Mitogen-Activated Protein Kinases - metabolism | Plasticity | Development | amyloid β-protein | Repair
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14. Full Text In vivo variation in same-day estimates of metabotropic glutamate receptor subtype 5 binding using [11C]ABP688 and [18F]FPEB
by DeLorenzo, Christine and Gallezot, Jean-Dominique and Gardus, John and Yang, Jie and Planeta, Beata and Nabulsi, Nabeel and Ogden, R Todd and Labaree, David C and