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The publication data currently available has been vetted by Vanderbilt faculty, staff, administrators and trainees. The data itself is retrieved directly from NCBI's PubMed and is automatically updated on a weekly basis to ensure accuracy and completeness.

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Results: 11 to 20 of 98

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mGlu5 positive allosteric modulation normalizes synaptic plasticity defects and motor phenotypes in a mouse model of Rett syndrome.
Gogliotti RG, Senter RK, Rook JM, Ghoshal A, Zamorano R, Malosh C, Stauffer SR, Bridges TM, Bartolome JM, Daniels JS, Jones CK, Lindsley CW, Conn PJ, Niswender CM
(2016) Hum Mol Genet 25: 1990-2004
MeSH Terms: Adult, Allosteric Regulation, Animals, Autistic Disorder, Autopsy, Disease Models, Animal, Female, Gene Expression Regulation, Hippocampus, Humans, Male, Methyl-CpG-Binding Protein 2, Mice, Mice, Knockout, Motor Cortex, Neuronal Plasticity, Pyrazoles, Pyrimidinones, Receptor, Metabotropic Glutamate 5, Rett Syndrome, Seizures, Signal Transduction, Young Adult
Added April 6, 2017
0 Communities
4 Members
0 Resources
23 MeSH Terms
An mGlu5-Positive Allosteric Modulator Rescues the Neuroplasticity Deficits in a Genetic Model of NMDA Receptor Hypofunction in Schizophrenia.
Balu DT, Li Y, Takagi S, Presti KT, Ramikie TS, Rook JM, Jones CK, Lindsley CW, Conn PJ, Bolshakov VY, Coyle JT
(2016) Neuropsychopharmacology 41: 2052-61
MeSH Terms: Allosteric Regulation, Animals, Disease Models, Animal, Hippocampus, Male, Mice, Inbred C57BL, Mice, Knockout, Neuronal Plasticity, Oxazoles, Proto-Oncogene Proteins c-akt, Pyridines, Racemases and Epimerases, Receptor, Metabotropic Glutamate 5, Receptors, N-Methyl-D-Aspartate, Schizophrenia, Signal Transduction
Added February 18, 2016
0 Communities
3 Members
0 Resources
16 MeSH Terms
Preliminary investigation of 6,7-dihydropyrazolo[1,5-a]pyrazin-4-one derivatives as a novel series of mGlu5 receptor positive allosteric modulators with efficacy in preclinical models of schizophrenia.
Conde-Ceide S, Alcázar J, Alonso de Diego SA, López S, Martín-Martín ML, Martínez-Viturro CM, Pena MA, Tong HM, Lavreysen H, Mackie C, Bridges TM, Daniels JS, Niswender CM, Jones CK, Macdonald GJ, Steckler T, Conn PJ, Stauffer SR, Lindsley CW, Bartolomé-Nebreda JM
(2016) Bioorg Med Chem Lett 26: 429-434
MeSH Terms: Allosteric Regulation, Animals, Antipsychotic Agents, HEK293 Cells, Humans, Male, Pyrazines, Pyrazoles, Rats, Sprague-Dawley, Receptor, Metabotropic Glutamate 5, Schizophrenia
Added February 18, 2016
0 Communities
3 Members
0 Resources
11 MeSH Terms
Pharmacological Treatments for Autism Spectrum Disorder: Will Emerging Approaches Yield New Treatments?
Gogliotti RG, Conn PJ
(2016) Neuropsychopharmacology 41: 376-7
MeSH Terms: Animals, Autism Spectrum Disorder, Drug Delivery Systems, Genetic Therapy, Humans, Insulin-Like Growth Factor I, Receptor, Metabotropic Glutamate 5, Receptors, GABA-B, Treatment Outcome
Added February 18, 2016
0 Communities
1 Members
0 Resources
9 MeSH Terms
VU0477573: Partial Negative Allosteric Modulator of the Subtype 5 Metabotropic Glutamate Receptor with In Vivo Efficacy.
Nickols HH, Yuh JP, Gregory KJ, Morrison RD, Bates BS, Stauffer SR, Emmitte KA, Bubser M, Peng W, Nedelcovych MT, Thompson A, Lv X, Xiang Z, Daniels JS, Niswender CM, Lindsley CW, Jones CK, Conn PJ
(2016) J Pharmacol Exp Ther 356: 123-36
MeSH Terms: Allosteric Regulation, Animals, Anti-Anxiety Agents, Astrocytes, Behavior, Animal, Brain, Dose-Response Relationship, Drug, Drug Discovery, GABA Agonists, HEK293 Cells, Humans, Inositol Phosphates, MAP Kinase Signaling System, Membrane Potentials, Mice, Mice, Inbred C57BL, Picolinic Acids, Pyridines, Radioligand Assay, Rats, Receptor, Metabotropic Glutamate 5, Synaptic Transmission
Added February 18, 2016
0 Communities
3 Members
0 Resources
22 MeSH Terms
Acyl dihydropyrazolo[1,5-a]pyrimidinones as metabotropic glutamate receptor 5 positive allosteric modulators.
Malosh C, Turlington M, Bridges TM, Rook JM, Noetzel MJ, Vinson PN, Steckler T, Lavreysen H, Mackie C, Bartolomé-Nebreda JM, Conde-Ceide S, Martínez-Viturro CM, Piedrafita M, Sánchez-Casado MR, Macdonald GJ, Daniels JS, Jones CK, Niswender CM, Conn PJ, Lindsley CW, Stauffer SR
(2015) Bioorg Med Chem Lett 25: 5115-20
MeSH Terms: Allosteric Regulation, Animals, Brain, Dogs, Humans, Ligands, Male, Motor Activity, Pyrazoles, Pyrimidines, Pyrimidinones, Rats, Rats, Sprague-Dawley, Receptor, Metabotropic Glutamate 5, Structure-Activity Relationship
Added February 18, 2016
0 Communities
4 Members
0 Resources
15 MeSH Terms
Development of Novel, CNS Penetrant Positive Allosteric Modulators for the Metabotropic Glutamate Receptor Subtype 1 (mGlu1), Based on an N-(3-Chloro-4-(1,3-dioxoisoindolin-2-yl)phenyl)-3-methylfuran-2-carboxamide Scaffold, That Potentiate Wild Type and Mutant mGlu1 Receptors Found in Schizophrenics.
Garcia-Barrantes PM, Cho HP, Niswender CM, Byers FW, Locuson CW, Blobaum AL, Xiang Z, Rook JM, Conn PJ, Lindsley CW
(2015) J Med Chem 58: 7959-71
MeSH Terms: Animals, Central Nervous System, Epilepsy, GABA Agonists, GABA Modulators, Half-Life, Humans, Molecular Conformation, Rats, Receptor, Metabotropic Glutamate 5, Receptors, Metabotropic Glutamate, Schizophrenia, Structure-Activity Relationship
Added February 18, 2016
0 Communities
3 Members
0 Resources
13 MeSH Terms
Partial mGlu₅ Negative Allosteric Modulators Attenuate Cocaine-Mediated Behaviors and Lack Psychotomimetic-Like Effects.
Gould RW, Amato RJ, Bubser M, Joffe ME, Nedelcovych MT, Thompson AD, Nickols HH, Yuh JP, Zhan X, Felts AS, Rodriguez AL, Morrison RD, Byers FW, Rook JM, Daniels JS, Niswender CM, Conn PJ, Emmitte KA, Lindsley CW, Jones CK
(2016) Neuropsychopharmacology 41: 1166-78
MeSH Terms: Alkynes, Allosteric Regulation, Animals, Anti-Anxiety Agents, Antidepressive Agents, Brain, Cocaine, Conditioning, Classical, Conditioning, Operant, Dose-Response Relationship, Drug, Drug-Seeking Behavior, Male, Mice, Motor Activity, Phencyclidine, Pyridines, Rats, Sprague-Dawley, Receptor, Metabotropic Glutamate 5, Self Administration, Thiazoles
Added February 18, 2016
0 Communities
4 Members
0 Resources
20 MeSH Terms
Further optimization of the mGlu5 PAM clinical candidate VU0409551/JNJ-46778212: Progress and challenges towards a back-up compound.
Zhou Y, Malosh C, Conde-Ceide S, Martínez-Viturro CM, Alcázar J, Lavreysen H, Mackie C, Bridges TM, Daniels JS, Niswender CM, Jones CK, Macdonald GJ, Steckler T, Conn PJ, Stauffer SR, Bartolomé-Nebreda JM, Lindsley CW
(2015) Bioorg Med Chem Lett 25: 3515-9
MeSH Terms: Allosteric Regulation, Drug Discovery, Humans, Molecular Structure, Receptor, Metabotropic Glutamate 5, Schizophrenia, Structure-Activity Relationship
Added February 18, 2016
0 Communities
3 Members
0 Resources
7 MeSH Terms
Biased mGlu5-Positive Allosteric Modulators Provide In Vivo Efficacy without Potentiating mGlu5 Modulation of NMDAR Currents.
Rook JM, Xiang Z, Lv X, Ghoshal A, Dickerson JW, Bridges TM, Johnson KA, Foster DJ, Gregory KJ, Vinson PN, Thompson AD, Byun N, Collier RL, Bubser M, Nedelcovych MT, Gould RW, Stauffer SR, Daniels JS, Niswender CM, Lavreysen H, Mackie C, Conde-Ceide S, Alcazar J, Bartolomé-Nebreda JM, Macdonald GJ, Talpos JC, Steckler T, Jones CK, Lindsley CW, Conn PJ
(2015) Neuron 86: 1029-1040
MeSH Terms: Allosteric Regulation, Animals, Antipsychotic Agents, Cognition, Glutamic Acid, HEK293 Cells, Hippocampus, Humans, Male, Rats, Sprague-Dawley, Receptor, Metabotropic Glutamate 5, Receptors, N-Methyl-D-Aspartate, Signal Transduction
Added February 18, 2016
0 Communities
5 Members
0 Resources
13 MeSH Terms