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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: 1 to 8 of 8

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Further optimization of the M1 PAM VU0453595: Discovery of novel heterobicyclic core motifs with improved CNS penetration.
Panarese JD, Cho HP, Adams JJ, Nance KD, Garcia-Barrantes PM, Chang S, Morrison RD, Blobaum AL, Niswender CM, Stauffer SR, Conn PJ, Lindsley CW
(2016) Bioorg Med Chem Lett 26: 3822-5
MeSH Terms: Allosteric Regulation, Animals, Central Nervous System, Central Nervous System Agents, Dose-Response Relationship, Drug, Drug Discovery, Heterocyclic Compounds, Molecular Structure, Pyridines, Pyrroles, Rats, Receptor, Muscarinic M1, Structure-Activity Relationship
Added April 6, 2017
0 Communities
2 Members
0 Resources
13 MeSH Terms
Discovery of (S)-2-cyclopentyl-N-((1-isopropylpyrrolidin2-yl)-9-methyl-1-oxo-2,9-dihydro-1H-pyrrido[3,4-b]indole-4-carboxamide (VU0453379): a novel, CNS penetrant glucagon-like peptide 1 receptor (GLP-1R) positive allosteric modulator (PAM).
Morris LC, Nance KD, Gentry PR, Days EL, Weaver CD, Niswender CM, Thompson AD, Jones CK, Locuson CW, Morrison RD, Daniels JS, Niswender KD, Lindsley CW
(2014) J Med Chem 57: 10192-7
MeSH Terms: Allosteric Regulation, Animals, Catalepsy, Central Nervous System Agents, Drug Synergism, Exenatide, Glucagon-Like Peptide 1, Glucagon-Like Peptide-1 Receptor, Haloperidol, High-Throughput Screening Assays, Indoles, Insulin, Insulin Secretion, Islets of Langerhans, Male, Mice, Inbred C57BL, Microsomes, Liver, Peptides, Pyrrolidines, Receptors, Glucagon, Structure-Activity Relationship, Venoms
Added February 16, 2015
0 Communities
4 Members
0 Resources
22 MeSH Terms
Opportunities and challenges in the discovery of allosteric modulators of GPCRs for treating CNS disorders.
Conn PJ, Lindsley CW, Meiler J, Niswender CM
(2014) Nat Rev Drug Discov 13: 692-708
MeSH Terms: Allosteric Regulation, Animals, Central Nervous System Agents, Central Nervous System Diseases, Drug Discovery, Humans, Receptors, G-Protein-Coupled, Treatment Outcome
Added January 24, 2015
1 Communities
3 Members
0 Resources
8 MeSH Terms
Total synthesis and biological evaluation of phidianidines A and B uncovers unique pharmacological profiles at CNS targets.
Brogan JT, Stoops SL, Lindsley CW
(2012) ACS Chem Neurosci 3: 658-64
MeSH Terms: Animals, CHO Cells, Cell Proliferation, Cell Survival, Central Nervous System Agents, Chromatography, High Pressure Liquid, Cricetinae, Cricetulus, Dopamine Plasma Membrane Transport Proteins, Gastropoda, Guanosine 5'-O-(3-Thiotriphosphate), HEK293 Cells, Humans, Indicators and Reagents, Indole Alkaloids, Ligands, Oxadiazoles, Radioligand Assay, Receptors, Opioid, mu, Serotonin Plasma Membrane Transport Proteins, Structure-Activity Relationship
Added March 7, 2014
1 Communities
1 Members
0 Resources
21 MeSH Terms
Sigma-1 receptors: potential targets for the treatment of substance abuse.
Robson MJ, Noorbakhsh B, Seminerio MJ, Matsumoto RR
(2012) Curr Pharm Des 18: 902-19
MeSH Terms: Animals, Central Nervous System Agents, Humans, Receptors, sigma, Substance-Related Disorders
Added July 10, 2013
0 Communities
1 Members
0 Resources
5 MeSH Terms
Allosteric modulation of seven transmembrane spanning receptors: theory, practice, and opportunities for central nervous system drug discovery.
Melancon BJ, Hopkins CR, Wood MR, Emmitte KA, Niswender CM, Christopoulos A, Conn PJ, Lindsley CW
(2012) J Med Chem 55: 1445-64
MeSH Terms: Allosteric Regulation, Animals, Central Nervous System Agents, Drug Discovery, Humans, Ligands, Receptors, G-Protein-Coupled, Receptors, Metabotropic Glutamate, Receptors, Muscarinic, Structure-Activity Relationship
Added February 19, 2015
0 Communities
2 Members
0 Resources
10 MeSH Terms
Subtype-selective allosteric modulators of muscarinic receptors for the treatment of CNS disorders.
Conn PJ, Jones CK, Lindsley CW
(2009) Trends Pharmacol Sci 30: 148-55
MeSH Terms: Allosteric Regulation, Alzheimer Disease, Animals, Antipsychotic Agents, Central Nervous System Agents, Humans, Mental Disorders, Muscarinic Agonists, Muscarinic Antagonists, Receptor, Muscarinic M1, Receptor, Muscarinic M4, Receptors, Muscarinic, Schizophrenia
Added March 5, 2014
1 Communities
2 Members
0 Resources
13 MeSH Terms
Phosphorylation and sequestration of serotonin transporters differentially modulated by psychostimulants.
Ramamoorthy S, Blakely RD
(1999) Science 285: 763-6
MeSH Terms: Antidepressive Agents, Biogenic Monoamines, Biotinylation, Carrier Proteins, Cell Line, Central Nervous System Agents, Cocaine, Dextroamphetamine, Enzyme Activation, Humans, Ligands, Membrane Glycoproteins, Membrane Transport Proteins, Models, Biological, Nerve Tissue Proteins, Neurotransmitter Agents, Phosphorylation, Protein Kinase C, Protein Kinases, Serotonin, Serotonin Antagonists, Serotonin Plasma Membrane Transport Proteins, Serotonin Uptake Inhibitors, Tetradecanoylphorbol Acetate
Added July 10, 2013
1 Communities
1 Members
0 Resources
24 MeSH Terms