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Discovery of Tricyclic Triazolo- and Imidazopyridine Lactams as M Positive Allosteric Modulators.
Engers JL, Bender AM, Kalbfleisch JJ, Cho HP, Lingenfelter KS, Luscombe VB, Han C, Melancon BJ, Blobaum AL, Dickerson JW, Rook JM, Niswender CM, Emmitte KA, Conn PJ, Lindsley CW
(2019) ACS Chem Neurosci 10: 1035-1042
MeSH Terms: Allosteric Regulation, Animals, Drug Discovery, Humans, Imidazoles, Lactams, Mice, Muscarinic Agonists, Pyridines, Rats, Receptor, Muscarinic M1
Added March 3, 2020
0 Communities
2 Members
0 Resources
11 MeSH Terms
Classics in Chemical Neuroscience: Xanomeline.
Bender AM, Jones CK, Lindsley CW
(2017) ACS Chem Neurosci 8: 435-443
MeSH Terms: Animals, Central Nervous System Diseases, Humans, Muscarinic Agonists, Neurosciences, Pyridines, Thiadiazoles
Added March 18, 2020
0 Communities
1 Members
0 Resources
MeSH Terms
Diverse Effects on M Signaling and Adverse Effect Liability within a Series of M Ago-PAMs.
Rook JM, Abe M, Cho HP, Nance KD, Luscombe VB, Adams JJ, Dickerson JW, Remke DH, Garcia-Barrantes PM, Engers DW, Engers JL, Chang S, Foster JJ, Blobaum AL, Niswender CM, Jones CK, Conn PJ, Lindsley CW
(2017) ACS Chem Neurosci 8: 866-883
MeSH Terms: Allosteric Regulation, Animals, Drug Discovery, Humans, Mice, Muscarinic Agonists, Rats, Receptor, Muscarinic M1, Structure-Activity Relationship
Added April 6, 2017
0 Communities
4 Members
0 Resources
9 MeSH Terms
Antipsychotic-like Effects of M4 Positive Allosteric Modulators Are Mediated by CB2 Receptor-Dependent Inhibition of Dopamine Release.
Foster DJ, Wilson JM, Remke DH, Mahmood MS, Uddin MJ, Wess J, Patel S, Marnett LJ, Niswender CM, Jones CK, Xiang Z, Lindsley CW, Rook JM, Conn PJ
(2016) Neuron 91: 1244-1252
MeSH Terms: Allosteric Regulation, Animals, Antipsychotic Agents, Corpus Striatum, Dopamine, Lipoprotein Lipase, Mice, Knockout, Muscarinic Agonists, Oxotremorine, Prepulse Inhibition, Pyridazines, Receptor, Cannabinoid, CB2, Receptor, Muscarinic M4, Thiophenes
Added April 6, 2017
0 Communities
6 Members
0 Resources
14 MeSH Terms
Application of Parallel Multiparametric Cell-Based FLIPR Detection Assays for the Identification of Modulators of the Muscarinic Acetylcholine Receptor 4 (M4).
Smith E, Chase P, Niswender CM, Utley TJ, Sheffler DJ, Noetzel MJ, Lamsal A, Wood MR, Conn PJ, Lindsley CW, Madoux F, Acosta M, Scampavia L, Spicer T, Hodder P
(2015) J Biomol Screen 20: 858-68
MeSH Terms: Allosteric Regulation, Animals, Cell Line, Drug Discovery, Gene Expression, High-Throughput Screening Assays, Humans, Muscarinic Agonists, Muscarinic Antagonists, Receptor, Muscarinic M4, Small Molecule Libraries
Added February 18, 2016
0 Communities
2 Members
0 Resources
11 MeSH Terms
Chemical modification of the M(1) agonist VU0364572 reveals molecular switches in pharmacology and a bitopic binding mode.
Digby GJ, Utley TJ, Lamsal A, Sevel C, Sheffler DJ, Lebois EP, Bridges TM, Wood MR, Niswender CM, Lindsley CW, Conn PJ
(2012) ACS Chem Neurosci 3: 1025-36
MeSH Terms: Allosteric Regulation, Allosteric Site, Animals, Benzamides, Biphenyl Compounds, CHO Cells, Cricetinae, Ligands, Muscarinic Agonists, Rats, Receptor, Muscarinic M1
Added March 7, 2014
1 Communities
3 Members
0 Resources
11 MeSH Terms
Targeting selective activation of M(1) for the treatment of Alzheimer's disease: further chemical optimization and pharmacological characterization of the M(1) positive allosteric modulator ML169.
Tarr JC, Turlington ML, Reid PR, Utley TJ, Sheffler DJ, Cho HP, Klar R, Pancani T, Klein MT, Bridges TM, Morrison RD, Blobaum AL, Xiang Z, Daniels JS, Niswender CM, Conn PJ, Wood MR, Lindsley CW
(2012) ACS Chem Neurosci 3: 884-95
MeSH Terms: Allosteric Regulation, Alzheimer Disease, Animals, Cognition, Drug Discovery, Indoles, Muscarinic Agonists, Myotonin-Protein Kinase, Neurons, Protein Serine-Threonine Kinases, Rats, Receptor, Muscarinic M1, Sulfones
Added March 7, 2014
1 Communities
3 Members
0 Resources
13 MeSH Terms
Novel allosteric agonists of M1 muscarinic acetylcholine receptors induce brain region-specific responses that correspond with behavioral effects in animal models.
Digby GJ, Noetzel MJ, Bubser M, Utley TJ, Walker AG, Byun NE, Lebois EP, Xiang Z, Sheffler DJ, Cho HP, Davis AA, Nemirovsky NE, Mennenga SE, Camp BW, Bimonte-Nelson HA, Bode J, Italiano K, Morrison R, Daniels JS, Niswender CM, Olive MF, Lindsley CW, Jones CK, Conn PJ
(2012) J Neurosci 32: 8532-44
MeSH Terms: Animals, Arrestins, Behavior, Animal, Benzamides, Biphenyl Compounds, Brain, CHO Cells, Calcium, Cell Line, Corpus Striatum, Cricetinae, Cricetulus, Extracellular Signal-Regulated MAP Kinases, Extracellular Space, Fear, Gene Expression Profiling, Hippocampus, Humans, Male, Maze Learning, Membrane Potentials, Mice, Mice, Inbred C57BL, Muscarinic Agonists, Phosphorylation, Prefrontal Cortex, Rats, Rats, Sprague-Dawley, Receptor, Muscarinic M1
Added March 7, 2014
1 Communities
5 Members
0 Resources
29 MeSH Terms
Muscarinic receptor pharmacology and circuitry for the modulation of cognition.
Bubser M, Byun N, Wood MR, Jones CK
(2012) Handb Exp Pharmacol : 121-66
MeSH Terms: Acetylcholine, Animals, Brain, Cognition, Cognition Disorders, Humans, Muscarinic Agonists, Muscarinic Antagonists, Nootropic Agents, Receptors, Muscarinic, Signal Transduction
Added March 14, 2018
0 Communities
2 Members
0 Resources
11 MeSH Terms
Contribution of both M1 and M4 receptors to muscarinic agonist-mediated attenuation of the cocaine discriminative stimulus in mice.
Thomsen M, Lindsley CW, Conn PJ, Wessell JE, Fulton BS, Wess J, Caine SB
(2012) Psychopharmacology (Berl) 220: 673-85
MeSH Terms: Animals, Cocaine, Conditioning, Operant, Discrimination Learning, Dose-Response Relationship, Drug, Male, Mice, Mice, Inbred C57BL, Mice, Knockout, Muscarinic Agonists, Receptor, Muscarinic M1, Receptor, Muscarinic M4, Self Administration
Added February 19, 2015
0 Communities
1 Members
0 Resources
13 MeSH Terms