Search Results - "Dickerson, Jonathan W."

M 1 muscarinic activation induces long-lasting increase in intrinsic excitability of striatal projection neurons by Lv, Xiaohui, Dickerson, Jonathan W, Rook, Jerri M, Lindsley, Craig W, Conn, P Jeffrey, Xiang, Zixiu

“…The dorsolateral striatum is critically involved in movement control and motor learning. Striatal function is regulated by a variety of neuromodulators…”
Get full text

Discovery of “Molecular Switches” within a Series of mGlu5 Allosteric Ligands Driven by a “Magic Methyl” Effect Affording Both PAMs and NAMs with In Vivo Activity, Derived from an M1 PAM Chemotype by Barbaro, Lisa, Rodriguez, Alice L, Blevins, Ashlyn N, Dickerson, Jonathan W, Billard, Natasha, Boutaud, Olivier, Rook, Jerri L, Niswender, Colleen M, Conn, P.Jeffrey, Engers, Darren W, Lindsley, Craig W

“…In the course of optimizing an M1 PAM chemotype, introduction of an ether moiety unexpectedly abolished M1 PAM activity while engendering a “molecular switch”…”
Get full text

Biased mGlu5-Positive Allosteric Modulators Provide In Vivo Efficacy without Potentiating mGlu5 Modulation of NMDAR Currents by Rook, Jerri M., Xiang, Zixiu, Lv, Xiaohui, Ghoshal, Ayan, Dickerson, Jonathan W., Bridges, Thomas M., Johnson, Kari A., Foster, Daniel J., Gregory, Karen J., Vinson, Paige N., Thompson, Analisa D., Byun, Nellie, Collier, Rebekah L., Bubser, Michael, Nedelcovych, Michael T., Gould, Robert W., Stauffer, Shaun R., Daniels, J. Scott, Niswender, Colleen M., Lavreysen, Hilde, Mackie, Claire, Conde-Ceide, Susana, Alcazar, Jesus, Bartolomé-Nebreda, José M., Macdonald, Gregor J., Talpos, John C., Steckler, Thomas, Jones, Carrie K., Lindsley, Craig W., Conn, P. Jeffrey

“…Schizophrenia is associated with disruptions in N-methyl-D-aspartate glutamate receptor subtype (NMDAR)-mediated excitatory synaptic signaling. The…”
Get full text

Preserved vascular integrity and enhanced survival following neuropilin-1 inhibition in a mouse model of CD8 T cell-initiated CNS vascular permeability by Suidan, Georgette L, Dickerson, Jonathan W, Johnson, Holly L, Chan, Theresa W, Pavelko, Kevin D, Pirko, Istvan, Seroogy, Kim B, Johnson, Aaron J

“…Altered permeability of the blood-brain barrier (BBB) is a feature of numerous neurological conditions including multiple sclerosis, cerebral malaria, viral…”
Get full text

M1-positive allosteric modulators lacking agonist activity provide the optimal profile for enhancing cognition by Moran, Sean P., Dickerson, Jonathan W., Cho, Hyekyung P., Xiang, Zixiu, Maksymetz, James, Remke, Daniel H., Lv, Xiaohui, Doyle, Catherine A., Rajan, Deepa H., Niswender, Colleen M., Engers, Darren W., Lindsley, Craig W., Rook, Jerri M., Conn, P. Jeffrey

“…Highly selective positive allosteric modulators (PAMs) of the M1 subtype of muscarinic acetylcholine receptor have emerged as an exciting new approach for…”
Get full text

M 1 -positive allosteric modulators lacking agonist activity provide the optimal profile for enhancing cognition by Moran, Sean P, Dickerson, Jonathan W, Cho, Hyekyung P, Xiang, Zixiu, Maksymetz, James, Remke, Daniel H, Lv, Xiaohui, Doyle, Catherine A, Rajan, Deepa H, Niswender, Colleen M, Engers, Darren W, Lindsley, Craig W, Rook, Jerri M, Conn, P Jeffrey

“…Highly selective positive allosteric modulators (PAMs) of the M subtype of muscarinic acetylcholine receptor have emerged as an exciting new approach for…”
Get full text

M1 muscarinic activation induces long-lasting increase in intrinsic excitability of striatal projection neurons by Lv, Xiaohui, Dickerson, Jonathan W., Rook, Jerri M., Lindsley, Craig W., Conn, P. Jeffrey, Xiang, Zixiu

“…The dorsolateral striatum is critically involved in movement control and motor learning. Striatal function is regulated by a variety of neuromodulators…”
Get full text

Development of a Selective and High Affinity Radioligand, [ 3 H]VU6013720, for the M 4 Muscarinic Receptor by Qi, Aidong, Kling, Haley E, Billard, Natasha, Rodriguez, Alice L, Peng, Li, Dickerson, Jonathan W, Engers, Julie L, Bender, Aaron M, Moehle, Mark S, Lindsley, Craig W, Rook, Jerri M, Niswender, Colleen M

“…M muscarinic receptors are highly expressed in the striatum and cortex, brain regions that are involved in diseases such as Parkinson's disease, schizophrenia,…”
Get full text

Synthesis and characterization of chiral 6-azaspiro[2.5]octanes as potent and selective antagonists of the M4 muscarinic acetylcholine receptor by Bender, Aaron M., Carter, Trever R., Spock, Matthew, Rodriguez, Alice L., Dickerson, Jonathan W., Rook, Jerri M., Chang, Sichen, Qi, Aidong, Presley, Christopher C., Engers, Darren W., Harp, Joel M., Bridges, Thomas M., Niswender, Colleen M., Conn, P. Jeffrey, Lindsley, Craig W.

“…[Display omitted] In this manuscript, we report a series of chiral 6-azaspiro[2.5]octanes and related spirocycles as highly potent and selective antagonists of…”
Get full text

Discovery and optimization of a novel CNS penetrant series of mGlu4 PAMs based on a 1,4-thiazepane core with in vivo efficacy in a preclinical Parkinsonian model by Kent, Caitlin N., Fulton, Mark G., Stillwell, Kaylee J., Dickerson, Jonathan W., Loch, Matthew T., Rodriguez, Alice L., Blobaum, Anna L., Boutaud, Olivier, Rook, Jerri L., Niswender, Colleen M., Conn, P. Jeffrey, Lindsley, Craig W.

“…[Display omitted] A high throughput screen (HTS) identified a novel, but weak (EC50 = 6.2 μM, 97% Glu Max) mGlu4 PAM chemotype based on a 1,4-thiazepane core,…”
Get full text

Discovery of VU6007496: Challenges in the Development of an M1 Positive Allosteric Modulator Backup Candidate by Engers, Julie L., Bollinger, Katrina A., Capstick, Rory A., Long, Madeline F., Bender, Aaron M., Dickerson, Jonathan W., Peng, Weimin, Presley, Christopher C., Cho, Hyekyung P., Rodriguez, Alice L., Niswender, Colleen M., Moran, Sean P., Xiang, Zixiu, Blobaum, Anna L., Boutaud, Olivier, Rook, Jerri M., Engers, Darren W., Conn, P. Jeffrey, Lindsley, Craig W.

“…Herein we report progress toward a backup clinical candidate to the M1 positive allosteric modulator (PAM) VU319/ACP-319. Scaffold-hopping from the…”
Get full text

Discovery of VU6007496: Challenges in the Development of an M 1 Positive Allosteric Modulator Backup Candidate by Engers, Julie L, Bollinger, Katrina A, Capstick, Rory A, Long, Madeline F, Bender, Aaron M, Dickerson, Jonathan W, Peng, Weimin, Presley, Christopher C, Cho, Hyekyung P, Rodriguez, Alice L, Niswender, Colleen M, Moran, Sean P, Xiang, Zixiu, Blobaum, Anna L, Boutaud, Olivier, Rook, Jerri M, Engers, Darren W, Conn, P Jeffrey, Lindsley, Craig W

“…Herein we report progress toward a backup clinical candidate to the M positive allosteric modulator (PAM) VU319/ACP-319. Scaffold-hopping from the pyrrolo[2,3-…”
Get full text

The metabotropic glutamate receptor 4-positive allosteric modulator VU0364770 produces efficacy alone and in combination with L-DOPA or an adenosine 2A antagonist in preclinical rodent models of Parkinson's disease by Jones, Carrie K, Bubser, Michael, Thompson, Analisa D, Dickerson, Jonathan W, Turle-Lorenzo, Nathalie, Amalric, Marianne, Blobaum, Anna L, Bridges, Thomas M, Morrison, Ryan D, Jadhav, Satyawan, Engers, Darren W, Italiano, Kimberly, Bode, Jacob, Daniels, J Scott, Lindsley, Craig W, Hopkins, Corey R, Conn, P Jeffrey, Niswender, Colleen M

“…Parkinson's disease (PD) is a debilitating neurodegenerative disorder associated with severe motor impairments caused by the loss of dopaminergic innervation…”
Get more information

A Novel M 1 PAM VU0486846 Exerts Efficacy in Cognition Models without Displaying Agonist Activity or Cholinergic Toxicity by Rook, Jerri M, Bertron, Jeanette L, Cho, Hyekyung P, Garcia-Barrantes, Pedro M, Moran, Sean P, Maksymetz, James T, Nance, Kellie D, Dickerson, Jonathan W, Remke, Daniel H, Chang, Sichen, Harp, Joel M, Blobaum, Anna L, Niswender, Colleen M, Jones, Carrie K, Stauffer, Shaun R, Conn, P Jeffrey, Lindsley, Craig W

“…Selective activation of the M subtype of muscarinic acetylcholine receptor, via positive allosteric modulation (PAM), is an exciting strategy to improve…”
Get full text

Co-Activation of Metabotropic Glutamate Receptor 3 and Beta-Adrenergic Receptors Modulates Cyclic-AMP and Long-Term Potentiation, and Disrupts Memory Reconsolidation by Walker, Adam G, Sheffler, Douglas J, Lewis, Andrew S, Dickerson, Jonathan W, Foster, Daniel J, Senter, Rebecca K, Moehle, Mark S, Lv, Xiaohui, Stansley, Branden J, Xiang, Zixiu, Rook, Jerri M, Emmitte, Kyle A, Lindsley, Craig W, Conn, P Jeffrey

“…Activation of β-adrenergic receptors (βARs) enhances both the induction of long-term potentiation (LTP) in hippocampal CA1 pyramidal cells and…”
Get full text

CD8 T Cell-Initiated Vascular Endothelial Growth Factor Expression Promotes Central Nervous System Vascular Permeability under Neuroinflammatory Conditions by Suidan, Georgette L, Dickerson, Jonathan W, Chen, Yi, McDole, Jeremiah R, Tripathi, Pulak, Pirko, Istvan, Seroogy, Kim B, Johnson, Aaron J

“…Dysregulation of the blood-brain barrier (BBB) is a hallmark feature of numerous neurologic disorders as diverse as multiple sclerosis, stroke, epilepsy, viral…”
Get full text

Discovery of VU6028418: A Highly Selective and Orally Bioavailable M 4 Muscarinic Acetylcholine Receptor Antagonist by Spock, Matthew, Carter, Trever R, Bollinger, Katrina A, Han, Changho, Baker, Logan A, Rodriguez, Alice L, Peng, Li, Dickerson, Jonathan W, Qi, Aidong, Rook, Jerri M, O'Neill, Jordan C, Watson, Katherine J, Chang, Sichen, Bridges, Thomas M, Engers, Julie L, Engers, Darren W, Niswender, Colleen M, Conn, P Jeffrey, Lindsley, Craig W, Bender, Aaron M

“…Herein, we report the SAR leading to the discovery of VU6028418, a potent M mAChR antagonist with high subtype-selectivity and attractive DMPK properties and…”
Get full text

Diverse Effects on M1 Signaling and Adverse Effect Liability within a Series of M1 Ago-PAMs by Rook, Jerri M, Abe, Masahito, Cho, Hyekyung P, Nance, Kellie D, Luscombe, Vincent B, Adams, Jeffrey J, Dickerson, Jonathan W, Remke, Daniel H, Garcia-Barrantes, Pedro M, Engers, Darren W, Engers, Julie L, Chang, Sichen, Foster, Jarrett J, Blobaum, Anna L, Niswender, Colleen M, Jones, Carrie K, Conn, P. Jeffrey, Lindsley, Craig W

“…Both historical clinical and recent preclinical data suggest that the M1 muscarinic acetylcholine receptor is an exciting target for the treatment of…”
Get full text

Development of a Peripherally Restricted 5-HT2B Partial Agonist for Treatment of Pulmonary Arterial Hypertension by Valentine, Michael S., Bender, Aaron M., Shay, Sheila, Paffenroth, Krista C., Gladson, Santhi, Dickerson, Jonathan W., Watson, Katherine J., Kapolka, Nicholas J., Boutaud, Olivier, Rook, Jerri M., Blackwell, Timothy S., Roth, Bryan L., Harrison, Fiona E., Austin, Eric D., West, James D., Lindsley, Craig W., Merryman, W. David

“…Ligands for the serotonin 2B receptor (5-HT2B) have shown potential to treat pulmonary arterial hypertension in preclinical models but cannot be used in humans…”
Get full text

Role of mGlu5 Receptors and Inhibitory Neurotransmission in M1 Dependent Muscarinic LTD in the Prefrontal Cortex: Implications in Schizophrenia by Ghoshal, Ayan, Moran, Sean P, Dickerson, Jonathan W, Joffe, Max E, Grueter, Brad A, Xiang, Zixiu, Lindsley, Craig W, Rook, Jerri M, Conn, P. Jeffrey

“…Selective potentiation of the mGlu5 subtype of metabotropic glutamate (mGlu) receptor using positive allosteric modulators (PAMs) has robust…”
Get full text