Search Results - "Gruner, John"

Correlation between ex vivo receptor occupancy and wake-promoting activity of selective H3 receptor antagonists by Le, Siyuan, Gruner, John A, Mathiasen, Joanne R, Marino, Michael J, Schaffhauser, Hervé

“…The histamine H3 receptor (H3R) modulates the release of neurotransmitters that are involved in vigilance, cognition, and sleep-wake regulation. H3R antagonism…”
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3-(1′-Cyclobutylspiro[4H-1,3-benzodioxine-2,4′-piperidine]-6-yl)-5,5-dimethyl-1,4-dihydropyridazin-6-one (CEP-32215), a new wake-promoting histamine H3 antagonist/inverse agonist by Hudkins, Robert L., Gruner, John A., Raddatz, Rita, Mathiasen, Joanne R., Aimone, Lisa D., Marino, Michael J., Bacon, Edward R., Williams, Michael, Ator, Mark A.

“…CEP-32215 is a new, potent, selective, and orally bioavailable inverse agonist of the histamine H3 receptor (H3R) with drug-like properties. High affinity in…”
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The Roles of Dopamine Transport Inhibition and Dopamine Release Facilitation in Wake Enhancement and Rebound Hypersomnolence Induced by Dopaminergic Agents by GRUNER, John A, MARCY, Val R, LIN, Yin-Guo, BOZYCZKO-COYNE, Donna, MARINO, Michael J, GASIOR, Maciej

“…Rebound hypersomnolence (RHS: increased sleep following increased wake) is a limiting side-effect of many wake-promoting agents. In particular, RHS in the…”
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3,4-Diaza-bicyclo[4.1.0]hept-4-en-2-one phenoxypropylamine analogs of irdabisant (CEP-26401) as potent histamine-3 receptor inverse agonists with robust wake-promoting activity by Hudkins, Robert L., Becknell, Nadine C., Lyons, Jacquelyn A., Aimone, Lisa D., Olsen, Mark, Haltiwanger, R. Curtis, Mathiasen, Joanne R., Raddatz, Rita, Gruner, John A.

“…A novel series of 3,4-diaza-bicyclo[4.1.0]hept-4-en-2-ones were designed and synthesized as H3R analogs of irdabisant 6. Separation of the isomers, assignment…”
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Characterization of pharmacological and wake-promoting properties of the dopaminergic stimulant sydnocarb in rats by Gruner, John A, Mathiasen, Joanne R, Flood, Dorothy G, Gasior, Maciej

“…Sydnocarb is a psychomotor stimulant structurally similar to d-amphetamine (D-AMPH) and is used in Russia for the treatment of a variety of neuropsychiatric…”
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Substituted phenoxypropyl-(R)-2-methylpyrrolidine aminomethyl ketones as histamine-3 receptor inverse agonists by Zulli, Allison L., Aimone, Lisa D., Mathiasen, Joanne R., Gruner, John A., Raddatz, Rita, Bacon, Edward R., Hudkins, Robert L.

“…Optimization of a series of aminomethyl ketone diamine H3R antagonists to reduce the brain exposure by lowering the pKa, led to molecules with improved…”
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Synthesis and evaluation of 4- and 5-pyridazin-3-one phenoxypropylamine analogues as histamine-3 receptor antagonists by Becknell, Nadine C., Lyons, Jacquelyn A., Aimone, Lisa D., Huang, Zeqi, Gruner, John A., Raddatz, Rita, Hudkins, Robert L.

“…A novel series of 4-pyridazin-3-one and 5-pyridazin-3-one analogues were designed and synthesized as H3R antagonists. Structure–activity relationship revealed…”
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Wake promoting agents: Search for next generation modafinil, lessons learned: Part III by Dunn, Derek, Hostetler, Greg, Iqbal, Mohamed, Marcy, Val R., Lin, Yin Guo, Jones, Bruce, Aimone, Lisa D., Gruner, John, Ator, Mark A., Bacon, Edward R., Chatterjee, Sankar

“…In searching for a next generation molecule to the novel wake promoting agent modafinil (compound 1), a series of fluorene-derived wakefulness enhancing agents…”
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4-Phenoxypiperidine pyridazin-3-one histamine H3 receptor inverse agonists demonstrating potent and robust wake promoting activity by Hudkins, Robert L., Zulli, Allison L., Dandu, Reddeppa reddy, Tao, Ming, Josef, Kurt A., Aimone, Lisa D., Curtis Haltiwanger, R., Huang, Zeqi, Lyons, Jacquelyn A., Mathiasen, Joanne R., Raddatz, Rita, Gruner, John A.

“…Structure–activity relationships for a series of phenoxypiperidine pyridazin-3-one H3R antagonists/inverse agonists are disclosed. The search for compounds…”
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Novel morpholine ketone analogs as potent histamine H3 receptor inverse agonists with wake activity by Sundar, Babu G., Bailey, Thomas R., Dunn, Derek, Hostetler, Greg A., Chatterjee, Sankar, Bacon, Edward R., Yue, Christoph, Schweizer, Dominique, Aimone, Lisa D., Gruner, John A., Lyons, Jacquelyn, Raddatz, Rita, Lesur, Brigitte

“…Structure–activity relationship on a novel ketone class of H3R antagonists/inverse agonists is disclosed. Compound 4 showed excellent target potency,…”
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Synthesis and structure–activity relationship of 5-pyridazin-3-one phenoxypiperidines as potent, selective histamine H3 receptor inverse agonists by Tao, Ming, Aimone, Lisa D., Gruner, John A., Mathiasen, Joanne R., Huang, Zeqi, Lyons, Jacquelyn, Raddatz, Rita, Hudkins, Robert L.

“…Optimization of the R2 and R6 positions of (5-{4-[3-(R)-2-methylpyrrolin-1-yl-propoxy]phenyl}-2H-pyridazin-3-one) 2a with constrained phenoxypiperidines led to…”
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Synthesis and evaluation of pyridone-phenoxypropyl-R-2-methylpyrrolidine analogues as histamine H₃ receptor antagonists by Becknell, Nadine C, Lyons, Jacquelyn A, Aimone, Lisa D, Gruner, John A, Mathiasen, Joanne R, Raddatz, Rita, Hudkins, Robert L

“…6-{4-[3-(R)-2-Methylpyrrolidin-1-yl)propoxy]-phenyl}-2H-pyridazin-3-one 6 (Irdabisant; CEP-26401) was recently reported as a potent H₃R antagonist with…”
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Armodafinil promotes wakefulness and activates Fos in rat brain by Fiocchi, Elaine M., Lin, Yin-Guo, Aimone, Lisa, Gruner, John A., Flood, Dorothy G.

“…Modafinil increases waking and labeling of Fos, a marker of neuronal activation. In the present study, armodafinil, the R-enantiomer of racemic modafinil, was…”
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4,5-Dihydropyridazin-3-one derivatives as histamine H3 receptor inverse agonists by Hudkins, Robert L., Aimone, Lisa D., Dandu, Reddeppa reddy, Dunn, Derek, Gruner, John A., Huang, Zeqi, Josef, Kurt A., Lyons, Jacquelyn A., Mathiasen, Joanne R., Tao, Ming, Zulli, Allison L., Raddatz, Rita

“…H3R structure–activity relationships for a new class of 4,5-dihydropyridazin-3-one H3R antagonists/inverse agonists are disclosed. Modification of the…”
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Synthesis and evaluation of pyridazinone–phenethylamine derivatives as selective and orally bioavailable histamine H₃ receptor antagonists with robust wake-promoting activity by Dandu, Reddeppa reddy, Gruner, John A, Mathiasen, Joanne R, Aimone, Lisa D, Hostetler, Greg, Benfield, Caitlyn, Bendesky, Robert J, Marcy, Val R, Raddatz, Rita, Hudkins, Robert L

“…A series of pyridazinone–phenethylamine derivatives with moderate to low nanomolar affinity for rat and human H₃R are described. These analogs exhibited…”
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Identification of pyridazin-3-one derivatives as potent, selective histamine H3 receptor inverse agonists with robust wake activity by Hudkins, Robert L., Aimone, Lisa D., Bailey, Thomas R., Bendesky, Robert J., Dandu, Reddeppa reddy, Dunn, Derek, Gruner, John A., Josef, Kurt A., Lin, Yin-Guo, Lyons, Jacquelyn, Marcy, Val R., Mathiasen, Joanne R., Sundar, Babu G., Tao, Ming, Zulli, Allison L., Raddatz, Rita, Bacon, Edward R.

“…H3R structure–activity relationships on a novel class of pyridazin-3-one H3R antagonists/inverse agonists are disclosed. Modifications of the pyridazinone…”
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Discovery of (1R,6S)-5-[4-(1-cyclobutyl-piperidin-4-yloxy)-phenyl]-3,4-diaza-bicyclo[4.1.0]hept-4-en-2-one (R,S-4a): Histamine H3 receptor inverse agonist demonstrating potent cognitive enhancing and wake promoting activity by Hudkins, Robert L., Josef, Kurt A., Becknell, Nadine C., Aimone, Lisa D., Lyons, Jacquelyn A., Mathiasen, Joanne R., Gruner, John A., Raddatz, Rita

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Hindlimb Motor Neurons Require Cu/Zn Superoxide Dismutase for Maintenance of Neuromuscular Junctions by Flood, Dorothy G., Reaume, Andrew G., Gruner, John A., Hoffman, Eric K., Hirsch, James D., Lin, Yin-Guo, Dorfman, Karen S., Scott, Richard W.

“…The role of oxidative damage in neurodegenerative disease was investigated in mice lacking cytoplasmic Cu/Zn superoxide dismutase (SOD), created by deletion of…”
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A monitored contusion model of spinal cord injury in the rat by Gruner, J A

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Long-term survival and outgrowth of mechanically engineered nervous tissue constructs implanted into spinal cord lesions by Iwata, Akira, Browne, Kevin D, Pfister, Bryan J, Gruner, John A, Smith, Douglas H

“…While most approaches to repair spinal cord injury (SCI) rely on promoting axon outgrowth, the extensive distance that axons would have to grow to bridge SCI…”
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