Search Results - "Marek, Gerard J"

When is a Proof-of-Concept (POC) not a POC? Pomaglumetad (LY2140023) as a Case Study for Antipsychotic Efficacy by Marek, Gerard J

“…Pomaglumetad methionil (LY2140023) is a mGlu2/3 receptor agonist prodrug reported in 2007 to possess antipsychotic efficacy based on results of a phase 2 trial…”
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Glutamatergic (N-methyl-D-aspartate receptor) hypofrontality in schizophrenia: too little juice or a miswired brain? by Marek, Gerard J, Behl, Berthold, Bespalov, Anton Y, Gross, Gerhard, Lee, Younglim, Schoemaker, Hans

“…Dopamine D2 receptor blockade has been an obligate mechanism of action present in all medications that effectively treat positive symptoms of schizophrenia…”
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CNS distribution of metabotropic glutamate 2 and 3 receptors: Transgenic mice and [3H]LY459477 autoradiography by Wright, Rebecca A., Johnson, Bryan G., Zhang, Ce, Salhoff, Craig, Kingston, Ann E., Calligaro, David O., Monn, James A., Schoepp, Darryle D., Marek, Gerard J.

“…Group II metabotropic glutamate (mGlu) receptor agonists were efficacious in randomized clinical research trials for schizophrenia and generalized anxiety…”
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Default-mode-like network activation in awake rodents by Upadhyay, Jaymin, Baker, Scott J, Chandran, Prasant, Miller, Loan, Lee, Younglim, Marek, Gerard J, Sakoglu, Unal, Chin, Chih-Liang, Luo, Feng, Fox, Gerard B, Day, Mark

“…During wakefulness and in absence of performing tasks or sensory processing, the default-mode network (DMN), an intrinsic central nervous system (CNS) network,…”
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Safety, Pharmacokinetics, and Pharmacodynamics of ASP3662, a Novel 11β‐Hydroxysteroid Dehydrogenase Type 1 Inhibitor, in Healthy Young and Elderly Subjects by Bellaire, Susan, Walzer, Mark, Wang, Tianli, Krauwinkel, Walter, Yuan, Nancy, Marek, Gerard J.

“…Inhibition of the enzyme 11β‐hydroxysteroid dehydrogenase type 1 (11β‐HSD1) represents a potential mechanism for improving pain conditions. ASP3662 is a potent…”
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β2-Adrenergic Receptor Activation Suppresses the Rat Phenethylamine Hallucinogen-Induced Head Twitch Response: Hallucinogen-Induced Excitatory Post-synaptic Potentials as a Potential Substrate by Marek, Gerard J., Ramos, Brian P.

“…5-Hydroxytryptamine2A (5-HT2A) receptors are enriched in layers I and Va of the rat prefrontal cortex and neocortex and their activation increases the…”
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Efficacy and safety evaluation of HSD-1 inhibitor ABT-384 in Alzheimer's disease by Marek, Gerard J, Katz, David A, Meier, Andreas, Greco, Nicholas, Zhang, Wuyan, Liu, Wei, Lenz, Robert A

“…Abstract Background In this study we assessed increased cortisol in Alzheimer's disease (AD) patients. The selective 11-β-hydroxysteroid dehydrogenase type 1…”
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Awake rat pharmacological magnetic resonance imaging as a translational pharmacodynamic biomarker: metabotropic glutamate 2/3 agonist modulation of ketamine-induced blood oxygenation level dependence signals by Chin, Chih-Liang, Upadhyay, Jaymin, Marek, Gerard J, Baker, Scott J, Zhang, Min, Mezler, Mario, Fox, Gerard B, Day, Mark

“…Neuroimaging techniques have been exploited to characterize the effect of N-methyl-d-aspartate (NMDA) receptor antagonists on brain activation in humans and…”
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The selective 5-HT2A receptor antagonist M100907 enhances antidepressant-like behavioral effects of the SSRI fluoxetine by Marek, Gerard J, Martin-Ruiz, Raul, Abo, Allyson, Artigas, Francesc

“…The addition of low doses of atypical antipsychotic drugs, which saturate 5-HT(2A) receptors, enhances the therapeutic effect of selective serotonin…”
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Metabotropic Glutamate2 Receptors Play a Key Role in Modulating Head Twitches Induced by a Serotonergic Hallucinogen in Mice by Benvenga, Mark J., Chaney, Stephen F., Baez, Melvyn, Britton, Thomas C., Hornback, William J., Monn, James A., Marek, Gerard J.

“…There is substantial evidence that glutamate can modulate the effects of 5-hydroxytryptamine 2A (5-HT 2A ) receptor activation through stimulation of…”
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Synergistic action of 5-HT2A antagonists and selective serotonin reuptake inhibitors in neuropsychiatric disorders by MAREK, Gerard J, CARPENTER, Linda L, MCDOUGLE, Christopher J, PRICE, Lawrence H

“…Recently, the addition of drugs with prominent 5-HT(2) receptor antagonist properties (risperidone, olanzapine, mirtazapine, and mianserin) to selective…”
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Serotonin and dopamine interactions in rodents and primates: implications for psychosis and antipsychotic drug development by Marek, Gerard J

“…Since the late 1950s, appreciation of dopamine receptor blockade has played a primary role in understanding the mechanism underlying the therapeutic effects of…”
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Pharmacological and pharmacokinetic properties of a structurally novel, potent, and selective metabotropic glutamate 2/3 receptor agonist: in vitro characterization of agonist (-)-(1R,4S,5S,6S)-4-amino-2-sulfonylbicyclo[3.1.0]-hexane-4,6-dicarboxylic acid (LY404039) by Rorick-Kehn, Linda M, Johnson, Bryan G, Burkey, Jennifer L, Wright, Rebecca A, Calligaro, David O, Marek, Gerard J, Nisenbaum, Eric S, Catlow, John T, Kingston, Ann E, Giera, Deborah D, Herin, Marc F, Monn, James A, McKinzie, David L, Schoepp, Darryle D

“…Group II metabotropic glutamate (mGlu) receptor agonists, including (1S,2S,5R,6S)-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylate monohydrate (LY354740) and…”
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Group III metabotropic glutamate receptor agonists selectively suppress excitatory synaptic currents in the rat prefrontal cortex induced by 5-hydroxytryptamine2A receptor activation by Zhang, Ce, Marek, Gerard J

“…Activation and blockade of prefrontal cortical 5-hydroxytryptamine2A (5-HT2A) receptors have been linked to the action of hallucinogenic and…”
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Xanomeline modulation of the blood oxygenation level-dependent signal in awake rats: development of pharmacological magnetic resonance imaging as a translatable pharmacodynamic biomarker for central activity and dose selection by Baker, Scott, Chin, Chih-Liang, Basso, Ana M, Fox, Gerard B, Marek, Gerard J, Day, Mark

“…In vivo translational imaging techniques, such as positron emission tomography and single-photon emission-computed tomography, are the only ways to adequately…”
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In vitro and in vivo evidence for a lack of interaction with dopamine D2 receptors by the metabotropic glutamate 2/3 receptor agonists 1S,2S,5R,6S-2-aminobicyclo[3.1.0]hexane-2,6-bicaroxylate monohydrate (LY354740) and (-)-2-oxa-4-aminobicyclo[3.1.0] Hexane-4,6-dicarboxylic acid (LY379268) by Fell, Matthew J, Perry, Kenneth W, Falcone, Julie F, Johnson, Bryan G, Barth, Vanessa N, Rash, Karen S, Lucaites, Virginia L, Threlkeld, Penny G, Monn, James A, McKinzie, David L, Marek, Gerard J, Svensson, Kjell A, Nelson, David L

“…Some recently published in vitro studies with two metabotropic glutamate 2/3 receptor (mGluR(2/3)) agonists [(-)-2-oxa-4-aminobicyclo[3.1.0]…”
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Extending the Specificity of DRL 72-s Behavior for Screening Antidepressant-Like Effects of Glutamatergic Clinically Validated Anxiolytic or Antidepressant Drugs in Rats by Marek, Gerard J., Salek, Allyson A.

“…Both an agonist and its associated prodrug for metabotropic glutamate 2/3 (mGlu 2/3 ) receptors demonstrated anxiolytic efficacy in large, randomized,…”
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Metabotropic glutamate2/3 (mGlu2/3) receptors, schizophrenia and cognition by Marek, Gerard J

“…Recently, a metabotropic glutamate(2/3) (mGlu(2/3)) receptor agonist prodrug was found to improve both the positive and negative symptoms of schizophrenic…”
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A randomized phase 1 single-dose polysomnography study of ASP8062, a GABAB receptor positive allosteric modulator by Walzer, Mark, Wu, Ruishan, Ahmad, Maha, Freeman, Jon, Zammit, Gary, Marek, Gerard J.

“…Rationale Previous research suggests that sleep polysomnography and EEG endpoints can be used to assess GABAergic activity; however, the impact of GABA B…”
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Phase 1 randomized study on the safety, tolerability, and pharmacodynamic cognitive and electrophysiological effects of a dopamine D 1 receptor positive allosteric modulator in patients with schizophrenia by Desai, Amit, Benner, Lauren, Wu, Ruishan, Gertsik, Lev, Maruff, Paul, Light, Gregory A, Uz, Tolga, Marek, Gerard J, Zhu, Tong

“…ASP4345, a novel dopamine D receptor positive allosteric modulator, is being evaluated for the treatment of cognitive impairment associated with schizophrenia…”
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