Search Results - "Schetz, John A"

Synthesis and structure–affinity relationships of novel small molecule natural product derivatives capable of discriminating between serotonin 5-HT1A, 5-HT2A, 5-HT2C receptor subtypes by Cummings, David F., Canseco, Diana C., Sheth, Pratikkumar, Johnson, James E., Schetz, John A.

“…Efforts to develop ligands that distinguish between clinically relevant 5-HT2A and 5-HT2C serotonin receptor subtypes have been challenging, because their…”
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Neuronal ablation of p-Akt at Ser473 leads to altered 5-HT1A/2A receptor function by Saunders, Christine, Siuta, Michael, Robertson, Sabrina D., Davis, Adeola R., Sauer, Jennifer, Matthies, Heinrich J.G., Gresch, Paul J., Airey, David C., Lindsley, Craig W., Schetz, John A., Niswender, Kevin D., Veenstra-Vanderweele, Jeremy M., Galli, Aurelio

“…•Neuronal insulin regulates central monoamine homeostasis via down-stream kinase Akt.•Neuronal ablation of p-Akt at Ser473 increases cortical 5-HT1A and -2A…”
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Adverse Neuropsychiatric Events and Recreational Use of Efavirenz and Other HIV-1 Antiretroviral Drugs by Dalwadi, Dhwanil A, Ozuna, Luis, Harvey, Brian H, Viljoen, Michelle, Schetz, John A

“…Efavirenz is a highly effective HIV-1 antiretroviral; however, it is also frequently associated with neuropsychiatric adverse events (NPAE) that include…”
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Three amino acids in the D₂ dopamine receptor regulate selective ligand function and affinity by Cummings, David F, Ericksen, Spencer S, Schetz, John A

“…The D₂ dopamine receptor is an important therapeutic target for the treatment of psychotic, agitated, and abnormal behavioral states. To better understand the…”
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Design, Synthesis, Radiolabeling, and in Vivo Evaluation of Carbon-11 Labeled N-[2-[4-(3-Cyanopyridin-2-yl)piperazin-1-yl]ethyl]-3-methoxybenzamide, a Potential Positron Emission Tomography Tracer for the Dopamine D4 Receptors by Lacivita, Enza, De Giorgio, Paola, Lee, Irene T, Rodeheaver, Sean I, Weiss, Bryan A, Fracasso, Claudia, Caccia, Silvio, Berardi, Francesco, Perrone, Roberto, Zhang, Ming-Rong, Maeda, Jun, Higuchi, Makoto, Suhara, Tetsuya, Schetz, John A, Leopoldo, Marcello

“…Here we describe the design, synthesis, and evaluation of physicochemical and pharmacological properties of D4 dopamine receptor ligands related to…”
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Activation of the sigma-1 receptor by haloperidol metabolites facilitates brain-derived neurotrophic factor secretion from human astroglia by Dalwadi, Dhwanil A., Kim, Seongcheol, Schetz, John A.

“…Glial cells play a critical role in neuronal support which includes the production and release of the neurotrophin brain-derived neurotrophic factor (BDNF)…”
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Treatment of Stroke at a Delayed Timepoint with a Repurposed Drug Targeting Sigma 1 Receptors by Schreihofer, Derek A., Dalwadi, Dhwanil, Kim, Seongcheol, Metzger, Daniel, Oppong-Gyebi, Anthony, Das-Earl, Paromita, Schetz, John A.

“…Sigma 1 receptors are intracellular chaperone proteins that have been explored as a subacute treatment to enhance post-stroke recovery. We recently identified…”
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Certain 1,4-disubstituted aromatic piperidines and piperazines with extreme selectivity for the dopamine D4 receptor interact with a common receptor microdomain by Kortagere, Sandhya, Gmeiner, Peter, Weinstein, Harel, Schetz, John A

“…We previously demonstrated that, in the D4 dopamine receptor, the aromatic microdomain that spans the interface of the second and third transmembrane segments…”
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Comparative Exploration of the Structure-Activity Space of Cloned α -Like Octopamine Receptors from a Marine and a Terrestrial Arthropod by Dalwadi, Dhwanil A, Schetz, John A

“…The -like octopamine receptors (OctR) are believed to be the evolutionary precursor to the vertebrate -adrenergic receptors ( -ARs) based upon sequence…”
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New Antiinfective and Human 5-HT2 Receptor Binding Natural and Semisynthetic Compounds from the Jamaican Sponge Smenospongia aurea by HU, Jin-Feng, SCHETZ, John A., KELLY, Michelle, PENG, Jiang-Nan, ANG, Kenny K. H., FLOTOW, Horst, LEONG, Chung Yan, NG, Siew Bee, BUSS, Antony D., WILKINS, Scott P., HAMANN, Mark T.

“…In addition to the sesquiterpene-phenol aureols (1), 6'-chloroaureol (2), and aureol acetate (3), eight indole alkaloids including the new…”
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The dual modulatory effects of efavirenz on GABAA receptors are mediated via two distinct sites by Huang, Renqi, Chen, Zhenglan, Dolan, Sean, Schetz, John A., Dillon, Glenn H.

“…Efavirenz is a widely prescribed medicine used to treat type 1 human immunodeficiency virus (HIV-1), the most prevalent pathogenic strain of the virus…”
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The dual modulatory effects of efavirenz on GABA A receptors are mediated via two distinct sites by Huang, Renqi, Chen, Zhenglan, Dolan, Sean, Schetz, John A, Dillon, Glenn H

“…Efavirenz is a widely prescribed medicine used to treat type 1 human immunodeficiency virus (HIV-1), the most prevalent pathogenic strain of the virus…”
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The HIV Antiretroviral Drug Efavirenz has LSD-Like Properties by GATCH, Michael B, KOZLENKOV, Alexey, SCHETZ, John A, HUANG, Ren-Qi, WENJUAN YANG, NGUYEN, Jacques D, GONZALEZ-MAESO, Javier, RICE, Kenner C, FRANCE, Charles P, DILLON, Glenn H, FORSTER, Michael J

“…Anecdotal reports have surfaced concerning misuse of the HIV antiretroviral medication efavirenz…”
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Ligand selectivity of D2 dopamine receptors is modulated by changes in local dynamics produced by sodium binding by Ericksen, Spencer S, Cummings, David F, Weinstein, Harel, Schetz, John A

“…We have uncovered a significant allosteric response of the D(2) dopamine receptor to physiologically relevant concentrations of sodium (140 mM), characterized…”
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Molecular mechanisms of serotonergic action of the HIV-1 antiretroviral efavirenz by Dalwadi, Dhwanil A., Kim, Seongcheol, Amdani, Shahnawaz M., Chen, Zhenglan, Huang, Ren-Qi, Schetz, John A.

“…[Display omitted] Efavirenz is highly effective at suppressing HIV-1, and the WHO guidelines list it as a component of the first-line antiretroviral (ARV)…”
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Transmembrane segment five serines of the D4 dopamine receptor uniquely influence the interactions of dopamine, norepinephrine, and Ro10-4548 by Cummings, David F, Ericksen, Spencer S, Goetz, Angela, Schetz, John A

“…Conserved serines of transmembrane segment (TM) five (TM5) are critical for the interactions of endogenous catecholamines with alpha(1)- and…”
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Ring substituents on substituted benzamide ligands indirectly mediate interactions with position 7.39 of transmembrane helix 7 of the D4 dopamine receptor by Ericksen, Spencer S, Cummings, David F, Teer, Michael E, Amdani, Shahnawaz, Schetz, John A

“…In an effort to delineate how specific molecular interactions of dopamine receptor ligand classes vary between D2-like dopamine receptor subtypes, a conserved…”
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An unambiguous assay for the cloned human sigma1 receptor reveals high affinity interactions with dopamine D4 receptor selective compounds and a distinct structure-affinity relationship for butyrophenones by LEE, Ivan T, CHEN, Shiuhwei, SCHETZ, John A

“…The ability of the sigma(1) receptor to interact with a huge range of drug structural classes coupled with its wide distribution in the body has contributed to…”
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A prototypical Sigma-1 receptor antagonist protects against brain ischemia by Schetz, John A, Perez, Evelyn, Liu, Ran, Chen, Shiuhwei, Lee, Ivan, Simpkins, James W

“…Abstract Previous studies indicate that the Sigma-1 ligand 4-phenyl-1-(4-phenylbutyl) piperidine (PPBP) protects the brain from ischemia. Less clear is whether…”
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Interactions of the Novel Antipsychotic Aripiprazole (OPC-14597) with Dopamine and Serotonin Receptor Subtypes by Lawler, Cindy P, Prioleau, Cassandra, Lewis, Mechelle M, Mak, Chun, Jiang, Dong, Schetz, John A, Gonzalez, Antonio M, Sibley, David R, Mailman, Richard B

“…OPC-14597 {aripiprazole; 7-(4-(4-(2,3-dichlorophenyl)-1-piperazinyl)butyloxy)-3,4-dihydro-2(1H)-quinolinone} is a novel candidate antipsychotic that has high…”
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