Search Results - "Pieschl, Rick L."

Effects of BMS-902483, an α7 nicotinic acetylcholine receptor partial agonist, on cognition and sensory gating in relation to receptor occupancy in rodents by Pieschl, Rick L., Miller, Regina, Jones, Kelli M., Post-Munson, Debra J., Chen, Ping, Newberry, Kimberly, Benitex, Yulia, Molski, Thaddeus, Morgan, Daniel, McDonald, Ivar M., Macor, John E., Olson, Richard E., Asaka, Yukiko, Digavalli, Siva, Easton, Amy, Herrington, James, Westphal, Ryan S., Lodge, Nicholas J., Zaczek, Robert, Bristow, Linda J., Li, Yu-Wen

“…The α7 nicotinic acetylcholine receptor is thought to play an important role in human cognition. Here we describe the in vivo effects of BMS-902483, a…”
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Characterization of the adrenocorticotrophic hormone - induced mouse model of resistance to antidepressant drug treatment by Srikumar, Bettadapura N., Paschapur, Mahesh, Kalidindi, Narasimharaju, Adepu, Bharath, Das, Manish L., Sreedhara, Muppana V., Kuchibhotla, Vijaya K., Pieschl, Rick L., Li, Yu-Wen, Ega, Durga Shiva Prasad, Louis, Justin V., Murugesan, Senthilkumar, Naidu, Pattipati S., Ramarao, Manjunath, Bristow, Linda J., Vikramadithyan, Reeba K.

“…Approximately 30–60% of patients treated with existing antidepressants fail to achieve remission of depressive symptoms leading to Treatment Resistant…”
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Molecular Dissection of Two Distinct Actions of Melatonin on the Suprachiasmatic Circadian Clock by Liu, Chen, Weaver, David R, Jin, Xiaowei, Shearman, Lauren P, Pieschl, Rick L, Gribkoff, Valentin K, Reppert, Steven M

“…The pineal hormone melatonin elicits two effects on the suprachiasmatic nuclei (SCN): acute neuronal inhibition and phase-shifting. Melatonin evokes its…”
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GABA Receptor-Mediated Inhibition of Neuronal Activity in Rat SCN In Vitro: Pharmacology and Influence of Circadian Phase by Gribkoff, Valentin K, Pieschl, Rick L, Dudek, F. Edward

“…1 Neuroscience Drug Discovery, Bristol-Myers Squibb Pharmaceutical Research Institute, Wallingford, Connecticut 06492 2 Department of Anatomy and Neurobiology,…”
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Discovery of Indole- and Indazole-acylsulfonamides as Potent and Selective NaV1.7 Inhibitors for the Treatment of Pain by Luo, Guanglin, Chen, Ling, Easton, Amy, Newton, Amy, Bourin, Clotilde, Shields, Eric, Mosure, Kathy, Soars, Matthew G, Knox, Ronald J, Matchett, Michele, Pieschl, Rick L, Post-Munson, Debra J, Wang, Shuya, Herrington, James, Graef, John, Newberry, Kimberly, Sivarao, Digavalli V, Senapati, Arun, Bristow, Linda J, Meanwell, Nicholas A, Thompson, Lorin A, Dzierba, Carolyn

“…3-Aryl-indole and 3-aryl-indazole derivatives were identified as potent and selective Nav1.7 inhibitors. Compound 29 was shown to be efficacious in the mouse…”
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Development of New Benzenesulfonamides As Potent and Selective Nav1.7 Inhibitors for the Treatment of Pain by Wu, Yong-Jin, Guernon, Jason, Shi, Jianliang, Ditta, Jonathan, Robbins, Kevin J, Rajamani, Ramkumar, Easton, Amy, Newton, Amy, Bourin, Clotilde, Mosure, Kathleen, Soars, Matthew G, Knox, Ronald J, Matchett, Michele, Pieschl, Rick L, Post-Munson, Debra J, Wang, Shuya, Herrington, James, Graef, John, Newberry, Kimberly, Bristow, Linda J, Meanwell, Nicholas A, Olson, Richard, Thompson, Lorin A, Dzierba, Carolyn

“…By taking advantage of certain features in piperidine 4, we developed a novel series of cyclohexylamine- and piperidine-based benzenesulfonamides as potent and…”
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Discovery of morpholine-based aryl sulfonamides as Nav1.7 inhibitors by Wu, Yong-Jin, Guernon, Jason, McClure, Andrea, Venables, Brian, Rajamani, Ramkumar, Robbins, Kevin J., Knox, Ronald J., Matchett, Michele, Pieschl, Rick L., Herrington, James, Bristow, Linda J., Meanwell, Nicholas A., Olson, Richard, Thompson, Lorin A., Dzierba, Carolyn

“…[Display omitted] Replacement of the piperidine ring in the lead benzenesulfonamide Nav1.7 inhibitor 1 with a weakly basic morpholine core resulted in a…”
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Phase Shifting of Circadian Rhythms and Depression of Neuronal Activity in the Rat Suprachiasmatic Nucleus by Neuropeptide Y: Mediation by Different Receptor Subtypes by Gribkoff, Valentin K, Pieschl, Rick L, Wisialowski, Todd A, van den Pol, Anthony N, Yocca, Frank D

“…Neuropeptide Y (NPY) has been implicated in the phase shifting of circadian rhythms in the hypothalamic suprachiasmatic nucleus (SCN). Using long-term,…”
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Discovery of new indole-based acylsulfonamide Nav1.7 inhibitors by Wu, Yong-Jin, Venables, Brian, Guernon, Jason, Chen, Jie, Sit, Sing-Yuen, Rajamani, Ramkumar, Knox, Ronald J., Matchett, Michele, Pieschl, Rick L., Herrington, James, Bristow, Linda J., Meanwell, Nicholas A., Thompson, Lorin A., Dzierba, Carolyn

“…[Display omitted] Screening of 100 acylsulfonamides from the Bristol-Myers Squibb compound collection identified the C3-cyclohexyl indole 6 as a potent Nav1.7…”
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Targeted Disruption of the Mouse Mel1b Melatonin Receptor by Jin, Xiaowei, von Gall, Charlotte, Pieschl, Rick L., Gribkoff, Valentin K., Stehle, Jorg H., Reppert, Steven M., Weaver, David R.

“…Article Usage Stats Services MCB Citing Articles Google Scholar PubMed Related Content Social Bookmarking CiteULike Delicious Digg Facebook Google+ Mendeley…”
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Correction to Discovery of Indole- and Indazole-acylsulfonamides as Potent and Selective Na V 1.7 Inhibitors for the Treatment of Pain by Luo, Guanglin, Chen, Ling, Easton, Amy, Newton, Amy, Bourin, Clotilde, Shields, Eric, Mosure, Kathy, Soars, Matthew G, Knox, Ronald J, Matchett, Michele, Pieschl, Rick L, Post-Munson, Debra J, Wang, Shuya, Herrington, James, Graef, John, Newberry, Kimberly, Sivarao, Digavalli V, Senapati, Arun, Bristow, Linda J, Meanwell, Nicholas A, Thompson, Lorin A, Dzierba, Carolyn

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Discovery of Indole- and Indazole-acylsulfonamides as Potent and Selective Na V 1.7 Inhibitors for the Treatment of Pain by Luo, Guanglin, Chen, Ling, Easton, Amy, Newton, Amy, Bourin, Clotilde, Shields, Eric, Mosure, Kathy, Soars, Matthew G, Knox, Ronald J, Matchett, Michele, Pieschl, Rick L, Post-Munson, Debra J, Wang, Shuya, Herrington, James, Graef, John, Newberry, Kimberly, Sivarao, Digavalli V, Senapati, Arun, Bristow, Linda J, Meanwell, Nicholas A, Thompson, Lorin A, Dzierba, Carolyn

“…3-Aryl-indole and 3-aryl-indazole derivatives were identified as potent and selective Na 1.7 inhibitors. Compound 29 was shown to be efficacious in the mouse…”
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A Functional Na V 1.7-Na V Ab Chimera with a Reconstituted High-Affinity ProTx-II Binding Site by Rajamani, Ramkumar, Wu, Sophie, Rodrigo, Iyoncy, Gao, Mian, Low, Simon, Megson, Lisa, Wensel, David, Pieschl, Rick L, Post-Munson, Debra J, Watson, John, Langley, David R, Ahlijanian, Michael K, Bristow, Linda J, Herrington, James

“…The Na 1.7 voltage-gated sodium channel is implicated in human pain perception by genetics. Rare gain of function mutations in Na 1.7 lead to spontaneous pain…”
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Discovery of morpholine-based aryl sulfonamides as Na v 1.7 inhibitors by Wu, Yong-Jin, Guernon, Jason, McClure, Andrea, Venables, Brian, Rajamani, Ramkumar, Robbins, Kevin J, Knox, Ronald J, Matchett, Michele, Pieschl, Rick L, Herrington, James, Bristow, Linda J, Meanwell, Nicholas A, Olson, Richard, Thompson, Lorin A, Dzierba, Carolyn

“…Replacement of the piperidine ring in the lead benzenesulfonamide Na 1.7 inhibitor 1 with a weakly basic morpholine core resulted in a significant reduction in…”
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B-973, a novel piperazine positive allosteric modulator of the α7 nicotinic acetylcholine receptor by Post-Munson, Debra J., Pieschl, Rick L., Molski, Thaddeus F., Graef, John D., Hendricson, Adam W., Knox, Ronald J., McDonald, Ivar M., Olson, Richard E., Macor, John E., Weed, Michael R., Bristow, Linda J., Kiss, Laszlo, Ahlijanian, Michael K., Herrington, James

“…The alpha7 (α7) nicotinic acetylcholine receptor is a therapeutic target for cognitive disorders. Here we describe…”
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Diminished responses to monoaminergic antidepressants but not ketamine in a mouse model for neuropsychiatric lupus by Srikumar, Bettadapura N, Naidu, Pattipati S, Kalidindi, Narasimharaju, Paschapur, Mahesh, Adepu, Bharath, Subramani, Siva, Nagar, Jignesh, Srivastava, Ratika, Sreedhara, Muppana V, Prasad, Durga Shiva, Das, Manish Lal, Louis, Justin V, Kuchibhotla, Vijaya K, Dudhgaonkar, Shailesh, Pieschl, Rick L, Li, Yu-Wen, Bristow, Linda J, Ramarao, Manjunath, Vikramadithyan, Reeba K

“…Background: A significant proportion of patients suffering from major depression fail to remit following treatment and develop treatment-resistant depression…”
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Development of New Benzenesulfonamides As Potent and Selective Na v 1.7 Inhibitors for the Treatment of Pain by Wu, Yong-Jin, Guernon, Jason, Shi, Jianliang, Ditta, Jonathan, Robbins, Kevin J, Rajamani, Ramkumar, Easton, Amy, Newton, Amy, Bourin, Clotilde, Mosure, Kathleen, Soars, Matthew G, Knox, Ronald J, Matchett, Michele, Pieschl, Rick L, Post-Munson, Debra J, Wang, Shuya, Herrington, James, Graef, John, Newberry, Kimberly, Bristow, Linda J, Meanwell, Nicholas A, Olson, Richard, Thompson, Lorin A, Dzierba, Carolyn

“…By taking advantage of certain features in piperidine 4, we developed a novel series of cyclohexylamine- and piperidine-based benzenesulfonamides as potent and…”
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Targeting acute ischemic stroke with a calcium-sensitive opener of maxi-K potassium channels by Gribkoff, Valentin K, Starrett, John E, Dworetzky, Steven I, Hewawasam, Piyasena, Boissard, Christopher G, Cook, Deborah A, Frantz, Stephen W, Heman, Karen, Hibbard, Jeffrey R, Huston, Kevin, Johnson, Graham, Krishnan, Bala S, Kinney, Gene G, Lombardo, Lynn A, Meanwell, Nicholas A, Molinoff, Perry B, Myers, Robert A, Moon, Sandra L, Ortiz, Astrid, Pajor, Lorraine, Pieschl, Rick L, Post-Munson, Debra J, Signor, Laura J, Srinivas, Nugehally, Taber, Matthew T, Thalody, George, Trojnacki, Joanne T, Wiener, Harvey, Yeleswaram, Krishnaswamy, Yeola, Sarita W

“…During ischemic stroke, neurons at risk are exposed to pathologically high levels of intracellular calcium (Ca++), initiating a fatal biochemical cascade. To…”
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A Reexamination of the Role of GABA in the Mammalian Suprachiasmatic Nucleus by Gribkoff, Valentin K., Pieschl, Rick L., Wisialowski, Todd A., Park, Won K., Strecker, George J., de Jeu, Marcel T. G., Pennartz, Cyriel M. A., Dudek, F. Edward

“…Three independent electrophysiological approaches in hypothalamic slices were used to test the hypothesis that [.gamma]-amino butyric acid (GABA)Areceptor…”
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Discovery of Indazoles as Potent, Orally Active Dual Neurokinin 1 Receptor Antagonists and Serotonin Transporter Inhibitors for the Treatment of Depression by Degnan, Andrew P, Tora, George O, Huang, Hong, Conlon, David A, Davis, Carl D, Hanumegowda, Umesh M, Hou, Xiaoping, Hsiao, Yi, Hu, Joanna, Krause, Rudolph, Li, Yu-Wen, Newton, Amy E, Pieschl, Rick L, Raybon, Joseph, Rosner, Thorsten, Sun, Jung-Hui, Taber, Matthew T, Taylor, Sarah J, Wong, Michael K, Zhang, Huiping, Lodge, Nicholas J, Bronson, Joanne J, Macor, John E, Gillman, Kevin W

“…Combination studies of neurokinin 1 (NK1) receptor antagonists and serotonin-selective reuptake inhibitors (SSRIs) have shown promise in preclinical models of…”
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