Search Results - "Brice, Nicola L."

Differential contribution of THIK-1 K + channels and P2X7 receptors to ATP-mediated neuroinflammation by human microglia by Rifat, Ali, Ossola, Bernardino, Bürli, Roland W, Dawson, Lee A, Brice, Nicola L, Rowland, Anna, Lizio, Marina, Xu, Xiao, Page, Keith, Fidzinski, Pawel, Onken, Julia, Holtkamp, Martin, Heppner, Frank L, Geiger, Jörg R P, Madry, Christian

“…Neuroinflammation is highly influenced by microglia, particularly through activation of the NLRP3 inflammasome and subsequent release of IL-1β. Extracellular…”
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A Phase I, First-in-Human, Healthy Volunteer Study to Investigate the Safety, Tolerability, and Pharmacokinetics of CVN424, a Novel G Protein-Coupled Receptor 6 Inverse Agonist for Parkinson's Disease by Margolin, David H, Brice, Nicola L, Davidson, Antonia M, Matthews, Kim L, Carlton, Mark B L

“…CVN424 is a novel small molecule and first-in-class candidate therapeutic to selectively modulate GPR6, an orphan G-protein coupled receptor. Expression of…”
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Mismatch negativity as an index of target engagement for excitation/inhibition-based treatment development: a double-blind, placebo-controlled, randomized, single-dose cross-over study of the serotonin type-3 receptor antagonist CVN058 by Sehatpour, Pejman, Javitt, Daniel C, De Baun, Heloise M, Carlson, Marlene, Beloborodova, Anna, Margolin, David H, Carlton, Mark B L, Brice, Nicola L, Kantrowitz, Joshua T

“…Serotonin type-3 receptor (5-HT R) antagonists show potential as a treatment for cognitive deficits in schizophrenia. CVN058, a brain-penetrant, potent and…”
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Discovery and Characterization of Novel CNS-Penetrant GPR55 Agonists by Hewer, Richard C., Christie, Louisa A., Doyle, Kevin J., Xu, Xiao, Roberts, Maxine J., Dickson, Louise, Cheung, Toni, Cadwalladr, David H., Pickford, Philip, Teall, Martin, Powell, Justin A. C., Sheardown, Steven, Narayana, Lakshminarayana, Brice, Nicola L., Dawson, Lee A., Carlton, Mark, Bürli, Roland W.

“…From our NETSseq-derived human brain transcriptomics data, we identified GPR55 as a potential molecular target for the treatment of motor symptoms in patients…”
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Discovery and first-time disclosure of CVN766, an exquisitely selective orexin 1 receptor antagonist by Glen, Angela, Bürli, Roland W., Livermore, David, Buffham, William, Merison, Stephanie, Rowland, Anna E., Newman, Robert, Fieldhouse, Charlotte, Miller, David J., Dawson, Lee A., Matthews, Kim, Carlton, Mark B., Brice, Nicola L.

“…[Display omitted] Modulators of orexin receptors are being developed for neurological illnesses such as sleep disorders, addictive behaviours and other…”
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Discovery of CVN417, a Novel Brain-Penetrant α6-Containing Nicotinic Receptor Antagonist for the Modulation of Motor Dysfunction by Christie, Louisa A., Brice, Nicola L., Rowland, Anna, Dickson, Louise, Anand, Rishi, Teall, Martin, Doyle, Kevin J., Narayana, Lakshminarayana, Mitchell, Christine, Harvey, Jenna R. M., Mulligan, Victoria, Dawson, Lee A., Cragg, Stephanie J., Carlton, Mark, Bürli, Roland W.

“…Nicotinic acetylcholine receptor (nAChR) α6 subunit RNA expression is relatively restricted to midbrain regions and is located presynaptically on dopaminergic…”
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Anti-hyperalgesic effects of a novel TRPM8 agonist in neuropathic rats: A comparison with topical menthol by Patel, Ryan, Gonçalves, Leonor, Leveridge, Mathew, Mack, Stephen R., Hendrick, Alan, Brice, Nicola L., Dickenson, Anthony H.

“…An in vivo electrophysiological characterisation of the pro- and anti-nociceptive effects of TRPM8 agonists reveals menthol and a novel TRPM8 agonist have…”
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First-Time Disclosure of CVN424, a Potent and Selective GPR6 Inverse Agonist for the Treatment of Parkinson’s Disease: Discovery, Pharmacological Validation, and Identification of a Clinical Candidate by Sun, Huikai, Monenschein, Holger, Schiffer, Hans H, Reichard, Holly A, Kikuchi, Shota, Hopkins, Maria, Macklin, Todd K, Hitchcock, Stephen, Adams, Mark, Green, Jason, Brown, Jason, Murphy, Sean T, Kaushal, Nidhi, Collia, Deanna R, Moore, Steve, Ray, William J, English, Nicole Marion, Carlton, Mark Beresford Lewis, Brice, Nicola L

“…Parkinson’s disease (PD) is a chronic and progressive movement disorder with the urgent unmet need for efficient symptomatic therapies with fewer side effects…”
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Characterisation of C101248: A novel selective THIK-1 channel inhibitor for the modulation of microglial NLRP3-inflammasome by Ossola, Bernardino, Rifat, Ali, Rowland, Anna, Hunter, Helen, Drinkall, Samuel, Bender, Clare, Hamlischer, Mayida, Teall, Martin, Burley, Russell, Barker, Daneil F., Cadwalladr, David, Dickson, Louise, Lawrence, Jason M.K., Harvey, Jenna R.M., Lizio, Marina, Xu, Xiao, Kavanagh, Edel, Cheung, Toni, Sheardown, Steve, Lawrence, Catherine B., Harte, Michael, Brough, David, Madry, Christian, Matthews, Kim, Doyle, Kevin, Page, Keith, Powell, Justin, Brice, Nicola L., Bürli, Roland W., Carlton, Mark B., Dawson, Lee A.

“…Neuroinflammation, specifically the NLRP3 inflammasome cascade, is a common underlying pathological feature of many neurodegenerative diseases. Evidence…”
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Development of CVN424: A Selective and Novel GPR6 Inverse Agonist Effective in Models of Parkinson Disease by Brice, Nicola L, Schiffer, Hans H, Monenschein, Holger, Mulligan, Victoria J, Page, Keith, Powell, Justin, Xu, Xiao, Cheung, Toni, Burley, J Russell, Sun, Huikai, Dickson, Louise, Murphy, Sean T, Kaushal, Nidhi, Sheardown, Steve, Lawrence, Jason, Chen, Yun, Bartkowski, Darian, Kanta, Anne, Russo, Joseph, Hosea, Natalie, Dawson, Lee A, Hitchcock, Stephen H, Carlton, Mark B

“…GPR6 is an orphan G-protein-coupled receptor that has enriched expression in the striatopallidal, indirect pathway and medium spiny neurons of the striatum…”
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Ionic mechanisms of spinal neuronal cold hypersensitivity in ciguatera by Patel, Ryan, Brice, Nicola L., Lewis, Richard J., Dickenson, Anthony H.

“…Cold hypersensitivity is evident in a range of neuropathies and can evoke sensations of paradoxical burning cold pain. Ciguatoxin poisoning is known to induce…”
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Synthesis and SAR of novel GPR39 agonists and positive allosteric modulators by Burley, Russell, Hewer, Richard C., Teall, Martin, Dickson, Louise, Ossola, Bernardino, Russell, Sam, Bender, Clare, Cheung, Toni, Powell, Justin A.C., Xu, Xiao, Brice, Nicola L., Otter, Lucy, Arimont, Marta, Kidd, Sarah L., Vidal, David, Dale, James W., Mervin, Lewis, Sore, Hannah F., Mateu, Natalia, Lakshminarayana, Narayana, Dawson, Lee A., Carlton, Mark, Bürli, Roland W.

“…[Display omitted] We report a significant decrease in transcription of the G protein-coupled receptor GPR39 in striatal neurons of Parkinson’s disease patients…”
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Discovery of CVN293, a Brain Permeable KCNK13 (THIK-1) Inhibitor Suitable for Clinical Assessment by Bürli, Roland W., Doyle, Kevin J., Dickson, Louise, Rowland, Anna, Matthews, Kim, Stott, Andrew J., Teall, Martin, Ossola, Bernardino, Russell, Samuel G., Harvey, Jenna R. M., Wu, Yiming, Narayana, Lakshminarayana, Brice, Nicola L., Carlton, Mark, Dawson, Lee A.

“…The potassium (K+) ion channel KCNK13 is specifically expressed in human microglia with elevated expression observed in post-mortem human brain tissue from…”
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Discovery of CVN636: A Highly Potent, Selective, and CNS Penetrant mGluR7 Allosteric Agonist by Dickson, Louise, Teall, Martin, Chevalier, Elodie, Cheung, Toni, Liwicki, Gemma M., Mack, Stephen, Stephenson, Anne, White, Kathryn, Fosbeary, Richard, Harrison, David C., Brice, Nicola L., Doyle, Kevin, Ciccocioppo, Roberto, Wu, Chaobo, Almond, Sarah, Patel, Toshal R., Mitchell, Philip, Barnes, Matt, Ayscough, Andrew P., Dawson, Lee A., Carlton, Mark, Bürli, Roland W.

“…The low affinity metabotropic glutamate receptor mGluR7 has been implicated in numerous CNS disorders; however, a paucity of potent and selective activators…”
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Discovery of CVN636 : A Highly Potent, Selective, and CNS Penetrant mGluR 7 Allosteric Agonist by Dickson, Louise, Teall, Martin, Chevalier, Elodie, Cheung, Toni, Liwicki, Gemma M, Mack, Stephen, Stephenson, Anne, White, Kathryn, Fosbeary, Richard, Harrison, David C, Brice, Nicola L, Doyle, Kevin, Ciccocioppo, Roberto, Wu, Chaobo, Almond, Sarah, Patel, Toshal R, Mitchell, Philip, Barnes, Matt, Ayscough, Andrew P, Dawson, Lee A, Carlton, Mark, Bürli, Roland W

“…The low affinity metabotropic glutamate receptor mGluR has been implicated in numerous CNS disorders; however, a paucity of potent and selective activators has…”
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CVN424, a GPR6 inverse agonist, for Parkinson's disease and motor fluctuations: a double-blind, randomized, phase 2 trial by Brice, Nicola L., Carlton, Mark, Margolin, David H., Bexon, Martin, Matthews, Kim L., Dawson, Lee A., Ellenbogen, Aaron L., Olanow, C. Warren, Dubow, Jordan, Kieburtz, Karl

“…CVN424 is a GPR6 inverse agonist that provides selective pharmacological control of the indirect striatopallidal pathway. We assessed the safety and efficacy…”
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Pharmacological targeting of glutamatergic neurons within the brainstem for weight reduction by Schneeberger, Marc, Brice, Nicola L., Pellegrino, Kyle, Parolari, Luca, Shaked, Jordan T., Page, Keith J., Marchildon, François, Barrows, Douglas W., Carroll, Thomas S., Topilko, Thomas, Mulligan, Victoria M., Newman, Robert, Doyle, Kevin, Bürli, Roland, Barker, Daniel F., Glen, Angela, Ortuño, María José, Nectow, Alexander R., Renier, Nicolas, Cohen, Paul, Carlton, Mark, Heintz, Nathaniel, Friedman, Jeffrey M.

“…Food intake and body weight are tightly regulated by neurons within specific brain regions, including the brainstem, where acute activation of dorsal raphe…”
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Differential plasma membrane targeting of voltage-dependent calcium channel subunits expressed in a polarized epithelial cell line by Brice, Nicola L., Dolphin, Annette C.

“…Voltage-dependent calcium channels (VDCCs) show a highly non-uniform distribution in many cell types, including neurons and other polarized secretory cells. We…”
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Author Correction: Pharmacological targeting of glutamatergic neurons within the brainstem for weight reduction by Schneeberger, Marc, Brice, Nicola L., Pellegrino, Kyle, Parolari, Luca, Shaked, Jordan T., Page, Keith J., Marchildon, François, Barrows, Douglas W., Carroll, Thomas S., Topilko, Thomas, Mulligan, Victoria M., Newman, Robert, Doyle, Kevin, Bürli, Roland, Barker, Daniel F., Glen, Angela, Ortuño, María José, Nectow, Alexander R., Renier, Nicolas, Cohen, Paul, Carlton, Mark, Heintz, Nathaniel, Friedman, Jeffrey M.

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The effect of overexpression of auxiliary Ca2+ channel subunits on native Ca2+ channel currents in undifferentiated mammalian NG108-15 cells by Wyatt, Christopher N., Page, Karen M., Berrow, Nicholas S., Brice, Nicola L., Dolphin, Annette C.

“…High voltage activated (HVA) Ca 2+ channels are composed of a pore-forming α1 subunit and the accessory β and α2–δ subunits. However, the subunit…”
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