Search Results - "BROAD, Lisa M."

Activation of Muscarinic M1 Acetylcholine Receptors Induces Long-Term Potentiation in the Hippocampus by Dennis, Siobhan H, Pasqui, Francesca, Colvin, Ellen M, Sanger, Helen, Mogg, Adrian J, Felder, Christian C, Broad, Lisa M, Fitzjohn, Steve M, Isaac, John T R, Mellor, Jack R

“…Muscarinic M1 acetylcholine receptors (M1Rs) are highly expressed in the hippocampus, and their inhibition or ablation disrupts the encoding of spatial memory…”
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Acetylcholine modulates gamma frequency oscillations in the hippocampus by activation of muscarinic M1 receptors by Betterton, Ruth T., Broad, Lisa M., Tsaneva‐Atanasova, Krasimira, Mellor, Jack R., Poirazi, Panayiota

“…Modulation of gamma oscillations is important for the processing of information and the disruption of gamma oscillations is a prominent feature of…”
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M1 muscarinic allosteric modulators slow prion neurodegeneration and restore memory loss by Bradley, Sophie J, Bourgognon, Julie-Myrtille, Sanger, Helen E, Verity, Nicholas, Mogg, Adrian J, White, David J, Butcher, Adrian J, Moreno, Julie A, Molloy, Colin, Macedo-Hatch, Timothy, Edwards, Jennifer M, Wess, Jurgen, Pawlak, Robert, Read, David J, Sexton, Patrick M, Broad, Lisa M, Steinert, Joern R, Mallucci, Giovanna R, Christopoulos, Arthur, Felder, Christian C, Tobin, Andrew B

“…The current frontline symptomatic treatment for Alzheimer's disease (AD) is whole-body upregulation of cholinergic transmission via inhibition of…”
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The atypical ‘hippocampal’ glutamate receptor coupled to phospholipase D that controls stretch‐sensitivity in primary mechanosensory nerve endings is homomeric purely metabotropic GluK2 by Thompson, Karen J., Watson, Sonia, Zanato, Chiara, Dall'Angelo, Sergio, De Nooij, Joriene C., Pace‐Bonello, Bethany, Shenton, Fiona C., Sanger, Helen E., Heinz, Beverly A., Broad, Lisa M., Grosjean, Noelle, McQuillian, Jessica R., Dubini, Marina, Pyner, Susan, Greig, Iain, Zanda, Matteo, Bleakman, David, Banks, Robert W., Bewick, Guy S.

“…A metabotropic glutamate receptor coupled to phospholipase D (PLD‐mGluR) was discovered in the hippocampus over three decades ago. Its pharmacology and direct…”
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TRPV3 in Drug Development by Broad, Lisa M, Mogg, Adrian J, Eberle, Elizabeth, Tolley, Marcia, Li, Dominic L, Knopp, Kelly L

“…Transient receptor potential vanilloid 3 (TRPV3) is a member of the TRP (Transient Receptor Potential) super-family. It is a relatively underexplored member of…”
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Mechanisms of capacitative calcium entry by Putney, Jr, J W, Broad, L M, Braun, F J, Lievremont, J P, Bird, G S

“…Capacitative Ca(2+) entry involves the regulation of plasma membrane Ca(2+) channels by the filling state of intracellular Ca(2+) stores in the endoplasmic…”
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In vitro pharmacological and rat pharmacokinetic characterization of LY3020371, a potent and selective mGlu 2/3 receptor antagonist by Witkin, Jeffrey M, Ornstein, Paul L, Mitch, Charles H, Li, Renhua, Smith, Stephon C, Heinz, Beverly A, Wang, Xu-Shan, Xiang, Chuanxi, Carter, Joan H, Anderson, Wesley H, Li, Xia, Broad, Lisa M, Pasqui, Francesca, Fitzjohn, Stephen M, Sanger, Helen E, Smith, Jodi L, Catlow, John, Swanson, Steven, Monn, James A

“…Metabotropic glutamate (mGlu ) receptors are of considerable interest owing to their role in modulating glutamate transmission via presynaptic, postsynaptic…”
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Identification and pharmacological profile of a new class of selective nicotinic acetylcholine receptor potentiators by Broad, Lisa M, Zwart, Ruud, Pearson, Kathy H, Lee, Martin, Wallace, Louise, McPhie, Gordon I, Emkey, Renee, Hollinshead, Sean P, Dell, Colin P, Baker, S Richard, Sher, Emanuele

“…Here we report the discovery, by high-throughput screening, of three novel (2-amino-5-keto)thiazole compounds that act as selective potentiators of nicotinic…”
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Current status of muscarinic M1 and M4 receptors as drug targets for neurodegenerative diseases by Felder, Christian C., Goldsmith, Paul J., Jackson, Kimberley, Sanger, Helen E., Evans, David A., Mogg, Adrian J., Broad, Lisa M.

“…The cholinergic signalling system has been an attractive pathway to seek targets for modulation of arousal, cognition, and attention which are compromised in…”
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A non-capacitative pathway activated by arachidonic acid is the major Ca2+ entry mechanism in rat A7r5 smooth muscle cells stimulated with low concentrations of vasopressin by Broad, Lisa M., Cannon, Toby R., Taylor, Colin W.

“…Depletion of the Ca 2+ stores of A7r5 cells stimulated Ca 2+ , though not Sr 2+ , entry. Vasopressin (AVP) or platelet-derived growth factor (PDGF) stimulated…”
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From structure to clinic: Design of a muscarinic M1 receptor agonist with potential to treatment of Alzheimer's disease by Brown, Alastair J H, Bradley, Sophie J, Marshall, Fiona H, Brown, Giles A, Bennett, Kirstie A, Brown, Jason, Cansfield, Julie E, Cross, David M, de Graaf, Chris, Hudson, Brian D, Dwomoh, Louis, Dias, João M, Errey, James C, Hurrell, Edward, Liptrot, Jan, Mattedi, Giulio, Molloy, Colin, Nathan, Pradeep J, Okrasa, Krzysztof, Osborne, Greg, Patel, Jayesh C, Pickworth, Mark, Robertson, Nathan, Shahabi, Shahram, Bundgaard, Christoffer, Phillips, Keith, Broad, Lisa M, Goonawardena, Anushka V, Morairty, Stephen R, Browning, Michael, Perini, Francesca, Dawson, Gerard R, Deakin, John F W, Smith, Robert T, Sexton, Patrick M, Warneck, Julie, Vinson, Mary, Tasker, Tim, Tehan, Benjamin G, Teobald, Barry, Christopoulos, Arthur, Langmead, Christopher J, Jazayeri, Ali, Cooke, Robert M, Rucktooa, Prakash, Congreve, Miles S, Weir, Malcolm, Tobin, Andrew B

“…Current therapies for Alzheimer's disease seek to correct for defective cholinergic transmission by preventing the breakdown of acetylcholine through…”
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TRPA1 Antagonist LY3526318 Inhibits the Cinnamaldehyde‐Evoked Dermal Blood Flow Increase: Translational Proof of Pharmacology by Bamps, Dorien, Blockeel, Anthony James, Dreesen, Erwin, Marynissen, Heleen, Laenen, Jolien, Van Hecken, Anne, Wilke, August, Shahabi, Shahram, Johnson, Kirk W., Collins, Emily Catherine, Broad, Lisa M., Phillips, Keith G., Hoon, Jan

“…Transient receptor potential Ankyrin 1 (TRPA1) is an ion channel expressed by sensory neurons, where it mediates pain signaling. Consequently, it has emerged…”
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Biased M1-muscarinic-receptor-mutant mice inform the design of next-generation drugs by Bradley, Sophie J., Molloy, Colin, Valuskova, Paulina, Dwomoh, Louis, Scarpa, Miriam, Rossi, Mario, Finlayson, Lisa, Svensson, Kjell A., Chernet, Eyassu, Barth, Vanessa N., Gherbi, Karolina, Sykes, David A., Wilson, Caroline A., Mistry, Rajendra, Sexton, Patrick M., Christopoulos, Arthur, Mogg, Adrian J., Rosethorne, Elizabeth M., Sakata, Shuzo, John Challiss, R. A., Broad, Lisa M., Tobin, Andrew B.

“…Cholinesterase inhibitors, the current frontline symptomatic treatment for Alzheimer’s disease (AD), are associated with low efficacy and adverse effects. M1…”
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Different phospholipase-C-coupled receptors differentially regulate capacitative and non-capacitative Ca2+ entry in A7r5 cells by Moneer, Zahid, Pino, Irene, Taylor, Emily J A, Broad, Lisa M, Liu, Yingjie, Tovey, Stephen C, Staali, Leila, Taylor, Colin W

“…Several receptors, including those for AVP (Arg8-vasopressin) and 5-HT (5-hydroxytryptamine), share an ability to stimulate PLC (phospholipase C) and so…”
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Bitopic Binding Mode of an M 1 Muscarinic Acetylcholine Receptor Agonist Associated with Adverse Clinical Trial Outcomes by Bradley, Sophie J, Molloy, Colin, Bundgaard, Christoffer, Mogg, Adrian J, Thompson, Karen J, Dwomoh, Louis, Sanger, Helen E, Crabtree, Michael D, Brooke, Simon M, Sexton, Patrick M, Felder, Christian C, Christopoulos, Arthur, Broad, Lisa M, Tobin, Andrew B, Langmead, Christopher J

“…The realization of the therapeutic potential of targeting the M muscarinic acetylcholine receptor (mAChR) for the treatment of cognitive decline in Alzheimer's…”
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The nicotinic α4β2 receptor selective agonist, TC-2559, increases dopamine neuronal activity in the ventral tegmental area of rat midbrain slices by YING CHEN, SHARPLES, Thomas J. W, PHILLIPS, Keith G, BENEDETTI, Giovanni, BROAD, Lisa M, ZWART, Ruud, SHER, Emanuele

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An Antibody Biosensor Establishes the Activation of the M1 Muscarinic Acetylcholine Receptor during Learning and Memory by Butcher, Adrian J., Bradley, Sophie J., Prihandoko, Rudi, Brooke, Simon M., Mogg, Adrian, Bourgognon, Julie-Myrtille, Macedo-Hatch, Timothy, Edwards, Jennifer M., Bottrill, Andrew R., Challiss, R.A.John, Broad, Lisa M., Felder, Christian C., Tobin, Andrew B.

“…Establishing the in vivo activation status of G protein-coupled receptors would not only indicate physiological roles of G protein-coupled receptors but would…”
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Synthesis and Pharmacological Characterization of C4 β -Amide-Substituted 2-Aminobicyclo[3.1.0]hexane-2,6-dicarboxylates. Identification of (1 S,2 S,4 S,5 R,6 S)-2-Amino-4-[(3-methoxybenzoyl)amino]bicyclo[3.1.0]hexane-2,6-dicarboxylic Acid (LY2794193), a Highly Potent and Selective mGlu 3 Receptor Agonist by Monn, James A, Henry, Steven S, Massey, Steven M, Clawson, David K, Chen, Qi, Diseroad, Benjamin A, Bhardwaj, Rajni M, Atwell, Shane, Lu, Frances, Wang, Jing, Russell, Marijane, Heinz, Beverly A, Wang, Xu-Shan, Carter, Joan H, Getman, Brian G, Adragni, Kofi, Broad, Lisa M, Sanger, Helene E, Ursu, Daniel, Catlow, John T, Swanson, Steven, Johnson, Bryan G, Shaw, David B, McKinzie, David L, Hao, Junliang

“…Multiple therapeutic opportunities have been suggested for compounds capable of selective activation of metabotropic glutamate 3 (mGlu ) receptors, but small…”
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Identification and pharmacological profile of SPP1, a potent, functionally selective and brain penetrant agonist at muscarinic M1 receptors by Broad, Lisa M, Sanger, Helen E, Mogg, Adrian J, Colvin, Ellen M, Zwart, Ruud, Evans, David A, Pasqui, Francesca, Sher, Emanuele, Wishart, Graham N, Barth, Vanessa N, Felder, Christian C, Goldsmith, Paul J

“…Background and Purpose We aimed to identify and develop novel, selective muscarinic M1 receptor agonists as potential therapeutic agents for the symptomatic…”
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Pharmacological characterisation of ligand- and voltage-gated ion channels expressed in human iPSC-derived forebrain neurons by Dage, Jeffrey L., Colvin, Ellen M., Fouillet, Antoine, Langron, Emily, Roell, William C., Li, Jingling, Mathur, Sachin X., Mogg, Adrian J., Schmitt, Matthew G., Felder, Christian C., Merchant, Kalpana M., Isaac, John, Broad, Lisa M., Sher, Emanuele, Ursu, Daniel

“…Introduction Genetic causes, or predisposition, are increasingly accepted to be part of the ethiopathogenesis of many neuropsychiatric diseases. While genes…”
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