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Items: 50

1.

Identification and pharmacological profile of SPP1, a potent, functionally selective and brain penetrant agonist at muscarinic M1 receptors.

Broad LM, Sanger HE, Mogg AJ, Colvin EM, Zwart R, Evans DA, Pasqui F, Sher E, Wishart GN, Barth VN, Felder CC, Goldsmith PJ.

Br J Pharmacol. 2019 Jan;176(1):110-126. doi: 10.1111/bph.14510. Epub 2018 Nov 16.

PMID:
30276808
2.

Bitopic Binding Mode of an M1 Muscarinic Acetylcholine Receptor Agonist Associated with Adverse Clinical Trial Outcomes.

Bradley SJ, Molloy C, Bundgaard C, Mogg AJ, Thompson KJ, Dwomoh L, Sanger HE, Crabtree MD, Brooke SM, Sexton PM, Felder CC, Christopoulos A, Broad LM, Tobin AB, Langmead CJ.

Mol Pharmacol. 2018 Jun;93(6):645-656. doi: 10.1124/mol.118.111872. Epub 2018 Apr 25.

3.

In Vitro Pharmacological Characterization and In Vivo Validation of LSN3172176 a Novel M1 Selective Muscarinic Receptor Agonist Tracer Molecule for Positron Emission Tomography.

Mogg AJ, Eessalu T, Johnson M, Wright R, Sanger HE, Xiao H, Crabtree MG, Smith A, Colvin EM, Schober D, Gehlert D, Jesudason C, Goldsmith PJ, Johnson MP, Felder CC, Barth VN, Broad LM.

J Pharmacol Exp Ther. 2018 Jun;365(3):602-613. doi: 10.1124/jpet.117.246454. Epub 2018 Apr 11.

4.

Current status of muscarinic M1 and M4 receptors as drug targets for neurodegenerative diseases.

Felder CC, Goldsmith PJ, Jackson K, Sanger HE, Evans DA, Mogg AJ, Broad LM.

Neuropharmacology. 2018 Jul 1;136(Pt C):449-458. doi: 10.1016/j.neuropharm.2018.01.028. Epub 2018 Jan 31. Review.

PMID:
29374561
5.

Synthesis and Pharmacological Characterization of C4β-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 mGlu3 Receptor Agonist.

Monn JA, Henry SS, Massey SM, Clawson DK, Chen Q, Diseroad BA, Bhardwaj RM, Atwell S, Lu F, Wang J, Russell M, Heinz BA, Wang XS, Carter JH, Getman BG, Adragni K, Broad LM, Sanger HE, Ursu D, Catlow JT, Swanson S, Johnson BG, Shaw DB, McKinzie DL, Hao J.

J Med Chem. 2018 Mar 22;61(6):2303-2328. doi: 10.1021/acs.jmedchem.7b01481. Epub 2018 Feb 6.

PMID:
29350927
6.

Acetylcholine modulates gamma frequency oscillations in the hippocampus by activation of muscarinic M1 receptors.

Betterton RT, Broad LM, Tsaneva-Atanasova K, Mellor JR.

Eur J Neurosci. 2017 Jun;45(12):1570-1585. doi: 10.1111/ejn.13582. Epub 2017 May 8.

7.

M1 muscarinic allosteric modulators slow prion neurodegeneration and restore memory loss.

Bradley SJ, Bourgognon JM, Sanger HE, Verity N, Mogg AJ, White DJ, Butcher AJ, Moreno JA, Molloy C, Macedo-Hatch T, Edwards JM, Wess J, Pawlak R, Read DJ, Sexton PM, Broad LM, Steinert JR, Mallucci GR, Christopoulos A, Felder CC, Tobin AB.

J Clin Invest. 2017 Feb 1;127(2):487-499. doi: 10.1172/JCI87526. Epub 2016 Dec 19.

8.

TRPV3 in Drug Development.

Broad LM, Mogg AJ, Eberle E, Tolley M, Li DL, Knopp KL.

Pharmaceuticals (Basel). 2016 Sep 9;9(3). pii: E55. doi: 10.3390/ph9030055. Review.

9.

The creation and characterisation of a National Compound Collection: the Royal Society of Chemistry pilot.

Andrews DM, Broad LM, Edwards PJ, Fox DNA, Gallagher T, Garland SL, Kidd R, Sweeney JB.

Chem Sci. 2016 Jun 1;7(6):3869-3878. doi: 10.1039/c6sc00264a. Epub 2016 Feb 23.

10.

Activation of transient receptor potential ankyrin 1 induces CGRP release from spinal cord synaptosomes.

Quallo T, Gentry C, Bevan S, Broad LM, Mogg AJ.

Pharmacol Res Perspect. 2015 Oct 25;3(6):e00191. doi: 10.1002/prp2.191. eCollection 2015 Dec.

11.

An Antibody Biosensor Establishes the Activation of the M1 Muscarinic Acetylcholine Receptor during Learning and Memory.

Butcher AJ, Bradley SJ, Prihandoko R, Brooke SM, Mogg A, Bourgognon JM, Macedo-Hatch T, Edwards JM, Bottrill AR, Challiss RA, Broad LM, Felder CC, Tobin AB.

J Biol Chem. 2016 Apr 22;291(17):8862-75. doi: 10.1074/jbc.M115.681726. Epub 2016 Jan 29.

12.

In vitro pharmacological and rat pharmacokinetic characterization of LY3020371, a potent and selective mGlu2/3 receptor antagonist.

Witkin JM, Ornstein PL, Mitch CH, Li R, Smith SC, Heinz BA, Wang XS, Xiang C, Carter JH, Anderson WH, Li X, Broad LM, Pasqui F, Fitzjohn SM, Sanger HE, Smith JL, Catlow J, Swanson S, Monn JA.

Neuropharmacology. 2017 Mar 15;115:100-114. doi: 10.1016/j.neuropharm.2015.12.021. Epub 2015 Dec 31.

PMID:
26748052
13.

Activation of Muscarinic M1 Acetylcholine Receptors Induces Long-Term Potentiation in the Hippocampus.

Dennis SH, Pasqui F, Colvin EM, Sanger H, Mogg AJ, Felder CC, Broad LM, Fitzjohn SM, Isaac JT, Mellor JR.

Cereb Cortex. 2016 Jan;26(1):414-26. doi: 10.1093/cercor/bhv227. Epub 2015 Oct 15.

14.

Synthesis and pharmacological characterization of C4-disubstituted analogs of 1S,2S,5R,6S-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylate: identification of a potent, selective metabotropic glutamate receptor agonist and determination of agonist-bound human mGlu2 and mGlu3 amino terminal domain structures.

Monn JA, Prieto L, Taboada L, Pedregal C, Hao J, Reinhard MR, Henry SS, Goldsmith PJ, Beadle CD, Walton L, Man T, Rudyk H, Clark B, Tupper D, Baker SR, Lamas C, Montero C, Marcos A, Blanco J, Bures M, Clawson DK, Atwell S, Lu F, Wang J, Russell M, Heinz BA, Wang X, Carter JH, Xiang C, Catlow JT, Swanson S, Sanger H, Broad LM, Johnson MP, Knopp KL, Simmons RM, Johnson BG, Shaw DB, McKinzie DL.

J Med Chem. 2015 Feb 26;58(4):1776-94. doi: 10.1021/jm501612y. Epub 2015 Feb 5.

PMID:
25602126
15.

123I-iododexetimide preferentially binds to the muscarinic receptor subtype M1 in vivo.

Bakker G, Vingerhoets WA, van Wieringen JP, de Bruin K, Eersels J, de Jong J, Chahid Y, Rutten BP, DuBois S, Watson M, Mogg AJ, Xiao H, Crabtree M, Collier DA, Felder CC, Barth VN, Broad LM, Bloemen OJ, van Amelsvoort TA, Booij J.

J Nucl Med. 2015 Feb;56(2):317-22. doi: 10.2967/jnumed.114.147488. Epub 2015 Jan 15.

16.

Pharmacological characterisation of ligand- and voltage-gated ion channels expressed in human iPSC-derived forebrain neurons.

Dage JL, Colvin EM, Fouillet A, Langron E, Roell WC, Li J, Mathur SX, Mogg AJ, Schmitt MG, Felder CC, Merchant KM, Isaac J, Broad LM, Sher E, Ursu D.

Psychopharmacology (Berl). 2014 Mar;231(6):1105-24. doi: 10.1007/s00213-013-3384-2. Epub 2014 Jan 16.

PMID:
24429870
17.

Pharmacological profiling of the TRPV3 channel in recombinant and native assays.

Grubisha O, Mogg AJ, Sorge JL, Ball LJ, Sanger H, Ruble CL, Folly EA, Ursu D, Broad LM.

Br J Pharmacol. 2014 May;171(10):2631-44. doi: 10.1111/bph.12303.

18.

Altered pharmacology of native rodent spinal cord TRPV1 after phosphorylation.

Mogg AJ, Mill CE, Folly EA, Beattie RE, Blanco MJ, Beck JP, Broad LM.

Br J Pharmacol. 2013 Feb;168(4):1015-29. doi: 10.1111/bph.12005.

19.

In vitro characterisation of the novel positive allosteric modulators of the mGlu₅ receptor, LSN2463359 and LSN2814617, and their effects on sleep architecture and operant responding in the rat.

Gilmour G, Broad LM, Wafford KA, Britton T, Colvin EM, Fivush A, Gastambide F, Getman B, Heinz BA, McCarthy AP, Prieto L, Shanks E, Smith JW, Taboada L, Edgar DM, Tricklebank MD.

Neuropharmacology. 2013 Jan;64:224-39. doi: 10.1016/j.neuropharm.2012.07.030. Epub 2012 Aug 1.

PMID:
22884720
20.

Pharmacological profiling of native group II metabotropic glutamate receptors in primary cortical neuronal cultures using a FLIPR.

Sanger H, Hanna L, Colvin EM, Grubisha O, Ursu D, Heinz BA, Findlay JD, Vivier RG, Sher E, Lodge D, Monn JA, Broad LM.

Neuropharmacology. 2013 Mar;66:264-73. doi: 10.1016/j.neuropharm.2012.05.023. Epub 2012 May 30.

PMID:
22659090
21.

Partial agonists for α4β2 nicotinic receptors stimulate dopaminergic neuron firing with relatively enhanced maximal effects.

Chen Y, Broad LM, Phillips KG, Zwart R.

Br J Pharmacol. 2012 Feb;165(4):1006-16. doi: 10.1111/j.1476-5381.2011.01628.x.

22.

Paradoxical effects of the cannabinoid CB2 receptor agonist GW405833 on rat osteoarthritic knee joint pain.

Schuelert N, Zhang C, Mogg AJ, Broad LM, Hepburn DL, Nisenbaum ES, Johnson MP, McDougall JJ.

Osteoarthritis Cartilage. 2010 Nov;18(11):1536-43. doi: 10.1016/j.joca.2010.09.005. Epub 2010 Sep 21.

23.

Up-regulation of astrocyte metabotropic glutamate receptor 5 by amyloid-β peptide.

Casley CS, Lakics V, Lee HG, Broad LM, Day TA, Cluett T, Smith MA, O'Neill MJ, Kingston AE.

Brain Res. 2009 Mar 13;1260:65-75. Epub 2009 Jan 18.

PMID:
19401173
24.

TRP channels as emerging targets for pain therapeutics.

Broad LM, Mogg AJ, Beattie RE, Ogden AM, Blanco MJ, Bleakman D.

Expert Opin Ther Targets. 2009 Jan;13(1):69-81. doi: 10.1517/14728220802616620 . Review.

PMID:
19063707
25.

Recent progress in the development of selective TRPV1 antagonists for pain.

Broad LM, Keding SJ, Blanco MJ.

Curr Top Med Chem. 2008;8(16):1431-41. Review.

PMID:
18991729
26.

Sazetidine-A is a potent and selective agonist at native and recombinant alpha 4 beta 2 nicotinic acetylcholine receptors.

Zwart R, Carbone AL, Moroni M, Bermudez I, Mogg AJ, Folly EA, Broad LM, Williams AC, Zhang D, Ding C, Heinz BA, Sher E.

Mol Pharmacol. 2008 Jun;73(6):1838-43. doi: 10.1124/mol.108.045104. Epub 2008 Mar 26.

PMID:
18367540
27.

Species selectivity of a nicotinic acetylcholine receptor agonist is conferred by two adjacent extracellular beta4 amino acids that are implicated in the coupling of binding to channel gating.

Young GT, Broad LM, Zwart R, Astles PC, Bodkin M, Sher E, Millar NS.

Mol Pharmacol. 2007 Feb;71(2):389-97. Epub 2006 Oct 25.

PMID:
17065235
28.

Epibatidine isomers and analogues: structure-activity relationships.

White R, Malpass JR, Handa S, Richard Baker S, Broad LM, Folly L, Mogg A.

Bioorg Med Chem Lett. 2006 Nov 1;16(21):5493-7. Epub 2006 Aug 28.

PMID:
16934977
29.

Identification and pharmacological profile of a new class of selective nicotinic acetylcholine receptor potentiators.

Broad LM, Zwart R, Pearson KH, Lee M, Wallace L, McPhie GI, Emkey R, Hollinshead SP, Dell CP, Baker SR, Sher E.

J Pharmacol Exp Ther. 2006 Sep;318(3):1108-17. Epub 2006 May 31.

PMID:
16738207
30.

5-I A-85380 and TC-2559 differentially activate heterologously expressed alpha4beta2 nicotinic receptors.

Zwart R, Broad LM, Xi Q, Lee M, Moroni M, Bermudez I, Sher E.

Eur J Pharmacol. 2006 Jun 6;539(1-2):10-7. Epub 2006 Apr 5.

PMID:
16674940
31.

Different phospholipase-C-coupled receptors differentially regulate capacitative and non-capacitative Ca2+ entry in A7r5 cells.

Moneer Z, Pino I, Taylor EJ, Broad LM, Liu Y, Tovey SC, Staali L, Taylor CW.

Biochem J. 2005 Aug 1;389(Pt 3):821-9.

32.

Stable expression and characterisation of a human alpha 7 nicotinic subunit chimera: a tool for functional high-throughput screening.

Craig PJ, Bose S, Zwart R, Beattie RE, Folly EA, Johnson LR, Bell E, Evans NM, Benedetti G, Pearson KH, McPhie GI, Volsen SG, Millar NS, Sher E, Broad LM.

Eur J Pharmacol. 2004 Oct 11;502(1-2):31-40.

PMID:
15464087
33.

Physiological roles of neuronal nicotinic receptor subtypes: new insights on the nicotinic modulation of neurotransmitter release, synaptic transmission and plasticity.

Sher E, Chen Y, Sharples TJ, Broad LM, Benedetti G, Zwart R, McPhie GI, Pearson KH, Baldwinson T, De Filippi G.

Curr Top Med Chem. 2004;4(3):283-97. Review.

PMID:
14754448
34.

The nicotinic alpha 4 beta 2 receptor selective agonist, TC-2559, increases dopamine neuronal activity in the ventral tegmental area of rat midbrain slices.

Chen Y, Sharples TJ, Phillips KG, Benedetti G, Broad LM, Zwart R, Sher E.

Neuropharmacology. 2003 Sep;45(3):334-44.

PMID:
12871651
35.

Recent progress in the development of subtype selective nicotinic acetylcholine receptor ligands.

Astles PC, Baker SR, Boot JR, Broad LM, Dell CP, Keenan M.

Curr Drug Targets CNS Neurol Disord. 2002 Aug;1(4):337-48. Review.

PMID:
12769608
36.

Expression and functional characterisation of a human chimeric nicotinic receptor with alpha6beta4 properties.

Evans NM, Bose S, Benedetti G, Zwart R, Pearson KH, McPhie GI, Craig PJ, Benton JP, Volsen SG, Sher E, Broad LM.

Eur J Pharmacol. 2003 Apr 11;466(1-2):31-9.

PMID:
12679139
37.

PSAB-OFP, a selective alpha 7 nicotinic receptor agonist, is also a potent agonist of the 5-HT3 receptor.

Broad LM, Felthouse C, Zwart R, McPhie GI, Pearson KH, Craig PJ, Wallace L, Broadmore RJ, Boot JR, Keenan M, Baker SR, Sher E.

Eur J Pharmacol. 2002 Oct 4;452(2):137-44.

PMID:
12354563
38.

5-Hydroxyindole potentiates human alpha 7 nicotinic receptor-mediated responses and enhances acetylcholine-induced glutamate release in cerebellar slices.

Zwart R, De Filippi G, Broad LM, McPhie GI, Pearson KH, Baldwinson T, Sher E.

Neuropharmacology. 2002 Sep;43(3):374-84.

PMID:
12243767
39.
40.

Mechanisms of capacitative calcium entry.

Putney JW Jr, Broad LM, Braun FJ, Lievremont JP, Bird GS.

J Cell Sci. 2001 Jun;114(Pt 12):2223-9. Review.

41.

Role of the phospholipase C-inositol 1,4,5-trisphosphate pathway in calcium release-activated calcium current and capacitative calcium entry.

Broad LM, Braun FJ, Lievremont JP, Bird GS, Kurosaki T, Putney JW Jr.

J Biol Chem. 2001 May 11;276(19):15945-52. Epub 2001 Feb 13.

42.

Mutual antagonism of calcium entry by capacitative and arachidonic acid-mediated calcium entry pathways.

Luo D, Broad LM, Bird GS, Putney JW Jr.

J Biol Chem. 2001 Jun 8;276(23):20186-9. Epub 2001 Mar 23.

43.

Signaling pathways underlying muscarinic receptor-induced [Ca2+]i oscillations in HEK293 cells.

Luo D, Broad LM, Bird GS, Putney JW Jr.

J Biol Chem. 2001 Feb 23;276(8):5613-21. Epub 2000 Nov 28.

44.

Stable activation of single Ca2+ release-activated Ca2+ channels in divalent cation-free solutions.

Braun FJ, Broad LM, Armstrong DL, Putney JW Jr.

J Biol Chem. 2001 Jan 12;276(2):1063-70.

45.
46.
48.

Pharmacological analysis of intracellular Ca2+ signalling: problems and pitfalls.

Taylor CW, Broad LM.

Trends Pharmacol Sci. 1998 Sep;19(9):370-5. Review.

PMID:
9786025
49.
50.

Characterisation of inositol 1,4,5-trisphosphate binding sites in rabbit aortic smooth muscle.

Murphy TV, Broad LM, Garland CJ.

Eur J Pharmacol. 1995 Jul 18;290(2):145-50.

PMID:
8575529

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