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Items: 1 to 50 of 132

1.

Modulation of TARP γ8-Containing AMPA Receptors as a Novel Therapeutic Approach for Chronic Pain.

Knopp KL, Simmons RMA, Guo W, Adams BL, Gardinier KM, Gernert DL, Ornstein PL, Porter W, Reel J, Ding C, Wang H, Qian Y, Burris KD, Need A, Barth V, Swanson S, Catlow J, Witkin JM, Zwart R, Sher E, Choong KC, Wall TM, Schober D, Felder CC, Kato AS, Bredt DS, Nisenbaum ES.

J Pharmacol Exp Ther. 2019 Jun;369(3):345-363. doi: 10.1124/jpet.118.250126. Epub 2019 Mar 25.

PMID:
30910921
2.

The impact of external innovation on new drug approvals: A retrospective analysis.

Liu X, Thomas CE, Felder CC.

Int J Pharm. 2019 May 30;563:273-281. doi: 10.1016/j.ijpharm.2018.12.093. Epub 2019 Jan 18. Review.

PMID:
30664998
3.

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
4.

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.

5.

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.

6.

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
7.

Identification, expression and functional characterization of M4L, a muscarinic acetylcholine M4 receptor splice variant.

Schober DA, Croy CH, Ruble CL, Tao R, Felder CC.

PLoS One. 2017 Dec 6;12(12):e0188330. doi: 10.1371/journal.pone.0188330. eCollection 2017.

8.

Isoform specific differences in phospholipase C beta 1 expression in the prefrontal cortex in schizophrenia and suicide.

Udawela M, Scarr E, Boer S, Um JY, Hannan AJ, McOmish C, Felder CC, Thomas EA, Dean B.

NPJ Schizophr. 2017 Apr 19;3:19. doi: 10.1038/s41537-017-0020-x. eCollection 2017.

9.

Further Evaluation of Mechanisms Associated with the Antidepressantlike Signature of Scopolamine in Mice.

Martin AE, Schober DA, Nikolayev A, Tolstikov VV, Anderson WH, Higgs RE, Kuo MS, Laksmanan A, Catlow JT, Li X, Felder CC, Witkin JM.

CNS Neurol Disord Drug Targets. 2017;16(4):492-500. doi: 10.2174/1871527316666170309142646.

PMID:
28294051
10.

Translational Pharmacology of the Metabotropic Glutamate 2 Receptor-Preferring Agonist LY2812223 in the Animal and Human Brain.

Felder CC, Schober DA, Tu Y, Quets A, Xiao H, Watt M, Siuda E, Nisenbaum E, Xiang C, Heinz B, Prieto L, McKinzie DL, Monn JA.

J Pharmacol Exp Ther. 2017 Apr;361(1):190-197. doi: 10.1124/jpet.116.237859. Epub 2017 Jan 30.

PMID:
28138041
11.

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.

12.

Characterization of PCS1055, a novel muscarinic M4 receptor antagonist.

Croy CH, Chan WY, Castetter AM, Watt ML, Quets AT, Felder CC.

Eur J Pharmacol. 2016 Jul 5;782:70-6. doi: 10.1016/j.ejphar.2016.04.022. Epub 2016 Apr 13.

PMID:
27085897
13.

Crystal structures of the M1 and M4 muscarinic acetylcholine receptors.

Thal DM, Sun B, Feng D, Nawaratne V, Leach K, Felder CC, Bures MG, Evans DA, Weis WI, Bachhawat P, Kobilka TS, Sexton PM, Kobilka BK, Christopoulos A.

Nature. 2016 Mar 17;531(7594):335-40. doi: 10.1038/nature17188. Epub 2016 Mar 9.

14.

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.

15.

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.

16.

Design and synthesis of N-[6-(Substituted Aminoethylideneamino)-2-Hydroxyindan-1-yl]arylamides as selective and potent muscarinic M₁ agonists.

Liu B, Croy CH, Hitchcock SA, Allen JR, Rao Z, Evans D, Bures MG, McKinzie DL, Watt ML, Stuart Gregory G, Hansen MM, Hoogestraat PJ, Jamison JA, Okha-Mokube FM, Stratford RE, Turner W, Bymaster F, Felder CC.

Bioorg Med Chem Lett. 2015 Oct 1;25(19):4158-63. doi: 10.1016/j.bmcl.2015.08.011. Epub 2015 Aug 8.

PMID:
26299349
17.

Antipsychotic-like effect of the muscarinic acetylcholine receptor agonist BuTAC in non-human primates.

Andersen MB, Croy CH, Dencker D, Werge T, Bymaster FP, Felder CC, Fink-Jensen A.

PLoS One. 2015 Apr 16;10(4):e0122722. doi: 10.1371/journal.pone.0122722. eCollection 2015.

18.

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.

19.

M1 and m2 muscarinic receptor subtypes regulate antidepressant-like effects of the rapidly acting antidepressant scopolamine.

Witkin JM, Overshiner C, Li X, Catlow JT, Wishart GN, Schober DA, Heinz BA, Nikolayev A, Tolstikov VV, Anderson WH, Higgs RE, Kuo MS, Felder CC.

J Pharmacol Exp Ther. 2014 Nov;351(2):448-56. doi: 10.1124/jpet.114.216804. Epub 2014 Sep 3.

PMID:
25187432
20.

Development of a radioligand, [(3)H]LY2119620, to probe the human M(2) and M(4) muscarinic receptor allosteric binding sites.

Schober DA, Croy CH, Xiao H, Christopoulos A, Felder CC.

Mol Pharmacol. 2014 Jul;86(1):116-23. doi: 10.1124/mol.114.091785. Epub 2014 May 7.

PMID:
24807966
21.

Characterization of the novel positive allosteric modulator, LY2119620, at the muscarinic M(2) and M(4) receptors.

Croy CH, Schober DA, Xiao H, Quets A, Christopoulos A, Felder CC.

Mol Pharmacol. 2014 Jul;86(1):106-15. doi: 10.1124/mol.114.091751. Epub 2014 May 7.

PMID:
24807965
22.

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
23.

Activation and allosteric modulation of a muscarinic acetylcholine receptor.

Kruse AC, Ring AM, Manglik A, Hu J, Hu K, Eitel K, Hübner H, Pardon E, Valant C, Sexton PM, Christopoulos A, Felder CC, Gmeiner P, Steyaert J, Weis WI, Garcia KC, Wess J, Kobilka BK.

Nature. 2013 Dec 5;504(7478):101-6. doi: 10.1038/nature12735. Epub 2013 Nov 20.

24.

The muscarinic acetylcholine receptor agonist BuTAC mediates antipsychotic-like effects via the M4 subtype.

Watt ML, Rorick-Kehn L, Shaw DB, Knitowski KM, Quets AT, Chesterfield AK, McKinzie DL, Felder CC.

Neuropsychopharmacology. 2013 Dec;38(13):2717-26. doi: 10.1038/npp.2013.186. Epub 2013 Aug 2.

25.

Probe dependence in the allosteric modulation of a G protein-coupled receptor: implications for detection and validation of allosteric ligand effects.

Valant C, Felder CC, Sexton PM, Christopoulos A.

Mol Pharmacol. 2012 Jan;81(1):41-52. doi: 10.1124/mol.111.074872. Epub 2011 Oct 11.

PMID:
21989256
26.

Pharmacological characterization of LY593093, an M1 muscarinic acetylcholine receptor-selective partial orthosteric agonist.

Watt ML, Schober DA, Hitchcock S, Liu B, Chesterfield AK, McKinzie D, Felder CC.

J Pharmacol Exp Ther. 2011 Aug;338(2):622-32. doi: 10.1124/jpet.111.182063. Epub 2011 May 10.

PMID:
21558436
27.

Transmembrane AMPA receptor regulatory proteins and cornichon-2 allosterically regulate AMPA receptor antagonists and potentiators.

Schober DA, Gill MB, Yu H, Gernert DL, Jeffries MW, Ornstein PL, Kato AS, Felder CC, Bredt DS.

J Biol Chem. 2011 Apr 15;286(15):13134-42. doi: 10.1074/jbc.M110.212522. Epub 2011 Feb 22.

28.

The role of transmembrane domain 3 in the actions of orthosteric, allosteric, and atypical agonists of the M4 muscarinic acetylcholine receptor.

Leach K, Davey AE, Felder CC, Sexton PM, Christopoulos A.

Mol Pharmacol. 2011 May;79(5):855-65. doi: 10.1124/mol.111.070938. Epub 2011 Feb 7.

PMID:
21300722
29.

Impact of species variability and 'probe-dependence' on the detection and in vivo validation of allosteric modulation at the M4 muscarinic acetylcholine receptor.

Suratman S, Leach K, Sexton P, Felder C, Loiacono R, Christopoulos A.

Br J Pharmacol. 2011 Apr;162(7):1659-70. doi: 10.1111/j.1476-5381.2010.01184.x.

30.

N-(4-((2-(trifluoromethyl)-3-hydroxy-4-(isobutyryl)phenoxy)methyl)benzyl)-1-methyl-1H-imidazole-4-carboxamide (THIIC), a novel metabotropic glutamate 2 potentiator with potential anxiolytic/antidepressant properties: in vivo profiling suggests a link between behavioral and central nervous system neurochemical changes.

Fell MJ, Witkin JM, Falcone JF, Katner JS, Perry KW, Hart J, Rorick-Kehn L, Overshiner CD, Rasmussen K, Chaney SF, Benvenga MJ, Li X, Marlow DL, Thompson LK, Luecke SK, Wafford KA, Seidel WF, Edgar DM, Quets AT, Felder CC, Wang X, Heinz BA, Nikolayev A, Kuo MS, Mayhugh D, Khilevich A, Zhang D, Ebert PJ, Eckstein JA, Ackermann BL, Swanson SP, Catlow JT, Dean RA, Jackson K, Tauscher-Wisniewski S, Marek GJ, Schkeryantz JM, Svensson KA.

J Pharmacol Exp Ther. 2011 Jan;336(1):165-77. doi: 10.1124/jpet.110.172957. Epub 2010 Oct 14.

PMID:
20947638
31.

Pharmacological characterization of the cannabinoid CB₁ receptor PET ligand ortholog, [³H]MePPEP.

Suter TM, Chesterfield AK, Bao C, Schaus JM, Krushinski JH, Statnick MA, Felder CC.

Eur J Pharmacol. 2010 Dec 15;649(1-3):44-50. doi: 10.1016/j.ejphar.2010.08.055. Epub 2010 Sep 17.

PMID:
20851117
32.

Structural determinants of allosteric agonism and modulation at the M4 muscarinic acetylcholine receptor: identification of ligand-specific and global activation mechanisms.

Nawaratne V, Leach K, Felder CC, Sexton PM, Christopoulos A.

J Biol Chem. 2010 Jun 18;285(25):19012-21. doi: 10.1074/jbc.M110.125096. Epub 2010 Apr 20.

33.

Cortical M1 receptor concentration increases without a concomitant change in function in Alzheimer's disease.

Overk CR, Felder CC, Tu Y, Schober DA, Bales KR, Wuu J, Mufson EJ.

J Chem Neuroanat. 2010 Sep;40(1):63-70. doi: 10.1016/j.jchemneu.2010.03.005. Epub 2010 Mar 27.

34.

Biodistribution and dosimetry in humans of two inverse agonists to image cannabinoid CB1 receptors using positron emission tomography.

Terry GE, Hirvonen J, Liow JS, Seneca N, Tauscher JT, Schaus JM, Phebus L, Felder CC, Morse CL, Pike VW, Halldin C, Innis RB.

Eur J Nucl Med Mol Imaging. 2010 Aug;37(8):1499-506. doi: 10.1007/s00259-010-1411-7. Epub 2010 Mar 24.

35.

Imaging and quantitation of cannabinoid CB1 receptors in human and monkey brains using (18)F-labeled inverse agonist radioligands.

Terry GE, Hirvonen J, Liow JS, Zoghbi SS, Gladding R, Tauscher JT, Schaus JM, Phebus L, Felder CC, Morse CL, Donohue SR, Pike VW, Halldin C, Innis RB.

J Nucl Med. 2010 Jan;51(1):112-20. doi: 10.2967/jnumed.109.067074. Epub 2009 Dec 15.

36.

Molecular mechanisms of action and in vivo validation of an M4 muscarinic acetylcholine receptor allosteric modulator with potential antipsychotic properties.

Leach K, Loiacono RE, Felder CC, McKinzie DL, Mogg A, Shaw DB, Sexton PM, Christopoulos A.

Neuropsychopharmacology. 2010 Mar;35(4):855-69. doi: 10.1038/npp.2009.194. Epub 2009 Nov 25.

37.

Quantitation of cannabinoid CB1 receptors in healthy human brain using positron emission tomography and an inverse agonist radioligand.

Terry GE, Liow JS, Zoghbi SS, Hirvonen J, Farris AG, Lerner A, Tauscher JT, Schaus JM, Phebus L, Felder CC, Morse CL, Hong JS, Pike VW, Halldin C, Innis RB.

Neuroimage. 2009 Nov 1;48(2):362-70. doi: 10.1016/j.neuroimage.2009.06.059. Epub 2009 Jun 30.

38.

Synthesis, ex vivo evaluation, and radiolabeling of potent 1,5-diphenylpyrrolidin-2-one cannabinoid subtype-1 receptor ligands as candidates for in vivo imaging.

Donohue SR, Krushinski JH, Pike VW, Chernet E, Phebus L, Chesterfield AK, Felder CC, Halldin C, Schaus JM.

J Med Chem. 2008 Sep 25;51(18):5833-42. doi: 10.1021/jm800416m.

39.

Allosteric modulation of the muscarinic M4 receptor as an approach to treating schizophrenia.

Chan WY, McKinzie DL, Bose S, Mitchell SN, Witkin JM, Thompson RC, Christopoulos A, Lazareno S, Birdsall NJ, Bymaster FP, Felder CC.

Proc Natl Acad Sci U S A. 2008 Aug 5;105(31):10978-83. doi: 10.1073/pnas.0800567105. Epub 2008 Aug 4.

40.

New insights into the function of M4 muscarinic acetylcholine receptors gained using a novel allosteric modulator and a DREADD (designer receptor exclusively activated by a designer drug).

Nawaratne V, Leach K, Suratman N, Loiacono RE, Felder CC, Armbruster BN, Roth BL, Sexton PM, Christopoulos A.

Mol Pharmacol. 2008 Oct;74(4):1119-31. doi: 10.1124/mol.108.049353. Epub 2008 Jul 15.

PMID:
18628403
41.

Selective muscarinic receptor agonist xanomeline as a novel treatment approach for schizophrenia.

Shekhar A, Potter WZ, Lightfoot J, Lienemann J, Dubé S, Mallinckrodt C, Bymaster FP, McKinzie DL, Felder CC.

Am J Psychiatry. 2008 Aug;165(8):1033-9. doi: 10.1176/appi.ajp.2008.06091591. Epub 2008 Jul 1.

PMID:
18593778
42.

Incensole acetate, an incense component, elicits psychoactivity by activating TRPV3 channels in the brain.

Moussaieff A, Rimmerman N, Bregman T, Straiker A, Felder CC, Shoham S, Kashman Y, Huang SM, Lee H, Shohami E, Mackie K, Caterina MJ, Walker JM, Fride E, Mechoulam R.

FASEB J. 2008 Aug;22(8):3024-34. doi: 10.1096/fj.07-101865. Epub 2008 May 20.

43.

Positron emission tomography imaging using an inverse agonist radioligand to assess cannabinoid CB1 receptors in rodents.

Terry G, Liow JS, Chernet E, Zoghbi SS, Phebus L, Felder CC, Tauscher J, Schaus JM, Pike VW, Halldin C, Innis RB.

Neuroimage. 2008 Jul 1;41(3):690-8. doi: 10.1016/j.neuroimage.2008.03.004. Epub 2008 Mar 18.

44.

Scintillation proximity assay.

Kahl SD, Felder CC.

Curr Protoc Neurosci. 2005 Feb;Chapter 7:Unit 7.15. doi: 10.1002/0471142301.ns0715s30.

PMID:
18428624
45.

The PET radioligand [11C]MePPEP binds reversibly and with high specific signal to cannabinoid CB1 receptors in nonhuman primate brain.

Yasuno F, Brown AK, Zoghbi SS, Krushinski JH, Chernet E, Tauscher J, Schaus JM, Phebus LA, Chesterfield AK, Felder CC, Gladding RL, Hong J, Halldin C, Pike VW, Innis RB.

Neuropsychopharmacology. 2008 Jan;33(2):259-69. Epub 2007 Mar 28.

46.

Cannabinoids biology: the search for new therapeutic targets.

Felder CC, Dickason-Chesterfield AK, Moore SA.

Mol Interv. 2006 Jun;6(3):149-61. Review.

PMID:
16809476
47.

Pharmacological characterization of endocannabinoid transport and fatty acid amide hydrolase inhibitors.

Dickason-Chesterfield AK, Kidd SR, Moore SA, Schaus JM, Liu B, Nomikos GG, Felder CC.

Cell Mol Neurobiol. 2006 Jul-Aug;26(4-6):407-23. Epub 2006 May 31.

PMID:
16736384
48.

Identification of a high-affinity binding site involved in the transport of endocannabinoids.

Moore SA, Nomikos GG, Dickason-Chesterfield AK, Schober DA, Schaus JM, Ying BP, Xu YC, Phebus L, Simmons RM, Li D, Iyengar S, Felder CC.

Proc Natl Acad Sci U S A. 2005 Dec 6;102(49):17852-7. Epub 2005 Nov 28.

49.

Rapid high-energy microwave fixation is required to determine the anandamide (N-arachidonoylethanolamine) concentration of rat brain.

Bazinet RP, Lee HJ, Felder CC, Porter AC, Rapoport SI, Rosenberger TA.

Neurochem Res. 2005 May;30(5):597-601.

PMID:
16176062
50.

Strategic Research Institute G-Protein-Coupled Receptors Drug Discovery World Summit.

Felder CC.

Expert Opin Investig Drugs. 2004 Aug;13(8):1071-4.

PMID:
15268643

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