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Items: 1 to 50 of 79

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 synthesis and evaluation of triazolopyrimidines as anti-tubercular agents.

Zuniga ES, Korkegian A, Mullen S, Hembre EJ, Ornstein PL, Cortez G, Biswas K, Kumar N, Cramer J, Masquelin T, Hipskind PA, Odingo J, Parish T.

Bioorg Med Chem. 2017 Aug 1;25(15):3922-3946. doi: 10.1016/j.bmc.2017.05.030. Epub 2017 May 19.

3.

Preclinical predictors that the orthosteric mGlu2/3 receptor antagonist LY3020371 will not engender ketamine-associated neurotoxic, motor, cognitive, subjective, or abuse-liability-related effects.

Witkin JM, Monn JA, Li J, Johnson B, McKinzie DL, Wang XS, Heinz BA, Li R, Ornstein PL, Smith SC, Mitch CH, Calligaro DO, Swanson S, Allen D, Phillips K, Gilmour G.

Pharmacol Biochem Behav. 2017 Apr;155:43-55. doi: 10.1016/j.pbb.2017.03.001. Epub 2017 Mar 8.

PMID:
28285123
4.

Comparative Effects of LY3020371, a Potent and Selective Metabotropic Glutamate (mGlu) 2/3 Receptor Antagonist, and Ketamine, a Noncompetitive N-Methyl-d-Aspartate Receptor Antagonist in Rodents: Evidence Supporting the Use of mGlu2/3 Antagonists, for the Treatment of Depression.

Witkin JM, Mitchell SN, Wafford KA, Carter G, Gilmour G, Li J, Eastwood BJ, Overshiner C, Li X, Rorick-Kehn L, Rasmussen K, Anderson WH, Nikolayev A, Tolstikov VV, Kuo MS, Catlow JT, Li R, Smith SC, Mitch CH, Ornstein PL, Swanson S, Monn JA.

J Pharmacol Exp Ther. 2017 Apr;361(1):68-86. doi: 10.1124/jpet.116.238121. Epub 2017 Jan 30.

PMID:
28138040
5.

Discovery of (1S,2R,3S,4S,5R,6R)-2-Amino-3-[(3,4-difluorophenyl)sulfanylmethyl]-4-hydroxy-bicyclo[3.1.0]hexane-2,6-dicarboxylic Acid Hydrochloride (LY3020371·HCl): A Potent, Metabotropic Glutamate 2/3 Receptor Antagonist with Antidepressant-Like Activity.

Chappell MD, Li R, Smith SC, Dressman BA, Tromiczak EG, Tripp AE, Blanco MJ, Vetman T, Quimby SJ, Matt J, Britton TC, Fivush AM, Schkeryantz JM, Mayhugh D, Erickson JA, Bures MG, Jaramillo C, Carpintero M, Diego JE, Barberis M, Garcia-Cerrada S, Soriano JF, Antonysamy S, Atwell S, MacEwan I, Condon B, Sougias C, Wang J, Zhang A, Conners K, Groshong C, Wasserman SR, Koss JW, Witkin JM, Li X, Overshiner C, Wafford KA, Seidel W, Wang XS, Heinz BA, Swanson S, Catlow JT, Bedwell DW, Monn JA, Mitch CH, Ornstein PL.

J Med Chem. 2016 Dec 22;59(24):10974-10993. Epub 2016 Dec 6.

PMID:
28002967
6.

Novel bicyclo[3.1.0]hexane analogs as antagonists of metabotropic glutamate 2/3 receptors for the treatment of depression.

Dressman BA, Tromiczak EG, Chappell MD, Tripp AE, Quimby SJ, Vetman T, Fivush AM, Matt J, Jaramillo C, Li R, Khilevich A, Blanco MJ, Smith SC, Carpintero M, de Diego JE, Barberis M, García-Cerrada S, Soriano JF, Schkeryantz JM, Witkin JM, Wafford KA, Seidel W, Britton T, Overshiner CD, Li X, Wang XS, Heinz BA, Catlow JT, Swanson S, Bedwell D, Ornstein PL, Mitch CH.

Bioorg Med Chem Lett. 2016 Dec 1;26(23):5663-5668. doi: 10.1016/j.bmcl.2016.10.067. Epub 2016 Oct 25.

PMID:
27836401
7.

Forebrain-selective AMPA-receptor antagonism guided by TARP γ-8 as an antiepileptic mechanism.

Kato AS, Burris KD, Gardinier KM, Gernert DL, Porter WJ, Reel J, Ding C, Tu Y, Schober DA, Lee MR, Heinz BA, Fitch TE, Gleason SD, Catlow JT, Yu H, Fitzjohn SM, Pasqui F, Wang H, Qian Y, Sher E, Zwart R, Wafford KA, Rasmussen K, Ornstein PL, Isaac JT, Nisenbaum ES, Bredt DS, Witkin JM.

Nat Med. 2016 Dec;22(12):1496-1501. doi: 10.1038/nm.4221. Epub 2016 Nov 7.

PMID:
27820603
8.

Discovery of the First α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptor Antagonist Dependent upon Transmembrane AMPA Receptor Regulatory Protein (TARP) γ-8.

Gardinier KM, Gernert DL, Porter WJ, Reel JK, Ornstein PL, Spinazze P, Stevens FC, Hahn P, Hollinshead SP, Mayhugh D, Schkeryantz J, Khilevich A, De Frutos O, Gleason SD, Kato AS, Luffer-Atlas D, Desai PV, Swanson S, Burris KD, Ding C, Heinz BA, Need AB, Barth VN, Stephenson GA, Diseroad BA, Woods TA, Yu H, Bredt D, Witkin JM.

J Med Chem. 2016 May 26;59(10):4753-68. doi: 10.1021/acs.jmedchem.6b00125. Epub 2016 Apr 29.

PMID:
27067148
9.

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
10.

GluK1 antagonists from 6-(tetrazolyl)phenyl decahydroisoquinoline derivatives: in vitro profile and in vivo analgesic efficacy.

Martinez-Perez JA, Iyengar S, Shannon HE, Bleakman D, Alt A, Clawson DK, Arnold BM, Bell MG, Bleisch TJ, Castaño AM, Del Prado M, Dominguez E, Escribano AM, Filla SA, Ho KH, Hudziak KJ, Jones CK, Mateo A, Mathes BM, Mattiuz EL, Ogden AM, Simmons RM, Stack DR, Stratford RE, Winter MA, Wu Z, Ornstein PL.

Bioorg Med Chem Lett. 2013 Dec 1;23(23):6463-6. doi: 10.1016/j.bmcl.2013.09.045. Epub 2013 Sep 24.

PMID:
24140446
11.

GluK1 antagonists from 6-(carboxy)phenyl decahydroisoquinoline derivatives. SAR and evaluation of a prodrug strategy for oral efficacy in pain models.

Martinez-Perez JA, Iyengar S, Shannon HE, Bleakman D, Alt A, Arnold BM, Bell MG, Bleisch TJ, Castaño AM, Del Prado M, Dominguez E, Escribano AM, Filla SA, Ho KH, Hudziak KJ, Jones CK, Mateo A, Mathes BM, Mattiuz EL, Ogden AM, Simmons RM, Stack DR, Stratford RE, Winter MA, Wu Z, Ornstein PL.

Bioorg Med Chem Lett. 2013 Dec 1;23(23):6459-62. doi: 10.1016/j.bmcl.2013.09.046. Epub 2013 Sep 25.

PMID:
24119554
12.

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.

13.

Anxiolytic-like effects through a GLUK5 kainate receptor mechanism.

Alt A, Weiss B, Ornstein PL, Gleason SD, Bleakman D, Stratford RE Jr, Witkin JM.

Neuropharmacology. 2007 Jun;52(7):1482-7. Epub 2007 Mar 2.

PMID:
17418283
14.

Antiallodynic and antihyperalgesic effects of selective competitive GLUK5 (GluR5) ionotropic glutamate receptor antagonists in the capsaicin and carrageenan models in rats.

Jones CK, Alt A, Ogden AM, Bleakman D, Simmons RM, Iyengar S, Dominguez E, Ornstein PL, Shannon HE.

J Pharmacol Exp Ther. 2006 Oct;319(1):396-404. Epub 2006 Jul 12.

PMID:
16837561
15.

Privileged structure based ligands for melanocortin receptors--4,4-disubstituted piperidine derivatives.

Kuklish SL, Backer RT, Briner K, Doecke CW, Husain S, Mullaney JT, Ornstein PL, Zgombick JM, O'Brien TP, Fisher MJ.

Bioorg Med Chem Lett. 2006 Jul 15;16(14):3843-6. Epub 2006 May 11.

PMID:
16697186
16.

Pharmacological characterization of the competitive GLUK5 receptor antagonist decahydroisoquinoline LY466195 in vitro and in vivo.

Weiss B, Alt A, Ogden AM, Gates M, Dieckman DK, Clemens-Smith A, Ho KH, Jarvie K, Rizkalla G, Wright RA, Calligaro DO, Schoepp D, Mattiuz EL, Stratford RE, Johnson B, Salhoff C, Katofiasc M, Phebus LA, Schenck K, Cohen M, Filla SA, Ornstein PL, Johnson KW, Bleakman D.

J Pharmacol Exp Ther. 2006 Aug;318(2):772-81. Epub 2006 May 11.

PMID:
16690725
17.

Privileged structure based ligands for melanocortin-4 receptors--aliphatic piperazine derivatives.

Briner K, Collado I, Fisher MJ, García-Paredes C, Husain S, Kuklish SL, Mateo AI, O'Brien TP, Ornstein PL, Zgombick J, de Frutos O.

Bioorg Med Chem Lett. 2006 Jul 1;16(13):3449-53. Epub 2006 May 2.

PMID:
16650763
18.

Synthesis and structure-activity relationships of novel dipeptides and reduced dipeptides as ligands for melanocortin subtype-4 receptor.

Shi Q, Ornstein PL, Briner K, Richardson TI, Arnold MB, Backer RT, Buckmaster JL, Canada EJ, Doecke CW, Hertel LW, Honigschmidt N, Hsiung HM, Husain S, Kuklish SL, Martinelli MJ, Mullaney JT, O'Brien TP, Reinhard MR, Rothhaar R, Shah J, Wu Z, Xie C, Zgombick JM, Fisher MJ.

Bioorg Med Chem Lett. 2006 May 1;16(9):2341-6. Epub 2005 Nov 15.

PMID:
16297618
19.

Privileged structure based ligands for melanocortin receptors--substituted benzylic piperazine derivatives.

Fisher MJ, Backer RT, Collado I, de Frutos O, Husain S, Hsiung HM, Kuklish SL, Mateo AI, Mullaney JT, Ornstein PL, Paredes CG, O'Brian TP, Richardson TI, Shah J, Zgombick JM, Briner K.

Bioorg Med Chem Lett. 2005 Nov 15;15(22):4973-8.

PMID:
16169215
20.

Privileged structure-based ligands for melanocortin receptors-tetrahydroquinolines, indoles, and aminotetralines.

Fisher MJ, Backer RT, Husain S, Hsiung HM, Mullaney JT, O'Brian TP, Ornstein PL, Rothhaar RR, Zgombick JM, Briner K.

Bioorg Med Chem Lett. 2005 Oct 15;15(20):4459-62.

PMID:
16112861
21.

Two prodrugs of potent and selective GluR5 kainate receptor antagonists actives in three animal models of pain.

Dominguez E, Iyengar S, Shannon HE, Bleakman D, Alt A, Arnold BM, Bell MG, Bleisch TJ, Buckmaster JL, Castano AM, Del Prado M, Escribano A, Filla SA, Ho KH, Hudziak KJ, Jones CK, Martinez-Perez JA, Mateo A, Mathes BM, Mattiuz EL, Ogden AM, Simmons RM, Stack DR, Stratford RE, Winter MA, Wu Z, Ornstein PL.

J Med Chem. 2005 Jun 30;48(13):4200-3.

PMID:
15974569
22.

Locomotor activity detects subunit-selective effects of agonists and decahydroisoquinoline antagonists at AMPA/kainic acid ionotropic glutamate receptors in adult rats.

O'neill MF, Sanger G, Ornstein PL, Osborne DJ, Woodhouse SM.

Psychopharmacology (Berl). 2005 Apr;179(1):181-8. Epub 2005 Jan 26.

PMID:
15821949
23.

LY293558, a novel AMPA/GluR5 antagonist, is efficacious and well-tolerated in acute migraine.

Sang CN, Ramadan NM, Wallihan RG, Chappell AS, Freitag FG, Smith TR, Silberstein SD, Johnson KW, Phebus LA, Bleakman D, Ornstein PL, Arnold B, Tepper SJ, Vandenhende F.

Cephalalgia. 2004 Jul;24(7):596-602.

PMID:
15196302
24.

Synthesis and structure-activity relationships of novel arylpiperazines as potent and selective agonists of the melanocortin subtype-4 receptor.

Richardson TI, Ornstein PL, Briner K, Fisher MJ, Backer RT, Biggers CK, Clay MP, Emmerson PJ, Hertel LW, Hsiung HM, Husain S, Kahl SD, Lee JA, Lindstrom TD, Martinelli MJ, Mayer JP, Mullaney JT, O'Brien TP, Pawlak JM, Revell KD, Shah J, Zgombick JM, Herr RJ, Melekhov A, Sampson PB, King CH.

J Med Chem. 2004 Jan 29;47(3):744-55.

PMID:
14736255
25.

A role for Ca2+ stores in kainate receptor-dependent synaptic facilitation and LTP at mossy fiber synapses in the hippocampus.

Lauri SE, Bortolotto ZA, Nistico R, Bleakman D, Ornstein PL, Lodge D, Isaac JT, Collingridge GL.

Neuron. 2003 Jul 17;39(2):327-41.

26.

Synthesis and structure-activity relationship studies of novel 2-diarylethyl substituted (2-carboxycycloprop-1-yl)glycines as high-affinity group II metabotropic glutamate receptor ligands.

Sørensen US, Bleisch TJ, Kingston AE, Wright RA, Johnson BG, Schoepp DD, Ornstein PL.

Bioorg Med Chem. 2003 Jan 17;11(2):197-205.

PMID:
12470714
27.

Ethyl (3S,4aR,6S,8aR)-6-(4-ethoxycar- bonylimidazol-1-ylmethyl)decahydroiso-quinoline-3-carboxylic ester: a prodrug of a GluR5 kainate receptor antagonist active in two animal models of acute migraine.

Filla SA, Winter MA, Johnson KW, Bleakman D, Bell MG, Bleisch TJ, Castaño AM, Clemens-Smith A, del Prado M, Dieckman DK, Dominguez E, Escribano A, Ho KH, Hudziak KJ, Katofiasc MA, Martinez-Perez JA, Mateo A, Mathes BM, Mattiuz EL, Ogden AM, Phebus LA, Stack DR, Stratford RE, Ornstein PL.

J Med Chem. 2002 Sep 26;45(20):4383-6.

PMID:
12238915
28.

Antagonists of GLU(K5)-containing kainate receptors prevent pilocarpine-induced limbic seizures.

Smolders I, Bortolotto ZA, Clarke VR, Warre R, Khan GM, O'Neill MJ, Ornstein PL, Bleakman D, Ogden A, Weiss B, Stables JP, Ho KH, Ebinger G, Collingridge GL, Lodge D, Michotte Y.

Nat Neurosci. 2002 Aug;5(8):796-804.

PMID:
12080343
29.

Synaptic activation of a presynaptic kainate receptor facilitates AMPA receptor-mediated synaptic transmission at hippocampal mossy fibre synapses.

Lauri SE, Delany C, J Clarke VR, Bortolotto ZA, Ornstein PL, T R Isaac J, Collingridge GL.

Neuropharmacology. 2001 Dec;41(8):907-15.

PMID:
11747895
30.

A critical role of a facilitatory presynaptic kainate receptor in mossy fiber LTP.

Lauri SE, Bortolotto ZA, Bleakman D, Ornstein PL, Lodge D, Isaac JT, Collingridge GL.

Neuron. 2001 Nov 20;32(4):697-709.

31.

[3H]N-2-(4-(N-benzamido)phenyl)propyl-2-propanesulfonamide: a novel AMPA receptor potentiator and radioligand.

Zarrinmayeh H, Bleakman D, Gates MR, Yu H, Zimmerman DM, Ornstein PL, McKennon T, Arnold MB, Wheeler WJ, Skolnick P.

J Med Chem. 2001 Feb 1;44(3):302-4. No abstract available.

PMID:
11462971
32.

[3H]LY341495 binding to group II metabotropic glutamate receptors in rat brain.

Wright RA, Arnold MB, Wheeler WJ, Ornstein PL, Schoepp DD.

J Pharmacol Exp Ther. 2001 Aug;298(2):453-60.

PMID:
11454905
33.

Novel AMPA receptor potentiators LY392098 and LY404187: effects on recombinant human AMPA receptors in vitro.

Miu P, Jarvie KR, Radhakrishnan V, Gates MR, Ogden A, Ornstein PL, Zarrinmayeh H, Ho K, Peters D, Grabell J, Gupta A, Zimmerman DM, Bleakman D.

Neuropharmacology. 2001 Jun;40(8):976-83.

PMID:
11406188
34.
35.

Biarylpropylsulfonamides as novel, potent potentiators of 2-amino-3- (5-methyl-3-hydroxyisoxazol-4-yl)- propanoic acid (AMPA) receptors.

Ornstein PL, Zimmerman DM, Arnold MB, Bleisch TJ, Cantrell B, Simon R, Zarrinmayeh H, Baker SR, Gates M, Tizzano JP, Bleakman D, Mandelzys A, Jarvie KR, Ho K, Deverill M, Kamboj RK.

J Med Chem. 2000 Nov 16;43(23):4354-8. No abstract available.

PMID:
11087558
36.

A novel, competitive mGlu(5) receptor antagonist (LY344545) blocks DHPG-induced potentiation of NMDA responses but not the induction of LTP in rat hippocampal slices.

Doherty AJ, Palmer MJ, Bortolotto ZA, Hargreaves A, Kingston AE, Ornstein PL, Schoepp DD, Lodge D, Collingridge GL.

Br J Pharmacol. 2000 Sep;131(2):239-44.

37.

Neuroprotective effects of LY379268, a selective mGlu2/3 receptor agonist: investigations into possible mechanism of action in vivo.

Bond A, Jones NM, Hicks CA, Whiffin GM, Ward MA, O'Neill MF, Kingston AE, Monn JA, Ornstein PL, Schoepp DD, Lodge D, O'Neill MJ.

J Pharmacol Exp Ther. 2000 Sep;294(3):800-9.

PMID:
10945827
38.

LY377770, a novel iGlu5 kainate receptor antagonist with neuroprotective effects in global and focal cerebral ischaemia.

O'Neill MJ, Bogaert L, Hicks CA, Bond A, Ward MA, Ebinger G, Ornstein PL, Michotte Y, Lodge D.

Neuropharmacology. 2000 Jul 10;39(9):1575-88.

PMID:
10854902
39.

Kainate receptors are involved in synaptic plasticity.

Bortolotto ZA, Clarke VR, Delany CM, Parry MC, Smolders I, Vignes M, Ho KH, Miu P, Brinton BT, Fantaske R, Ogden A, Gates M, Ornstein PL, Lodge D, Bleakman D, Collingridge GL.

Nature. 1999 Nov 18;402(6759):297-301.

PMID:
10580501
40.
41.

Pharmacological characterization of a GluR6 kainate receptor in cultured hippocampal neurons.

Bleakman D, Ogden AM, Ornstein PL, Hoo K.

Eur J Pharmacol. 1999 Aug 13;378(3):331-7.

PMID:
10493110
42.

Structure-activity relationship of a series of diaminoalkyl substituted benzimidazole as neuropeptide Y Y1 receptor antagonists.

Zarrinmayeh H, Zimmerman DM, Cantrell BE, Schober DA, Bruns RF, Gackenheimer SL, Ornstein PL, Hipskind PA, Britton TC, Gehlert DR.

Bioorg Med Chem Lett. 1999 Mar 8;9(5):647-52.

PMID:
10201822
43.

The potent mGlu receptor antagonist LY341495 identifies roles for both cloned and novel mGlu receptors in hippocampal synaptic plasticity.

Fitzjohn SM, Bortolotto ZA, Palmer MJ, Doherty AJ, Ornstein PL, Schoepp DD, Kingston AE, Lodge D, Collingridge GL.

Neuropharmacology. 1998 Dec;37(12):1445-58.

PMID:
9886667
44.

[3H]LY341495, a highly potent, selective and novel radioligand for labeling Group II metabotropic glutamate receptors.

Ornstein PL, Arnold MB, Bleisch TJ, Wright RA, Wheeler WJ, Schoepp DD.

Bioorg Med Chem Lett. 1998 Jul 21;8(14):1919-22.

PMID:
9873459
45.

Heteroatom-substitution as a strategy for increasing the potency of competitive NMDA antagonists.

Ornstein PL, Arnold MB, Lunn WH, Heinz LJ, Leander JD, Lodge D, Schoepp DD.

Bioorg Med Chem Lett. 1998 Feb 17;8(4):389-94.

PMID:
9871691
46.

Structure-activity relationships of a series of 1-substituted-4-methylbenzimidazole neuropeptide Y-1 receptor antagonists.

Zimmerman DM, Cantrell BE, Smith EC, Nixon JA, Bruns RF, Gitter B, Hipskind PA, Ornstein PL, Zarrinmayeh H, Britton TC, Schober DA, Gehlert DR.

Bioorg Med Chem Lett. 1998 Mar 3;8(5):473-6.

PMID:
9871601
47.

Actions of kainate and AMPA selective glutamate receptor ligands on nociceptive processing in the spinal cord.

Procter MJ, Houghton AK, Faber ES, Chizh BA, Ornstein PL, Lodge D, Headley PM.

Neuropharmacology. 1998 Oct-Nov;37(10-11):1287-97.

PMID:
9849666
48.

The GluR5 subtype of kainate receptor regulates excitatory synaptic transmission in areas CA1 and CA3 of the rat hippocampus.

Vignes M, Clarke VR, Parry MJ, Bleakman D, Lodge D, Ornstein PL, Collingridge GL.

Neuropharmacology. 1998 Oct-Nov;37(10-11):1269-77.

PMID:
9849664
49.

Decahydroisoquinolines: novel competitive AMPA/kainate antagonists with neuroprotective effects in global cerebral ischaemia.

O'Neill MJ, Bond A, Ornstein PL, Ward MA, Hicks CA, Hoo K, Bleakman D, Lodge D.

Neuropharmacology. 1998 Oct-Nov;37(10-11):1211-22.

PMID:
9849659
50.

Kainate GluR5 receptor subtype mediates the nociceptive response to formalin in the rat.

Simmons RM, Li DL, Hoo KH, Deverill M, Ornstein PL, Iyengar S.

Neuropharmacology. 1998;37(1):25-36.

PMID:
9680256

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