Paul L Ornstein, Ph.D. - Publications

Affiliations: 
1984-2012 Discovery Chemistry Eli Lilly & Co 
 2012-2017 College of Pharmacy Roosevelt University, Chicago, IL, United States 
 2016- Apollod Drug Discovery Consulting 
 2017-2019 School of Pharmacy Medical College of Wisconsin, Millwauke, Wauwatosa, WI, United States 
Area:
Excitatory Amino Acids

98 high-probability publications. We are testing a new system for linking publications to authors. You can help! If you notice any inaccuracies, please sign in and mark papers as correct or incorrect matches. If you identify any major omissions or other inaccuracies in the publication list, please let us know.

Year Citation  Score
2021 Hembre E, Early JV, Odingo J, Shelton C, Anoshchenko O, Guzman J, Flint L, Dennison D, McNeil MB, Korkegian A, Ovechkina Y, Ornstein P, Masquelin T, Hipskind PA, Parish T. Novel Trifluoromethyl Pyrimidinone Compounds With Activity Against . Frontiers in Chemistry. 9: 613349. PMID 33996738 DOI: 10.3389/fchem.2021.613349  0.651
2019 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, et al. Modulation of TARP γ8-containing AMPA Receptors as a Novel Therapeutic Approach for Chronic Pain. The Journal of Pharmacology and Experimental Therapeutics. PMID 30910921 DOI: 10.1124/Jpet.118.250126  0.399
2017 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. The synthesis and evaluation of triazolopyrimidines as anti-tubercular agents. Bioorganic & Medicinal Chemistry. PMID 28576632 DOI: 10.1016/J.Bmc.2017.05.030  0.665
2017 Witkin JM, Mitchell S, Wafford K, Carter G, Gilmour G, Li J, Eastwood B, Overshiner C, Li X, Rorick-Kehn L, Rasmussen K, Anderson W, Nikolayev A, Tolstikov V, Kuo MS, ... ... Ornstein P, et al. Comparative Effects of LY3020371, a Potent and Selective mGlu2/3 Receptor Antagonist, and Ketamine, a Non-Competitive NMDA Receptor Antagonist, in Rodents: Evidence Supporting Use for the Treatment of Depression. The Journal of Pharmacology and Experimental Therapeutics. PMID 28138040 DOI: 10.1124/Jpet.116.238121  0.43
2016 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, ... ... Ornstein PL, et al. 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. Journal of Medicinal Chemistry. 59: 10974-10993. PMID 28002967 DOI: 10.1021/Acs.Jmedchem.6B01119  0.404
2016 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, ... ... Ornstein PL, et al. Novel bicyclo[3.1.0]hexane analogs as antagonists of metabotropic glutamate 2/3 receptors for the treatment of depression. Bioorganic & Medicinal Chemistry Letters. PMID 27836401 DOI: 10.1016/J.Bmcl.2016.10.067  0.474
2016 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, ... ... Ornstein PL, et al. Forebrain-selective AMPA-receptor antagonism guided by TARP γ-8 as an antiepileptic mechanism. Nature Medicine. PMID 27820603 DOI: 10.1038/Nm.4221  0.439
2016 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, et al. The Discovery of The First α-Amino-3-Hydroxy-5-Methyl-4-Isoxazolepropionic Acid (AMPA) Receptor Antagonist Dependent Upon Transmembrane AMPA Receptor Regulatory Protein (TARP) Gamma-8. Journal of Medicinal Chemistry. PMID 27067148 DOI: 10.1021/Acs.Jmedchem.6B00125  0.475
2015 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, et al. In Vitro Pharmacological and Rat Pharmacokinetic Characterization of LY3020371, a Potent and Selective mGlu2/3 Receptor Antagonist. Neuropharmacology. PMID 26748052 DOI: 10.1016/J.Neuropharm.2015.12.021  0.46
2013 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, ... ... Ornstein PL, et al. GluK1 antagonists from 6-(tetrazolyl)phenyl decahydroisoquinoline derivatives: in vitro profile and in vivo analgesic efficacy. Bioorganic & Medicinal Chemistry Letters. 23: 6463-6. PMID 24140446 DOI: 10.1016/J.Bmcl.2013.09.045  0.437
2013 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, ... ... Ornstein PL, et al. GluK1 antagonists from 6-(carboxy)phenyl decahydroisoquinoline derivatives. SAR and evaluation of a prodrug strategy for oral efficacy in pain models. Bioorganic & Medicinal Chemistry Letters. 23: 6459-62. PMID 24119554 DOI: 10.1016/J.Bmcl.2013.09.046  0.397
2011 Schober DA, Gill MB, Yu H, Gernert DL, Jeffries MW, Ornstein PL, Kato AS, Felder CC, Bredt DS. Transmembrane AMPA receptor regulatory proteins and cornichon-2 allosterically regulate AMPA receptor antagonists and potentiators. The Journal of Biological Chemistry. 286: 13134-42. PMID 21343286 DOI: 10.1074/Jbc.M110.212522  0.433
2010 ORNSTEIN PL, ARNOLD MB, ALLEN NK, BLEISCH T, BORROMEO PS, LUGAR CW, LEANDER JD, LODGE D, SCHOEPP DD. ChemInform Abstract: Structure-Activity Studies of 6-(Tetrazolylalkyl)-Substituted Decahydroisoquinoline-3-carboxylic Acid AMPA Receptor Antagonists. Part 1. Effects of Stereochemistry, Chain Length, and Chain Substitution. Cheminform. 27: no-no. DOI: 10.1002/CHIN.199637201  0.313
2010 ORNSTEIN PL, ARNOLD MB, ALLEN NK, LEANDER JD, TIZZANO JP, LODGE D, SCHOEPP DD. ChemInform Abstract: (3SR,4aRS,6SR,8aRS)-6-(1H-Tetrazol-5-yl)decahydroisoquinoline-3- carboxylic Acid, a Novel, Competitive, Systemically Active NMDA, and AMPA Receptor Antagonist. Cheminform. 27: no-no. DOI: 10.1002/CHIN.199616173  0.356
2007 Alt A, Weiss B, Ornstein PL, Gleason SD, Bleakman D, Stratford RE, Witkin JM. Anxiolytic-like effects through a GLUK5 kainate receptor mechanism. Neuropharmacology. 52: 1482-7. PMID 17418283 DOI: 10.1016/J.Neuropharm.2007.02.005  0.449
2006 Jones CK, Alt A, Ogden AM, Bleakman D, Simmons RM, Iyengar S, Dominguez E, Ornstein PL, Shannon HE. Antiallodynic and antihyperalgesic effects of selective competitive GLUK5 (GluR5) ionotropic glutamate receptor antagonists in the capsaicin and carrageenan models in rats. The Journal of Pharmacology and Experimental Therapeutics. 319: 396-404. PMID 16837561 DOI: 10.1124/Jpet.106.105601  0.493
2006 Kuklish SL, Backer RT, Briner K, Doecke CW, Husain S, Mullaney JT, Ornstein PL, Zgombick JM, O'Brien TP, Fisher MJ. Privileged structure based ligands for melanocortin receptors--4,4-disubstituted piperidine derivatives. Bioorganic & Medicinal Chemistry Letters. 16: 3843-6. PMID 16697186 DOI: 10.1016/J.Bmcl.2006.04.016  0.414
2006 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, ... ... Ornstein PL, et al. Pharmacological characterization of the competitive GLUK5 receptor antagonist decahydroisoquinoline LY466195 in vitro and in vivo. The Journal of Pharmacology and Experimental Therapeutics. 318: 772-81. PMID 16690725 DOI: 10.1124/Jpet.106.101428  0.438
2006 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. Privileged structure based ligands for melanocortin-4 receptors--aliphatic piperazine derivatives. Bioorganic & Medicinal Chemistry Letters. 16: 3449-53. PMID 16650763 DOI: 10.1016/J.Bmcl.2006.04.002  0.398
2006 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, et al. Synthesis and structure-activity relationships of novel dipeptides and reduced dipeptides as ligands for melanocortin subtype-4 receptor. Bioorganic & Medicinal Chemistry Letters. 16: 2341-6. PMID 16297618 DOI: 10.1016/J.Bmcl.2005.10.103  0.396
2005 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, et al. Privileged structure based ligands for melanocortin receptors--substituted benzylic piperazine derivatives. Bioorganic & Medicinal Chemistry Letters. 15: 4973-8. PMID 16169215 DOI: 10.1016/J.Bmcl.2005.08.018  0.456
2005 Fisher MJ, Backer RT, Husain S, Hsiung HM, Mullaney JT, O'Brian TP, Ornstein PL, Rothhaar RR, Zgombick JM, Briner K. Privileged structure-based ligands for melanocortin receptors-tetrahydroquinolines, indoles, and aminotetralines. Bioorganic & Medicinal Chemistry Letters. 15: 4459-62. PMID 16112861 DOI: 10.1016/J.Bmcl.2005.07.035  0.405
2005 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, ... ... Ornstein PL, et al. Two prodrugs of potent and selective GluR5 kainate receptor antagonists actives in three animal models of pain. Journal of Medicinal Chemistry. 48: 4200-3. PMID 15974569 DOI: 10.1021/Jm0491952  0.457
2005 O'neill MF, Sanger G, Ornstein PL, Osborne DJ, Woodhouse SM. Locomotor activity detects subunit-selective effects of agonists and decahydroisoquinoline antagonists at AMPA/kainic acid ionotropic glutamate receptors in adult rats. Psychopharmacology. 179: 181-8. PMID 15821949 DOI: 10.1007/S00213-004-2055-8  0.501
2004 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. LY293558, a novel AMPA/GluR5 antagonist, is efficacious and well-tolerated in acute migraine. Cephalalgia : An International Journal of Headache. 24: 596-602. PMID 15196302 DOI: 10.1111/J.1468-2982.2004.00723.X  0.319
2004 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, et al. Synthesis and structure-activity relationships of novel arylpiperazines as potent and selective agonists of the melanocortin subtype-4 receptor. Journal of Medicinal Chemistry. 47: 744-55. PMID 14736255 DOI: 10.1021/Jm0304109  0.424
2003 O'Neill MF, Heron-Maxwell C, Conway MW, Monn JA, Ornstein P. Group II metabotropic glutamate receptor antagonists LY341495 and LY366457 increase locomotor activity in mice. Neuropharmacology. 45: 565-74. PMID 12941370 DOI: 10.1016/S0028-3908(03)00232-6  0.41
2003 Lauri SE, Bortolotto ZA, Nistico R, Bleakman D, Ornstein PL, Lodge D, Isaac JT, Collingridge GL. A role for Ca2+ stores in kainate receptor-dependent synaptic facilitation and LTP at mossy fiber synapses in the hippocampus. Neuron. 39: 327-41. PMID 12873388 DOI: 10.1016/S0896-6273(03)00369-6  0.317
2003 Sørensen US, Bleisch TJ, Kingston AE, Wright RA, Johnson BG, Schoepp DD, Ornstein PL. 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. Bioorganic & Medicinal Chemistry. 11: 197-205. PMID 12470714 DOI: 10.1016/S0968-0896(02)00387-5  0.477
2002 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, ... ... Ornstein PL, et al. 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. Journal of Medicinal Chemistry. 45: 4383-6. PMID 12238915 DOI: 10.1021/Jm025548Q  0.459
2002 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, et al. Antagonists of GLU(K5)-containing kainate receptors prevent pilocarpine-induced limbic seizures. Nature Neuroscience. 5: 796-804. PMID 12080343 DOI: 10.1038/Nn880  0.396
2002 Bessières B, Schoenfelder A, Verrat C, Mann A, Ornstein P, Pedregal C. Synthesis of constrained cycloalkyl analogues of glutamic acid with an ω-phosphonic acid function Tetrahedron Letters. 43: 7659-7662. DOI: 10.1016/S0040-4039(02)01858-0  0.359
2001 Lauri SE, Delany C, J Clarke VR, Bortolotto ZA, Ornstein PL, T R Isaac J, Collingridge GL. Synaptic activation of a presynaptic kainate receptor facilitates AMPA receptor-mediated synaptic transmission at hippocampal mossy fibre synapses. Neuropharmacology. 41: 907-15. PMID 11747895 DOI: 10.1016/S0028-3908(01)00152-6  0.41
2001 Lauri SE, Bortolotto ZA, Bleakman D, Ornstein PL, Lodge D, Isaac JT, Collingridge GL. A critical role of a facilitatory presynaptic kainate receptor in mossy fiber LTP. Neuron. 32: 697-709. PMID 11719209 DOI: 10.1016/S0896-6273(01)00511-6  0.368
2001 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. Novel AMPA receptor potentiators LY392098 and LY404187: effects on recombinant human AMPA receptors in vitro. Neuropharmacology. 40: 976-83. PMID 11406188 DOI: 10.1016/S0028-3908(01)00027-2  0.446
2001 Bortolotto ZA, Clarke VRJ, 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, et al. Erratum: correction: Kainate receptors are involved in synaptic plasticity Nature. 409: 542-542. DOI: 10.1038/35054109  0.419
2000 Wright RA, Arnold MB, Wheeler WJ, Ornstein PL, Schoepp DD. Binding of [3H](2S,1'S,2'S)-2-(9-xanthylmethyl)-2-(2'-carboxycyclopropyl) glycine ([3H]LY341495) to cell membranes expressing recombinant human group III metabotropic glutamate receptor subtypes. Naunyn-Schmiedeberg's Archives of Pharmacology. 362: 546-54. PMID 11138847 DOI: 10.1007/S002100000305  0.398
2000 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, et al. Biarylpropylsulfonamides as novel, potent potentiators of 2-amino-3- (5-methyl-3-hydroxyisoxazol-4-yl)- propanoic acid (AMPA) receptors. Journal of Medicinal Chemistry. 43: 4354-8. PMID 11087558 DOI: 10.1021/jm0002836  0.374
2000 Doherty AJ, Palmer MJ, Bortolotto ZA, Hargreaves A, Kingston AE, Ornstein PL, Schoepp DD, Lodge D, Collingridge GL. 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. British Journal of Pharmacology. 131: 239-44. PMID 10991916 DOI: 10.1038/Sj.Bjp.0703574  0.47
2000 O'Neill MJ, Bogaert L, Hicks CA, Bond A, Ward MA, Ebinger G, Ornstein PL, Michotte Y, Lodge D. LY377770, a novel iGlu5 kainate receptor antagonist with neuroprotective effects in global and focal cerebral ischaemia. Neuropharmacology. 39: 1575-88. PMID 10854902 DOI: 10.1016/S0028-3908(99)00250-6  0.343
1999 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, et al. Kainate receptors are involved in synaptic plasticity. Nature. 402: 297-301. PMID 10580501 DOI: 10.1038/46290  0.448
1999 Johnson BG, Wright RA, Arnold MB, Wheeler WJ, Ornstein PL, Schoepp DD. [3H]-LY341495 as a novel antagonist radioligand for group II metabotropic glutamate (mGlu) receptors: characterization of binding to membranes of mGlu receptor subtype expressing cells. Neuropharmacology. 38: 1519-29. PMID 10530814 DOI: 10.1016/S0028-3908(99)00053-2  0.4
1999 Bleakman D, Ogden AM, Ornstein PL, Hoo K. Pharmacological characterization of a GluR6 kainate receptor in cultured hippocampal neurons. European Journal of Pharmacology. 378: 331-7. PMID 10493110 DOI: 10.1016/S0014-2999(99)00478-1  0.454
1999 Zarrinmayeh H, Zimmerman DM, Cantrell BE, Schober DA, Bruns RF, Gackenheimer SL, Ornstein PL, Hipskind PA, Britton TC, Gehlert DR. Structure-activity relationship of a series of diaminoalkyl substituted benzimidazole as neuropeptide Y Y1 receptor antagonists. Bioorganic & Medicinal Chemistry Letters. 9: 647-52. PMID 10201822 DOI: 10.1016/S0960-894X(99)00082-7  0.453
1999 Schoepp DD, Cartmell J, Johnson BG, Wright RA, Andis S, Salhoff CR, Tizzano JP, Ornstein PL, Monn JA. Development of metabotropic glutamate receptor subtype selective drugs European Neuropsychopharmacology. 9: 204-205. DOI: 10.1016/S0924-977X(99)80109-6  0.399
1999 Siegel MG, Chaney MO, Bruns RF, Clay MP, Schober DA, Van Abbema AM, Johnson DW, Cantrell BE, Hahn PJ, Hunden DC, Gehlert DR, Zarrinmayeh H, Ornstein PL, Zimmerman DM, Koppel GA. Rapid parallel synthesis applied to the optimization of a series of potent nonpeptide neuropeptide Y-1 receptor antagonists Tetrahedron. 55: 11619-11639. DOI: 10.1016/S0040-4020(99)00683-3  0.457
1998 Fitzjohn SM, Bortolotto ZA, Palmer MJ, Doherty AJ, Ornstein PL, Schoepp DD, Kingston AE, Lodge D, Collingridge GL. The potent mGlu receptor antagonist LY341495 identifies roles for both cloned and novel mGlu receptors in hippocampal synaptic plasticity. Neuropharmacology. 37: 1445-58. PMID 9886667 DOI: 10.1016/S0028-3908(98)00145-2  0.476
1998 Ornstein PL, Arnold MB, Bleisch TJ, Wright RA, Wheeler WJ, Schoepp DD. [3H]LY341495, a highly potent, selective and novel radioligand for labeling Group II metabotropic glutamate receptors. Bioorganic & Medicinal Chemistry Letters. 8: 1919-22. PMID 9873459 DOI: 10.1016/S0960-894X(98)00329-1  0.448
1998 Ornstein PL, Arnold MB, Lunn WH, Heinz LJ, Leander JD, Lodge D, Schoepp DD. Heteroatom-substitution as a strategy for increasing the potency of competitive NMDA antagonists. Bioorganic & Medicinal Chemistry Letters. 8: 389-94. PMID 9871691 DOI: 10.1016/S0960-894X(98)00038-9  0.522
1998 Zimmerman DM, Cantrell BE, Smith EC, Nixon JA, Bruns RF, Gitter B, Hipskind PA, Ornstein PL, Zarrinmayeh H, Britton TC, Schober DA, Gehlert DR. Structure-activity relationships of a series of 1-substituted-4-methylbenzimidazole neuropeptide Y-1 receptor antagonists. Bioorganic & Medicinal Chemistry Letters. 8: 473-6. PMID 9871601 DOI: 10.1016/S0960-894X(98)00048-1  0.474
1998 Procter MJ, Houghton AK, Faber ES, Chizh BA, Ornstein PL, Lodge D, Headley PM. Actions of kainate and AMPA selective glutamate receptor ligands on nociceptive processing in the spinal cord. Neuropharmacology. 37: 1287-97. PMID 9849666 DOI: 10.1016/S0028-3908(98)00136-1  0.416
1998 Vignes M, Clarke VR, Parry MJ, Bleakman D, Lodge D, Ornstein PL, Collingridge GL. The GluR5 subtype of kainate receptor regulates excitatory synaptic transmission in areas CA1 and CA3 of the rat hippocampus. Neuropharmacology. 37: 1269-77. PMID 9849664 DOI: 10.1016/S0028-3908(98)00148-8  0.4
1998 O'Neill MJ, Bond A, Ornstein PL, Ward MA, Hicks CA, Hoo K, Bleakman D, Lodge D. Decahydroisoquinolines: novel competitive AMPA/kainate antagonists with neuroprotective effects in global cerebral ischaemia. Neuropharmacology. 37: 1211-22. PMID 9849659 DOI: 10.1016/S0028-3908(98)00134-8  0.513
1998 Simmons RM, Li DL, Hoo KH, Deverill M, Ornstein PL, Iyengar S. Kainate GluR5 receptor subtype mediates the nociceptive response to formalin in the rat. Neuropharmacology. 37: 25-36. PMID 9680256 DOI: 10.1016/S0028-3908(97)00188-3  0.456
1998 Kingston AE, Ornstein PL, Wright RA, Johnson BG, Mayne NG, Burnett JP, Belagaje R, Wu S, Schoepp DD. LY341495 is a nanomolar potent and selective antagonist of group II metabotropic glutamate receptors. Neuropharmacology. 37: 1-12. PMID 9680254 DOI: 10.1016/S0028-3908(97)00191-3  0.489
1998 Zarrinmayeh H, Nunes AM, Ornstein PL, Zimmerman DM, Arnold MB, Schober DA, Gackenheimer SL, Bruns RF, Hipskind PA, Britton TC, Cantrell BE, Gehlert DR. Synthesis and evaluation of a series of novel 2-[(4-chlorophenoxy)methyl]benzimidazoles as selective neuropeptide Y Y1 receptor antagonists. Journal of Medicinal Chemistry. 41: 2709-19. PMID 9667962 DOI: 10.1021/jm9706630  0.396
1998 Ornstein PL, Bleisch TJ, Arnold MB, Kennedy JH, Wright RA, Johnson BG, Tizzano JP, Helton DR, Kallman MJ, Schoepp DD, Hérin M. 2-substituted (2SR)-2-amino-2-((1SR,2SR)-2-carboxycycloprop-1-yl)glycines as potent and selective antagonists of group II metabotropic glutamate receptors. 2. Effects of aromatic substitution, pharmacological characterization, and bioavailability. Journal of Medicinal Chemistry. 41: 358-78. PMID 9464367 DOI: 10.1021/Jm970498O  0.488
1998 Ornstein PL, Bleisch TJ, Arnold MB, Wright RA, Johnson BG, Schoepp DD. 2-Substituted (2SR)-2-amino-2-((1SR,2SR)-2-carboxycycloprop-1-yl)glycines as potent and selective antagonists of group II metabotropic glutamate receptors. 1. Effects of alkyl, arylalkyl, and diarylalkyl substitution. Journal of Medicinal Chemistry. 41: 346-57. PMID 9464366 DOI: 10.1021/jm970497w  0.414
1997 Clarke VR, Ballyk BA, Hoo KH, Mandelzys A, Pellizzari A, Bath CP, Thomas J, Sharpe EF, Davies CH, Ornstein PL, Schoepp DD, Kamboj RK, Collingridge GL, Lodge D, Bleakman D. A hippocampal GluR5 kainate receptor regulating inhibitory synaptic transmission. Nature. 389: 599-603. PMID 9335499 DOI: 10.1038/39315  0.493
1997 Bleisch TJ, Ornstein PL, Allen NK, Wright RA, Lodge D, Schoepp DD. Structure-activity studies of aryl-spaced decahydroisoquinoline-3-carboxylic acid AMPA receptor antagonists Bioorganic and Medicinal Chemistry Letters. 7: 1161-1166. DOI: 10.1016/S0960-894X(97)00185-6  0.496
1996 Schoepp DD, Salhoff CR, Fuson KS, Sacaan AI, Tizzano JP, Ornstein PL, May PC. Selective protection against AMPA- and kainate-evoked neurotoxicity by (3S,4aR,6R,8aR)-6-[2-(1(2)H-tetrazole-5-yl)ethyl]decahyd roisoquinoline- 3-carboxylic acid (LY293558) and its racemate (LY215490). Journal of Neural Transmission (Vienna, Austria : 1996). 103: 905-16. PMID 9013384 DOI: 10.1007/Bf01291781  0.492
1996 Ornstein PL, Arnold MB, Allen NK, Bleisch T, Borromeo PS, Lugar CW, Leander JD, Lodge D, Schoepp DD. Structure-activity studies of 6-substituted decahydroisoquinoline-3-carboxylic acid AMPA receptor antagonists. 2. Effects of distal acid bioisosteric substitution, absolute stereochemical preferences, and in vivo activity. Journal of Medicinal Chemistry. 39: 2232-44. PMID 8667366 DOI: 10.1021/jm950913h  0.389
1996 Ornstein PL, Arnold MB, Allen NK, Bleisch T, Borromeo PS, Lugar CW, Leander JD, Lodge D, Schoepp DD. Structure-activity studies of 6-(tetrazolylalkyl)-substituted decahydroisoquinoline-3-carboxylic acid AMPA receptor antagonists. 1. Effects of stereochemistry, chain length, and chain substitution. Journal of Medicinal Chemistry. 39: 2219-31. PMID 8667365 DOI: 10.1021/jm950912p  0.396
1996 Ornstein PL, Arnold MB, Allen NK, Schoepp DD. Synthesis and Characterization of Phosphonic Acid-Substituted Amino Acids as Excitatory Amino Acid Receptor Antagonists Phosphorus Sulfur and Silicon and the Related Elements. 109: 309-312. DOI: 10.1080/10426509608046260  0.408
1995 Schoepp DD, Lodge D, Bleakman D, Leander JD, Tizzano JP, Wright RA, Palmer AJ, Salhoff CR, Ornstein PL. In vitro and in vivo antagonism of AMPA receptor activation by (3S, 4aR, 6R, 8aR)-6-[2-(1(2)H-tetrazole-5-yl) ethyl] decahydroisoquinoline-3-carboxylic acid. Neuropharmacology. 34: 1159-68. PMID 8532186 DOI: 10.1016/0028-3908(95)00099-R  0.486
1995 Ornstein PL, Arnold MB, Allen NK, Leander JD, Tizzano JP, Lodge D, Schoepp DD. (3SR,4aRS,6SR,8aRS)-6-(1H-tetrazol-5-yl)decahydroisoquinoline-3-carboxylic acid, a novel, competitive, systemically active NMDA and AMPA receptor antagonist. Journal of Medicinal Chemistry. 38: 4885-90. PMID 8523401  0.418
1994 Ornstein PL, Augenstein NK, Arnold MB. Stereoselective Synthesis of 6-Substituted Decahydroisoquinoline-3-carboxylates: Intermediates for the Preparation of Conformationally Constrained Acidic Amino Acids Journal of Organic Chemistry. 59: 7862-7869. DOI: 10.1021/Jo00104A051  0.357
1994 Ornstein PL, Melikian A, Martinelli MJ. Intramolecular Diels-Alder route to 6-oxodecahydroisoquinoline-3-carboxylates: Intermediates for the synthesis of conformationally constrained excitatory amino acid antagonists Tetrahedron Letters. 35: 5759-5762. DOI: 10.1016/S0040-4039(00)78176-7  0.423
1993 Ornstein PL, Arnold MB, Augenstein NK, Lodge D, Leander JD, Schoepp DD. (3SR,4aRS,6RS,8aRS)-6-[2-(1H-tetrazol-5-yl)ethyl]decahydroisoquinoline-3 - carboxylic acid: a structurally novel, systemically active, competitive AMPA receptor antagonist. Journal of Medicinal Chemistry. 36: 2046-8. PMID 8393116  0.313
1993 Ornstein PL, Arnold MB, Augenstein NK, Deeter JB, Leander JD, Lodge D, Calligaro DO, Schoepp DD. Unusual stereochemical preferences of decahydroisoquinoline-3-cargoxylic acid competitive NMDA antagonists Bioorganic and Medicinal Chemistry Letters. 3: 2067-2072. DOI: 10.1016/S0960-894X(01)81017-9  0.445
1993 Ornstein PL, Arnold MB, Evrard D, Leander JD, Lodge D, Schoepp DD. Tetrazole amino acids as competitive NMDA antagonists Bioorganic and Medicinal Chemistry Letters. 3: 43-48. DOI: 10.1016/S0960-894X(00)80089-X  0.452
1992 Fuller RW, Hemrick-Luecke SK, Ornstein PL. Protection against amphetamine-induced neurotoxicity toward striatal dopamine neurons in rodents by LY274614, an excitatory amino acid antagonist. Neuropharmacology. 31: 1027-32. PMID 1436384 DOI: 10.1016/0028-3908(92)90104-W  0.392
1992 Ornstein PL, Schoepp DD, Arnold MB, Augenstein NK, Lodge D, Millar JD, Chambers J, Campbell J, Paschal JW, Zimmerman DM. 6-substituted decahydroisoquinoline-3-carboxylic acids as potent and selective conformationally constrained NMDA receptor antagonists. Journal of Medicinal Chemistry. 35: 3547-60. PMID 1404235  0.42
1992 Ornstein PL, Schoepp DD, Arnold MB, Jones ND, Deeter JB, Lodge D, Leander JD. NMDA antagonist activity of (+/-)-(2SR,4RS)-4-(1H-tetrazol-5-ylmethyl)piperidine-2-carboxylic acid resides with the (-)-2R,4S-isomer. Journal of Medicinal Chemistry. 35: 3111-5. PMID 1387167 DOI: 10.1021/Jm00095A004  0.45
1992 McQuaid LA, Smith EC, South KK, Mitch CH, Schoepp DD, True RA, Calligaro DO, O'Malley PJ, Lodge D, Ornstein PL. Synthesis and excitatory amino acid pharmacology of a series of heterocyclic-fused quinoxalinones and quinazolinones. Journal of Medicinal Chemistry. 35: 3319-24. PMID 1382133 DOI: 10.1021/Jm00096A002  0.467
1992 Thurkauf A, Mattson MV, Richardson S, Mirsadeghi S, Ornstein PL, Harrison EA, Rice KC, Jacobson AE, Monn JA. Analogues of the dioxolanes dexoxadrol and etoxadrol as potential phencyclidine-like agents. Synthesis and structure-activity relationships. Journal of Medicinal Chemistry. 35: 1323-9. PMID 1349351 DOI: 10.1021/Jm00086A001  0.372
1992 Evans DA, Miller SJ, Ennis MD, Ornstein PL. Asymmetric synthesis of macbecin I The Journal of Organic Chemistry. 57: 1067-1069. DOI: 10.1021/Jo00030A006  0.544
1991 Schoepp DD, Ornstein PL, Salhoff CR, Leander JD. Neuroprotectant effects of LY274614, a structurally novel systemically active competitive NMDA receptor antagonist. Journal of Neural Transmission. General Section. 85: 131-43. PMID 1834088 DOI: 10.1007/Bf01244705  0.462
1991 Rasmussen K, Fuller RW, Stockton ME, Perry KW, Swinford RM, Ornstein PL. NMDA receptor antagonists suppress behaviors but not norepinephrine turnover or locus coeruleus unit activity induced by opiate withdrawal. European Journal of Pharmacology. 197: 9-16. PMID 1832640 DOI: 10.1016/0014-2999(91)90358-W  0.364
1991 Ornstein PL, Schoepp DD, Arnold MB, Leander JD, Lodge D, Paschal JW, Elzey T. 4-(Tetrazolylalkyl)piperidine-2-carboxylic acids. Potent and selective N-methyl-D-aspartic acid receptor antagonists with a short duration of action. Journal of Medicinal Chemistry. 34: 90-7. PMID 1825117 DOI: 10.1021/Jm00105A016  0.503
1991 Ornstein PL, Arnold MB, Augenstein NK, Paschal JW. Syntheses of 6-oxodecahydroisoquinoline-3-carboxylates. Useful intermediates for the preparation of conformationally defined excitatory amino acid antagonists Journal of Organic Chemistry. 56: 4388-4392. DOI: 10.1021/Jo00014A012  0.453
1990 Schoepp DD, Gamble AY, Salhoff CR, Johnson BG, Ornstein PL. Excitatory amino acid-induced convulsions in neonatal rats mediated by distinct receptor subtypes. European Journal of Pharmacology. 182: 421-7. PMID 2171944 DOI: 10.1016/0014-2999(90)90039-9  0.47
1990 Shuman RT, Ornstein PL, Paschal JW, Gesellchen PD. An improved synthesis of homoproline and derivatives Journal of Organic Chemistry. 55: 738-741. DOI: 10.1021/Jo00289A058  0.326
1989 France CP, Woods JH, Ornstein P. The competitive N-methyl-D-aspartate (NMDA) antagonist CGS 19755 attenuates the rate-decreasing effects of NMDA in rhesus monkeys without producing ketamine-like discriminative stimulus effects. European Journal of Pharmacology. 159: 133-9. PMID 2651134 DOI: 10.1016/0014-2999(89)90697-3  0.353
1989 Schoepp DD, Salhoff CR, Hillman CC, Ornstein PL. CGS-19755 and MK-801 selectively prevent rat striatal cholinergic and gabaergic neuronal degeneration induced by N-methyl-D-aspartate and ibotenate in vivo. Journal of Neural Transmission. General Section. 78: 183-93. PMID 2553073 DOI: 10.1007/Bf01249228  0.456
1989 Ornstein PL, Schaus JM, Chambers JW, Huser DL, Leander JD, Wong DT, Paschal JW, Jones ND, Deeter JB. Synthesis and pharmacology of a series of 3- and 4-(phosphonoalkyl)pyridine- and -piperidine-2-carboxylic acids. Potent N-methyl-D-aspartate receptor antagonists. Journal of Medicinal Chemistry. 32: 827-33. PMID 2539478  0.429
1989 Ornstein PL. An enantioselective synthesis of D-(-)-2-amino-5-phosphonopentanoic acid Journal of Organic Chemistry. 54: 2251-2253. DOI: 10.1021/Jo00270A045  0.336
1989 ORNSTEIN PL, SCHAUS JM, CHAMBERS JW, HUSER DL, LEANDER JD, WONG DT, PASCHAL JW, JONES ND, DEETER JB. ChemInform Abstract: Synthesis and Pharmacology of a Series of 3- and 4-(Phosphonoalkyl)pyridine(piperidine)-2-carboxylic Acids. Potent N-Methyl-D-aspartate Receptor Antagonists. Cheminform. 20. DOI: 10.1002/CHIN.198938339  0.387
1988 Leander JD, Lawson RR, Ornstein PL, Zimmerman DM. N-methyl-D-aspartic acid-induced lethality in mice: selective antagonism by phencyclidine-like drugs. Brain Research. 448: 115-20. PMID 3292008 DOI: 10.1016/0006-8993(88)91107-9  0.391
1988 Lodge D, Davies SN, Jones MG, Millar J, Manallack DT, Ornstein PL, Verberne AJ, Young N, Beart PM. A comparison between the in vivo and in vitro activity of five potent and competitive NMDA antagonists. British Journal of Pharmacology. 95: 957-65. PMID 2905186 DOI: 10.1111/J.1476-5381.1988.Tb11726.X  0.437
1987 Koek W, Woods JH, Ornstein P. A simple and rapid method for assessing similarities among directly observable behavioral effects of drugs: PCP-like effects of 2-amino-5-phosphonovalerate in rats. Psychopharmacology. 91: 297-304. PMID 2882539 DOI: 10.1007/Bf00518181  0.329
1986 Koek W, Woods JH, Ornstein P. Phencyclidine-like behavioral effects in pigeons induced by systemic administration of the excitatory amino acid antagonist, 2-amino-5-phosphonovalerate. Life Sciences. 39: 973-8. PMID 2875374 DOI: 10.1016/0024-3205(86)90285-7  0.421
1983 Trost BM, Ornstein PL. An unusual migratory aptitude in a cyclopropylcarbinyl-cyclobutyl rearrangement. Synthesis of 2,4-disubstituted cyclobutanones The Journal of Organic Chemistry. 48: 1131-1133. DOI: 10.1021/Jo00155A050  0.418
1983 Trost BM, Ornstein PL. Bifunctional cyclopropyl reagents: a total synthesis of 7-E,9-Z methyl trisporate B Tetrahedron Letters. 24: 2833-2836. DOI: 10.1016/S0040-4039(00)88036-3  0.444
1983 TROST BM, ORNSTEIN PL. ChemInform Abstract: BIFUNCTIONAL CYCLOPROPYL REAGENTS: A TOTAL SYNTHESIS OF 7-E,9-Z METHYL TRISPORATE B Chemischer Informationsdienst. 14. DOI: 10.1002/chin.198343337  0.32
1983 TROST BM, ORNSTEIN PL. ChemInform Abstract: AN UNUSUAL MIGRATORY APTITUDE IN A CYCLOPROPYLCARBINYL-CYCLOBUTYL REARRANGEMENT. SYNTHESIS OF 2,4-DISUBSTITUTED CYCLOBUTANONES Chemischer Informationsdienst. 14. DOI: 10.1002/chin.198334151  0.332
1982 Trost BM, Ornstein PL. Bifunctional cyclopropyl reagents: stereocontrolled approach to vinyl sulfides and chemodifferentiated 1,4-dicarbonyl systems The Journal of Organic Chemistry. 47: 748-751. DOI: 10.1021/Jo00343A034  0.338
1981 Trost BM, Ornstein PL. A chemoselective desulfurization method via homogeneous nickel catalysis Tetrahedron Letters. 22: 3463-3466. DOI: 10.1016/S0040-4039(01)81932-8  0.394
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