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A hippocampal GluR5 kainate receptor regulating inhibitory synaptic transmissionGluK1 antagonists from 6-(tetrazolyl)phenyl decahydroisoquinoline derivatives: in vitro profile and in vivo analgesic efficacyAntagonists of GLU(K5)-containing kainate receptors prevent pilocarpine-induced limbic seizuresLY293558, a novel AMPA/GluR5 antagonist, is efficacious and well-tolerated in acute migraine.(3SR,4aRS,6RS,8aRS)-6-[2-(1H-tetrazol-5-yl)ethyl]decahydroisoquinoline-3 - carboxylic acid: a structurally novel, systemically active, competitive AMPA receptor antagonist.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.Pharmacological discrimination of GluR5 and GluR6 kainate receptor subtypes by (3S,4aR,6R,8aR)-6-[2-(1(2)H-tetrazole-5-yl)ethyl]decahyd roisdoquinoline-3 carboxylic-acid.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.The potent mGlu receptor antagonist LY341495 identifies roles for both cloned and novel mGlu receptors in hippocampal synaptic plasticity.In vitro pharmacological and rat pharmacokinetic characterization of LY3020371, a potent and selective mGlu2/3 receptor antagonist.Anxiolytic-like effects through a GLUK5 kainate receptor mechanism.Two prodrugs of potent and selective GluR5 kainate receptor antagonists actives in three animal models of pain.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.Synthesis and evaluation of a series of novel 2-[(4-chlorophenoxy)methyl]benzimidazoles as selective neuropeptide Y Y1 receptor antagonists.Phencyclidine-like behavioral effects in pigeons induced by systemic administration of the excitatory amino acid antagonist, 2-amino-5-phosphonovalerate.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.Transmembrane AMPA receptor regulatory proteins and cornichon-2 allosterically regulate AMPA receptor antagonists and potentiatorsSynthesis and pharmacology of a series of 3- and 4-(phosphonoalkyl)pyridine- and -piperidine-2-carboxylic acids. Potent N-methyl-D-aspartate receptor antagonists.A role for Ca2+ stores in kainate receptor-dependent synaptic facilitation and LTP at mossy fiber synapses in the hippocampus.Privileged structure based ligands for melanocortin receptors--substituted benzylic piperazine derivatives.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 ActKainate GluR5 receptor subtype mediates the nociceptive response to formalin in the rat.The GluR5 subtype of kainate receptor regulates excitatory synaptic transmission in areas CA1 and CA3 of the rat hippocampus.Decahydroisoquinolines: novel competitive AMPA/kainate antagonists with neuroprotective effects in global cerebral ischaemia.Antiallodynic and antihyperalgesic effects of selective competitive GLUK5 (GluR5) ionotropic glutamate receptor antagonists in the capsaicin and carrageenan models in rats.GluK1 antagonists from 6-(carboxy)phenyl decahydroisoquinoline derivatives. SAR and evaluation of a prodrug strategy for oral efficacy in pain models.Schedule-controlled behavioral effects of the selective 2-amino-3-(5-methyl-3-hydroxyisoxazol-4-yl)propanoic acid antagonist LY293558 in pigeons.Synthesis and excitatory amino acid pharmacology of a series of heterocyclic-fused quinoxalinones and quinazolinonesNeuroprotectant effects of LY274614, a structurally novel systemically active competitive NMDA receptor antagonistExcitatory amino acid-induced convulsions in neonatal rats mediated by distinct receptor subtypesCGS-19755 and MK-801 selectively prevent rat striatal cholinergic and gabaergic neuronal degeneration induced by N-methyl-D-aspartate and ibotenate in vivo(3SR,4aRS,6SR,8aRS)-6-(1H-tetrazol-5-yl)decahydroisoquinoline-3-carboxylic acid, a novel, competitive, systemically active NMDA and AMPA receptor antagonistStructure-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 activityCyclothiazide acts at a site on the alpha-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid receptor complex that does not recognize competitive or noncompetitive AMPA receptor antagonistsSelective 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)LY377770, a novel iGlu5 kainate receptor antagonist with neuroprotective effects in global and focal cerebral ischaemiaNeuroprotective effects of LY379268, a selective mGlu2/3 receptor agonist: investigations into possible mechanism of action in vivoStructure-activity relationship of a series of diaminoalkyl substituted benzimidazole as neuropeptide Y Y1 receptor antagonistsActions of kainate and AMPA selective glutamate receptor ligands on nociceptive processing in the spinal cordHeteroatom-substitution as a strategy for increasing the potency of competitive NMDA antagonists
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Q24318925-9C4BBDD0-ABDC-4EF3-901A-29EAFB5264C6Q27687299-E4DD1263-6593-4156-83F5-A391E01E5E5FQ28564498-49D02EBF-F46C-4ECE-8F4A-FE4F72169B8DQ34326873-6C8E820E-BB6A-4F4B-B0C1-82F2FC9E04E8Q34356576-FD8B67D6-6131-4716-A577-9AEF669A1A77Q34368594-7828FFC9-B119-4979-8039-F98D7CBFF84AQ34376387-33E34B0C-373E-4EE8-B7F9-91627CA5962EQ34456241-D385A44E-85E9-4DC6-9CB6-E991A43DD28EQ34487239-3DF461CE-4EB9-44AC-8DDD-BF876A5544BAQ38805426-BAE5B0C4-54B4-4B0E-9698-40EE92E97239Q40148018-831B6066-8B17-4850-80E5-F8394004CA67Q40405823-834B6A96-FC8C-43E8-A181-5F211D1657AAQ40703167-9C4B3FD9-3A8E-4BCC-A688-C2F3810FD4DDQ41024659-C9D9AA72-1473-4C44-9E0C-C6E54FA65D81Q41342422-E5198EB5-51CC-478F-800A-D8FD9C0880E1Q41343829-F5712EEE-896C-4A0D-989B-5E7B4465DD49Q41958491-7D901706-3AEB-4CFE-9A41-5AE32FFF6B3DQ42149590-222EE310-AF65-4E57-BC7B-21A489A1D856Q44520403-6BB32212-8988-4F82-B398-EA92C85991B4Q46708676-91BB169F-E1EA-4F4F-9D68-756F333330FAQ46954842-11B28DCE-6A1B-45DF-B5CC-67FE285C9F6EQ47782247-8210AA8F-6D85-479E-B4C3-339760069F8BQ48331477-7E180A45-9F92-4AD1-AE8A-40281EBE72D1Q48331516-DA5F5530-125B-4E2C-BC8D-86FD6E3B32FEQ48473620-6AFF4995-D808-4A16-AF82-0B0B85E877FAQ51777522-56D0BDEC-A6E5-41E5-A306-96472CF4C3BEQ52205810-E41A7212-A6D3-4754-AFAE-FF814DAD32F9Q67542644-627C3E68-E740-4897-BA82-DED56119E1CAQ67903723-AF1D7843-45C2-491B-9E12-F6067BE88D26Q68483162-25412893-8BB4-4347-AAFB-DB8A83443E2FQ69358112-4465A459-DF69-46D2-A252-2EA099F0319AQ70791851-83C92614-F30E-4359-AFD1-90F3425A544BQ71153101-BACEB184-B21B-4E40-8ADB-1676D764B614Q71667262-435254ED-E2C8-413C-9408-4CDC97206869Q73024836-301EDEDC-C6F5-4490-AAB4-370FCCE25C54Q73898225-128E2956-BBF0-4624-AA27-793555D40628Q74181711-AF980536-12A5-4662-9FBC-635286CAB847Q77320096-100CD5E5-719E-49BF-ABAD-3BE21775D3ECQ77668758-EFF5CC23-7879-431F-9CF7-C718A534A622Q77744390-3EAEB577-3469-458C-8262-C011D0399653
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description
onderzoeker
@nl
researcher
@en
հետազոտող
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name
Paul L Ornstein
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Paul L Ornstein
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Paul L Ornstein
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Paul L Ornstein
@nl
Paul L Ornstein
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Paul L Ornstein
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Paul L Ornstein
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Paul L Ornstein
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Paul L Ornstein
@nl
Paul L Ornstein
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prefLabel
Paul L Ornstein
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Paul L Ornstein
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Paul L Ornstein
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Paul L Ornstein
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Paul L Ornstein
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P106
P21
P31
P496
0000-0002-4335-1877