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The Glycine Site on the NMDA Receptor: Structure-Activity Relationships and Therapeutic Potential

Journal of medicinal chemistry, 1994-11, Vol.37 (24), p.4053-4067

1994

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7-Chlorokynurenic Acid is a Selective Antagonist at the Glycine Modulatory Site of the N-methyl-D-aspartate Receptor Complex

Proceedings of the National Academy of Sciences - PNAS, 1988-09, Vol.85 (17), p.6547-6550

1988

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Effect of Plasma Protein Binding on in Vivo Activity and Brain Penetration of Glycine/NMDA Receptor Antagonists

Journal of medicinal chemistry, 1997-12, Vol.40 (25), p.4053-4068

1997

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5-(4-Chlorophenyl)-4-methyl-3-(1-(2- phenylethyl)piperidin-4-yl)isoxazole: A Potent, Selective Antagonist at Human Cloned Dopamine D4 Receptors

Journal of medicinal chemistry, 1996-05, Vol.39 (10), p.1943-1945

1996

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The Design of Leadlike Combinatorial Libraries

Angewandte Chemie (International ed.), 1999-12, Vol.38 (24), p.3743-3748

1999

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Enantiomers of HA-966 (3-Amino-1-Hydroxypyrrolid-2-One) Exhibit Distinct Central Nervous System Effects: (+)-HA-966 is a Selective Glycine/N- Methyl-D-Aspartate Receptor Antagonist, But (-)-HA-966 is a Potent γ-Butyrolactone-Like Sedative

Proceedings of the National Academy of Sciences - PNAS, 1990-01, Vol.87 (1), p.347-351

1990

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Is There a Difference between Leads and Drugs? A Historical Perspective

Journal of Chemical Information and Computer Sciences, 2001-09, Vol.41 (5), p.1308-1315

2001

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The glycine site of the NMDA receptor — five years on

Trends in pharmacological sciences (Regular ed.), 1993, Vol.14 (1), p.20-25

1993

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An analysis of the attrition of drug candidates from four major pharmaceutical companies

Nature reviews. Drug discovery, 2015-07, Vol.14 (7), p.475-486

2015

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4-Amido-2-carboxytetrahydroquinolines. Structure-activity relationships for antagonism at the glycine site of the NMDA receptor

Journal of medicinal chemistry, 1992-05, Vol.35 (11), p.1954-1968

1992

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Characterization of the binding of [3H]L-689,560, an antagonist for the glycine site on the N-methyl-D-aspartate receptor, to rat brain membranes

Molecular pharmacology, 1992-05, Vol.41 (5), p.923-930

1992

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4-Substituted-3-phenylquinolin-2(1H)-ones: Acidic and Nonacidic Glycine Site N-Methyl-d-aspartate Antagonists with in Vivo Activity

Journal of medicinal chemistry, 1997-02, Vol.40 (5), p.754-765

1997

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The atypical neuroleptic profile of the glycine/N-methyl-D-aspartate receptor antagonist, L-701,324, in rodents

The Journal of pharmacology and experimental therapeutics, 1996-05, Vol.277 (2), p.578

1996

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Anticonvulsant and behavioral profile of L-701,324, a potent, orally active antagonist at the glycine modulatory site on the N-methyl-D-aspartate receptor complex

The Journal of pharmacology and experimental therapeutics, 1996-11, Vol.279 (2), p.492

1996

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Kynurenic acid derivatives. Structure-activity relationships for excitatory amino acid antagonism and identification of potent and selective antagonists at the glycine site on the N-methyl-D-aspartate receptor

Journal of medicinal chemistry, 1991-04, Vol.34 (4), p.1243-1252

1991

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3-Nitro-3,4-dihydro-2(1H)quinolones. Excitatory amino acid antagonists acting at glycine-site NMDA and (RS)-α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptors

Journal of medicinal chemistry, 1993-10, Vol.36 (22), p.3397-3408

1993

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2-Carboxytetrahydroquinolines. Conformational and stereochemical requirements for antagonism of the glycine site on the NMDA receptor

Journal of medicinal chemistry, 1992-05, Vol.35 (11), p.1942-1953

1992

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Kynurenic acid analogues with improved affinity and selectivity for the glycine site on the N-methyl-D-aspartate receptor from rat brain

Molecular pharmacology, 1992-05, Vol.41 (5), p.914-922

1992

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4-Heterocyclylpiperidines as Selective High-Affinity Ligands at the Human Dopamine D4 Receptor

Journal of medicinal chemistry, 1997-07, Vol.40 (15), p.2374-2385

1997

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The anticonvulsant and behavioural profile of L‐687,414, a partial agonist acting at the glycine modulatory site on the N‐methyl‐D‐aspartate (NMDA) receptor complex

British journal of pharmacology, 1994-11, Vol.113 (3), p.729-736

1994

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Biological profile of L-745,870, a selective antagonist with high affinity for the dopamine D4 receptor

The Journal of pharmacology and experimental therapeutics, 1997-11, Vol.283 (2), p.636

1997

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A thyromimetic that decreases plasma cholesterol levels without increasing cardiac activity

Nature (London), 1986-12, Vol.324 (6096), p.425-429

1986

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Time-Related Differences in the Physical Property Profiles of Oral Drugs

Journal of medicinal chemistry, 2004-12, Vol.47 (25), p.6338-6348

2004

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A Comparison of Physiochemical Property Profiles of Development and Marketed Oral Drugs

Journal of medicinal chemistry, 2003-03, Vol.46 (7), p.1250-1256

2003

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L-745,870, a subtype selective dopamine D4 receptor antagonist, does not exhibit a neuroleptic-like profile in rodent behavioral tests

The Journal of pharmacology and experimental therapeutics, 1997-12, Vol.283 (3), p.1256

1997

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The Glycine Site on the NMDA Receptor: Structure-Activity Relationships and Therapeutic Potential

7-Chlorokynurenic Acid is a Selective Antagonist at the Glycine Modulatory Site of the N-methyl-D-aspartate Receptor Complex

Effect of Plasma Protein Binding on in Vivo Activity and Brain Penetration of Glycine/NMDA Receptor Antagonists

5-(4-Chlorophenyl)-4-methyl-3-(1-(2- phenylethyl)piperidin-4-yl)isoxazole: A Potent, Selective Antagonist at Human Cloned Dopamine D4 Receptors

The Design of Leadlike Combinatorial Libraries

Enantiomers of HA-966 (3-Amino-1-Hydroxypyrrolid-2-One) Exhibit Distinct Central Nervous System Effects: (+)-HA-966 is a Selective Glycine/N- Methyl-D-Aspartate Receptor Antagonist, But (-)-HA-966 is a Potent γ-Butyrolactone-Like Sedative

Is There a Difference between Leads and Drugs? A Historical Perspective

The glycine site of the NMDA receptor — five years on

An analysis of the attrition of drug candidates from four major pharmaceutical companies

4-Amido-2-carboxytetrahydroquinolines. Structure-activity relationships for antagonism at the glycine site of the NMDA receptor

Characterization of the binding of [3H]L-689,560, an antagonist for the glycine site on the N-methyl-D-aspartate receptor, to rat brain membranes

4-Substituted-3-phenylquinolin-2(1H)-ones: Acidic and Nonacidic Glycine Site N-Methyl-d-aspartate Antagonists with in Vivo Activity

The atypical neuroleptic profile of the glycine/N-methyl-D-aspartate receptor antagonist, L-701,324, in rodents

Anticonvulsant and behavioral profile of L-701,324, a potent, orally active antagonist at the glycine modulatory site on the N-methyl-D-aspartate receptor complex

Kynurenic acid derivatives. Structure-activity relationships for excitatory amino acid antagonism and identification of potent and selective antagonists at the glycine site on the N-methyl-D-aspartate receptor

3-Nitro-3,4-dihydro-2(1H)quinolones. Excitatory amino acid antagonists acting at glycine-site NMDA and (RS)-α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptors

2-Carboxytetrahydroquinolines. Conformational and stereochemical requirements for antagonism of the glycine site on the NMDA receptor

Kynurenic acid analogues with improved affinity and selectivity for the glycine site on the N-methyl-D-aspartate receptor from rat brain

4-Heterocyclylpiperidines as Selective High-Affinity Ligands at the Human Dopamine D4 Receptor

The anticonvulsant and behavioural profile of L‐687,414, a partial agonist acting at the glycine modulatory site on the N‐methyl‐D‐aspartate (NMDA) receptor complex

Biological profile of L-745,870, a selective antagonist with high affinity for the dopamine D4 receptor

A thyromimetic that decreases plasma cholesterol levels without increasing cardiac activity

Time-Related Differences in the Physical Property Profiles of Oral Drugs

A Comparison of Physiochemical Property Profiles of Development and Marketed Oral Drugs

L-745,870, a subtype selective dopamine D4 receptor antagonist, does not exhibit a neuroleptic-like profile in rodent behavioral tests

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