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Drug−Protein Adducts: An Industry Perspective on Minimizing the Potential for Drug Bioactivation in Drug Discovery and Development

Chemical research in toxicology, 2004-01, Vol.17 (1), p.3-16

2004

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Fluorination of 3-(3-(Piperidin-1-yl)propyl)indoles and 3-(3-(Piperazin-1-yl)propyl)indoles Gives Selective Human 5-HT1D Receptor Ligands with Improved Pharmacokinetic Profiles

Journal of medicinal chemistry, 1999-06, Vol.42 (12), p.2087-2104

1999

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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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long-term effect of dietary advice on the diet of men with angina: the diet and angina randomized trial

Journal of human nutrition and dietetics, 2004-04, Vol.17 (2), p.117-119

2004

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Liver fluke ( Fasciola hepatica)-derived peptides activate rat peritoneal mast cells

International immunopharmacology, 2003-05, Vol.3 (5), p.775-781

2003

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N-Heteroaryl-2-phenyl-3-(benzyloxy)piperidines: A Novel Class of Potent Orally Active Human NK1 Antagonists

Journal of medicinal chemistry, 1996-07, Vol.39 (15), p.2907-2914

1996

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Synthesis and Serotonergic Activity of 3-[2-(Pyrrolidin-1-yl)ethyl]indoles: Potent Agonists for the h5-HT1D Receptor with High Selectivity over the h5-HT1B Receptor

Journal of medicinal chemistry, 1999-02, Vol.42 (4), p.677-690

1999

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Synthesis and Serotonergic Activity of N,N-Dimethyl-2-[5-(1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl]ethylamine and Analogs: Potent Agonists for 5-HT1D Receptors

Journal of medicinal chemistry, 1995-05, Vol.38 (10), p.1799-1810

1995

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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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3-(Piperazinylpropyl)indoles: Selective, Orally Bioavailable h5-HT1D Receptor Agonists as Potential Antimigraine Agents

Journal of medicinal chemistry, 1999-02, Vol.42 (4), p.691-705

1999

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Enhancement of Oral Absorption in Selective 5-HT1D Receptor Agonists: Fluorinated 3-[3-(Piperidin-1-yl)propyl]indoles

Journal of medicinal chemistry, 1998-07, Vol.41 (15), p.2667-2670

1998

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Endothelium‐dependent modulation of resistance vessel contraction: studies with NG‐nitro‐l‐arginine methyl ester and NG‐nitro‐l‐arginine

British journal of pharmacology, 1992-10, Vol.107 (2), p.616-621

1992

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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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Selective, Orally Active 5-HT1D Receptor Agonists as Potential Antimigraine Agents

Journal of medicinal chemistry, 1997-10, Vol.40 (22), p.3501-3503

1997

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5-(Piperidin-2-yl)- and 5-(Homopiperidin-2-yl)-1,4-benzodiazepines: High-Affinity, Basic Ligands for the Cholecystokinin-B Receptor

Journal of medicinal chemistry, 1997-08, Vol.40 (16), p.2491-2501

1997

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2-Aryl indole NK1 receptor antagonists : Optimisation of indole substitution

Bioorganic & medicinal chemistry letters, 2001-05, Vol.11 (9), p.1233-1236

2001

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Endothelium-dependent relaxation in resistance vessels from the spontaneously hypertensive rats

Journal of hypertension, 1989-08, Vol.7 (8), p.661-666

1989

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Brain penetration of aprepitant, a substance P receptor antagonist, in ferrets

Drug metabolism and disposition, 2003-06, Vol.31 (6), p.785

2003

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Controlled Modification of Acidity in Cholecystokinin B Receptor Antagonists: N-(1,4-Benzodiazepin-3-yl)-N ‘-[3-(tetrazol-5-ylamino)phenyl]ureas

Journal of medicinal chemistry, 1996-02, Vol.39 (4), p.842-849

1996

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In Vitro and In Vivo Inhibition of Inositol Monophosphatase by the Bisphosphonate L‐690,330

Journal of neurochemistry, 1993-02, Vol.60 (2), p.652-658

1993

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Determination of the in vitro metabolism of (+)- and (−)-epibatidine

Journal of Chromatography A, 2000-10, Vol.896 (1), p.229-238

2000

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High-Affinity and Potent, Water-Soluble 5-Amino-1,4-benzodiazepine CCKB/Gastrin Receptor Antagonists Containing a Cationic Solubilizing Group

Journal of medicinal chemistry, 1994-03, Vol.37 (6), p.719-721

1994

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Use of chiral liquid chromatography–tandem mass spectrometry to investigate the metabolism of racemic cholecystokinin-B antagonists

Journal of Chromatography A, 2000-10, Vol.896 (1), p.217-227

2000

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Neutrophils and eosinophils: clinical implications of their appearance, presence and disappearance in asthma and COPD

Current drug targets. Inflammation & allergy, 2005-08, Vol.4 (4), p.415

2005

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Measurement of Lithium‐Induced Changes in Mouse Inositol(1)Phosphate Levels In Vivo

Journal of neurochemistry, 1992-11, Vol.59 (5), p.1946-1954

1992

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Drug−Protein Adducts: An Industry Perspective on Minimizing the Potential for Drug Bioactivation in Drug Discovery and Development

Fluorination of 3-(3-(Piperidin-1-yl)propyl)indoles and 3-(3-(Piperazin-1-yl)propyl)indoles Gives Selective Human 5-HT1D Receptor Ligands with Improved Pharmacokinetic Profiles

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

long-term effect of dietary advice on the diet of men with angina: the diet and angina randomized trial

Liver fluke ( Fasciola hepatica)-derived peptides activate rat peritoneal mast cells

N-Heteroaryl-2-phenyl-3-(benzyloxy)piperidines: A Novel Class of Potent Orally Active Human NK1 Antagonists

Synthesis and Serotonergic Activity of 3-[2-(Pyrrolidin-1-yl)ethyl]indoles: Potent Agonists for the h5-HT1D Receptor with High Selectivity over the h5-HT1B Receptor

Synthesis and Serotonergic Activity of N,N-Dimethyl-2-[5-(1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl]ethylamine and Analogs: Potent Agonists for 5-HT1D Receptors

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

3-(Piperazinylpropyl)indoles: Selective, Orally Bioavailable h5-HT1D Receptor Agonists as Potential Antimigraine Agents

Enhancement of Oral Absorption in Selective 5-HT1D Receptor Agonists: Fluorinated 3-[3-(Piperidin-1-yl)propyl]indoles

Endothelium‐dependent modulation of resistance vessel contraction: studies with NG‐nitro‐l‐arginine methyl ester and NG‐nitro‐l‐arginine

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

Selective, Orally Active 5-HT1D Receptor Agonists as Potential Antimigraine Agents

5-(Piperidin-2-yl)- and 5-(Homopiperidin-2-yl)-1,4-benzodiazepines: High-Affinity, Basic Ligands for the Cholecystokinin-B Receptor

2-Aryl indole NK1 receptor antagonists : Optimisation of indole substitution

Endothelium-dependent relaxation in resistance vessels from the spontaneously hypertensive rats

Brain penetration of aprepitant, a substance P receptor antagonist, in ferrets

Controlled Modification of Acidity in Cholecystokinin B Receptor Antagonists: N-(1,4-Benzodiazepin-3-yl)-N ‘-[3-(tetrazol-5-ylamino)phenyl]ureas

In Vitro and In Vivo Inhibition of Inositol Monophosphatase by the Bisphosphonate L‐690,330

Determination of the in vitro metabolism of (+)- and (−)-epibatidine

High-Affinity and Potent, Water-Soluble 5-Amino-1,4-benzodiazepine CCKB/Gastrin Receptor Antagonists Containing a Cationic Solubilizing Group

Use of chiral liquid chromatography–tandem mass spectrometry to investigate the metabolism of racemic cholecystokinin-B antagonists

Neutrophils and eosinophils: clinical implications of their appearance, presence and disappearance in asthma and COPD

Measurement of Lithium‐Induced Changes in Mouse Inositol(1)Phosphate Levels In Vivo

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