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Your search keyword '"Caroline J. Goodacre"' showing total 5 results
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5 results on '"Caroline J. Goodacre"'

1. The identification of novel orally active mGluR5 antagonist GSK2210875

Author

Pier D’Alessandro, Doug Minick, Sonia Delle-Fratte, Sharon Butler, Paul W. Smith, Adelheid Roth, Stephen P. Watson, Ezio Bettini, Vincenzo Garzya, Michela Andreoli, Caroline J. Goodacre, Palmina Cavallini, Roberto Benedetti, Catherine Ball, Parita Shah, Olivier Lorthioir, Fiona Brown, Ben Tehan, Maria Pilla, and Michela Tessari

Subjects
Mglur5 antagonist, Receptor, Metabotropic Glutamate 5, animal diseases, Clinical Biochemistry, Allosteric regulation, Administration, Oral, Pharmaceutical Science, Pharmacology, Receptors, Metabotropic Glutamate, Biochemistry, Mice, Structure-Activity Relationship, Allosteric Regulation, Oral administration, mental disorders, Drug Discovery, Animals, Molecular Biology, Chemistry, Organic Chemistry, Antagonist, Brain, Biological activity, Rats, stomatognathic diseases, Orally active, nervous system, Molecular Medicine, Heterocyclic Compounds, 3-Ring
Abstract

The identification of novel orally active mGluR5 antagonist GSK2210875 is described.

Published
2010

2. New quinoline NK3 receptor antagonists with CNS activity

Author

Paul W. Smith, Caroline J. Goodacre, Wyman Paul Adrian, Sara A. Coggon, Vong Antonio Kuok Keong, Jeannette M. Watson, William J. Martin, Kirsten L. Searle, Daniel Marcus Bradley, Zining Wu, Peter J. Lovell, Lee A. Dawson, Harrington Frank Peter, David R. Thomas, Roderick A. Porter, Graham Murkitt, Halina T Serafinowska, and Sean Thomas Flynn

Subjects
Central Nervous System, Male, medicine.drug_class, Clinical Biochemistry, Pharmaceutical Science, Carboxamide, Gerbil, Biochemistry, Rats, Sprague-Dawley, chemistry.chemical_compound, In vivo, Drug Discovery, Talnetant, medicine, Animals, Amines, Molecular Biology, Cerebral Cortex, Chemistry, Organic Chemistry, Quinoline, Antagonist, Brain, Receptors, Neurokinin-3, Rats, Models, Chemical, Area Under Curve, Lipophilicity, Quinolines, Molecular Medicine, Gerbillinae, Ex vivo, medicine.drug
Abstract

Lead optimisation starting from the previously reported selective quinoline NK3 receptor antagonists talnetant 2 (SB-223412) and 3 (SB-222200) led to the identification of 3-aminoquinoline NK3 antagonist 10 (GSK172981) with excellent CNS penetration. Investigation of a structurally related series of sulfonamides with reduced lipophilicity led to the discovery of 20 (GSK256471). Both 10 and 20 are high affinity, potent NK3 receptor antagonists which despite having different degrees of CNS penetration produced excellent NK3 receptor occupancy in an ex vivo binding study in gerbil cortex.

Published
2008

3. 3,4-Dihydro-2H-benzoxazinones as dual-acting 5-HT1A receptor antagonists and serotonin reuptake inhibitors

Author

Claire M. Scott, Vong Antonio Kuok Keong, Paul W. Smith, Caroline J. Goodacre, Jeannette M. Watson, Frank E. Blaney, Simon E. Ward, Kathryn R. Starr, Peter J. Lovell, and Kevin M. Thewlis

Subjects
Models, Molecular, Magnetic Resonance Spectroscopy, Stereochemistry, Pyridines, Clinical Biochemistry, Guinea Pigs, Pharmaceutical Science, CHO Cells, Inhibitory postsynaptic potential, Biochemistry, Chemical synthesis, Binding, Competitive, Mass Spectrometry, Piperazines, Cell Line, chemistry.chemical_compound, Radioligand Assay, Cricetulus, Cricetinae, Drug Discovery, Animals, Humans, Receptor, Molecular Biology, Cerebral Cortex, Bicyclic molecule, Chemistry, Benzoxazinones, Organic Chemistry, Antagonist, Callithrix, Benzoxazines, Rats, Receptor, Serotonin, 5-HT1D, Receptor, Serotonin, 5-HT1A, Receptor, Serotonin, 5-HT1B, Molecular Medicine, 5-HT1A receptor, Indicators and Reagents, Serotonin Antagonists, Lead compound, Selective Serotonin Reuptake Inhibitors, Synaptosomes
Abstract

Investigation of halogen substitution in lead compound 1 has led to the identification of analogues which combine high affinity for 5-HT(1A) receptors and potent serotonin reuptake inhibitory activity. Several compounds show an improved selectivity over 5-HT(1B) and 5-HT(1D) receptors and a superior pharmacokinetic profile in the rat.

Published
2006

5. A series of bisaryl imidazolidin-2-ones has shown to be selective and orally active 5-HT2C receptor antagonists

Author

Peter J. Lovell, Caroline J. Goodacre, Brenda K. Trail, Graham J. Riley, Kathryn R. Starr, Michael Allen, Steven Mark Bromidge, Vicky Holland, David E. Clapham, Lorraine Campbell, Frank D. King, and Martyn D. Wood

Subjects
Stereochemistry, Clinical Biochemistry, Pharmaceutical Science, Administration, Oral, Imidazolidines, Biochemistry, Chemical synthesis, Sensitivity and Specificity, Cell Line, Substrate Specificity, chemistry.chemical_compound, Structure-Activity Relationship, Oral administration, Drug Discovery, Receptor, Serotonin, 5-HT2B, Receptor, Serotonin, 5-HT2C, Inverse agonist, Animals, Humans, Receptor, Serotonin, 5-HT2A, Receptor, Molecular Biology, 5-HT receptor, Molecular Structure, Chemistry, Organic Chemistry, Antagonist, Rats, 5-HT2C receptor, SB-243213, Serotonin 5-HT2 Receptor Antagonists, Molecular Medicine
Abstract

Bisaryl cyclic ureas have been identified as high affinity 5-HT2C receptor antagonists with selectivity over 5-HT2A and 5-HT2B. Compounds such as 8 and 22 have shown oral activity in a centrally mediated pharmacodynamic model of 5-HT2C function in rodents.

Published
2005

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