4-Amido-2-carboxytetrahydroquinolines. Structure-activity relationships for antagonism at the glycine site of the NMDA receptor PD Leeson, RW Carling, KW Moore, AM Moseley, JD Smith, G Stevenson, ... Journal of medicinal chemistry 35 (11), 1954-1968, 2002 | 260 | 2002 |
Design and selection parameters to accelerate the discovery of novel central nervous system positron emission tomography (PET) ligands and their application in the development … L Zhang, A Villalobos, EM Beck, T Bocan, TA Chappie, L Chen, ... Journal of medicinal chemistry 56 (11), 4568-4579, 2013 | 178 | 2013 |
Identification of molecular determinants that are important in the assembly of N-methyl-D-aspartate receptors E Meddows, B Le Bourdelles, S Grimwood, K Wafford, S Sandhu, ... Journal of Biological Chemistry 276 (22), 18795-18803, 2001 | 173 | 2001 |
Effect of plasma protein binding on in vivo activity and brain penetration of glycine/NMDA receptor antagonists M Rowley, JJ Kulagowski, AP Watt, D Rathbone, GI Stevenson, ... Journal of medicinal chemistry 40 (25), 4053-4068, 1997 | 171 | 1997 |
2-Carboxytetrahydroquinolines. Conformational and stereochemical requirements for antagonism of the glycine site on the N-methyl-D-aspartate (NMDA) receptor RW Carling, PD Leeson, AM Moseley, R Baker, AC Foster, S Grimwood, ... Journal of medicinal chemistry 35 (11), 1942-1953, 1992 | 134 | 1992 |
Target site occupancy: emerging generalizations from clinical and preclinical studies S Grimwood, PR Hartig Pharmacology & therapeutics 122 (3), 281-301, 2009 | 130 | 2009 |
Duration of action of a broad range of selective κ-opioid receptor antagonists is positively correlated with c-Jun N-terminal kinase-1 activation EJ Melief, M Miyatake, FI Carroll, C Beguin, WA Carlezon, BM Cohen, ... Molecular pharmacology 80 (5), 920-929, 2011 | 129 | 2011 |
3-Nitro-3, 4-dihydro-2 (1H)-quinolones. Excitatory amino acid antagonists acting at glycine-site NMDA and (RS)-. alpha.-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptors RW Carling, PD Leeson, KW Moore, JD Smith, CR Moyes, IM Mawer, ... Journal of medicinal chemistry 36 (22), 3397-3408, 1993 | 122 | 1993 |
Anticonvulsant activity of glycine-site NMDA antagonists. 2. trans 2-carboxy-4-substituted tetrahydroquinolines. RW Carling, PD Leeson, AM Moseley, JD Smith, K Saywell, ... Bioorganic & Medicinal Chemistry Letters 3 (1), 65-70, 1993 | 117 | 1993 |
NR2B-containing NMDA receptors are up-regulated in temporal cortex in schizophrenia S Grimwood, P Slater, JFW Deakin, PH Hutson Neuroreport 10 (3), 461-465, 1999 | 116 | 1999 |
Development of an intact cell reporter gene β-lactamase assay for G protein-coupled receptors for high-throughput screening P Kunapuli, R Ransom, KL Murphy, D Pettibone, J Kerby, S Grimwood, ... Analytical biochemistry 314 (1), 16-29, 2003 | 114 | 2003 |
Recombinant Human NMDA Homomeric NR1 Receptors Expressed in Mammalian Cells Form a High‐Affinity Glycine Antagonist Binding Site S Grimwood, B Le Bourdellès, PJ Whiting Journal of neurochemistry 64 (2), 525-530, 1995 | 105 | 1995 |
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. S Grimwood, AM Moseley, RW Carling, PD Leeson, AC Foster Molecular pharmacology 41 (5), 923-930, 1992 | 96 | 1992 |
4-Substituted-3-phenylquinolin-2(1H)-ones: Acidic and Nonacidic Glycine Site N-Methyl-d-aspartate Antagonists with in Vivo Activity RW Carling, PD Leeson, KW Moore, CR Moyes, M Duncton, ML Hudson, ... Journal of medicinal chemistry 40 (5), 754-765, 1997 | 92 | 1997 |
Discovery of the Potent and Selective M1 PAM-Agonist N-[(3R,4S)-3-Hydroxytetrahydro-2H-pyran-4-yl]-5-methyl-4-[4-(1,3-thiazol-4-yl)benzyl]pyridine-2 … JE Davoren, CW Lee, M Garnsey, MA Brodney, J Cordes, K Dlugolenski, ... Journal of medicinal chemistry 59 (13), 6313-6328, 2016 | 87 | 2016 |
Kynurenic acid analogues with improved affinity and selectivity for the glycine site on the N-methyl-D-aspartate receptor from rat brain. AC Foster, JA Kemp, PD Leeson, S Grimwood, AE Donald, GR Marshall, ... Molecular pharmacology 41 (5), 914-922, 1992 | 82 | 1992 |
Application of cross-species PET imaging to assess neurotransmitter release in brain SJ Finnema, M Scheinin, M Shahid, J Lehto, E Borroni, B Bang-Andersen, ... Psychopharmacology 232, 4129-4157, 2015 | 81 | 2015 |
Phosphodiesterase 9A regulates central cGMP and modulates responses to cholinergic and monoaminergic perturbation in vivo RJ Kleiman, DS Chapin, C Christoffersen, J Freeman, KR Fonseca, ... Journal of Pharmacology and Experimental Therapeutics 341 (2), 396-409, 2012 | 81 | 2012 |
Pharmacological characterization of 2-methyl-N-((2′-(pyrrolidin-1-ylsulfonyl) biphenyl-4-yl) methyl) propan-1-amine (PF-04455242), a high-affinity antagonist selective for κ … S Grimwood, Y Lu, AW Schmidt, MA Vanase-Frawley, A Sawant-Basak, ... Journal of Pharmacology and Experimental Therapeutics 339 (2), 555-566, 2011 | 69 | 2011 |
Generation and Characterisation of Stable Cell Lines Expressing Recombinant Human N‐Methyl‐d‐Aspartate Receptor Subtypes S Grimwood, B Le Bourdellès, JR Atack, C Barton, W Cockett, SM Cook, ... Journal of neurochemistry 66 (6), 2239-2247, 1996 | 68 | 1996 |