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Paul Leeson

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Robert W Carling; Kevin W Moore; Leslie J Street; Deborah Wild; Catherine Isted; Paul D Leeson; Steven Thomas; desmond oconnor; Ruth M McKernan; Kathleen Quirk; Susan M Cook; John R Atack; Keith A Wafford; Sally-Anne Thompson; Gerard R Dawson; Pushpinder Ferris; José L Castro
3-phenyl-6-(2-pyridyl)methyloxy-1,2,4-triazolo[3,4-a]phthalazines and analogues: high-affinity gamma-aminobutyric acid-A benzodiazepine receptor ligands with alpha 2, alpha 3, and alpha 5-subtype binding selectivity over alpha 1.
Robert W Carling; Kevin W Moore; Christopher Moyes; E A Jones; K Bonner; F Emms; Rose Marwood; Smita Patel; S Patel; AE Fletcher; M Beer; Bindi Sohal; Andrew Pike; Paul D Leeson
1-(3-Cyanobenzylpiperidin-4-yl)-5-methyl-4-phenyl-1, 3-dihydroimidazol-2-one: a selective high-affinity antagonist for the human dopamine D(4) receptor with excellent selectivity over ion channels.
Kevin W Moore; K Bonner; E A Jones; F Emms; Paul D Leeson; Rose Marwood; Smita Patel; S Patel; Michael Rowley; Steven Thomas; Robert W Carling
4-N-linked-heterocyclic piperidine derivatives with high affinity and selectivity for human dopamine D4 receptors.

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All Publications

2004: Robert W Carling; Kevin W Moore; Leslie J Street; Deborah Wild; Catherine Isted; Paul D Leeson; Steven Thomas; desmond oconnor; Ruth M McKernan; Kathleen Quirk; Susan M Cook; John R Atack; Keith A Wafford; Sally-Anne Thompson; Gerard R Dawson; Pushpinder Ferris; José L Castro
3-phenyl-6-(2-pyridyl)methyloxy-1,2,4-triazolo[3,4-a]phthalazines and analogues: high-affinity gamma-aminobutyric acid-A benzodiazepine receptor ligands with alpha 2, alpha 3, and alpha 5-subtype binding selectivity over alpha 1.
Journal of medicinal chemistry 2004;47(7):1807-22.
1999: Robert W Carling; Kevin W Moore; Christopher Moyes; E A Jones; K Bonner; F Emms; Rose Marwood; Smita Patel; S Patel; AE Fletcher; M Beer; Bindi Sohal; Andrew Pike; Paul D Leeson
1-(3-Cyanobenzylpiperidin-4-yl)-5-methyl-4-phenyl-1, 3-dihydroimidazol-2-one: a selective high-affinity antagonist for the human dopamine D(4) receptor with excellent selectivity over ion channels.
Journal of medicinal chemistry 1999;42(14):2706-15.
1999: Kevin W Moore; K Bonner; E A Jones; F Emms; Paul D Leeson; Rose Marwood; Smita Patel; S Patel; Michael Rowley; Steven Thomas; Robert W Carling
4-N-linked-heterocyclic piperidine derivatives with high affinity and selectivity for human dopamine D4 receptors.
Bioorganic & medicinal chemistry letters 1999;9(9):1285-90.
1999: Neil R Curtis; Janusz J Kulagowski; Paul D Leeson; Mark P Ridgill; F Emms; SB Freedman; Smita Patel; S Patel
Synthesis and sar of 2- and 3-substituted 7-azaindoles as potential dopamine D4 ligands.
Bioorganic & medicinal chemistry letters 1999;9(4):585-8.
1998: S Bourrain; Ian Collins; Joseph G Neduvelil; Michael Rowley; Paul D Leeson; Smita Patel; S Patel; F Emms; Rose Marwood; Kerry L Chapman; AE Fletcher; GA Showell
Substituted pyrazoles as novel selective ligands for the human dopamine D4 receptor.
Bioorganic & medicinal chemistry 1998;6(10):1731-43.
1998: Ian Collins; Michael Rowley; William B Davey; F Emms; Rose Marwood; Smita Patel; S Patel; A Fletcher; I C Ragan; Paul D Leeson; A L Scott; TP Broten
3-(1-piperazinyl)-4,5-dihydro-1H-benzo[g]indazoles: high affinity ligands for the human dopamine D4 receptor with improved selectivity over ion channels.
Bioorganic & medicinal chemistry 1998;6(6):743-53.
1998: GA Showell; F Emms; Rose Marwood; desmond oconnor; Smita Patel; Paul D Leeson
Binding of 2,4-disubstituted morpholines at human D4 dopamine receptors.
Bioorganic & medicinal chemistry 1998;6(1):1-8.
1997: Michael Rowley; Janusz J Kulagowski; Alan P Watt; D Rathbone; GI Stevenson; Robert W Carling; R Baker; George R Marshall; J A Kemp; A C Foster; Sarah Grimwood; Richard Hargreaves; C Hurley; KL Saywell; mark david tricklebank; Paul D Leeson
Effect of plasma protein binding on in vivo activity and brain penetration of glycine/NMDA receptor antagonists.
Journal of medicinal chemistry 1997;40(25):4053-68.
1997: Linda J Bristow; Neil Collinson; Gina P Cook; Neil R Curtis; SB Freedman; Janusz J Kulagowski; Paul D Leeson; Smita Patel; C Ian Ragan; Mark P Ridgill; KL Saywell; mark david tricklebank
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;283(3):1256-63.
1997: Smita Patel; S Freedman; Kerry L Chapman; F Emms; AE Fletcher; M Knowles; Rose Marwood; George McAllister; Janice Myers; Neil R Curtis; Janusz J Kulagowski; Paul D Leeson; Mark P Ridgill; M Graham; S Matheson; D Rathbone; Alan P Watt; Linda J Bristow; Nadia M J Rupniak; E Baskin; Joseph J Lynch; C Ian Ragan
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;283(2):636-47.
1997: Michael Rowley; Ian Collins; Howard B Broughton; William B Davey; R Baker; F Emms; Rose Marwood; Smita Patel; S Patel; C Ian Ragan; SB Freedman; R Ball; Paul D Leeson
4-Heterocyclylpiperidines as selective high-affinity ligands at the human dopamine D4 receptor.
Journal of medicinal chemistry 1997;40(15):2374-85.
1997: Robert W Carling; Paul D Leeson; Kevin W Moore; Christopher Moyes; M Duncton; M L Hudson; R Baker; A C Foster; Sarah Grimwood; J A Kemp; George R Marshall; mark david tricklebank; KL Saywell
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;40(5):754-65.
1996: Smita Patel; S Patel; Rose Marwood; F Emms; D Marston; Paul D Leeson; Neil R Curtis; Janusz J Kulagowski; S B Freedman
Identification and pharmacological characterization of [125I]L-750,667, a novel radioligand for the dopamine D4 receptor.
Molecular pharmacology 1996;50(6):1658-64.
1996: Linda J Bristow; Peter H Hutson; Janusz J Kulagowski; Paul D Leeson; S Matheson; Fraser Murray; D Rathbone; KL Saywell; L Thorn; Alan P Watt; mark david tricklebank
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;279(2):492-501.
1996: Michael Rowley; Howard B Broughton; Ian Collins; R Baker; F Emms; Rose Marwood; Smita Patel; S Patel; C Ian Ragan; S B Freedman; Paul D Leeson
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;39(10):1943-5.
1996: Janusz J Kulagowski; Howard B Broughton; Neil R Curtis; I M Mawer; Mark P Ridgill; R Baker; F Emms; S B Freedman; Rose Marwood; Smita Patel; S Patel; C Ian Ragan; Paul D Leeson
3-((4-(4-Chlorophenyl)piperazin-1-yl)-methyl)-1H-pyrrolo-2,3-b-pyridine: an antagonist with high affinity and selectivity for the human dopamine D4 receptor.
Journal of medicinal chemistry 1996;39(10):1941-2.
1996: Linda J Bristow; K L Flatman; Peter H Hutson; Janusz J Kulagowski; Paul D Leeson; L Young; mark david tricklebank
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;277(2):578-85.
1995: Sarah Grimwood; Janusz J Kulagowski; I M Mawer; Michael Rowley; Paul D Leeson; A C Foster
Allosteric modulation of the glutamate site on the NMDA receptor by four novel glycine site antagonists.
European journal of pharmacology 1995;290(3):221-6.
1994: Paul D Leeson; L L Iversen
The glycine site on the NMDA receptor: structure-activity relationships and therapeutic potential.
Journal of medicinal chemistry 1994;37(24):4053-67.
1994: mark david tricklebank; Linda J Bristow; Peter H Hutson; Paul D Leeson; Michael Rowley; KL Saywell; L Singh; F David Tattersall; L Thorn; B J Williams
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;113(3):729-36.
1994: Janusz J Kulagowski; R Baker; Neil R Curtis; Paul D Leeson; I M Mawer; A M Moseley; Mark P Ridgill; Michael Rowley; I Stansfield; A C Foster
3'-(Arylmethyl)- and 3'-(aryloxy)-3-phenyl-4-hydroxyquinolin-2(1H)-ones: orally active antagonists of the glycine site on the NMDA receptor.
Journal of medicinal chemistry 1994;37(10):1402-5.
1993: Robert W Carling; Paul D Leeson; Kevin W Moore; J D Smith; Christopher Moyes; I M Mawer; Steven Thomas; T Chan; R Baker; A C Foster
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.
Journal of medicinal chemistry 1993;36(22):3397-408.
1993: Michael Rowley; Paul D Leeson; GI Stevenson; A M Moseley; I Stansfield; I Sanderson; L Robinson; R Baker; J A Kemp; George R Marshall
3-Acyl-4-hydroxyquinolin-2(1H)-ones. Systemically active anticonvulsants acting by antagonism at the glycine site of the N-methyl-D-aspartate receptor complex.
Journal of medicinal chemistry 1993;36(22):3386-96.
1992: Paul D Leeson; Robert W Carling; Kevin W Moore; A M Moseley; J D Smith; G Stevenson; T Chan; R Baker; A C Foster; Sarah Grimwood
4-Amido-2-carboxytetrahydroquinolines. Structure-activity relationships for antagonism at the glycine site of the NMDA receptor.
Journal of medicinal chemistry 1992;35(11):1954-68.
1992: Robert W Carling; Paul D Leeson; A M Moseley; R Baker; A C Foster; Sarah Grimwood; J A Kemp; George R Marshall
2-Carboxytetrahydroquinolines. Conformational and stereochemical requirements for antagonism of the glycine site on the NMDA receptor.
Journal of medicinal chemistry 1992;35(11):1942-53.
1992: L Iversen; A C Foster; Raymond G Hill; S D Iversen; J A Kemp; Paul D Leeson; Nadia M J Rupniak; KL Saywell; mark david tricklebank; B J Williams
Neurotoxin-related research: from the laboratory to the clinic.
Annals of the New York Academy of Sciences 1992;648():207-18.
1992: Sarah Grimwood; A M Moseley; Robert W Carling; Paul D Leeson; A C Foster
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;41(5):923-30.
1992: A C Foster; J A Kemp; Paul D Leeson; Sarah Grimwood; A E Donald; George R Marshall; T Priestley; J D Smith; Robert W Carling
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;41(5):914-22.
1991: David G Reid; K Gajjar; S P Robinson; Deirdre M B Hickey; Gregory Martin Benson; C Haynes; Paul D Leeson; C M Whittaker
Precipitation and 13C-NMR relaxation enhancement measurements of the interactions of bile acids with synthetic cationic bile acid derivatives, and with spin labelled fatty acids.
Chemistry and physics of lipids 1991;60(2):143-51.
1991: Paul D Leeson; R Baker; Robert W Carling; Neil R Curtis; Kevin W Moore; B J Williams; A C Foster; A E Donald; J A Kemp; George R Marshall
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;34(4):1243-52.
1990: Paul D Leeson; Robert W Carling; K James; J D Smith; Kevin W Moore; E H Wong; R Baker
Role of hydrogen bonding in ligand interaction with the N-methyl-D-aspartate receptor ion channel.
Journal of medicinal chemistry 1990;33(5):1296-305.
1990: L Singh; A E Donald; A C Foster; Peter H Hutson; L L Iversen; S D Iversen; J A Kemp; Paul D Leeson; George R Marshall; R J Oles
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 gamma-butyrolactone-like sedative.
Proceedings of the National Academy of Sciences of the United States of America 1990;87(1):347-51.
1990: Paul D Leeson; K James; Robert W Carling; E H Wong; R Baker
MK-801 analogues: molecular properties required for recognition by the N-methyl-D-aspartate receptor.
Progress in clinical and biological research 1990;361():513-8.
1989: David G Reid; Lesley K MacLachlan; M Voyle; Paul D Leeson
A proton and fluorine-19 nuclear magnetic resonance and fluorescence study of the binding of some natural and synthetic thyromimetics to prealbumin (transthyretin).
The Journal of biological chemistry 1989;264(4):2013-23.
1989: Paul D Leeson; J C Emmett; V P Shah; G A Showell; R Novelli; H D Prain; Gregory Martin Benson; D Ellis; N J Pearce; A H Underwood
Selective thyromimetics. Cardiac-sparing thyroid hormone analogues containing 3'-arylmethyl substituents.
Journal of medicinal chemistry 1989;32(2):320-36.
1988: J A Kemp; A C Foster; Paul D Leeson; T Priestley; R Tridgett; L L Iversen; G N Woodruff
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 of the United States of America 1988;85(17):6547-50.
1988: Paul D Leeson; D Ellis; J C Emmett; V P Shah; G A Showell; A H Underwood
Thyroid hormone analogues. Synthesis of 3'-substituted 3,5-diiodo-L-thyronines and quantitative structure-activity studies of in vitro and in vivo thyromimetic activities in rat liver and heart.
Journal of medicinal chemistry 1988;31(1):37-54.
1986: A H Underwood; J C Emmett; D Ellis; S B Flynn; Paul D Leeson; Gregory Martin Benson; R Novelli; N J Pearce; V P Shah
A thyromimetic that decreases plasma cholesterol levels without increasing cardiac activity.
Nature 1986;324(6096):425-9.
1984: Gregory Martin Benson; D Ellis; J C Emmett; Paul D Leeson; N J Pearce; V P Shah; A H Underwood
3'-Acetyl-3,5-diiodo-L-thyronine: a novel highly active thyromimetic with low receptor affinity.
Biochemical pharmacology 1984;33(20):3143-9.