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1. Mitochondrial C5aR1 activity in macrophages controls IL-1β production underlying sterile inflammation

Author

Niyonzima, Nathalie, primary, Rahman, Jubayer, additional, Kunz, Natalia, additional, West, Erin E., additional, Freiwald, Tilo, additional, Desai, Jigar V., additional, Merle, Nicolas S., additional, Gidon, Alexandre, additional, Sporsheim, Bjørnar, additional, Lionakis, Michail S., additional, Evensen, Kristin, additional, Lindberg, Beate, additional, Skagen, Karolina, additional, Skjelland, Mona, additional, Singh, Parul, additional, Haug, Markus, additional, Ruseva, Marieta M., additional, Kolev, Martin, additional, Bibby, Jack, additional, Marshall, Olivia, additional, O’Brien, Brett, additional, Deeks, Nigel, additional, Afzali, Behdad, additional, Clark, Richard J., additional, Woodruff, Trent M., additional, Pryor, Milton, additional, Yang, Zhi-Hong, additional, Remaley, Alan T., additional, Mollnes, Tom E., additional, Hewitt, Stephen M., additional, Yan, Bingyu, additional, Kazemian, Majid, additional, Kiss, Máté G., additional, Binder, Christoph J., additional, Halvorsen, Bente, additional, Espevik, Terje, additional, and Kemper, Claudia, additional

Published
2021
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6. Discovery of Tetrahydropyrazolopyridine as Sphingosine 1-Phosphate Receptor 3 (S1P3)-Sparing S1P1 Agonists Active at Low Oral Doses

Author

Demont, Emmanuel H., primary, Bailey, James M., additional, Bit, Rino A., additional, Brown, Jack A., additional, Campbell, Colin A., additional, Deeks, Nigel, additional, Dowell, Simon J., additional, Eldred, Colin, additional, Gaskin, Pam, additional, Gray, James R. J., additional, Haynes, Andrea, additional, Hirst, David J., additional, Holmes, Duncan S., additional, Kumar, Umesh, additional, Morse, Mary A., additional, Osborne, Greg J., additional, Renaux, Jessica F., additional, Seal, Gail A. L., additional, Smethurst, Chris A., additional, Taylor, Simon, additional, Watson, Robert, additional, Willis, Robert, additional, and Witherington, Jason, additional

Published
2016
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7. Navigating CYP1A Induction and Arylhydrocarbon Receptor Agonism in Drug Discovery. A Case History with S1P1 Agonists

Author

Taylor, Simon J., primary, Demont, Emmanuel H., additional, Gray, James, additional, Deeks, Nigel, additional, Patel, Aarti, additional, Nguyen, Dung, additional, Taylor, Maxine, additional, Hood, Steve, additional, Watson, Robert J., additional, Bit, Rino A., additional, McClure, Fiona, additional, Ashall, Holly, additional, and Witherington, Jason, additional

Published
2015
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10. Discovery of Tetrahydropyrazolopyridine as Sphingosine 1-Phosphate Receptor 3 (S1P3)-Sparing S1P1 Agonists Active at Low Oral Doses.

Author

Demont, Emmanuel H., Bailey, James M., Bit, Rino A., Brown, Jack A., Campbell, Colin A., Deeks, Nigel, Dowell, Simon J., Eldred, Colin, Gaskin, Pam, Gray, James R. J., Haynes, Andrea, Hirst, David J., Holmes, Duncan S., Kumar, Umesh, Morse, Mary A., Osborne, Greg J., Renaux, Jessica F., Seal, Gail A. L., Smethurst, Chris A., and Taylor, Simon

Published
2016
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12. The utility of pharmacokinetic–pharmacodynamic modeling in the discovery and optimization of selective S1P1agonists

Author

Taylor, Simon, primary, Gray, James R. J., additional, Willis, Robert, additional, Deeks, Nigel, additional, Haynes, Andrea, additional, Campbell, Colin, additional, Gaskin, Pam, additional, Leavens, Karen, additional, Demont, Emmanuel, additional, Dowell, Simon, additional, Cryan, Jenni, additional, Morse, Mary, additional, Patel, Aarti, additional, Garden, Helen, additional, and Witherington, Jason, additional

Published
2012
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13. Discovery of a Brain-Penetrant S1P3-Sparing Direct Agonist of the S1P1 and S1P5 Receptors Efficacious at Low Oral Dose

Author

Demont, Emmanuel H., primary, Arpino, Sandra, additional, Bit, Rino A., additional, Campbell, Colin A., additional, Deeks, Nigel, additional, Desai, Sapna, additional, Dowell, Simon J., additional, Gaskin, Pam, additional, Gray, James R. J., additional, Harrison, Lee A., additional, Haynes, Andrea, additional, Heightman, Tom D., additional, Holmes, Duncan S., additional, Humphreys, Philip G., additional, Kumar, Umesh, additional, Morse, Mary A., additional, Osborne, Greg J., additional, Panchal, Terry, additional, Philpott, Karen L., additional, Taylor, Simon, additional, Watson, Robert, additional, Willis, Robert, additional, and Witherington, Jason, additional

Published
2011
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14. Discovery of a Selective S1P1 Receptor Agonist Efficacious at Low Oral Dose and Devoid of Effects on Heart Rate

Author

Demont, Emmanuel H., primary, Andrews, Benjamin I., additional, Bit, Rino A., additional, Campbell, Colin A., additional, Cooke, Jason W. B., additional, Deeks, Nigel, additional, Desai, Sapna, additional, Dowell, Simon J., additional, Gaskin, Pam, additional, Gray, James R. J., additional, Haynes, Andrea, additional, Holmes, Duncan S., additional, Kumar, Umesh, additional, Morse, Mary A., additional, Osborne, Greg J., additional, Panchal, Terry, additional, Patel, Bela, additional, Perboni, Alcide, additional, Taylor, Simon, additional, Watson, Robert, additional, Witherington, Jason, additional, and Willis, Robert, additional

Published
2011
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16. Tricyclic azepine derivatives as selective brain penetrant 5-HT6 receptor antagonists

Author

Trani, Giancarlo, primary, Baddeley, Stuart M., additional, Briggs, Michael A., additional, Chuang, Tsu T., additional, Deeks, Nigel J., additional, Johnson, Christopher N., additional, Khazragi, Abir A., additional, Mead, Tania L., additional, Medhurst, Andrew D., additional, Milner, Peter H., additional, Quinn, Leann P., additional, Ray, Alison M., additional, Rivers, Dean A., additional, Stean, Tania O., additional, Stemp, Geoffrey, additional, Trail, Brenda K., additional, and Witty, David R., additional

Published
2008
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19. Bicyclic heteroarylpiperazines as selective brain penetrant 5-HT6 receptor antagonists

Author

Ahmed, Mahmood, primary, Briggs, Michael A., additional, Bromidge, Steven M., additional, Buck, Tania, additional, Campbell, Lorraine, additional, Deeks, Nigel J., additional, Garner, Ashley, additional, Gordon, Laurie, additional, Hamprecht, Dieter W., additional, Holland, Vicky, additional, Johnson, Christopher N., additional, Medhurst, Andrew D., additional, Mitchell, Darren J., additional, Moss, Stephen F., additional, Powles, Jenifer, additional, Seal, Jon T., additional, Stean, Tania O., additional, Stemp, Geoffrey, additional, Thompson, Mervyn, additional, Trail, Brenda, additional, Upton, Neil, additional, Winborn, Kim, additional, and Witty, David R., additional

Published
2005
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20. WITHDRAWN: Bicyclic heteroarylpiperazines as selective brain penetrant 5-HT6 receptor antagonists

Author

Ahmed, Mahmood, primary, Briggs, Michael A., additional, Bromidge, Steven M., additional, Buck, Tania, additional, Campbell, Lorraine, additional, Deeks, Nigel J., additional, Garner, Ashley, additional, Gordon, Laurie, additional, Hamprecht, Dieter W., additional, Holland, Vicky, additional, Johnson, Christopher N., additional, Medhurst, Andrew D., additional, Mitchell, Darren J., additional, Moss, Stephen F., additional, Powles, Jenifer, additional, Seal, Jon T., additional, Stean, Tania O., additional, Stemp, Geoffrey, additional, Thompson, Mervyn, additional, Trail, Brenda, additional, Upton, Neil, additional, Winborn, Kim, additional, and Witty, David R., additional

Published
2005
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21. SB-656104-A, a novel selective 5-HT7receptor antagonist, modulates REM sleep in rats

Author

Thomas, David R, primary, Melotto, Sergio, additional, Massagrande, Mario, additional, Gribble, Andrew D, additional, Jeffrey, Phillip, additional, Stevens, Alexander J, additional, Deeks, Nigel J, additional, Eddershaw, Peter J, additional, Fenwick, Susan H, additional, Riley, Graham, additional, Stean, Tania, additional, Scott, Claire M, additional, Hill, Matthew J, additional, Middlemiss, Derek N, additional, Hagan, Jim J, additional, Price, Gary W, additional, and Forbes, Ian T, additional

Published
2003
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22. Pharmacological profile of SB-357134: A potent, selective, brain penetrant, and orally active 5-HT6 receptor antagonist

Author

Stean, Tania O, primary, Hirst, Warren D, additional, Thomas, David R, additional, Price, Gary W, additional, Rogers, Derek, additional, Riley, Graham, additional, Bromidge, Steven M, additional, Serafinowska, Halina T, additional, Smith, Douglas R, additional, Bartlett, Sarah, additional, Deeks, Nigel, additional, Duxon, Mark, additional, and Upton, Neil, additional

Published
2002
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23. Characterization of SB-269970-A, a selective 5-HT7receptor antagonist

Author

Hagan, Jim J, primary, Price, Gary W, additional, Jeffrey, Phillip, additional, Deeks, Nigel J, additional, Stean, Tania, additional, Piper, David, additional, Smith, Martin I, additional, Upton, Neil, additional, Medhurst, Andrew D, additional, Middlemiss, Derek N, additional, Riley, Graham J, additional, Lovell, Peter J, additional, Bromidge, Steven M, additional, and Thomas, David R, additional

Published
2000
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24. WITHDRAWN: Bicyclic heteroarylpiperazines as selective brain penetrant 5-HT 6 receptor antagonists

Author

Ahmed, Mahmood, Briggs, Michael A., Bromidge, Steven M., Buck, Tania, Campbell, Lorraine, Deeks, Nigel J., Garner, Ashley, Gordon, Laurie, Hamprecht, Dieter W., Holland, Vicky, Johnson, Christopher N., Medhurst, Andrew D., Mitchell, Darren J., Moss, Stephen F., Powles, Jenifer, Seal, Jon T., Stean, Tania O., Stemp, Geoffrey, Thompson, Mervyn, Trail, Brenda, Upton, Neil, Winborn, Kim, and Witty, David R.

Published
2005
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25. Bicyclic heteroarylpiperazines as selective brain penetrant 5-HT 6 receptor antagonists

Author

Ahmed, Mahmood, Briggs, Michael A., Bromidge, Steven M., Buck, Tania, Campbell, Lorraine, Deeks, Nigel J., Garner, Ashley, Gordon, Laurie, Hamprecht, Dieter W., Holland, Vicky, Johnson, Christopher N., Medhurst, Andrew D., Mitchell, Darren J., Moss, Stephen F., Powles, Jenifer, Seal, Jon T., Stean, Tania O., Stemp, Geoffrey, Thompson, Mervyn, Trail, Brenda, Upton, Neil, Winborn, Kim, and Witty, David R.

Published
2005
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28. The utility of pharmacokinetic-pharmacodynamic modeling in the discovery and optimization of selective S1P1 agonists.

Author

Taylor, Simon, Gray, James R. J., Willis, Robert, Deeks, Nigel, Haynes, Andrea, Campbell, Colin, Gaskin, Pam, Leavens, Karen, Demont, Emmanuel, Dowell, Simon, Cryan, Jenni, Morse, Mary, Patel, Aarti, Garden, Helen, and Witherington, Jason

Subjects
LYMPHOPENIA, ALLOMETRY, MATHEMATICAL optimization, PHARMACODYNAMICS, CHEMICAL agonists, DRUG design
Abstract

Sphingosine-1-phosphate (S1P1) receptor agonists such as Fingolimod (FTY-720) are a novel class of immunomodulators that have clinical utility in the treatment of remitting relapsing multiples sclerosis. This class of compound act by inducing peripheral lymphopenia. Using an integrated pharmacokinetic/pharmacodynamic (PK–PD) approach based on an in vivo rat model, novel S1P1 agonists were identified with a predicted more rapid rate of reversibility of lymphocyte reduction in human compared to Fingolimod. The in vivo potency of 15 compounds based on PK–PD modelling of the rat lymphocyte reduction model was correlated with in vitro measures of potency at the S1P1 receptor using β arrestin recruitment and G-protein signalling. A structurally novel S1P1 agonist was identified and predictions of human pharmacokinetics and clinical dose are presented. [ABSTRACT FROM AUTHOR]

Published
2012
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29. Discovery of a Brain-Penetrant S1P3-Sparing Direct Agonist of the S1P1and S1P5Receptors Efficacious at Low Oral Dose.

Author

Demont, Emmanuel H., Arpino, Sandra, Bit, Rino A., Campbell, Colin A., Deeks, Nigel, Desai, Sapna, Dowell, Simon J., Gaskin, Pam, Gray, James R. J., Harrison, Lee A., Haynes, Andrea, Heightman, Tom D., Holmes, Duncan S., Humphreys, Philip G., Kumar, Umesh, Morse, Mary A., Osborne, Greg J., Panchal, Terry, Philpott, Karen L., and Taylor, Simon

Published
2011
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30. Selective alpha7 nicotinic acetylcholine receptor agonists worsen disease in experimental colitis.

Author

Snoek, Susanne A, Verstege, Marleen I, Van Der Zanden, Esmerij P, Deeks, Nigel, Bulmer, David C, Skynner, Michael, Lee, Kevin, Te Velde, Anje A, Boeckxstaens, Guy E, and De Jonge, Wouter J

Subjects
CHOLINERGIC receptors, COLITIS, VAGUS nerve, INFLAMMATION, DRUG dosage, CYTOKINES, TARGETED drug delivery, LABORATORY mice, ANIMAL experimentation, BIOLOGICAL models, CELL culture, COMPARATIVE studies, DOSE-effect relationship in pharmacology, HYDROCARBONS, INJECTIONS, MACROPHAGES, RESEARCH methodology, MEDICAL cooperation, MICE, NICOTINE, RESEARCH, DNA-binding proteins, EVALUATION research, SEVERITY of illness index, NICOTINIC agonists, PHARMACODYNAMICS
Abstract

Background and Purpose: In various models vagus nerve activation has been shown to ameliorate intestinal inflammation, via nicotinic acetylcholine receptors (nAChRs) expressed on immune cells. As the alpha7 nAChR has been put forward to mediate this effect, we studied the effect of nicotine and two selective alpha7 nAChR agonists (AR-R17779, (-)-spiro[1-azabicyclo[2.2.2] octane-3,5'-oxazolidin-2'-one and GSK1345038A) on disease severity in two mouse models of experimental colitis.Experimental Approach: Colitis was induced by administration of 1.5% dextran sodium sulphate (DSS) in drinking water or 2 mg 2,4,6-trinitrobenzene sulphonic acid (TNBS) intrarectally. Nicotine (0.25 and 2.50 micromol.kg(-1)), AR-R17779 (0.6-30 micromol.kg(-1)) or GSK1345038A (6-120 micromol.kg(-1)) was administered daily by i.p. injection. After 7 (DSS) or 5 (TNBS) days clinical parameters and colonic inflammation were scored.Key Results: Nicotine and both alpha7 nAChR agonists reduced the activation of NF-kappaB and pro-inflammatory cytokines in whole blood and macrophage cultures. In DSS colitis, nicotine treatment reduced colonic cytokine production, but failed to reduce disease parameters. Reciprocally, treatment with AR-R17779 or GSK1345038A worsened disease and led to increased colonic pro-inflammatory cytokine levels in DSS colitis. The highest doses of GSK1345038A (120 micromol.kg(-1)) and AR-R17779 (30 micromol.kg(-1)) ameliorated clinical parameters, without affecting colonic inflammation. Neither agonist ameliorated TNBS-induced colitis.Conclusions and Implications: Although nicotine reduced cytokine responses in vitro, both selective alpha7 nAChR agonists worsened the effects of DSS-induced colitis or were ineffective in those of TNBS-induced colitis. Our data indicate the need for caution in evaluating alpha7 nAChR as a drug target in colitis. [ABSTRACT FROM AUTHOR]

Published
2010
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31. Short papers in pharmaceutical analysis

Author

Thomas, Nicolette, primary, Thompson, Colin W., additional, Woldemariam, Tibebe Z., additional, Linley, Peter A., additional, Fell, Anthony F., additional, Deeks, Nigel J., additional, Smith, Graeme T., additional, Undre, Nas A., additional, Thawley, Alan R., additional, Winton, Colin F., additional, Fowles, S. E., additional, Pierce, D. M., additional, Hodge, A. Vere, additional, Meredith, Christopher N. C., additional, White, Trevor J., additional, Everett, Jeremy R., additional, Hart, Janet, additional, and Robins, Keith, additional

Published
1990
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32. SB-656104-A, a novel selective 5-HT7 receptor antagonist, modulates REM sleep in rats.

Author

Thomas, David R., Melotto, Sergio, Massagrande, Mario, Gribble, Andrew D., Jeffrey, Phillip, Stevens, Alexander J., Deeks, Nigel J., Eddershaw, Peter J., Fenwick, Susan H., Riley, Graham, Stean, Tania, Scott, Claire M., Hill, Matthew J., Middlemiss, Derek N., Hagan, Jim J., Price, Gary W., and Forbes, Ian T.

Subjects
SEROTONIN, RAPID eye movement sleep, BODY temperature, PHARMACOKINETICS, GUINEA pigs, LABORATORY rats
Abstract

1 (6-((R)-2-(2-[4-(4-Chloro-phenoxy)-piperidin-1-yll-ethyll-pyrrolidine-l-sulphonyl)-1 H-indole hydrochloride) (SB-656104-A). a novel 5-hydroxytryptamine (5-HT7) receptor antagonist, potently inhibited [3H]-SB-269970 binding to the human cloned 5-HT7/.../ (pK... 8.7±0.1) and 5-HT7(b) (pK... 8.5 ±0.2) receptor variants and the rat native receptor (pK1 8.8 ±0.2). The compound displayed at least 30-fold selectivity for the human 5-HT7(a), receptor versus other human cloned 5-HT receptors apart from the 5-HTiD receptor (∼10-fold selective). 2 SB-656104-A antagonised competitively the 5-carboxamidotryptamine (5-CT)-induced accumulation of cyclic AMP in h5-HT7(a)/HEK293 cells with a pA2 of 8.5. 3 Following a constant rate iv infusion to steady state in rats, SB-656104 had a blood clearance (CLb) of 58±6ml min-1 kg-1 and was CNS penetrant with a steady-state brain: blood ratio of 0.9:1. Following i.p. administration to rats (l0 mg kg-1), the compound displayed a t1 2 of l.4 h with mean brain and blood concentrations (at 1 h after dosing) of 0.80 and 1.0 μM. respectively. 4 SB-656104-A produced a significant reversal of the 5-CT-induced hypothermic effect in guinea pigs, a pharmacodynamic model of 5-HT7 receptor interaction in viro (ED50 2mg kg-1). 5 SB-656I04-A, administered to rats at the beginning of the sleep period (CT 0), significantly increased the latency to onset of rapid eye movement (REM) sleep at 30mgkg-1 i.p. ( + 93%) and reduced the total amount of REM sleep at 10 and 30mgkg-1 i.p. with no significant effect on the latency to, or amount of, non-REM sleep. SB-269970-A produced qualitatively similar effects in the same study. 6 In summary. SB-656104-A is a novel 5-HT7 receptor antagonist which has been utilised in the present study to provide further evidence for a role for 5-HT7 receptors in the modulation of REM sleep. [ABSTRACT FROM AUTHOR]

Published
2003
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34. Bicyclic heteroarylpiperazines as selective brain penetrant 5-HT6 receptor antagonists

Author

Ahmed, Mahmood, Briggs, Michael A., Bromidge, Steven M., Buck, Tania, Campbell, Lorraine, Deeks, Nigel J., Garner, Ashley, Gordon, Laurie, Hamprecht, Dieter W., Holland, Vicky, Johnson, Christopher N., Medhurst, Andrew D., Mitchell, Darren J., Moss, Stephen F., Powles, Jenifer, Seal, Jon T., Stean, Tania O., Stemp, Geoffrey, Thompson, Mervyn, and Trail, Brenda

Subjects
*CELL receptors, *BRAIN, *CENTRAL nervous system, *BINDING sites
Abstract

Abstract: Starting from the potent and selective but poorly brain penetrant 5-HT6 receptor antagonist SB-271046, a successful strategy for improving brain penetration was adopted involving conformational constraint with concomitant reduction in hydrogen bond count. This provided a series of bicyclic heteroarylpiperazines with high 5-HT6 receptor affinity. 5-Chloroindole 699929 combined high 5-HT6 receptor affinity with excellent brain penetration and also had good oral bioavailability in both rat and dog. [Copyright &y& Elsevier]

Published
2005
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35. Pharmacological profile of SB-357134: A potent, selective, brain penetrant, and orally active 5-HT6 receptor antagonist.

Author

Stean, Tania O., Hirst, Warren D., Thomas, David R., Price, Gary W., Rogers, Derek, Riley, Graham, Bromidge, Steven M., Serafinowska, Halina T., Smith, Douglas R., Bartlett, Sarah, Deeks, Nigel, Duxon, Mark, and Upton, Neil

Subjects
*SEROTONIN, *HELA cells, *CYCLIC adenylic acid
Abstract

N-(2,5-Dibromo-3-fluorophenyl)-4-methoxy-3-piperazin-1-ylbenzenesulfonamide (SB-357134) potently inhibited [125I]SB-258585 and [3H]LSD binding in a HeLa cell line expressing human 5-HT6 receptors (pKi=8.6 and 8.54, respectively). Furthermore, SB-357134 inhibited [125I]SB-258585 binding in human caudate–putamen and in rat and pig striatum membranes (pKi=8.82, 8.44, and 8.61, respectively). SB-357134 displayed over 200-fold selectivity for the 5-HT6 receptor versus 72 other receptors and enzymes. 5-HT-stimulated cyclic AMP (cAMP) accumulation in human 5-HT6 receptors was competitively antagonised by SB-357134 (pA2=7.63). SB-357134 inhibited ex vivo [125I]SB-258585 binding in the rat with an ED50 of 4.9±1.3 mg/kg po, 4 h postdose. In the rat maximal electroshock seizure threshold (MEST) test, SB-357134 produced a potent and dose-dependent increase in seizure threshold, with a minimum effective dose of 0.1 mg/kg po. At 10 mg/kg po, maximum activity occurred between 4 and 6 h postdose. Good exposure was observed with SB-357134 at 10 mg/kg po, reaching maximal blood and brain concentrations of 4.3±0.2 and 1.3±0.06 μM, respectively, 1 h postdose. In addition, SB-357134 (10 mg/kg po) enhanced memory and learning following chronic administration (twice a day for 7 days) in the rat water maze. Overall, these studies demonstrate that SB-357134 is a potent, selective, brain penetrant, and orally active 5-HT6 receptor antagonist. [Copyright &y& Elsevier]

Published
2002
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36. Tricyclic azepine derivatives as selective brain penetrant 5-HT6 receptor antagonists

Author

Trani, Giancarlo, Baddeley, Stuart M., Briggs, Michael A., Chuang, Tsu T., Deeks, Nigel J., Johnson, Christopher N., Khazragi, Abir A., Mead, Tania L., Medhurst, Andrew D., Milner, Peter H., Quinn, Leann P., Ray, Alison M., Rivers, Dean A., Stean, Tania O., Stemp, Geoffrey, Trail, Brenda K., and Witty, David R.

Subjects
*AZEPINES, *CHEMICAL inhibitors, *SULFONAMIDES, *BLOOD-brain barrier, *BRAIN function localization, *CLINICAL chemistry
Abstract

Abstract: Starting from a benzazepine sulfonamide 5-HT6 receptor antagonist lead with limited brain penetration, application of a strategy of conformational constraint and reduction of hydrogen bond donor count led to a novel series of tricyclic derivatives with high 5-HT6 receptor affinity and excellent brain:blood ratios. [Copyright &y& Elsevier]

Published
2008
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