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13
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68949159640
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submitted for publication
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Teegarden, B. R.; Li, H.; Jayakumar, H.; Strah-Pleynet, S.; Dosa, P. I.; Selaya, S. D.; Kato, N.; Elwell, K. H.; Davidson, J.; Cheng, K.; Saldana, H.; Frazer, J. M.; Whelan, K.; Foster, J.; Espitia, S.; Webb, R. R; Beeley, N.R.A.; Kilduff, T.S.; Morairty, S.; Thomsen, W.; Al-Shamma, H., submitted for publication.
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Teegarden, B.R.1
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more..
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14
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33646584548
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2A antagonist see:
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2A antagonist see:. Ladduwahetty T., Boase A.L., Mitchinson A., Quin C., Patel S., Chapman K., and MacLeod A.M. Bioorg. Med. Chem. Lett. (2006) 3201
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Hughes, D.L.1
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16
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68949099282
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For experimental details, see: Teegarden, B.; Jayakumar, H.; Li, H.; Strah-Pleynet, S.; Dosa, P. I. Preparation of diaryl and arylheteroaryl urea derivatives, in particular pyrazolylphenyl ureas, as 5-HT2A serotonin receptor modulators. WO2005012254, 2005.
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For experimental details, see: Teegarden, B.; Jayakumar, H.; Li, H.; Strah-Pleynet, S.; Dosa, P. I. Preparation of diaryl and arylheteroaryl urea derivatives, in particular pyrazolylphenyl ureas, as 5-HT2A serotonin receptor modulators. WO2005012254, 2005.
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17
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68949097324
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Teegarden, B.; Xiong, Y.; Strah-Pleynet, S.; Jayakumar, H.; Dosa, P. I.; Feichtinger, K.; Casper, M.; Lehmann, J.; Jones, R. M.; Unett, D. J. Preparation of 3-phenylpyrazole derivatives as modulators of 5-HT2A serotonin receptors for the treatment of related disorders. WO2006055734, 2006.
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Teegarden, B.; Xiong, Y.; Strah-Pleynet, S.; Jayakumar, H.; Dosa, P. I.; Feichtinger, K.; Casper, M.; Lehmann, J.; Jones, R. M.; Unett, D. J. Preparation of 3-phenylpyrazole derivatives as modulators of 5-HT2A serotonin receptors for the treatment of related disorders. WO2006055734, 2006.
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18
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68949158247
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note
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The solubilities of compound 13 (0.25 mg/ml in sodium phosphate buffer and 2.8 mg/ml in 0.01 N HCl) and compound 19 (0.15 mg/ml and 3.3 mg/ml) were similar to that of compound 3.
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19
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43549117468
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Adams J.W., Ramirez J., Ortuno D., Shi Y., Thomsen W., Richman J.G., Morgan M., Dosa P., Teegarden B.R., Al-Shamma H., Behan D.P., and Connolly D.T. Eur. J. Pharmacol. 586 (2008) 234
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Adams, J.W.1
Ramirez, J.2
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Morgan, M.7
Dosa, P.8
Teegarden, B.R.9
Al-Shamma, H.10
Behan, D.P.11
Connolly, D.T.12
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20
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68949163580
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note
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Inhibition of the hERG channel varied based on the substituents in the compounds, but in general molecules containing the less basic morpholino group, like 54 and 56 (29% at 3 μM), showed less inhibition than those with more basic groups like 32 (90% at 3 μM) and 50 (64% at 1 μM).
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