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56249123698
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2) was added. 10 μl from the compound plates was then added immediately to cell plates using a FLIPR 3 calcium imaging instrument and changes in fluorescence were measured over a 1 min timeframe. Maximum change in fluorescence over baseline was used to determine agonist response and concentration-response curves were constructed, using a 4-parameter logistic equation. The intrinsic activity of target compounds was calculated by using the maximum asymptote of its concentration-response curve relative to the maximum asymptote of the motilin concentration-response curve.
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17
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23744515594
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18
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0344010043
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It is unlikely that the activity observed for Compound 22 in the rabbit gastric antrum assay is partly or wholly due to action on the ghrelin receptor: other analogues in the series with no activity at the ghrelin receptor showed comparable or greater activity in the antrum assay (unpublished data); and ghrelin itself does not show enhancement of EFS mediated contractions in rabbit gastric antrum, see
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It is unlikely that the activity observed for Compound 22 in the rabbit gastric antrum assay is partly or wholly due to action on the ghrelin receptor: other analogues in the series with no activity at the ghrelin receptor showed comparable or greater activity in the antrum assay (unpublished data); and ghrelin itself does not show enhancement of EFS mediated contractions in rabbit gastric antrum, see. Dass N.B., Hill J., Muir A., Testa T., Wise A., and Sanger G.J. Brit. J. Pharmacol. 140 (2003) 948
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56249099097
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+).
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22
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56249132980
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note
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Westaway, S. M.; Brown, S. L.; Conway, E.; Heightman, T. D.; Johnson, C. N.; Lapsley, K.; Macdonald, G. J.; MacPherson, D. T.; Mitchell, D. J.; Myatt, J. W.; Seal, J. T.; Stanway, S. J.; Stemp, G.; Thompson, M.; Colombo, A.; Consonni, A.; Gagliardi, S.; Roccaboni, M.; Ronzoni, S.; Briggs, M. A.; Matthews, K. L.; Stevens, A. J.; Bolton, V. J.; Jarvie, E. M.; Stratton, S. C.; Sanger, G. J. Bioorg. Med. Chem. Lett. 2008, doi:10.1016/j.bmcl.2008.10.072.
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