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more..
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12444316598
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note
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3): δ 3.14-3.19 (2H, t, J = 7.4 Hz), 3.64-3.69 (2H, t, J = 7.4 Hz), 4.10-4.12 (2H, d, J = 6.2 Hz), 4.87 (1H, br s), 5.29 (2H, s), 6.88-6.93 (2H, t, J = 8.7 Hz), 7.13-7.38 (9H, m), 7.60-7.68 (2H, m), 8.21 (1H, s), 8.46-8.51 (2H, m)
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18
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12444291435
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note
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Intracellular Ca mobilization data were obtained using recombinant CHO cells transfected with human and rat LHRH receptor cDNA. The cells were preincubated with a variable concentration of test compounds for 20 min at 25°C. Fluorescence changes indicating mobilization of cytoplasmic calcium (Flu-3 AM, Molecular Probes) were measured on a FDSS-3000 machine (Hamamatsu photonics) after the stimulation with 10 nM LHRH for human receptor expressing cells and 1 nM LHRH for rat receptor expressing cells. The inhibitory effect of the compounds was calculated by comparing the Integral ratio (ratio = actual fluorescence/initial fluorescence)
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19
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12444255447
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note
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12 were incubated with 150 pM of [125I]-D-Trp6-LHRH (Pharmacia) in the presence of various concentration of compounds in assay buffer. The total binding was defined as that measured in the absence of a competing agent. Nonspecific binding was determined in the presence of 10 μM D-Trp6-LHRH
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20
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15444355594
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N. Cho, M. Harada, T. Imaeda, T. Imada, H. Matsumoto, Y. Hayase, S. Sasaki, S. Furuya, N. Suzuki, S. Okubo, K. Ogi, S. Endo, H. Onda, and M. Fujino J. Med. Chem. 41 1998 4190
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Cho, N.1
Harada, M.2
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Imada, T.4
Matsumoto, H.5
Hayase, Y.6
Sasaki, S.7
Furuya, S.8
Suzuki, N.9
Okubo, S.10
Ogi, K.11
Endo, S.12
Onda, H.13
Fujino, M.14
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