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3, 400 MHz): δ 7.76 (d, J = 7.8 Hz, 1H), 7.50-7.48 (m, 2H), 7.37-7.19 (m, 7H), 7.06 (d, J = 7.8 Hz, 1H), 6.94 (d, J = 7.8 Hz, 1H), 3.30-3.27 (m, 2H), 2.81 (t, J = 7.4 Hz, 2H), 2.68 (br s, 1H), 2.61-2.54 (m, 2H), 2.39-2.35 (m, 2H), 2.16 (s, 3H), 2.04 (br s, 1H), 1.87 (br s, 3H), 1.25 (br s, 2H), 0.88-084 (m, 2H); ESMS: m/z 485.4 (M+1)
-
3, 400 MHz): δ 7.76 (d, J = 7.8 Hz, 1H), 7.50-7.48 (m, 2H), 7.37-7.19 (m, 7H), 7.06 (d, J = 7.8 Hz, 1H), 6.94 (d, J = 7.8 Hz, 1H), 3.30-3.27 (m, 2H), 2.81 (t, J = 7.4 Hz, 2H), 2.68 (br s, 1H), 2.61-2.54 (m, 2H), 2.39-2.35 (m, 2H), 2.16 (s, 3H), 2.04 (br s, 1H), 1.87 (br s, 3H), 1.25 (br s, 2H), 0.88-084 (m, 2H); ESMS: m/z 485.4 (M+1).
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50 for the compound was calculated by graph pad prism software using the average CPM values
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77956172116
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note
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Functional response of compounds was assessed using the IP3-SPA-YSI method. Briefly, CHO-K1 cells stably expressing hMCHR1 were incubated overnight with 0.5 μCi/well of 3H-myo-inositol to generate a pool of 3H-PIP2. After aspiration of labeling medium, the cells were incubated with test compounds followed by stimulation with 80 nM of agonist (MCH peptide). The resulting pool of 3H-IPs was extracted with formic acid and the amount of 3H-IPs generated in the cells was detected using the non-derivatized yttrium silicate SPA beads.
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77956177640
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note
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C57BL/6J mice were fed a high fat diet (60% calories from fat, D12492 feed) for nearly 3 months until they reached an average body weight of approximately 45 g. Animals were grouped based on initial body weight. Compounds to be tested were then administered per orally twice daily for a period of 7 days. Body weight and food intake of the animals was recorded on a daily basis during the experimental duration.
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