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6.13.16. (+)-N-{1-(1-Adamantyl)methyl-2,4-dioxo-5-[2-(N-
morpholino)ethyl]-2,3,4,5-tetrahydro-1H-1,5-benzodiazepin-3-
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It was synthesized as described for 67. Y = 90%, HPLC: retention
time 6.9 min. For the analytical characterization, see the descrip-
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6.14. Optical resolution via tosyl mandelate
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morpholino)ethyl]-2,3,4,5-tetrahydro-1H-1,5-benzodiazepin-3-yl}-
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outlined in Scheme 5 and according to the experimental procedure
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6.15. Biological section
For the in vitro assays, inhibition constants (Ki) were deter-
mined for all compounds in Guinea Pig brain (CCK2) and rat pan-
creas (CCK1) membranes using [3H]-CCK8s at a concentration of
0.2 nM as the radiolabelled standard; the membranes were incu-
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hour before the experiments, are placed in the centre of the white
compartment; then the time spent exploring both the white and
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side the better is the anxiolytic effect of the compound. The anxio-
lytic effect was measured at 2, 4, 6 and 8 h.
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Acknowledgments
Acknowledgments for the Analytical and Spectroscopic support
to Michele Dal Cin, Stefano Provera and Ornella Curcuruto
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