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. Author manuscript; available in PMC: 2016 Sep 1.
Published in final edited form as: Bioorg Med Chem. 2015 Jul 16;23(17):5709–5724. doi: 10.1016/j.bmc.2015.07.013

Table 1.

7-Alkoxy tetrahydroisoquinoline orexin antagonists.

graphic file with name nihms709265u2.jpg
No R OX1 Ke (nM)a OX2 Ke (nM)a or % inhibition at 10 μM
10a Methyl 512 ± 36 1680 ± 330
10b Ethyl 37.3 ± 7.8 b
10c n-Propyl 23.7 ± 7.9 2550 ± 260
10d iso-Propyl 49.7 ± 11 b
10e n-Butyl 230 ± 70 b
a

Ke values are the mean ± SEM of three independent experiments performed in duplicate. Results where Ke > 10 μM are N=2.

b

Less than 50% inhibition at 10 μM.