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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 2.

6-Alkoxy Tetrahydroisoquinoline Orexin Antagonists.

graphic file with name nihms709265u3.jpg
No. R OX1 Ke (nM)a OX2 Ke (nM)a or % inhibition at 10 μM
17a n-Propyl >10000 b
17b 2,2,2-Trifluoroethyl >10000 b
17c iso-Propyl >10000 b
17d Benzyl >10000 b
17e graphic file with name nihms709265t1.jpg 1000 ± 190c b
17f graphic file with name nihms709265t2.jpg >10000 b
18a Methylsulfonyl >10000 1330 ± 260
18b Benzenesulfonyl >10000 b
19 Propionoyl >10000 1290 ± 130
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.

c

Pre-incubation of antagonist and test compound was 1 hr.