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. Author manuscript; available in PMC: 2012 May 15.
Published in final edited form as: Bioorg Med Chem Lett. 2011 Mar 21;21(10):2980–2985. doi: 10.1016/j.bmcl.2011.03.048

Table 2.

Activity of 4-dimethylaminophenyl quinoline ureas against OX1R and OX2R.

graphic file with name nihms283908t2.jpg
No. R1 R2 X Y Ke (nM)
OX1a OX2b
24 8-F H O NH 2.4±1.7 171±25
25 8-F Me O NH 65±33 >10,000
26 8-F H S NH 1115.1 >10,000
27 6-CF3 H O NH >10,000 >10,000
28 8-CF3 H O NH 131±33 >10,000
29 8-F H O CH2 >10,000 >10,000
a

values are the mean of at least three independent experiments in duplicate.

b

values are the mean of at least two independent experiments in duplicate