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. Author manuscript; available in PMC: 2011 Sep 21.
Published in final edited form as: Bioorg Med Chem Lett. 2008 Sep 11;18(20):5443–5447. doi: 10.1016/j.bmcl.2008.09.032

Table 3.

Functional Activity of TBPB Amide Analogues 15.

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Cmpd X M1 EC50 (μM)a %CCh Maxa D2 IC50 (μM)a
15a 4-F >10 46 1.1
15b 6-F 9.6 72 1.9
15c 5-CI 3.6 90 >10
a

EC50s, % CCh maximum (measures M1 activation relative to 100% CCh response) and IC50s are the mean of at least three independent determinations. All analogues in this Table are selective for M1 (>30 μM vs. M2–M5).