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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 1.

Functional Activity of TBPB Amide Analogues 5.

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Cmpd R1 R2 M1 EC50 (μM)a %CCh Maxa
5a 2-CH3 H 0.88 60
5b 2-CH3 CI 2.71 56
5c 3-CH3 H 0.51 53
5d 3-CH3 CI 2.11 50
5e 2-CF3 H 0.91 32
5f 2-CF3 CI 11.1 24
5g 3-CI H 0.93 21
5h 3-CI CI 7.11 21
a

EC50S and % CCh maximum (measures activation of M1 relative to 100% response of CCh) are the mean of at least three independent detrminations. All analogues in this Table are selective for M1 (no activation of M2–M5 at conc. up to 30 μM).