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. Author manuscript; available in PMC: 2012 May 1.
Published in final edited form as: Bioorg Med Chem Lett. 2010 Dec 3;21(9):2711–2714. doi: 10.1016/j.bmcl.2010.11.119

Table 3.

Structures and activities of analogs 21 and 22.

graphic file with name nihms260881u3.jpg
Cmpd R Pharmacology IC50 (μM)a EC50 (μMa) Glu Max (%)a
21a graphic file with name nihms260881t14.jpg Part. Antag. 0.28 NA 16
22a Ago-PAM NA 0.08 70
21b/20c graphic file with name nihms260881t15.jpg NAM 0.37 NA 5.8
22b/20e PAM NA 0.65 38
21c graphic file with name nihms260881t16.jpg Part. Antag. 0.6 NA 24
22c Ago-PAM NA 0.31 80
21d graphic file with name nihms260881t17.jpg NAM 2.5 NA 9.2
22d PAM NA 3.5 58
21e graphic file with name nihms260881t18.jpg NAM 0.73 NA 0.9
22e NAM 10 NA 34
21f graphic file with name nihms260881t19.jpg NAM 10 NA 46
22f PAM NA 1.4 93
21g graphic file with name nihms260881t20.jpg NAM 4.7 NA 16
22g PAM NA 0.46 59
21h graphic file with name nihms260881t21.jpg NAM 10 NA 47
22h PAM NA 2.3 91
21i graphic file with name nihms260881t22.jpg Inactive - - -
22i PAM NA 2.9 95
a

Average of at least three independent determinations. NA, not applicable.