Table 3.
| |||||
---|---|---|---|---|---|
Cmpd | R | Pharmacology | IC50 (μM)a | EC50 (μMa) | Glu Max (%)a |
21a | Part. Antag. | 0.28 | NA | 16 | |
22a | Ago-PAM | NA | 0.08 | 70 | |
21b/20c | NAM | 0.37 | NA | 5.8 | |
22b/20e | PAM | NA | 0.65 | 38 | |
21c | Part. Antag. | 0.6 | NA | 24 | |
22c | Ago-PAM | NA | 0.31 | 80 | |
21d | NAM | 2.5 | NA | 9.2 | |
22d | PAM | NA | 3.5 | 58 | |
21e | NAM | 0.73 | NA | 0.9 | |
22e | NAM | 10 | NA | 34 | |
21f | NAM | 10 | NA | 46 | |
22f | PAM | NA | 1.4 | 93 | |
21g | NAM | 4.7 | NA | 16 | |
22g | PAM | NA | 0.46 | 59 | |
21h | NAM | 10 | NA | 47 | |
22h | PAM | NA | 2.3 | 91 | |
21i | Inactive | - | - | - | |
22i | PAM | NA | 2.9 | 95 |
Average of at least three independent determinations. NA, not applicable.