Table 3.
Compound | R | R1 | R2 | I (%) a |
---|---|---|---|---|
17 | H | H | H | 0 |
18a | CH2CH3 | H | H | 0 |
18b | CH2CH2CH3 | H | H | 4.0 ± 2.3 |
18c | CH2CH2CH2CH3 | H | H | 10.3 ± 4.9 |
19a | CH2CH3 | CH2CH3 | H | 14.3 ± 7.4 |
19b | CH2CH2CH3 | CH2CH2CH3 | H | 21 ± 7.8 |
19c | CH2CH2CH3 | CH2CH2CH3 | CH2CH2CH3 | 28.0 ± 6.9 |
24 | CH2-Ph | CH2-Ph | H | 42.7 ± 2.4 (4) |
23 | CH2-Ph | H | H | 16.3 ± 6.4 |
29 | CH2CH2-Ph | H | CH2CH2-Ph | 25.3 ± 0.9 |
28 | CH2CH2-Ph | H | H | 22.7 ± 5.5 |
30 | CH2CH2-Ph | CH2-Ph | H | 30.0 ± 7.2 |
a The compounds are tested in triplicate (unless indicated otherwise in brackets) using the Voltage Clamp technique on Xenopus Laevis oocytes expressing Panx-1 channels (at a concentration of 50 µM).