Table 3.
IC50 Values for Inhibition of Human and Rat α6/α3β4 nAChRs by PeIA- and Ala-Substituted Analoguesa
| human |
rat |
|||||
|---|---|---|---|---|---|---|
| peptide | IC50 (nM) | n | log change in IC50 |
IC50 (nM) | n | log change in IC50 |
| [Ala4] PeIA | 22.0 (17.8–27.4) | 4 | 0.5 | 175 (151–202) | 4 | 0.1 |
| [Ala5] PeIA | 7610 (5449–10 630) | −4 | 3.1 | >10 000 | 4 | >1.9 |
| [Ala6] PeIA | 1915 (1378–2662) | −4 | 2.5 | >10 000 | 4 | >1.9 |
| [Ala9] PeIA | 60.5 (55.1–66.4) | 4 | 1.0 | 399 (345–461) | 4 | 0.5 |
| [Ala10] PeIA | 22.1 (19.0–25.6) | 4 | 0.5 | 137 (111–168) | 4 | 0.1 |
| [Ala11] PeIA | 10.7 (8.84–12.8) | 4 | 0.2 | 56.6 (52.8–62.9) | 4 | −0.4 |
| [Ala12] PeIA | 16 060 (9586–26 920) | 4 | 3.4 | >10 000 | 4 | >1.9 |
| b [Ala13] PeIA | 73.3 (66.8–80.5) | 4 | 1.1 | 381 (317–456) | 4 | 0.5 |
| [Ala14] PeIA | 68.0 (61.8–74.9) | 4 | 1.0 | 230 (206–256) | 7 | 0.2 |
| [Ala15] PeIA | 89.4 (81.0–98.8) | 4 | 1.1 | 237 (211–265) | 4 | 0.3 |
a
Values within parentheses indicate the 95% confidence interval; log change in IC50 calculated relative to native PeIA.
b
Values from (16); n indicates the number of oocytes tested.