Table 5.
IC50 Values for α3β2-Selective Peptidesa
|
α3β2 nAChR |
α6/α3β2β3 nAChR |
|||||
|---|---|---|---|---|---|---|
| peptide | residue differences with PeIA | IC50 (nM) | n | IC50 (nM) | n | IC50 ratio |
| PeIA-4769 | His9,Leu10 | 0.29 (0.25–0.34) | 4 | 1.04 (0.921–1.18) | 4 | 3 |
| PeIA-5115 | His9,Leu10,Asp11 | 1.67 (1.44–1.95) | 4 | 19.9 (17.8–22.3) | 4 | 12 |
| PeIA-5080 | His9,Leu10,Glu11 | 1.22 (1.06–1.40) | 4 | 16.2 (13.3–19.8) | 4 | 14 |
| PeIA-5415 | His9,Leu10,Aad11 | 3.01 (2.40–3.78) | 5 | 155 (122–197) | 5 | 52 |
| PeIA-5355 | His9,Leu10,Api11 | 0.38 (0.36–0.44) | 4 | 22.3 (19.9–24.9) | 4 | 59 |
| PeIA-5587 | His9,Leu10,Asu11 | 1.28 (1.06–1.54) | 4 | 50.3 (40.4–62.7) | 4 | 39 |
| PeIA-5106 | His9,Leu10,Ile15 | 0.28 (0.23–0.33) | 5 | 0.86 (0.77–0.96) | 4 | 3 |
| PeIA-5413 | His9,Leu10,Api11,Ile15 | 0.57 (0.44–0.74) | 4 | 58.2 (51.4–65.8) | 5 | 102 |
| PeIA-5416 | His9,Nle10,Api11 | 1.33 (1.17–1.53) | 5 | 286 (220–373) | 4 | 220 |
| PeIA-5466 | His9,Nle10,Api11,Ile15 | 1.34 (1.13–1.60) | 4 | 377 (275–508) | 4 | 290 |
a
Values in parentheses indicate the 95% CI of the IC50 values. IC50 ratio calculated as (α6/α3β2β3)/(α3β2).