Table 10.
Binding and intracerebroventricular antinociception as a function of helix stability: glucopeptides.
Compound | Message sequence | Link | Helical address sequence | Ki (nM) |
A50 |
||
---|---|---|---|---|---|---|---|
δ receptor | μ receptor | κ receptor | Intracerebroventricular (nmol) | ||||
41* | YtFGL | P | NLBEKBLKS*L-NH2 | 11 | 9.1 | 6.9 | 1.13 |
42*/33 | YtFGL | P | NLBEKALKS*L-NH2 | 3.6 | 2.3 | 2.6 | 0.58 |
43* | YtFGL | P | NLAEKBLKS*L-NH2 | 14 | 6.1 | 12 | 1.46 |
44* | YtFGL | P | NLAEKALKS*L-NH2 | 7.9 | 6.2 | 8.9 | 1.44 |
45* | YtFGL | P | NLAEKGLKS*L-NH2 | 6.3 | 2.2 | 6.3 | 1.47 |
46* | YtFGL | P | NLGEKALKS*L-NH2 | 5.7 | 2.9 | 11 | 2.54 |
47* | YtFGL | P | NLGEKGLKS*L-NH2 | 7.1 | 3.5 | 4.4 | 2.12 |
S = OH; S* = Glc; S** = Lact.
P: Proline; S: Serine.