Table 2. Therapeutic windows of G protein-biased κOR agonists in antinociception versus various adverse effects.
Green indicates that the minimum dose producing an adverse effect is higher than the antinociceptive dose or the antinociceptive ED50. Red indicates that the adverse effect occurs at or below the antinociceptive dose/ED50. Yellow indicates that the doses tested were below the antinociceptive dose/ED50 and the results are therefore ambiguous. A “u” means this adverse effect is untested for this agonist. Design credit: [47].
Aversion | Sedation | Pro-anxiety/ depression | |
---|---|---|---|
Nalfurafine | |||
Sal A | |||
RB-64 | |||
EOM Sal B | |||
Mesyl Sal B | |||
16-Bromo Sal A | u | ||
Triazole 1.1 | u | ||
HS665 | u | u | |
HS666 | u | ||
BPHA | u | u# | u |
6’-GNTI | u | ||
LOR17 | u | ||
Compound 4a | u | u | |
Helianorphin19 | u | u | u |
This property was studied but there is no antinociceptive data for BPHA