TABLE 4.
In vivo pharmacological characterization of some G protein-biased KOR agonists in rodents.
| Compound (Reference) |
Analgesia | Antipruritic effect | CPA | ICSS | Hypolo-comotion | rotarod performance | Additional effect |
| RB-64 (dose) (White et al., 2015) mice |
Yes (55°C hot plate) (3 & 10 mg/kg) | Yes (1 & 3 mg/kg) | No effect (1 mg/kg) | No effect (3 mg/kg) | No effect (3 & 10 mg/kg) | ||
| Triazole 1.1 (dose) (Brust et al., 2016), mice except ICSS |
Yes (49°C warm water tail immersion) (15, 30 mg/kg) |
Yes (against chloroquine) (1, 3 mg/kg) |
No effect in rats (4, 8, 16, 24 mg/kg) | No (3, 15 & 30 mg/kg) | No effect on dopamine release in the N accumbens | ||
| Isoquinolinone 2.1 (dose) (Morgenweck et al., 2015), mice | Yes (against norBNI or chloroquine) (1, 3 mg/kg) | No effect (3 mg/kg) |
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| HS 665 (dose) (Spetea et al., 2017) |
Yes, 55°C warm-water tail withdrawal, ED50 3.74 nmole, icv | Yes 30 nmole, icv |
No effect 10 nmole, icv | ||||
| HS 666 icv (dose) (Spetea et al., 2017) |
Yes, 55°C warm-water tail withdrawal, ED50 6.02 nmole, icv | No 150 nmole, icv |
No effect, 30 nmole, icv | ||||
| 16-Bromo SalA (Paton et al., 2020), mice | Yes, 50°C warm-water tail withdrawal, ED50, 2.06 mg/kg; not effective in 2% formaldehyde Induced inflammatory pain at 1, 2 mg/kg | No, 0.3 mg/kg; no conditioned taste aversion, 0.3 mg/kg |
Impaired performance at 2 mg/kg, but not at 1 mg/kg | No axiogenic effect in the elevated plus maze test (1, 2 mg/kg) | |||
| LOR17 (dose) (Bedini et al., 2020) |
Yes, 52°C warm water tail immersion, ED50 10.07 mg/kg, sc; acetic acid abdominal writhing, ED50 5.74 mg/kg. sc) | No (10 mg/kg, sc) | No (10 mg/kg, sc) | Attenuated oxaliplatin-induced cold hypersensitivity (10 and 20 mg/kg, sc); No effect in the forced swim test (10 mg/kg, s.c.) |