Biological Activity
CR4056 is an imidazoline-I2 ligand for pain signaling and monoaminergic research. CR4056 antinociceptive ED50 was 5.8 mg/kg.
In Vitro
| Endpoint | Model / conditions / source | Reported result |
|---|---|---|
| Target context | I2-imidazoline ligand and human MAO-A assays. [1] | The compound combined I2-site pharmacology with MAO-A inhibition. The animal ED50 values are not receptor-binding affinities. |
In Vivo
| Endpoint | Model / conditions / source | Reported result |
|---|---|---|
| Inflammatory analgesia | Rat complete-Freund-adjuvant pain model; oral administration. [1] | CR4056 antinociceptive ED50 was 5.8 mg/kg. |
| Capsaicin hyperalgesia | Rat model; oral dose-response. [1] | Reported ED50 was 4.1 mg/kg and ED100 was 17.9 mg/kg; idazoxan antagonized the effect. |
| Noradrenaline response | 20 mg/kg orally each day for 4 days. [1] | Noradrenaline increased by 63.1 ± 4.2% in cortex and 51.3 ± 6.7% in lumbar spinal cord. |
Interpretation
ED50 values are animal-dose endpoints, not biochemical IC50 values or human dosing guidance.
