The Adjuvant arthritis (AA) model and Collagen-induced arthritis (CIA) model have similar pathogenesis and pathological characteristics to human rheumatoid arthritis (RA).
IDO2-IN-1 (compound 22) (100 mg/kg; p.o.; once dose) exhibits excellent anti-inflammatory activity, higher than naproxen, a prescription drug reducing pain, swelling, and joint stiffness from arthritis[1].
IDO2-IN-1 (25, 50, 100 mg/kg; i.p.; once daily, for 19 d) exhibits excellent inhibitory effect on mice paw swelling, shows efficacy in a collagen-induced arthritis model in mice[1].
IDO2-IN-1 (30, 60, 120 mg/kg; i.p.; once daily, for 15 d) inhibits joint inflammation and displays potential effect in autoimmune arthritis improvement[1].
Pharmacokinetic Profile in Rat[1]
| Route | Dose (mg/kg) | T1/2/sub> (h) | Tmax (h) | Cmax (ng/mL) | AUC(0-∞) (h?ng/mL) | CL (mL/h/kg) | Vz (mL/kg) | MRT(0-∞) (h) | F (%) |
| i.v. | 1 | 0.69 | / | / | 375.1 | 2673 | 2675 | 0.55 | / |
| p.o. | 10 | 2.02 | 0.75 | 153.8 | 670.5 | / | / | 7.48 | 17.87 |
| Animal Model: | Xylene-induced ear swelling mouse model (ICR mice, male, 6 weeks old)[1] |
| Dosage: | 100 mg/kg |
| Administration: | Oral gavage; once dose; evenly coated right ear with 25 μL of xylene after 1 h treatment |
| Result: | Significantly relieved mouse ear swelling with a high swelling inhibition rate of 65.32%.
|
| Animal Model: | Collagen-induced arthritis (CIA) mice model (DBA/1J mice, male, 6 weeks old)[1] |
| Dosage: | 25, 50, 100 mg/kg |
| Administration: | Intraperitoneal injection; once daily; 19 days, began on day 56 after collagen induced |
| Result: | Decreased the expression of inflammatory cytokines IL-18 and IL-33.
Reduced inflammation and cartilage and bone erosions symptoms.
|
| Animal Model: | Adjuvant arthritis (AA) rat model (Sprague-Dawley rats, male, 180 ± 20 g)[1] |
| Dosage: | 30, 60, 120 mg/kg |
| Administration: | Intraperitoneal injection; once daily; 15 days, began on day 21 after chondrex induced |
| Result: | Significantly reduced IL-6 and TNF-α levels.
Decreased synovial hyperplasia accompanied by inflammatory cell infiltration, pannus formation, and bone erosion of cartilage in a dose-dependent manner.
|
