Bay 59-3074, is a novel cannabinoid CB1/CB2 receptor partial agonist with antihyperalgesic and antiallodynic effects.
ChEBI: 4,4,4-trifluoro-1-butanesulfonic acid is an aromatic ether.
Novel CB 1 /CB 2 receptor partial agonist (K i values are 48.3 and 45.5 nM at human CB 1 and CB 2 receptors respectively). Orally active CB 1 agonist in vivo . Displays anti-hyperalgesic and antiallodynic properties in rat models of chronic neuropathic and inflammatory pain.
BAY 59-3074 (0.3-3 mg/kg; oral administration; daily; for 2 weeks; male Wistar rats) treatment improves antihyperalgesic and antiallodynic effects against thermal or mechanical stimuli in rat models of chronic neuropathic and inflammatory pain.
| Animal Model: | Male Wistar rats (160-250 g)[1] |
| Dosage: | 0.3 mg/kg, 1 mg/kg, and 3 mg/kg |
| Administration: | Oral administration; daily; for 2 weeks. |
| Result: | Antiallodynic efficacy in the spared nerve injury model was maintained after 2 weeks of daily administration. Tolerance developed rapidly (within 5 days) for cannabinoid-related side effects. Antihyperalgesic and antiallodynic efficacy was maintained/increased.
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CB1: 48.3 nM (Ki); CB2: 45.5 nM (Ki)
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