tcsc5806 Bay 59-3074

Bay 59-3074 is a novel, selective CB1/CB2 receptor partial agonist with Ki values of 48.3 and 45.5 nM at human CB1 and CB2 receptors respectively . Orally active CB1 agonist in vivo.

target: CB1/CB2 receptor partial agonist.

Ki: 48.3 and 45.5 nM (CB1 and CB2 receptors)

In vitro: analgesic, antihyperalgesic, and antiallodynic properties in rat models of acute and chronic pain. The reference concentration is 10 μM. [1]

In vivo: administration of BAY 59-3074 (ED50 value: 0.41 mg/kg).Orally active CB1 agonist in vivo. [2] BAY 59-3074 (0.3-3 mg/kg, p.o.) induce antihyperalgesic and antiallodynic effects against thermal or mechanical stimuli in rat models of chronic neuropathic. Antiallodynic efficacy of BAY 59-3074 (1 mg/kg, p.o.) in the spared nerve injury model was maintained after 2 weeks of daily administration. However, tolerance developed rapidly (within 5 days) for cannabinoid-related side effect. [1] BAY 59-3074 have analgesic, antihyperalgesic, and antiallodynic properties in rat models of acute and chronic pain.[1]