BAY 59-3074 is a structurally novel cannabinoid CB1/CB2 receptor partial agonist with analgesic properties. Rats learned to discriminate BAY 59-3074 (0.5 mg/kg, p.o., t-1 h) from vehicle in a fixed-ratio: 10, food-reinforced two-lever procedure after a median number of 28 training sessions. BAY 59-3074 generalized dose-dependently (ED50: 0.081 mg/kg, p.o.) and the cue was detectable between 0.25 and 4 h after administration. Complete generalization was also obtained after i.p. administration of BAY 59-3074 (ED50 value: 0.41 mg/kg), and the reference cannabinoids BAY 38-7271 (0.011 mg/kg), CP 55,940 (0.013 mg/kg), HU-210 (0.022 mg/kg), WIN 55,212-2 (0.41 mg/kg) and (-)-Delta9-tetrahydrocannabinol (0.41 mg/kg). The discriminative stimulus effects of BAY 59-3074 are specifically mediated by cannabinoid CB1 receptor activation[3]. BAY 59-3074 (0.3-3 mg/kg, p.o.) induced antihyperalgesic and antiallodynic effects against thermal or mechanical stimuli in rat models of chronic neuropathic (chronic constriction injury, spared nerve injury, tibial nerve injury, and spinal nerve ligation models) and inflammatory pain (carrageenan and complete Freund's adjuvant models). 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[4].
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