BAY 38-7271

BAY 38-7271 is selective and highly potent and cannabinoid CB₁/CB₂ receptor agonist, with K_is of 1.85 nM and 5.96 nM for recombinant human CB₁ receptor and CB₂ receptor, respectively. BAY 38-7271 has strong neuroprotective properties^[1]. In Vitro: BAY 38-7271 shows only minor interactions at the micromolar range with other binding sites such as adenosine A₃ receptor (IC₅₀ = 7.5 μM), peripheral GABA_A benzodiazepine receptor (IC₅₀ = 971 nM), melatonin ML₁ receptor (IC₅₀ = 3.3 μM), and at the monoamine transporter (IC₅₀ = 1.7 μM)^[1].
In Vivo: BAY 38-7271 (Ed₅₀ = 0.02 mg/kg; i.v. and 0.5 mg/kg; i.p.) induces a potent and dose-de-pendent reduction in core body temperature^[1].
BAY 38-7271 has low physical dependence liability and is not essentially different from that of other cannabinoid CB₁ receptor agonists^[1].
BAY 38-7271 (1-1000 ng/kg/h; i.v. infusion; for 4 hours) shows neuroprotective efficacy in the rat SDH model^[1].
BAY 38-7271 also has neuroprotective efficacy in models of transient and permanent occlusion of the middle cerebral artery and brain edema models^[1].