Synapse · 2014 · 17 citations · 9 references
MedicineNeurosciencePharmacologyExperimental PharmacologyNeuropharmacologyPsychopharmacologyAntidepressant PharmacologyBlood-brain Barrier PenetrationBlood-brain Barrier PharmacologyAdrenergic Receptor AgonistsAdrenergic Receptor SignalingBlood - Brain Barrier UptakeBlood-brain Barrier PermeabilityBlood-brain Barrier Uptake MechanismsNorepinephrine Transporter Inhibition
We report the use of β3 adrenergic receptor mediated activation of rat brain frontal cortex using mirabegron (a selective β3 adrenoceptor agonist), measured by (18)F-FDG PET/CT. Another β3 agonist, CL 316,243, did not have this effect due to impermeability through the blood brain barrier (BBB), while atomoxetine, a norepinephrine transporter blocker, did increase (18)F-FDG uptake in the frontal cortex. Mirabegron exhibited a dose-dependent increase in frontal cortex (18)F-FDG uptake. These findings suggest a possible use of selective β3 adrenoceptor agonists in reversing regional glucose hypometabolism in the brain.
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