Serotonin and norepinephrine transporter occupancy of tramadol in non-human primate using positron emission tomography.
Authors of this article are:
Arakawa R, Takano A, Halldin C.
A summary of the article is shown below:
Background: Tramadol, a centrally acting analgesic drug, has relatively high affinity to serotonin transporter (5-HTT) and norepinephrine transporter (NET) in addition to μ-opioid receptor. Based on this characteristic, tramadol is expected to have antidepressant effect.Methods: Positron emission tomography measurements with [ 11C]MADAM and [ 18F]FMeNER-D2 were performed at the baseline and after intravenous administration of three different doses (1, 2, and 4mg/kg) of tramadol using six cynomolgus monkeys. The relationship between dose and occupancy for 5-HTT and NET was estimated.Results: Tramadol occupied similarly both 5-HTT (40 – 72%) and NET (7 – 73%) in a dose dependent manner. The Kd was 2.2mg/kg and 2.0 mg/kg for 5-HTT and NET, respectively.Conclusions: Both 5-HTT and NET of in vivo brain were blocked at over 70% at a clinically relevant high dose of tramadol. This study suggests tramadol has the potential antidepressant effects through the inhibitions of 5-HTT and NET in the brain.
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