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A positron emission tomography imaging study found that single oral 50 mg and 100 mg doses of tramadol to human volunteers resulted in 34.7% and 50.2% respective mean occupation of the serotonin transporter (SERT) in the thalamus.[76] The estimated median effective dose (ED50) for SERT occupancy hence was 98.1 mg, which was associated with a plasma tramadol level of about 330 ng/mL (1,300 nM).[76] It was also estimated that the maximum daily dosage of tramadol of 400 mg (100 mg q.i.d.) would result in as much as 78.7% occupancy of the SERT (in association with a plasma concentration of 1,220 ng/mL or 4,632 nM).[76] This is close to that of selective serotonin reuptake inhibitors (SSRIs), which occupy the SERT by 80% or more.[76]
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