Title : Occupancy of Norepinephrine Transporter by Duloxetine in Human Brains Measured by Positron Emission Tomography with (S,S)-[18F]FMeNER-D2.

Pub. Date : 2017 Dec 1

PMID : 29016875






6 Functional Relationships(s)
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1 Occupancy of Norepinephrine Transporter by Duloxetine in Human Brains Measured by Positron Emission Tomography with (S,S)-[18F]FMeNER-D2. Duloxetine Hydrochloride solute carrier family 6 member 2 Homo sapiens
2 However, the relationship between dose and plasma concentration of duloxetine and norepinephrine transporter occupancy in the human brain has not been determined. Duloxetine Hydrochloride solute carrier family 6 member 2 Homo sapiens
3 In this study, we examined norepinephrine transporter occupancy by different doses of duloxetine. Duloxetine Hydrochloride solute carrier family 6 member 2 Homo sapiens
4 Results: Norepinephrine transporter occupancy by duloxetine was 29.7% at 20 mg, 30.5% at 40 mg, and 40.0% at 60 mg. Duloxetine Hydrochloride solute carrier family 6 member 2 Homo sapiens
5 The estimated dose of duloxetine inducing 50% norepinephrine transporter occupancy was 76.8 mg, and the estimated plasma drug concentration inducing 50% norepinephrine transporter occupancy was 58.0 ng/mL. Duloxetine Hydrochloride solute carrier family 6 member 2 Homo sapiens
6 Conclusions: Norepinephrine transporter occupancy by clinical doses of duloxetine was approximately 30% to 40% in human brain as estimated using positron emission tomography with (S,S)-[18F]FMeNER-D2. Duloxetine Hydrochloride solute carrier family 6 member 2 Homo sapiens