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Inhibition of serotonin transport by (+)McN5652 is noncompetitive.

Abstract：

INTRODUCTION:Imaging of the serotonergic innervation of the brain using positron emission tomography (PET) with the serotonin transporter (SERT) ligand [11C] (+)McN5652 might be affected by serotonin in the synaptic cleft if there is relevant interaction between [11C] (+)McN5652 and serotonin at the SERT. The aim of the present study therefore was to pharmacologically characterize the interaction of [11C] (+)McN5652 and serotonin at the SERT. METHODS:In vitro saturation analyses of [3H]serotonin uptake into HEK293 cells stably expressing the human SERT were performed in the absence and presence of unlabelled (+)McN5652. Data were evaluated assuming Michaelis-Menten kinetics. RESULTS:Unlabelled (+)McN5652 significantly reduced the maximal rate of serotonin transport V(max) of SERT without affecting the Michaelis-Menten constant K(M). CONCLUSIONS:This finding indicates that (+)McN5652 inhibits serotonin transport through the SERT in a noncompetitive manner. This might suggest that [11C] (+)McN5652 PET is not significantly affected by endogenous serotonin.

journal_name

Nucl Med Biol

journal_title

Nuclear medicine and biology

authors

Hummerich R,Schulze O,Rädler T,Mikecz P,Reimold M,Brenner W,Clausen M,Schloss P,Buchert R

doi

10.1016/j.nucmedbio.2005.12.009

subject

Has Abstract

pub_date

2006-04-01 00:00:00

pages

317-23

issue

3

eissn

0969-8051

issn

1872-9614

pii

S0969-8051(05)00305-7

journal_volume

33

pub_type

杂志文章

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