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• W2022204064 abstract "Abstract The binding characteristics of [ 125 I]3β‐(4‐ethyl‐3‐iodophenyl)nortropane‐2β‐carboxylic acid methyl ester ([ 125 I]EINT), a high‐affinity selective ligand for the serotonin transporter (5‐HTT), and its binding characteristics to rat brain membranes were determined. [ 125 I]EINT binding to rat cerebral cortex membranes was saturable and reversible, and its specific binding represented approximately 90% of the total binding. [ 125 I]EINT labeled a single site with K d = 0.22 ± 0.03 nM and B max = 583 ± 38 fmol/mg protein. Kinetic analysis revealed a t 1/2 for association and dissociation of 20 and 24 min, respectively. Pharmacological characterization of [ 125 I]EINT confirmed its high specificity for the 5‐HTT. The pattern of brain region distribution in vivo of intravenously administered [ 125 I]EINT indicated greater accumulation of the radioligand in 5‐HTT‐rich brain regions. However, the signal‐to‐background ratio was low. Thus, [ 125 I]EINT appears to be a useful radioligand for studying the 5‐HTT in vitro, but it may not be a good in vivo ligand. Synapse 41:241–247, 2001. © 2001 Wiley‐Liss, Inc." @default.
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• W2022204064 date "2001-06-06" @default.
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• W2022204064 title "[125 I]3?-(4-ethyl-3-iodophenyl)nortropane-2?-carboxylic acid methyl ester ([125I]EINT): A potent and selective radioligand for the brain serotonin transporter" @default.
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• W2022204064 doi "https://doi.org/10.1002/syn.1081" @default.
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