Comparative in vivo study of iodine-123-labeled beta-CIT and nor-beta-CIT binding to serotonin transporters in rat brain

L. Reneman; J. Booij; J. Lavalaye; K. de Bruin; F. A. de Wolff; R. P. Koopmans; J. C. Stoof; G. J. den Heeten

doi:https://doi.org/10.1002/(SICI)1098-2396(199910)34:1<77::AID-SYN9>3.0.CO;2-Y

Comparative in vivo study of iodine-123-labeled beta-CIT and nor-beta-CIT binding to serotonin transporters in rat brain

L. Reneman, J. Booij, J. Lavalaye, K. de Bruin, F. A. de Wolff, R. P. Koopmans, J. C. Stoof, G. J. den Heeten

Other Departments

Research output: Contribution to journal › Article › Academic › peer-review

14 Citations (Scopus)

Abstract

Both iodine-123-labeled beta-CIT (2beta-carbomethoxy-3beta-(4-iodophenyl)tropane) and nor-beta-CIT (2beta-carbomethoxy-3beta-(4-iodophenyl)nortropane) have shown to be suitable radioligands for imaging serotonin (5-HT) transporters. [(123)I]nor-beta-CIT has the highest in vitro affinity for 5-HT transporters among beta-CIT analogs reported so far. However, no direct comparison-studies of these two radiotracers as to their in vivo binding to 5-HT transporters have been reported so far. Therefore, it is still unclear which of the two radiotracers is more suitable for single photon emission computed tomography (SPECT) imaging of 5-HT transporters. The purpose of this study was to compare directly in a controlled design the in vivo [(123)I]beta-CIT and [(123)I]nor-beta-CIT binding to 5-HT transporters under the same conditions in rats with the focus on brain kinetic characteristics by means of a two-compartment analysis. We observed that [(123)I]beta-CIT has a higher binding potential and faster kinetics for 5-HT transporters than [(123)I]nor-beta-CIT, suggesting that [(123)I]beta-CIT may be a more suitable radioligand than [(123)I]nor-beta-CIT for imaging 5-HT transporters with SPECT

Original language	English
Pages (from-to)	77-80
Journal	Synapse (New York, N.Y.)
Volume	34
Issue number	1
DOIs	https://doi.org/10.1002/(SICI)1098-2396(199910)34:1<77::AID-SYN9>3.0.CO;2-Y
Publication status	Published - 1999

Access to Document

https://doi.org/10.1002/(SICI)1098-2396(199910)34:1<77::AID-SYN9>3.0.CO;2-Y

Cite this

@article{ea54d2faccd7480e85220d6b4a2c338e,

title = "Comparative in vivo study of iodine-123-labeled beta-CIT and nor-beta-CIT binding to serotonin transporters in rat brain",

abstract = "Both iodine-123-labeled beta-CIT (2beta-carbomethoxy-3beta-(4-iodophenyl)tropane) and nor-beta-CIT (2beta-carbomethoxy-3beta-(4-iodophenyl)nortropane) have shown to be suitable radioligands for imaging serotonin (5-HT) transporters. [(123)I]nor-beta-CIT has the highest in vitro affinity for 5-HT transporters among beta-CIT analogs reported so far. However, no direct comparison-studies of these two radiotracers as to their in vivo binding to 5-HT transporters have been reported so far. Therefore, it is still unclear which of the two radiotracers is more suitable for single photon emission computed tomography (SPECT) imaging of 5-HT transporters. The purpose of this study was to compare directly in a controlled design the in vivo [(123)I]beta-CIT and [(123)I]nor-beta-CIT binding to 5-HT transporters under the same conditions in rats with the focus on brain kinetic characteristics by means of a two-compartment analysis. We observed that [(123)I]beta-CIT has a higher binding potential and faster kinetics for 5-HT transporters than [(123)I]nor-beta-CIT, suggesting that [(123)I]beta-CIT may be a more suitable radioligand than [(123)I]nor-beta-CIT for imaging 5-HT transporters with SPECT",

author = "L. Reneman and J. Booij and J. Lavalaye and {de Bruin}, K. and {de Wolff}, {F. A.} and Koopmans, {R. P.} and Stoof, {J. C.} and {den Heeten}, {G. J.}",

note = "Times Cited: 9 Article English Reneman, L Univ Amsterdam, Acad Med Ctr, Dept Nucl Med, Grad Sch Neurosci, F2N,Meibergdreef 9, NL-1105 AZ Amsterdam, Netherlands Cited References Count: 11 230TR WILEY-LISS DIV JOHN WILEY & SONS INC, 605 THIRD AVE, NEW YORK, NY 10158-0012 USA NEW YORK 27",

year = "1999",

doi = "https://doi.org/10.1002/(SICI)1098-2396(199910)34:1<77::AID-SYN9>3.0.CO;2-Y",

language = "English",

volume = "34",

pages = "77--80",

journal = "Synapse (New York, N.Y.)",

issn = "0887-4476",

publisher = "Wiley-Liss Inc.",

number = "1",

}

TY - JOUR

T1 - Comparative in vivo study of iodine-123-labeled beta-CIT and nor-beta-CIT binding to serotonin transporters in rat brain

AU - Reneman, L.

AU - Booij, J.

AU - Lavalaye, J.

AU - de Bruin, K.

AU - de Wolff, F. A.

AU - Koopmans, R. P.

AU - Stoof, J. C.

AU - den Heeten, G. J.

N1 - Times Cited: 9 Article English Reneman, L Univ Amsterdam, Acad Med Ctr, Dept Nucl Med, Grad Sch Neurosci, F2N,Meibergdreef 9, NL-1105 AZ Amsterdam, Netherlands Cited References Count: 11 230TR WILEY-LISS DIV JOHN WILEY & SONS INC, 605 THIRD AVE, NEW YORK, NY 10158-0012 USA NEW YORK 27

PY - 1999

Y1 - 1999

N2 - Both iodine-123-labeled beta-CIT (2beta-carbomethoxy-3beta-(4-iodophenyl)tropane) and nor-beta-CIT (2beta-carbomethoxy-3beta-(4-iodophenyl)nortropane) have shown to be suitable radioligands for imaging serotonin (5-HT) transporters. [(123)I]nor-beta-CIT has the highest in vitro affinity for 5-HT transporters among beta-CIT analogs reported so far. However, no direct comparison-studies of these two radiotracers as to their in vivo binding to 5-HT transporters have been reported so far. Therefore, it is still unclear which of the two radiotracers is more suitable for single photon emission computed tomography (SPECT) imaging of 5-HT transporters. The purpose of this study was to compare directly in a controlled design the in vivo [(123)I]beta-CIT and [(123)I]nor-beta-CIT binding to 5-HT transporters under the same conditions in rats with the focus on brain kinetic characteristics by means of a two-compartment analysis. We observed that [(123)I]beta-CIT has a higher binding potential and faster kinetics for 5-HT transporters than [(123)I]nor-beta-CIT, suggesting that [(123)I]beta-CIT may be a more suitable radioligand than [(123)I]nor-beta-CIT for imaging 5-HT transporters with SPECT

AB - Both iodine-123-labeled beta-CIT (2beta-carbomethoxy-3beta-(4-iodophenyl)tropane) and nor-beta-CIT (2beta-carbomethoxy-3beta-(4-iodophenyl)nortropane) have shown to be suitable radioligands for imaging serotonin (5-HT) transporters. [(123)I]nor-beta-CIT has the highest in vitro affinity for 5-HT transporters among beta-CIT analogs reported so far. However, no direct comparison-studies of these two radiotracers as to their in vivo binding to 5-HT transporters have been reported so far. Therefore, it is still unclear which of the two radiotracers is more suitable for single photon emission computed tomography (SPECT) imaging of 5-HT transporters. The purpose of this study was to compare directly in a controlled design the in vivo [(123)I]beta-CIT and [(123)I]nor-beta-CIT binding to 5-HT transporters under the same conditions in rats with the focus on brain kinetic characteristics by means of a two-compartment analysis. We observed that [(123)I]beta-CIT has a higher binding potential and faster kinetics for 5-HT transporters than [(123)I]nor-beta-CIT, suggesting that [(123)I]beta-CIT may be a more suitable radioligand than [(123)I]nor-beta-CIT for imaging 5-HT transporters with SPECT

U2 - https://doi.org/10.1002/(SICI)1098-2396(199910)34:1<77::AID-SYN9>3.0.CO;2-Y

DO - https://doi.org/10.1002/(SICI)1098-2396(199910)34:1<77::AID-SYN9>3.0.CO;2-Y

M3 - Article

C2 - 10459174

SN - 0887-4476

VL - 34

SP - 77

EP - 80

JO - Synapse (New York, N.Y.)

JF - Synapse (New York, N.Y.)

IS - 1

ER -