[(123/125)I]RTI-55, an in vivo label for the serotonin transporter

U. Scheffel, Robert F Dannals, E. J. Cline, George Ricaurte, F. I. Carroll, P. Abraham, A. H. Lewin, M. J. Kuhar

Research output: Contribution to journalArticle

Abstract

[123I]RTI-55, an iodinated derivative of the cocaine analog 3β- phenyltropane-2β-carboxylic acid methyl ester, was evaluated as an agent for in vivo labeling of the serotonin transporter. Labeling of the precursor of RTI-55 with I-123 was efficient and yielded a high specific activity product. After intravenous injection of [123I]RTI-55 into rats, the tracer accumulated in regions with high densities of serotonin and dopamine uptake sites. The distribution of [123I]RTI-55 binding in areas rich in serotonin uptake sites correlated with [3H]serotonin uptake measured in vitro in the same regions. Specific [123I]RTI-55 binding to serotonin uptake sites was inhibited by paroxetine but not by GBR 12,909. Treatment of rats with neurotoxic doses of fenfluramine caused decreases of 66% (in the hypothalamus) to 83% (in the superior colliculi) of specific [125I]RTI-55 binding in all areas except in the striatum and the olfactory tubercles (regions rich in dopamine transporters). These results indicate that [(123/125)I]RTI-55 binds, although not selectively, to the serotonin transporter in vivo. Furthermore, they suggest that [123I]RTI-55 holds promise as a SPECT imaging agent for the study of the serotonin transporter in humans in health and disease.

Original languageEnglish (US)
Pages (from-to)134-139
Number of pages6
JournalSynapse
Volume11
Issue number2
DOIs
StatePublished - 1992

Fingerprint

Serotonin Plasma Membrane Transport Proteins
Serotonin
Fenfluramine
Paroxetine
Dopamine Plasma Membrane Transport Proteins
RTI 55
Superior Colliculi
Carboxylic Acids
Single-Photon Emission-Computed Tomography
Cocaine
Intravenous Injections
Hypothalamus
Dopamine
Esters
Health

ASJC Scopus subject areas

  • Neuroscience(all)
  • Physiology
  • Pharmacology

Cite this

Scheffel, U., Dannals, R. F., Cline, E. J., Ricaurte, G., Carroll, F. I., Abraham, P., ... Kuhar, M. J. (1992). [(123/125)I]RTI-55, an in vivo label for the serotonin transporter. Synapse, 11(2), 134-139. https://doi.org/10.1002/syn.890110206

[(123/125)I]RTI-55, an in vivo label for the serotonin transporter. / Scheffel, U.; Dannals, Robert F; Cline, E. J.; Ricaurte, George; Carroll, F. I.; Abraham, P.; Lewin, A. H.; Kuhar, M. J.

In: Synapse, Vol. 11, No. 2, 1992, p. 134-139.

Research output: Contribution to journalArticle

Scheffel, U, Dannals, RF, Cline, EJ, Ricaurte, G, Carroll, FI, Abraham, P, Lewin, AH & Kuhar, MJ 1992, '[(123/125)I]RTI-55, an in vivo label for the serotonin transporter', Synapse, vol. 11, no. 2, pp. 134-139. https://doi.org/10.1002/syn.890110206
Scheffel, U. ; Dannals, Robert F ; Cline, E. J. ; Ricaurte, George ; Carroll, F. I. ; Abraham, P. ; Lewin, A. H. ; Kuhar, M. J. / [(123/125)I]RTI-55, an in vivo label for the serotonin transporter. In: Synapse. 1992 ; Vol. 11, No. 2. pp. 134-139.
@article{6b44f011c955499dad328e87c6a3f12e,
title = "[(123/125)I]RTI-55, an in vivo label for the serotonin transporter",
abstract = "[123I]RTI-55, an iodinated derivative of the cocaine analog 3β- phenyltropane-2β-carboxylic acid methyl ester, was evaluated as an agent for in vivo labeling of the serotonin transporter. Labeling of the precursor of RTI-55 with I-123 was efficient and yielded a high specific activity product. After intravenous injection of [123I]RTI-55 into rats, the tracer accumulated in regions with high densities of serotonin and dopamine uptake sites. The distribution of [123I]RTI-55 binding in areas rich in serotonin uptake sites correlated with [3H]serotonin uptake measured in vitro in the same regions. Specific [123I]RTI-55 binding to serotonin uptake sites was inhibited by paroxetine but not by GBR 12,909. Treatment of rats with neurotoxic doses of fenfluramine caused decreases of 66{\%} (in the hypothalamus) to 83{\%} (in the superior colliculi) of specific [125I]RTI-55 binding in all areas except in the striatum and the olfactory tubercles (regions rich in dopamine transporters). These results indicate that [(123/125)I]RTI-55 binds, although not selectively, to the serotonin transporter in vivo. Furthermore, they suggest that [123I]RTI-55 holds promise as a SPECT imaging agent for the study of the serotonin transporter in humans in health and disease.",
author = "U. Scheffel and Dannals, {Robert F} and Cline, {E. J.} and George Ricaurte and Carroll, {F. I.} and P. Abraham and Lewin, {A. H.} and Kuhar, {M. J.}",
year = "1992",
doi = "10.1002/syn.890110206",
language = "English (US)",
volume = "11",
pages = "134--139",
journal = "Synapse",
issn = "0887-4476",
publisher = "Wiley-Liss Inc.",
number = "2",

}

TY - JOUR

T1 - [(123/125)I]RTI-55, an in vivo label for the serotonin transporter

AU - Scheffel, U.

AU - Dannals, Robert F

AU - Cline, E. J.

AU - Ricaurte, George

AU - Carroll, F. I.

AU - Abraham, P.

AU - Lewin, A. H.

AU - Kuhar, M. J.

PY - 1992

Y1 - 1992

N2 - [123I]RTI-55, an iodinated derivative of the cocaine analog 3β- phenyltropane-2β-carboxylic acid methyl ester, was evaluated as an agent for in vivo labeling of the serotonin transporter. Labeling of the precursor of RTI-55 with I-123 was efficient and yielded a high specific activity product. After intravenous injection of [123I]RTI-55 into rats, the tracer accumulated in regions with high densities of serotonin and dopamine uptake sites. The distribution of [123I]RTI-55 binding in areas rich in serotonin uptake sites correlated with [3H]serotonin uptake measured in vitro in the same regions. Specific [123I]RTI-55 binding to serotonin uptake sites was inhibited by paroxetine but not by GBR 12,909. Treatment of rats with neurotoxic doses of fenfluramine caused decreases of 66% (in the hypothalamus) to 83% (in the superior colliculi) of specific [125I]RTI-55 binding in all areas except in the striatum and the olfactory tubercles (regions rich in dopamine transporters). These results indicate that [(123/125)I]RTI-55 binds, although not selectively, to the serotonin transporter in vivo. Furthermore, they suggest that [123I]RTI-55 holds promise as a SPECT imaging agent for the study of the serotonin transporter in humans in health and disease.

AB - [123I]RTI-55, an iodinated derivative of the cocaine analog 3β- phenyltropane-2β-carboxylic acid methyl ester, was evaluated as an agent for in vivo labeling of the serotonin transporter. Labeling of the precursor of RTI-55 with I-123 was efficient and yielded a high specific activity product. After intravenous injection of [123I]RTI-55 into rats, the tracer accumulated in regions with high densities of serotonin and dopamine uptake sites. The distribution of [123I]RTI-55 binding in areas rich in serotonin uptake sites correlated with [3H]serotonin uptake measured in vitro in the same regions. Specific [123I]RTI-55 binding to serotonin uptake sites was inhibited by paroxetine but not by GBR 12,909. Treatment of rats with neurotoxic doses of fenfluramine caused decreases of 66% (in the hypothalamus) to 83% (in the superior colliculi) of specific [125I]RTI-55 binding in all areas except in the striatum and the olfactory tubercles (regions rich in dopamine transporters). These results indicate that [(123/125)I]RTI-55 binds, although not selectively, to the serotonin transporter in vivo. Furthermore, they suggest that [123I]RTI-55 holds promise as a SPECT imaging agent for the study of the serotonin transporter in humans in health and disease.

UR - http://www.scopus.com/inward/record.url?scp=0026613049&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0026613049&partnerID=8YFLogxK

U2 - 10.1002/syn.890110206

DO - 10.1002/syn.890110206

M3 - Article

C2 - 1385663

AN - SCOPUS:0026613049

VL - 11

SP - 134

EP - 139

JO - Synapse

JF - Synapse

SN - 0887-4476

IS - 2

ER -