A simple probe measures the pharmacokinetics of [125I]RTI-55 in mouse brain in vivo

Takao Mochizuki, Victor L. Villemagne, Ursula Scheffel, Liu Xiang Liu, John L. Musachio, Robert F Dannals, Henry N. Wagner

Research output: Contribution to journalArticle

Abstract

A simple external radiation detector system was used to assess brain dopamine and serotonin transporters in mice in vivo using [125I]RTI-55. The results were compared to ex vivo dissection data. Methyl 3β-(4-iodophenyl) tropane-2β-carboxic acid methyl ester (RTI-55 or β-CIT), a high-affinity cocaine antagonist, binds to presynaptic dopamine and serotonin transporters in the brain. Radiotracer accumulation increased far the first 150 min after intravenous injection and then remained constant. When unlabeled RTI-55 was injected, either before or CO min after radiotracer administration, a significant decrease in tracer accumulation was observed. [125I]RTI-55 binding was also displaced by blocking doses of 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-[3-phenylpropyl]piperazine dihydrochloride (GBR 12909) and paroxetine. The results were similar to the ex vivo dissection data. The results demonstrate the feasibility of using the probe detector system to study the presynaptic transporter system in vivo in the mouse brain. The technique is applicable to other cerebral neurotransmitter systems.

Original languageEnglish (US)
Pages (from-to)17-23
Number of pages7
JournalEuropean Journal of Pharmacology
Volume338
Issue number1
DOIs
StatePublished - Oct 29 1997

Fingerprint

Pharmacokinetics
Serotonin Plasma Membrane Transport Proteins
Dopamine Plasma Membrane Transport Proteins
Brain
Dissection
Tropanes
Paroxetine
Carbon Monoxide
Cocaine
Intravenous Injections
Neurotransmitter Agents
Esters
Radiation
Acids
RTI 55
vanoxerine

Keywords

  • 5-HT (5-hydroxytryptamine, serotonin) transporter
  • Dopamine transporter
  • GBR 12909
  • Paroxetine
  • RTI-55
  • Single photon detection system

ASJC Scopus subject areas

  • Cellular and Molecular Neuroscience
  • Pharmacology

Cite this

Mochizuki, T., Villemagne, V. L., Scheffel, U., Xiang Liu, L., Musachio, J. L., Dannals, R. F., & Wagner, H. N. (1997). A simple probe measures the pharmacokinetics of [125I]RTI-55 in mouse brain in vivo. European Journal of Pharmacology, 338(1), 17-23. https://doi.org/10.1016/S0014-2999(97)01307-1

A simple probe measures the pharmacokinetics of [125I]RTI-55 in mouse brain in vivo. / Mochizuki, Takao; Villemagne, Victor L.; Scheffel, Ursula; Xiang Liu, Liu; Musachio, John L.; Dannals, Robert F; Wagner, Henry N.

In: European Journal of Pharmacology, Vol. 338, No. 1, 29.10.1997, p. 17-23.

Research output: Contribution to journalArticle

Mochizuki, T, Villemagne, VL, Scheffel, U, Xiang Liu, L, Musachio, JL, Dannals, RF & Wagner, HN 1997, 'A simple probe measures the pharmacokinetics of [125I]RTI-55 in mouse brain in vivo', European Journal of Pharmacology, vol. 338, no. 1, pp. 17-23. https://doi.org/10.1016/S0014-2999(97)01307-1
Mochizuki, Takao ; Villemagne, Victor L. ; Scheffel, Ursula ; Xiang Liu, Liu ; Musachio, John L. ; Dannals, Robert F ; Wagner, Henry N. / A simple probe measures the pharmacokinetics of [125I]RTI-55 in mouse brain in vivo. In: European Journal of Pharmacology. 1997 ; Vol. 338, No. 1. pp. 17-23.
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