Synthesis and evaluation of iodinated TZTP-derivatives as potential radioligands for imaging of muscarinic M-2 receptors with SPET

Remco J. J. Knol; Tamme Doornbos; Jan C. van den Bos; Kora de Bruin; Martin Pfaffendorf; Wim Aanhaanen; Anton G. M. Janssen; Joseph A. J. M. Vekemans; Berthe L. F. van Eck-Smit; Jan Booij

doi:https://doi.org/10.1016/S0969-8051(03)00095-7

Synthesis and evaluation of iodinated TZTP-derivatives as potential radioligands for imaging of muscarinic M-2 receptors with SPET

Remco J. J. Knol, Tamme Doornbos, Jan C. van den Bos, Kora de Bruin, Martin Pfaffendorf, Wim Aanhaanen, Anton G. M. Janssen, Joseph A. J. M. Vekemans, Berthe L. F. van Eck-Smit, Jan Booij

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

3 Citations (Scopus)

Abstract

A series of iodinated thiadiazolyltetrahydro-1-methyl-pyridine (TZTP) compounds was synthesized and evaluated in vitro and in vivo as potential radioligands for imaging of the muscarinic M-2 receptor subtype with SPET. One of these compounds, 5-(E)-iodopentenylthio-TZTP, has high in vitro affinity (K-i = 4.9 nM) and moderate selectivity for the muscarinic M, receptor subtype. Although the uptake pattern in the biodistribution studies in rats is consistent with muscarinic M2 receptor distribution, specific in vivo binding to these receptors could not be demonstrated. The usefulness of this tracer in human SPET imaging may therefore be limited. (C) 2004 Elsevier Inc. All rights reserved

Original language	English
Pages (from-to)	111-123
Journal	Nuclear medicine and biology
Volume	31
Issue number	1
DOIs	https://doi.org/10.1016/S0969-8051(03)00095-7
Publication status	Published - 2004

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https://doi.org/10.1016/S0969-8051(03)00095-7

Cite this

Knol, R. J. J., Doornbos, T., van den Bos, J. C., de Bruin, K., Pfaffendorf, M., Aanhaanen, W., Janssen, A. G. M., Vekemans, J. A. J. M., van Eck-Smit, B. L. F., & Booij, J. (2004). Synthesis and evaluation of iodinated TZTP-derivatives as potential radioligands for imaging of muscarinic M-2 receptors with SPET. Nuclear medicine and biology, 31(1), 111-123. https://doi.org/10.1016/S0969-8051(03)00095-7

@article{120a6096975d49bd893122309a7a7742,

title = "Synthesis and evaluation of iodinated TZTP-derivatives as potential radioligands for imaging of muscarinic M-2 receptors with SPET",

abstract = "A series of iodinated thiadiazolyltetrahydro-1-methyl-pyridine (TZTP) compounds was synthesized and evaluated in vitro and in vivo as potential radioligands for imaging of the muscarinic M-2 receptor subtype with SPET. One of these compounds, 5-(E)-iodopentenylthio-TZTP, has high in vitro affinity (K-i = 4.9 nM) and moderate selectivity for the muscarinic M, receptor subtype. Although the uptake pattern in the biodistribution studies in rats is consistent with muscarinic M2 receptor distribution, specific in vivo binding to these receptors could not be demonstrated. The usefulness of this tracer in human SPET imaging may therefore be limited. (C) 2004 Elsevier Inc. All rights reserved",

author = "Knol, {Remco J. J.} and Tamme Doornbos and {van den Bos}, {Jan C.} and {de Bruin}, Kora and Martin Pfaffendorf and Wim Aanhaanen and Janssen, {Anton G. M.} and Vekemans, {Joseph A. J. M.} and {van Eck-Smit}, {Berthe L. F.} and Jan Booij",

year = "2004",

doi = "https://doi.org/10.1016/S0969-8051(03)00095-7",

language = "English",

volume = "31",

pages = "111--123",

journal = "Nuclear medicine and biology",

issn = "0969-8051",

publisher = "Elsevier Inc.",

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Knol, RJJ, Doornbos, T, van den Bos, JC, de Bruin, K, Pfaffendorf, M, Aanhaanen, W, Janssen, AGM, Vekemans, JAJM, van Eck-Smit, BLF & Booij, J 2004, 'Synthesis and evaluation of iodinated TZTP-derivatives as potential radioligands for imaging of muscarinic M-2 receptors with SPET', Nuclear medicine and biology, vol. 31, no. 1, pp. 111-123. https://doi.org/10.1016/S0969-8051(03)00095-7

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AU - Knol, Remco J. J.

AU - Doornbos, Tamme

AU - van den Bos, Jan C.

AU - de Bruin, Kora

AU - Pfaffendorf, Martin

AU - Aanhaanen, Wim

AU - Janssen, Anton G. M.

AU - Vekemans, Joseph A. J. M.

AU - van Eck-Smit, Berthe L. F.

AU - Booij, Jan

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AB - A series of iodinated thiadiazolyltetrahydro-1-methyl-pyridine (TZTP) compounds was synthesized and evaluated in vitro and in vivo as potential radioligands for imaging of the muscarinic M-2 receptor subtype with SPET. One of these compounds, 5-(E)-iodopentenylthio-TZTP, has high in vitro affinity (K-i = 4.9 nM) and moderate selectivity for the muscarinic M, receptor subtype. Although the uptake pattern in the biodistribution studies in rats is consistent with muscarinic M2 receptor distribution, specific in vivo binding to these receptors could not be demonstrated. The usefulness of this tracer in human SPET imaging may therefore be limited. (C) 2004 Elsevier Inc. All rights reserved

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