| Title : Synthesis and evaluation of iodinated TZTP-derivatives as potential radioligands for imaging of muscarinic M2 receptors with SPET - Knol_2004_Nucl.Med.Biol_31_111 |
| Author(s) : Knol RJ , Doornbos T , van den Bos JC , de Bruin K , Pfaffendorf M , Aanhaanen W , Janssen AG , Vekemans JA , van Eck-Smit BL , Booij J |
| Ref : Nucl Med Biol , 31 :111 , 2004 |
|
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 M2 receptor subtype with SPET. One of these compounds, 5-(E)-iodopentenylthio-TZTP, has high in vitro affinity (Ki = 4.9 nM) and moderate selectivity for the muscarinic M2 receptor subtype. Although the uptake pattern in the biodistribution studies in rats is consistent with muscarinic M2 receptor disribution, specific in vivo binding to these receptors could not be demonstrated. The usefulness of this tracer in human SPET imaging may therefore be limited. |
| PubMedSearch : Knol_2004_Nucl.Med.Biol_31_111 |
| PubMedID: 14741576 |
Knol RJ, Doornbos T, van den Bos JC, de Bruin K, Pfaffendorf M, Aanhaanen W, Janssen AG, Vekemans JA, van Eck-Smit BL, Booij J (2004)
Synthesis and evaluation of iodinated TZTP-derivatives as potential radioligands for imaging of muscarinic M2 receptors with SPET
Nucl Med Biol
31 :111
Knol RJ, Doornbos T, van den Bos JC, de Bruin K, Pfaffendorf M, Aanhaanen W, Janssen AG, Vekemans JA, van Eck-Smit BL, Booij J (2004)
Nucl Med Biol
31 :111