Synthesis and evaluation of tritium labelled 10-methylgalanthamine iodide: a novel compound to examine the mechanism of interaction of galanthamine derivatives with the nicotinic acetylcholine receptors
✍ Scribed by Andreas Schildan; Ralf Schirrmacher; Esther Schirrmacher; Marek Samochocki; Claudia Christner; Alfred Maelicke; Frank Rösch
- Publisher
- John Wiley and Sons
- Year
- 2003
- Tongue
- French
- Weight
- 127 KB
- Volume
- 46
- Category
- Article
- ISSN
- 0022-2135
- DOI
- 10.1002/jlcr.744
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✦ Synopsis
Abstract
A new promising galanthamine derivative, 10‐[^3^H]methylgalanthamine iodide, was synthesized for binding studies to nicotinic acetylcholine receptors expressed in Torpedo electric ray electroplaques. Galanthamine was reacted with [^3^H]methyl iodide to yield 10‐[^3^H]methylgalanthamine iodide with a radiochemical yield of >70% and a specific activity of 32 Ci/mmol after purification via solid phase extraction. To test the ligand properties of the radioligand, calcium imaging and electrophysiology of the non‐radioactive analogue were performed to obtain an EC~50~ of 270 nM, a Hill coefficient of 1.9 and the induced cell current. Copyright © 2003 John Wiley & Sons, Ltd.