6533b862fe1ef96bd12c6b8c
RESEARCH PRODUCT
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
Andreas SchildanAndreas SchildanEsther SchirrmacherMarek SamochockiRalf SchirrmacherClaudia ChristnerAlfred MaelickeFrank Röschsubject
chemistry.chemical_classificationStereochemistryOrganic ChemistryIodideLigand (biochemistry)BiochemistryMedicinal chemistryChemical synthesisAnalytical Chemistrylaw.inventionchemistry.chemical_compoundNicotinic agonistchemistrylawDrug DiscoveryRadioligandRadiology Nuclear Medicine and imagingSpectroscopyTorpedoAcetylcholine receptorMethyl iodidedescription
Summary 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 EC50 of 270 nM, a Hill coefficient of 1.9 and the induced cell current. Copyright # 2003 John Wiley & Sons, Ltd.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2003-08-29 | Journal of Labelled Compounds and Radiopharmaceuticals |