Synthesis and 5-HT-3 receptor binding activity of 5-[125I]iodo-2,3-dimethoxy-N-(1-azabicyclo[2.2.2]oct-3-yl)benzamide and its 5-halogen-2-alkoxyl homologues

Add time:08/18/2019    Source:sciencedirect.com

Summary(S)-5-Iodo-2,3-dimethoxy-N-(1-azabicyclo[2.2.2]oct-3-yl)benzamide (MIZAC) was prepared from 5-iodo-2,3-dimethoxybenzoyl chloride and (S)-3-aminoquinuclidine. [125I]Iodode-stannylation of its corresponding 5-tri-n-butyltin derivative gave [125I]-MIZAC at 1800 Ci/mmol. Binding of [125I]-MIZAC in rat entorhinal cortex revealed a KD of 1.37 ± 0.21 nM. A series of racemic 2-O-alkyl derivatives of MIZAC were prepared and 5-HT-3 receptor affinities were determined by inhibition of [125I]-MIZAC binding. Optimal affinity for the receptor was obtained with small, electron-withdrawing substituents in the aromatic 5-position and with bulky substituents in the 3-position. [125I]-MIZAC is a selective radioligand useful for in vitro identification of the 5-HT-3 receptor.

We also recommend Trading Suppliers and Manufacturers of (S)-N-(1-Azabicyclo[2.2.2]oct-3-yl)-5,6,7,8-tetrahydro-1-naphthalenecarboxamide (cas 135729-78-1). Pls Click Website Link as below: cas 135729-78-1 suppliers

Prev:Synthesis and 5-HT-3 Receptor Binding of 2- and 3-(Halo)alkoxyl Substituted (S)-N-(1-Azabicyclo [2.2.2]oct-3-yl)-5-chlorobenzamides as Potential Radioligands
Next:Evaluation of 1-azabicyclo[2.2.2]oct-3-yl α-fluoroalkyl-α-hydroxy-α-phenylacetates as potential ligands for the study of muscarinic receptor density by positron emission tomography☆)