Pyrrolovesamicols - Synthesis, structure and VAChT binding of two 4-fluorobenzoyl regioisomers


Pyrrolovesamicols - Synthesis, structure and VAChT binding of two 4-fluorobenzoyl regioisomers

Wenzel, B.; Li, Y.; Kraus, W.; Sorger, D.; Sabri, O.; Brust, P.; Steinbach, J.

This letter describes the synthesis of two regioisomers of a new class of vesamicol analogs as possible ligands for imaging the vesicular acetylcholine transporter in future PET studies. The reaction mechanism of the synthesis of these two pyrrolovesamicols was studied by HPLC and the molecular structures were determined by X-Ray structure analysis. Binding affinities to VAChT were evaluated by competitive binding analysis using a cell line stably transfected with ratVAChT.

Keywords: Pyrrolovesamicol; Vesamicol; VAChT; Pyrrole

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