Synthesis and biological characterization of stable and radioiodinated (±)-trans-2-hydroxy-3-P{4-(3-iodophenyl)piperidyl}-1,2,3,4-tetrahydronaphthalene (3′-IBVM)

Add time:08/14/2019    Source:sciencedirect.com

The vesamicol analogue (±)-trans-2-Hydroxy-3-{4-(3-iodophenyl)piperidyl}-1,2,3,4-tetrahydronaphthalene (3′-IBVM), a potent ligand for the vesicular acetylcholine transporter (VAChT), was evaluated as a potential radiotracer for studying VAChT density in vivo. In radioligand binding experiments, 3′-IBVM displays subnanomolar affinity for VAChT and 100-fold selectivity for VAChT over σ1 and σ2 receptors. Consistent with this profile, radioiodinated (±)-3′-IBVM distributed heterogenously in the rat brain following a bolus IV injection, displaying high concentrations in the striatum and moderate to low concentrations in the cortex and cerebellum, respectively. However, co-injection of the radiotracer with the sigma ligand haloperidol resulted in significant reductions of radiotracer levels in all brain regions examined. Therefore, radioiodinated (±)-IBVM appears to bind to both VAChT and sigma receptors in vivo.

We also recommend Trading Suppliers and Manufacturers of N-(1(S)-carboxy-(4-hydroxy-3-iodophenyl)ethyl)-alanylproline (cas 104531-07-9). Pls Click Website Link as below: cas 104531-07-9 suppliers

Prev:ArticleRemoval of chloride from simulated acidic wastewater in the zinc production☆
Next:Full Length ArticleIon selective electrodes based on methyl 6-(hydroxymethyl) picolinate ionophore for electrochemical determination of Fe(III) in petroleum water samples)