N-(3-iodophenyl)trozamicol (IPHT) and related inhibitors of vesicular acetylcholine transport: synthesis and preliminary biological characterization
| Autor: | A.B Khare, Rosemary B. Langason, Simon M. N. Efange, Stanley M. Parsons, Robert H. Mach |
|---|---|
| Rok vydání: | 1999 |
| Předmět: |
Male
Cancer Research Vesamicol Stereochemistry Vesicular Acetylcholine Transport Proteins Vesicular Transport Proteins Ligands Binding Competitive Chemical synthesis Piperazines Iodine Radioisotopes Structure-Activity Relationship chemistry.chemical_compound Isomerism Piperidines Vesicular acetylcholine transporter Acetylcholine transport medicine Animals Receptors sigma Tissue Distribution Radiology Nuclear Medicine and imaging Rats Wistar Molecular Structure Iodobenzenes Ligand Brain Membrane Transport Proteins Transporter Acetylcholine Rats Kinetics chemistry Molecular Medicine Cholinergic Indicators and Reagents Carrier Proteins medicine.drug |
| Zdroj: | Nuclear Medicine and Biology. 26:609-617 |
| ISSN: | 0969-8051 |
| DOI: | 10.1016/s0969-8051(99)00013-x |
| Popis: | Four isomeric N -(halophenyl)trozamicol analogues (6a–d) were synthesized and evaluated as potential vesicular acetylcholine transporter (VAChT) ligands. Of the four compounds, N -(3-bromophenyl)trozamicol (6b) and N -(3-iodophenyl)trozamicol (6d) displayed the highest affinity for the VAChT in vitro , whereas the para -substituted compound 6c showed the lowest affinity for this transporter. Tissue distribution studies of N -(3-[ 125 I]iodophenyl)trozamicol ([ 125 I]6d, [ 125 I]IPHT) suggest that the central distribution of the latter is consistent with cholinergic innervation. However, only moderate target-to-background ratios were obtained, suggesting little improvement over the N -(halobenzyl)trozamicols described previously. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Full Text from ScienceDirect