ArticleJournal of medicinal chemistry2013
Heteroaromatic and aniline derivatives of piperidines as potent ligands for vesicular acetylcholine transporter.
Article in Journal of medicinal chemistry, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
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Who cites it
21 citing papers in PubMed.
- Discovery and in vivo evaluation of a fluorine-18 pro-drug tracer for imaging sphingosine-1-phosphate receptor 2 in the brain.Bioorganic & medicinal chemistry · 2026Article
- Synthesis and in vivo biological characterization of six carbon-11 sigma-1 receptor radiotracers in rodent and nonhuman primate.Bioorganic & medicinal chemistry · 2025Article
- Discovery ofCells · 2025Article
- Radiation dosimetry and fasting-dependent hepatobiliary clearance of the VAChT-specific PET radioligandEJNMMI research · 2025Article
- The Benzoylpiperidine Fragment as a Privileged Structure in Medicinal Chemistry: A Comprehensive Review.Molecules (Basel, Switzerland) · 2024Review
- Development and Optimization ofACS pharmacology & translational science · 2023Review
- In vitro characterization of [European journal of pharmacology · 2021Article
- Radiosynthesis and evaluation of a fluorine-18 labeled radioligand targeting vesicular acetylcholine transporter.Bioorganic & medicinal chemistry letters · 2018Article
- Exploration of Sulfur-Containing Analogues for Imaging Vesicular Acetylcholine Transporter in the Brain.ChemMedChem · 2018Article
- Kinetic modeling of [Journal of neurochemistry · 2018Article
- In Vivo and In Vitro Characteristics of Radiolabeled Vesamicol Analogs as the Vesicular Acetylcholine Transporter Imaging Agents.Contrast media & molecular imaging · 2018Review
- Structure-Based Optimization of Pyridoxal 5'-Phosphate-Dependent Transaminase Enzyme (BioA) Inhibitors that Target Biotin Biosynthesis in Mycobacterium tuberculosis.Journal of medicinal chemistry · 2017Article
- Synthesis, resolution, and in vitro evaluation of three vesicular acetylcholine transporter ligands and evaluation of the lead fluorine-18 radioligand in a nonhuman primate.Organic & biomolecular chemistry · 2017Article
- Comparison of [Pharmacology research & perspectives · 2016Article
- Kinetics modeling and occupancy studies of a novel C-11 PET tracer for VAChT in nonhuman primates.Nuclear medicine and biology · 2016Article
- Article
- Synthesis and biological characterization of a promising F-18 PET tracer for vesicular acetylcholine transporter.Bioorganic & medicinal chemistry · 2015Article
- In vitro and ex vivo characterization of (-)-TZ659 as a ligand for imaging the vesicular acetylcholine transporter.European journal of pharmacology · 2015Article
- Syntheses and radiosyntheses of two carbon-11 labeled potent and selective radioligands for imaging vesicular acetylcholine transporter.Molecular imaging and biology · 2014Article
- In vitro and in vivo characterization of two C-11-labeled pet tracers for vesicular acetylcholine transporter.Molecular imaging and biology · 2014Article
Corrections and comments
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Authors and funding
13 authors.
Funding
Abstract
To identify suitable lipophilic compounds having high potency and selectivity for vesicular acetylcholine transporter (VAChT), a heteroaromatic ring or a phenyl group was introduced into the carbonyl-containing scaffold for VAChT ligands. Twenty new compounds with ALogD values between 0.53 and 3.2 were synthesized, and their in vitro binding affinities were assayed. Six of them (19a, 19e, 19g, 19k, and 24a-b) displayed high affinity for VAChT (Ki = 0.93-18 nM for racemates) and moderate to high selectivity for VAChT over σ1 and σ2 receptors (Ki = 44-4400-fold). These compounds have a methyl or a fluoro substitution that provides the position for incorporating PET radioisotopes C-11 or F-18. Compound (-)-[(11)C]24b (Ki = 0.78 nM for VAChT, 1200-fold over σ receptors) was successfully synthesized and evaluated in vivo in rats and nonhuman primates. The data revealed that (-)-[(11)C]24b has highest binding in striatum and has favorable pharmacokinetics in the brain.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.