ArticleJournal of medicinal chemistry2011
Synthesis and in vitro biological evaluation of carbonyl group-containing analogues for σ1 receptors.
Article in Journal of medicinal chemistry, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Who cites it
17 citing papers in PubMed, 21 citations in OpenAlex.
- Design, synthesis, and characterization of F-18 sigma-1 receptor radiotracers for Alzheimer disease.European journal of medicinal chemistry · 2026Article
- A Full-Spectrum Evaluation of Sigma-1 Receptor (S1R) Positron Emission Tomography (PET) Radioligands from Binding Affinity to Clinical Imaging.Molecules (Basel, Switzerland) · 2025Review
- Synthesis and in vivo biological characterization of six carbon-11 sigma-1 receptor radiotracers in rodent and nonhuman primate.Bioorganic & medicinal chemistry · 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
- Evaluation of [Molecular imaging and biology · 2022Article
- Piperidinyl Ureas Chemically Control Defective in Cullin Neddylation 1 (DCN1)-Mediated Cullin Neddylation.Journal of medicinal chemistry · 2018Article
- Kinetic modeling of [Journal of neurochemistry · 2018Article
- 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
- Chiral resolution of serial potent and selective σBioorganic & medicinal chemistry · 2017Article
- 4-aroylpiperidines and 4-(α-hydroxyphenyl)piperidines as selective sigma-1 receptor ligands: synthesis, preliminary pharmacological evaluation and computational studies.Chemistry Central journal · 2016Article
- Synthesis and biological characterization of a promising F-18 PET tracer for vesicular acetylcholine transporter.Bioorganic & medicinal chemistry · 2015Article
- In vitro and in vivo characterization of two C-11-labeled pet tracers for vesicular acetylcholine transporter.Molecular imaging and biology · 2014Article
- Syntheses and radiosyntheses of two carbon-11 labeled potent and selective radioligands for imaging vesicular acetylcholine transporter.Molecular imaging and biology · 2014Article
- Radiosynthesis andMedChemComm · 2014Article
- Positron emission tomography imaging of dopamine D2 receptors using a highly selective radiolabeled D2 receptor partial agonist.NeuroImage · 2013Article
- Synthesis and evaluation of in vitro bioactivity for vesicular acetylcholine transporter inhibitors containing two carbonyl groups.Bioorganic & medicinal chemistry · 2012Article
Corrections and comments
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Authors and funding
9 authors at 4 institutions in 1 country.
Funding
Abstract
To identify the ligands for σ(1) receptors that are potent and selective, analogues of prezamicol and trozamicol scaffolds of carbonyl-containing vesicular acetylcholine transporter (VAChT) inhibitors were explored. Of the 23 analogues synthesized and tested, 5 displayed very high affinity for σ(1) (K(i) = 0.48-4.05 nM) and high selectivity for σ(1) relative to σ(2) receptors (σ(1)/σ(2) selectivity of >749-fold). Four of the five compounds (14a, 14b, 14c, and 14e) showed very low affinity for VAChT (K(i) > 290 nM), and the fifth compound (14g) showed moderate affinity for VAChT (K(i) = 44.2 nM). The compound [1'-(4-fluorobenzyl)-3'-hydroxy[1,4']bipiperidinyl-4-yl]-(4-fluorophenyl)methanone (14a) displayed very high affinity and selectivity for σ(1) receptor (K(i) = 0.48 nM, σ(1)/σ(2) > 3600). All four of these most promising compounds (14a, 14b, 14c, and 14e) can be radiosynthesized with fluorine-18 or carbon-11, which will allow further evaluation of their properties as PET probes for imaging σ(1) receptor in vivo.
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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.