ArticleJournal of medicinal chemistry2010
Novel α3β4 nicotinic acetylcholine receptor-selective ligands. Discovery, structure-activity studies, and pharmacological evaluation.
Article in Journal of medicinal chemistry, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 33 papers.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
33 citing papers in PubMed.
- An accessory orthosteric ligand binding site in the (α3)Cell reports · 2026Article
- Synthesis of α3β4 Nicotinic Acetylcholine Receptor Modulators Derived from Aristoquinoline That Reduce Reinstatement of Cocaine-Seeking Behavior.Journal of medicinal chemistry · 2024Article
- SAL0114: a novel deuterated dextromethorphan-bupropion combination with improved antidepressant efficacy and safety profile.Frontiers in pharmacology · 2024Article
- Review
- Review
- Cholinergic Boutons are Distributed Along the Dendrites and Somata of VIP Neurons in the Inferior Colliculus.Journal of the Association for Research in Otolaryngology : JARO · 2023Article
- Selective αInternational journal of molecular sciences · 2023Article
- What We Have Gained from Ibogaine: α3β4 Nicotinic Acetylcholine Receptor Inhibitors as Treatments for Substance Use Disorders.Journal of medicinal chemistry · 2023Review
- Functional α7 nicotinic acetylcholine receptors in GABAergic neurons of the interpeduncular nucleus.Neuropharmacology · 2022Article
- Ethanol interaction with α3β4 nicotinic acetylcholine receptors in neurons of the laterodorsal tegmentum.Alcoholism, clinical and experimental research · 2021Article
- Molecular insights into the benefits of nicotine on memory and cognition (Review).Molecular medicine reports · 2021Review
- Synaptic Components, Function and Modulation Characterized by GCaMP6f CaFrontiers in physiology · 2021Article
- αFrontiers in neural circuits · 2021Article
- Cholinergic System and Its Therapeutic Importance in Inflammation and Autoimmunity.Frontiers in immunology · 2021Review
- Activation of nicotinic acetylcholine receptors induces potentiation and synchronization within in vitro hippocampal networks.Journal of neurochemistry · 2020Article
- Neuronal nicotinic acetylcholine receptors mediate ∆Addiction biology · 2020Article
- Design, synthesis, and biological activity of 5'-phenyl-1,2,5,6-tetrahydro-3,3'-bipyridine analogues as potential antagonists of nicotinic acetylcholine receptors.Bioorganic & medicinal chemistry letters · 2017Article
- A Simple Representation of Three-Dimensional Molecular Structure.Journal of medicinal chemistry · 2017Article
- High-Throughput Patch Clamp Screening in Human α6-Containing Nicotinic Acetylcholine Receptors.SLAS discovery : advancing life sciences R & D · 2017Article
- Habenula cholinergic neurons regulate anxiety during nicotine withdrawal via nicotinic acetylcholine receptors.Neuropharmacology · 2016Article
Corrections and comments
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Authors and funding
5 authors.
Funding
Abstract
Antagonist activity at the α3β4 nicotinic acetylcholine receptor (nAChR) is thought to contribute to the antiaddictive properties of several compounds. However, truly selective ligands for the α3β4 nAChR have not been available. We report the discovery and SAR of a novel class of compounds that bind to the α3β4 nAChR and have no measurable affinity for the α4β2 or α7 subtype. In functional assays the lead compound antagonized epibatidine-induced Ca(2+) flux in α3β4-transfected cells in a noncompetitive manner.
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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.