ArticleBioorganic & medicinal chemistry letters2011
Discovery of non-peptide, small molecule antagonists of α9α10 nicotinic acetylcholine receptors as novel analgesics for the treatment of neuropathic and tonic inflammatory pain.
Article in Bioorganic & medicinal chemistry letters, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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The trial behind it
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Who cites it
20 citing papers in PubMed.
- The role of acetylcholine and its receptors in tumor immune regulation: mechanisms and potential therapeutic targets.Molecular cancer · 2025Review
- New Alpha9 nAChR Ligands Based on a 5-(Quinuclidin-3-ylmethyl)-1,2,4-oxadiazole Scaffold.ACS chemical neuroscience · 2024Article
- From 2-Triethylammonium Ethyl Ether of 4-Stilbenol (MG624) to Selective Small-Molecule Antagonists of Human α9α10 Nicotinic Receptor by Modifications at the Ammonium Ethyl Residue.Journal of medicinal chemistry · 2022Article
- Development of Immunochromatographic Strip for Detection of αB-VxXXIVA-Conotoxin Based on 5E4 Monoclonal Antibody.Toxins · 2022Article
- Detection of αB-Conotoxin VxXXIVA (αB-CTX) by ic-ELISA Based on an Epitope-Specific Monoclonal Antibody.Toxins · 2022Article
- Characterizing the Access of Cholinergic Antagonists to Efferent Synapses in the Inner Ear.Frontiers in neuroscience · 2021Article
- RgIA4 Accelerates Recovery from Paclitaxel-Induced Neuropathic Pain in Rats.Marine drugs · 2019Article
- α9-containing nicotinic acetylcholine receptors and the modulation of pain.British journal of pharmacology · 2018Review
- Nicotinic acetylcholine receptors in neuropathic and inflammatory pain.FEBS letters · 2018Review
- Crystal structure of 4,4'-bis-[3-(piperidin-1-yl)prop-1-yn-1-yl]-1,1'-biphen-yl.Acta crystallographica. Section E, Crystallographic communications · 2017Article
- RgIA4 Potently Blocks Mouse α9α10 nAChRs and Provides Long Lasting Protection against Oxaliplatin-Induced Cold Allodynia.Frontiers in cellular neuroscience · 2017Article
- Comparison crystal structure conformations of two structurally related biphenyl analogues: 4,4'-bis-[3-(pyrrolidin-1-yl)prop-1-yn-1-yl]-1,1'-biphenyl and 4,4'-bis-{3-[(S)-2-methyl-pyrrolidin-1-yl]prop-1-yn-1-yl}-1,1'-biphen-yl.Acta crystallographica. Section E, Crystallographic communications · 2015Article
- Comparison of the crystal structures of 4,4'-bis-[3-(4-methyl-piperidin-1-yl)prop-1-yn-1-yl]-1,1'-biphenyl and 4,4'-bis-[3-(2,2,6,6-tetra-methyl-piperidin-1-yl)prop-1-yn-1-yl]-1,1'-biphen-yl.Acta crystallographica. Section E, Crystallographic communications · 2015Article
- Cloning, synthesis, and characterization of αO-conotoxin GeXIVA, a potent α9α10 nicotinic acetylcholine receptor antagonist.Proceedings of the National Academy of Sciences of the United States of America · 2015Article
- Conotoxins targeting nicotinic acetylcholine receptors: an overview.Marine drugs · 2014Review
- A novel inhibitor of α9α10 nicotinic acetylcholine receptors from Conus vexillum delineates a new conotoxin superfamily.PloS one · 2013Article
- Novel small molecule α9α10 nicotinic receptor antagonist prevents and reverses chemotherapy-evoked neuropathic pain in rats.Anesthesia and analgesia · 2012Article
- Molecular basis for the differential sensitivity of rat and human α9α10 nAChRs to α-conotoxin RgIA.Journal of neurochemistry · 2012Article
- Nicotinic acetylcholine receptors in dorsal root ganglion neurons include the α6β4* subtype.FASEB journal : official publication of the Federation of American Societies for Experimental Biology · 2012Article
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8 authors.
Funding
Abstract
A series of azaaromatic quaternary ammonium analogs has been discovered as potent and selective α9α10 nicotinic acetylcholine receptor (nAChR) antagonists. The preliminary structure-activity relationships of these analogs suggest that increased rigidity in the linker units results in higher potency in inhibition of α9α10 nAChRs and greater selectivity over α7 nAChRs. These analogs represent a new class of analgesic for the treatment of neuropathic and tonic inflammatory pain.
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Registered trials
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