ArticleMolecular pharmacology2008
Multiple pharmacophores for the selective activation of nicotinic alpha7-type acetylcholine receptors.
Article in Molecular pharmacology, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 38 papers.
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Who cites it
38 citing papers in PubMed, 52 citations in OpenAlex.
- A new framework for nicotinic receptor-targeted therapeutic strategies in psychiatric and neurodegenerative disorders.Frontiers in cellular neuroscience · 2026Article
- New Alpha9 nAChR Ligands Based on a 5-(Quinuclidin-3-ylmethyl)-1,2,4-oxadiazole Scaffold.ACS chemical neuroscience · 2024Article
- Coffee and cigarettes: Modulation of high and low sensitivity α4β2 nicotinic acetylcholine receptors by n-MP, a biomarker of coffee consumption.Neuropharmacology · 2022Article
- Sulfonium Ligands of the α7 nAChR.Molecules (Basel, Switzerland) · 2021Article
- Therapeutic Targeting ofPharmacological reviews · 2021Review
- Nicotinic acetylcholine receptors: Conventional and unconventional ligands and signaling.Neuropharmacology · 2020Review
- Synthesis, Pharmacological Characterization, and Structure-Activity Relationships of Noncanonical Selective Agonists for α7 nAChRs.Journal of medicinal chemistry · 2019Article
- Cracking the Betel Nut: Cholinergic Activity of Areca Alkaloids and Related Compounds.Nicotine & tobacco research : official journal of the Society for Research on Nicotine and Tobacco · 2019Article
- Higher Gestational Choline Levels in Maternal Infection Are Protective for Infant Brain Development.The Journal of pediatrics · 2019Article
- Macroscopic and Microscopic Activation ofMolecular pharmacology · 2019Article
- Novel 5-(quinuclidin-3-ylmethyl)-1,2,4-oxadiazoles to investigate the activation of the α7 nicotinic acetylcholine receptor subtype: Synthesis and electrophysiological evaluation.European journal of medicinal chemistry · 2018Article
- Pharmacological modulation of the α7 nicotinic acetylcholine receptor in a mouse model of mecamylamine-precipitated nicotine withdrawal.Psychopharmacology · 2018Article
- NS6740, an α7 nicotinic acetylcholine receptor silent agonist, disrupts hippocampal synaptic plasticity.Neuroscience letters · 2018Article
- Persistent activation of α7 nicotinic ACh receptors associated with stable induction of different desensitized states.British journal of pharmacology · 2018Article
- Orthosteric and allosteric potentiation of heteromeric neuronal nicotinic acetylcholine receptors.British journal of pharmacology · 2018Review
- New Insights on Neuronal Nicotinic Acetylcholine Receptors as Targets for Pain and Inflammation: A Focus on α7 nAChRs.Current neuropharmacology · 2018Review
- Critical Molecular Determinants of α7 Nicotinic Acetylcholine Receptor Allosteric Activation: SEPARATION OF DIRECT ALLOSTERIC ACTIVATION AND POSITIVE ALLOSTERIC MODULATION.The Journal of biological chemistry · 2016Article
- Dissection of N,N-diethyl-N'-phenylpiperazines as α7 nicotinic receptor silent agonists.Bioorganic & medicinal chemistry · 2016Article
- A Promising PET Tracer for Imaging of α₇ Nicotinic Acetylcholine Receptors in the Brain: Design, Synthesis, and in Vivo Evaluation of a Dibenzothiophene-Based Radioligand.Molecules (Basel, Switzerland) · 2015Article
- An Unaltered Orthosteric Site and a Network of Long-Range Allosteric Interactions for PNU-120596 in α7 Nicotinic Acetylcholine Receptors.Chemistry & biology · 2015Article
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
Abstract
The activation of heteromeric and homomeric nicotinic acetylcholine receptors was studied in Xenopus laevis oocytes to identify key structures of putative agonist molecules associated with the selective activation of homomeric alpha7 receptors. We observed that selectivity between alpha7 and alpha4beta2 was more readily obtained than selectivity between alpha7 and alpha3beta4. Based on structural comparisons of previously characterized selective and nonselective agonists, we hypothesize at least three chemical motifs exist that, when present in molecules containing an appropriate cationic center, could be associated with the selective activation of alpha7 receptors. We identify the three distinct structural motifs based on prototypical drugs as the choline motif, the tropane motif, and the benzylidene motif. The choline motif involves the location of an oxygen-containing polar group such as a hydroxyl or carbonyl separated by two carbons from the charged nitrogen. The tropane motif provides alpha7-selectivity based on the addition of multiple small hydrophobic groups positioned away from the cationic center in specific orientations. We show that this motif can convert the nonselective agonists quinuclidine and ethyltrimethyl-ammonium to the alpha7-selective analogs methyl-quinuclidine and diethyldimethyl-ammonium, respectively. We have shown previously that the benzylidene group of 3-2,4, dimethoxy-benzylidene anabaseine (GTS-21) converts anabaseine into an alpha7-selective agonist. The benzylidene motif was also applied to quinuclidine to generate another distinct family of alpha7-selective agonists. Our results provide insight for the further development of nicotinic therapeutics and will be useful to direct future experiments with protein structure-based modeling and site-directed mutagenesis.
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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.