ArticleMolecular pharmacology2019
Allosteric Agonism of
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Article in Molecular pharmacology, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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22citing papers in PubMed
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Who cites it
22 citing papers in PubMed.
- Two types of axonal muscarinic acetylcholine receptors mediate formation of saliva cocktail in the tick Ixodes ricinus.Nature communications · 2026Article
- Structural basis for allosteric agonism of human α7 nicotinic acetylcholine receptors.Cell discovery · 2025Article
- Competitive Antagonism of Xylazine on α7 Nicotinic Acetylcholine Receptors and Reversal by Curcuminoids.ACS chemical neuroscience · 2025Article
- Functional expression and properties of the tick α6 homomeric nicotinic acetylcholine receptor inCurrent research in parasitology & vector-borne diseases · 2025Article
- Mechanisms of Action Underlying Conductance-Modifying Positive Allosteric Modulators of the NMDA Receptor.Molecular pharmacology · 2024Article
- Recent Advances in the Discovery of Nicotinic Acetylcholine Receptor Allosteric Modulators.Molecules (Basel, Switzerland) · 2023Review
- Dose-dependent effects of GAT107, a novel allosteric agonist-positive allosteric modulator (ago-PAM) for the α7 nicotinic cholinergic receptor: a BOLD phMRI and connectivity study on awake rats.Frontiers in neuroscience · 2023Article
- Differential Activation and Desensitization States Promoted by NoncanonicalThe Journal of pharmacology and experimental therapeutics · 2022Article
- Differential interactions of resting, activated, and desensitized states of the α7 nicotinic acetylcholine receptor with lipidic modulators.Proceedings of the National Academy of Sciences of the United States of America · 2022Article
- Sulfonium Ligands of the α7 nAChR.Molecules (Basel, Switzerland) · 2021Article
- Stable desensitization of αEuropean journal of pharmacology · 2021Article
- The Allosteric Activation of α7 nAChR by α-Conotoxin MrIC Is Modified by Mutations at the Vestibular Site.Toxins · 2021Article
- Therapeutic Targeting ofPharmacological reviews · 2021Review
- Design, synthesis, and electrophysiological evaluation of NS6740 derivatives: Exploration of the structure-activity relationship for alpha7 nicotinic acetylcholine receptor silent activation.European journal of medicinal chemistry · 2020Article
- A Computational Analysis of the Factors Governing the Dynamics of α7 nAChR and Its Homologs.Biophysical journal · 2020Article
- Nicotinic receptor pharmacology in silico: Insights and challenges.Neuropharmacology · 2020Review
- Differing Activity Profiles of the Stereoisomers of 2,3,5,6TMP-TQS, a Putative Silent Allosteric Modulator ofMolecular pharmacology · 2020Article
- Nicotinic acetylcholine receptors: Conventional and unconventional ligands and signaling.Neuropharmacology · 2020Review
- In Silico Modeling of the α7 Nicotinic Acetylcholine Receptor: New Pharmacological Challenges Associated with Multiple Modes of Signaling.Mini reviews in medicinal chemistry · 2020Review
- Synthesis, Pharmacological Characterization, and Structure-Activity Relationships of Noncanonical Selective Agonists for α7 nAChRs.Journal of medicinal chemistry · 2019Article
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Authors and funding
7 authors.
Alican GulsevinDepartments of Chemistry (A.G., M.Q., N.A.H.) and Pharmacology and Therapeutics (R.L.P, C.S., M.Q.), University of Florida, Gainesville, Florida; and Department of Pharmaceutical Sciences, School of Pharmacy, Bouvé College of Health Sciences, Northeastern University, Boston, Massachusetts (S.G., G.A.T.).ORCID 0000-0002-8724-5777
Roger L PapkeDepartments of Chemistry (A.G., M.Q., N.A.H.) and Pharmacology and Therapeutics (R.L.P, C.S., M.Q.), University of Florida, Gainesville, Florida; and Department of Pharmaceutical Sciences, School of Pharmacy, Bouvé College of Health Sciences, Northeastern University, Boston, Massachusetts (S.G., G.A.T.) rlpapke@ufl.edu.ORCID 0000-0002-4468-8658
Clare StokesDepartments of Chemistry (A.G., M.Q., N.A.H.) and Pharmacology and Therapeutics (R.L.P, C.S., M.Q.), University of Florida, Gainesville, Florida; and Department of Pharmaceutical Sciences, School of Pharmacy, Bouvé College of Health Sciences, Northeastern University, Boston, Massachusetts (S.G., G.A.T.).ORCID 0000-0002-4076-5361
Sumanta GaraiDepartments of Chemistry (A.G., M.Q., N.A.H.) and Pharmacology and Therapeutics (R.L.P, C.S., M.Q.), University of Florida, Gainesville, Florida; and Department of Pharmaceutical Sciences, School of Pharmacy, Bouvé College of Health Sciences, Northeastern University, Boston, Massachusetts (S.G., G.A.T.).
Ganesh A ThakurDepartments of Chemistry (A.G., M.Q., N.A.H.) and Pharmacology and Therapeutics (R.L.P, C.S., M.Q.), University of Florida, Gainesville, Florida; and Department of Pharmaceutical Sciences, School of Pharmacy, Bouvé College of Health Sciences, Northeastern University, Boston, Massachusetts (S.G., G.A.T.).ORCID 0000-0001-8228-5799
Marta QuadriDepartments of Chemistry (A.G., M.Q., N.A.H.) and Pharmacology and Therapeutics (R.L.P, C.S., M.Q.), University of Florida, Gainesville, Florida; and Department of Pharmaceutical Sciences, School of Pharmacy, Bouvé College of Health Sciences, Northeastern University, Boston, Massachusetts (S.G., G.A.T.).ORCID 0000-0003-2174-9793
Nicole A HorensteinDepartments of Chemistry (A.G., M.Q., N.A.H.) and Pharmacology and Therapeutics (R.L.P, C.S., M.Q.), University of Florida, Gainesville, Florida; and Department of Pharmaceutical Sciences, School of Pharmacy, Bouvé College of Health Sciences, Northeastern University, Boston, Massachusetts (S.G., G.A.T.) horen@chem.ufl.edu.
Funding
Targeting of Alpha7 nAChR for therapeutic effectsR01GM057481 · NIGMS · UNIVERSITY OF FLORIDA · PI PAPKE, ROGER L · 2000 to 2023
$7.6MNIGMS NIH HHS R01 GM057481
Abstract
Nicotinic acetylcholine receptors (nAChRs) are members of the Cys-loop superfamily of ligand-gated ion channels. Typically, channel activation follows the binding of agonists to the orthosteric binding sites of the receptor.
Indexed as
MutationAllosteric RegulationAllosteric Sitealpha7 Nicotinic Acetylcholine ReceptorAnimalsBinding SitesCell LineHumansIsoxazolesMaleModels, MolecularMolecular Docking SimulationMolecular Dynamics SimulationNicotinic AgonistsPhenylurea CompoundsPiperazines1-(5-chloro-2,4-dimethoxyphenyl)-3-(5-methylisoxazol-3-yl)urea4-(4-bromophenyl)-3a,4,5,9b-tetrahydro-3H-cyclopenta(c)quinoline-8-sulfonamidealpha7 Nicotinic Acetylcholine ReceptorIsoxazolesNicotinic AgonistsPhenylurea CompoundsPiperazinesQuinolinesSulfonamides
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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.