ArticleACS chemical neuroscience2025
Enantiospecific Positive Allosteric Modulation of α4β2 Nicotinic Receptor Subtypes.
Josue Gaona, Pradip K Gadekar, Khaldoun S Abdelwahed, Nataly E Sanchez, Amaya Rolling, Robert Beaudoin, Brent Bill, Andrew T Kerr, Ganesh A Thakur, Ayman K Hamouda
Abstract read
In one paragraphArticle in ACS chemical neuroscience, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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5 · Who and what moneyAuthors and funding
10 authors.
Josue GaonaDepartment of Pharmaceutical Sciences and Health Outcomes, The University of Texas at Tyler, Tyler, Texas 75799, United States.
Pradip K GadekarDepartment of Pharmaceutical Sciences, Northeastern University, Boston, Massachusetts 02115, United States.ORCID 0000-0002-9129-8812 Khaldoun S AbdelwahedDepartment of Pharmaceutical Sciences and Health Outcomes, The University of Texas at Tyler, Tyler, Texas 75799, United States.
Nataly E SanchezDepartment of Pharmaceutical Sciences and Health Outcomes, The University of Texas at Tyler, Tyler, Texas 75799, United States.
Amaya RollingDepartment of Pharmaceutical Sciences and Health Outcomes, The University of Texas at Tyler, Tyler, Texas 75799, United States.
Robert BeaudoinDepartment of Pharmaceutical Sciences and Health Outcomes, The University of Texas at Tyler, Tyler, Texas 75799, United States.
Brent BillDepartment of Biology, The University of Texas at Tyler, Tyler, Texas 75799, United States.
Andrew T KerrCenter for Biomolecular Science and Engineering, US Naval Research Laboratory, Washington D.C. 20375, United States.
Ganesh A ThakurDepartment of Pharmaceutical Sciences, Northeastern University, Boston, Massachusetts 02115, United States.ORCID 0000-0002-7468-8819 Ayman K HamoudaDepartment of Pharmaceutical Sciences and Health Outcomes, The University of Texas at Tyler, Tyler, Texas 75799, United States.ORCID 0000-0001-7819-3074 Funding
Selective Positive Allosteric Modulators of a4b2 Nicotinic ReceptorsR01DA059985 · NIDA · NORTHEASTERN UNIVERSITY · PI CHRISTIE D FOWLER, Ayman K. Hamouda · 2024 to 2026
$2.1MIn vitro pharmacology and In vivo neuroprotective effects of CMPI analogues in an optimized Zebrafish model of Parkinsons diseaseR16NS129676 · NINDS · UNIVERSITY OF TEXAS TYLER · PI HAMOUDA, AYMAN K. · 2022 to 2025
$588kNIDA NIH HHS R01 DA059985NINDS NIH HHS R16 NS129676
6 · The paper itselfAbstract
Nicotinic acetylcholine receptors (nAChRs) are integral to brain function, playing critical roles in cognition and reward pathways. Among these, α4β2 nAChRs are key targets for developing therapeutics to address nicotine addiction and cognitive disorders. Here, we report the synthesis, stereochemical resolution, and pharmacological evaluation of GAT2800, a racemic compound identified as a positive allosteric modulator (PAM) of α4β2 nAChRs. Enantiomeric resolution yielded the inactive
Indexed as
Nicotinic AgonistsReceptors, NicotinicAllosteric RegulationAnimalsHumansOocytesPatch-Clamp TechniquesStereoisomerismXenopus laevisNicotinic Agonistsnicotinic receptor alpha4beta2Receptors, Nicotinicchiral separation and X-ray crystallographycognitive disorderscomputational dockingnicotine addictionnicotinic acetylcholine receptorspositive allosteric modulatorstwo-electrode voltage clamp (TEVC)α4β2 nAChRs
Identifiers
PMID40299711
PMCPMC13093463
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