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Sulfonium as a Surrogate for Ammonium: A New α7 Nicotinic Acetylcholine Receptor Partial Agonist with Desensitizing Activity.
Quadri, Marta; Stokes, Clare; Gulsevin, Alican; Felts, Ashley C J; Abboud, Khalil A; Papke, Roger L; Horenstein, Nicole A.
Afiliación
  • Quadri M; Department of Chemistry, University of Florida , P.O. Box 117200, Gainesville, Florida 32611-7200, United States.
  • Stokes C; Department of Pharmacology and Therapeutics, University of Florida , P.O. Box 100267, Gainesville, Florida 32610, United States.
  • Gulsevin A; Department of Pharmacology and Therapeutics, University of Florida , P.O. Box 100267, Gainesville, Florida 32610, United States.
  • Felts ACJ; Department of Chemistry, University of Florida , P.O. Box 117200, Gainesville, Florida 32611-7200, United States.
  • Abboud KA; Department of Chemistry, Center of X-Ray Crystallography, University of Florida , P.O. Box 117200, Gainesville, Florida 32611-7200, United States.
  • Papke RL; Department of Chemistry, Center of X-Ray Crystallography, University of Florida , P.O. Box 117200, Gainesville, Florida 32611-7200, United States.
  • Horenstein NA; Department of Pharmacology and Therapeutics, University of Florida , P.O. Box 100267, Gainesville, Florida 32610, United States.
J Med Chem ; 60(18): 7928-7934, 2017 09 28.
Article en En | MEDLINE | ID: mdl-28885019
ABSTRACT
Weak partial agonists that promote a desensitized state of the α7 nicotinic acetylcholine receptor (nAChR) have been associated with anti-inflammatory effects. Exemplar compounds feature a tertiary or quaternary ammonium group. We report the synthesis, structure, and electrophysiological evaluation of 1-ethyl-4-phenylthiomorpholin-1-ium triflate, a weak partial agonist with a sulfonium isostere of the ammonium pharmacophore. These results offer new insights in understanding nAChR-ligand interactions and provide a new chemical space to target the α7 nAChR.
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Texto completo: 1 Bases de datos: MEDLINE Asunto principal: Compuestos Onio / Compuestos de Sulfonio / Morfolinas / Agonistas Nicotínicos / Receptor Nicotínico de Acetilcolina alfa 7 Límite: Animals / Humans Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 2017 Tipo del documento: Article País de afiliación: Estados Unidos
Texto completo
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Texto completo: 1 Bases de datos: MEDLINE Asunto principal: Compuestos Onio / Compuestos de Sulfonio / Morfolinas / Agonistas Nicotínicos / Receptor Nicotínico de Acetilcolina alfa 7 Límite: Animals / Humans Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 2017 Tipo del documento: Article País de afiliación: Estados Unidos