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Expeditious Synthesis, EnantiomericResolution, andEnantiomer Functional Characterization of (4-(4-Bromophenyl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-8-sulfonamide(4BP-TQS): An Allosteric Agonist-Positive Allosteric Modulator ofα7 Nicotinic Acetylcholine Receptors
- Source :
-
Journal of Medicinal Chemistry . Vol. 56 Issue 21, p8943-8947. 5p. - Publication Year :
- 2013
-
Abstract
- Anexpeditious microwave-assisted synthesis of 4BP-TQS, its enantiomericseparation, and their functional evaluation is reported. Electrophysiologicalcharacterization in Xenopusoocytesrevealed that activity exclusively resided in the (+)-enantiomer 1b(GAT107) and (−)-enantiomer 1adidnot affect its activity when coapplied. X-ray crystallography studiesrevealed the absolute stereochemistry of 1bto be 3aR,4S,9bS. 1brepresents the most potent ago-PAM of α7 nAChRs availableto date and is considered for further in vivo evaluation. [ABSTRACT FROM AUTHOR]
Details
- Language :
- English
- ISSN :
- 00222623
- Volume :
- 56
- Issue :
- 21
- Database :
- Academic Search Index
- Journal :
- Journal of Medicinal Chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 92050764
- Full Text :
- https://doi.org/10.1021/jm401267t