Ontology highlight
ABSTRACT:
SUBMITTER: German N
PROVIDER: S-EPMC3200116 | biostudies-literature | 2011 Oct
REPOSITORIES: biostudies-literature
Journal of medicinal chemistry 20111003 20
Desformylflustrabromine (dFBr; 1), perhaps the first selective positive allosteric modulator of α4β2 neuronal nicotinic acetylcholine (nACh) receptors, was deconstructed to determine which structural features contribute to its actions on receptors expressed in Xenopus ooycytes using two-electrode voltage clamp techniques. Although the intact structure of 1 was found to be optimal, several deconstructed analogs retained activity. Neither the 6-bromo substituent nor the entire 2-position chain i ...[more]