Ontology highlight
ABSTRACT:
SUBMITTER: Jepsen TH
PROVIDER: S-EPMC4094251 | biostudies-literature | 2014 Jul
REPOSITORIES: biostudies-literature
ACS medicinal chemistry letters 20140520 7
Dihydro-β-erythroidine (DHβE) is a member of the Erythrina family of alkaloids and a potent competitive antagonist of the α4β2-subtype of the nicotinic acetylcholine receptors (nAChRs). Guided by an X-ray structure of DHβE in complex with an ACh binding protein, we detail the design, synthesis, and pharmacological characterization of a series of DHβE analogues in which two of the four rings in the natural product has been excluded. We found that the direct analogue of DHβE maintains affinity for ...[more]