title: Synthesis and evaluation of highly potent GABA(A) receptor antagonists based on gabazine (SR-95531).
abstract: A selection of highly potent analogues based on the gabazine structure is described. Their syntheses are carried out in just four steps, and their potencies for antagonism at the GABA(A) receptor were measured. All antagonists showed significantly higher potencies compared to the parent competitive antagonist, gabazine.
authors.affiliation: Department of Chemistry, University College London, 20 Gordon Street, London WC1H 0AJ, United Kingdom.
authors.forename: Favaad
authors.initials: F
authors.lastname: Iqbal
authors.forename: Ryan
authors.initials: R
authors.lastname: Ellwood
authors.forename: Martin
authors.initials: M
authors.lastname: Mortensen
authors.forename: Trevor G
authors.initials: TG
authors.lastname: Smart
authors.forename: James R
authors.initials: JR
authors.lastname: Baker
mesh_terms: D058787:GABA-A Receptor Antagonists / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011724:Pyridazines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D011963:Receptors, GABA-A / Q000737:chemistry* / Q000378:metabolism
chemical_list: D058787:GABA-A Receptor Antagonists; D011724:Pyridazines; D011963:Receptors, GABA-A; C049853:gabazine