title: New class of biphenylene dibenzazocinones as potent ligands for the human EP1 prostanoid receptor.
abstract: A new class of potent and selective ligands for the human EP1 prostanoid receptor is described. SAR studies reported herein allowed the identification of several potent dibenzazocinones bearing an acylsulfonamide side chain. The binding affinity of these compounds on all eight human prostanoid receptors is reported.
authors.affiliation: Merck Frosst Centre for Therapeutic Research, Pointe Claire - Dorval, Québec, Canada.
authors.forename: R
authors.initials: R
authors.lastname: Ruel
authors.forename: P
authors.initials: P
authors.lastname: Lacombe
authors.forename: M
authors.initials: M
authors.lastname: Abramovitz
authors.forename: C
authors.initials: C
authors.lastname: Godbout
authors.forename: S
authors.initials: S
authors.lastname: Lamontagne
authors.forename: C
authors.initials: C
authors.lastname: Rochette
authors.forename: N
authors.initials: N
authors.lastname: Sawyer
authors.forename: R
authors.initials: R
authors.lastname: Stocco
authors.forename: N M
authors.initials: NM
authors.lastname: Tremblay
authors.forename: K M
authors.initials: KM
authors.lastname: Metters
authors.forename: M
authors.initials: M
authors.lastname: Labelle
mesh_terms: D001392:Azocines / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D001713:Biphenyl Compounds / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D006801:Humans; D008024:Ligands; D011485:Protein Binding; D018078:Receptors, Prostaglandin E / Q000187:drug effects* / Q000378:metabolism; D058306:Receptors, Prostaglandin E, EP1 Subtype; D013329:Structure-Activity Relationship
chemical_list: D001392:Azocines; D001713:Biphenyl Compounds; D008024:Ligands; C545635:PTGER1 protein, human; D018078:Receptors, Prostaglandin E; D058306:Receptors, Prostaglandin E, EP1 Subtype