title: IKCa-channel blockers. Part 2: discovery of cyclohexadienes.
abstract: Novel cyclohexadienes have been identified as potent and specific IK(Ca)-channel blockers. In this communication we describe their synthesis as well as their chemical and biological properties. A selected derivative is being enriched in rat brain and reduces the infarct volume, intracranial pressure as well as the water content in a rat subdural hematoma model of traumatic brain injury after iv administration.
authors.affiliation: Institute of Medicinal Chemistry, Pharma Research Center, Bayer Health Care, D-42096 Wuppertal, FRG. klaus.urbahns@astrazeneca.com
authors.forename: Klaus
authors.initials: K
authors.lastname: Urbahns
authors.forename: Siegfried
authors.initials: S
authors.lastname: Goldmann
authors.forename: Jochen
authors.initials: J
authors.lastname: Krüger
authors.forename: Ervin
authors.initials: E
authors.lastname: Horváth
authors.forename: Joachim
authors.initials: J
authors.lastname: Schuhmacher
authors.forename: Rolf
authors.initials: R
authors.lastname: Grosser
authors.forename: Volker
authors.initials: V
authors.lastname: Hinz
authors.forename: Frank
authors.initials: F
authors.lastname: Mauler
mesh_terms: D000818:Animals; D001834:Body Water / Q000187:drug effects* / Q000378:metabolism; D020520:Brain Infarction / Q000188:drug therapy; D001930:Brain Injuries / Q000188:drug therapy; D003510:Cyclohexanes / Q000138:chemical synthesis / Q000494:pharmacology*; D053138:Cyclohexenes; D004195:Disease Models, Animal; D006408:Hematoma, Subdural / Q000188:drug therapy; D051660:Intermediate-Conductance Calcium-Activated Potassium Channels; D007427:Intracranial Pressure / Q000187:drug effects*; D026902:Potassium Channel Blockers / Q000138:chemical synthesis / Q000494:pharmacology*; D015221:Potassium Channels / Q000378:metabolism*; D051381:Rats; D013329:Structure-Activity Relationship
chemical_list: D003510:Cyclohexanes; D053138:Cyclohexenes; D051660:Intermediate-Conductance Calcium-Activated Potassium Channels; C491575:Kcnn4 protein, rat; D026902:Potassium Channel Blockers; D015221:Potassium Channels; C048401:1,4-cyclohexadiene