Literature DB >> 15603962

IKCa-channel blockers. Part 2: discovery of cyclohexadienes.

Klaus Urbahns1, Siegfried Goldmann, Jochen Krüger, Ervin Horváth, Joachim Schuhmacher, Rolf Grosser, Volker Hinz, Frank Mauler.   

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.

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Year:  2005        PMID： 15603962     DOI： 10.1016/j.bmcl.2004.10.063

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  10 in total

Review 1.  K+ channel modulators for the treatment of neurological disorders and autoimmune diseases.

Authors:  Heike Wulff; Boris S Zhorov
Journal:  Chem Rev       Date:  2008-05       Impact factor: 60.622

2.  Therapeutic potential of KCa3.1 blockers: recent advances and promising trends.

Authors:  Heike Wulff; Neil A Castle
Journal:  Expert Rev Clin Pharmacol       Date:  2010-05       Impact factor: 5.045

3.  NS6180, a new K(Ca) 3.1 channel inhibitor prevents T-cell activation and inflammation in a rat model of inflammatory bowel disease.

Authors:  D Strøbæk; D T Brown; D P Jenkins; Y-J Chen; N Coleman; Y Ando; P Chiu; S Jørgensen; J Demnitz; H Wulff; P Christophersen
Journal:  Br J Pharmacol       Date:  2013-01       Impact factor: 8.739

4.  Structural Insights into the Atomistic Mechanisms of Action of Small Molecule Inhibitors Targeting the KCa3.1 Channel Pore.

Authors:  Hai M Nguyen; Vikrant Singh; Brandon Pressly; David Paul Jenkins; Heike Wulff; Vladimir Yarov-Yarovoy
Journal:  Mol Pharmacol       Date:  2017-01-26       Impact factor: 4.436

Review 5.  Trafficking of intermediate (KCa3.1) and small (KCa2.x) conductance, Ca(2+)-activated K(+) channels: a novel target for medicinal chemistry efforts?

Authors:  Corina M Balut; Kirk L Hamilton; Daniel C Devor
Journal:  ChemMedChem       Date:  2012-08-07       Impact factor: 3.466

6.  Expression and Role of the Intermediate-Conductance Calcium-Activated Potassium Channel KCa3.1 in Glioblastoma.

Authors:  Luigi Catacuzzeno; Bernard Fioretti; Fabio Franciolini
Journal:  J Signal Transduct       Date:  2012-05-17

Review 7.  Pose Classification Using Three-Dimensional Atomic Structure-Based Neural Networks Applied to Ion Channel-Ligand Docking.

Authors:  Heesung Shim; Hyojin Kim; Jonathan E Allen; Heike Wulff
Journal:  J Chem Inf Model       Date:  2022-04-21       Impact factor: 6.162

8.  Identification of KCa3.1 Channel as a Novel Regulator of Oxidative Phosphorylation in a Subset of Pancreatic Carcinoma Cell Lines.

Authors:  Ilya Kovalenko; Andrea Glasauer; Laura Schöckel; Daniel R P Sauter; Alexander Ehrmann; Florian Sohler; Andrea Hägebarth; Ivana Novak; Sven Christian
Journal:  PLoS One       Date:  2016-08-05       Impact factor: 3.240

Review 9.  Functional Roles of the Ca2+-activated K+ Channel, KCa3.1, in Brain Tumors.

Authors:  Giuseppina D'Alessandro; Cristina Limatola; Myriam Catalano
Journal:  Curr Neuropharmacol       Date:  2018       Impact factor: 7.363

10.  KCa3.1 Channel Modulators as Potential Therapeutic Compounds for Glioblastoma.

Authors:  Brandon M Brown; Brandon Pressley; Heike Wulff
Journal:  Curr Neuropharmacol       Date:  2018       Impact factor: 7.363
  10 in total

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