4-Phenyl-4H-pyrans as IK(Ca) channel blockers

Bioorg Med Chem Lett. 2003 Aug 18;13(16):2637-9. doi: 10.1016/s0960-894x(03)00560-2.

Abstract

4-Phenyl-4H-pyrans have been identified as potent and specific IK(Ca) channel blockers. Their synthesis and structure-activity relationships are described. A selected derivative, rac-11, reduces the infarct volume in a rat subdural hematoma model of traumatic brain injury after iv administration.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Blood Pressure
  • Brain / metabolism
  • Brain / pathology
  • Brain Infarction / drug therapy
  • Brain Injuries / drug therapy
  • Disease Models, Animal
  • Dose-Response Relationship, Drug
  • Heart Rate
  • Hematoma, Subdural / drug therapy
  • Hematoma, Subdural / pathology
  • Intermediate-Conductance Calcium-Activated Potassium Channels
  • Nifedipine / analogs & derivatives
  • Nifedipine / pharmacology
  • Potassium Channel Blockers / administration & dosage
  • Potassium Channel Blockers / chemical synthesis*
  • Potassium Channel Blockers / pharmacology
  • Potassium Channels / drug effects*
  • Potassium Channels / metabolism
  • Pyrans / administration & dosage
  • Pyrans / chemical synthesis*
  • Pyrans / pharmacology
  • Rats
  • Structure-Activity Relationship
  • Time Factors

Substances

  • Intermediate-Conductance Calcium-Activated Potassium Channels
  • Kcnn4 protein, rat
  • Potassium Channel Blockers
  • Potassium Channels
  • Pyrans
  • Nifedipine