Ciproxifan, a histamine H₃ receptor antagonist, reversibly inhibits monoamine oxidase A and B.

ABSTRACT: Ciproxifan is a well-investigated histamine H₃ receptor (H3R) inverse agonist/antagonist, showing an exclusively high species-specific affinity at rodent compared to human H3R. It is well studied as reference compound for H3R in rodent models for neurological diseases connected with neurotransmitter dysregulation, e.g. attention deficit hyperactivity disorder or Alzheimer's disease. In a screening for potential monoamine oxidase A and B inhibition ciproxifan showed efficacy on both enzyme isoforms. Further characterization of ciproxifan revealed IC₅₀ values in a micromolar concentration range for human and rat monoamine oxidases with slight preference for monoamine oxidase B in both species. The inhibition by ciproxifan was reversible for both human isoforms. Regardin

SUBMITTER: Hagenow S 

PROVIDER: S-EPMC5233962 | biostudies-literature | 2017 Jan

REPOSITORIES: biostudies-literature