Terfenadine

  • Chemical Properties
CAS No. 50679-08-8 Cat. No. BCP43974
Name Terfenadine
Synonyms BRN 5857899; BRN5857899; BRN-5857899; Seldane; Terfen;
Formula C32H41NO2 M. Wt 471.67
  • Biological Activity
Description Terfenadine is a prodrug that is metabolized by intestinal CYP3A4 to the active form fexofenadine, a selective histamine H1-receptor antagonist with antihistaminic and non-sedative effects. Terfenadine's active metabolite competitively binds peripheral H1-receptors, thereby stabilizing an inactive conformation of the receptor. Consequently, usual allergic responses as a result of mast-cell degranulation followed by the release of multiple inflammatory mediators, such as interleukins, prostaglandins, and leukotriene precursors, are blocked, thereby preventing the triggering of pro-inflammatory pathways.
Pathways Ion Channel/Membrane Transporter Neuro Signaling Pathway Apoptosis Pathway GPCR/G Protein 
Targets Histamine Receptor Potassium Channel Caspase 

Structure

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