NCIt definition : A first generation ethanolamine with antiinflammatory, sedative and antihistamine
properties. Doxylamine competitively inhibits the histamine 1 (H1) receptor, thereby
preventing the action of endogenous histamine as well as the subsequent release of
pro-inflammatory mediators from basophils and mast cells. This agent acts as an inverse
agonist that combines with, and stabilizes the inactive form of the H1-receptor, shifting
the H1 receptor equilibrium toward the inactive state. This results in downregulation
of nuclear factor-kappaB (NF-kappaB) and NF-kappaB dependent antigen presentation,
chemotaxis, as well as expression of cell-adhesion molecules and pro-inflammatory
cytokines.;