Modulation of IgE-mediated histamine release from human leukocytes by a new class of histamine H2-agonists

Authors:
Publisher website
Google Scholar
Abstract
A new class of phenyl (pyridylalcyl) guanidines, acting as potent histamine H2-agonists, inhibits IgE-mediated human basophil histamine release in a nanomolar range. IC30-level of three substitutes of this group (arpromidine, BUA-75, and FRA-19) were found to be 0.02, 0.015 and 0.008 μM. The inhibition appeared with a fast onset (plateau after 10 min. preincubation) and claimed its maximum (60±2.9%, 63±1.8%, and 61±3.1%,n=7) with 10 μM of the compounds. H2-mediated inhibition was totally blocked by 10 μM famotidine, a potent histamine H2-antagonist. The amount of anti-IgE or antigen for the initiation of the immunological release influenced the strength of inhibition of H2-agonist FRA-19 (p2-receptors exclusively. New, potent H2-receptor stimulating compounds with positive inotropic effects possess additional potent anti-allergic properties.

This publication has 18 references indexed in Scilit: