Journal article

Publication year: 2006

Pages: 161-170

Journal: European Journal of Pharmacology

Volume number: 546

Issue number: 1-3

ISSN: 0014-2999

DOI Link: https://doi.org/10.1016/j.ejphar.2006.07.047

Publisher: Elsevier

Abstract: 

The aim of the present study was to investigate the effect of histamine, a product of e.g. mast cells, on short-circuit current (I-sc) across rat distal colon. Histamine concentration-dependently stimulated an increase in I-sc which often was preceded by a transient negative cur-rent. Neither a release of neurotransmitters nor a release of prostaglandins contributed to the histamine response. The histamine-induced increase in I-sc was blocked by the histamine H-1 antagonist, pyrilamine, but was resistant against the histamine H-2 antagonist, cimetidine. Conversely, the histamine H-1 agonist, TMPH (2-(3-trifluoromethylphenyl)histamine), exclusively evoked an increase in I-sc, whereas the histamine H-2 agonist, amthamine, evoked only a decrease in I-sc suggesting that stimulation of different types of histamine receptors is responsible for the two phases of the response evoked by native histamine.

Histamine induces the opening of glibenclamide-sensitive Cl- channels and of charybdotoxin-sensitive K+ channels in the apical membrane as demonstrated by experiments at basolaterally depolarized epithelia. A further action site is the basolateral membrane, because histamine stimulates a charybdotoxin- and tetrapentylammonium-sensitive K+ conductance in this membrane as observed in tissues, in which the apical membrane was permeabilized with an ionophore, nystatin.

The increase in I-sc evoked by histamine was blocked after depletion of intracellular Ca2+ stores with cyclopiazonic acid and after blockade of inositol 1,4,5-trisphosphate ON receptors, suggesting a release of stored Ca2+. This was confirmed by the observation that the histamine H-1 agonist TMPH induced an increase in the fura-2 ratio signal of epithelial cells within isolated colonic crypts. Consequently, the mediator histamine seems to stimulate both histamine H-1 and H-2 receptors, from which the former seems to be prominently involved in the induction of epithelial chloride secretion.

Harvard Citation style: Schultheiss, G., Hennig, B., Schunack, W., Prinz, G. and Diener, M. (2006) Histamine-induced ion secretion across rat distal colon: Involvement of histamine H1 and H2 receptors, European Journal of Pharmacology, 546(1-3), pp. 161-170. https://doi.org/10.1016/j.ejphar.2006.07.047

APA Citation style: Schultheiss, G., Hennig, B., Schunack, W., Prinz, G., & Diener, M. (2006). Histamine-induced ion secretion across rat distal colon: Involvement of histamine H1 and H2 receptors. European Journal of Pharmacology. 546(1-3), 161-170. https://doi.org/10.1016/j.ejphar.2006.07.047