Rupatadine effectively prevents the histamine-induced up regulation of histamine H1R and bradykinin B2R receptor gene expression in the rat paw.

Abstract

BACKGROUND:

Activation of histamine H1 receptor (H1R) is a well-known hallmark of allergic and inflammatory pathology. Both types of bradykinin receptors (B1R and B2R) are also known to contribute significantly to the latter and some sort of functional interaction between them and H1R has been alluded to in the past. Here we use an experimental model of rat paw oedema formation to examine the effect of exogenously added histamine on the gene expression of H1R and bradykinin receptors B1R and B2R, alone or in combination to rupatadine, a second generation antihistamine agent.

METHODS:

Histamine-induced oedema formation was monitored with a plethysmometer. The gene expression of H1R, B1R and B2R was analyzed with both conventional and real-time PCR. Rupatadine fumarate was used in pure form and administered intraperitoneally, prior to histamine injection into the paw. Microscopy of haematoxylin and eosin-stained sections of paw tissue was used to examine effects on tissue architecture.

RESULTS:

Histamine injection into the paw resulted in significant up regulation of H1R and B2R without inducing significant cellular infiltration, but appears to affect less the expression of B1R. Rupatadine was, under the conditions used in this study, very effective in preventing this effect and in suppressing oedema formation through its antihistamine action.

CONCLUSION:

Rupatadine has a suppressing effect on H1R and B2R gene expression which could add to its efficacy towards allergy and allergy-like conditions.

• Authors: Dimitra Molyva, Konstantinos Kalokasidis, Christos Poulios, Hara Dedi, George Karkavelas, Vassiliki Mirtsou, Antonis Goulas
• Journal: Pharmacological reports : PR (Pharmacol Rep) Vol. 66 Issue 6 Pg. 952-5 (Dec 2014) ISSN: 2299-5684 [Electronic] Switzerland
• PMID: 25443720 (Publication Type: Journal Article)
• Copyright: Copyright © 2014 Institute of Pharmacology, Polish Academy of Sciences. Published by Elsevier Urban & Partner Sp. z o.o. All rights reserved.

Chemical References

• Histamine H1 Antagonists
• Receptor, Bradykinin B1
• Receptor, Bradykinin B2
• Receptors, Histamine H1
• rupatadine
• Cyproheptadine
• Histamine

Topics

• Animals
• Cyproheptadine (analogs & derivatives, pharmacology)
• Edema (prevention & control)
• Gene Expression Regulation (drug effects)
• Histamine (metabolism)
• Histamine H1 Antagonists (pharmacology)
• Rats
• Real-Time Polymerase Chain Reaction
• Receptor, Bradykinin B1 (genetics)
• Receptor, Bradykinin B2 (genetics)
• Receptors, Histamine H1 (genetics)
• Up-Regulation (drug effects)