The University of Southampton
University of Southampton Institutional Repository

In vitro characterisation of the duration of action of the histamine-1 receptor antagonist azelastine

Slack, Robert J. and Hart, Adam D. (2011) In vitro characterisation of the duration of action of the histamine-1 receptor antagonist azelastine European Journal of Pharmacology, 670, (2-3), pp. 586-592. (doi:10.1016/j.ejphar.2011.09.017). (PMID:21946109).

Record type: Article

Abstract

Azelastine is a selective antagonist at the human histamine-1 receptor and is used clinically in the treatment of allergic rhinitis. In this study we have investigated its duration of action in vitro in an effort to characterise the receptor and tissue components involved. Chinese hamster ovary cell membrane fragments were used to determine the kinetics of azelastine at the H1 receptor in a radioligand binding assay. Further duration of action studies were completed in tissue preparations using guinea-pig trachea and human bronchus. In radioligand binding studies, azelastine reached steady state at the H1 receptor after approximately 41 min and exhibited a significantly slower dissociation rate constant from the receptor than the first generation antihistamine, diphenhydramine. In washout studies completed in guinea-pig and human airway in vitro tissue preparations, azelastine continued to antagonise the effects of histamine at the H1 receptor for at least 18 h post-washout of the antagonist. This outcome was reversed following removal of the epithelium from guinea-pig isolated tracheal strips. These studies indicate there is a tissue component contributing to azelastine's duration of action, in addition to its direct H1 receptor binding, with evidence suggesting a role for the epithelial layer.

Full text not available from this repository.

More information

Published date: 30 November 2011
Keywords: allergic rhinitis, zelastine, duration of action, epithelium, histamine-1 receptor, histamine antagonist
Organisations: Centre for Biological Sciences

Identifiers

Local EPrints ID: 344346
URI: http://eprints.soton.ac.uk/id/eprint/344346
ISSN: 0014-2999
PURE UUID: 03fc4d37-e7a9-4fb7-bf33-c195dcc90f2c

Catalogue record

Date deposited: 18 Oct 2012 10:57
Last modified: 18 Jul 2017 05:17

Export record

Altmetrics

Contributors

Author: Robert J. Slack
Author: Adam D. Hart

University divisions

Download statistics

Downloads from ePrints over the past year. Other digital versions may also be available to download e.g. from the publisher's website.

View more statistics

Atom RSS 1.0 RSS 2.0

Contact ePrints Soton: eprints@soton.ac.uk

ePrints Soton supports OAI 2.0 with a base URL of http://eprints.soton.ac.uk/cgi/oai2

This repository has been built using EPrints software, developed at the University of Southampton, but available to everyone to use.

We use cookies to ensure that we give you the best experience on our website. If you continue without changing your settings, we will assume that you are happy to receive cookies on the University of Southampton website.

×