Pharmacological basis for duration of effect: formoterol and salmeterol versus short-acting beta 2-adrenoceptor agonists
(1996) In Lung 174(1). p.1-22- Abstract
- The mechanisms behind the long duration of bronchodilating action of the beta 2-adrenoceptor agonists formoterol and salmeterol are only partially understood. This review compares pharmacological characteristics of long-acting versus short-acting beta 2-adrenoceptor agonists in human and animal airways. Based upon the reviewed evidence, it is concluded that for beta 2-adrenoceptor agonists, long duration of action may depend upon several factors. Both formoterol and salmeterol display a higher lipophilicity and have a higher affinity, selectivity, and potency than most short-acting agonists at the beta 2-adrenoceptor. Of these factors, lipophilicity may prove to be one of the most important ones by determining the amount of drug entering... (More)
- The mechanisms behind the long duration of bronchodilating action of the beta 2-adrenoceptor agonists formoterol and salmeterol are only partially understood. This review compares pharmacological characteristics of long-acting versus short-acting beta 2-adrenoceptor agonists in human and animal airways. Based upon the reviewed evidence, it is concluded that for beta 2-adrenoceptor agonists, long duration of action may depend upon several factors. Both formoterol and salmeterol display a higher lipophilicity and have a higher affinity, selectivity, and potency than most short-acting agonists at the beta 2-adrenoceptor. Of these factors, lipophilicity may prove to be one of the most important ones by determining the amount of drug entering into the cell membrane in the vicinity of the beta 2-adrenoceptor. However, the receptor affinity, maximal relaxant effect (efficacy or intrinsic activity), potency, and receptor selectivity may also be of importance in determining how much beta 2-adrenoceptor agonist must remain at the receptor for sustained action. (Less)
Please use this url to cite or link to this publication:
https://lup.lub.lu.se/record/1110645
- author
- Linden, A ; Rabe, K F and Löfdahl, Claes-Göran LU
- publishing date
- 1996
- type
- Contribution to journal
- publication status
- published
- subject
- keywords
- Airway smooth-muscle relaxation - beta2-adrenoceptor agonists - Bronchodilator - Duration of action - Exosite - Formoterol - Microkinetic diffusion - Salmeterol
- in
- Lung
- volume
- 174
- issue
- 1
- pages
- 1 - 22
- publisher
- Springer
- external identifiers
-
- pmid:8746998
- scopus:0030047987
- ISSN
- 1432-1750
- DOI
- 10.1007/BF00167947
- language
- English
- LU publication?
- no
- id
- 9d7a8214-42d5-4cd9-bb70-1340fad599f0 (old id 1110645)
- date added to LUP
- 2016-04-01 16:59:41
- date last changed
- 2022-01-28 23:33:59
@article{9d7a8214-42d5-4cd9-bb70-1340fad599f0,
abstract = {{The mechanisms behind the long duration of bronchodilating action of the beta 2-adrenoceptor agonists formoterol and salmeterol are only partially understood. This review compares pharmacological characteristics of long-acting versus short-acting beta 2-adrenoceptor agonists in human and animal airways. Based upon the reviewed evidence, it is concluded that for beta 2-adrenoceptor agonists, long duration of action may depend upon several factors. Both formoterol and salmeterol display a higher lipophilicity and have a higher affinity, selectivity, and potency than most short-acting agonists at the beta 2-adrenoceptor. Of these factors, lipophilicity may prove to be one of the most important ones by determining the amount of drug entering into the cell membrane in the vicinity of the beta 2-adrenoceptor. However, the receptor affinity, maximal relaxant effect (efficacy or intrinsic activity), potency, and receptor selectivity may also be of importance in determining how much beta 2-adrenoceptor agonist must remain at the receptor for sustained action.}},
author = {{Linden, A and Rabe, K F and Löfdahl, Claes-Göran}},
issn = {{1432-1750}},
keywords = {{Airway smooth-muscle relaxation - beta2-adrenoceptor agonists - Bronchodilator - Duration of action - Exosite - Formoterol - Microkinetic diffusion - Salmeterol}},
language = {{eng}},
number = {{1}},
pages = {{1--22}},
publisher = {{Springer}},
series = {{Lung}},
title = {{Pharmacological basis for duration of effect: formoterol and salmeterol versus short-acting beta 2-adrenoceptor agonists}},
url = {{http://dx.doi.org/10.1007/BF00167947}},
doi = {{10.1007/BF00167947}},
volume = {{174}},
year = {{1996}},
}