Exosites: their current status, and their relevance to the duration of action of long-acting beta 2-adrenoceptor agonists.

Article Details

Citation

Coleman RA, Johnson M, Nials AT, Vardey CJ

Exosites: their current status, and their relevance to the duration of action of long-acting beta 2-adrenoceptor agonists.

Trends Pharmacol Sci. 1996 Sep;17(9):324-30.

PubMed ID
8885698 [ View in PubMed
]
Abstract

The four beta 2-adrenoceptor agonists, clenbuterol, bambuterol, formoterol and salmeterol, are all long-acting bronchodilators, that have distinct mechanisms for their extended durations of action. Various theories have been put forward in an attempt to explain these mechanisms. In this respect, there is strong evidence for the existence of specific additional binding sites (exosites) for salmeterol and related compounds, and that exosites exist on non-ligand recognition regions of the beta 2-adrenoceptor protein. Here, Robert Coleman and colleagues compare and contrast the profiles of action of these long-acting beta 2-adrenoceptor agonists, particularly as they relate to the role of exosites.

DrugBank Data that Cites this Article

Drug Targets
DrugTargetKindOrganismPharmacological ActionActions
BambuterolBeta-2 adrenergic receptorProteinHumans
Yes
Agonist
Details
ClenbuterolBeta-2 adrenergic receptorProteinHumans
Yes
Agonist
Details
FormoterolBeta-2 adrenergic receptorProteinHumans
Yes
Agonist
Details
SalmeterolBeta-2 adrenergic receptorProteinHumans
Yes
Agonist
Details