Title : Desensitisation of mast cell beta2-adrenoceptor-mediated responses by salmeterol and formoterol.

Pub. Date : 2004 Jan

PMID : 14662724






3 Functional Relationships(s)
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1 The long-acting beta(2)-adrenoceptor agonist formoterol (10(-10)-10(-6) m) inhibited the IgE-dependent release of histamine from human lung mast cells in a concentration-dependent manner. Histamine adrenoceptor beta 2 Homo sapiens
2 By contrast, the long-acting beta(2)-adrenoceptor agonist salmeterol (10(-10)-10(-6) m) was about two-thirds less efficacious than either formoterol or isoprenaline as an inhibitor of histamine release. Histamine adrenoceptor beta 2 Homo sapiens
3 The desensitisation induced by long-term treatments with salmeterol and formoterol was specific for beta(2)-adrenoceptor-mediated inhibition of histamine release as the inhibitory effects of alternative cAMP-elevating compounds, prostaglandin E(2), a receptor-mediated activator of adenylate cyclase, and forskolin, a direct activator of adenylate cyclase, were unaffected by desensitising treatments. Histamine adrenoceptor beta 2 Homo sapiens