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

Pub. Date : 2004 Jan

PMID : 14662724






5 Functional Relationships(s)
Download
Sentence
Compound Name
Protein Name
Organism
1 Desensitisation of mast cell beta2-adrenoceptor-mediated responses by salmeterol and formoterol. Salmeterol Xinafoate 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. Salmeterol Xinafoate 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. Salmeterol Xinafoate adrenoceptor beta 2 Homo sapiens
4 Isoprenaline, formoterol and salmeterol (all at 10(-6) m) reduced beta(2)-adrenoceptor density by 13+/-5 (P>0.05), 49+/-13 (P<0.05) and 35+/-17% (P>0.05), respectively. Salmeterol Xinafoate adrenoceptor beta 2 Homo sapiens
5 These data indicate that long-term exposure of mast cells to both salmeterol and formoterol can cause substantial levels of desensitisation to beta(2)-adrenoceptor-mediated responses in mast cells. Salmeterol Xinafoate adrenoceptor beta 2 Homo sapiens