Title : Kinetics of 5-HT2B receptor signaling: profound agonist-dependent effects on signaling onset and duration.

Pub. Date : 2013 Dec

PMID : 24049061






2 Functional Relationships(s)
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1 We evaluated a panel of 5-hydroxytryptamine2B (5-HT2B) receptor agonists in kinetic radioligand binding assays and in transient, calcium flux assays, and inositol phosphate accumulation assays; two functional readouts emanating from Galphaq-mediated activation of phospholipase C. In binding studies, ergot derivatives demonstrated slow receptor association and dissociation rates, resulting in significantly reduced potency in calcium assays relative to inositol phosphate accumulation assays. Calcium 5-hydroxytryptamine receptor 2B Homo sapiens
2 We evaluated a panel of 5-hydroxytryptamine2B (5-HT2B) receptor agonists in kinetic radioligand binding assays and in transient, calcium flux assays, and inositol phosphate accumulation assays; two functional readouts emanating from Galphaq-mediated activation of phospholipase C. In binding studies, ergot derivatives demonstrated slow receptor association and dissociation rates, resulting in significantly reduced potency in calcium assays relative to inositol phosphate accumulation assays. Calcium 5-hydroxytryptamine receptor 2B Homo sapiens