Comparison of antagonist activity of spantide family at human neurokinin receptors measured by aequorin luminescence-based functional calcium assay4401

Last updated on 22-8-2019 by Anonymous (not verified)

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Peer reviewed scientific article

Abstract:

Neurokinin receptors (NK1, NK2, NK3) are G-protein-coupled receptors, which upon activation by a peptide agonist induce a transient increase in the concentration of intracellular calcium. The functional assay based on aequorin-derived luminescence triggered by receptor-mediated changes in Ca2+ levels was used to compare the effect of spantides I-III on SP-, NKA- and NKB-stimulated NK1, NK2 and NK3 receptors, respectively. Recombinant cell lines expressing neurokinin receptors and apoaequorin were used in the study. The obtained results indicate that all three spantides acted as competitive …

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