Label-free versus conventional cellular assays: Functional investigations on the human histamine H1 receptor

Pharmacological profile of the neuropeptide S receptor: Dynamic mass redistribution studies

“…NPS fragments (NPS (2)(3)(4)(5)(6)(7)(8)(9)(10)(11)(12)(13)(14)(15)(16)(17)(18)(19)(20), NPS (3)(4)(5)(6)(7)(8)(9)(10)(11)(12)(13)(14)(15)(16)(17)(18)(19)(20), NPS(1-6), NPS(1-10) 23…”

“…These results are summarized in Table 1. Specifically, NPS (3)(4)(5)(6)(7)(8)(9)(10)(11)(12)(13)(14)(15)(16)(17)(18)(19)(20) and [Bip 2 ]NPS at 10 μmol L −1 , but not at 1 μmol L −1 , elicited a significant DMR response in wild-type cells, thus for these compounds, 1 μmol L −1 was selected as highest concentration for further studies. PWT1-NPS caused a significant DMR effect at 1 and 0.1 μmol L −1 in wild-type cells, thus further experiments in HEK293 mNPSR were performed using 0.01 μmol L −1 as highest concentration for this ligand.…”

“…Several intracellular events can lead to changes in the cells refractive index, that is, protein recruitment, receptor internalization and recycling, second messenger alternation, cytoskeletal remodeling, and cell adhesion changes . DMR has been already applied to study the pharmacological properties of new ligands acting at various GPCRs, such as histamine H 1 , β 2 adrenergic, muscarinic M 3 , purinergic P2Y, formyl peptide, and protease‐activated receptors. Classical opioid and the nociceptin/orphanin FQ peptide (NOP) receptors were also investigated in DMR studies.…”

“…Classical opioid and the nociceptin/orphanin FQ peptide (NOP) receptors were also investigated in DMR studies. Additionally, the DMR assay, together with different biochemical tools, has been successfully used for GPCRs signaling deconvolution studies …”

“…Additionally, the DMR assay, together with different biochemical tools, has been successfully used for GPCRs signaling deconvolution studies. 7,9,21,22 The present study investigates the pharmacological profile and signaling of the murine NPSR expressed in human embryonic kidney 293 (HEK293) cells using the DMR assay. Importantly, this isoform of the receptor and these cells have been chosen based on the fact that all the compounds investigated in the present study have been previously characterized in calcium mobilization studies performed on HEK293 mNPSR cells, thus making possible a direct comparison of the DMR and calcium mobilization results.…”