Measuring Tachykinin Receptor Signaling

The tachykinin receptors elicit intracellular signalling responses primarily through coupling to, and the activation of, Gα_q/11 G proteins. The activation of these G proteins results in the generation of inositol phosphates (IPs; inositol trisphospate and its metabolites inositol bisphosphate and inositol monophosphate). Loading of cells with a radiolabelled precursor ([³H]-myo-inositol) ensures that the generated IPs are radiolabelled. These can be isolated using ion exchange chromatography and their radioactivity measured, with the amount of radiolabelled IP generated (i.e., the level of radioactivity measured) being proportional to the signalling activity of the receptor [48 ].

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Suthiram J., Pieters A., Mohamed Moosa Z., Zeevaart J.R., Sathekge M.M., Ebenhan T., Anderson R.C, & Newton C.L. (2023). Tachykinin Receptor-Selectivity of the Potential Glioblastoma-Targeted Therapy, DOTA-[Thi8,Met(O2)11]-Substance P. International Journal of Molecular Sciences, 24(3), 2134.

Publication 2023

Cells G proteins Gαq proteins Inositol phosphates Intracellular Ion exchange chromatography Myo inositol Radioactivity Tachykinin receptors

Corresponding Organization : University of Edinburgh

Other organizations : South African Nuclear Energy Corporation (South Africa), Steve Biko Hospital

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Variable analysis

independent variables

Stimulation of tachykinin receptors

dependent variables

Generation of inositol phosphates (IPs; inositol trisphosphate and its metabolites inositol bisphosphate and inositol monophosphate)
Radioactivity measured from radiolabelled IPs

control variables

Loading of cells with a radiolabelled precursor ([3H]-myo-inositol)

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