In the proximal tubule, the activation of GLP1-R leads to the onset of the cAMP signaling cascade with phosphorylation of NHE3 (Na + /H + exchanger isotope 3) and reduction of its function
Hematology Am Soc Hematol Educ Program , 2019 (1), 315322
This results in a lower ability to promote receptor internalization compared with endogenous GLP-1, so it allows to have an increased GLP-1R expression on the cell surface, which translates in more robust insulinotropic properties, possibly explaining the enhanced insulin secretion (in both diabetic and not diabetic human islets), induced by TZP (19) by approximately 25% more than the one induced by only one of the two agents
A higher blood level is not the same as a health benefit A trial can demonstrate absorption or a biomarker increase without proving that participants feel better, function better, avoid disease, or live longer
In many cases, the term microdosing is used loosely and may refer to unsupervised or nonstandard dosing practices rather than medically guided titration