Assay-Dependent Inverse Agonism at the A₃ Adenosine Receptor: When Neutral Is Not Neutral.

ABSTRACT: The A₃ adenosine receptor (A₃AR) is implicated in a variety of (patho)physiological conditions. While most research has focused on agonists and antagonists, inverse agonism at A₃AR has been scarcely studied. Therefore, this study aimed at exploring inverse agonism, using two previously engineered cell lines (hA₃ARLgBiT-SmBiTβarr2 and hA₃ARLgBiT-SmBiTminiGα_i), both employing the NanoBiT technology. The previously established inverse agonist PSB-10 showed a decrease in basal signal in the β-arrestin 2 (βarr2) but not the miniGα_i recruitment assay, indicative of inverse agonism in the former assay. Control experiments confirmed the specificity and reversibility of this observation. Evaluation of a set of presumed neu

SUBMITTER: Pottie E 

PROVIDER: S-EPMC10496142 | biostudies-literature | 2023 Sep

REPOSITORIES: biostudies-literature