PMC:7796052 / 13955-15331 JSONTXT 2 Projects

Annnotations TAB TSV DIC JSON TextAE

Id Subject Object Predicate Lexical cue
T91 0-4 Sentence denotes 3.2.
T92 5-20 Sentence denotes In Vitro Assays
T93 22-28 Sentence denotes 3.2.1.
T94 29-55 Sentence denotes Ligand Displacement Assays
T95 56-222 Sentence denotes Raloxifene was tested for its ability to displace reference ligands on human recombinant bradykinin B1 or B2 receptors, respectively, expressed in CHO cells at 20 µM.
T96 223-431 Sentence denotes For this purpose, first saturation isotherms were obtained with reference ligands ([3H] des-Arg10-BK (0.35 nM) in the case of B1, and [3H]-bradykinin (0.2 nM) for B2) incubated for 60 min at room temperature.
T97 432-565 Sentence denotes Nonspecific binding was evaluated by adding a reference compound (desArg9[Leu8]-BK at 10 µM in the case of B1 and BK at 1 µM for B2).
T98 566-798 Sentence denotes Antagonism of raloxifene was measured as a percent inhibition of specific binding of [3H]-bradykinin as control, obtained in the presence of raloxifene at 20 µM and using as reference compounds desArg10-KD for B1 and NPC-567 for B2.
T99 800-806 Sentence denotes 3.2.2.
T100 807-833 Sentence denotes Functional Efficacy Assays
T101 834-964 Sentence denotes Measurementent of the efficacy of the compound on the B2 receptor was carried out following the protocol described elsewhere [31].
T102 965-1147 Sentence denotes The method is based on measuring differences in intracellular Ca2+ concentrations produced in diverse conditions on CHO cells expressing recombinant human B2 receptor by fluorometry.
T103 1148-1268 Sentence denotes Agonism was measured through the capacity of the compound to increase Ca2+ concentration compared to BK (EC50 ~ 2.4 pM).
T104 1269-1376 Sentence denotes Antagonism was measured through the capacity to antagonize BK based on the reduction of Ca2+ concentration.