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. |