Binding characteristics of [3H]-JSM10292: a new cell membrane-permeant non-peptide bradykinin B2 receptor antagonist.

ABSTRACT:

Background and purpose

A (3) H-labelled derivative of the novel small-molecule bradykinin (BK) B(2) receptor antagonist JSM10292 was used to directly study its binding properties to human and animal B(2) receptors in intact cells and to closely define its binding site.

Experimental approach

Equilibrium binding, dissociation and competition studies with various B(2) receptor ligands and [(3) H]-JSM10292 were performed at 4°C and 37°C. The experiments were carried out using HEK293 cells stably (over)expressing wild-type and mutant B(2) receptors of human and animal origin.

Key results

[(3) H]-JSM10292 bound to B(2) receptors at 4°C and at 37°C with the same high affinity. Its dissociation strongly depended on the temperature and increased when unlabelled B(2) receptor a

SUBMITTER: Faussner A 

PROVIDER: S-EPMC3575783 | biostudies-literature | 2012 Oct

REPOSITORIES: biostudies-literature