Bradykinin and B₂ receptor antagonism in rat and human articular chondrocytes.

ABSTRACT:

Background and purpose

In osteoarthritis (OA), bradykinin (BK) is known to contribute to pain and synovitis, but not to cartilage degradation. Here, we investigated effects of BK and its antagonists on chondrocytes, cells involved in cartilage homeostasis.

Experimental approach

BK receptor density and affinities of BK, its analogues and antagonists were measured in cultured human and rat chondrocytes by radioligand binding. Effects of BK were assessed by accumulation of inositol phosphates (IP) and release of interleukin (IL)-6 and IL-8.

Key results

Density of [³H]-BK binding sites was higher (13-30-fold) and BK evoked a greater (48-fold) IP production, in human than in rat chondrocytes. The BK B₂ receptor antagonists MEN16132 and icatibant displayed similar binding a

SUBMITTER: Meini S 

PROVIDER: S-EPMC3041251 | biostudies-literature | 2011 Feb

REPOSITORIES: biostudies-literature