Referenced in: none

Automatically associated channels: Kir2.3

Title: Minodronic acid, a third-generation bisphosphonate, antagonizes purinergic P2X(2/3) receptor function and exerts an analgesic effect in pain models.

Authors: Shuichiro Kakimoto, Yukinori Nagakura, Seiji Tamura, Tomonari Watabiki, Kumiko Shibasaki, Shohei Tanaka, Masamichi Mori, Masao Sasamata, Masamichi Okada

Journal, date & volume: Eur. J. Pharmacol., 2008 Jul 28 , 589, 98-101

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/18565509

Abstract
The P2X(2/3) receptor has an important role in the nociceptive transmission. Minodronic acid is a third third-generation bisphosphonate and a potent inhibitor of bone resorption. We found that minodronic acid inhibited alpha,beta-methylene ATP-induced cation uptake with the potency higher than that of suramin in the P2X(2/3) receptor receptor-expressing cells. Other bisphosphonates did not show such activity. Subcutaneously administered (10-50 mg/kg) minodronic acid significantly inhibited the alpha,beta-methylene ATP-, acetic acid- and formalin-induced nociceptive behaviors in mice. These unique effects of minodronic acid would be beneficial for the treatment of accelerated bone turnover diseases accompanied by bone pain, including bone metastases.