Article

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

Drug Discovery Research, Astellas Pharma Inc, Tsukuba, Ibaraki, Japan. <>
European Journal of Pharmacology (impact factor: 2.52). 06/2008; 589(1-3):98-101. DOI:10.1016/j.ejphar.2008.05.011 pp.98-101
Source: PubMed

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.

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Keywords

acetic acid-
 
bisphosphonates
 
bone metastases
 
bone pain
 
bone resorption
 
bone turnover diseases
 
formalin-induced nociceptive behaviors
 
mice
 
nociceptive transmission
 
third third-generation bisphosphonate