Effects of the P2X4 receptor antagonist BR11595 in a guinea pig model of
chronic asthma
Abstract
Background and Purpose: Asthma is characterized by airway
hyperresponsiveness (AHR), allergic inflammation, and airway remodeling.
Although recent studies showed that asthma pathophysiology involves P2X
purinoceptor 4 (P2X4) activation, a potential link with chronic asthma
remains to be explored. We investigated the effect of a novel P2X4
receptor antagonist BR11595 on allergen-induced airway responses in a
guinea pig model of chronic asthma. Experimental Approach: Sensitized
guinea pigs were exposed to saline or ovalbumin (OVA) once weekly via
aerosolization for 12 weeks. BR11595 (10 mg·kg⁻¹) was injected
intraperitoneally 5 times per week, for 4 different regimens: all 12
weeks, first 6 weeks, last 6 weeks, or last week only. Airway
responsiveness to histamine was assessed 24h before and 6h after OVA
exposure in week 1, 6 and 12. Lung tissue Inflammation and remodeling
were determined 24h after the last OVA exposure. Key Results: OVA
induced AHR at week 1, 6 and 12 compared to saline-challenged animals.
The AHR was less pronounced in week 12 compared to week 1. BR11595
significantly reduced OVA-induced AHR in week 6 in guinea pigs treated
with BR11595 for 6 weeks. AHR in week 12 was reduced after BR11595
treatment in week 12 only, next to OVA-induced eosinophilia and Goblet
cell hyperplasia, indicating an acute role of P2X4 receptors on chronic
inflammation. Conclusion and Implications: The P2X4-receptor antagonist
BR11595 acutely inhibits AHR, eosinophilia, and Goblet cell hyperplasia
after 12 weeks, indicating its potential as a therapeutic target for
acute intervention of chronic asthma attacks or exacerbations.