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Effects of the P2X4 receptor antagonist BR11595 in a guinea pig model of chronic asthma
  • +11
  • Martina Schmidt,
  • Dan Li,
  • Hoeke Baarsma,
  • Melissa Mol-van der Veen,
  • Vicky Verschut,
  • Kimberley Belfor,
  • Tanja de Boer,
  • Harm Maarsingh,
  • Oliver-Martina Fischer,
  • Carolin Ebert,
  • Hana Cernecka,
  • Muriel Lizé,
  • Reinoud Gosens (CLOSED),
  • Loes Kistemaker
Martina Schmidt
Groningen University Faculty of Science and Engineering

Corresponding Author:m.schmidt@rug.nl

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Dan Li
Groningen University Faculty of Science and Engineering
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Hoeke Baarsma
Groningen University Faculty of Science and Engineering
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Melissa Mol-van der Veen
Groningen University Faculty of Science and Engineering
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Vicky Verschut
Aquilo BV, Groningen, Netherlands
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Kimberley Belfor
Aquilo BV, Groningen, Netherlands
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Tanja de Boer
Groningen University Faculty of Science and Engineering
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Harm Maarsingh
Department of Pharmaceutical Sciences, Lloyd L. GrePalm Beach Atlantic University, West Palm Beach, FL, United States
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Oliver-Martina Fischer
Bayer AG, Berlin, Germany
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Carolin Ebert
Bayer AG, Wuppertal, Germany
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Hana Cernecka
Bayer AG, Wuppertal, Germany
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Muriel Lizé
Bayer AG, Wuppertal, Germany
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Reinoud Gosens (CLOSED)
Groningen University Faculty of Science and Engineering
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Loes Kistemaker
Aquilo BV, Groningen, Netherlands
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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.
21 Dec 2024Submitted to British Journal of Pharmacology
23 Dec 2024Submission Checks Completed
23 Dec 2024Assigned to Editor
23 Dec 2024Review(s) Completed, Editorial Evaluation Pending
03 Jan 2025Reviewer(s) Assigned