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The dual PDE3/PDE4 phosphodiesterase inhibitor RPL554 produces more complete bronchodilator responses than the beta2-agonist salbutamol and the anti-muscarinic agent ipratropium bromide, alone and in combination, in guinea-pig isolated trachea

Radhakrishnan Venkatasamy, Clive Page, Domenico Spina
European Respiratory Journal 2015 46: PA3960; DOI: 10.1183/13993003.congress-2015.PA3960
Radhakrishnan Venkatasamy
Sackler Institute of Pulmonary Pharmacology, King's College London, London, United Kingdom
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Clive Page
Sackler Institute of Pulmonary Pharmacology, King's College London, London, United Kingdom
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Domenico Spina
Sackler Institute of Pulmonary Pharmacology, King's College London, London, United Kingdom
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Abstract

Introduction: RPL554 causes clinically effective bronchodilation in asthma and COPD (Franciosi, L.G et al. Lancet Respir Med 2013; 1:714-727) by relaxation of human airway smooth muscle (Calzetta, L et al. J Pharmacol Exp Ther 2013; 346:414-423).

Aims: To investigate whether RPL554 provides additional functional antagonism to relaxant agonists against bronchomotor tone induced by different spasmogens.

Methods: Bronchomotor tone in guinea-pig isolated trachea was elicited by carbachol/histamine (10 µM each) in the absence or presence of LTC4 (100 nM) or K+ ions (40 mM) and carbachol (10 µM) followed by relaxation to ipratropium bromide (IB), salbutamol (SALB) alone, in combination (1:5.7, respectively, and referred to as Combivent); glycopyrrolate (GLY); and RPL554. Maximal relaxation (% Emax papaverine) expressed as mean±sem (N=3-6 animals).

Results: In tissues contracted with carbachol/histamine, only IB failed to fully reverse bronchomotor tone (75±5 %). In tissues contracted with LTC4/histamine/carbachol the response to these agents differed (IB, 69±9; SALB, 72±6; 'combivent', 95±3, GLY, 62±4, and RPL554, 97±1). Tissues contracted with potassium ions & carbachol were more resistant to these agents (IB, 73±6; SALB, 48±8; Combivent, 82±4, RPL554, 90±5). RPL554 provided additional relaxation when bronchodilator drugs did not achieve maximum relaxation in this preparation.

Conclusion . RPL554 has the clinical potential to produce additional bronchodilation over and above that of standard bronchodilators in highly constricted airways.

  • Pharmacology
  • Airway smooth muscle
  • Bronchodilators
  • Copyright ©ERS 2015
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The dual PDE3/PDE4 phosphodiesterase inhibitor RPL554 produces more complete bronchodilator responses than the beta2-agonist salbutamol and the anti-muscarinic agent ipratropium bromide, alone and in combination, in guinea-pig isolated trachea
Radhakrishnan Venkatasamy, Clive Page, Domenico Spina
European Respiratory Journal Sep 2015, 46 (suppl 59) PA3960; DOI: 10.1183/13993003.congress-2015.PA3960

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The dual PDE3/PDE4 phosphodiesterase inhibitor RPL554 produces more complete bronchodilator responses than the beta2-agonist salbutamol and the anti-muscarinic agent ipratropium bromide, alone and in combination, in guinea-pig isolated trachea
Radhakrishnan Venkatasamy, Clive Page, Domenico Spina
European Respiratory Journal Sep 2015, 46 (suppl 59) PA3960; DOI: 10.1183/13993003.congress-2015.PA3960
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More in this TOC Section

  • RPL554, an inhaled PDE3/4 inhibitor, causes comparable bronchodilation to high dose nebulised salbutamol in asthmatics with fewer systemic effects
  • TRPM3: A regulator of airway sensory nerves and respiratory reflexes
  • Anti-inflammatory activity of the bradykinin B1R antagonist in a model of LPS-induced lung inflammation in cynomolgus monkey
Show more 5.1 Airway Pharmacology and Treatment

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