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Bronchospasmolytic effects of RU 42173
J Fichelle1, E Naline, J L Freslon
1Centre de Recherches Roussel Uclaf, Romainville, France.
Fundamental & Clinical Pharmacology
|January 1, 1988
Summary
RU 42173, a novel beta-adrenergic stimulant, effectively relaxes airways by inhibiting contractions. This bronchodilator demonstrates rapid action and prolonged effects, comparable in potency to salbutamol.
Area of Science:
- Pharmacology
- Respiratory Medicine
- Drug Discovery
Background:
- Beta-adrenergic stimulants are crucial for managing respiratory conditions.
- Developing novel bronchodilators with improved profiles is an ongoing need.
- RU 42173 is a cyclic arylethanolamine analogue with a unique structure.
Purpose of the Study:
- To evaluate the bronchodilator properties of RU 42173.
- To compare RU 42173's efficacy against established bronchodilators like salbutamol and isoprenaline.
- To assess RU 42173's effects on various bronchoconstrictive agents and its duration of action.
Main Methods:
- In vitro studies using isolated guinea pig and human bronchi.
- In vivo studies in guinea pigs administered RU 42173 via intravenous and aerosol routes.
- Assessment of inhibition against histamine, acetylcholine, KCl, methacholine, and platelet-activating factor (PAF) induced bronchospasm.
Main Results:
- RU 42173 demonstrated equipotent inhibition of contractile responses in isolated airways.
- In vivo, RU 42173 dose-dependently inhibited histamine, acetylcholine, and methacholine-induced bronchospasm.
- RU 42173 effectively inhibited PAF-induced bronchoconstriction and hyperreactivity, exhibiting rapid onset and prolonged action.
- The potency of RU 42173 was found to be similar to that of salbutamol.
Conclusions:
- RU 42173 possesses significant bronchodilator properties.
- Its efficacy in vitro and in vivo suggests potential therapeutic value for respiratory diseases.
- RU 42173 offers a promising alternative with comparable potency and favorable pharmacokinetic properties to salbutamol.
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