Formoterol on airway smooth muscle and human lung mast cells: a comparison with salbutamol and salmeterol.
Formoterol, like salbutamol and salmeterol, relaxed isolated preparations of guinea-pig trachea and human bronchus, and inhibited antigen-induced mediator release from human lung fragments in a concentration-related fashion. In each case, these actions were mediated through beta 2-adrenoceptors, with formoterol being 50-120-fold more potent than salbutamol, and 2-27-fold more potent than salmeterol. The duration of action of formoterol was longer than that of salbutamol in all preparations, but was markedly shorter than that of salmeterol, whose actions persisted for many hours despite continuous or extensive washing of the tissues. In conscious guinea-pigs, inhaled formoterol, salbutamol and salmeterol all caused dose-related inhibition of histamine-induced bronchoconstriction. Formoterol was again more potent (10-20-fold) than either salbutamol or salmeterol. However, while the actions of a threshold-effective dose of formoterol persisted for less than 3 h, somewhat longer than those of salbutamol (< 1.5 h), an equivalent dose of salmeterol was active for at least 6 h. Therefore, while formoterol is a potent beta 2-adrenoceptor agonist in vitro and in vivo, and is consistently longer-acting than salbutamol, its duration of action is markedly shorter than that of salmeterol.
Nials
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Department of Cardiovascular and Respiratory Pharmacology, Glaxo Group Research Ltd., Ware, Hertfordshire, UK.
Ball
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Butchers
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Coleman
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Humbles
A A
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Johnson
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Vardey
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CJ
D000420:Albuterol / Q000031:analogs & derivatives* / Q000493:pharmacokinetics / Q000494:pharmacology*; D000818:Animals; D001980:Bronchi / Q000187:drug effects*; D001993:Bronchodilator Agents / Q000494:pharmacology*; D002478:Cells, Cultured; D015237:Dinoprost / Q000494:pharmacology; D004558:Electric Stimulation; D004983:Ethanolamines / Q000493:pharmacokinetics / Q000494:pharmacology*; D000068759:Formoterol Fumarate; D006168:Guinea Pigs; D006801:Humans; D066298:In Vitro Techniques; D008168:Lung / Q000166:cytology* / Q000187:drug effects*; D008297:Male; D008407:Mast Cells / Q000187:drug effects*; D009126:Muscle Relaxation / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects*; D000068299:Salmeterol Xinafoate; D014132:Trachea / Q000187:drug effects*
D001993:Bronchodilator Agents; D004983:Ethanolamines; D000068299:Salmeterol Xinafoate; D015237:Dinoprost; D000420:Albuterol; D000068759:Formoterol Fumarate