학술논문
Pharmacological Assessment of the In Vitro Functional Selectivity of Aclidinium Bromide at M and M Muscarinic Receptors in Human Tissue.
Document Type
Article
Author
Source
Subject
*BROMIDES
*IPRATROPIUM (Drug)
*DRUG antagonism
*MUSCARINIC receptors
*CHOLINERGIC receptors
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Language
ISSN
2364-1746
Abstract
M antagonist activity was assessed in electrically stimulated human bronchial strips; potency, onset and offset of action of aclidinium, tiotropium and ipratropium were determined. M antagonist activity was assessed in electrically stimulated isolated human left atria; duration of action was calculated. Aclidinium demonstrated competitive antagonism at M receptors with similar potency to comparators. Onset of action of aclidinium was similar to ipratropium and faster than tiotropium ( P < 0.05); duration of action was similar to tiotropium and longer than ipratropium ( P < 0.05). At M receptors, duration of action of aclidinium was shorter than tiotropium and longer than ipratropium. All antagonists exhibited a shorter duration of action at M versus M receptors. Aclidinium exhibited kinetic selectivity for human bronchial versus atrial receptors, supporting a favorable cardiovascular safety profile. [ABSTRACT FROM AUTHOR]