Pharmacological Assessment of the In Vitro Functional Selectivity of Aclidinium Bromide at M3 and M2 Muscarinic Receptors in Human Tissue
Tóm tắt
M3 antagonist activity was assessed in electrically stimulated human bronchial strips; potency, onset and offset of action of aclidinium, tiotropium and ipratropium were determined. M2 antagonist activity was assessed in electrically stimulated isolated human left atria; duration of action was calculated. Aclidinium demonstrated competitive antagonism at M3 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 M2 receptors, duration of action of aclidinium was shorter than tiotropium and longer than ipratropium. All antagonists exhibited a shorter duration of action at M2 versus M3 receptors. Aclidinium exhibited kinetic selectivity for human bronchial versus atrial receptors, supporting a favorable cardiovascular safety profile.
Tài liệu tham khảo
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