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首页> 外文期刊>Pulmonary therapy. >Pharmacological Assessment of the In Vitro Functional Selectivity of Aclidinium Bromide at M3 and M2 Muscarinic Receptors in Human Tissue
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Pharmacological Assessment of the In Vitro Functional Selectivity of Aclidinium Bromide at M3 and M2 Muscarinic Receptors in Human Tissue

机译：人体对组织中M3和M2毒蕈碱受体的溴氰化铵体外功能选择性的药理评估

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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 2 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.
机译：在电刺激的人支气管条中评估了M 3 拮抗剂的活性。测定了aclidinium，噻托铵和异丙托铵的效力，起效和抵消。在电刺激的分离的人左心房中评估了M 2 拮抗剂活性。计算作用时间。 Aclidinium对M 3 受体表现出竞争性拮抗作用，其功效与比较剂相似。 Aclidinium的起效与异丙托铵相似，且比噻托溴铵（P 2 受体快，aclidinium的作用持续时间短于噻托溴铵，但长于异丙托铵，所有拮抗剂在M 2的作用持续时间均较短。 对M 3 受体：Aclidinium对人支气管对心房受体表现出动力学选择性，支持良好的心血管安全性。

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