Azelastine inhibits stimulated histamine release from human lung tissue in vitro but does not alter cyclic nucleotide content.

Azelastine inhibits stimulated histamine release from human lung tissue in vitro but does not alter cyclic nucleotide content.
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氮卓斯汀在体外抑制人肺组织刺激的组胺释放,但不改变环核苷酸含量。

DOI:
10.1007/bf02022975
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发表时间:
1989
期刊:
Agents and actions
影响因子:
--
通讯作者:
Casale,TB
Casale,TB
中科院分区:
--
文献类型:
--
作者:
Little,MM;Wood,DR;Casale,TB

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为了研究氮卓斯汀在哮喘治疗中可能有效的机制,我们研究了其抑制抗IgE和钙离子载体A23187刺激的人肺组胺释放和改变肺环核苷酸水平的能力。肺组织在氮卓斯汀中预孵育30分钟后,抗IgE和A23187刺激的人体组织中组胺释放均受到显著抑制。在氮卓斯汀浓度≥5 μM时,抗IgE刺激的组胺释放始终受到显著抑制,且呈剂量依赖性(r= 0.71,p <0.05),最大平均抑制率为53± 11%。对于A23187刺激的肺组织,直到我们使用30 μMazelastine时才发现组胺释放的一致抑制,平均值为35± 11%。氮卓斯汀浓度低于30 μ M时的抑制作用可变且不显著。肺组织在100 μMazelastine中孵育未显著改变肺环AMP和环GMP含量。我们的结论是氮卓斯汀抑制体外人肺组织组胺的刺激释放,但不改变环核苷酸的含量。
To investigate the mechanism by which azelastine may be effective therapeutically in asthma, we studied its ability to inhibit anti-IgE- and calcium ionophore A23187-stimulated histamine release from human lung and to alter lung cyclic nucleotide levels. Significant inhibition of histamine release from both anti-IgE- and A23187-stimulated human tissue was aparent after 30 minutes preincubation of the lung tissue in azelastine. Significant inhibition of anti-IgE-stimulated histamine release was consistently seen in azelastine concentrations ≥5 μM, and was dose dependent (r=0.71,p<0.05) with maximal mean inhibition of 53±11%. For A23187-stimulated lung tissue, consistent inhibition of histamine release was not found until we used 30 μMazelastine, mean 35±11%. Inhibition in azelastine concentrations below 30 μMwas variable and not significant. Lung cyclic AMP and cyclic GMP content was not significantly altered by incubation of lung tissue in 100 μMazelastine. We conclude that azelastine inhibits stimulated histamine release from human lung tissuein vitrobut does not alter cyclic nucleotide content.
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