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结缔组织激活。IX. 药物制剂的修饰作用。

Connective tissue activation. IX. Modification by pharmacologic agents.

作者信息

Castor C W

出版信息

Arthritis Rheum. 1975 Sep-Oct;18(5):451-60. doi: 10.1002/art.1780180504.

Abstract

Alpha- and beta-adrenergic blocking agents and imipramine inhibit the increased hyaluronate synthesis that may be induced in human synovial cultures by connective tissue activating peptide (CTAP). Considerations of drug concentration requirements, actions of analogues, and time studies all indicate that the adrenergic blockers do not act in this circumstance as conventional blockers of alpha or beta receptor sites. It is suggested that the membrane-stabilizing properties of these agents may be the important determinant for their limited "antiactivation" effect. Ethacrynic acid, a potent and more complete inhibitor of connective tissue activation, appears to act via a different mechanism.

摘要

α-和β-肾上腺素能阻断剂以及丙咪嗪可抑制结缔组织激活肽(CTAP)诱导的人滑膜培养物中透明质酸合成增加。对药物浓度要求、类似物作用以及时间研究的考量均表明,在这种情况下,肾上腺素能阻断剂并非作为传统的α或β受体位点阻断剂发挥作用。有人提出,这些药物的膜稳定特性可能是其有限的“抗激活”作用的重要决定因素。依他尼酸是一种强效且更完全的结缔组织激活抑制剂,其作用机制似乎不同。

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