盐酸尼立替林（RHC 3432-A）的抗过敏活性。II. 介质释放抑制与环磷酸腺苷水平之间缺乏相关性。
Antiallergic activity of nylidrin hydrochloride (RHC 3432-A). II. A lack of correlation between inhibition of mediator release and levels of cyclic AMP.
作者信息
Coutts S M, Khandwala A, Weinryb I
出版信息
Int Arch Allergy Appl Immunol. 1983;70(4):303-10.
Nylidrin hydrochloride has weak beta-adrenergic agonist properties with rat mast cells, and shows synergy with 3-isobutyl-1-methylxanthine (IBMX) in raising intracellular cAMP in purified mast cells; both of these properties can be blocked by dl-propranolol. However, the action of nylidrin hydrochloride as an inhibitor of histamine secretion from purified rat mast cells is not antagonized by dl-propranolol, nor is it potentiated by IBMX. Nylidrin-induced elevation of cellular cAMP in purified rat mast cells shows no correlation with nylidrin-induced inhibition of histamine release. Thus, nylidrin hydrochloride inhibits release of histamine from mast cells by a novel, non-adrenergic mechanism, which is not dependent on increased levels of cAMP.
盐酸尼立替林对大鼠肥大细胞具有较弱的β-肾上腺素能激动剂特性，并且在纯化的肥大细胞中与3-异丁基-1-甲基黄嘌呤（IBMX）协同作用以提高细胞内cAMP水平；这两种特性均可被dl-普萘洛尔阻断。然而，盐酸尼立替林作为纯化大鼠肥大细胞组胺分泌抑制剂的作用既不被dl-普萘洛尔拮抗，也不被IBMX增强。盐酸尼立替林诱导的纯化大鼠肥大细胞中细胞cAMP升高与盐酸尼立替林诱导的组胺释放抑制无关。因此，盐酸尼立替林通过一种新的、非肾上腺素能机制抑制肥大细胞组胺释放，该机制不依赖于cAMP水平的升高。
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