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一种模拟肾上腺素对α-肾上腺素能受体作用的钙离子载体。

A calcium ionophore simulating the action of epinephrine on the alpha-adrenergic receptor.

作者信息

Selinger Z, Eimerl S, Schramm M

出版信息

Proc Natl Acad Sci U S A. 1974 Jan;71(1):128-31. doi: 10.1073/pnas.71.1.128.

Abstract

Calcium acting through the ionophore A-23187 caused massive K(+) release from rat parotid slices. The ionophore thus simulates the action of epinephrine on the alpha-adrenergic receptor in this system. The alpha-adrenergic and cholinergic receptors are, however, not involved in the action of the ionophore since phetolamine and atropine had no effect on the ionophore-induced K(+) release. Amylase secretion, which is induced by epinephrine through the beta-adrenergic receptor but does not require Ca(++) in the medium, was only slightly increased by the ionophore in the presence of Ca(++). The K(+) released by Ca(++) through the ionophore was regained by the cells upon chelation of Ca(++) with ethylene glycol bis(beta-aminoethyl ether)-N,N'-tetraacetic acid. Similar to the action of epinephrine on the alpha-adrenergic receptor, the K(+) release induced by the ionophore is specific for Ca(++), which cannot be substituted by 2.5 mM Sr(++), Mg(++), or Ba(++). The results suggest that epinephrine, like the ionophore, introduces Ca(++) into the cell to mediate K(+) release. It is proposed that the ionophore A-23187 may be an effective probe to test whether other Ca(++)-requiring hormones and neurotransmitters act in a similar fashion to produce their diverse physiological responses.

摘要

通过离子载体A - 23187起作用的钙会导致大鼠腮腺切片大量释放钾离子。因此,该离子载体模拟了肾上腺素在这个系统中对α - 肾上腺素能受体的作用。然而,α - 肾上腺素能受体和胆碱能受体并不参与离子载体的作用,因为酚妥拉明和阿托品对离子载体诱导的钾离子释放没有影响。淀粉酶分泌是由肾上腺素通过β - 肾上腺素能受体诱导产生的,但在培养基中不需要钙离子,在有钙离子存在的情况下,离子载体只会使其略有增加。当钙离子与乙二醇双(β - 氨基乙醚)- N,N' - 四乙酸螯合时,细胞会重新摄取通过离子载体由钙离子释放的钾离子。与肾上腺素对α - 肾上腺素能受体的作用类似,离子载体诱导的钾离子释放对钙离子具有特异性,2.5 mM的锶离子、镁离子或钡离子不能替代钙离子。结果表明,肾上腺素与离子载体一样,将钙离子引入细胞以介导钾离子释放。有人提出,离子载体A - 23187可能是一种有效的探针,用于测试其他需要钙离子的激素和神经递质是否以类似的方式发挥作用以产生它们多样的生理反应。

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