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白细胞儿茶酚胺受体的特异性研究。

Specificity studies of leukocytic catecholamine receptors.

作者信息

Sokol W N, Beall G N, Kruger S R

出版信息

Int J Clin Pharmacol Biopharm. 1978 Apr;16(4):173-6.

PMID:206516
Abstract

Using tritium-labeled dl(+/-)epinephrine, we have extended previous studies demonstrating binding of epinephrine to human leukocytes. We have now further assessed the biological significance of this catecholamine binding by comparing the specificity of binding by human leukocytes with the ability of these compounds to inhibit epinephrine-stimulated adenyl cyclase. Binding is specific for catechols, but does not distinguish between physiologically active and inactive stereo isomers, nor between alpha- and beta-adrenergic agonists. Although 2.5 X 10(-4) M 1(-)DOPA, dopamine, d(+)epinephrine and serotonin failed to stimulate leukocytic adenyl cyclase and prevented adenyl cyclase stimulation by 2.5 X 10(-4) M 1(-)epinephrine, the inhibition of adenyl cyclase by d(+)epinephrine is noncompetitive. This catechol-binding site is clearly not the beta-adrenergic receptor. Its physiological significance, if any, remains to be elucidated.

摘要

利用氚标记的dl(+/-)肾上腺素,我们扩展了先前的研究,这些研究证明了肾上腺素与人白细胞的结合。我们现在通过比较人白细胞结合的特异性与这些化合物抑制肾上腺素刺激的腺苷酸环化酶的能力,进一步评估了这种儿茶酚胺结合的生物学意义。结合对儿茶酚具有特异性,但不能区分生理活性和非活性立体异构体,也不能区分α-和β-肾上腺素能激动剂。尽管2.5×10(-4)M的L(-)多巴、多巴胺、D(+)肾上腺素和血清素未能刺激白细胞腺苷酸环化酶,且能阻止2.5×10(-4)M的L(-)肾上腺素对腺苷酸环化酶的刺激,但D(+)肾上腺素对腺苷酸环化酶的抑制是非竞争性的。这个儿茶酚结合位点显然不是β-肾上腺素能受体。其生理意义(如果有的话)仍有待阐明。

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