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火鸡红细胞中β-肾上腺素能受体的亲和标记物。

Affinity label for beta-adrenergic receptor in turkey erythrocytes.

作者信息

Atlas D, Steer M L, Levitzki A

出版信息

Proc Natl Acad Sci U S A. 1976 Jun;73(6):1921-5. doi: 10.1073/pnas.73.6.1921.

DOI:10.1073/pnas.73.6.1921
PMID:180528
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC430419/
Abstract

The compound N-[2-hydroxy-3-(1-naphthoxy)-propyl]-N'-bromoacetylethylenediamine (NHNP-NBE) was found to label covalently the beta-adrenergic receptor in turkey erythrocytes. The compound inhibits irreversibly 1-epinephrine-dependent adenylate cyclase activity [ATP pyrophosphate-lyase (cyclizing), EC 4.6.1.1] in the whole turkey erythrocyte as well as in the erythrocyte membranes possessing the beta-receptor. The affinity label blocks, also irreversibly, the specific [3H] propranolol binding, whereas other bromoacetyl compounds tested have no effect on binding, even at high concentrations, which cause enzyme inactivation. 1-Epinephrine and propranolol offer protection against the affinity label in whole turkey erythrocytes as well as in membranes prepared from these cells. The potential usefulness of an irreversible beta-antagonist is discussed.

摘要

化合物N-[2-羟基-3-(1-萘氧基)-丙基]-N'-溴乙酰乙二胺（NHNP-NBE）被发现可共价标记火鸡红细胞中的β-肾上腺素能受体。该化合物在整个火鸡红细胞以及具有β-受体的红细胞膜中不可逆地抑制1-肾上腺素依赖性腺苷酸环化酶活性[ATP焦磷酸裂解酶（环化），EC 4.6.1.1]。亲和标记也不可逆地阻断特异性[3H]普萘洛尔结合，而测试的其他溴乙酰化合物即使在高浓度下也对结合无影响，高浓度会导致酶失活。1-肾上腺素和普萘洛尔在整个火鸡红细胞以及从这些细胞制备的膜中对亲和标记具有保护作用。讨论了不可逆β拮抗剂的潜在用途。

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Stereospecific binding of propranolol and catecholamines to the beta-adrenergic receptor.普萘洛尔和儿茶酚胺与β-肾上腺素能受体的立体特异性结合。
Proc Natl Acad Sci U S A. 1974 Oct;71(10):4246-8. doi: 10.1073/pnas.71.10.4246.
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Proc Natl Acad Sci U S A. 1974 Jul;71(7):2773-6. doi: 10.1073/pnas.71.7.2773.
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