Vandewalle B, Revillion F, Lefebvre J
Laboratoire d'Endocrinologie Expérimentale, Centre Oscar Lambret, Lille, France.
J Cancer Res Clin Oncol. 1990;116(3):303-6. doi: 10.1007/BF01612908.
Using L-[3H]dihydroalprenolol [( 3H]DHA), a potent beta-adrenergic antagonist, we demonstrated in breast cancer cells the presence of beta-adrenergic receptors with high affinity (Kd 1-9 nM) as shown by Scatchard analyses. Natural and synthetic agonists inhibited the [3H]DHA binding in the following order of potency: L-isoproterenol = L epinephrine much much greater L-norepinephrine, identical to the well-established order of potency for these compounds in producing beta-adrenergic responses. We verified that these compounds actually stimulated cAMP production in breast cancer cells. At the present time, the pathophysiological significance of beta-adrenergic receptors remains unclear. In view of the importance of cAMP in lactose production and in tumor growth mechanisms, it seems to be important to characterize the beta-adrenergic receptors in breast cancer cells in more detail and study their possible involvement in breast tumor growth.
使用强效β-肾上腺素能拮抗剂L-[3H]二氢阿普洛尔[(3H]DHA),我们通过Scatchard分析证明,乳腺癌细胞中存在高亲和力(Kd 1-9 nM)的β-肾上腺素能受体。天然和合成激动剂抑制[3H]DHA结合的效力顺序如下:L-异丙肾上腺素 = L-肾上腺素 >> L-去甲肾上腺素,这与这些化合物产生β-肾上腺素能反应时公认的效力顺序相同。我们证实这些化合物实际上刺激了乳腺癌细胞中cAMP的产生。目前,β-肾上腺素能受体的病理生理意义仍不清楚。鉴于cAMP在乳糖产生和肿瘤生长机制中的重要性,更详细地表征乳腺癌细胞中的β-肾上腺素能受体并研究它们可能参与乳腺肿瘤生长似乎很重要。