Fyles J M, Cawthorne M A, Howell S L
Biosci Rep. 1987 Jan;7(1):17-22. doi: 10.1007/BF01122723.
The selective alpha 2 adrenergic antagonist yohimbine has been shown to prevent the noradrenaline induced inhibition of insulin secretion from isolated rat islets of Langerhans. Binding studies utilizing [3H]yohimbine showed specific binding to dispersed rat islet cells with a Kd of 2.9 nM and receptor concentration of 645 fmols/mg protein. The use of chloroquine to inhibit receptor recycling did not affect binding of the ligand. Binding studies and secretion data are consistent with the suggestion that adrenergic receptors of the alpha 2 sub-type may play a dominant role in the regulation of insulin secretion.
选择性α2肾上腺素能拮抗剂育亨宾已被证明可预防去甲肾上腺素诱导的离体大鼠胰岛胰岛素分泌抑制。利用[3H]育亨宾进行的结合研究显示,其与分散的大鼠胰岛细胞存在特异性结合,解离常数(Kd)为2.9 nM,受体浓度为645 fmol/mg蛋白质。使用氯喹抑制受体再循环并不影响配体的结合。结合研究和分泌数据与以下观点一致:α2亚型肾上腺素能受体可能在胰岛素分泌调节中起主导作用。