Bender A S, Hertz L
Department of Pharmacology, University of Saskatchewan, Saskatoon, Canada.
Brain Res. 1987 Dec 8;436(1):189-92. doi: 10.1016/0006-8993(87)91575-7.
Atrial natriuretic peptide (ANP) was found potently (IC50 = 88 nM) to inhibit [3H]diazepam binding to astrocytes in primary cultures but not to a corresponding preparation of neurons. Based upon this finding and literature data demonstrating a pronounced correlation between the distribution of 'peripheral-type' benzodiazepine receptors and ANP receptors, it is suggested that ANP may be an allosteric regulator of the astrocytic benzodiazepine binding site. Since ANP is known to increase the level of cGMP it was also investigated whether 8-bromoguanosine 3':5' cyclic monophosphate, a permeable cGMP analog, displaced diazepam binding. This was the case, suggesting that cGMP might be involved in the ANP effect on the astrocytic benzodiazepine receptor.
心房利钠肽(ANP)被发现能有效(IC50 = 88 nM)抑制原代培养星形胶质细胞中[3H]地西泮的结合,但对相应的神经元制剂则无此作用。基于这一发现以及文献数据表明“外周型”苯二氮䓬受体分布与ANP受体之间存在显著相关性,提示ANP可能是星形胶质细胞苯二氮䓬结合位点的变构调节剂。由于已知ANP可提高cGMP水平,还研究了一种可渗透的cGMP类似物8-溴鸟苷3':5'环一磷酸是否能取代地西泮结合。情况确实如此,这表明cGMP可能参与了ANP对星形胶质细胞苯二氮䓬受体的作用。