Brown J, Czarnecki A
Physiological Laboratory, Cambridge, United Kingdom.
Am J Physiol. 1990 Apr;258(4 Pt 2):R1078-83. doi: 10.1152/ajpregu.1990.258.4.R1078.
The presence and distribution of atrial natriuretic peptide (ANP) clearance receptors in rat brain were investigated by use of des[Gln18,Ser19,Gly20,Leu21,Gly22]ANP-(4-2 3) (C-ANP), a specific ligand of this receptor, to displace bound alpha-125I-labeled ANP. alpha-125I-ANP (200 pM) bound significantly to arachnoid mater, subfornical organ, choroid plexus, area postrema, median preoptic nucleus, and supraoptic and paraventricular nuclei. Binding was reversible at all sites with unlabeled alpha-ANP. Binding dissociation constants for alpha-ANP were measured for the first three sites and were all in the nanomolar range. C-ANP competed with alpha-125I-ANP only for binding sites on arachnoid mater, 1 microM C-ANP displacing radioligand from at least 60% of these sites. No alpha-125I-ANP was displaced by completely unrelated peptides. The reversible binding of 125I-Tyr0-ANP-(5-25), another relatively selective ligand of the clearance receptor, was also concentrated on arachnoid mater. Therefore, high-affinity binding sites for alpha-ANP on arachnoid mater may be clearance receptors for ANP.
利用心房利钠肽(ANP)清除受体的特异性配体des[Gln18,Ser19,Gly20,Leu21,Gly22]ANP-(4 - 23)(C - ANP)来置换结合的α - 125I标记的ANP,研究大鼠脑中ANP清除受体的存在和分布情况。α - 125I - ANP(200 pM)与蛛网膜、穹窿下器官、脉络丛、最后区、视前正中核以及视上核和室旁核有显著结合。在所有部位,未标记的α - ANP可使结合可逆。测定了前三个部位α - ANP的结合解离常数,均在纳摩尔范围内。C - ANP仅与蛛网膜上的α - 125I - ANP结合位点竞争,1 μM C - ANP可从至少60%的这些位点置换放射性配体。完全不相关的肽不能置换α - 125I - ANP。清除受体的另一种相对选择性配体125I - Tyr0 - ANP-(5 - 25)的可逆结合也集中在蛛网膜上。因此,蛛网膜上α - ANP的高亲和力结合位点可能是ANP的清除受体。