Amenta F, Ricci A
Sezione di Anatomia Umana, Università di Camerino, Italy.
Clin Exp Hypertens. 1995 May;17(4):669-88. doi: 10.3109/10641969509037415.
The pharmacological profile and the anatomical localization of dopamine D2-like receptors were studied in sections of the rat adrenal gland using combined radioligand binding and autoradiographic techniques with [3H]-spiroperidol as a ligand. [3H]-Spiroperidol was bound to sections of the rat adrenal gland in a manner consistent with the labelling of dopamine D2-like receptor sites. The binding was time-, temperature- and concentration-dependent and of high affinity with a dissociation constant (Kd) value of 1.6 +/- 0.04 nM and a maximum density of binding sites (Bmax) of 60 +/- 3.6 fmol/mg tissue. Experiments on the pharmacological specificity of [3H]-spiroperidol binding to sections of the rat adrenal gland suggest the labelling of dopamine D3 and/or D4 receptors. The presence of dopamine D3 and D4 receptors in the rat adrenal gland was confirmed by the demonstration of a specific binding for the D3 radioligand [3H]-7-hydroxy-N,N-di-n-propyl-2-aminotetralin (DPAT) and for the D4 radioligand [3H]-clozapine. Light microscope autoradiography showed the highest accumulation of silver grains which correspond to [3H]-spiroperidol binding sites in the rat adrenal medulla. In the adrenal cortex, where density of silver grains is about 40% lower than in the medulla, the radioligand is accumulated primarily in the zona glomerulosa and to a lesser extent in the zona reticularis. These findings suggest that dopamine D2-like receptor sites in the rat adrenal gland cortex are primarily involved in the modulation of catecholamine secretion from the medulla and of aldosterone secretion from the cortex. The possible relevance of the occurrence of dopamine D3 and D4 receptor subtypes in the adrenal gland is discussed.
利用联合放射性配体结合和放射自显影技术,以[3H]-螺哌啶醇作为配体,在大鼠肾上腺切片中研究了多巴胺D2样受体的药理学特征和解剖定位。[3H]-螺哌啶醇与大鼠肾上腺切片的结合方式与多巴胺D2样受体位点的标记一致。这种结合具有时间、温度和浓度依赖性,且亲和力高,解离常数(Kd)值为1.6±0.04 nM,结合位点的最大密度(Bmax)为60±3.6 fmol/mg组织。关于[·3H]-螺哌啶醇与大鼠肾上腺切片结合的药理学特异性实验表明标记的是多巴胺D3和/或D4受体。通过证明D3放射性配体[3H]-7-羟基-N,N-二正丙基-2-氨基四氢萘(DPAT)和D4放射性配体[3H]-氯氮平的特异性结合,证实了大鼠肾上腺中存在多巴胺D3和D4受体。光学显微镜放射自显影显示,大鼠肾上腺髓质中与[3H]-螺哌啶醇结合位点相对应的银颗粒积累最多。在肾上腺皮质中——银颗粒密度比髓质低约40%——放射性配体主要积聚在球状带,在网状带的积聚程度较小。这些发现表明,大鼠肾上腺皮质中的多巴胺D2样受体位点主要参与调节髓质儿茶酚胺分泌和皮质醛固酮分泌。文中讨论了肾上腺中多巴胺D3和D4受体亚型出现的可能相关性。