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自发性高血压大鼠中[3H] DAMGO的中枢结合位点特征

Characteristics of central binding sites for [3H] DAMGO in spontaneously hypertensive rats.

作者信息

Gulati A, Bhargava H N

机构信息

Department of Pharmacodynamics, University of Illinois, Chicago 60612.

出版信息

Life Sci. 1990;47(2):159-66. doi: 10.1016/0024-3205(90)90229-k.

Abstract

The binding of [3H] DAMGO, a highly selective ligand for mu-opiate receptors, to membranes of discrete brain regions and spinal cord of 10 week old spontaneously hypertensive (SHR) and normotensive Wistar-Kyoto (WKY) rats was determined. The brain regions examined were hypothalamus, amygdala, hippocampus, corpus striatum, pons and medulla, midbrain and cortex. [3H] DAMGO bound to membranes of brain regions and spinal cord at a single high affinity site. The receptor density (Bmax value) and apparent dissociation constant (Kd value) of [3H] DAMGO to bind to membranes of hippocampus, corpus striatum, pons and medulla, cortex and spinal cord of WKY and SHR rats did not differ. The Bmax value of [3H] DAMGO in membranes of hypothalamus and midbrain of SHR rats was significantly higher than in WKY rats but the Kd values in the two strains did not differ. On the other hand, the Bmax value of [3H] DAMGO in membranes of amygdala of SHR rats was lower than that of WKY rats but the Kd values in the two strains were similar. It is concluded that SHR rats have higher density of mu-opiate receptors in hypothalamus and midbrain but lower density in amygdala in comparison with WKY rats, and that such differences in the distribution of mu-opiate receptors may be related to the elevated blood pressure in SHR rats.

摘要

测定了[3H] DAMGO(一种对μ-阿片受体具有高度选择性的配体)与10周龄自发性高血压(SHR)大鼠和正常血压的Wistar-Kyoto(WKY)大鼠的离散脑区及脊髓膜的结合情况。所检测的脑区包括下丘脑、杏仁核、海马体、纹状体、脑桥和延髓、中脑及皮层。[3H] DAMGO在脑区及脊髓膜的单一高亲和力位点结合。WKY大鼠和SHR大鼠海马体、纹状体、脑桥和延髓、皮层及脊髓膜上[3H] DAMGO的受体密度(Bmax值)和表观解离常数(Kd值)并无差异。SHR大鼠下丘脑和中脑膜上[3H] DAMGO的Bmax值显著高于WKY大鼠,但两品系的Kd值并无差异。另一方面,SHR大鼠杏仁核膜上[3H] DAMGO的Bmax值低于WKY大鼠,但两品系的Kd值相似。结论是,与WKY大鼠相比,SHR大鼠下丘脑和中脑的μ-阿片受体密度较高,而杏仁核的密度较低,且μ-阿片受体分布的这种差异可能与SHR大鼠的血压升高有关。

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