Thyagarajan R, Brennan T, Ticku M K
Eur J Pharmacol. 1983 Sep 30;93(3-4):127-36. doi: 10.1016/0014-2999(83)90130-9.
The binding of GABA to its central receptor sites and of benzodiazepines to central and peripheral types of binding sites was compared in age-matched spontaneously hypertensive rat (SHR) and normotensive (WKY) rat. The KD and Bmax values of GABA agonist binding were not significantly different between SHR and WKY rat in the forebrain, cerebellum or pons-medulla. The binding of [3H]flunitrazepam to central types of binding sites was also not different in 12 week-old SHR and WKY rat. However, the binding of [3H]flunitrazepam and [3H]RO5-4864 was significantly lower in the SHR kidney, as compared to WKY rat kidney. This decrease was due to a lower Bmax in SHR kidney. In contrast, the binding of these radioligands in the hearts of the two strains was not different. These results indicate that the SHR has lower peripheral benzodiazepine binding sites in the kidney as compared to age-matched normotensive WKY rat kidney.
在年龄匹配的自发性高血压大鼠(SHR)和正常血压大鼠(WKY)中,比较了γ-氨基丁酸(GABA)与其中枢受体位点的结合以及苯二氮䓬类药物与中枢和外周类型结合位点的结合情况。在SHR和WKY大鼠的前脑、小脑或脑桥-延髓中,GABA激动剂结合的解离常数(KD)和最大结合容量(Bmax)值没有显著差异。在12周龄的SHR和WKY大鼠中,[3H]氟硝西泮与中枢类型结合位点的结合也没有差异。然而,与WKY大鼠肾脏相比,SHR肾脏中[3H]氟硝西泮和[3H]RO5-4864的结合显著降低。这种降低是由于SHR肾脏中Bmax较低。相反,这两种品系大鼠心脏中这些放射性配体的结合没有差异。这些结果表明,与年龄匹配的正常血压WKY大鼠肾脏相比,SHR肾脏中的外周苯二氮䓬结合位点较低。