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  • 标题:Potentiated Modulation of Pregnolone on GABAA Receptors in Behaviorally Stressed Borderline-Hypertensive Rats
  • 本地全文:下载
  • 作者:Hyoung Chul Choi ; Jong-Yeon Kim ; Jong-Bum Lee
  • 期刊名称:Biological and Pharmaceutical Bulletin
  • 印刷版ISSN:0918-6158
  • 电子版ISSN:1347-5215
  • 出版年度:2004
  • 卷号:27
  • 期号:1
  • 页码:122-124
  • DOI:10.1248/bpb.27.122
  • 出版社:The Pharmaceutical Society of Japan
  • 摘要:The modulatory effects of behavioral stress on [3H]flunitrazepam, an agonist for the central-type benzodiazepine receptor binding to the GABAA-benzodiazepine receptor complex, in borderline hypertensive rats (BHR) were examined. In repeatedly immobilized (for 2 weeks, for 2 h/d) BHR, enhancement of [3H]flunitrazepam binding to the receptor was observed to be potentiated. The percent enhancement of [3H]flunitrazepam binding in BHR was higher than that in normotensive control Wistar-Kyoto rats. Pregnanolone, a neuroactive steroid that has been reported to be a putative endogenous modulator in the stress response, concentration dependently enhanced [3H]flunitrazepam binding to the receptor. Enhancement of [3H]flunitrazepam binding was observed to be potentiated by the same immobilized stress, and the EC50 values of pregnanolone in BHR was significantly lower than those in controls and E max values were higher. From the above results, it can be concluded that neural modulation to behavioral stress, especially in GABAergic neurotransmission, is exaggerated in BHR. We propose strain-specific differences of stress reactivity as an important pathogenetic factor in psychosomatic disorders including stress-induced hypertension. This is supported by reports showing exaggerated cardiovascular and symathoadrenal responses to stress in BHR.
  • 关键词:borderline-hypertensive rat;behavioral stress;benzodiazepine receptor;neuroactive steroid
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