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首页> 外文期刊>Current drug targets. CNS and neurological disorders >The vasopressin V1b receptor as a therapeutic target in stress-related disorders.
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The vasopressin V1b receptor as a therapeutic target in stress-related disorders.

机译：加压素V1b受体可作为应激相关疾病的治疗靶标。

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The complexity of the stress response would appear to provide multiple opportunities for intervention, but treatment strategies are often centered on the improvement of symptoms rather than attempting to "treat" the stress response. However, recent efforts have begun to focus on the development of pharmacological agents that can attenuate the stress response itself, rather than the symptoms associated with stress. Although CRF, which is the main regulator of the stress system, is the focus of current interest, there is an accumulating body of evidence suggesting that the vasopressinergic system may play an equal role in the regulation of the stress response, and that V(1b) receptor antagonists may be of potential therapeutic benefit. The availability of SSR149415, the first selective antagonist for the V(1b) receptor has allowed us to evaluate this hypothesis. SSR149415 is able to attenuate some but not all stress-related behaviors in rodents. While the antidepressant-like activity of the compound was comparable to that of reference antidepressants, the overall profile displayed in anxiety tests was different from that of classical anxiolytics, such as benzodiazepines. The latter were active in a wide range of anxiety models, whereas the V(1b) receptor antagonist showed clear-cut effects only in particularly stressful situations. It is important to note that SSR149415 is devoid of central depressant effects, even at high doses, and does not affect cognitive processes, suggesting a large therapeutic window. Altogether, these findings suggest that V(1b) receptor antagonists might be useful as a treatment for major depression and stress disorders that result from traumatic events.
机译：压力反应的复杂性似乎为干预提供了多种机会，但是治疗策略通常集中在症状的改善上，而不是试图“治疗”压力反应。但是，最近的努力已经开始集中在可以减轻压力反应本身而不是与压力有关的症状的药理剂的开发上。尽管作为应激系统主要调节因子的CRF是当前关注的焦点，但有大量证据表明血管加压素系统可能在应激反应的调节中起着同等作用，并且V（1b受体拮抗剂可能具有潜在的治疗益处。 SSR149415，V（1b）受体的第一个选择性拮抗剂的可用性使我们能够评估这一假设。 SSR149415能够减弱啮齿动物中某些但并非所有与压力有关的行为。尽管该化合物的抗抑郁药样活性与参考抗抑郁药相当，但在焦虑测试中显示的总体特征与经典抗焦虑药（如苯二氮卓）不同。后者在广泛的焦虑模型中很活跃，而V（1b）受体拮抗剂仅在特别紧张的情况下显示出明确的作用。重要的是要注意，即使在高剂量下，SSR149415也没有中枢抑制作用，并且不影响认知过程，这表明治疗窗很大。总而言之，这些发现表明，V（1b）受体拮抗剂可能可用于治疗由创伤事件引起的严重抑郁和压力障碍。

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