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首页> 外文期刊>CNS drug reviews >Bremazocine: A kappa-Opioid Agonist with Potent Analgesic and Other Pharmacologic Properties.
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Bremazocine: A kappa-Opioid Agonist with Potent Analgesic and Other Pharmacologic Properties.

机译：Bremazocine：一种具有有效止痛和其他药理作用的kappa阿片类激动剂。

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Bremazocine is a kappa-opioid receptor agonist with potent analgesic and diuretic activities. As an analgesic it is three- to four-times more potent than morphine, as determined in both hot plate and tail flick tests. Bremazocine and other benzomorphan analogs were synthesized in an effort to produce opiates with greater kappa-opioid receptor selectivity and with minimal morphine-like side effects. Unlike morphine bremazocine is devoid of physical and psychological dependence liability in animal models and produces little or no respiratory depression. While bremazocine does not produce the characteristic euphoria associated with morphine and its abuse, it has been shown to induce dysphoria, a property that limits its clinical usefulness. Similarly to morphine, repeated administration of bremazocine leads to tolerance to its analgesic effect. It has been demonstrated that the marked diuretic effect of bremazocine is mediated primarily by the central nervous system. Because of its psychotomimetic side effects (disturbance in the perception of space and time, abnormal visual experience, disturbance in body image perception, de-personalization, de-realization and loss of self control) bremazocine has limited potential as a clinical analgesic. However, its possible utility for the therapy of alcohol and drug addiction warrants further consideration because of its ability to decrease ethanol and cocaine self-administration in non-human primates. In addition, the ability of bremazocine-like drugs to lower intraocular pressure and to minimize ischemic damage in animal models suggests their possible use in the therapy of glaucoma and cardiovascular disease.
机译：Bremazocine是一种具有有效止痛和利尿作用的κ阿片受体激动剂。作为镇痛药，如在热板试验和甩尾试验中所确定的那样，其效力是吗啡的三至四倍。为了产生具有更高κ-阿片受体选择性并且具有最小吗啡样副作用的鸦片，合成了布雷马索星和其他苯并吗啡类似物。与吗啡不同，在动物模型中，bremazocine没有生理和心理依赖性，并且几乎不产生呼吸抑制。尽管布雷马西星不产生与吗啡及其滥用有关的特征性欣快感，但已证明会诱发烦躁不安，这是限制其临床实用性的一种特性。与吗啡相似，反复给予溴咪唑嗪会导致其镇痛作用耐受。已经证明，溴咪唑嗪的显着利尿作用主要由中枢神经系统介导。由于其拟精神病的副作用（对空间和时间的感知产生干扰，异常的视觉体验，对身体图像感知的干扰，去人格化，去实现和失去自我控制），溴咪唑嗪作为临床止痛药的潜力有限。然而，由于其在非人灵长类动物中减少乙醇和可卡因自我给药的能力，因此其在酒精和药物成瘾治疗中的潜在用途值得进一步考虑。此外，在动物模型中，类溴唑嗪样药物具有降低眼内压并使缺血性损害最小化的能力，表明它们可能用于治疗青光眼和心血管疾病。

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