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Up-regulation of μ-opioid receptors in the spinal cord of morphine-tolerant rats

机译:吗啡耐受大鼠脊髓中μ阿片受体的上调

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Though morphine remains the most powerful drug for treating pain, its effectiveness is limited by the development of tolerance and dependence. The mechanism underlying development of tolerance to morphine is still poorly understood. One of the factors could be an alteration in the number of μ-receptors within specific parts of the nervous system. However, reports on changes in the μ-opioid receptor density in the spinal cord after chronic morphine administration are conflicting. Most of the studies have used subcutaneously implanted morphine pellets to produce tolerance. However, it does not simulate clinical conditions, where it is more common to administer morphine at intervals, either by injections or orally. In the present study, rats were made tolerant to morphine by injecting increasing doses of morphine (10-50 mg/kg, subcutaneously) for five days. In vitro tissue autoradiography for localization of μ-receptor in the spinal cord was done using [~3H]-DAMGO. As compared to the spinal cord of control rats, the spinal cord of tolerant rats showed an 18-8% increase or up-regulation in the density of μ-receptors in the superficial layers of the dorsal horn. This up-regulation of μ-receptors after morphine tolerance suggests that a fraction of the receptors have been rendered desensitized, which in turn could lead to tolerance.
机译:尽管吗啡仍然是治疗疼痛最有效的药物,但其耐受性和依赖性的发展限制了它的有效性。对吗啡耐受性发展的潜在机制仍知之甚少。因素之一可能是神经系统特定部位的μ受体数量发生变化。然而,关于长期服用吗啡后脊髓中μ阿片受体密度变化的报道相互矛盾。大多数研究使用皮下植入吗啡药丸来产生耐受性。但是,它不能模拟临床情况,在这种情况下,更常见的是通过注射或口服定期给予吗啡。在本研究中,通过增加剂量的吗啡(10-50 mg / kg,皮下注射)五天使大鼠对吗啡具有耐受性。使用[〜3H] -DAMGO对脊髓中的μ受体进行定位的体外组织放射自显影。与对照大鼠的脊髓相比,耐受性大鼠的脊髓在背角表层的μ受体密度显示出18-8%的增加或上调。吗啡耐受后,μ受体的这种上调表明一部分受体已脱敏,这又可能导致耐受。

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