Tang A H
Life Sci. 1985 Oct 21;37(16):1475-82. doi: 10.1016/0024-3205(85)90178-x.
U-50,488E is a novel analgesic agent with a specific agonist property on the kappa opioid receptor. It is found to protect against the lethal effect of temporary bilateral carotid occlusion (BCO) in Mongolian gerbils and rats of the Fischer strain. Pretreatment with U-50,488E in gerbils before 7 min of BCO reduced the development of behavioral hyperactivity and preserved the hippocampal neurons from ischemic death. This protective effect of U-50,488E resided predominantly in the levo-enantiomer which is also more potent as a kappa analgesic. Two other kappa opioid analgesics, ethylketocyclazocine and bremazocine, shared the effects of U-50,488E in the gerbils. Naloxone and dynorphin 1-13, on the other hand, were without protective effects in the same ischemic model. The ischemic protective effects of U-50,488E may involve the kappa opioid receptor.
U - 50,488E是一种新型镇痛药，对κ阿片受体具有特异性激动剂特性。研究发现，它能保护蒙古沙鼠和Fischer品系大鼠免受短暂双侧颈动脉闭塞（BCO）的致死效应。在BCO 7分钟前用U - 50,488E预处理沙鼠，可减少行为多动的发展，并保护海马神经元免于缺血死亡。U - 50,488E的这种保护作用主要存在于左旋对映体中，该对映体作为κ镇痛药也更有效。另外两种κ阿片类镇痛药，乙基酮环唑新和布马佐辛，在沙鼠中具有与U - 50,488E相同的作用。另一方面，纳洛酮和强啡肽1 - 13在相同的缺血模型中没有保护作用。U - 50,488E的缺血保护作用可能涉及κ阿片受体。
