Kolik L G, Zhukov V N, Seredenin S B
Eksp Klin Farmakol. 2007 Mar-Apr;70(2):8-11.
The antinociceptive and anxiolytic properties of the new drug GB-115 (0.0125-4 mg/kg, i.p.), which is a short peptide antagonist of CCK2-receptors, have been studied in rats and mice using thermal models of nociception and the standard "elevated plus-maze" (EPM) test for measuring anxiety. It s established that GB-115 (4 mg/kg) significantly increases the response latency in naloxone-independent manner in the "hot plate" test in mice and produced a moderate naloxone-reversible analgesic effect in the "tail flick" test in mice. The blocking of opioid receptors by naloxone does not influence the anxiolytic effects of GB-115 (0.025 and 4 mg/kg) in the EPM test on rats. It has been suggested that GB-115 produced anxiolytic acting on CCK2-receptors, and its role in the control of pain perception is manifested through the interaction with opioidergic mechanisms on a spinal level rather than with non-opioid mechanisms on a supraspinal level.
新型药物GB - 115（0.0125 - 4毫克/千克，腹腔注射）是一种CCK2受体的短肽拮抗剂，其抗伤害感受和抗焦虑特性已在大鼠和小鼠中使用伤害感受的热模型以及测量焦虑的标准“高架十字迷宫”（EPM）试验进行了研究。已确定GB - 115（4毫克/千克）在小鼠的“热板”试验中以不依赖纳洛酮的方式显著增加反应潜伏期，并在小鼠的“甩尾”试验中产生中度纳洛酮可逆的镇痛作用。纳洛酮对阿片受体的阻断并不影响GB - 115（0.025和4毫克/千克）在大鼠EPM试验中的抗焦虑作用。有人提出，GB - 115通过作用于CCK2受体产生抗焦虑作用，其在疼痛感知控制中的作用是通过在脊髓水平与阿片能机制相互作用而非在脊髓上水平与非阿片机制相互作用来体现的。
