Kolik L G, Kadnikov I A, Zhukov V N, Gudasheva T A, Seredenin S B
Eksp Klin Farmakol. 2011;74(10):7-11.
The effects of GB-115 dipeptide, a retroanalog of endogenous CCK-4, on the behavioral indices in "elevated plus maze" (EPM) test and on the content of biogenic amines in the brain structures after discontinuation of a chronic administration of benzodiazepine (BZ) derivatives phenazepam (2.0 mg/kg, i.p.) and diazepam (4.0 mg/kg, i.p.) have been studied in outbred and inbred MR/MNRA rats. It is established that, in 24-48 h following BZ withdrawal, GB-115 dipeptide administered in doses of 0.1 and 0.5 mg/kg, i.p., produced an anxiolytic effect in all animals, which was manifested by increasing the stay time and number of entries in EPM. In the striatum of outbred rats, GB-115 increased DOPAC (+25%) and DA (+31.6%) levels that were decreased during diazepam withdrawal syndrome. The obtained results showed the GB-115 efficiency in attenuating the anxiety caused by BZ withdrawal.
在远交系和近交系MR/MNRA大鼠中,研究了内源性CCK-4的反向类似物GB-115二肽对“高架十字迷宫”(EPM)试验中行为指标以及在长期给予苯二氮䓬(BZ)衍生物非那西泮(2.0毫克/千克,腹腔注射)和地西泮(4.0毫克/千克,腹腔注射)停药后脑结构中生物胺含量的影响。结果表明,在BZ撤药后的24至48小时内,腹腔注射剂量为0.1和0.5毫克/千克的GB-115二肽对所有动物均产生抗焦虑作用,表现为在EPM中的停留时间增加和进入次数增多。在远交系大鼠的纹状体中,GB-115使在安定戒断综合征期间降低的DOPAC(增加25%)和DA(增加31.6%)水平升高。所得结果表明GB-115在减轻BZ撤药引起的焦虑方面具有有效性。