Deutsch S I, Mastropaolo J
Psychiatry Service, Department of Veterans Affairs Medical Center, Washington, DC 20422.
Pharmacol Biochem Behav. 1993 Dec;46(4):963-5. doi: 10.1016/0091-3057(93)90229-m.
3-Alpha-5-alpha-tetrahydrodeoxycorticosterone (alloTHDOC) is a 3-alpha ring A-reduced metabolite of deoxycorticosterone that has been shown to act via nongenomic mechanisms to modulate the GABAA receptor complex allosterically in vitro. Moreover, there are behavioral data consistent with the anxiolytic actions of GABA-receptor positive steroids. The drug discrimination paradigm was used in rats to demonstrate that effects of alloTHDOC are mediated by the GABAA receptor complex in the intact animal. In rats trained to discriminate 1.8 mg/kg of midazolam from saline, alloTHDOC substituted for the training stimulus.
3-α-5-α-四氢脱氧皮质酮(别孕四氢脱氧皮质酮,alloTHDOC)是脱氧皮质酮的一种3-α环A还原代谢产物,已证明其在体外通过非基因组机制变构调节GABAA受体复合物。此外,有行为学数据与GABA受体阳性甾体的抗焦虑作用一致。在大鼠中采用药物辨别范式来证明别孕四氢脱氧皮质酮的作用是由完整动物体内的GABAA受体复合物介导的。在经过训练以区分1.8mg/kg咪达唑仑和生理盐水的大鼠中,别孕四氢脱氧皮质酮可替代训练刺激物。