Sawynok J, Dickson C
Prog Neuropsychopharmacol Biol Psychiatry. 1984;8(4-6):729-31. doi: 10.1016/0278-5846(84)90047-2.
Following intrathecal administration into the spinal subarachnoid space, baclofen produced dose related increases in tail flick latency. L-Baclofen was twice as potent as the DL-racemate and 100 times more potent than D-baclofen. When D-baclofen was injected intrathecally 15 min prior to L-baclofen, the subsequent effect of L-baclofen was markedly reduced. This reduction was dose-related for D-baclofen in doses at least 20 times the L-baclofen dose. D-baclofen administered concomitantly with L-baclofen only slightly increased the effect of L-baclofen. Pretreatment with D-baclofen (up to 10 times the dose of L-baclofen) did not inhibit the effect of L-baclofen when drugs were injected intraperitoneally. These results indicate that D-baclofen can antagonize the antinociceptive effect of L-baclofen following intrathecal administration. D-Baclofen should prove to be a useful tool for investigation of the role of stereoselective baclofen receptors in a variety of pharmacological processes.
鞘内注射到脊髓蛛网膜下腔后，巴氯芬使甩尾潜伏期呈剂量依赖性增加。L-巴氯芬的效力是DL-消旋体的两倍，比D-巴氯芬强100倍。当在L-巴氯芬鞘内注射前15分钟鞘内注射D-巴氯芬时，L-巴氯芬随后的作用明显减弱。对于D-巴氯芬，这种减弱与剂量相关，其剂量至少是L-巴氯芬剂量的20倍。与L-巴氯芬同时给药时，D-巴氯芬只会轻微增强L-巴氯芬的作用。当腹腔注射药物时，用D-巴氯芬预处理（剂量高达L-巴氯芬的10倍）并不抑制L-巴氯芬的作用。这些结果表明，鞘内给药后D-巴氯芬可拮抗L-巴氯芬的镇痛作用。D-巴氯芬应被证明是研究立体选择性巴氯芬受体在各种药理过程中作用的有用工具。
