Anadón A, Martinez-Larrañaga M R
Naunyn Schmiedebergs Arch Pharmacol. 1987 Feb;335(2):200-3. doi: 10.1007/BF00177724.
In plexus containing preparations of the longitudinal muscle of the guinea-pig ileum, an inhibitory action of tetracyclines on twitch-responses to electrical field stimulation was found. Tetracycline, chlortetracycline, minocycline and doxycycline, but not oxytetracycline (0.02 to 1.6 mmol/l) caused a concentration-dependent presynaptic inhibition of acetylcholine release. The inhibitory effect of the tetracyclines was also obtained after ganglion block by hexamethonium (30 mumol/l). The inhibitory effect of the tetracyclines was not antagonized by piperoxan (2 mumol/l) or yohimbine (1 mumol/l) and was partly reduced by the presence of naloxone (1 to 50 nmol/l). After exposing the preparation the peptidase inhibitors, i.e., to the combination of bestatin (10 mumol/l), captopril (10 mumol/l) and thiorphan (0.3 mumol/l), the inhibitory effect of tetracyclines was significantly increased. From these results it would appear that twitch-inhibition caused by tetracycline, chlortetracycline, minocycline and doxycycline is mainly mediated via the release of endogenous opioids from the myenteric plexus.
在豚鼠回肠纵肌含神经丛的标本中，发现四环素类药物对电场刺激引起的抽搐反应有抑制作用。四环素、金霉素、米诺环素和强力霉素（而非土霉素，浓度为0.02至1.6毫摩尔/升）可引起乙酰胆碱释放的浓度依赖性突触前抑制。六甲铵（30微摩尔/升）阻断神经节后，四环素类药物仍有抑制作用。哌罗克生（2微摩尔/升）或育亨宾（1微摩尔/升）不能拮抗四环素类药物的抑制作用，而纳洛酮（1至50纳摩尔/升）可部分减弱其抑制作用。将标本暴露于肽酶抑制剂（即贝司他汀，10微摩尔/升、卡托普利，10微摩尔/升和硫醇苯丙氨酸，0.3微摩尔/升的组合）后，四环素类药物的抑制作用显著增强。从这些结果来看，四环素、金霉素、米诺环素和强力霉素引起的抽搐抑制作用主要是通过肌间神经丛释放内源性阿片类物质介导的。
