Helmeste D M
Life Sci. 1986 Jul 21;39(3):223-7. doi: 10.1016/0024-3205(86)90534-5.
Mianserin stereoselectively decreases rat cortical S2 binding, the (+)enantiomer having higher potency. This and other data suggest that an alpha-2 receptor is unlikely to contribute to the mechanism of rapid S2 down-regulation by mianserin. Yohimbine, an alpha-2 antagonist which enhances desipramine-induced S2 decreases, was not dependent on NE or 5-HT release for its effect. Depletion of NE by 75% or 5-HT by 94% did not alter the ability of yohimbine and desipramine to decrease binding. These results raise previously unsuspected mechanisms involved in acute down-regulation of S2 binding by mianserin and yohimbine.
米安色林可立体选择性地降低大鼠皮质S2结合，其中（+）对映体具有更高的效力。这一结果以及其他数据表明，α2受体不太可能参与米安色林对S2的快速下调机制。育亨宾是一种α2拮抗剂，可增强地昔帕明诱导的S2降低，其作用不依赖于去甲肾上腺素（NE）或5-羟色胺（5-HT）的释放。NE耗竭75%或5-HT耗竭94%并不改变育亨宾和地昔帕明降低结合的能力。这些结果揭示了米安色林和育亨宾对S2结合急性下调所涉及的前所未有的机制。
