Gross G, Hante K, Göthert M
Psychopharmacology (Berl). 1987;91(2):175-81. doi: 10.1007/BF00217058.
The effect of antidepressant and neuroleptic drugs on the electrically evoked release of serotonin (5-HT) was investigated in rat brain cortical slices preincubated with 0.1 mumol/l 3H-5-HT. Zimelidine, trazodone, clomipramine, doxepin, and viloxazine (1 mumol/l each) enhanced the electrically-induced 3H overflow by 20-44%. Six other antidepressants and five neuroleptics did not increase the evoked transmitter release. Only trazodone and viloxazine also increased the 3H overflow in experiments in which neuronal 5-HT reuptake was already blocked by 6-nitroquipazine. 5-HT and clonidine inhibited the electrically-induced 3H-5-HT release by stimulation of presynaptic 5-HT autoreceptors and alpha 2-adrenoceptors, respectively; trazodone and viloxazine had no effect on the concentration-response curves of 5-HT and clonidine. Other psychotropic agents with well known antiserotonergic activities also failed to block presynaptic 5-HT autoreceptors. It is concluded that zimelidine, clomipramine, and doxepin enhanced the 3H-5-HT overflow by inhibition of neuronal 5-HT uptake, whereas the increase produced by trazodone and viloxazine cannot be explained by reuptake inhibition or interaction with presynaptic receptors.
在预先用0.1μmol/L 3H-5-羟色胺（5-HT）孵育的大鼠脑皮质切片中，研究了抗抑郁药和抗精神病药对电诱发的5-HT释放的影响。齐美利定、曲唑酮、氯米帕明、多塞平和维洛沙嗪（各1μmol/L）使电诱导的3H溢出增加了20%-44%。其他六种抗抑郁药和五种抗精神病药并未增加诱发的递质释放。在神经元5-HT再摄取已被6-硝基喹哌嗪阻断的实验中，只有曲唑酮和维洛沙嗪也增加了3H溢出。5-HT和可乐定分别通过刺激突触前5-HT自身受体和α2-肾上腺素能受体来抑制电诱导的3H-5-HT释放；曲唑酮和维洛沙嗪对5-HT和可乐定的浓度-反应曲线没有影响。其他具有众所周知的抗5-羟色胺能活性的精神药物也未能阻断突触前5-HT自身受体。得出的结论是，齐美利定、氯米帕明和多塞平通过抑制神经元5-HT摄取来增加3H-5-HT溢出，而曲唑酮和维洛沙嗪产生的增加不能用再摄取抑制或与突触前受体的相互作用来解释。
