Baran L, Maj J, Rogóz Z, Skuza G
Pol J Pharmacol Pharm. 1979 Jan-Feb;31(1):25-33.
Trazodone, an antidepressant drug with an unknown mechanism of action, has been examined in order to demonstrate its central antiserotonin action. Trazodone antagonizes the head twitch response induced by 5-hydroxytryptophan in rats and mice, or by-5-methoxytryptamine in rats (the ED50 values are 9.3, 5.2, and 10.8 mg/kg respectively). It counteracts convulsions induced by tryptamine in rats (ED50=3.75 mg/kg). Trazodone abolishes hyperthermia induced by serotoninomimetics (LSD, quipazine, fenfluramine) in rabbits. It does not affect ptosis induced by reserpine, and diminishes stimulation of the locomotor activity induced by amphetamine. Our findings demonstrate that trazodone has a central antiserotonin action, similarly as three other antidepressant drugs: mianserin, danitracen and doxepin, whose central antiserotonin action has been found previously.
曲唑酮是一种作用机制不明的抗抑郁药物,为证明其中枢抗血清素作用而进行了研究。曲唑酮可拮抗5-羟色氨酸在大鼠和小鼠中或5-甲氧基色胺在大鼠中诱导的头部抽搐反应(ED50值分别为9.3、5.2和10.8 mg/kg)。它可对抗色胺在大鼠中诱导的惊厥(ED50 = 3.75 mg/kg)。曲唑酮可消除血清素模拟物(LSD、喹哌嗪、芬氟拉明)在兔子中诱导的体温过高。它不影响利血平诱导的眼睑下垂,并减弱安非他明诱导的运动活性刺激。我们的研究结果表明,曲唑酮具有中枢抗血清素作用,与另外三种抗抑郁药物米安色林、达尼曲辛和多塞平类似,它们的中枢抗血清素作用此前已被发现。