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Trazodone

曲唑酮
Mechanism of action:
Trazodone 是一種血清素拮抗與再回收抑制劑(serotonin antagonist and reuptake inhibitor)。Trazodone 對 5-HT₂A 與 5-HT₂C 受體具有明顯拮抗作用,阻止血清素對這些受體促發 Gq/11 蛋白偶聯傳遞。Trazodone 亦可抑制血清素轉運蛋白(serotonin transporter),使突觸間隙血清素濃度上升,增強血清素對除了 5-HT₂A/5-HT₂C 受體以外的其他血清素受體的作用。
Reference(s):
1. Marek GJ et al. (1992). A comparison of trazodone and fluoxetine: implications for a serotonergic mechanism of antidepressant action. Psychopharmacology (Berl).
2. Jauch R et al. (1976). [Pharmacokinetics and metabolism of trazodone in man (author's transl)]. Arzneimittelforschung.
3. Rotzinger S et al. (1998). Trazodone is metabolized to m-chlorophenylpiperazine by CYP3A4 from human sources. Drug Metab Dispos.
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