The Sound of Evolution
Trazodone
Mechanism of action:
Trazodone is a serotonin antagonist and reuptake inhibitor. It has marked antagonistic effects on the 5-HT2A and 5-HT2C receptors, blocking serotonin-induced Gq/11 protein-coupled signaling through these receptors. Trazodone also inhibits the serotonin transporter, increasing serotonin concentration in the synaptic cleft and enhancing serotonin activity at serotonin receptors other than 5-HT2A and 5-HT2C.
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.