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Quetiapine

喹硫平

Mechanism of action:

Quetiapine 是一種二苯并噻氮平類(dibenzothiazepine)衍生物。Quetiapine 對 5-HT₂A 受體 的拮抗作用強於對多巴胺 D₂ 受體的阻斷。正常情況下,5-HT₂A 受體被活化時,會透過 Gq/11 蛋白偶聯活化磷脂酶 Cβ(phospholipase Cβ),提升 IP₃/DAG,使細胞質鈣離子上升與活化蛋白激酶 C(protein kinase C),導致皮質錐體神經元興奮性上升 。而當 quetiapine 抑制 5-HT₂A 受體後,會使其興奮性下降。多巴胺 D₂ 受體在活化時,會透過 Gi/o 蛋白偶聯抑制腺苷酸環化酶(adenylyl cyclase),使 cAMP 減少,讓神經元放電下降。但 quetiapine會拮抗多巴胺 D₂ 受體,可抑制中腦邊緣通路(mesolimbic pathway)中過度的多巴胺訊號傳導,減少精神異常的產生。

​Reference(s):

1. Dev V et al. (2000). Quetiapine: a review of its safety in the management of schizophrenia. Drug Saf. 


2. Mukaddes NM et al. (2003). Quetiapine treatment of children and adolescents with Tourette's disorder. J Child Adolesc Psychopharmacol. 


3. Tallerico T et al. (2001). Schizophrenia: elevated mRNA for dopamine D2(Longer) receptors in frontal cortex. Brain Res Mol Brain Res.

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