Thiethylperazine 是一种吩噻嗪衍生物,是一种口服有效的多巴胺D2受体和组胺H1受体拮抗剂。Thiethylperazine 也是一种选择性的ABCC1激活剂,可减少小鼠中的淀粉样 β (Aβ) 负荷。Thiethylperazine 具有止吐,抗精神病和抗菌作用。
产品描述
Thiethylperazine, a phenothiazine derivate, is an orally active and potent dopamine D2-receptor and histamine H1-receptor antagonist. Thiethylperazine is also a selective ABCC1 activator that reduces amyloid-β (Aβ) load in mice. Thiethylperazine has anti-emetic, antipsychotic and antimicrobial effects [1] [2] [3].
体外活性
Thiethylperazine can enhance the antibiotic (Vancomycin) activity at a concentration as low as 2 μg/mL. Thiethylperazine inhibits Vancomycin-sensitive E. faecalis ATCC 29212, Vancomycin-resistant E. faecalis ATCC 51299 and vancomycin-resistant E. faecalis (VREF) isolates with MIC values of 8 μg/mL, 16 μg/mL and 8 μg/mL, respectively [3].
体内活性
Thiethylperazine (3 mg/kg; intramuscular injection; twice daily; for 30 days) significantly reduces Aβ42 levels in young APP/PS1 mice [2]. Animal Model: Young Aβ precursor protein (APPswe) and mutant presenilin-1 (PS1) ( APP/PS1 ) mice [2] Dosage: 3 mg/kg Administration: Intramuscular injection; twice daily; for 30 days Result: Significantly reduced Aβ42 levels in APP/PS1 mice.
Cas No.
1420-55-9
分子式
C22H29N3S2
分子量
399.62
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years