Thiethylperazine dimaleate |
| カタログ番号GC64935 |
フェノチアジン誘導体であるチエチルペラジン ジマレエートは、経口活性で強力なドーパミン D2 受容体およびヒスタミン H1 受容体拮抗薬です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1179-69-7
Sample solution is provided at 25 µL, 10mM.
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Thiethylperazine dimaleate, a phenothiazine derivate, is an orally active and potent dopamine D2-receptor and histamine H1-receptor antagonist. Thiethylperazine dimaleate is also a selective ABCC1activator that reduces amyloid-β (Aβ) load in mice. Thiethylperazine dimaleate has anti-emetic, antipsychotic and antimicrobial effects[1][2][3].
Thiethylperazine could 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].
Thiethylperazine (3 mg/kg; intramuscular injection; twice daily; for 30 days; young APP/PS1 mice) treatment significantly reduces Aβ42 levels in APP/PS1 mice[2].
[1]. Czeizel AE, et al. Case-control study of teratogenic potential of thiethylperazine, an anti-emetic drug. BJOG. 2003 May;110(5):497-9.
[2]. Krohn M, et al. Cerebral amyloid-β proteostasis is regulated by the membrane transport protein ABCC1 in mice. J Clin Invest. 2011 Oct;121(10):3924-31.
[3]. Rahbar M, et al. Enhancement of vancomycin activity by phenothiazines against vancomycin-resistant Enterococcus faecium in vitro. Basic Clin Pharmacol Toxicol. 2010 Aug;107(2):676-9.
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