Thiethylperazine
(Synonyms: 乙巯匹拉嗪) 目录号 : GC64934
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。
Cas No.:1420-55-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
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- Purity: >99.00%
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- SDS (Safety Data Sheet)
- Datasheet
Thiethylperazine, a phenothiazine derivate, is an orally active and potent dopamine D2-receptor and histamine H1-receptor antagonist. Thiethylperazine is also a selective ABCC1activator that reduces amyloid-β (Aβ) load in mice. Thiethylperazine has anti-emetic, antipsychotic and antimicrobial effects[1][2][3].
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].
Thiethylperazine (3 mg/kg; intramuscular injection; twice daily; for 30 days) significantly reduces Aβ42 levels in young 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.
| Cas No. | 1420-55-9 | SDF | Download SDF |
| 别名 | 乙巯匹拉嗪 | ||
| 分子式 | C22H29N3S2 | 分子量 | 399.62 |
| 溶解度 | DMSO : 100 mg/mL (250.24 mM; Need ultrasonic) | 储存条件 | 4°C, protect from light |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5024 mL | 12.5119 mL | 25.0238 mL |
| 5 mM | 0.5005 mL | 2.5024 mL | 5.0048 mL |
| 10 mM | 0.2502 mL | 1.2512 mL | 2.5024 mL |
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2.
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Thiethylperazine and tardive dyskinesia
Acta Neurol Scand 1984 Nov;70(5):369-72.PMID:6507047DOI:10.1111/j.1600-0404.1984.tb00838.x.
Over a 14-month period in the outpatient department of a geriatric hospital, 7 female patients over 75 years of age were identified with tardive dyskinesia associated with the use of Thiethylperazine. The indication for Thiethylperazine treatment had been vertigo or dizziness. 3 of the patients also had symptoms related to cerebral arteriosclerosis and 2 had mild Parkinson's disease without levodopa therapy. None of them were markedly demented nor had chronic psychosis. Tardive dyskinesia appeared after a treatment period of 3 weeks to 6 years. These findings suggest that association of tardive dyskinesia with the use of Thiethylperazine is not uncommon in geriatric outpatients.
The influence of Thiethylperazine on the absorption of effervescent aspirin in migraine
Br J Clin Pharmacol 1976 Dec;3(6):1015-21.PMID:22216523DOI:10.1111/j.1365-2125.1976.tb00351.x.
The absorption of effervescent aspirin was studied in three groups of patients during attacks of migraine. The first group received intramuscular Thiethylperazine 10 min before effervescent aspirin; the second group received intramuscular metoclopramide 10 min before effervescent aspirin; and the third group received effervescent aspirin alone. Where possible each patient was retested when headache-free but under conditions which were otherwise as similar as possible to those during the acute attack. Intramuscular metoclopramide corrected the impairment of drug absorption that occurred during a migraine attack, whereas Thiethylperazine did not. In the group of patients treated with Thiethylperazine and aspirin, the impairment of absorption did not correlate with the duration of the symptoms, nor with the severity of the headache and nausea. Patients treated with Thiethylperazine and aspirin tended to take longer to recover than those patients treated with metoclopramide and aspirin. However, in the Thiethylperazine treated group, the time to recover did not correlate with the salicylate level achieved.
Use of PET Imaging to Assess the Efficacy of Thiethylperazine to Stimulate Cerebral MRP1 Transport Activity in Wild-Type and APP/PS1-21 Mice
Int J Mol Sci 2022 Jun 10;23(12):6514.PMID:35742960DOI:10.3390/ijms23126514.
Multidrug resistance-associated protein 1 (MRP1, encoded by the ABCC1 gene) may contribute to the clearance of amyloid-beta (Aβ) peptides from the brain into the blood and stimulation of MRP1 transport activity may be a therapeutic approach to enhance brain Aβ clearance. In this study, we assessed the effect of Thiethylperazine, an antiemetic drug which was shown to stimulate MRP1 activity in vitro and to decrease Aβ load in a rapid β-amyloidosis mouse model (APP/PS1-21), on MRP1 transport activity by means of positron emission tomography (PET) imaging with the MRP1 tracer 6-bromo-7-[11C]methylpurine. Groups of wild-type, APP/PS1-21 and Abcc1(-/-) mice underwent PET scans before and after a 5-day oral treatment period with Thiethylperazine (15 mg/kg, once daily). The elimination rate constant of radioactivity (kelim) was calculated from time-activity curves in the brain and the lungs as a measure of tissue MRP1 activity. Treatment with Thiethylperazine had no significant effect on MRP1 activity in the brain and the lungs of wild-type and APP/PS1-21 mice. This may either be related to a lack of an MRP1-stimulating effect of Thiethylperazine in vivo or to other factors, such as substrate-dependent MRP1 stimulation, insufficient target tissue exposure to Thiethylperazine or limited sensitivity of the PET tracer to measure MRP1 stimulation.
Case-control study of teratogenic potential of Thiethylperazine, an anti-emetic drug
BJOG 2003 May;110(5):497-9.PMID:12742335DOI:10.1046/j.1471-0528.2003.02230.x.
Objective: Thiethylperazine is a commonly used anti-emetic drug during pregnancy in Hungary. One experimental study in mice and rats found an increased occurrence of cleft palate after the use of Thiethylperazine during pregnancy but the human data of Thiethylperazine have not been reported. Thus, the aim of the study was to investigate the possible human teratogenic effect of Thiethylperazine. Design: Case-control approach. Setting: The teratogenic potential of Thiethylperazine was evaluated in the population-based large data set of the Hungarian Case-Control Surveillance of Congenital Abnormalities between 1980 and 1996. Sample: Of 38,151 newborn infants without any congenital abnormalities (control group), 746 (2.0%) had mothers who were treated with Thiethylperazine, while of 22,843 cases with congenital abnormalities, 411 (1.8%) had mothers who were treated with Thiethylperazine during pregnancy. Methods: Case-control pair analysis. Main outcome measures: Different congenital abnormalities. Results: The pairs of cases with congenital abnormalities and their matched controls without congenital abnormalities were compared and this approach showed a somewhat higher rate of cleft lip +/- palate (OR: 2.0 with 95% CI: 1.0-4.0) in infants born to mothers with Thiethylperazine treatment during the first trimester of pregnancy. Conclusion: Our data do not indicate clear teratogenic effect of Thiethylperazine, however, a weak association was found between Thiethylperazine use and cleft lip +/- palate.
THE EFFECTS OF Thiethylperazine DIMALEATE (TORECAN) ON NAUSEA AND VOMITING
Can Med Assoc J 1965 Feb 20;92(8):422-3.PMID:14261157doi
A double-blind study of Thiethylperazine dimaleate (Torecan) and a placebo, given intramuscularly, was carried out on 40 patients with nausea and/or vomiting due to a variety of causes. No effect on these symptoms was noted in five patients who received the drug and in six who received the placebo. Thiethylperazine dimaleate was judged to have a good effect in 14 patients and the placebo in five patients. The placebo had a slight effect in nine patients and the drug in one.