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Thiethylperazine 

Cat. No. M28383
Thiethylperazine  Structure
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Biological Activity

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.

Chemical Information
Molecular Weight 399.62
Formula C22H29N3S2
CAS Number 1420-55-9
Form Solid
Solubility (25°C) DMSO 100 mg/mL (ultrasonic)
Storage 4°C, protect from light
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Michael Wölfl-Duchek, et al. Int J Mol Sci. Use of PET Imaging to Assess the Efficacy of Thiethylperazine to Stimulate Cerebral MRP1 Transport Activity in Wild-Type and APP/PS1-21 Mice

[2] No authors listed. Thiethylperazine

[3] A E Czeizel, et al. BJOG. Case-control study of teratogenic potential of thiethylperazine, an anti-emetic drug

[4] R Sulkava. Acta Neurol Scand. Thiethylperazine and tardive dyskinesia

[5] B Larkman. Can J Psychiatr Nurs. Thiethylperazine--Torecan

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