| Bioactivity | Methapyrilene (Thenylpyramine) hydrochloride is an orally active H1-receptor antihistamine and an anticholinergic agent of the pyridine chemical class. Methapyrilene hydrochloride has hepatotoxicity and can be used as a hepatotoxin that cause periportal hepatic necrosis in vivo[2] |
| Invitro | Methapyrilene hydrochloride (650 μM) results in a down-regulation of TF and up-regulation of FTL, while the level of HMOX1 is not changed. Additionally, the levels of CD44 and SOX9 proteins and the expression of PROM1 (CD133), hepatic stem cell-associated markers are increased[1].Methapyrilene hydrochloride (650 μM) decreases CYP2E1, CYP3A4, NR1l3, ALB, mRNA expression and increases CD133 expression[1]. |
| In Vivo | Methapyrilene hydrochloride (oral gavage; 40 or 80 mg/kg; 5 days per week; 6 weeks) results in changes in the expression of classic hepatotoxicity-related marker genes and iron homeostasis-related genes, especially a prominent, dose-dependent down-regulation of the transferrin (Tf) gene and an up-regulation of the ferritin, light chain (FTL) gene in rats[1].Methapyrilene hydrochloride (oral gavage; 150 mg/kg; 3 days) causes periportal liver necrosis at high dosage. Methapyrilene is sufficient to induce liver necrosis, or a subtoxic dose of 50 mg/kg/day[2]. |
| Name | Methapyrilene hydrochloride |
| CAS | 135-23-9 |
| Formula | C14H20ClN3S |
| Molar Mass | 297.85 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Iryna Kindrat, et al.Effect of methapyrilene hydrochloride on hepatic intracellular iron metabolism in vivo and in vitro. Toxicol Lett. 2017 Nov 5;281:65-73. [2]. Andrew Craig, et al. Systems toxicology: integrated genomic, proteomic and metabonomic analysis of methapyrilene induced hepatotoxicity in the rat. J Proteome Res. 2006 Jul;5(7):1586-601. [3]. Shawkat-Muhialdin Jangi, et al. H1 histamine receptor antagonists induce genotoxic and caspase-2-dependent apoptosis in human melanoma cells. Carcinogenesis. 2006 Sep;27(9):1787-96. |
Methapyrilene hydrochloride
CAS: 135-23-9 F: C14H20ClN3S W: 297.85
Methapyrilene (Thenylpyramine) hydrochloride is an orally active H1-receptor antihistamine and an anticholinergic agent
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