Comparative toxicokinetic/toxicodynamic study of rubber antioxidants, 2-mercaptobenzimidazole and its methyl substituted derivatives, by repeated oral administration in rats was written by Sakemi, Kazue;Ito, Rieno;Umemura, Takashi;Ohno, Yasuo;Tsuda, Mitsuhiro. And the article was included in Archives of Toxicology in 2002.HPLC of Formula: 4887-83-6 This article mentions the following:
2-Mercaptobenzimidazole (MBI), a rubber antioxidant, is known to exhibit potent thyroid toxicity in rats, whereas its methylated derivatives are much less toxic. To characterize this methyl-substituent effect on the thyroid toxicity of MBI, comparative toxicokinetic analyses have been conducted in the present study. MBI and the MMBIs [4-methylated MBI (4-MMBI) and 5-methylated MBI (5-MMBI), and a 1:1 mixture of these 4- and 5-methylated isomers (MMBI mix)] suspended in corn oil were repeatedly administered (at 0.3-0.6 mmol/kg) to male Wistar rats by gavage once daily for 2 wk. After the first and last administrations, blood and urine samples were collected, and the levels of unchanged compounds and their desulfurated metabolites were determined by high performance liquid chromatog. After repeated oral administration (roa), the Cmax and area under concentration-time curve (AUC) of MBI were markedly increased, while the MMBIs essentially were cleared from the blood within 10 h. After roa, the Cmax and AUC of 4-MMBI decreased markedly, suggesting metabolic enzyme induction. However, the toxicokinetic parameters of 5-MMBI were not markedly altered by roa. The inhibitory potencies (IC50) against lactoperoxidase of MBI, 4-MMBI, and 5-MMBI were 20.6 μM, 45.6 μM and 31.6 μM, resp. Thus, the authors suggest that the marked decrease of thyroid toxicity by Me substitution of MBI is caused mainly by a decrease in systemic exposure to the compounds and partly by a decrease in inhibition of thyroid hormone synthesis. In the experiment, the researchers used many compounds, for example, 7-Methyl-1H-benzo[d]imidazole (cas: 4887-83-6HPLC of Formula: 4887-83-6).
7-Methyl-1H-benzo[d]imidazole (cas: 4887-83-6) belongs to imidazole derivatives. Imidazole is the basic core of some natural products such as histidine, purine, histamine and DNA based structures, etc. Among the different heterocyclic compounds, imidazole is better known due to its broad range of chemical and biological properties. The pharmacophore of imidazole exists in bioactive compounds including amino acids, plant growth regulators and therapeutic agents.n increase of the alkyl chain length of the alcohols. HPLC of Formula: 4887-83-6
Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem