《Identification and optimization of 2-aminobenzimidazole derivatives as novel inhibitors of TRPC4 and TRPC5 channels》 was published in British Journal of Pharmacology in 2015. These research results belong to Zhu, Yingmin; Lu, Yungang; Qu, Chunrong; Miller, Melissa; Tian, Jinbin; Thakur, Dhananjay P.; Zhu, Jinmei; Deng, Zixin; Hu, Xianming; Wu, Meng; McManus, Owen B.; Li, Min; Hong, Xuechuan; Zhu, Michael X.; Luo, Huai-Rong. COA of Formula: C10H12N2O The article mentions the following:
Background and Purpose : Transient receptor potential canonical (TRPC) channels play important roles in a broad array of physiol. functions and are involved in various diseases. However, due to a lack of potent subtype-specific inhibitors the exact roles of TRPC channels in physiol. and pathophysiol. conditions have not been elucidated. Exptl. Approach : Using fluorescence membrane potential and Ca2+ assays and electrophysiol. recordings, we characterized new 2-aminobenzimidazole-based small mol. inhibitors of TRPC4 and TRPC5 channels identified from cell-based fluorescence high-throughput screening. Key Results : The original compound, M084, was a potent inhibitor of both TRPC4 and TRPC5, but was also a weak inhibitor of TRPC3. Structural modifications of the lead compound resulted in the identification of analogs with improved potency and selectivity for TRPC4 and TRPC5 channels. The aminobenzimidazole derivatives rapidly inhibited the TRPC4- and TRPC5-mediated currents when applied from the extracellular side and this inhibition was independent of the mode of activation of these channels. The compounds effectively blocked the plateau potential mediated by TRPC4-containing channels in mouse lateral septal neurons, but did not affect the activity of heterologously expressed TRPA1, TRPM8, TRPV1 or TRPV3 channels or that of the native voltage-gated Na+, K+ and Ca2+ channels in dissociated neurons. Conclusions and Implications : The TRPC4/C5-selective inhibitors developed here represent novel and useful pharmaceutical tools for investigation of physiol. and pathophysiol. functions of TRPC4/C5 channels.3-(1H-Benzo[d]imidazol-2-yl)propan-1-ol(cas: 2403-66-9COA of Formula: C10H12N2O) was used in this study.
3-(1H-Benzo[d]imidazol-2-yl)propan-1-ol(cas: 2403-66-9) belongs to imidazoles.Imidazole rings are part of unnatural cyclic peptides and are used as ester isosteres in peptidomimetic studies.
COA of Formula: C10H12N2O However, the application of imidazoles is not limited to the field of peptides and peptidomimetics.
Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem