Computed Properties of C8H8FN. Aromatic heterocyclic compounds can also be classified according to the number of heteroatoms contained in the heterocycle: single heteroatom, two heteroatoms, three heteroatoms and four heteroatoms. Compound: 5-Fluoroindoline, is researched, Molecular C8H8FN, CAS is 2343-22-8, about Design, synthesis and biological evaluation of novel 2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole triazole derivatives as potent TRPV1 antagonists. Author is Li, Jinyu; Nie, Cunbin; Qiao, Yue; Hu, Jing; Li, Qifei; Wang, Qiang; Pu, Xiaohui; Yan, Lin; Qian, Hai.
The design, synthesis, and pharmacol. evaluation of a class of TRPV1 antagonists constructed on 2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole as A-region and triazole as B-region I (R = 2-Cl 2,5-Me2, 2-NO2-4-Cl, etc.) have been reported. The SAR anal. indicated that 2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole analogs I displayed excellent antagonism of hTRPV1 activation by capsaicin and showed better potency compared to the corresponding dihydroindole analogs. Optimization of this design led to the eventual identification of compound I (R = 2-CF3), a potent TRPV1 antagonist. In vitro, using cells expressing recombinant human TRPV1 channels, I (R = 2-CF3) displayed potent antagonism activated by capsaicin (IC 50 = 0.075 μM) and only partially blocked acid activation of TRPV1. In vivo, I (R = 2-CF3) exhibited good efficacy in capsaicin-induced and heat-induced pain models and had almost no hyperthermia side-effect. Furthermore, pharmacokinetic studies revealed that compound I (R = 2-CF3) had a superior oral exposure after oral administration in rats. To understand its binding interactions with the receptor, the docking study of I (R = 2-CF3) was performed in rTRPV1 model and showed an excellent fit to the binding site. On the basis of its superior profiles, I (R = 2-CF3) could be considered as the lead candidate for the further development of antinociceptive drugs.
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