AMG 9810 (E)-3-(4-t-butylphenyl)- N-(2, 3- dihydrobenzo [b] [1,4] dioxin-6-yl) acrylamide is a potent, non-vanilloid, competitive antagonist of the vanilloid receptor 1 (TRPV1) receptor with IC50 values for human TRPV1 of 24.5 nM; rat TRPV1, 85.6 nM. Additionally, it has been shown to compete with other modes of TRPV1 activation, including protons (IC50s = 92.7 and 294 nM for human and rat, respectively), heat (IC50s = 15.8 and 21 nM for human and rat, respectively), and the endogenous ligands: anandamide, N-arachidonyl dopamine (IC50s = 8.5 and 260 nM for human and rat, respectively), and oleoyldopamine. Furthermore, AMG 9810 blocks capsaicin- induced calcitonin gene-related peptide (CGRP) release and capsaicin-evoked depolarization in rat dorsal root ganglia neurons. Finally AMG 9810 was shown to be a potent and selective antagonist of TRPV1 that can significantly reverse thermal and mechanical hyperalgesia in an animal model of inflammatory pain1.
产品描述
A Blocker of TRPV1 Channel
产品形式
AMG 9810 (E)-3-(4-t-butylphenyl)- N-(2, 3- dihydrobenzo [b] [1,4] dioxin-6-yl) acrylamide is a potent, non-vanilloid, competitive antagonist of the vanilloid receptor 1 (TRPV1) receptor with IC50 values for human TRPV1 of 24.5 nM; rat TRPV1, 85.6 nM. Additionally, it has been shown to compete with other modes of TRPV1 activation, including protons (IC50s = 92.7 and 294 nM for human and rat, respectively), heat (IC50s = 15.8 and 21 nM for human and rat, respectively), and the endogenous ligands: anandamide, N-arachidonyl dopamine (IC50s = 8.5 and 260 nM for human and rat, respectively), and oleoyldopamine. Furthermore, AMG 9810 blocks capsaicin- induced calcitonin gene-related peptide (CGRP) release and capsaicin-evoked depolarization in rat dorsal root ganglia neurons. Finally AMG 9810 was shown to be a potent and selective antagonist of TRPV1 that can significantly reverse thermal and mechanical hyperalgesia in an animal model of inflammatory pain.