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- Li, H. et al. (2011) Proc. Natl. Acad. Sci. U.S.A. 108, 8497.
- Vriens, J. et al. (2009) Mol. Pharmacol. 75, 1262.
- Caterina, M.J. et al. (1997) Nature 389, 816.
- McNamara, F.N. et al. (2005) Br. J. Pharmacol. 144, 781.
- Alomone Labs Capsaicin induces Ca2+ influx via activation of TRPV1 channels expressed in C6 cells.Cells were loaded with Fluo-3 AM and stimulated with Capsaicin (#C-125). Changes in intracellular Ca2+ were detected via changes in Fluo-3 emission following application. The left panel shows normalized fluorescence before and after application, at 20 seconds, of 0-10 µM Capsaicin (as indicated). The right panel shows normalized fluorescence plotted against Capsaicin concentrations.
- Caterina, M.J. et al. (1997) Nature 389, 816.
- Tominaga, M. et al. (1998) Neuron 21, 531.
- Vriens, J. et al. (2009) Mol. Pharmacol. 75, 1262.
- Li, H. et al. (2011) Proc. Natl. Acad. Sci. U.S.A. 108, 8497.
- Jordt, S.E. and Julius, D. et al. (2002) Cell 108, 421.
- Jung, J. et al. (1999) J. Neurosci. 19, 529.
- McNamara, F.N. et al. (2005) Br. J. Pharmacol. 144, 781.
- Weltzin, M.M. and Schulte, M.K. et al. (2010) J. Pharmacol. 334, 917.
Vanilloid receptor 1 (VR1, TRPV1) is a nonselective cation channel that is activated by heat and acid, as well as vanilloids1,2.
Capsaicin is a TRPV1 agonist, which acts directly on TRPV13. Being small and hydrophobic, capsaicin crosses the plasma membrane readily to reach its intracellular ligand-binding site on TRPV1, leading to channel activation and cation permeation4-6.
Capsaicin acts directly on TRPV11, with half-maximal effective concentration of 711.9 nM in Xenopus oocytes3 and 0.29 µM in HEK293 cells7.
Alomone Labs Capsaicin activates TRPV1 in CHO transfected cells.Cells were transfected with wild type (WT) TRPV1 and different mutant forms of the channel. Voltage-dependence was measured by voltage-step protocol with depolarizing pulses from −120 mV to +160 mV. A. In a Ca2+-free solution, voltage-dependent currents are measured in WT and T406A mutant. B. Application of 3.3 μM Capsaicin (#C-125) induces robust voltage-dependent currents in CHO cells expressing TRPV1. C. Voltage-activated currents one minute after washout of Capsaicin shows an increased dependence of T406D mutant compared to WT and T406A which returned to baseline.Adapted from Jendryke, T. et al. (2016) Sci. Rep. 6, 22007. with permission of NATURE SPRINGER.
Capsaicin (#C-125) is a highly pure, natural, and biologically active compound.
Applications
Citations
- Jendryke, T. et al. (2016) Sci. Rep. 6, 22007.
- Silva, M. et al. (2016) Neuropharmacology 107, 49.
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