Overview
- Straub, I. et al. (2013) Br. J. Pharmacol. 168, 1835.
Centrifuge all products before use (10000 x g 5 min).
Alomone Labs Ononetin activates TRPA1 channels expressed in HEK-293 cells.Dose response curve of the activation of human TRPA1 channels by increasing concentrations of Ononetin (#O-135). Cells were loaded with Calcium 5 dye. Changes in intracellular Ca2+ following Ononetin application were detected as changes in relative fluorescence (RFU). EC50 was determined at 19.7 µM.
- Straub, I. et al. (2013) Br. J. Pharmacol. 168, 1835.
- Held, K. et al. (2015) Temperature 2, 201.
- Klionsky, L. et al. (2007) Mol. Pain 3, 39.
Ononetin is a deoxybenzoin that acts as a potent TRPM3 channel blocker with an IC50 of 0.3 µM and a TRPA1 channel activator between 10-100 µM. The compound binds at an extracellularly accessible binding site of the channel1.
TRPM3, the third member of the melastatin-related TRPM channel subfamily, is a Ca2+-permeable non-selective cation channel expressed highly in the brain, spinal cord, sensory neurons, pituitary, kidney, eye, testis and adipose tissue. TRPM3 acts as a volume-regulated ion channel involved in the modulation of insulin release in pancreatic islets2.
TRPA1, transient receptor potential ankyrin 1, is a non-selective cation channel expressed in the small neurons of the dorsal root and trigeminal ganglia. It plays an important role in models of inflammatory and neuropathic pain and have the ability to detect pungent or irritant compounds3.
Ononetin (#O-135) is a highly pure, synthetic, and biologically active compound.
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