| Bioactivity | Ononetin, a natural deoxybenzoin, is a potent and selective TRPM3 channel blocker with an IC50 of 0.3 μM[1]. | ||||||||||||
| Invitro | Ononetin (1-10 μM) completely and reversibly abrogates Ca2+ entry and ionic currents through recombinantly expressed TRPM3α2 and block the pregnenolone sulphate-inducible Ca2+ entry in primary cultures of mouse or rat dorsal root ganglia (DRG) neurones, indicating biological activity towards endogenously expressed TRPM3[1].Oxidative intermediates of Ononetin may be involved in activating TRPA1, but not in the block of TRPM3 by Ononetin[1]. | ||||||||||||
| In Vivo | Ononetin (10 mg/kg, i.p.) treatment completely reverses established Freund's Complete Adjuvant (FCA)-induced heat hypersensitivity, demonstrating that the loss of hypersensitivity in Trpm3-/- mice is unlikely to be caused by developmental or compensatory mechanisms and suggests that TRPM3 may be a tractable target for inflammatory pain[2]. | ||||||||||||
| Name | Ononetin | ||||||||||||
| CAS | 487-49-0 | ||||||||||||
| Formula | C15H14O4 | ||||||||||||
| Molar Mass | 258.27 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. I Straub, et al. Citrus fruit and fabacea secondary metabolites potently and selectively block TRPM3. Br J Pharmacol. 2013 Apr;168(8):1835-50. [2]. Omar Alkhatib, et al. Promiscuous G-Protein-Coupled Receptor Inhibition of Transient Receptor Potential Melastatin 3 Ion Channels by Gβγ Subunits. J Neurosci. 2019 Oct 2;39(40):7840-7852. |