Coronaridine 

Coronaridine, an iboga type alkaloid, inhibits the wnt signaling pathway by decreasing β-catenin expression^[1].

Coronaridine (0-40 μM; 24 hours) is against non-cancer cells with IC₅₀ values >40 μM. It agaisnt wnt-dependent cells with IC₅₀ values of 10.4, 11.6 and 24.4 μM for SW480, HCT116 and DLD1cells, respectively^[1].
Coronaridine (0-40 μM; 24 hours) inhibits β-catenin expression, but the protein levels of p-β--catenin at Ser33, Ser37, and Thr41 and p-β-catenin at Ser 45 [p-b-catenin (S45)] are unchanged^[1].
In whole-cell patch clamp recordings,Catharanthine (1-300 μM) are respectively co-applied with GABA at concentrations corresponding to the EC₃₀ value for each receptor subtype. Both congeners potentiated different GABAARs in a concentration-dependent manner^[2].
At higher concentrations, however, Catharanthine starts to inhibit GABA-activated currents due to the reduced amplitude and rebound current, where the threshold concentration depended on the receptor subtype (e.g., > 30 μM for hα1β2; > 100 μM for hα1β2γ2 and hα2β2γ2). The PAM activity of Catharanthine's are depended on the receptor subtype: hα1β2 (4.6±0.8 μM), >hα2β2γ2 (12.6±3.8 μM), hα1β2γ2 (14.4 ± 4.6 μM)^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

338.44

C₂₁H₂₆N₂O₂

467-77-6

Solid

White to off-white

COC([C@]12[C@@]3([H])[N@@](CCC4=C2NC5=CC=CC=C45)C[C@@](C[C@@H]3CC)([H])C1)=O

Room temperature in continental US; may vary elsewhere.

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

• [1]. Kensuke Ohishi, et al. Coronaridine, an iboga type alkaloid from Tabernaemontana divaricata, inhibits the Wnt signaling pathway by decreasing β-catenin mRNA expression. Bioorg Med Chem Lett. 2015 Sep 15;25(18):3937-40.  [Content Brief]

  [2]. Hugo R Arias, et al. Coronaridine congeners potentiate GABA A receptors and induce sedative activity in mice in a benzodiazepine-insensitive manner. Prog Neuropsychopharmacol Biol Psychiatry. 2020 Jul 13;101:109930  [Content Brief]