Picrotin (CAS 21416-53-5)

Picrotin, a natural picrotoxane, exhibits antagonistic activity against glycine receptors (GlyRs). It specifically targets α1 and α2 homodimeric GlyRs, with IC50 values of 57 µM and 117 µM, respectively. Additionally, it inhibits α3 homodimeric GlyRs. Notably, Picrotin does not display inhibitory effects on γ-aminobutyric acid (GABA) type A and type C receptors. This compound naturally occurs in picrotoxin, a plant-derived poison, where it exists in equimolar quantities with picrotoxinin. As an analytical standard, Picrotin is provided with high chromatographic purity, serving as a reference material for qualitative determination. Structurally, it is an organic heteropentacyclic compound formed from picrotoxinin through the addition of water to the olefinic double bond, resulting in a tertiary alcohol. Picrotin represents the less toxic component of picrotoxin, devoid of GABA activity. Functionally, it acts as a plant metabolite and belongs to the group of organic heteropentacyclic compounds, possessing characteristics such as being an epoxide, tertiary alcohol, gamma-lactone, diol, and picrotoxane sesquiterpenoid. Its origin can be traced back to picrotoxinin. Picrotin′s selective antagonism of glycine receptors, coupled with its distinct chemical properties, highlights its importance as a compound of interest in various research fields, particularly in understanding receptor interactions and conducting qualitative determinations.