21416-53-5

Picrotin is a natural picrotoxane that antagonizes glycine receptors (GlyRs; IC₅₀s = 57 and 117 μM for α₁ and α₂ homodimeric GlyRs, respectively). It also inhibits α₃ homodimeric GlyRs. Picrotin is inactive in inhibiting γ-aminobutyric acid (GABA) type A and type C receptors. Picrotin occurs in the natural plant-derived poison picrotoxin , equimolar with picrotoxinin.

GABAa receptor antagonist

ChEBI: Picrotin is an organic heteropentacyclic compound that is picrotoxinin in which the olefinic double bond has undergone addition of water to give the corresponding tertiary alcohol. It is the less toxic component of picrotoxin, lacking GABA activity. It has a role as a plant metabolite. It is an organic heteropentacyclic compound, an epoxide, a tertiary alcohol, a gamma-lactone, a diol and a picrotoxane sesquiterpenoid. It is functionally related to a picrotoxinin.

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