Picrotin is a natural picrotoxane that antagonizes glycine receptors (GlyRs; IC50s = 57 and 117 ?M for α1 and α2 homodimeric GlyRs, respectively).1,2 It also inhibits α3 homodimeric GlyRs.3 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.
1.Lynch, J.W., Rajendra, S., Barry, P.H., et al.Mutations affecting the glycine receptor agonist transduction mechanism convert the competitive antagonist, picrotoxin, into an allosteric potentiatorJ. Biol. Chem.270(23)13799-13806(1995) 2.Yang, Z., Cromer, B.A., Harvey, R.J., et al.A proposed structural basis for picrotoxinin and picrotin binding in the glycine receptor poreJ. Neurochem.103(2)580-589(2007)