FSL0784

Structure

• InChI=1S/C15H16O6/c1-5(2)7-8-11(16)19-9(7)10-13(3)14(8,18)4-6-15(13,21-6)12(17)20-10/h6-10,18H,1,4H2,2-3H3/t6?,7-,8?,9?,10+,13+,14+,15-/m0/s1
• InChIKey=PIMZUZSSNYHVCU-LJGWEWMTSA-N

Synonyms

• 124-87-8
• Picrotoxin

Origin

Biological activities

A noncompetitive antagonist at GABA receptors

Therapeutic

CNS stimulant

Target

GABA-A receptors

Assay information

Inhibition of tiagabine-elicited depolarizations (100 μM) as the GABA_a receptor antagonist
A potent antagonist of GABA receptors (IC₅₀: 237 nM) at synapses in central nervous system
Inhibition of 35S-t-buthylbicyclophosphoro-thionate binding to the Cl-channel (IC₅₀: 1.7 μM)

References

• Hu RQ, Davies JA
  Tigabine hydrochloride, an inhibitor of gamma-aminobutyric acid (GABA) uptake, induces cortical depolarizations in vitro.
  Brain Res, 753(2): 260-268 (1997)  9125411
• Qian H, Dowling JE
  Pharmacology of novel GABA receptors found on rod horizontal cells of the white perch retina.
  J Neurosci, 14(7): 4299-4307 (1994)  8027780
• Anderson SM, De Souza RJ, Cross AJ
  The human neuroblastoma cell line, IMR-32 possesses a GABAA receptor lacking the benzodiazepine modulatory site.
  Neuropharmacology, 32(5): 455-460 (1993)  8391667
• Akaike N, Hattori K, Oomura Y, Carpenter DO
  Bicuculline and picrotoxin block gamma-aminobutyric acid-gated Cl- conductance by different mechanisms.
  Experientia, 41(1): 70-71 (1985)  2578409