FSL0586

Structure

• InChI=1S/C20H24O9/c1-7-12(22)26-10-6-17-9-5-8(16(2,3)4)18(17)11(21)13(23)28-15(18)29-20(17,14(24)27-9)19(7,10)25/h7-11,15,21,25H,5-6H2,1-4H3
• InChIKey=FPUXKXIZEIDQKW-UHFFFAOYSA-N

Synonyms

• 15291-75-5
• Ginkgolide A from Ginkgo leaves

Origin

Ginkgo biloba

Biological activities

Antagonist of Glycin and GABA_a receptors
PAF membrane platelet receptor

Therapeutic

Antiinflammatory

Target

Glycin and GABA_a receptors

Assay information

Antagonist activity against GABA receptors (α1β2γ2LGABA receptor: IC₅₀ = 2.6 μM at 10 μM GABA, 13.0 μM at 40 μM GABA)
Antagonist activity against Glycine receptors (α1: IC₅₀ = 5.9 μM, α2: IC₅₀ = 11.9 μM, α1β: IC₅₀ = 9.6 μM, α2β: IC₅₀ = 1.2 μM)
Antagonist activity against platelet-activating factor (PAF) membrane platelet receptor (IC₅₀ = 0.74 μM)

References

• Hawthorne R, Cromer BA, Ng HL, Parker MW, Lynch JW
  Molecular determinants of ginkgolide binding in the glycine receptor pore.
  J Neurochem, 98(2): 395-407 (2006)  16805834  doi: 10.1111/j.1471-4159.2006.03875.x
• Huang SH, Duke RK, Chebib M, Sasaki K, Wada K, Johnston GA
  Ginkgolides, diterpene trilactones of Ginkgo biloba, as antagonists at recombinant alpha1beta2gamma2L GABAA receptors.
  Eur J Pharmacol, 494(2-3): 131-138 (2004)  15212966  doi: 10.1016/j.ejphar.2004.04.051
• Lihong Hu, Zhongliang Chen, Xiaofang Cheng, Y. Xie
  Chemistry of ginkgolides: structure-activity relationship as PAF antagonists
  Pure Appl Chem., 71(6): 1153-1156 (1999)
• Nakanishi K
  The ginkgolides.
  Pure Appl Chem, 14(1): 89-113 (1967)  6036635