(+)-Bicuculline
- Structure
- InChI=1S/C20H17NO6/c1-21-5-4-10-6-14-15(25-8-24-14)7-12(10)17(21)18-11-2-3-13-19(26-9-23-13)16(11)20(22)27-18/h2-3,6-7,17-18H,4-5,8-9H2,1H3/t17-,18+/m0/s1
- InChIKey=IYGYMKDQCDOMRE-ZWKOTPCHSA-N
- Synonyms
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- Origin
- Adlumia fungosa
Capnoides sempervirens
Corydalis govaniana
Dicentra cucullaria
- Biological activities
- GABAA antagonist
- Therapeutic
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Antidepressant
Antiepileptic
- Target
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GABAa receptor channels
SK channels
- Assay information
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Antagonistic activity against [3H]GABA binding to hepatocytes (IC50 = 50 μM)
Blocking activity against SK (small-conductance calcium-activated potassium) channels: IC50 of 46.3 μM for SK1, and of 63.3 μM for SK2 at -60 mV
Inhibitor of [3H]muscimol binding on spinal cord (IC50 = 16 μM), brain (IC50 = 5 μM), and cultured neurons (IC50 = 5 μM)
- References
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Khawaled R, Bruening-Wright A, Adelman JP, Maylie J
Bicuculline block of small-conductance calcium-activated potassium channels.
Pflugers Arch, 438(3): 314-321 (1999) 10398861
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Minuk GY, Bear CE, Sarjeant EJ
Sodium-independent, bicuculline-sensitive [3H]GABA binding to isolated rat hepatocytes.
Am J Physiol, 252(5 Pt 1): G642-G647 (1987) 3578523
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Frere RC, Macdonald RL, Young AB
GABA binding and bicuculline in spinal cord and cortical membranes from adult rat and from mouse neurons in cell culture.
Brain Res, 244(1): 145-153 (1982) 6288176
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Can J Chem, 39: 1801-1804 (1961)
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Can J Res, 8: 142-146 (1933)
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Can J Res, 7: 265-269 (1932)