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Bicuculline is a neuromodulatory GABA-A receptor antagonist used to study regional variation of GABA receptors and the role of GABA-A receptors in motor disorders, pain, seizure, nociception, anxiety, and memory. Through its inhibition of GABA-A receptors, bicuculline potentiates activation at NMDA receptors and produces membrane depolarization, inhibiting K+ conductance and prolonging Ca2+-dependent action potentials in neurons. Specific rotation +130 (20 D, chloroform c=2)
| Cas No. | 485-49-4 |
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| Purity | ≥98% |
| Formula | C20H17NO6 |
| Formula Wt. | 367.35 |
| IUPAC Name | (6R)-6-[(5S)-6-methyl-7,8-dihydro-5H-[1,3]dioxolo[4, 5-g]isoquinolin-5-yl]-6H-furo[3,4-g][1,3]benzodioxol-8-one |
| Appearance | White to off white powder |
| Store Temp | Ambient |
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| Ship Temp | Ambient |
| MSDS | |
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| Info Sheet |
Dela Peña IJ, Lee HL, Yoon SY, et al. The ethanol extract of Cirsium japonicum increased chloride ion influx through stimulating GABA(A) receptor in human neuroblastoma cells and exhibited anxiolytic-like effects in mice. Drug Discov Ther. 2013 Feb;7(1):18-23. PMID: 23524939.
Torkaman-Boutorabi A, Soltani S, Oryan S, et al. Involvement of the dorsal hippocampal GABA-A receptors in histamine-induced facilitation of memory in the Morris water maze. Pharmacol Biochem Behav. 2013 Apr;105:142-50. PMID: 23438692.
Ionov ID, Roslavtseva LA. Coadministration of bicuculline and NMDA induces paraplegia in the rat. Brain Res. 2012 Apr 27;1451:27-33. PMID: 22445063
Ji G, Neugebauer V. Pain-related deactivation of medial prefrontal cortical neurons involves mGluR1 and GABA(A) receptors. J Neurophysiol. 2011 Nov;106(5):2642-52. PMID: 21880942.
Costa LG, Doctor SV, Murphy SD. Antinociceptive and hypothermic effects of trimethyltin. Life Sci. 1982 Sep 13;31(11):1093-102. PMID: 6890611.
Heyer EJ, Nowak LM, Macdonald RL. Membrane depolarization and prolongation of calcium-dependent action potentials of mouse neurons in cell culture by two convulsants: bicuculline and penicillin. Brain Res. 1982 Jan 28;232(1):41-56. PMID: 7055710.